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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 4335. Отображено 100.
05-01-2012 дата публикации

Organic semiconductor material and organic thin-film transistor

Номер: US20120001162A1
Автор: Katsuhiro Mizoguchi, Keiichi Kaneto, Shuichi Nagamatsu, Shuzi Hayase, Tatsuo Okauchi, Tetsuji Moriguchi, Wataru Takashima
Принадлежит: Kyushu Institute of Technology NUC

An organic thin-film transistor comprising a gate electrode, a gate insulator layer, an organic semiconductor layer, a source electrode and a drain electrode wherein the organic semiconductor layer consists of the organic semiconductor material having the structure represented by the general formula (1) shown below, and the organic semiconductor layer has crystallinity: wherein L represents a bivalent linker group having the structure consisting of one group or any combination of two or more groups selected from unsubstituted or fluorinated benzene residue, unsubstituted or fluorinated thiophene residue, unsubstituted or fluorinated thienothophene residue; R 1 represents carbonyl group, cyano group or C 1 -C 6 fluorinated alkyl group; R 2 represents halogen atom, cyano group, carbonyl group or acetyl group.

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Номер записи: 1
21-06-2012 дата публикации

Leaving substituent-containing compound, organic semiconductor material, organic semiconductor film containing the material, organic electronic device containing the film, method for producing film-like product, pi-electron conjugated compound and method for producing the pi-electron conjugated compound

Номер: US20120153271A1
Автор: Daisuke Goto, Keiichiro Yutani, Masataka Mohri, Masato Shinoda, Satoshi Yamamoto, Shinji Matsumoto, Takashi Okada, Takuji Kato, Toshiya Sagisaka
Принадлежит: Ricoh Co Ltd

A leaving substituent-containing compound including a partial structure represented by the following General Formula (I): where a pair of X 1 and X 2 or a pair of Y 1 and Y 2 each represent a hydrogen atom; the other pair each represent a group selected from the group consisting of a halogen atom and a substituted or unsubstituted acyloxy group having one or more carbon atoms; a pair of the acyloxy groups represented by the pair of X 1 and X 2 or the pair of Y 1 and Y 2 may be identical or different, or may be bonded together to form a ring; R 1 to R 4 each represent a hydrogen atom or a substituent; and Q 1 and Q 2 each represent a hydrogen atom, a halogen atom or a monovalent organic group, and may be bonded together to form a ring.

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Номер записи: 2
19-07-2012 дата публикации

Organic Semiconductors

Номер: US20120184089A1
Автор: Sheena Zuberi, Tania Zuberi
Принадлежит: Cambridge Display Technology Ltd

A semiconducting compound comprising the structure: where R1 to R4 independently comprise, but are not limited to, optionally substituted straight, branched or cyclic alkyl chains having 2 to 20 (e.g. 2 to 12) carbon atoms, alkoxy, amino, amido, silyl, alkyl, alkenyl, aryl or hetero aryl; where X1 and X2 independently comprise S, O, NR5 or SiR6R7 where R8 to R7 independently comprise C1 to C5 branched, straight or cyclic alkyl chains; and where Ar1 comprises a heterocyclic ring, and where n is an integer between 1 and 4.

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Номер записи: 3
16-08-2012 дата публикации

Novel heterocyclic aromatic compound and polymer

Номер: US20120208978A1
Автор: Koji Morimoto, Setsuko Ishioka, Tetsuya Hosomi, Toshifumi Dohi, Yasuyuki Kita, Yoshiyuki Morita
Принадлежит: Nagase Chemtex Corp

An electrically conductive polymer obtained by oxidative polymerization of a heterocycle-containing aromatic compound as a monomer, wherein the heterocycle-containing aromatic compound is represented by the formula: A-B. In the above formula, A represents a substituted or unsubstituted thiophene ring group, or a substituted or unsubstituted pyrrole ring group; B represents a substituted or unsubstituted hydrocarbon aromatic ring group, a substituted or unsubstituted thiophene ring group, or a substituted or unsubstituted pyrrole ring group; the ring represented by A and the ring represented by B are directly linked; however, A and B represent structures that are different from each other. The compound can be produced by a coupling reaction using a hypervalent iodine reactant.

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Номер записи: 4
07-03-2013 дата публикации

Maleimide-based compound, and tautomer or stereoisomer thereof, dye for photoelectric conversion, and semiconductor electrode, photoelectric conversion element and photoelectrochemical cell using the same

Номер: US20130056690A1
Автор: Katsumi Maeda, Kentaro Nakahara, Shin Nakamura
Принадлежит: NEC Corp

It is an object to provide a maleimide-based compound having excellent photoelectric conversion characteristics, and a tautomer or a stereoisomer thereof, a dye for photoelectric conversion, a semiconductor electrode, a photoelectric conversion element, and a photoelectrochemical cell. In order to accomplish the above-described objects, a dye for photoelectric conversion including at least one compound represented by the following general formula (1) is provided. (In the formula (1), R 1 represents a direct bond, or a substituted or unsubstituted alkylene group. X represents an acidic group. D represents an organic group containing an electron-donating substituent. Z represents a linking group that has at least one hydrocarbon group selected from aromatic rings or heterocyclic rings).

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Номер записи: 5
14-03-2013 дата публикации

Compounds Having Semiconducting Properties and Related Compositions and Devices

Номер: US20130062598A1
Автор: Antonio Facchetti, Damien Boudinet, Hakan Usta, Jordan Quinn
Принадлежит: Individual

Disclosed are new compounds having semiconducting properties. Such compounds can be processed in solution-phase at a temperature of less than about 50° C. into thin film semiconductors that exhibit high carrier mobility and/or good current modulation characteristics.

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Номер записи: 6
21-03-2013 дата публикации

COMPOUND COMPRISING A FIVE-MEMBERED HETERO RING, AN ORGANIC ELECTRICAL ELEMENT USING THE SAME AND A TERMINAL THEREOF

Номер: US20130069049A1
Автор: Ji Heesun, Kim Daesung, Lee Bumsung, LEE Sunhee, Mun Soungyun, PARK Junghwan
Принадлежит: DUKSAN HIGH METAL CO., LTD.

Disclosed are a compound comprising a five-membered hetero ring, an organic electrical element using the same and a terminal thereof. 2. The compound as claimed in claim 1 , wherein Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , and Rand Reach form a substituted or unsubstituted claim 1 , saturated or unsaturated ring together with an adjacent group.5. An organic electrical element comprising one or more organic material layers comprising the compound as claimed in .6. The organic electrical element as claimed in claim 5 , wherein the organic material layers are formed to comprise the compound by a soluble process.7. The organic electrical element as claimed in claim 5 , wherein the organic electrical element comprises an organic light emitting diode (OLED) having a structure in which a first electrode claim 5 , the one or more organic material layers claim 5 , and a second electrode are sequentially laminated.8. The organic electrical element as claimed in claim 7 , wherein the organic material layers comprise any one of a hole injection layer claim 7 , a hole transport layer claim 7 , a light emitting layer claim 7 , an electron transport layer claim 7 , and an electron injection layer.9. The organic electrical element as claimed in claim 7 , wherein the organic material layers comprise a hole injection layer claim 7 , and the compound is used as a hole transport material in the hole transport layer.10. A terminal comprising a display device claim 7 , which comprises the organic electrical element as claimed in claim 7 , and a control unit for driving the display device.11. The terminal as claimed in claim 10 , wherein the organic electrical element comprises any one of an organic light emitting diode (OLED) claim 10 , an organic solar cell claim 10 , an organic photo conductor (OPC) drum claim 10 , and an organic transistor (organic TFT). The present invention relates to a compound including a five-membered hetero ring, an organic electrical element using the ...

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Номер записи: 7
21-03-2013 дата публикации

COMPOUNDS FOR TREATING PROTEIN FOLDING DISORDERS

Номер: US20130072473A1
Автор: Cullen Matthew, Powell Noel A., Tait Bradley
Принадлежит:

The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis. 112-. (canceled)1427-. (canceled)28. The method of claim 13 , wherein Dis N(R) and wherein each Ris independently selected from the group consisting of hydrogen and optionally substituted C-Calkyl.2932-. (canceled)33. The method of claim 28 , wherein Gis an optionally substituted 5/6-membered fused heteroaryl.34. The method of claim 33 , wherein Gis benzothiazolyl claim 33 , benzoxazolyl claim 33 , benzimidazolyl claim 33 , benzothiophenyl claim 33 , and benzofuranyl claim 33 , each optionally substituted.3646-. (canceled)47. The method of claim 35 , wherein Gis an optionally substituted 5/6-membered fused heteroaryl.48. The method of claim 47 , wherein Gis benzothiazolyl claim 47 , benzoxazolyl claim 47 , benzimidazolyl claim 47 , benzothiophenyl claim 47 , and benzofuranyl claim 47 , each optionally substituted.5065-. (canceled)70. The method of claim 13 , wherein the condition is associated with a dysfunction in the proteostasis of a protein selected from the group consisting of hexosamine A claim 13 , cystic fibrosis transmembrane conductance regulator claim 13 , aspartylglucsaminidase claim 13 , a-galactosidase A claim 13 , cysteine transporter claim 13 , acid ceremidase claim 13 , acid α-L-fucosidase claim 13 , protective protein claim 13 , cathepsin A claim 13 , acid β-glucosidase claim 13 , acid β-galactosidase claim 13 , iduronate 2-sulfatase claim 13 , α-L-iduronidase claim 13 , galactocerebrosidase claim 13 , acid α-mannosidase claim 13 , acid β-mannosidase claim 13 , arylsulfatase B claim 13 , arylsulfatase A claim 13 , N-acetylgalactosamine-6-sulfate sulfatase claim 13 , acid β-galactosidase claim 13 , N-acetylglucosamine-1-phosphotransferase claim 13 , acid sphingmyelinase ...

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Номер записи: 8
21-03-2013 дата публикации

THIENOPYRIDINE ESTER DERIVATIVE CONTAINING CYANO GROUP, PREPARATION METHOD, USE AND COMPOSITION THEREOF

Номер: US20130072521A1
Автор: CHEN Furong, HUANG Changjiang, LIU Bingni, LIU Dengke, Liu Mo, Liu Peng, Liu Ying, TAN Chubing, TANG Lida, YUE Nan, ZHAO Yigui, ZHI Deguang, ZHOU Yunsong
Принадлежит: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH

A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation. 2. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is selected from one of the following compounds:I-1: 5-(2-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate;I-2: 5-(3-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate;I-3: 5-(4-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate.3. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the pharmaceutically acceptable salt comprises the salt formed by the compound of formula I with an inorganic acid or an organic acid.4. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 3 , wherein the pharmaceutically acceptable salt is selected from hydrochlorides claim 3 , hydrobromides claim 3 , hydriodates claim 3 , sulfates claim 3 , hydrosulfates claim 3 , phosphates claim 3 , hydrophosphates claim 3 , acetates claim 3 , propionates claim 3 , butyrates claim 3 , lactates claim 3 , mesylates claim 3 , tosilates claim 3 , maleates claim 3 , benzoates claim 3 , succinates claim 3 , tartrates claim 3 , citrates claim 3 , fumarates claim 3 , taurates claim 3 , gluconates claim 3 , and amino acid salts of the compound of formula I.5. A method for preparing the compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , ...

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Номер записи: 9
28-03-2013 дата публикации

Fused Thiazole Derivatives as Kinase Inhibitors

Номер: US20130079330A1
Автор: Alexander Rikki Peter, Aujla Pavandeep Singh, Crepy Karen Viviane Lucile, Foley Anne Marie, Franklin Richard Jeremy
Принадлежит: UCB PHARMA, S.A.

A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. 2. The compound as claimed in wherein Rrepresents Calkyl.3. The compound as claimed in wherein Rrepresents Calkyl.4. The compound as claimed in wherein T represents N—R.5. The compound as claimed in wherein V is carbon.6. The compound as claimed in wherein W is carbon.7. A compound as claimed in wherein Rrepresents hydrogen claim 1 , cyano claim 1 , carboxy claim 1 , Calkoxycarbonyl claim 1 , di(C)alkylaminocarbonyl claim 1 , [(C)alkyl][cyano(C)alkyl]aminocarbonyl claim 1 , [(C)alkoxy(C)alkyl][(C)alkyl]-aminocarbonyl or azetidinylcarbonyl.8. The compound as claimed in wherein Rrepresents hydrogen.9. The compound as claimed in wherein Rrepresents methyl.10. (canceled)11. The pharmaceutical composition comprising a compound of formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , in association with a pharmaceutically acceptable carrier.12. (canceled)13. (canceled)14. (canceled)15. A method for the treatment and/or prevention of a disorder for which the administration of a selective PI3K inhibitor is indicated which comprises administering to a patient in need of such treatment an effective amount of a compound of formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt or solvate thereof. The present invention relates to a class of fused thiazole derivatives, and to their use in therapy. More particularly, the invention provides a family of 6,7-dihydro-[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety. These compounds are selective ...

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Номер записи: 10
28-03-2013 дата публикации

THIENO (2, 3B) PYRAZINE COMPOUNDS AS B-RAF INHIBITORS

Номер: US20130079341A1
Автор: Corte Real Goncalves Azevedo Rita, Folmer Brigitte Johanna Bernita, Gernette Elisabeth Sophia, Ibrahim Hemen, Man de Adrianus Petrus Antonius
Принадлежит:

The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer. 2. The compound according to wherein X and Y are independently NHCO or CONH.3. The compound according to wherein X is NHCO.4. The compound according to wherein Y is CONH.5. The compound according to wherein the ar ring is (2-5C)heteroaryl substituted with one or more groups selected from (1-6C)alkyl claim 1 , phenyl claim 1 , (di)[(1-4C)alkyl]amino or pyrrolidinyl.7. The compound according to wherein R8 in the phenyl ring is (1-4C)alkyl claim 6 , optionally substituted with one or more CN claim 6 , aminocarbonyl claim 6 , halogen; (1-4C)alkoxy; (di)[(1-4C)alkyl]amino; or (2-5C)heteroaryl.8. The compound according to wherein R8 in the phenyl ring is (1-4C)alkyl claim 7 , optionally substituted with one or more CN or halogen.9. The compound according to wherein R7 claim 6 , R9 claim 6 , R10 and R11 are H.10. The compound according to wherein R1 is H; halogen; hydroxy; CN; amino; (1-2C)alkyl; (1-2C)alkylcarbonyl; (1-2C)alkoxy or (di)[(1-2C)alkyl]amino claim 1 , the alkyl group of which is optionally substituted with hydroxy; andR2 is H; halogen; hydroxy; CN; amino; (1-6C)alkyl; (di)[(1-6C)alkyl]amino, the alkyl group of which is optionally substituted with one or more hydroxy, (di)[(1-4C)alkylamino, (1-6C)alkoxy, (2-5C)heterocycloalkyl, (2-5C)heteroaryl or aryl; (1-4C)alkylcarbonyl; (1-4C)alkoxy, optionally substituted with (di)[(1-4C)alkyl]amino; (2-5C)heterocycloalkyl, optionally substituted with one or more groups selected from hydroxy, amino, (1-6C)alkyloxycarbonylamino) or (1-4C)alkyl, the alkyl optionally substituted with hydroxy; (2-5C)heteroaryl, optionally substituted with halogen, CN, (1-4C)alkoxy, (di)[(1-4C)alkyl]amino or (1-4C)alkyl; phenyl optionally substituted with halogen, CN, (1-4C)alkyl, (1-4C)alkoxy or (di)[(1-4C)alkyl]amino; 2-5C)heteroarylamino; phenylamino; or (2-5C) ...

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Номер записи: 11
28-03-2013 дата публикации

NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA

Номер: US20130079359A1
Автор: FRUTOS Rogelio Perez, KIM Soojin, MULDER Jason Alan, NICKOLAUS Peter, PATEL Nitinchandra D., POUZET Pascale A.J., SENANAYAKE Chris Hugh, TAMPONE Thomas Gabriel, WEI Xudong, WERTHMANN Ulrike, YANG Bing-Shiou
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, 2. The compound of formula I according to claim 1 , wherein R is in the para-position of Ring A claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or an enantiomer or racemate thereof.3. The compound of formula I according to claim 1 , wherein Ring A is selected from the group consisting of phenyl claim 1 , pyridinyl and pyrimidinyl claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or an enantiomer or racemate thereof.4. The compound of formula I according to claim 2 , wherein Ring A is selected from the group consisting of phenyl claim 2 , pyridinyl and pyrimidinyl claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , or an enantiomer or racemate thereof.7. The compound according to claim 1 , wherein S* is in the R-configuration.8. The compound according to claim 1 , wherein S* is in the S-configuration.9. A crystalline anhydrous compound of formula III according to claim 6 , which shows a reflex peak in the X-ray powder diffraction diagram with a d-value of 4.62 Å.10. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 6.82 Å claim 6 , and 10.09 Å.11. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 4.17 Å claim 6 , and 3.66 Å.12. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 6.82 Å claim 6 , 10.09 Å claim 6 , 3.93 Å claim 6 , and 4.94 Å.13. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 4.17 Å claim 6 , 3.66 Å claim 6 , 3.73 Å claim 6 , and 18.47 Å.14. A ...

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Номер записи: 12
28-03-2013 дата публикации

ORGANIC COMPOUNDS, PROCESS FOR PREPARING SAME AND USES IN ELECTRONICS

Номер: US20130079529A1
Автор: Lacroix Jean-Christophe, Trippé-Allard Gaëlle
Принадлежит:

The present disclosure relates to novel organic compounds, to the processes for preparing same and to the uses thereof, firstly in the electronics field, in particular in the fields referred to as plastic electronics and molecular electronics, and, secondly, in the coatings field, in particular in the fields of adhesion primers and intelligent coatings. The disclosure also relates to a material comprising a novel compound according to the invention. 2. The compound of formula (I) as claimed in claim 1 , in which:{'sub': '1', 'Rrepresents a hydrogen atom or thiophene;'}{'sub': 2', '2, 'Rrepresents the amino (—NH) group or the aniline group;'}Z represents thiophene;n=1, 2 or 3;m=0 or 1;{'sub': '1', 'wherein, when Rrepresents a hydrogen atom and m=0, then n is other than 1.'}3. The compound of formula (I) as claimed in claim 1 , in which:{'sub': '1', 'Rrepresents a hydrogen atom or thiophene;'}{'sub': 2', '2', '2, 'sup': '+', 'Rrepresents the aniline group, the phenyl group substituted by the diazo (N) group or the phenyl group substituted by the —NOgroup;'}Z represents thiophene;n=1, 2 or 3;m=0 or 1;{'sub': '1', 'wherein, when Rrepresents a hydrogen atom and m=0, then n is other than 1.'}4. The compound of formula (I) as claimed in claim 3 , wherein claim 3 , when m=0 claim 3 , n is other than 1.5. The compound of formula (I) as claimed in claim 1 , wherein:{'sub': '1', 'Rrepresents a hydrogen atom;'}{'sub': '2', 'Rrepresents the aniline group;'}n=2; andm=0.6. The compound of formula (I) as claimed in claim 1 , wherein:{'sub': '1', 'Rrepresents thiophene;'}{'sub': '2', 'Rrepresents the aniline group;'}n=1; andm=0.7. The compound of formula (I) as claimed in claim 1 , wherein:{'sub': '1', 'Rrepresents a hydrogen atom;'}{'sub': '2', 'Rrepresents the aniline group;'}Z represents thiophene;n=1; andm=1.8. The compound of formula (I) as claimed in claim 1 , wherein:{'sub': '1', 'Rrepresents a hydrogen atom;'}{'sub': '2', 'Rrepresents the aniline group;'}n=3; andm=0.9. The ...

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Номер записи: 13
04-04-2013 дата публикации

HETEROCYCLIC COMPOUNDS AND THEIR USES

Номер: US20130085151A1
Автор: Lucas Brian
Принадлежит: AMGEN INC

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. 2. A method of treating rheumatoid arthritis claim 1 , ankylosing spondylitis claim 1 , osteoarthritis claim 1 , psoriatic arthritis claim 1 , psoriasis claim 1 , inflammatory diseases and autoimmune diseases claim 1 , inflammatory bowel disorders claim 1 , inflammatory eye disorders claim 1 , inflammatory or unstable bladder disorders claim 1 , skin complaints with inflammatory components claim 1 , chronic inflammatory conditions claim 1 , autoimmune diseases claim 1 , systemic lupus erythematosis (SLE) claim 1 , myestenia gravis claim 1 , rheumatoid arthritis claim 1 , acute disseminated encephalomyelitis claim 1 , idiopathic thrombocytopenic purpura claim 1 , multiples sclerosis claim 1 , Sjoegren's syndrome and autoimmune hemolytic anemia claim 1 , allergic conditions and hypersensitivity claim 1 , ...

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Номер записи: 14
04-04-2013 дата публикации

CRYSTALLINE FORMS OF PRASUGREL SALTS

Номер: US20130085154A1
Автор: Biljan Tomislav, Tuksar Mihaela, Zegarac Miroslav
Принадлежит:

Salts of prasugrel were prepared including, for example, crystalline forms of prasugrel hydrobromide. These salts are useful, for example, in medicaments that inhibit the aggregation of platelets. 1. Crystalline Form 1 of Prasugrel hydrobromide.2. The crystalline Form I of Prasugrel hydrobromide according to claim 1 , characterized by data selected from: an X-ray powder diffraction pattern having peaks at 7.8 claim 1 , 14.4 claim 1 , 16.9 claim 1 , 22.0 and 25.1 degrees two theta±0.2 degrees two theta; an XRPD pattern substantially as depicted in ; a solid-state C MAR spectrum having peaks at 7.1 claim 1 , 11.2 claim 1 , 63.6 claim 1 , 123.7 and 203.4±0.2 ppm; a solid-state C NMR spectrum substantially as depicted in ; and combinations thereof.3. Crystalline Form IA of Prasugrel hydrobromide.4. The crystalline Form IA of Prasugrel hydrobromide according to claim 3 , characterized by data selected from: an X-ray powder diffraction pattern having peaks at 7.9 claim 3 , 8.1 claim 3 , 13.5 claim 3 , 14.6 and 25.2 degrees two theta±0.2 degrees two theta; an XRPD pattern substantially as depicted in ; and combinations thereof.6. The use of at least one crystalline form according to in the manufacture of a pharmaceutical composition.7. The use of a crystalline form according to in the manufacture of prasugrel hydrochloride.8. A crystalline form according to for use as a medicament.9. A crystalline form according to for use as a medicament for inhibiting aggregation of platelets.10. A pharmaceutical composition comprising at least one crystalline form according to claim 1 , and at least one pharmaceutically acceptable excipient.11. A method for inhibiting aggregation of platelets comprising administering a pharmaceutically effective amount of at least one crystalline form according to claim 1 , to a subject in need of such treatment.12. A process for preparing Prasugrel hydrochloride comprising preparing any one of the crystalline forms according to by the process of the ...

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Номер записи: 15
11-04-2013 дата публикации

Inhibitors of Protein Tyrosine Kinase Activity

Номер: US20130090327A1
Автор: Hata Seiji, Raeppel Franck, Raeppel Stéphane, Vaisburg Arkadii, Yuki Yohei
Принадлежит: METHYLGENE INC.

The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling. 5. A composition comprising a compound according to any of to and a pharmaceutically acceptable carrier.6. A method of treating an opthalmic disease , condition or disorder , the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to any of to or a composition thereof , wherein the ophthalmic disease , disorder or condition is selected from the group consisting of (a) a disease , disorder or condition caused by choroidal angiogenesis , (b) diabetic retinopathy and (c) retinal oedema.7. The method according to claim 6 , wherein the ophthalmic disease claim 6 , disorder or condition is age-related macular degeneration. 1. Field of the InventionThis invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling.2. Summary of the Related ArtTyrosine kinases may be classified as growth factor receptor (e.g. EGFR, PDGFR, FGFR and erbB2) or non-receptor (e.g. c-src and bcr-abl) kinases. The receptor type tyrosine kinases make up about 20 different subfamilies. The non-receptor type tyrosine kinases make up numerous subfamilies. ...

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Номер записи: 16
11-04-2013 дата публикации

PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY

Номер: US20130090335A1
Автор: Bao Rudi, Cai Xiong, Lai Chengjung, Qian Changgeng, Zhai Haixiao
Принадлежит:

The invention provides a compound of Formula I, 2. The compound of wherein R is RC(O)— claim 1 , wherein Ris substituted or unsubstituted C-C-alkyl; substituted or unsubstituted C-C-alkenyl claim 1 , preferably C-C-alkenyl claim 1 , and more preferably C-C-alkenyl; substituted or unsubstituted C-C-alkynyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl.3. The compound of wherein R is H or acetyl.5. A pharmaceutical composition comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.6. A pharmaceutical composition for oral administration comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.7. A pharmaceutical composition comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.8. A pharmaceutical composition for oral administration comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.9. A method of treating a PI3K related disease or disorder in a subject in need thereof claim 5 , the method comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of .10. The method of claim 9 , wherein said PI3K related disease or disorder is a cell proliferative disorder.11. The method of wherein the cell proliferative disorder is a cancer.12. The method of claim 11 , wherein the cancer is selected from the group consisting of papilloma claim 11 , blastoglioma claim 11 , Kaposi's sarcoma claim 11 , melanoma claim 11 , non-small cell lung cancer claim 11 , ovarian cancer claim 11 , prostate cancer claim 11 , squamous cell carcinoma claim 11 , astrocytoma claim 11 , head cancer claim 11 , neck cancer claim 11 , bladder cancer claim 11 , breast cancer claim 11 , lung cancer claim 11 , colorectal cancer claim 11 , thyroid cancer claim 11 , pancreatic cancer claim 11 , gastric cancer claim 11 , hepatocellular carcinoma claim 11 , leukemia claim 11 , lymphoma claim ...

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Номер записи: 17
11-04-2013 дата публикации

ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130090364A1
Автор: Bennani Youssef L., Chan Chun Kong Laval, Cottrell Kevin M., Das Sanjoy Kumar, Giroux Simon, Liu Bingcan, Maxwell John, Morris Mark A., Reddy Jagadeeswar T., Xu Jingwang, Yannopoulos Constantin
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I 6. The compound according to any one of to , wherein{'sub': 1', 'p, 'each A is independently cyclopropyl, cyclohexyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, piperadinyl, phenyl, naphthalenyl, thienyl, furanyl, pyrrolyl, pyrazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl, oxadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, indolyl, indazolyl, benzimidazolyl, benzoxazolyl, benzodioxolyl, benzothiazolyl, benzothiadiazolyl, dihydrobenzodioxine, thienofuranyl, thienothienyl, thienopyrrolyl, quinolinyl, quinoxalinyl, quinazolinyl, cinnolinyl, or triazolyl; and wherein each A is independently substituted with (R).'}712.-. (canceled)13. The compound according to claim 1 , wherein B and B′ are independently absent claim 1 , Calkyl or Calkynyl.1416.-. (canceled)1823.-. (canceled)24. The compound according to claim 1 , wherein Ris halogen claim 1 , Calkyl which is unsubstituted or substituted one or more times by R claim 1 , —C(═O)OR claim 1 , —C(O)NRR claim 1 , hydroxyl claim 1 , cyano claim 1 , or Calkoxy.25. The compound according to claim 24 , wherein Ris chloro claim 24 , fluoro claim 24 , bromo claim 24 , methyl claim 24 , ethyl claim 24 , propyl claim 24 , butyl claim 24 , —CHOH claim 24 , difluoromethyl claim 24 , trifluoromethyl claim 24 , —C(═O)OR claim 24 , hydroxyl claim 24 , cyano claim 24 , or methoxy.26. The compound according to claim 1 , wherein R′ is fluoro claim 1 , methyl claim 1 , trifluoromethyl claim 1 , iodo claim 1 , CHOH claim 1 , or NHC(O)CH.27. The compound according to claim 26 , wherein s is 0.28. The compound according to claim 1 , wherein each Ris independently fluoro or methyl.29. The compound according to claim 28 , wherein s is 0.30. The compound according to claim 1 , wherein Rand R′ are H or methyl.3233.-. (canceled)34. The compound according to claim 1 , wherein m and n are independently 1 or 2.35. (canceled)37. The compound according to claim 1 , wherein Rand R′ are each ...

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Номер записи: 18
18-04-2013 дата публикации

POLYMERS WITH TUNABLE BAND GAPS FOR PHOTONIC AND ELECTRONIC APPLICATIONS

Номер: US20130092912A1
Автор: You Wei
Принадлежит:

The present invention provides, among other things, a copolymer comprising at least one donor monomer and at least one acceptor monomer. The polymer may optionally further comprise at least one additional comonomer. The polymers are useful as a charge-transport, semiconducting, electrochemical conducting, photoconducting, or light emitting material. Microelectronic devices comprising such polymers (e.g., as a heterojunction therein) are also described. 2. The copolymer of having a number average molecular weight of from 500 to 1 claim 1 ,000 claim 1 ,000 grams per mole.3. The copolymer of claim 1 , further comprising at least one additional comonomer.11. The copolymer of claim 10 , wherein Rand Rare fluoro.12. The copolymer of claim 10 , wherein each R and Ris C1-C20 alkyl.13. The copolymer of claim 10 , wherein R claim 10 , R claim 10 , Rand Rare each H.14. The copolymer of claim 10 , having a number average molecular weight for said polymer of from 500 to 1 claim 10 ,000 claim 10 ,000 grams per mole.16. The polymer of having a number average molecular weight of from 500 to 1 claim 15 ,000 claim 15 ,000 grams per mole.17. The polymer of claim 15 , wherein said polymer is a homopolymer.18. The polymer of claim 15 , wherein said polymer is a copolymer with at least one additional monomer.20. (canceled)21. A microelectronic device comprising a polymer of .22. The device of claim 21 , wherein said device is an optoelectronic device.23. The device of claim 21 , wherein said polymer comprises a heterojunction in said device.24. The device of claim 21 , wherein said device is a photovoltaic cell claim 21 , field effect transistor claim 21 , light emitting diode claim 21 , photodectector claim 21 , photovoltaic detector claim 21 , imaging device claim 21 , lasing device claim 21 , storage element claim 21 , amplifier claim 21 , emitter claim 21 , or electrochromic display.25. The device of claim 21 , wherein said device comprises a first electrode claim 21 , a second ...

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Номер записи: 19
18-04-2013 дата публикации

Inhibitors of Protein Tyrosine Kinase Activity

Номер: US20130096088A1
Автор: Claridge Stephen William, Kishida Masashi, Raeppel Franck, Raeppel Stéphane, Vaisburg Arkadii, Yuki Yohei
Принадлежит: METHYLGENE INC.

The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling. 12. A composition comprising a compound according to and a pharmaceutically acceptable carrier.13. A method of treating an ophthalmic disease claim 1 , condition or disorder claim 1 , the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to or a composition thereof claim 1 , wherein the ophthalmic disease claim 1 , disorder or condition is selected from the group consisting of (a) a disease claim 1 , disorder or condition caused by choroidal angiogenesis claim 1 , (b) diabetic retinopathy and (c) retinal oedema.14. The method according to claim 13 , wherein the ophthalmic disease claim 13 , disorder or condition is age-related macular degeneration. This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling.Tyrosine kinases may be classified as growth factor receptor (e.g. EGFR, PDGFR, FGFR and erbB2) or non-receptor (e.g. c-src and bcr-abl) kinases. The receptor type tyrosine kinases make up about 20 different subfamilies. The non-receptor type tyrosine kinases make up numerous subfamilies. These tyrosine kinases ...

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Номер записи: 20
18-04-2013 дата публикации

Inhibitors of Protein Tyrosine Kinase Activity

Номер: US20130096136A1
Автор: Claridge Stephen William, Hata Seiji, Raeppel Stéphane, Vaisburg Arkadii, Yuki Yohei
Принадлежит: METHYLGENE INC.

The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling. 12. A composition comprising a compound according to and a pharmaceutically acceptable carrier.13. A method of treating an opthalmic disease claim 1 , condition or disorder claim 1 , the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to or a composition thereof claim 1 , wherein the ophthalmic disease claim 1 , disorder or condition is selected from the group consisting of (a) a disease claim 1 , disorder or condition caused by choroidal angiogenesis claim 1 , (b) diabetic retinopathy and (c) retinal oedema.14. The method according to claim 13 , wherein the ophthalmic disease claim 13 , disorder or condition is age-related macular degeneration. This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling.Tyrosine kinases may be classified as growth factor receptor (e.g. EGFR, PDGFR, FGFR and erbB2) or non-receptor (e.g. c-src and bcr-abl) kinases. The receptor type tyrosine kinases make up about 20 different subfamilies. The non-receptor type tyrosine kinases make up numerous subfamilies. These tyrosine kinases have diverse biological ...

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Номер записи: 21
16-05-2013 дата публикации

COMPLIMENTARY POLYMER ELECTROCHROMIC DEVICE

Номер: US20130120821A1
Автор: Chandrasekhar Prasanna
Принадлежит: ASHWIN-USHAS CORPORATION, INC.

A complimentary polymer or “dual-polymer” electrochromic device and methods of preparing the same are provided. 1. A complimentary electrochromic device comprising:(a) a first electrode comprising a cathodically coloring conducting polymeric material, the cathodically coloring conducting polymeric material comprising a substituted or unsubstituted 2,2-dibenzyl-3,4-propylenedioxythiophene monomer;(b) a second electrode comprising an anodically coloring conducting polymeric material;(c) an electrolyte disposed between and in electrochemical communication with the first electrode and the second electrode; andwherein the redox potential of the cathodically coloring conducting polymeric material is substantially matched to the redox potential of the anodically coloring conducting polymeric material such that when one said polymeric material is fully oxidized, the other said polymeric material is fully reduced.2. The electrochromic device of claim 1 , wherein at least one benzyl moiety of the substituted 2 claim 1 ,2-dibenzyl-3 claim 1 ,4-propylenedioxythiophene is para substituted with a substituent selected from the group consisting of halo claim 1 , sulfonyl claim 1 , nitro claim 1 , and alkyl.3. The electrochromic device of claim 1 , wherein at least one benzyl moiety of the substituted 2 claim 1 ,2-dibenzyl-3 claim 1 ,4-propylenedioxythiophene has a substituent selected from the group consisting of chloro and bromo.4. The electrochromic device of claim 1 , wherein at least one benzyl moiety of the substituted 2 claim 1 ,2-dibenzyl-3 claim 1 ,4-propylenedioxythiophene has a substituent selected from the group consisting of n-propyl claim 1 , iso-propyl claim 1 , n-butyl claim 1 , iso-butyl claim 1 , n-pentyl claim 1 , and n-hexyl.5. The electrochromic device of claim 1 , wherein at least one benzyl moiety of the substituted 2 claim 1 ,2-dibenzyl-3 claim 1 ,4-propylenedioxythiophene has an amino substituent.6. The electrochromic device of claim 1 , wherein the ...

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Номер записи: 22
16-05-2013 дата публикации

ACC INHIBITORS AND USES THEREOF

Номер: US20130123231A1
Автор: Bhat Sathesh, Greenwood Jeremy Robert, Harriman Geraldine C., Harwood James, Masse Craig E.
Принадлежит: Nimbus Apollo, Inc.

The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same. 2. The compound according to claim 1 , wherein X is —S—.3. The compound according to claim 2 , wherein Ris methyl or trifluoromethyl.4. The compound according to claim 3 , wherein Ris halogen claim 3 , —C(O)OR claim 3 , —C(O)N(R) claim 3 , or oxazolyl.5. The compound according to claim 3 , wherein Rand Rare taken together to form a 5-6 membered partially unsaturated carbocyclic ring.6. The compound according to claim 3 , wherein Ris tetrazolyl claim 3 , —C(O)OR claim 3 , —C(O)N(R) claim 3 , or —OR.10. A composition comprising a compound according to and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.11. A method of inhibiting ACC in a patient in need thereof claim 10 , comprising administering to said patient the composition according to .12. A method of inhibiting ACC in a biological sample claim 1 , comprising contacting the biological sample with the compound according to .13. A method for treating a metabolic disorder in a patient in need thereof claim 10 , comprising administering to said patient the composition according to .14. The method according to claim 13 , wherein the metabolic disorder is obesity.15. The method according to claim 13 , wherein the metabolic disorder is dyslipidemia or hyperlipidemia.16. The method according to claim 14 , wherein the obesity is a symptom of Prader-Willi syndrome claim 14 , Bardet-Biedl syndrome claim 14 , Cohen syndrome or MOMO syndrome.17. The method according to claim 14 , wherein the obesity is a side effect of the administration of another medication claim 14 , including but not limited to insulin claim 14 , sulfonylureas claim 14 , thiazolidinediones claim 14 , antipsychotics claim 14 , antidepressants claim 14 , steroids claim 14 , anticonvulsants (including phenyloin and valproate) claim 14 , pizotifen claim 14 , or hormonal ...

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Номер записи: 23
23-05-2013 дата публикации

NOVEL PSYCHOTROPIC AGENTS HAVING GLUTAMATE NMDA ACTIVITY

Номер: US20130131048A1
Автор: Gil-ad Irit, PORTNOY Moshe, WEIZMAN Avraham
Принадлежит: Ramot at Tel-Aviv University Ltd.

The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders. 1. A compound , or a salt or stereoisomer thereof , of the general formula L-M-V , whereinL is a central nervous system (CNS) active moiety selected from the group consisting of clozapine and quetiapine;{'sub': 1', '8', '3', '8', '2', '2', '2', 'n', '2', 'n', '2', 'n', '2', '2', 'n', '1', '4', '2', '4', '2', '4, 'M is optionally present and is a linker selected from the group consisting of —NH—, —O—, —S—, C-C-alkylene, C-C-cycloalkylene, —CH—O—CH, —(CH)—O—(CH)—, —(CH—O)—, and —(CHCH—O)—, said alkylene and cycloalkylene being optionally substituted by one or more groups selected from the group consisting of C-Calkyl, C-Calkenyl, and C-Calkynyl;'}V is a modulator of a glutamate N-methyl-D-aspartate (NMDA) receptor selected from the group consisting of an amino acid, an ester of the amino acid, an amide of the amino acid, and an alkylated amine of the amino acid; wherein said amino acid is selected from the group consisting of glycinyl, sarcosinyl, serinyl, and cysteinyl; andn, independently of each other, is an integer from 0 to 3.2. The compound claim 1 , or a salt or stereoisomer thereof claim 1 , according to claim 1 , wherein said linker is selected from the group consisting of —NH— claim 1 , —O— claim 1 , —S— claim 1 , —(CH)— wherein m is an integer between 1 and 8 claim 1 , —(CH—CH═CH—CH)— claim 1 , —(CH═CH—CH—CH)— claim 1 , —(CH—CH═CH—CH—CH—CH)— claim 1 , —(CH—C≡C—CH)— claim 1 , —(C≡C—CH—CH)— claim 1 , —(CH—NH—CH═CH—CH)— claim 1 , —(CH—NH—CH—CH—CH)— claim 1 , —(CH—O—CH—CH)— claim 1 , —(CH)—O—(CH)— claim 1 , —CH—O—CH claim 1 , —(CH—O)— claim 1 , and —(CHCH—O)— wherein n is an integer from 0 to 3 claim 1 , and substituted derivatives thereof.3. The compound claim 1 , or a salt or stereoisomer thereof claim 1 , according to claim 1 , wherein the bonds between M and L and between M and V are non-hydrolizable.5. A ...

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Номер записи: 24
06-06-2013 дата публикации

NOVEL COMPOUNDS AND THERAPEUTIC USE THEREOF FOR PROTEIN KINASE INHIBITION

Номер: US20130143887A1
Автор: WU Zhanggui
Принадлежит:

Novel compound having the following formula: 117-. (canceled)19. The method according to claim 18 , wherein the cancer to be treated is selected from the group consisting of lung cancer claim 18 , liver cancer claim 18 , leucocythaemia claim 18 , osteocarcinoma claim 18 , pancreas cancer claim 18 , skin cancer claim 18 , melanoma claim 18 , metrocarcinoma claim 18 , oophoroma claim 18 , rectal carcinoma claim 18 , gastric carcinoma claim 18 , colon cancer claim 18 , breast carcinoma claim 18 , salpinx carcinoma claim 18 , endometrial carcinoma claim 18 , cervix carcinoma claim 18 , vagina carcinoma claim 18 , carcinoma of vulva claim 18 , esophagus carcinoma claim 18 , small intestine carcinoma claim 18 , incretion carcinoma claim 18 , soft tissue sarcoma claim 18 , urethra carcinoma claim 18 , prostatic cancer claim 18 , lymphocytoma claim 18 , bladder cancer claim 18 , nephridium cancer claim 18 , tumors of vertebral column claim 18 , tumors in the neuroglia of the brain claim 18 , and pituitary adenoma. The present application is a divisional application of U.S. application Ser. No. 12/349,888 which claims priority to Chinese Patent application No. CN200810000936.9, filed on Jan. 8, 2008, the entire specification, drawings, and disclosure of which are incorporated herein by reference for all purposes.The invention is directed to compounds, pharmaceutical compositions comprising same, and method using the same to inhibit protein kinase. The invention is further directed to methods of synthesis of the compounds and compositions.A major threat to human health is cancer, and worldwide at least 5 million people die from cancer annually. Most cancers in humans are caused by environmental factors. Although certain methods of cancer treatment are available, such as surgery, radiotherapy, and chemotherapy, the rate of success is still quite limited. Among available methods of treatment, chemotherapy is one of the most effective.One category of cancer chemotherapy agents ...

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Номер записи: 25
13-06-2013 дата публикации

THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS

Номер: US20130150573A1
Автор: Archibald Sarah Catherine, Brookings Daniel Christopher, Davis Jeremy Martin, Hutchings Clive Martin, Johnson James Andrew, Langham Barry John, Neuss Judi Charlotte
Принадлежит: UCB PHARMA S.A.

Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability. 2. A process according to claim 1 , wherein Ris hydrogen claim 1 , optionally substituted Calkyl claim 1 , optionally substituted Ccycloalkyl(C)alkyl claim 1 , optionally substituted Cheterocycloalkyl or optionally substituted Cheterocycloalkyl-(C)alkyl.3. A process according to claim 1 , wherein Rand Rare taken together with the nitrogen atom to which they are attached to form a cyclic group selected from optionally substituted azetidin-1-yl claim 1 , optionally substituted pyrrolidin-1-yl claim 1 , optionally substituted piperidin-1-yl claim 1 , optionally substituted morpholin-4-yl claim 1 , optionally substituted piperazin-1-yl and optionally substituted homopiperazin-1-yl.4. A process according to claim 1 , wherein Ror the cyclic group formed by Rand Rand the nitrogen atom to which they are attached is optionally substituted with one or more of Calkyl claim 1 , Calkoxy(C)alkyl claim 1 , hydroxy claim 1 , hydroxy(C)alkyl claim 1 , amino claim 1 , amino(C)alkyl claim 1 , carboxymethyl claim 1 , Calkoxycarbonyl claim 1 , Calkoxycarbonyl-(C)alkyl claim 1 , di(C)alkylamino claim 1 , Calkoxycarbonylamino and Calkoxycarbonyl-amino(C)alkyl.5. A process according to wherein Ror the cyclic group formed by Rand Rand the nitrogen atom to which they are attached is ...

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Номер записи: 26
20-06-2013 дата публикации

TRICYCLIC NECROSTATIN COMPOUNDS

Номер: US20130158024A1
Автор: Cuny Gregory D., Degterev Alexei, Hitomi Junichi, Jagtap Prakash, Yuan Junying
Принадлежит:

The present invention features compounds, pharmaceutical compositions, and methods for treating trauma, ischemia, stroke, degenerative diseases associated with cellular necrosis, and other conditions. Screening assays for identifying compounds useful for treating these conditions are also described. 2. The Nec-3 compound of claim 1 , wherein said Nec-3 compound is a substantially pure (3R claim 1 ,3aR)-rel isomer claim 1 ,or a pharmaceutically acceptable salt thereof.3. The Nec-3 compound of claim 2 , wherein Ris —C(O)R claim 2 , and Ris substituted Calkyl claim 2 ,or a pharmaceutically acceptable salt thereof.4. The Nec-3 compound of claim 2 , wherein said Nec-3 compound is a substantially pure (3R claim 2 ,3aR)-enantiomer claim 2 ,or a pharmaceutically acceptable salt thereof.5. The Nec-3 compound of claim 2 , wherein said Nec-3 compound is a substantially pure (3S claim 2 ,3aS)-enantiomer claim 2 ,or a pharmaceutically acceptable salt thereof.6. The Nec-3 compound of claim 2 , wherein{'sub': '2', 'the bond indicated by (a) is a double bond; Z is CH; and'}{'sub': 1', '2', '4', '6', '7', '10', '11, 'each of R, R, R, R, R, R, and R, independently, represents hydrogen,'}or a pharmaceutically acceptable salt thereof.7. The Nec-3 compound of claim 6 , wherein{'sub': '8', 'Ris H,'}or a pharmaceutically acceptable salt thereof.8. The Nec-3 compound of claim 2 , wherein{'sub': 3', '5', '2', '9, 'Rrepresents methoxyl; Rrepresents C(O)CHOH; and Rrepresents alkoxy of one to six carbon atoms,'}a pharmaceutically acceptable salt thereof.10. The Nec-3 compound of claim 9 , wherein said Nec-3 compound is a substantially pure (3R claim 9 ,3aR)-enantiomer claim 9 ,or a pharmaceutically acceptable salt thereof.11. The Nec-3 compound of claim 9 , wherein said Nec-3 compound is a substantially pure (3S claim 9 ,3aS)-enantiomer claim 9 ,or a pharmaceutically acceptable salt thereof.12. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) the ...

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Номер записи: 27
27-06-2013 дата публикации

CONJUGATED POLYMERS

Номер: US20130161567A1
Автор: Blouin Nicolas, Carrasco-Orozco Miguel, Meyer Frank Egon, Mitchell William, Tierney Steven
Принадлежит: Merck Patent Gesellschaft Mit Beschrankter Haftung

The invention relates to novel polymers containing repeating units based on benzo[2,1,3]thiadiazole-5,6-dicarboxylic acid bis-ester, monomers and methods for their preparation, their use as semiconductors in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices, and to OE and OPV devices comprising these polymers. 2. Polymer according to claim 1 , wherein Rand Rin formula I are selected from straight-chain claim 1 , branched or cyclic alkyl with 1 to 35 C atoms claim 1 , in which one or more non-adjacent C atoms are optionally replaced by —O— claim 1 , —S— claim 1 , —C(O)— claim 1 , —C(O)—O— claim 1 , —O—C(O)— claim 1 , —O—C(O)—O— claim 1 , —CR═CR— or —C≡C— and in which one or more H atoms are optionally replaced by F claim 1 , Cl claim 1 , Br claim 1 , I or CN claim 1 , or denote aryl claim 1 , heteroaryl claim 1 , aryloxy claim 1 , heteroaryloxy claim 1 , arylcarbonyl claim 1 , heteroarylcarbonyl claim 1 , arylcarbonyloxy claim 1 , heteroarylcarbonyloxy claim 1 , aryloxycarbonyl or heteroaryloxycarbonyl having 4 to 30 ring atoms that is unsubstituted or substituted by one or more non-aromatic groups R claim 1 , wherein{'sup': 3', '0', '00', '0', '0', '0', '00', '0', '0, 'sub': 2', '3', '2', '2', '3', '5, 'Ris on each occurrence identically or differently F, Br, Cl, —CN, —NC, —NCO, —NCS, —OCN, —SCN, —C(O)NRR, —C(O)X, —C(O)R, —NH, —NRR, —SH, —SR, —SOH, —SOR, —OH, —NO, —CF, —SF, optionally substituted silyl, carbyl or hydrocarbyl with 1 to 40 C atoms that is optionally substituted and optionally comprises one or more hetero atoms, or P-Sp-,'}{'sup': 0', '00, 'sub': '1-40', 'Rand Rare independently of each other H or optionally substituted Ccarbyl or hydrocarbyl,'}P is a polymerisable or crosslinkable group,Sp is a spacer group or a single bond, and{'sup': '0', 'Xis halogen.'}4. Polymer according to claim 3 , which is selected of formula IIa{'br': None, 'sup': 4', '1', '2', '3', '5, 'sub': x', 'y', 'n, 'R—[(Ar—U—Ar)—(Ar)]—R\u2003\u2003IIa ...

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Номер записи: 28
27-06-2013 дата публикации

2-SUBSTITUTED-THIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS

Номер: US20130165471A1
Автор: Phadke Avinash, Wiles Jason Allan
Принадлежит: Achillion Pharmaceuticals Inc.

Disclosed herein are 2-substituted-thienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula 2. A compound or salt of wherein claim 1 ,{'sub': 2', 'a', 'a', '1', '6, 'Ris amino, halogen, or —COR, where Ris C-Calkyl.'}3. A compound or salt of claim 2 , wherein Ris acetyl.4. A compound or salt of claim 1 , wherein Ris hydrogen claim 1 , or a benzenesulfonyl group substituted with 0 or 1 or more substituents independently chosen from halogen claim 1 , hydroxyl claim 1 , amino claim 1 , C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkoxy claim 1 , C-Chaloalkyl claim 1 , and C-Chaloalkoxy.5. A compound or salt of claim 4 , wherein Ris hydrogen.6. A compound or salt of claim 4 , wherein Ris a benzenesulfonyl group substituted with 0 or 1 or 2 substituents independently chosen from halogen claim 4 , hydroxyl claim 4 , amino claim 4 , methyl claim 4 , methoxy claim 4 , trifluoromethyl claim 4 , and trifluoromethoxy.7. A compound or salt of claim 1 , wherein Ris C-Calkanoyl or (C-Calkylester)C-Calkyl.8. A compound or salt of wherein claim 1 ,{'sub': '7', 'Ris a nitrogen-linked 5- to 6-membered heterocycloalkyl group, having 0 or 1 additional ring heteroatoms selected from N, O, and S, which nitrogen-linked 5- to 6-membered heterocycloalkyl group is substituted with at least 1 substituent independently chosen from (a) or (b) and 0 or 1 or more substituents independently chosen from (c); wherein'}{'sub': 1', '2', '1', '3, '(a) is amino, aminoC-Calkyl, and aminoC-Calkenyl;'}{'sub': 1', '6', '0', '4', '1', '6', '0', '4', '0', '4', '1', '4', '1', '4, '(b) is (C-Calkylcarbamate)C-Calkyl, (C-Calkylcarboxamide)C-Calkyl, and (benzenesulfonylamino)C-Calkyl, where each of (a) and (b) is other than amino substituted with 0 to 2 substituents independently chosen from halogen, amino, C-Calkyl, and C-Calkoxy; and'}{'sub': 1', '4', '2', '4', '1', '4', '1', '2', '1', '2, '(c) is halogen, hydroxyl, amino, C- ...

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Номер записи: 29
27-06-2013 дата публикации

OPTICALLY ACTIVE 2-HYDROXY TETRAHYDROTHIENOPYRIDINE DERIVATIVES, PREPARATION METHOD AND USE IN MANUFACTURE OF MEDICAMENT THEREOF

Номер: US20130165476A1
Автор: Shan Jiaqi, Sun Hongbin, Yuan Fang, Zhang Boyu
Принадлежит: JIANGSU VCARE PHARMATECH CO., LTD.

Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases. 4. The optically active 2-hydroxytetrahydrothienopyridine derivative according to claim 1 , wherein said derivative comprises an acid addition salt formed by the compound of Formula I with an acid below: hydrochloric acid claim 1 , hydrobromic acid claim 1 , sulfuric acid claim 1 , citric acid claim 1 , tartaric acid claim 1 , phosphoric acid claim 1 , lactic acid claim 1 , acetic acid claim 1 , maleic acid claim 1 , fumaric acid claim 1 , malic acid claim 1 , mandelic acid claim 1 , methanesulfonic acid claim 1 , benzenesulfonic acid claim 1 , p-toluenesulfonic acid claim 1 , pamoic acid claim 1 , oxalic acid claim 1 , or succinic acid.5. The optically active 2-hydroxytetrahydrothienopyridine derivative according to claim 1 , wherein said derivative comprises:(S)-methyl 2-(2-acetoxy-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)-2-(2-chlorophenyl)-acetate I-2;(S)-methyl 2-(2-propanoyloxy-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)-2-(2-chlorophenyl)-acetate I-3;(S)-methyl 2-(2-butanoyloxy-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)-2-(2-chlorophenyl)-acetate I-4;(S)-methyl 2-(2-(2-acetoxybenzoyloxy)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)-2-(2-chlorophenyl)-acetate I-5;(S)-methyl 2-(2-pivaloyloxy-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)-2-(2-chlorophenyl)-acetate I-7;(S)-methyl 2 ...

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Номер записи: 30
27-06-2013 дата публикации

INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY

Номер: US20130165477A1
Автор: Claridge Stephen William, Gaudette Frederic, Isakovic Ljubomir, Mannion Michael, Raeppel Stéphane, Saavedra Oscar Mario, Vaisburg Arkadii, Zhan Lijie
Принадлежит: METHYLGENE INC.

This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. 3. The compound according to claim 1 , wherein each Ris independently selected from the group consisting of halo claim 1 , —C(O)O—(CH)NRR claim 1 , —(CH)NR(CH)S(O)(C-Calkyl) claim 1 , —(CH)NR(CH)[O(CH)](CH)R claim 1 , —(CH)NR(CH)R claim 1 , —(CH)P(═O)(C-Calkyl) claim 1 , —(CH)NRCH(CH)P(═O)(C-Calkyl) claim 1 , —NRC(X)NR-arylP(═O)(C-Calkyl)and —NRC(X)NR-heteroarylP(═O)(C-Calkyl).20. A composition comprising a compound according to and a pharmaceutically acceptable carrier. This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling.Tyrosine kinases may be classified as growth factor receptor (e.g. EGFR, PDGFR, FGFR and erbB2) or non-receptor (e.g. c-src and bcr-abl) kinases. The receptor type tyrosine kinases make up about 20 different subfamilies. The non-receptor type tyrosine kinases make up numerous subfamilies. These tyrosine kinases have diverse biological activity. Receptor tyrosine kinases are large enzymes that span the cell membrane ...

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Номер записи: 31
11-07-2013 дата публикации

TRICYCLIC COMPOUNDS AND PBK INHIBITORS CONTAINING THE SAME

Номер: US20130178459A1
Автор: AHMED Feryan, CUI Wenge, DECORNEZ Helene, GAUUAN Polivina Jolicia F., GURRAM Mahender, HISADA Shoji, Huntley Raymond, JENKINS David M., KARGBO Robert B., Matsuo Yo, Nakamura Yusuke, SAJJADI-HASHEMI Zohreh, Walker Joel R.
Принадлежит: Oncotherapy Science, Inc.

Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer. 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris hydrogen claim 2 , cyano claim 2 , C-Calkyl optionally substituted with hydroxyl or halogen claim 2 , C-Ccycloalkyl claim 2 , C-Calkenyl claim 2 , C-Calkynyl claim 2 , or halogen.4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris hydrogen claim 2 , hydroxyl claim 2 , halogen claim 2 , C-Calkoxy claim 2 , or C-Caryl optionally substituted with hydroxyl.5. The compound of or a pharmaceutically acceptable salt claim 2 , wherein Ris hydrogen claim 2 , hydroxyl claim 2 , halogen claim 2 , C-Calkoxy claim 2 , or dihydroxyphenyl.6. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris selected from the group consisting of: hydrogen; hydroxyl; C-Calkyl optionally substituted with hydroxyl claim 2 , halogen claim 2 , or hydroxyethylamino; halogen; C-Calkoxy optionally substituted with dimethylamino or morpholinyl; C-Calkylphenyl claim 2 , wherein the aliphatic carbons are optionally substituted with —NRR; cyano; nitro; amino; 3- to 8-membered heterocycloalkyl optionally substituted with amino; heteroaryl; —OSOCH; —OSOCF; —OCOR claim 2 , wherein Rrepresents C-Calkyl; —OCOORwherein Rrepresents C-Calkyl; —OCONRRwherein Rand Reach independently represent hydrogen or C-Calkyl claim 2 , or Rand Rtaken together form morpholinyl; and —CONH.7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein when Ris a 3- to 8-membered heterocycloalkyl claim 6 , the 3- to 8-membered heterocycloalkyl is selected from the group consisting of piperidyl claim 6 , pyrrolidinyl claim 6 , morpholinyl claim 6 , or piperazinyl and optionally substituted with amino; and when Ris heteroaryl claim 6 , the heteroaryl is pyridyl.8. The compound of ...

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Номер записи: 32
18-07-2013 дата публикации

Prodrugs of Secondary Amine Compounds

Номер: US20130184265A1
Автор: Almarsson Örn, ALVAREZ JUAN, Blumberg Laura Cook, Lowe John A., Zeidan Tarek A.
Принадлежит: ALKERMES PHARMA IRELAND LIMITED

The present invention relates to compounds of Formula I: 2. A compound according to claim 1 , wherein said parent drug is selected from atenolol claim 1 , atomoxetine claim 1 , clozapine claim 1 , desipramine claim 1 , desloratadine (clarinex) claim 1 , diclofenac claim 1 , doripenem claim 1 , duloxetine claim 1 , enalapril claim 1 , ertapenem claim 1 , fluoxetine claim 1 , metoprolol claim 1 , mecamylamine claim 1 , meropenem claim 1 , methylphenidate claim 1 , dtmp (dextrorotary methylphenidate) claim 1 , olanzapine claim 1 , paroxetine claim 1 , pramipexole claim 1 , rasagiline claim 1 , (r)-rasagiline claim 1 , salbutamol/albuterol claim 1 , tamsulosin claim 1 , varenicline (chantix) claim 1 , and vildagliptin.3. A compound according to claim 1 , wherein said parent drug is alprenolol claim 1 , acebutolol claim 1 , amidephrine claim 1 , amineptine claim 1 , amosulalol claim 1 , amoxapine claim 1 , amphetaminil claim 1 , atenolol claim 1 , atomoxetine claim 1 , balofloxacin claim 1 , bamethan claim 1 , befunolol claim 1 , benazepril claim 1 , benfluorex claim 1 , benzoctamine claim 1 , betahistine claim 1 , betaxolol claim 1 , bevantolol claim 1 , bifemelane claim 1 , bisoprolol claim 1 , brinzolamide claim 1 , bufeniode claim 1 , butethamine claim 1 , camylofine claim 1 , carazolol claim 1 , carticaine claim 1 , carvedilol claim 1 , cephaeline claim 1 , ciprofloxacin claim 1 , clozapine claim 1 , clobenzorex claim 1 , clorprenaline claim 1 , cyclopentamine claim 1 , delapril claim 1 , demexiptiline claim 1 , denopamine claim 1 , desipramine claim 1 , desloratadine (clarinex) claim 1 , diclofenac claim 1 , dimetofrine claim 1 , dioxadrol claim 1 , dobutamine claim 1 , dopexamine claim 1 , doripenem claim 1 , dorzolamide claim 1 , droprenilamine claim 1 , duloxetine claim 1 , eltoprazine claim 1 , enalapril claim 1 , enoxacin claim 1 , epinephrine claim 1 , ertapenem claim 1 , esaprazole claim 1 , esmolol claim 1 , etoxadrol claim 1 , fasudil claim 1 , fendiline ...

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Номер записи: 33
08-08-2013 дата публикации

1,2-DIHYDRO-4-HYDROXY-2-OXO-QUINOLINE-3-CARBOXANILIDES AS AHR ACTIVATORS

Номер: US20130203703A1
Автор: Pettersson Lars
Принадлежит: Immunahr AB

The present invention relates to compounds which are 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment. 2. A compound according to claim 1 , wherein{'sub': 3', '3', '2, 'A, B and C are independently chosen from the group comprising H, Me, OMe, CF, OCF, F, Cl, and Br, or A and B represents OCHO and C is H; and'}{'sub': 3', '3', '2, 'R5 and R6 are independently chosen from the group comprising H, Me, Et, OMe, SMe, S(O)Me, CF, OCF, F, Cl, and Br, or R5 and R6 represents OCHO.'}3. A compound according to claim 1 , wherein{'sub': 3', '3', '2, 'A, B and C are independently chosen from the group comprising Me, OMe, CF, OCF, F, and Cl, or A and B represents OCHO and C is H; and'}{'sub': 3', '2, 'R5 and R6 are independently chosen from the group comprising Me, Et, OMe, SMe, S(O)Me, CF, F, and Cl, or R5 and R6 represents OCHO.'}4. A compound according to claim 1 , wherein{'sub': 2', '3', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '2', '2, 'sup': +', '+, 'RN is chosen from the group comprising H, C(O)Me, C(O)Et, C(O)Pr, C(O)CH(Me), C(O)C(Me), C(O)Ph, C(O)CHPh, COMe, COEt, and optionally substituted 1-3 times by substituents chosen from the group comprising Me, Et, OMe, OEt, SMe, S(O)Me, S(O)Me, S(O)NMe, CF, OCF, F, Cl, OH, COH, COMe, COEt, C(O)NH, C(O)NMe, NH, NH, NMe, NMe, NHC(O)Me, NC(═NH)NH, OS(O)OH, S(O)OH, OP(O)(OH), and P(O)(OH); and,'}{'sub ...

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Номер записи: 34
15-08-2013 дата публикации

Tricyclic Proteasome Activity Enhancing Compounds

Номер: US20130210845A1
Автор: Finley Daniel J., Gahman Timothy C., King Randall W., Lee Byung-Hoon, Lee Min J.
Принадлежит: President and Fellows of Harvard College

Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies. 3. The compound of claim 2 , wherein Ris alkyl claim 2 , cycloalkyl claim 2 , heterocyclyl claim 2 , aryl claim 2 , heteroaryl claim 2 , cycloalkylalkyl claim 2 , heterocyclylalkyl claim 2 , aralkyl claim 2 , heteroaralkyl or alkylcarbonyl.4. The compound of claim 2 , wherein Ris alkyl.57-. (canceled)8. The compound of claim 2 , wherein Ris alkyl claim 2 , cycloalkyl claim 2 , heterocyclyl claim 2 , aryl claim 2 , heteroaryl claim 2 , cycloalkylalkyl claim 2 , heterocyclylalkyl claim 2 , aralkyl or heteroaralkyl.910-. (canceled)11. The compound of claim 2 , wherein Ris methyl claim 2 , ethyl claim 2 , cyclopropyl claim 2 , cyclobutyl claim 2 , cyclopentyl claim 2 , phenyl claim 2 , benzyl claim 2 , or methylcarbonyl.12. The compound of claim 1 , wherein W is N-heterocyclyl.13. The compound of claim 12 , wherein W is azetidin1-yl claim 12 , pyrrolidin-1-yl claim 12 , piperidin-1-yl claim 12 , morpholin-1-yl or N-methyl piperazin-1-yl.14. (canceled)1718-. (canceled)21. The compound of claim 1 , wherein Ris hydrogen claim 1 , halo claim 1 , lower alkyl claim 1 , lower haloalkyl claim 1 , cyano claim 1 , lower alkyloxy claim 1 , lower haloalkoxy or amino.22. (canceled)24. (canceled)26. The compound of claim 25 , wherein Ris cycloalkylalkyl claim 25 , heterocyclylalkyl claim 25 , aralkyl claim 25 , or heteroaralkyl.2729-. (canceled)30. The compound of claim 25 , wherein Ris benzyl substituted with 0 claim 25 , 1 claim 25 , 2 claim 25 , 3 claim 25 , 4 or 5 substituents independently selected from the group consisting of alkyl claim ...

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Номер записи: 35
22-08-2013 дата публикации

MEGLUMINE SALT OF 6-FLUORO-3-HYDROXY-2-PYRAZINE CARBOXAMIDE

Номер: US20130217708A1
Автор: Nakamatsu Namika, Nakashima Takayoshi, Takakura Keiko, Takeshima Sakiko
Принадлежит: Toyama Chemical Co., Ltd.

A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection. 1: A meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a hydrate thereof.2: The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 1 , in a crystal form.3: The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 1 , in an amorphous form.4: An injectable preparation comprising the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of .5: The injectable preparation of claim 4 , wherein the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof is in a crystal form.6: The injectable preparation of claim 4 , wherein the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof is in an amorphous form.7: The injectable preparation of claim 4 , further comprising an amino acid and a saccharide claim 4 , or an amino acid and a sugar alcohol.8: A lyophilized preparation comprising a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.9: The lyophilized preparation of claim 8 , wherein the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide is in a crystal form.10: The lyophilized preparation of claim 8 , wherein the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide is in an amorphous form.11: The lyophilized preparation of claim 8 , further comprising an amino acid and a saccharide claim 8 , or an amino acid and a sugar alcohol.12: A process for producing a lyophilized preparation comprising a crystal of a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide claim 8 , the process comprising:(1) cooling an aqueous solution comprising 6-fluoro-3-hydroxy-2-pyrazinecarboxamide and meglumine to produce a frozen product;(2) increasing the temperature of the frozen product;(3) cooling the frozen product again; and(4) carrying ...

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Номер записи: 36
05-09-2013 дата публикации

IRAK INHIBITORS AND USES THEREOF

Номер: US20130231328A1
Автор: Greenwood Jeremy Robert, Harriman Geraldine C., Kapeller-Libermann Rosana, Masse Craig E., Robinson Shaughnessy, Romero Donna L., Shelley Mee, Wessel Matthew David, Wester Ronald T.
Принадлежит: Nimbus Iris, Inc.

The present invention provides compounds, compositions thereof, and methods of using the same. 2. (canceled)7. (canceled)10. (canceled)12. The compound of any one of claim 11 , wherein Ris —OH or F claim 11 , or pharmaceutically acceptable salt thereof.14. (canceled)1618-. (canceled)21. The compound of wherein n is 1 claim 1 , and Ris —NRor Cy claim 1 , or pharmaceutically acceptable salt thereof.22. The compound of claim 1 , wherein n is 1 and Ris morpholino claim 1 , or pharmaceutically acceptable salt thereof.23. The compound of claim 1 , wherein n is 1 and Ris —N(CH) claim 1 , or pharmaceutically acceptable salt thereof.24. The compound of claim 1 , wherein n is 1 and Ring A is a 1 claim 1 ,4-trans-substituted cyclohexyl ring claim 1 , or a pharmaceutically acceptable salt thereof.25. The compound claim 1 , wherein Ris hydrogen claim 1 , or a pharmaceutically acceptable salt thereof.26. The compound of claim 1 , or a pharmaceutically acceptable salt thereof.27. The compound of wherein Lis —NH— claim 1 , or a pharmaceutically acceptable salt thereof.29. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.3032-. (canceled)33. A method of treating an IRAK-mediated disorder claim 1 , disease claim 1 , or condition in a patient comprising administering to said patient a compound according to claim 1 , or a pharmaceutical composition thereof.3439-. (canceled) The present invention relates to compounds and methods useful for inhibiting one or more interleukin-1 receptor-associated kinases (“IRAK”). The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.The search for new therapeutic agents has been greatly aided in recent years by a better understanding of the structure of enzymes and other biomolecules associated with diseases. One ...

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Номер записи: 37
05-09-2013 дата публикации

MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

Номер: US20130231364A1
Автор: Binch Hayley, Grootenhuis Peter D.J., Hadida Ruah Sara S., Zhou Jinglan
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. 3. The compound according to claim 2 , wherein Ais an optionally substituted 6 membered aromatic ring having 0-4 heteroatoms claim 2 , wherein said heteroatom is nitrogen.4. The compound according to claim 2 , wherein Ais an optionally substituted phenyl.5. The compound according to claim 2 , wherein Ais an optionally substituted 6 membered aromatic ring having 0-4 heteroatoms independently selected from nitrogen claim 2 , oxygen claim 2 , or sulfur.6. The compound according to claim 2 , wherein Ais an optionally substituted 5-membered aromatic ring having 0-3 heteroatoms independently selected from nitrogen claim 2 , oxygen claim 2 , or sulfur.7. The compound according to claim 2 , wherein Ais a 5-membered aromatic ring having 1-2 nitrogen atoms.9. The compound according to claim 1 , wherein Rand Ris hydrogen.10. The compound according to claim 9 , wherein Ris hydrogen.13. The compound according to claim 12 , wherein each of X claim 12 , X claim 12 , X claim 12 , X claim 12 , and Xin formula IIIA′ is CH14. The compounds according to claim 12 , wherein X claim 12 , X claim 12 , X claim 12 , X claim 12 , and Xtaken together in compound of formula IIIA′ is an optionally substituted ring selected from pyridyl claim 12 , pyrazinyl claim 12 , or pyrimidinyl.17. The compound according to claim 16 , wherein ring Ais an optionally substituted claim 16 , saturated claim 16 , unsaturated claim 16 , or aromatic 5-7 membered ring with 0-3 heteroatoms selected from O claim 16 , S claim 16 , or N.22. The compound according to claim 21 , wherein WRis hydrogen claim 21 , C1-C6 aliphatic claim 21 , C(O)C1-C6 aliphatic claim 21 , or C(O)OC1-C6 aliphatic.23 ...

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Номер записи: 38
12-09-2013 дата публикации

COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR-ANTAGONISTS

Номер: US20130237527A1
Автор: NICKOLAUS Peter
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. 1. A medicament , comprising a PDE4-inhibitors and an EP4 receptor antagonist.2. The medicament according to claim 1 , wherein the EP4-receptor antagonist is an EP4-specific antagonist.3. The medicament according to claim 1 , the EP4-receptor antagonist is:[N-{[4-(5,9-diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulphonyl}-2-(2-methoxyphenyl)acetamide] (2.1);5-butyl-2,4-dihydro-4-[[2′-[N-(3-methyl-2-thiophene-carbonyl)sulphamoyl]biphenyl-4-yl]methyl]-2-[(2-trifluoromethyl)phenyl]-1,2,4-triazol-3-one (2.2);(4-{(1S)-1-[({5-chloro-2-[(4-fluorophenyl)oxy]phenyl}carbonyl)amino]ethyl}benzoic acid (2.3);N-[({2-[4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}-amino)carbonyl]-4-methylbenzene sulphonamide (2.4);4-[[4-(5-methoxy-2-pyridinyl)phenoxy]methyl]-5-methyl-N-[(2-methylphenyl)sulphonyl]-2-furancarboxamide (2.5);methyl 11alpha, 15alpha-dihydroxy-16-(3-methoxymethylphenyl)-9-oxo-17,18,19,20-tetranor-5-thia-13(E) prostanoate (2.6);4-cyano-2-[[2-(4-fluoro-1-naphthalenyl)-1-oxopropyl]amino]-benzenebutanoic acid (2.7); orN-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl}-benzene sulphonamide (2.8).5. The medicament according to claim 4 , wherein:X is SO,{'sup': '1', 'Ris H;'}{'sup': 2', '2.1', '2.1', '2.2', '2.3', '2.1', '2.1', '2.1', '2.2', '2.3', '2.2', '2.3', '2.1', '2.1', '2.2', '2.3', '2.2', '2.3, 'sub': 1-6', '3', '2', '2', '2', '3-7', '2', '3', '2', '2', '1-2', '2, 'claim-text': [{'sup': '2.1', 'sub': 3-7', '1-2', '1-2', '1-2', '3-7', '1-2, 'wherein Ris H or a group selected from methyl, ethyl, propyl, isopropyl, monocyclic Ccycloalkyl, phenyl-C-alkylene, hetaryl-C-alkylene, het-C-alkylene, C- ...

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Номер записи: 39
19-09-2013 дата публикации

Progesterone-containing compositions and devices

Номер: US20130245570A1
Автор: Gregg A. Jackson
Принадлежит: Individual

Progesterone-containing compositions and devices that can maintain opening of a body passageway are described. One aspect of the invention provides a therapeutically effective (e.g., relaxative, anti-oxidative, anti-restenotic, anti-angiogenic, anti-neoplastic, anti-cancerous, anti-precancerous and/or anti-thrombotic) composition or formulation containing progesterone and optionally vitamin E and/or conjugated linoleic acid. Another aspect of the invention provides a drug eluting device, such as a drug eluting stent, with at least one coating layer comprising a progesterone composition that can minimize or eliminate inflammation, thrombosis, restenosis, neo-intimal hyperplasia, rupturing of vulnerable plaque, and/or other effects related to device implantation, treatment, or interaction. Other aspects of the invention provide for methods of using such compositions, formulations, and devices.

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Номер записи: 40
03-10-2013 дата публикации

NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF

Номер: US20130261106A1
Автор: Carry Jean-Christophe, CHATREAUX Fabienne, Deprets Stéphanie, DUCLOS Olivier, LEROY Vincent, Mallart Sergio, MELON-MANGUER Dominique, MENDEZ-PEREZ Maria, VERGNE Fabrice
Принадлежит: SANOFI

The present invention relates to compounds of formula (I): 2. A compound according to claim 1 , wherein:{'sub': 6', '2', 'α', 'β', 'α', 'β', '1', '6, 'Ris —CONHor a —C(R)(R)(OH) group wherein R and R are, independently of one another, a hydrogen atom or a (C-C)alkyl group;'}or a pharmaceutically acceptable salt thereof.3. A compound according to claim 1 , wherein:R is a phenyl, pyridinyl or pyrazolyl group substituted with R1, R′1, R2 and R3;or a pharmaceutically acceptable salt thereof.5. A compound according to claim 1 , wherein R1 is a hydrogen atom or is selected from the following groups: (C-C)alkyl claim 1 , (C-C)alkoxy claim 1 , (C-C)cycloalkyl and aryl;or a pharmaceutically acceptable salt thereof.6. A compound according to claim 1 , wherein R′1 is a hydrogen atom or an isopropyloxy group;or a pharmaceutically acceptable salt thereof.7. A compound according to claim 1 , wherein: a hydrogen or chlorine atom or a methyl, cyclopropyl or methoxy group;', {'sub': 2', '1', '6', '3', '7', '1', '6', '1', '6, 'claim-text': {'sub': 1', '6', '1', '6', '2, 'claim-text': wherein:', {'sub': r', '6, 'R4 and R5 each is, independently of one another, a hydrogen atom, a (CC)alkyl group or a heterocycloalkyl group;'}, 'or else R4 and R5 together form, with the nitrogen atom bearing them, a 4- to 7-membered ring; and, 'said (C-C)alkyl group being optionally substituted with a halogen atom or a (C-C)alkoxy, heterocycloalkyl, NHor OH group;'}, 'a pyrrolidinyl, piperidinyl, tetrahydropyridinyl, piperazinyl, tetrahydropyranyl, 1,4-diazepan-1-yl, diazabicycloheptanyl, (8aR)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl, 1,7-diazaspiro[4.4]non-7-yl, octahydroindolizinyl, dihydroimidazo-pyrazinyl, piperazinyl-CH, pyrazolyl, imidazolyl, triazolyl or pyridinyl group; these groups being optionally substituted with one or more substituents selected, independently in each instance, from: (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkoxy, heterocycloalkyl, carboxy(C-C)alkyl, NR4R5 and OR4;'}, a hydrogen ...

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Номер записи: 41
17-10-2013 дата публикации

PIPERAZINO-DIHYDROTHIENOPYRIMIDINE DERIVATIVES

Номер: US20130274264A1
Автор: Fiegen Dennis, Fox Thomas, GOEGGEL Rolf, HOENKE Christoph, Klinder Klaus, NICKOLAUS Peter, Pouzet Pascale
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

A method for treating diseases associated with the inhibition of phosphodiesterase 4 (PDE4) enzyme in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a dihydrothienopyrimidinesulphoxide of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof 7. The method according to claim 1 , wherein:{'sup': 2', '2.1', '2.1', '2.1', '2.1', '2.1', '2.1', '2.1', '2.2', '2.3', '2.1', '2.2', '2.3, 'sub': 3', '2', '2', '1-3', '2', '1-6', '3-10', '1-6', '1-6', '1-6', '3', '2', '2', '1-6, 'Ris a group selected from monocyclic, saturated three-, four-, five-, six- or seven-membered heterocyclic groups with 1, 2, or 3 heteroatoms in each case selected from N, O, and S, each optionally substituted by one or more groups selected from fluorine, OH, CF, CHF, CHF, and oxo or by one or more groups selected from OR, C-alkylene-OR, SR, SO—R, SO—R, COOR, COR, C-alkanol, C-cycloalkyl, phenyl, C-alkyl, phenyl-C-alkylene, hetaryl-C-alkylene, het, hetaryl, and NRR, each optionally substituted by one or more groups selected from OH, OR, oxo, F, Cl, CF, CHF, CHF, C-alkyl, phenyl, and NRR,'}and the pharmacologically acceptable salts thereof.8. The method according to claim 7 , wherein:{'sup': '2', 'sub': 3', '2', '2', '2', '3', '3', '2, 'Ris a group selected from a monocyclic, saturated six-membered heterocyclic group with at least one heteroatom selected in each case from N, O, and S, each optionally be substituted by one or more groups selected from F, CF, CHF, CHF, OH, oxo, NH, NHCH, N(CH), methyl, ethyl, propyl, isopropyl, cyclopropyl, methoxy, and ethoxy,'}and the pharmacologically acceptable salts thereof.9. The method according to claim 8 , wherein:{'sup': '2', 'sub': 3', '2', '2', '2', '3', '3', '2, 'Ris a group selected from piperidine or tetrahydropyran, each optionally substituted by one or more groups selected from F, OH, CF, CHF, CHF, NH, NHCH, N(CH), oxo, methyl, ...

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Номер записи: 42
17-10-2013 дата публикации

PREPARATION OF PRASUGREL HYDROCHLORIDE

Номер: US20130274284A1
Автор: Aalla Sampath, Anumula Raghupathi Reddy, Charagondla Kavitha, Gilla Goverdhan, Kurella Srinivas, Metil Dattatray Shamrao
Принадлежит:

The present application relates to process for the preparation of prasugrel, its pharmaceutically acceptable salts, and its intermediates. 114-. (canceled)15. A process comprising:a) reacting 5,6,7,7a-tetrahydro-thieno[3,2-c]pyridin-2(4H)-one or a salt thereof with 2-bromo-1-cyclopropyl-2-(2-fluorophenyl)ethanone in the presence of an inorganic base and in a solvent to produce 5-(2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl)-5,6,7,7a-tetrahydrothieno[3,2-c]pyridin-2(4H)-one;b) acetylating in situ the obtained 5-(2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl)-5,6,7,7a-tetrahydrothieno[3,2-c]pyridin-2(4H)-one in step a), into prasugrel by treating with an acetylating agent in the presence of an organic base; andc) optionally converting the prasugrel of step b), into prasugrel hydrochloride in the presence of a source of hydrogen chloride in an organic solvent.16. The process of claim 15 , wherein the solvent of step a) is an ether solvent claim 15 , a ketone solvent claim 15 , an ester solvent claim 15 , an alcohol solvent claim 15 , a nitrile solvent claim 15 , an amide solvent claim 15 , a sulfoxide solvent claim 15 , water claim 15 , or mixtures thereof.17. The process of claim 15 , wherein step b) is carried out without isolating the 5-(2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl)-5 claim 15 ,6 claim 15 ,7 claim 15 ,7a-tetrahydrothieno[3 claim 15 ,2- c]pyridin-2(4H)-one obtained in step a).18. The process of claim 15 , wherein the acetylating agent of step b) is acetic anhydride.19. Prasugrel or a pharmaceutically acceptable salt thereof claim 15 , prepared according to claim 15 , containing less than 0.1% 5-[(1RS)-2-cyclopropyl-1-(3-fluorophenyl)-2-oxoethyl]-4 claim 15 ,5 claim 15 ,6 claim 15 ,7-tetrahydrothieno[3 claim 15 ,2-c]pyridin-2-yl acetate.20. Prasugrel or a pharmaceutically acceptable salt thereof claim 15 , prepared according to claim 15 , having less than about 0.1% of the methyl impurity claim 15 , the propionyl impurity claim 15 , the desfluoro ...

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Номер записи: 43
17-10-2013 дата публикации

SODIUM SALT OF 6-FLUORO-3-HYDROXY-2-PYRAZINE CARBOXAMIDE

Номер: US20130274472A1
Автор: Nakamatsu Namika, Takakura Keiko, Takeshima Sakiko, Uehara Sayuri
Принадлежит: Toyama Chemical Co., Ltd.

A preparation replete with crystals of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection. 1. A crystal of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a hydrate thereof.2. An injectable preparation containing a crystal of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a hydrate thereof.3. A lyophilized preparation containing a crystal of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.4. A process for producing a lyophilized preparation containing a crystal of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide , comprising the steps:(1) cooling an aqueous solution containing a sodium salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide to produce a frozen product;(2) increasing the temperature of the frozen product;(3) cooling the frozen product again; and(4) carrying out lyophilization.5. The process according to claim 4 , wherein the achieving temperature of the frozen product falls within the range of −15 to −5° C. in the step of increasing the temperature of the frozen product. The present invention relates to a crystal of sodium salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide (hereinafter referred to as “Compound A”), an injectable preparation containing the same, and a process thereof.These days, worldwide pandemic has been caused by H1N1 influenza virus, and occurrence of pandemic by a further virulent virus in the future is a concern.At present, as therapeutic agents for influenza, e.g., Oseltamivir, Zanamivir, Peramivir, Laninamivir, and Amantadine are used. However, these therapeutic agents have, for example, the following drawbacks. Oseltamivir cannot be administered to patients having difficulty in oral administration. It is difficult to administer Zanamivir to children and aged persons. It takes a long time to administer Peramivir. Amantadine is ineffective against Type B influenza virus and resistant viruses have emerged. ...

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Номер записи: 44
24-10-2013 дата публикации

BICYCLIC ARYL AND BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS

Номер: US20130281468A1
Автор: Ding Pingyu, Goff Dane, Heckrodt Thilo J., Holland Sacha, Litvak Joane, Singh Rajinder, Yu Jiaxin, Zhang Jing
Принадлежит:

Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. 1. A compound which is N-(3-(bicyclo[2.2.1]heptan-2-yl)-1 ,2 ,3 ,4 ,5 ,6-hexahydrobenzo[d]azocin-8-yl)-1-(2-chloro-7-methylthieno[3 ,2-d]pyrimidin-4-yl)-1H-1 ,2 ,4-triazole-3 ,5-diamine , as an isolated stereoisomer or a mixture of stereoisomers , or a pharmaceutically acceptable salt thereof.2. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the compound of claim 1 , as an isolated stereoisomer or a mixture of stereoisomers claim 1 , or a pharmaceutically acceptable salt thereof.3. A method of inhibiting Axl activity in a mammal claim 1 , comprising administering to the mammal an effective amount of the compound of claim 1 , as an isolated stereoisomer or a mixture of stereoisomers claim 1 , or a pharmaceutically acceptable salt thereof.4. The method of wherein a disease or condition in the mammal is alleviated by the inhibition of Axl activity.5. The method of wherein the disease or condition is selected from the group consisting of rheumatoid arthritis claim 4 , vascular disease claim 4 , vascular injury claim 4 , psoriasis claim 4 , visual impairment due to macular degeneration claim 4 , diabetic retinopathy claim 4 , retinopathy of prematurity claim 4 , kidney disease claim 4 , osteoporosis claim 4 , osteoarthritis and cataracts.6. The method of claim 4 , wherein a manifestation of the disease or condition is solid tumor formation in the mammal.7. The method of claim 6 , wherein the disease or condition is selected from the group consisting of breast carcinoma claim 6 , renal carcinoma claim 6 , endometrial carcinoma claim 6 , ovarian carcinoma claim 6 , thyroid carcinoma claim 6 , non- ...

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Номер записи: 45
31-10-2013 дата публикации

THIENOPYRIMIDINEDIONE DERIVATIVES AS TRPA1 MODULATORS

Номер: US20130289054A1
Автор: KHAIRATKAR-JOSHI Neelima, Kumar Sukeerthi, Margal Sanjay, Mukhopadhyay Indranil, Thomas Abraham, Waghmare Nayan Taterao
Принадлежит:

The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. 150.-. (canceled)52. The method according to claim 51 , wherein L is CH.53. The method according to claim 51 , wherein Rand Rare (C-C)alkyl.54. The method according to claim 53 , wherein (C-C)alkyl is methyl.55. The method according to claim 51 , wherein Ris hydrogen.56. The method according to claim 51 , wherein U is thiazole claim 51 , imidazole claim 51 , isoxazole claim 51 , pyrazole claim 51 , thiadiazole or pyrimidine.57. The method according to claim 51 , wherein V is aryl.58. The method according to claim 57 , wherein aryl is phenyl.60. The method according to claim 59 , wherein Rand Rare methyl.61. The method according to claim 59 , wherein R claim 59 , R claim 59 , Rand Rare independently selected from the group consisting of hydrogen claim 59 , fluoro claim 59 , trifluoromethyl or trifluoromethoxy.62. The method according to claim 59 , wherein Rand Rare hydrogen.63. The method according to wherein compound is selected from:2-(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)-N-[4-(trifluoromethyl)-1,3-thiazol-2-yl]acetamide;N-[4-(4-Chlorophenyl)-1,3-thiazol-2-yl]-2-(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetamide;2-(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)-N-{4-[3-(trifluoromethoxy)phenyl]-1,3-thiazol-2-yl}acetamide;2-(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)-N-[4-(4- ...

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Номер записи: 46
07-11-2013 дата публикации

LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY

Номер: US20130296317A1
Автор: Bilodeau Mark T., Greshock Thomas J., Kern Jonathan T., Kim Boyoung, McCauley John A., Rada Vanessa L., Rajapakse Hemaka A., Sanders John, Stevenson Heather H.
Принадлежит:

Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO—, —O— or NR—, wherein Rac is H, or Calkyl and Rthrough Rare defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease. 2. A compound of of Formula I wherein “A” is —S— or —NH— or a pharmaceutically acceptable salt thereof.3. A compound of of Formula I wherein “A” is —S— or a pharmaceutically acceptable salt thereof.4. A compound of of Formula I wherein “A” is —NH— or a pharmaceutically acceptable salt thereof.10. A compound of of Formula IB wherein R is —H claim 9 , or cyclopentyl-; and R is methyl- or a pharmaceutically acceptable salt thereof.12. A compound selected from:3-(Methylsulfanyl)-1-(1H-pyrazol-3-yl)-6,7-dihydrothieno[3,4-c]pyridin-4(5H)-one;6-benzyl-3-(methylsulfanyl)-1-(1H-pyrazol-3-yl)-6,7-dihydrothieno[3,4-c]pyridin-4(5)-one;6-methyl-3-(methylsulfanyl)-1-(1H-pyrazol-3-yl)-6,7-dihydrothieno[3,4-c]pyridin-4(5)-one;tert-butyl-6-methyl-3-(methylsulfanyl)-1-(1H-pyrazol-3-yl)-6,7-dihydrothieno[3,4-c]pyridin-5-(4H)-carboxylate;3′-(methylsulfanyl)-4′-oxo-1′-(1H-pyrazol-3-yl)-7′H-spiro[cyclobutane-1,6′-thieno[3,4-1]pyridine]-4′(5′H)-one;tert-butyl-6-methyl-3′-(methylsulfanyl)-4′-oxo-1′-(1H-pyrazol-3-yl)-7′H-spiro[cyclobutane-1,6′-thieno[3,4-1]pyridine]-5′(4′H)-carboxylate;3′-(methylsulfanyl)-4′-oxo-1′-(1H-pyrazol-3-yl)-7′H-spiro[cyclopropane-1,6′-thieno[3,4-1]pyridine]-4′(5′H)-one;3′-(methylsulfanyl)-4′-oxo-1′-(1H-pyrazol-3-yl)-7′H-spiro[cyclopentane-1,6′-thieno[3,4-1]pyridine]-4′(5′H)-one;6-trifluoromethyl-3-(methylsulfanyl)-1-(1H-pyrazol-3-yl)-6,7-dihydrothieno[3,4-c]pyridin-4(5)-one;(6R)-3-(methylsulfanyl)-6-phenyl-1-(1H-pyrazol-3-yl)-6,7-dihydrothieno[3,4-c]pyridin-4(5)-one;6-methoxymethyl-3-(methylsulfanyl)-1-(1H- ...

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Номер записи: 47
14-11-2013 дата публикации

NOVEL (HETEROCYCLE/TETRAHYDROPYRIDINE)-(PIPERAZINYL)-1-ALCANONE AND (HETEROCYCLE/DIHYDROPYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE DERIVATIVES, AND USE THEREOF AS p75 INHIBITORS

Номер: US20130303520A1
Автор: BARONI Marco, BONO Françoise, DELBARY-GOSSART Sandrine, VERCESI Valentina
Принадлежит:

The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): 3. The method according to claim 1 , wherein for the compound of formula (I):{'sub': 1', '4, 'R and R1, located on any of the available positions, independently represent a hydrogen atom, a halogen atom or a group (C-C)alkyl or COOalkyl; or a pharmaceutically acceptable salt thereof.'}7. The method according to claim 1 , wherein the pathology is selected from the group consisting of senile dementia claim 1 , epilepsy claim 1 , Alzheimer's disease claim 1 , Parkinson's disease claim 1 , Huntington's chorea claim 1 , Down's syndrome claim 1 , prion diseases claim 1 , amnesia claim 1 , schizophrenia claim 1 , depression claim 1 , bipolar disorder claim 1 , amyotrophic lateral sclerosis claim 1 , multiple sclerosis claim 1 , post-ischemic heart damage claim 1 , cardiomyopathies claim 1 , myocardial infarction claim 1 , cardiac insufficiency claim 1 , cardiac ischemia claim 1 , cerebral infarction claim 1 , peripheral neuropathies claim 1 , optic nerve and retinal damage claim 1 , retinal pigment degeneration claim 1 , glaucoma claim 1 , retinal ischemia claim 1 , macular degeneration claim 1 , spinal cord trauma claim 1 , cranial trauma claim 1 , atherosclerosis claim 1 , stenosis claim 1 , wound healing disorders claim 1 , and alopecia.8. The method according to claim 1 , wherein the pathology is selected from the group consisting of pancreatitis and hepatic fibrosis.9. The method according to claim 1 , wherein the pathology is cancer wherein the cancer is selected from the group consisting of lung cancer claim 1 , thyroid cancer claim 1 , pancreatic cancer claim 1 , prostate cancer claim 1 , small intestine cancer claim 1 , colorectal cancer and breast cancer.10. The method according to claim 1 , wherein the pathology is selected from the group consisting of pulmonary inflammation claim 1 , allergy ...

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Номер записи: 48
21-11-2013 дата публикации

NOVEL ACRIDINE DERIVATIVES

Номер: US20130310411A1
Автор: Cousin David, Frigerio Mark, Hummersone Marc Geoffery
Принадлежит: PHARMINOX LIMITED

The present invention relates to novel acridine derivatives of formula (I), or pharmaceutically acceptable salts thereof, which are inhibitors of the telomerase enzyme function. These compounds are useful for the treatment cellular proliferation disorders, such as cancer. 2. A compound according to claim 1 , wherein X is O.3. A compound according to claim 1 , wherein X is S.4. A compound according to claim 1 , wherein Z is N.5. A compound according to claim 1 , wherein Z is N-Q.6. A compound according to claim 5 , wherein Q is selected from the group consisting of O claim 5 , (1-6C)alkyl claim 5 , (2-6C)alkenyl and (2-6C)alkynyl claim 5 , or Q is a group of the formula:{'br': None, 'sup': 1', '1, '-L-Q'}wherein:{'sup': '1', 'Lis (1-6C)alkylene which is optionally substituted with one or more (1-4C)alkyl groups;'}{'sup': '1', 'sub': 9', '9', '10', 'p', '9', '9', '9', '9', '9', '10', '10', '9', '10', '10', '9', '2', '9', '9', '2, 'Qis selected from the group consisting of —OR, —NRR, —S(O)R(wherein p is 0, 1 or 2), —C(O)R, —C(O)OR, —OC(O)R, —C(O)NRR, —N(R)C(O)R, —N(R)CON(R)R—, —SON(R)—, —N(R)SO—, (3-8C)cycloalkyl, aryl, heterocyclyl, and heteroaryl, and wherein the (3-8C)cycloalkyl, aryl, heterocyclyl or heteroaryl group is optionally substituted by one or more substituents independently selected from the group consisting of halogen, cyano, nitro, hydroxy, amino and (1-4C)alkoxy;'}{'sub': '9', 'Ris selected from the group consisting of hydrogen, (1-6C)alkyl, (3-8C)cycloalkyl, aryl, heterocyclyl, and heteroaryl, and wherein the (1-6C)alkyl, (3-8C)cycloalkyl, aryl, heterocyclyl, or heteroaryl group is optionally substituted by one or more substituents independently selected from the group consisting of halogen, cyano, nitro, hydroxy, amino and (1-4C)alkoxy; and'}{'sub': '10', 'Ris selected from hydrogen or (1-6C)alkyl.'}7. A compound according to claim 5 , wherein Q is selected from O or (1-6C)alkyl or Q is a group of the formula:{'br': None, 'sup': 1', '1, '-L-Q'} [{' ...

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Номер записи: 49
28-11-2013 дата публикации

PHARMACEUTICAL COMPOUNDS

Номер: US20130317017A1
Автор: Baker Stewart J., Chuckowree Irina S., Folkes Adrian J., Hancox Timothy C., Latif Mohammed A., Shuttleworth Stephen J., Sohal Sukhjit, Wan Nan Chi
Принадлежит: F. Hoffman-La Roche AG

Fused pyrimidines of formula (I): 2. The pharmaceutical composition of formulated in a capsule.3. The pharmaceutical composition of formulated in a tablet.4. The pharmaceutical composition of formulated in the form of oil-in-water emulsion.5. The pharmaceutical composition of comprising an amount of 10 mg to 1000 mg of the thienopyrimidine of formula (I).6. The pharmaceutical composition of comprising an amount of 100 mg to 300 mg of the thienopyrimidine of formula (I).7. The pharmaceutical composition formulated of comprising a carrier claim 1 , diluent or excipient selected from lactose claim 1 , sodium carboxymethylcellulose claim 1 , and magnesium stearate.8. The pharmaceutical composition of comprising an amount of 10 mg to 1000 mg of the thienopyrimidine of formula (I).9. The pharmaceutical composition of comprising an amount of 100 mg to 300 mg of the thienopyrimidine of formula (I). This application is a continuation of U.S. application Ser. No. 13/415,672, filed Mar. 8, 2012, which is a continuation of U.S. application Ser. No. 12/789,773, filed May 28, 2010, which is now U.S. Pat. No. 8,153,629 issued Apr. 10, 2012, which is a continuation of U.S. application Ser. No. 11/893,414, filed Aug. 16, 2007, which is now U.S. Pat. No. 7,750,002 issued Jul. 6, 2010, which is a continuation of PCT/GB2005/004129, filed Oct. 25, 2005, which claims priority from UK Application No. 0423653.5, filed Oct. 25, 2004, which applications are incorporated herein by reference.The present invention relates to pyrimidine derivatives and their use as inhibitors of phosphatidylinositol 3-kinase (PI3K).Phosphatidylinositol (hereinafter abbreviated as “PI”) is one of a number of phospholipids found in cell membranes. In recent years it has become clear that PI plays an important role in intracellular signal transduction. In the late 1980s, a PI3 kinase (PI3K) was found to be an enzyme which phosphorylates the 3-position of the inositol ring of phosphatidylinositol (D. Whitman et al, ...

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Номер записи: 50
28-11-2013 дата публикации

THIENOPYRIDINE AND THIENOPYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20130317045A1
Автор: Hadd Michael J., Holladay Mark W., Setti Eduardo
Принадлежит: AMBIT BIOSCIENCES CORPORATION

Provided herein are thienopyridine and thienopyrimidine compounds of formula (I) for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. 3. The compound of claim 1 , wherein{'sup': 1', '1', '2, 'sub': '2', 'Lis —C(R)(R)—, —S(O)— or —S(O)—;'}{'sup': 1', '2, 'claim-text': [{'sup': 1', '2, '(i) Rand Rtogether form ═O;'}, {'sup': 1', '2, '(ii) Ris hydrogen or halo; and Ris halo;'}, {'sup': 1', '2, '(iii) Ris alkyl, and Ris hydrogen, alkyl, halo, hydroxy or alkoxy; or'}, {'sup': 1', '2, '(iv) Ris halo, hydroxy or alkoxy; and Ris hydrogen or alkyl;'}], 'Rand Rare selected as follows5. The compound of claim 1 , wherein Ris hydrogen or alkyl.6. The compound of claim 1 , wherein each Ris independently hydrogen claim 1 , deutero claim 1 , cyano claim 1 , halo claim 1 , alkyl claim 1 , alkoxy claim 1 , haloalkoxy or cycloalkyl.7. The compound of claim 1 , wherein each Ris hydrogen.8. The compound of claim 1 , wherein Ris halo.10. The compound of claim 9 , whereinB is phenyl, pyridinyl or pyrimidinyl;{'sup': 3', '4', '3', '4, 'Aand Aare selected from N and CH, such that at least one of Aor Ais N;'}{'sup': 1', '1', '2, 'sub': '2', 'Lis —C(R)(R)—, —S(O)— or —S(O)—;'}{'sup': 1', '2, 'claim-text': [{'sup': 1', '2, '(i) Rand Rtogether form ═O;'}, {'sup': 1', '2, '(ii) Ris hydrogen or halo; and Ris halo;'}, {'sup': 1', '2, '(iii) Ris alkyl, and Ris hydrogen, alkyl, halo, hydroxy or alkoxy; and'}, {'sup': 1', '2, '(iv) Ris halo, hydroxy or alkoxy; and Ris hydrogen or alkyl;'}], 'Rand Rare selected from (i), (ii), (iii) and (iv) as follows{'sup': '3', 'Ris hydrogen, alkyl or cycloalkyl,'}{'sup': '4', 'Ris hydrogen or alkyl;'}{'sup': '5', 'Ris hydrogen or alkyl;'}{'sup': '6', 'Ris hydrogen, deutero, halo, cyano, alkyl, haloalkyl, alkoxy or haloalkoxy;'}{'sup': '6a', 'each Ris hydrogen or alkyl;'}{'sup': ...

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Номер записи: 51
19-12-2013 дата публикации

ASYMMETRIC REDUCTION PROCESS

Номер: US20130338377A1
Автор: Andretto Mauro, Cotarca Livius, Nardi Antonio, Verzini Massimo, Volpicelli Raffaella
Принадлежит: ZACH SYSTEM S.P.A.

The present invention relates to a stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SOand Ris hydrogen or an SONHgroup, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof. 2. A process according to claim 1 , wherein X is SO.3. A process according to claim 1 , wherein the hydrogen source is formic acid or a salt thereof claim 1 , said salt being sodium claim 1 , ammonium or triethylammonium formate.4. A process according to claim 1 , wherein the hydrogenating step takes place in the presence of a base selected from triethylamine claim 1 , ammonia; an alkali hydroxide claim 1 , an alkaline earth hydroxide claim 1 , methylated sodium claim 1 , methylated potassium claim 1 , sodium tert-butoxide and potassium tert-butoxide.5. A process according to claim 4 , wherein the base is triethylamine.6. A process according to claim 5 , wherein a cosolvent is acetonitrile.7. A process according to claim 1 , wherein the hydrogenating step takes place in the presence of a catalyst of formula (III).8. A process according to claim 1 , wherein the reduction takes place in the presence of a catalyst of formula (IV).10. A process according to claim 9 , wherein claim 9 , in a compound of formula (V) claim 9 , R is SOCH-p-CH claim 9 , and Rand Rare both an unsubstituted phenyl group.11. A process according to claim 10 , wherein claim 10 , in a compound of formula (VI) claim 10 , Ris 1-CH-4-CH(CH).13. A process according to claim 1 , wherein the catalyst of formula (III) or (IV) is formed before contact with the reaction mixture.14. A process according to claim 13 , wherein the catalyst is RuCl(p-cymene)[(S claim 13 ,S)-Ts-DPEN].15. A process according to claim 1 , further comprising the transformation of the compound of formula (I) into dorzolamide or into ...

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Номер записи: 52
26-12-2013 дата публикации

METHOD FOR PRODUCTION OF PRASUGREL HYDROCHLORIDE HAVING HIGH PURITY

Номер: US20130345428A1
Автор: MIYATA Hiroyuki, WADA Yukinori, YOKOTA Naoyuki
Принадлежит:

A method for producing prasugrel hydrochloride with a reduced content of 2-acetoxy-5-[5-chloro-1-(2-fluorophenyl)-2-oxopentyl]-4,5,6,7-tetrahydrothieno[3,2-6]pyridine by carrying out the following steps: 2. The method according to claim 1 , wherein claim 1 , in step (i) claim 1 , the temperature during the adding claim 1 , optionally dropwise claim 1 , of the chlorinating agent is −10° C. to 5° C. claim 1 , and the reaction temperature after the adding claim 1 , optionally dropwise claim 1 , of the chlorinating agent is −10° C. to 5° C.3. The method according to claim 1 , wherein claim 1 , in step (i) claim 1 , the temperature during the adding claim 1 , optionally dropwise claim 1 , of the chlorinating agent is −5° C. to 5° C. claim 1 , and the reaction temperature after the adding claim 1 , optionally dropwise claim 1 , of the chlorinating agent is −5° C. to 5° C.4. The method according to any one of to claim 1 , further comprising a post-treatment after the end of the reaction in step (i) which is carried out at a temperature of −20° C. to 15° C.5. The method according to any one of to claim 1 , further comprising a post-treatment after the end of the reaction in step (i) which is carried out at a temperature of −10° C. to 15° C.6. The method according to any one of to claim 1 , further comprising a post-treatment after the end of the reaction in step (i) which is carried out at a temperature of 0° C. to 15° C.7. The method according to any one of to claim 1 , wherein the chlorinating agent is chlorine gas.9. The method according to claim 8 , wherein R claim 8 , Rand Rindependently represent an alkyl group having 1 to 5 carbons or a phenyl group.10. The method according to any one of to claim 8 , wherein R is a tert-butyldimethylsilyl group.11. The method according to any one of to claim 8 , wherein the resultant compound represented by the formula (II) is recrystallized from an ether or a nitrile in step (ii).12. The method according to any one of to claim 8 , ...

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Номер записи: 53
02-01-2014 дата публикации

NOVEL FUSED RING COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Номер: US20140001442A1
Автор: Lee Jung-Sub, Yang Seung-Gak
Принадлежит: Samsung Display Co., Ltd.

A fused ring compound represented by Formula 1: 2. The fused ring compound of claim 1 , wherein Xis one of S claim 1 , O claim 1 , and Si(R)(R).3. The fused ring compound of claim 1 , wherein Yand Yare each N claim 1 , and Yis C; Yand Yare each N claim 1 , and Yis C; Yand Yare each N claim 1 , and Yis C; or Y claim 1 , Y claim 1 , and Yare each N.4. The fused ring compound of claim 1 , wherein Yand Yare each N claim 1 , and Yis C; or Y claim 1 , Y claim 1 , and Yare each N.6. The fused ring compound of claim 1 , wherein Arto Arare each independently one of a substituted or unsubstituted C-Caryl group claim 1 , and a substituted or unsubstituted C-Cheteroaryl group;{'sub': 1', '3, 'Lto Lare each independently one of a substituted or unsubstituted phenylene group, and a substituted or unsubstituted naphthalene group; and'}a, b and c are each independently an integer from 0 to 1.7. The fused ring compound of claim 1 , wherein Ato Arare each independently one of a substituted or unsubstituted phenyl group claim 1 , a substituted or unsubstituted naphthyl group claim 1 , a substituted or unsubstituted anthryl group claim 1 , a substituted or unsubstituted phenanthrenyl group claim 1 , a substituted or unsubstituted phenalenyl group claim 1 , a substituted or unsubstituted pyrenyl group claim 1 , a substituted or unsubstituted chrysenyl group claim 1 , a substituted or unsubstituted triphenylenyl group claim 1 , a substituted or unsubstituted tetracenyl group claim 1 , a substituted or unsubstituted tetraphenyl group claim 1 , a substituted or unsubstituted benzoanthryl group claim 1 , a substituted or unsubstituted benzophenanthrenyl group claim 1 , a substituted or unsubstituted biphenyl group claim 1 , a substituted or unsubstituted terphenyl group claim 1 , a substituted or unsubstituted indenyl group claim 1 , a substituted or unsubstituted fluorenyl group claim 1 , a substituted or unsubstituted benzofluorenyl group claim 1 , a substituted or unsubstituted ...

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Номер записи: 54
09-01-2014 дата публикации

Biotin Derivatives

Номер: US20140011255A1
Автор: Branchauo Bruce, Ying Lai-Qiang, Yue Stephen, Zhang Yu-Zhong
Принадлежит: LIFE TECHNOLOGIES CORPORATION

Biotin derivatives, methods of using the biotin derivatives and kits comprising the biotin derivatives. 1153.-. (canceled)155. The biotin derivative of claim 154 , wherein if Ris H claim 154 , Ris a derivative group and if Ris H claim 154 , Ris a derivative group.156. The biotin derivative of claim 154 , wherein Ris a derivative group.157. The biotin derivative of claim 156 , wherein Rcomprises 1 to 8 carbon atoms.158. The biotin derivative of claim 154 , wherein Ris a derivative group.159. The biotin derivative of claim 158 , wherein Rcomprises 1 to 8 carbon atoms.160. The biotin derivative of claim 154 , wherein L is a linker.161. The biotin derivative of claim 160 , wherein L is selected from a polyethylene glycol linker and an oligopeptide linker.162. The biotin derivative of claim 160 , wherein the linker comprises a detectable moiety.163. The biotin derivative of claim 162 , wherein the detectable moiety comprises: a chromophore claim 162 , a fluorescent dye claim 162 , a fluorescent protein claim 162 , a nanocrystal claim 162 , an enzyme claim 162 , or a radioisotope.164. The biotin derivative of claim 163 , wherein the detectable moiety is a fluorescent dye.166. The biotin derivative of claim 165 , wherein Ris —ORor —COOR.167. The biotin derivative of claim 166 , wherein Ris H or comprises 1 to 8 carbon atoms.168. The biotin derivative of claim 154 , wherein Ris a reactive group.169. The biotin derivative of claim 168 , wherein the reactive group is selected from:(a) isothiocyanate, sulfonyl chloride, 4,6-dichlorotriazinyl, a carboxylate, a halo acetyl, hydrazide, a succinimidyl ester, a 4-sulfonyl-3,5-dichlorophenol ester, a maleimide, an iodoacetamide; an azide, and an alkyne, when L is a linker; or(b) hydroxyl, hydrazinyl, N-hydroxysuccinimidyl, and 4-sulfonyl-3,5-dichlorophenol, when L is absent.171. The biotin derivative of claim 154 , wherein Ris selected from a polypeptide claim 154 , a peptide claim 154 , an amino acid claim 154 , a dextran claim 154 ...

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Номер записи: 55
09-01-2014 дата публикации

ENANTIOMERS OF FLUCONAZOLE ANALOGUES CONTAINING THIENO-[2,-3-D]PYRIMIDIN-4(3H)-ONE MOIETY AS ANTIFUNGAL AGENTS

Номер: US20140011818A1
Автор: Borate Hanumant Bapurao, Chandavarkar Mohan Anand, Chavan Gajanan Jalindar, Chavan Subhash Prataprao, Iyer Ramkrishnan Ramachandran, Maujan Suleman Riyajsaheb, Nawathye Vikas Vasanat, Rao Deepali Damodar, Sawargave Sangmeshwer Prabhkara, Tawte Amit Chandrakant
Принадлежит:

The present invention discloses novel enantiomeric antifungal compounds of Formula (1a) and Formula (1b) containing thieno-[2,3-d]Jpyrimidin-4(3H)-one moiety and pharmaceutically acceptable salts thereof, method of preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these compounds. 112-. (canceled)14. The antifungal compounds of Formula (1b) as claimed in claim 13 , wherein at least one of Rand Ris said linear or branched alkyl group having from 1 to 20 carbon atoms.15. The antifungal compounds of Formula (1b) as claimed in claim 13 , wherein said arylalkyl group comprises a phenyl group claim 13 , said phenyl group being optionally substituted with an alkyl group having 1 to 3 carbon atoms.17. The antifungal compounds of Formula (1a) as claimed in claim 16 , wherein said arylalkyl group comprises a phenyl group claim 16 , said phenyl group being optionally substituted with an alkyl group having 1 to 3 carbon atoms.20. The process as claimed in claim 18 , wherein the base is selected from the group consisting of organic and inorganic bases.21. The process as claimed in claim 18 , wherein the base is selected from the group consisting of potassium carbonate claim 18 , sodium carbonate and cesium carbonate.22. The process as claimed in claim 19 , wherein the base is selected from the group consisting of organic and inorganic bases.23. The process as claimed in claim 19 , wherein the base is selected from the group consisting of potassium carbonate claim 19 , sodium carbonate and cesium carbonate.24. The process as claimed in claim 18 , wherein the catalyst is selected from the group consisting of tetrabutylammonium bromide claim 18 , tetrabutylammonium chloride claim 18 , triethylbenzylammonium chloride or cetyltrimethylammonium bromide claim 18 , and mixtures thereof.25. The process as claimed in claim 19 , wherein the catalyst is selected from the group consisting of ...

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Номер записи: 56
16-01-2014 дата публикации

IRAK INHIBITORS AND USES THEREOF

Номер: US20140018343A1
Автор: Greenwood Jeremy Robert, Robinson Shaughnessy, Romero Donna L., Wessel Matthew David
Принадлежит:

The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same. 7. The compound of wherein m is 0.8. The compound of claim 1 , wherein Ring B is a 6-membered heteroaromatic fused ring having 1-2 nitrogens claim 1 , or a pharmaceutically acceptable salt thereof.9. The compound of claim 1 , wherein Ring B is a 5-membered heteroaromatic fused ring having 1-2 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , and sulfur; or a pharmaceutically acceptable salt thereof.10. The compound of claim 1 , wherein said compound is selected from any one of the compounds depicted in Table 1 claim 1 , or a pharmaceutically acceptable salt thereof.11. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.12. A method of inhibiting an IRAK protein kinase in a patient or biological sample comprising administering to said patient claim 1 , or contacting said biological sample with a compound according to claim 1 , or a pharmaceutical composition thereof.13. The method of claim 12 , wherein the IRAK protein kinase is an IRAK-4 protein kinase.14. The method of claim 12 , wherein the IRAK protein kinase is an IRAK-1 protein kinase.15. A method of treating an IRAK-mediated disorder claim 1 , disease claim 1 , or condition in a patient comprising administering to said patient a compound according to claim 1 , or a pharmaceutical composition thereof.16. The method of claim 15 , wherein the IRAK-mediated disorder claim 15 , disease or condition is selected from the group consisting of a cancer claim 15 , a neurodegenerative disorder claim 15 , a viral disease claim 15 , an autoimmune disease claim 15 , an inflammatory disorder claim 15 , a hereditary disorder claim 15 , a hormone-related disease claim 15 , a metabolic disorder claim 15 , conditions associated with organ transplantation claim 15 , ...

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Номер записи: 57
16-01-2014 дата публикации

IRAK INHIBITORS AND USES THEREOF

Номер: US20140018357A1
Автор: Greenwood Jeremy Robert, Harriman Geraldine C., Masse Craig E., Robinson Shaughnessy, Romero Donna L., Wester Ronald T.
Принадлежит:

The present invention provides thienopyridine compounds, compositions thereof, and methods of using the same. 6. The compound of wherein m is 0.9. The compound of claim 1 , wherein said compound is selected from any one of the compounds depicted in Table 1 claim 1 , or a pharmaceutically acceptable salt thereof.10. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.11. A method of inhibiting an IRAK protein kinase in a patient or biological sample comprising administering to said patient claim 1 , or contacting said biological sample with a compound according to claim 1 , or a pharmaceutical composition thereof.12. The method of claim 11 , wherein the IRAK protein kinase is an IRAK-4 protein kinase.13. The method of claim 11 , wherein the IRAK protein kinase is an IRAK-1 protein kinase.14. A method of treating an IRAK-mediated disorder claim 1 , disease claim 1 , or condition in a patient comprising administering to said patient a compound according to claim 1 , or a pharmaceutical composition thereof.15. The method of claim 14 , wherein the IRAK-mediated disorder claim 14 , disease or condition is selected from the group consisting of a cancer claim 14 , a neurodegenerative disorder claim 14 , a viral disease claim 14 , an autoimmune disease claim 14 , an inflammatory disorder claim 14 , a hereditary disorder claim 14 , a hormone-related disease claim 14 , a metabolic disorder claim 14 , conditions associated with organ transplantation claim 14 , immunodeficiency disorders claim 14 , a destructive bone disorder claim 14 , a proliferative disorder claim 14 , an infectious disease claim 14 , a condition associated with cell death claim 14 , thrombin-induced platelet aggregation claim 14 , liver disease claim 14 , pathologic immune conditions involving T cell activation claim 14 , a cardiovascular disorder claim 14 , and a CNS disorder.16. The method of claim 15 , ...

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Номер записи: 58
23-01-2014 дата публикации

COMPOUNDS, SCREENS, AND METHODS OF TREATMENT

Номер: US20140024662A1
Автор: Degterev Alexei, Yuan Chengye, Yuan Junying
Принадлежит:

The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associate with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described. 5. The compound of claim 1 , wherein said compound is selected from the group consisting of compounds 6 to 31 of Table 2; compounds 32 to 51 of Table 3; compounds 52 to 62 of Table 4; compounds 63 to 78 of Table 5; compounds 79 to 92 of Table 6; compounds 93 to 103 of Table 7; compounds 104 to 118 of Table 8; compounds 119 to 122 of Table 9; compounds 123 to 126 of Table 10; compounds 127 to 129 of Table 11; compounds 130 to 132 of Table 12; compounds 133 to 136 of Table 13; compounds 137 to 139 of Table 14; compounds 140 to 142 of Table 15; compounds 143 to 148 of Table 16; compounds 149 to 153 of Table 17; compounds to 154 to 157 of Table 18; compounds 158 to 161 of Table 19; compounds 162 to 169 of Table 20; compounds 170 to 172 of Table 21; and compounds 173 to 182 of Table 22.6. The compound of claim 1 , wherein said compound is selected from the group consisting of compounds 6 claim 1 , 13 claim 1 , 24 claim 1 , and 25 of Table 2; compounds 33 to 35 claim 1 , 38 to 41 claim 1 , 43 claim 1 , 44 claim 1 , and 47 to 49 of Table 3; compounds 53 claim 1 , 55 claim 1 , and 58 of Table 4; compounds 67 claim 1 , 68 claim 1 , and 72 to 76 of Table 5; compounds 87 and 90 of Table 6; compounds 98 and 103 of Table 7; compounds 106 and 114 of Table 8; compounds 119 and 121 of Table 9; compounds 123 and 125 of Table 10; compounds 127 to 129 of Table 11; compound 130 of Table 12; compounds 133 to 136 of Table 13; compounds 137 and 138 of Table 14; compounds 144 and 146 of Table 16; compound 150 of Table 17; compounds 154 and 156 of Table 18; and compound 167 of Table 20.7. The compound of claim 6 , wherein said compound is an active Nec-5 compound.9. The pharmaceutical composition of claim ...

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Номер записи: 59
23-01-2014 дата публикации

Process For The Preparation Of A Sulfated Derivative Of 3,5-Diiodo-O-[3-Iodophenyl]-L-Tyrosine

Номер: US20140024717A1
Автор: ANELLI Pier Lucio, Argese Maria, BOI Valeria, CAVALIERI Livio, Galimberti Laura, Gazzetto Sonia, Lattuada Luciano, MAISANO Federico, RIVOLTA Giovanni, VELLA Fulvia
Принадлежит: BRACCO IMAGING S.P.A.

The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chloro-sulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives. 2. The process according to claim 1 , wherein said inorganic salt is a sodium salt.3. The process according to claim 1 , wherein the molar ratio between CSA and the compound of formula I is comprised from 4 to 10.4. The process according to claim 1 , wherein in step a) the concentration of the compound of formula I in DMAC is comprised from 0.060 to 0.090 mol/L of DMAC.5. The process according to claim 1 , wherein the sulfation reaction in step a) is carried out at a temperature below 10° C.6. The process according to claim 5 , wherein the sulfation in step a) is left to occur for at least 2 hours.7. The process according to claim 1 , wherein the salification according to step b) is carried out in an aqueous solution of NaHCO.8. The process according to claim 1 , wherein step c) is preceded by a filtration step.9. The process according to claim 1 , wherein said decreasing polarity mixture is a mixture of water and a polar solvent in a ratio comprised from 1.0:0 to 0.7:0.3.109. The process according to any one of - claims 8 , wherein after elution claims 8 , the solution is concentrated to at least 10 g of Formula II compound/kg claims 8 , and the solution is brought to pH values comprised from 5.5 to 6.5.11. The process according to claim 1 , wherein the compound of formula II is obtained as a solid after treatment ...

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Номер записи: 60
30-01-2014 дата публикации

POCHOXIME CONJUGATES USEFUL FOR THE TREATMENT OF HSP90 RELATED PATHOLOGIES

Номер: US20140031302A1
Автор: BARLUENGA Sofia, WINSSINGER Nicolas
Принадлежит: Universite De Strasbourg

The present invention includes novel derivatives, analogs, and intermediates of the natural products radicicol, pochonins, pochoximes, and their syntheses. The present invention also provides a pharmaceutical composition comprising the present compound and the use of the compound as inhibitors of kinases and of the enzyme family known as heat shock protein 90 (HSP90). 2. The compound of claim 1 , wherein X is O or NR.3. The compound of claim 1 , wherein Y is —OR claim 1 , —O—(CH)COOR or —O—(CH)CON(R).4. The compound of claim 1 , wherein Rand Rare independently hydrogen claim 1 , halogen claim 1 , or lower alkyl.5. The compound of claim 4 , wherein{'sup': '1', 'Ris hydrogen, halogen, or lower alkyl; and'}{'sup': '2', 'Ris hydrogen.'}6. The compound of claim 1 , wherein Ris lower alkyl claim 1 , alkoxy-substituted lower alkyl claim 1 , or aryl-substituted lower alkyl.7. The compound of claim 6 , wherein Ris methyl claim 6 , ethyl claim 6 , isopropyl claim 6 , n-propyl claim 6 , n-butyl claim 6 , isobutyl claim 6 , t-butyl claim 6 , methoxy-ethyl claim 6 , methoxy-methyl claim 6 , chloromethyl claim 6 , or benzyl.8. The compound of claim 1 , wherein L-TM is an oxygen or nitrogen-based functional group.14. A compound selected from the group consisting of the compounds exemplified by Scheme 2 as described in the specification claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , and/or prodrug thereof.15. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.16. A method of treating a patient with a disease comprising administering to the patient with the disease an effective amount of a compound of claim 1 , wherein the disease is mediated by kinases and Heat Shock Protein 90 (HSP90).17. The method of claim 16 , wherein the disease is an autoimmune disease claim 16 , inflammatory disease claim 16 , neurological or neurodegenerative disease claim 16 , cancer claim 16 , cardiovascular disease claim 16 , ...

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Номер записи: 61
30-01-2014 дата публикации

THERAPEUTIC PYRAZOLYL THIENOPYRIDINES

Номер: US20140031385A1
Автор: Barrett Stephen D., Boys Mark L., Chen Huifen, Kramer James B.
Принадлежит: Medicis Phamaceutical Corporation

The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, 23-. (canceled)4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris a thieno[2 claim 1 ,3-c]pyridinyl claim 1 , which may be optionally substituted with one to three substituents each independently selected from the group consisting of: —OH claim 1 , C-Calkyl claim 1 , halo claim 1 , and —O—C-Calkyl.5. (canceled)7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare independently selected from the group consisting of: hydrogen claim 1 , C-C-alkyl claim 1 , —(C-C-alkyl)-O—(C-C-alkyl) claim 1 , —O—C-C-alkyl claim 1 , —C(O)O—C-C-alkyl claim 1 , —C(O)O—H claim 1 , C(O)NH claim 1 , —C(O)NH(C-Calkyl) claim 1 , —C(O)N(C-Calkyl) claim 1 , halo claim 1 , —CN claim 1 , —OH claim 1 , and a C-C-cycloalkyl.8. The compound of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein Rand Rare independently selected from the group consisting of: hydrogen claim 7 , and C-Calkyl.9. The compound of claim 8 , or a pharmaceutically acceptable salt thereof claim 8 , wherein Ris C-Calkyl and Ris hydrogen.10. The compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , or a pharmaceutically acceptable salt thereof wherein R claim 9 , R claim 9 , and Rare H claim 9 , and Ris C-C-alkyl.11. The compound of claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , wherein Ris methyl.12. The compound of claim 11 , or a pharmaceutically acceptable salt thereof wherein Ris a thieno[2 claim 11 ,3-c]pyridinyl claim 11 , which may be optionally substituted with one to three substituents each independently selected from the group consisting of: —OH claim 11 , C-Calkyl claim 11 , halo claim 11 , and —O—C-Calkyl.13. The compound of claim 12 , or a pharmaceutically acceptable salt thereof wherein Ris a thieno[2 claim 12 ,3-c]pyridin-2-yl claim 12 , which may be optionally ...

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Номер записи: 62
30-01-2014 дата публикации

Novel anti-platelet compound addition salt

Номер: US20140031386A1
Автор: Xiaojing Yan
Принадлежит: GUANGZHOU HEERSHI PHARMA DEV CO Ltd

The present invention relates to a use of haloid acid salt and sulfonate of a compound of formula I and a salt of the compound of formula I in preparation of medicament for preventing or treating diseases caused by thrombosis or embolism. The present invention provides acid addition salts, especially haloid acid and sulfonic acid addition salts of a compound of formula I having high inhibition effect on platelet aggregation, and preparation method of the same, a medicament comprising the same, and a use and/or method for preventing or treating diseases caused by thrombosis or embolism.

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Номер записи: 63
13-02-2014 дата публикации

2-AMINO-4-ARYLTHIAZOLE COMPOUNDS AS TRPA1 ANTAGONISTS

Номер: US20140045865A1
Автор: Chaudhari Sachin Sundarlal, Gudi Girish, Kansagra Bipin Parsottam, KHAIRATKAR-JOSHI Neelima, Kumar Sukeerthi, Mukhopadhyay Indranil, Thomas Abraham, Yemireddy Venkata Ramana
Принадлежит: Glenmark Pharmaceuticals, S.A.

The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. 142.-. (canceled)43. A compound selected from[2-{[(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-4-[3-fluoro-4-(trifluoromethyl)phenyl]-1,3-thiazol-3 (2H)-yl]methyl-2-methyl propanoate;[4-[2,4-Difluoro-3-(trifluoromethyl)phenyl]-2-{[(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl-2-methylpropanoate;[4-[3-Chloro-4-(trifluoromethoxy)phenyl]-2-{[(1,3,6-trimethyl-2,4-dioxo-1,2,3,4-tetrahydrofuro[2,3-d]pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl 2,2-dimethylpropanoate;[4-[2,4-Difluoro-3-(trifluoromethyl)phenyl]-2-{[(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl L-prolinate;[4-[2,4-Difluoro-3-(trifluoromethyl)phenyl]-2-{[(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl L-prolinate hydrochloride;[2-{[(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-4-[3-fluoro-4-(trifluoromethyl)phenyl]-1,3-thiazol-3 (2H)-yl]methylpiperidine-4-carboxylate;[2-{[(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-4-[3-fluoro-4-(trifluoromethyl)phenyl]-1,3-thiazol-3 (2H)-yl]methylpiperidine-4-carboxylate hydrochloride;[4-[2,4-Difluoro-3-(trifluoromethyl)phenyl]-2-{[(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d] ...

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Номер записи: 64
10-04-2014 дата публикации

PROCESS FOR MAKING THIENOPYRIMIDINE COMPOUNDS

Номер: US20140100366A1
Автор: Babu Srinivasan, CHENG Zhigang, Gosselin Francis, Hidber Pirmin, Hoffmann Ursula, Humphries Theresa, Reents Reinhard, Tian Qingping, Yajima Herbert
Принадлежит: Genentech, Inc.

Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure: 2. The process of wherein the salt of (S)-2-hydroxy-1-(piperazin-1-yl)propan-1-one 6 is the oxalate salt.3. The process of wherein the oxalate salt of (S)-2-hydroxy-1-(piperazin-1-yl)propan-1-one is prepared by a process comprising reacting (S)-ethyl 2-hydroxypropanoate with piperazine claim 2 , followed by oxalic acid.5. The process of wherein the oxalate salt (S)-2-hydroxy-1-(piperazin-1-yl)propan-1-one V is prepared by a process comprising:(a) acetylation of (S)-2-hydroxypropanoic acid (L-lactic acid) 1 to give (S)-2-acetoxypropanoic acid;(b) reacting (S)-2-acetoxypropanoic acid with a chlorinating reagent to give (S)-1-chloro-1-oxopropan-2-yl acetate;(c) reacting S)-1-chloro-1-oxopropan-2-yl acetate with 1-benzylpiperazine to give (S)-1-(4-benzylpiperazin-1-yl)-1-oxopropan-2-yl acetate;(d) hydrolysis of the acetate of (S)-1-(4-benzylpiperazin-1-yl)-1-oxopropan-2-yl acetate to give (S)-1-(4-benzylpiperazin-1-yl)-2-hydroxypropan-1-one;(e) reductive removal of the benzyl group of (S)-1-(4-benzylpiperazin-1-yl)-2-hydroxypropan-1-one with a palladium catalyst to give (5)-2-hydroxy-1-(piperazin-1-yl)propan-1-one; and(f) reacting (S)-2-hydroxy-1-(piperazin-1-yl)propan-1-one with oxalic acid to give V.7. The process of wherein 2-aminopyrimidin-5-ylboronic acid III is prepared by a process comprising:(a) reacting 5-bromopyrimidin-2-amine with lithium bis(trimethylsilyl)amide and then n-butyllithium, followed by a trialkyl borate reagent; and(b) treatment of the mixture with aqueous acid to give III.13. The process of wherein the palladium catalyst is selected from PdCl(PPh) claim 1 , Pd(t-Bu) claim 1 , PdCldppf CHCl claim 1 , Pd(PPh) claim 1 , Pd(OAc)/PPh claim 1 , ClPd[(Pet)] claim 1 , Pd(DIPHOS) claim 1 , ClPd(Bipy) claim 1 , [PdCl(PhPCHPPh)] ...

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Номер записи: 65
07-01-2016 дата публикации

MODULATION OF SALTY TASTE PERCEPTION BY ALTERING THE FUNCTION OF BITTER- OR PKD2L1-EXPRESSING TASTE RECEPTOR CELLS

Номер: US20160000126A1
Автор: OKA Yuki, Zuker Charles
Принадлежит: The Trustees of Columbia University in the City of New York

The current invention is in the field of taste and relates to methods and compositions to modulate the perceived taste of saltiness in food or food products where salty taste is desired. The methods and compositions relate to altering the activation and/or activity of the bitter-sensing taste receptor cells and the PKD2L1-expressing taste receptor cells. The invention also relates to food and food products containing agents and composition that alter the activation and/or activity of the bitter-sensing taste receptor cells and the PKD2L1-expressing taste receptor cells. 1. A method for modulating the perceived saltiness of a salty taste stimulant in a food or food product , comprising administering to a subject who is ingesting the food or food product , an agent that alters the activation or activity of bitter-sensing taste receptor cells (TRCs) and/or their concomitant pathway.2. The method of claim 1 , wherein the agent is administered before claim 1 , during or slightly after the subject ingests the food or food product.3. The method of claim 1 , wherein the food or food product contains sodium chloride.4. The method of claim 1 , wherein the food or food product contains a sodium substitute.5. The method of claim 4 , wherein the sodium substitute is chosen from the group consisting of potassium chloride claim 4 , magnesium chloride claim 4 , and calcium chloride.6. The method of claim 1 , wherein the food or food product is chosen from the group consisting of crackers claim 1 , potato chips claim 1 , corn chips claim 1 , tortilla chips claim 1 , sauces claim 1 , canned soups claim 1 , and canned vegetables.7. The method of claim 1 , wherein the agent is chosen from the group consisting of chemicals claim 1 , phytochemicals claim 1 , pharmaceuticals claim 1 , biologics claim 1 , small organic molecules claim 1 , antibodies claim 1 , nucleic acids claim 1 , peptides claim 1 , and proteins.8. The method of claim 1 , wherein the agent is allyl isothiocyanate.9. A ...

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Номер записи: 66
07-01-2016 дата публикации

IRAK INHIBITORS AND USES THEREOF

Номер: US20160002256A1
Автор: Greenwood Jeremy R., Harriman Geraldine C., Masse Craig E., Robinson Shaughnessy, Romero Donna L., Wester Ronald T.
Принадлежит:

The present invention provides thienopyridine compounds, compositions thereof, and methods of using the same. 6. The compound of wherein m is 0.9. The compound of claim 1 , wherein said compound is selected from any one of the compounds depicted in Table 1 claim 1 , or a pharmaceutically acceptable salt thereof.10. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.11. A method of inhibiting an IRAK protein kinase in a patient or biological sample comprising administering to said patient claim 1 , or contacting said biological sample with a compound according to claim 1 , or a pharmaceutical composition thereof.12. The method of claim 11 , wherein the IRAK protein kinase is an IRAK-4 protein kinase.13. The method of claim 11 , wherein the IRAK protein kinase is an IRAK-1 protein kinase.14. A method of treating an IRAK-mediated disorder claim 1 , disease claim 1 , or condition in a patient comprising administering to said patient a compound according to claim 1 , or a pharmaceutical composition thereof.15. The method of claim 14 , wherein the IRAK-mediated disorder claim 14 , disease or condition is selected from the group consisting of a cancer claim 14 , a neurodegenerative disorder claim 14 , a viral disease claim 14 , an autoimmune disease claim 14 , an inflammatory disorder claim 14 , a hereditary disorder claim 14 , a hormone-related disease claim 14 , a metabolic disorder claim 14 , conditions associated with organ transplantation claim 14 , immunodeficiency disorders claim 14 , a destructive bone disorder claim 14 , a proliferative disorder claim 14 , an infectious disease claim 14 , a condition associated with cell death claim 14 , thrombin-induced platelet aggregation claim 14 , liver disease claim 14 , pathologic immune conditions involving T cell activation claim 14 , a cardiovascular disorder claim 14 , and a CNS disorder.16. The method of claim 15 , ...

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Номер записи: 67
07-01-2016 дата публикации

IRAK INHIBITORS AND USES THEREOF

Номер: US20160002257A1
Автор: Greenwood Jeremy Robert, Robinson Shaughnessy, Romero Donna L., Wessel Matthew David
Принадлежит:

The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same. 7. The compound of wherein m is 0.8. The compound of claim 1 , wherein Ring B is a 6-membered heteroaromatic fused ring having 1-2 nitrogens claim 1 , or a pharmaceutically acceptable salt thereof.9. The compound of claim 1 , wherein Ring B is a 5-membered heteroaromatic fused ring having 1-2 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , and sulfur; or a pharmaceutically acceptable salt thereof.10. The compound of claim 1 , wherein said compound is selected from any one of the compounds depicted in Table 1 claim 1 , or a pharmaceutically acceptable salt thereof.11. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.12. A method of inhibiting an IRAK protein kinase in a patient or biological sample comprising administering to said patient claim 1 , or contacting said biological sample with a compound according to claim 1 , or a pharmaceutical composition thereof.13. The method of claim 12 , wherein the IRAK protein kinase is an IRAK-4 protein kinase.14. The method of claim 12 , wherein the IRAK protein kinase is an IRAK-1 protein kinase.15. A method of treating an IRAK-mediated disorder claim 1 , disease claim 1 , or condition in a patient comprising administering to said patient a compound according to claim 1 , or a pharmaceutical composition thereof.16. The method of claim 15 , wherein the IRAK-mediated disorder claim 15 , disease or condition is selected from the group consisting of a cancer claim 15 , a neurodegenerative disorder claim 15 , a viral disease claim 15 , an autoimmune disease claim 15 , an inflammatory disorder claim 15 , a hereditary disorder claim 15 , a hormone-related disease claim 15 , a metabolic disorder claim 15 , conditions associated with organ transplantation claim 15 , ...

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Номер записи: 68
07-01-2016 дата публикации

Process for Preparation of Olanzapine Pamoate

Номер: US20160002258A1
Автор: LAXMALLA Sampath Kumar, NEELA Praveenkumar, Ravi Ponnaiah, REDDY Kubireddy Vigneshwar, WADEKAR Kashyap Ravindrabhai
Принадлежит:

An improved process for preparation of Olanzapine pamoate monohydrate from Olanzpaine is disclosed which comprises mixing at room temperature a solution of olanzapine prepared in water in presence of an acid, with a solution of pamoic acid prepared in water in presence of a base; stirring and maintaining the reaction mixture for a sufficient time till precipitation of solid and drying the solid to obtain olazapine pamoate monohydrate. 1. An improved process for preparation of olanzapine pamoate monohydrate from olanzpaine comprising:(i) preparing a solution of olanzapine in water in presence of an acid;(ii) preparing a solution of pamoic acid in water in presence of a base;(iii) mixing the pamoic acid solution prepared in step (ii) with the olanzapine solution prepared in step (i);(iv) maintaining the reaction mixture for a sufficient time till precipitation of solid;(v) optionally, filtering the reaction mass;(vi) drying the solid to obtain olazapine pamoate monohydrate.2. The process as claimed in claim 1 , wherein the olanzapine is selected from olanzapine Form-I claim 1 , any polymorphic form of olanzapine and any solvate of olanzapine.3. The process as claimed in claim 1 , wherein said acid is an organic acid or inorganic acid.4. The process as claimed in claim 3 , wherein said organic acid is selected from the group comprising of mono- and polycarboxylic acids having a linear or cyclic aliphatic group with 2 to 50 carbon atoms claim 3 , condensed aliphatic heterocyclic group with 2 to 14 carbon atoms and at least one heteroatom (preferably 1 to 3 heteroatoms) such as a nitrogen atom claim 3 , an oxygen atom and/or a sulfur atom.5. The process as claimed in claim 3 , wherein the inorganic acid is selected from the group comprising of sulfuric acid claim 3 , phosphoric acid claim 3 , nitric acid claim 3 , hydrochloric acid and hydrobromic acid.6. The process as claimed in claim 1 , wherein the base is selected from an inorganic or organic base.7. The process as ...

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Номер записи: 69
07-01-2016 дата публикации

THIENO[3,2-D]PYRIMIDINE-6-CARBOXAMIDES AND ANALOGUES AS SIRTUIN MODULATORS

Номер: US20160002273A1
Автор: BLUM Charles A., Disch Jeremy S., EVINDAR Ghotas, Perni Robert B.
Принадлежит:

Provided herein are novel substituted thieno[3,2-d]pyrimidine-6-carboxamide sirtuin inhibitors and methods of use thereof. The sirtuin inhibitors may be used for inhibiting a sirtuin-mediated biological process, and, e.g. for treating and/or preventing diseases and disorders including, but not limited to cancer, neurodegenerative disease and inflammation. Also provided herein are pharmaceutical compositions comprising these sirtuin inhibitors and compositions comprising a sirtuin inhibitor in combination with another therapeutic agent. 4. The compound or salt of claim 1 , wherein W is S.5. The compound or salt of claim 1 , wherein X is —C(═O)—NH.6. The compound or salt of claim 1 , wherein Y is selected from CH—(C-Cstraight chain or branched alkyl)-NH—C(═O)—R claim 1 , CH—(C-Cstraight chain or branched alkyl)-NRR claim 1 , N—(C-Cstraight chain or branched alkyl)-NH—C(═O)—R claim 1 , N—(C-Cstraight chain or branched alkyl)-NRR claim 1 , CH—(C-Cstraight chain or branched alkyl)-R claim 1 , and CH—(C-Cstraight chain or branched alkyl)-NH—C(═S)—R.15. The compound or salt of claim 1 , wherein Ris selected from a 5- to 6-membered saturated or unsaturated carbocycle or heterocycle claim 1 , —C-Cstraight chain or branched alkyl claim 1 , —O—(C-Cstraight chain or branched alkyl) claim 1 , and —OH.16. The compound or salt of claim 1 , wherein Ris selected from —C-Cstraight chain or branched alkyl and —S(═O)—CH.17. The compound or salt of claim 1 , wherein two Rbound to the same nitrogen are taken together with the nitrogen atom to form an optionally substituted 5- to 6-membered saturated heterocycle.18. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or diluent.19. A method for treating a subject suffering from a neurodegenerative disorder or cancer comprising administering to the subject in need thereof a composition of .20. A method of detecting sirtuin-dependence in a biological signal comprising comparing the biological ...

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Номер записи: 70
07-01-2021 дата публикации

MODULATORS OF THE NMDA RECEPTOR

Номер: US20210002292A1
Автор: Ascic Erhad, David Laurent, Kilburn John Paul, Marigo Mauro
Принадлежит:

The present invention is directed to novel modulators of the NMDA receptor. Separate aspects of the inventions are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat neurological disorders or neuropsychiatric disorders such as depression. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': '1', 'sub': '1-4', 'Ris selected from the group consisting of a hydrogen, halogen, and Calkyl;'}{'sup': '2', 'sub': '1-4', 'Ris selected from the group consisting of hydrogen, halogen, and Calkyl;'}{'sup': '3', 'sub': '1-4', 'Ris selected from the group consisting of hydrogen, halogen, and Calkyl;'}{'sup': 4', '6', '7, 'sub': 1-4', '1-4', '1-4, 'Ris selected from the group consisting of hydrogen, halogen, Calkyl, Chaloalkyl, Chydroxyalkyl, OR, and R;'}{'sup': '6', 'sub': 1-4', '1-4, 'Ris selected from the group consisting of Calkyl, and Chaloalkyl; and'}{'sup': '7', 'sub': 3-6', '1-3', '1-3', '1-3', '1-3, 'Ris selected from the group consisting of a Ccycloalkyl and phenyl, wherein said cycloalkyl and phenyl is independently unsubstituted or substituted with 1, 2 or 3 substituents independently selected from halogen, Calkyl, Calkoxy, wherein said Calkyl and Calkoxy are independently unsubstituted or substituted withl, 2 or 3 F.'}3. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.4. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.5. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , Calkyl claim 1 , and halogen.6. The compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of hydrogen claim 5 , fluoro claim 5 , and methyl.7. The compound according to claim 6 , or ...

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Номер записи: 71
07-01-2021 дата публикации

HETEROCYCLIC COMPOUNDS AS BET INHIBITORS

Номер: US20210002293A1
Автор: BARDE Anup, CHAKRAVARTY Sarvajit, CHEN Jiyun, KANKANALA Jayakanth, Miller Chris P., Nayak Anjan Kumar, Pettigrew Jeremy D., Pham Son Minh
Принадлежит:

Novel bromodomain and extraterminal domain (BET) inhibitors and to therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided. 5. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein X is O.6. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gis CH.7. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Zis C—W—Rand Ris C-Caryl optionally substituted by R.8. The compound of claim 7 , or a tautomer or isomer thereof claim 7 , or a pharmaceutically acceptable salt of any of the foregoing claim 7 , wherein Ris phenyl optionally substituted by halogen or C-Calkyl.9. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Zis CH.10. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Zis CH.11. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Ris C-Calkyl.12. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Ris —C(O)NRR claim 1 , 5- to 10-membered heteroaryl claim 1 , —(C-Calkylene)3- to 6-membered heterocyclyl claim 1 , or C-Calkyl claim 1 , each of which is independently optionally substituted by R.13. The compound of claim 12 , or a tautomer or isomer thereof claim 12 , or a pharmaceutically acceptable salt of any of the foregoing claim 12 , wherein Ris —C(O)NRRwhich is optionally substituted by R claim 12 , wherein Rand Rare each independently hydrogen claim 12 , ...

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Номер записи: 72
07-01-2021 дата публикации

COMPOUND AND COLOR CONVERSION FILM COMPRISING SAME

Номер: US20210002294A1
Автор: Cho Seongmi, LEE Hoyong, SON Seonkyoung, SONG Cheol Jun
Принадлежит: LG CHEM, LTD.

The present specification relates to a compound represented by Formula 1, and a color conversion film, a backlight unit, and a display device each including the compound. 4. The compound of claim 1 , wherein Ar1 and Ar2 are the same as or different from each other claim 1 , and are each independently hydrogen; deuterium; a halogen group; a nitrile group; an alkyl group; an alkoxy group; an aryl group unsubstituted or substituted with a halogen group claim 1 , a nitrile group claim 1 , a haloalkyl group claim 1 , an alkyl group claim 1 , C(═O)ORa claim 1 , an alkoxy group claim 1 , an aryl group claim 1 , or a heterocyclic group; or a heterocyclic group which is unsubstituted or substituted with an alkyl group claim 1 , an aryl group claim 1 , or an alkylaryl group claim 1 , or bonding to at least one adjacent group to form a substituted or unsubstituted monocyclic to tricyclic ring claim 1 , andRa is hydrogen; deuterium; or an alkyl group.6. The compound of claim 1 , wherein L1 and L2 are the same as or different from each other claim 1 , and are each independently a direct bond; —O—; a phenylene group; a biphenylene group; a fluorenylene group unsubstituted or substituted with a methyl group or a phenyl group; a spirobifluorenylene group; a divalent carbazole group; a divalent dibenzofuran group; or a divalent quinoline group.8. The compound of claim 1 , wherein R1 and R2 are each hydrogen.10. A color conversion film comprising:a resin matrix; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound according to , the compound being dispersed in the resin matrix.'}11. A backlight unit comprising the color conversion film according to claim10.12. A display device comprising the backlight unit according to .13. The color conversion film of claim 10 , comprising the compound in amount of 0.001 to 20 wt % based on the total weight of the film.14. The color conversion film of claim 10 , wherein the resin matrix is a thermoplastic polymer or a thermosetting ...

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Номер записи: 73
02-01-2020 дата публикации

Compound and Organic Solar Cell Comprising Same

Номер: US20200002468A1
Автор: Choi Doowhan, Jang Songrim, Kim Ji Hoon, Lim Bogyu
Принадлежит: LG CHEM, LTD.

The present specification provides a compound including a unit of Formula 1 and an organic solar cell including the same. 2. The compound of claim 1 , wherein X1 to X3 are each S.4. The compound of claim 1 , wherein R1 to R8 are the same as or different from each other claim 1 , and are each independently hydrogen; a halogen group; a substituted or unsubstituted alkyl group; or a substituted or unsubstituted alkoxy group.5. The compound of claim 1 , wherein R9 and R10 are the same as or different from each other claim 1 , and are each independently a substituted or unsubstituted alkyl group.6. The compound of claim 1 , wherein R11 and R12 are the same as or different from each other claim 1 , and are each independently hydrogen; a halogen group; or a substituted or unsubstituted alkoxy group.7. The compound of claim 1 , wherein Y1 to Y4 are each S.8. The compound of claim 1 , wherein p and q are the same as each other claim 1 , and are each 0 or 1 claim 1 , andr and s are the same as each other, and are each 1 or 2.10. An organic solar cell comprising:a first electrode;a second electrode provided to face the first electrode; andan organic material layer having one or more layers provided between the first electrode and the second electrode and comprising a photoactive layer,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein one or more layers of the organic material layer comprise the compound according .'}11. The organic solar cell of claim 10 , wherein the organic material layer comprises a hole transport layer claim 10 , a hole injection layer or a layer which simultaneously transports and injects holes claim 10 , andthe hole transport layer, the hole injection layer, or the layer which simultaneously transports and injects holes comprises the compound.12. The organic solar cell of claim 10 , wherein the organic material layer comprises an electron injection layer claim 10 , an electron transport layer or a layer which simultaneously injects and ...

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Номер записи: 74
01-01-2015 дата публикации

Organic Transparent Electrode, Method for Producing Organic Transparent Electrode, Touch Panel, Display, Organic Metal, Method for Producing Organic Metal, Compound or Salt Thereof, Electric Wire and Electronic Device

Номер: US20150005511A1
Автор: KOBAYASHI Yuka, Sumi Satoshi, Terauchi Takeshi
Принадлежит: NATIONAL INSTITUTE FOR MATERIALS SCIENCE

Provided are a compound capable of becoming an organic transparent electrode, etc. One aspect of the present invention relates to an organic transparent electrode, which is configured from an organic molecule having a Brønsted acid functional group, electron-donating properties, and a π-conjugated plane, characterized by being self-assembled. Another aspect of the present invention relates to the organic transparent electrode characterized in that the Brønsted acid functional group is one member selected from among a carboxylic acid functional group, a sulfonic acid functional group, a phosphonic acid functional group and a thiophosphonic acid functional group. 138-. (canceled)39. An organic transparent electrode formed from an organic molecule having a Brønsted acid functional group , an electron-donating ability , and a π-conjugated plane , and being self-assembling.40. The organic transparent electrode according to claim 39 , wherein the Brønsted acid functional group is any of a carboxylic acid functional group claim 39 , a sulfonic acid functional group claim 39 , a phosphonic acid functional group claim 39 , and a thiophosphonic acid functional group.41. The organic transparent electrode according to claim 40 , wherein a hydrogen bond is formed to the Brønsted acid functional group in a self-assembled state.42. An organic transparent electrode formed from a compound that comprises a fused tetrathiafulvalene derivative moiety in a skeleton and has a protonic acid functional group.47. A method for producing an organic transparent electrode claim 40 , comprising recrystallizing from an organic solvent a fused sulfur-containing π compound to which a carboxylic acid functional group has been introduced.48. An organic transparent electrode wherein charges are not in equilibrium due to a ratio of a cation and an anion present in a hydrogen bond network not being 1:1 claim 40 , and a radical cation or a radical anion is generated to replenish a lost charge.49. A ...

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Номер записи: 75
07-01-2021 дата публикации

ANTHRADITHIOPHENE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND POLYMERS THAT CONTAIN THEM

Номер: US20210005817A1
Автор: Bianchi Gabriele, Nitti Andrea, Pasini Dario
Принадлежит:

An Anthradithiophene derivative having general formula (I): 2. The Anthradithiophene derivative having general formula (I) according to claim 1 , wherein in said general formula (I):Z, mutually identical, represent a sulfur atom;Y, mutually identical, represent an oxygen atom;{'sub': 1', '1', '30, 'R, mutually identical, represent a C-Calkoxy group;'}{'sub': '2', 'R, mutually identical, represent a hydrogen atom.'}4. A Process for the preparation of an anthradithiophene derivative having general formula (I) according to claim 3 , wherein:in said step (a) said halogenating agent is selected from bromine, iodine, chlorine, fluorine, and/orin said step (a) said dihalogenated aryl compound having general formula (II) and said halogenating agent, are used in molar ratios ranging from 1:2 to 1:10; and/orin said step (a) said ultraviolet radiations have a wavelength ranging from 200 nm to 500 nm; and/or{'sub': 3', '2', '2', '4, 'said step (a) is carried out in the presence of at least one halogenated organic solvent, said halogenated organic solvent being selected from chloroform (CHCl), dichloromethane (CHCl), carbon tetrachloride (CCl), or mixtures thereof; and/or'}in said step (a) said dihalogenated aryl compound having general formula (II) is used in said halogenated organic solvent at a molar concentration ranging from 0.05 mmol/ml to 2 mmol/ml; and/orsaid step (a) is carried out at a temperature ranging from 40° C. to 130° C.; and/orsaid step (a) is carried out for a time ranging from 30 minutes to 12 hours; and/or{'sub': '3', 'in said step (b) said silver-based oxidizing agent is selected from silver(I)-nitrate (AgNO), silver(I)chloride (AgCl); and/or'}in said step (b) said compound having general formula (III) and said oxidizing agent are used in molar ratios ranging from 1:3 to 1:20; and/or{'sub': 2', '3', '3, 'said step (b) is carried out in the presence of at least one protic or aprotic organic solvent, said protic organic solvent being selected from water (HO), ...

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Номер записи: 76
20-01-2022 дата публикации

CRYSTALLINE FORMS OF A MCL-1 INHIBITOR, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Номер: US20220017533A1
Автор: AUVRAY Julien, DE BAETS Emilie, LEBLANC Nicolas, Lynch Michael
Принадлежит:

Crystalline forms of Compound A: 131-. (canceled)32. A crystalline Form M of 2-{[5-{3-Chloro-2-methyl-4-[2-(4-methylpiperazine-1-yl) ethoxy]phenyl}-6-(4-fluorophenyl)thieno[2 ,3-d]pyrimidin-4-yl]oxy}-3-(2-{[2-(2-methoxyphenyl)pyrimidin-4-yl]methoxy}phenyl)propanoic acid (Compound A).33. The crystalline Form M of Compound A according to in substantially pure form.34. The crystalline Form M of Compound A according to claim 32 , having an X-ray powder diffraction diagram which exhibits at least the following diffraction lines (Bragg's angle 2 theta claim 32 , expressed in degrees±0.2°) 8.94 and 18.24.35. The crystalline Form M of Compound A according to claim 32 , having an X-ray powder diffraction diagram which exhibits at least 4 claim 32 , 5 claim 32 , 6 claim 32 , 7 claim 32 , 8 claim 32 , 9 claim 32 , 10 claim 32 , 11 claim 32 , 12 claim 32 , 13 claim 32 , 14 or all of the following diffraction lines (Bragg's angle 2 theta claim 32 , expressed in degrees±0.2°): 6.27; 8.94; 9.09; 12.16; 13.67; 14.75; 15.06; 16.97; 17.22; 17.44; 18.24; 19.16; 19.93; 20.91; and 25.88.36. The crystalline Form M of Compound A according to claim 35 , having an X-ray powder diffraction diagram which exhibits the following diffraction lines (Bragg's angle 2 theta claim 35 , expressed in degrees±0.2°); 8.94; 13.67; 14.75; 17.22; and 18.24.37. The crystalline Form M of Compound A according to claim 35 , having an X-ray powder diffraction diagram which exhibits the following diffraction lines (Bragg's angle 2 theta claim 35 , expressed in degrees±0.2°); 6.27; 8.94; 9.09; 12.16; 13.67; 14.75; 15.06; 16.97; 17.22; 17.44; 18.24; 19.16; 19.93; 20.91; and 25.88.39. The crystalline Form M of Compound A according to claim 32 , having a solid-state C CP/MAS NMR spectrum which exhibits the following peaks (expressed in ppm±0.2 ppm): 175.1 claim 32 , 153.7 claim 32 , 134.8 claim 32 , 108.9 claim 32 , 71.4 and 35.1.40. The crystalline Form M of Compound A according to claim 32 , having a solid-state C ...

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Номер записи: 77
12-01-2017 дата публикации

NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA

Номер: US20170008903A9
Автор: FRUTOS Rogelio P., KIM Soojin, MULDER Jason Alan, NICKOLAUS Peter, PATEL Nitinchandra D., POUZET Pascale A.J., SENANAYAKE Chris Hugh, TAMPONE Thomas Gabriel, WEI Xudong, WERTHMANN Ulrike, YANG Bing-Shiou
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Piperidino-dihydrothienopyrimidine sulfoxides of formula I 2. The method of claim 1 , wherein R is Cl and is located in the para-position of Ring A.3. The method of claim 1 , wherein Ring A is phenyl claim 1 , pyridinyl claim 1 , or pyrimidinyl.6. The method of claim 1 , wherein S* is in the R-configuration.7. The method of claim 2 , wherein S* is in the R-configuration.8. The method of claim 4 , wherein S* is in the R-configuration.9. The method of claim 5 , wherein S* is in the R-configuration.10. The method of claim 1 , wherein S* is in the S-configuration.11. The method of claim 2 , wherein S* is in the S-configuration.12. The method of claim 4 , wherein S* is in the S-configuration.13. The method of claim 5 , wherein S* is in the S-configuration.14. The method of claim 5 , wherein the compound of formula I shows a reflex peak in the X-ray powder diffraction diagram with a d-value of 4.62 Å.15. The method of claim 5 , wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 5 , 6.82 Å claim 5 , and 10.09 Å.16. The method of claim 5 , wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 5 , 4.17 Å claim 5 , and 3.66 Å.17. The method of claim 5 , wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 5 , 6.82 Å claim 5 , 10.09 Å claim 5 , 3.93 Å claim 5 , and 4.94 Å.18. The method of claim 5 , wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 5 , 4.17 Å claim 5 , 3.66 Å claim 5 , 3.73 Å claim 5 , and 18.47 Å.19. The method of claim 5 , wherein the compound of formula I shows a reflex peak in the X-ray powder diffraction diagram with a d-value of 4.12 Å.20. The method of claim 5 , wherein the compound of formula I shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.12 ...

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Номер записи: 78
14-01-2016 дата публикации

Bicyclic and Tricyclic Pyrimidine Tyrosine Kinase Inhibitors with Antitubulin Activity and Methods of Treating a Patient

Номер: US20160009731A1
Автор: Gangjee Aleem
Принадлежит:

Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed. 2. (canceled)4. The pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.613.-. (canceled)16. A pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.18139.-. (canceled)142. A pharmaceutical composition according to comprising at least one pharmaceutically acceptable carrier.143145.-. (canceled) This divisional utility patent application claims the benefit of co-pending U.S. patent application Ser. No. 13/364,930, filed on Feb. 2, 2012, which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/439,470, filed Feb. 4, 2011. The entire contents of U.S. patent application Ser. No. 13/364,930 and U.S. Provisional Patent Application Ser. No. 61/439,470 are incorporated by reference into this divisional utility patent application.1. Field of the InventionThe present invention relates to bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity. The compositions of this invention have dual activity of potent vascular endothelial growth factor receptor inhibitory activity along with cytotoxic activity in a single agent. The compositions of this invention may be made into salts that are water soluble for providing orally active antiangiogenic agents. Methods of using these compositions for treating a patient are also provided.2. Description of the Background ArtAntitubulin agents are some of the most successful ...

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Номер записи: 79
08-01-2015 дата публикации

METHOD FOR PREPARING D-BIOTIN

Номер: US20150011777A1
Автор: DING WENZHEN, GU LIXIN, HE YIMIN, PAN YAJIN, Pi Shiqing, WEI ANGFENG
Принадлежит:

Abstract The invention discloses a D-biotin preparation method. In the prior art, with a synthesis method utilizing malonic acid diester as raw materials, impurities are also produced along with the obtained D-biotin. The D-biotin preparation method is characterized in that with the presence of dimethyl sulfoxide and inorganic base as catalysts, methane tricarboxylic acid trialkyl ester and (3aR, 8aS, 8bS)-1,3-dibenzyl-2-oxo-10H-iminazole [3,4-d] thiophene [1,2-a] sulfuryl halide are subjected to condensation reaction in methylbenzene solvent to obtain intermediate (3 aS,4S,6aR)- 1,3 -dibenzyl-4-(ω,ω,ω-3-methoxycarbonylbutyl)-4H- 1H-thiophene[3,4-d]iminazol e-2,4(1H)-ketone, and the D-biotin is obtained after the intermediate is treated by the aftertreatment method. By the D-biotin preparation method, production of the impurities is avoided, quality of the biotin is greatly improved on the existing basis, and side reaction is avoided too. 2. The D-biotin preparation method of is characterized in that the chemical formula of the methane tricarboxylic acid trialkyl ester is CH(COOR) claim 1 , wherein the R is the alkyl group comprising 1-5 carbon atoms claim 1 , and the Rs on the three carboxylic acid groups are same or different alkyl groups.3. The D-biotin preparation method of is characterized in that the R in the chemical formula of the methane tricarboxylic acid trialkyl ester is methyl.4. The D-biotin preparation method of is characterized in that the R in the chemical formula of the methane tricarboxylic acid trialkyl ester is ethyl.5. The improved D-biotin preparation method of is characterized in that the inorganic base is sodium hydride or potassium hydride.6. The D-biotin preparation method of is characterized by including specific steps of 1) suspending the sodium hydride or potassium hydride in the methylbenzene and dripping the dimethyl sulfoxide as the catalyst at the room temperature to obtain mixture; 2) dripping the methylbenzene solvent of the ...

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Номер записи: 80
09-01-2020 дата публикации

HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME

Номер: US20200010476A1
Автор: CHO Seong Mi, HEO Dong Uk, JUNG Min Woo, Lee Dong Hoon, LEE Jung Ha, Park Tae Yoon
Принадлежит:

Disclosed are a heterocyclic compound represented by Formula 1 and an organic light emitting device using the same. The heterocyclic compound is used as a material for hole injection layer, hole transport layer, hole injection and transport layer, light emission layer, electron transport layer, or electron injection layer of the organic light emitting device and provides improved efficiency, low driving voltage, and improved lifetime characteristic. 6. The compound of claim 1 , wherein Ris hydrogen or a substituted or unsubstituted Calkyl.11. An organic light emitting device comprising: a first electrode; a second electrode provided to face the first electrode; and at least one layer of an organic material layer provided between the first electrode and the second electrode claim 1 , wherein the at least one layer of the organic material layer includes the compound according to .12. The organic light emitting device of claim 11 , wherein the organic material layer including said compound is a light emitting layer.13. The organic light emitting device of claim 12 , wherein the compound is a host material in the light emitting layer.14. The organic light emitting device of claim 13 , wherein the light emitting layer further includes a dopant material.15. The organic light emitting device of claim 11 , wherein the organic material layer including said compound is an electron injection layer; an electron transport layer claim 11 , or a layer simultaneously performing electron injection and electron transport. This application is a National Phase entry pursuant to 35 U.S.C. § 371 of PCT/KR2018/008233 filed on Jul. 20, 2018, and claims priority to and the benefit of Korean Patent Application No. 10-2017-0092174 filed on Jul. 20, 2017 and Korean Patent Application No. 10-2018-0084348 filed on Jul. 19, 2018 with the Korean Intellectual Property Office, the disclosures of which are incorporated herein by reference in their entirety.The present disclosure relates to a novel ...

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Номер записи: 81
14-01-2016 дата публикации

Light-Emitting Element, Compound, Display Module, Lighting Module, Light-Emitting Device, Display Device, Lighting Device, and Electronic Device

Номер: US20160013421A1
Автор: HAMADA Takao, Inoue Hideko, Kanamoto Miki, Takahashi Tatsuyoshi
Принадлежит: SEMICONDUCTOR ENERGY LABORATORY CO., LTD.

A light-emitting element with high emission efficiency is provided. In addition, a light-emitting element having a low driving voltage is provided. Furthermore, a novel compound which can be used for a transport layer, a host material, or a light-emitting material of a light-emitting element is provided. A novel compound including a benzothienopyrimidine skeleton is provided. Furthermore, a light-emitting element including a pair of electrodes and an EL layer sandwiched between the pair of electrodes is provided. The EL layer contains a substance including the benzothienopyrimidine skeleton. 1. A light-emitting element comprising:a pair of electrodes; andan EL layer provided between the pair of electrodes,wherein the EL layer comprises a substance including a benzothienopyrimidine skeleton.2. The light-emitting element according to claim 1 ,wherein the EL layer comprises a layer comprising the substance including the benzothienopyrimidine skeleton, andwherein the layer comprises an iridium complex.3. The light-emitting element according to claim 1 , wherein the benzothienopyrimidine skeleton is a benzothieno[3 claim 1 ,2-d]pyrimidine skeleton.8. The light-emitting element according to claim 6 , wherein the both Rand Rrepresent hydrogen.9. The light-emitting element according to claim 6 , wherein Rto Reach represent hydrogen.10. A light-emitting device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the light-emitting element according to ; and'}a unit for controlling the light-emitting element.11. A display device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the light-emitting element according to in a display portion; and'}a unit for controlling the light-emitting element.12. A lighting device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the light-emitting element according to in a lighting portion; and'}a unit for controlling the light-emitting element.13. An electronic device comprising the light-emitting element ...

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Номер записи: 82
14-01-2016 дата публикации

Novel Condensed Polycyclic Aromatic Compound And Use Thereof

Номер: US20160013428A1
Автор: Hamada Masahiro, Sadamitsu Yuichi, Shinamura Shoji, Takimiya Kazuo
Принадлежит:

[Problem] To provide: a novel compound which has high mobility and on/off ratio and is useful for organic electronic devices; and a method for producing the compound. 2. The condensed polycyclic aromatic compound according to claim 1 , wherein Xand Xare sulfur atoms.3. The condensed polycyclic aromatic compound according to claim 1 , wherein Rand Rare hydrogen atoms.4. The condensed polycyclic aromatic compound according to claim 1 , wherein Rand Rare each an aliphatic hydrocarbon group having 1 to 30 carbon atoms.5. The condensed polycyclic aromatic compound according to claim 4 , wherein Rand Rare each a straight-chain or branched-chain alkyl group having 1 to 30 carbon atoms.6. An organic semiconductor material comprising the condensed polycyclic aromatic compound according to any one of to .7. The organic semiconductor material according to claim 6 , wherein the organic semiconductor material is a transistor material.8. A composition for forming a thin film comprising the condensed polycyclic aromatic compound according to any one of to claim 6 , and an organic solvent.9. The composition for forming a thin film according to claim 8 , wherein the content of the condensed polycyclic aromatic compound is in the range of 0.01 part by weight or higher and 10 parts by weight or lower relative to 100 parts by weight of the organic solvent.105. A thin film comprising the condensed polycyclic aromatic compound according to any one of to .11. An organic semiconductor device comprising the thin film according to .12. The organic semiconductor device according to claim 11 , wherein the device is an organic transistor device.13. A method for producing an organic semiconductor device claim 8 , comprising a step of applying the composition for forming a thin film according to onto a substrate by a solution process.14. A method for producing an organic semiconductor device claim 9 , comprising a step of applying the composition for forming a thin film according to onto a ...

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Номер записи: 83
19-01-2017 дата публикации

NEW TRICYCLIC QUINONE DERIVATIVE

Номер: US20170015677A1
Автор: Ban Hitoshi, FURUTA Tomoyuki, KAMIOKA Seiji, KITANO Hiroyuki, LI Chiang Jia, RI Shoukou
Принадлежит: Boston Biomedical, Inc.

This invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. Specifically, the present invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof [Therein, A is O, S, or N—R; ring G is a 5-membered or 6-membered aromatic ring, etc., including 1-3 heteroatoms selected from O, S and N as constituent atoms; Rand Rare each independently a hydrogen atom, a halogen atom, or an optionally-substituted Calkyl carbonyl group, etc.; R, Rand Rare each independently a hydrogen atom, a halogen atom, or an optionally-substituted Calkyl carbonyl group, etc.; and Ris a hydrogen atom or an optionally-substituted Calkyl group, etc.]. 2. The compound of or a pharmacologically acceptable salt thereof claim 1 , wherein A is S.3. The compound of or a pharmacologically acceptable salt thereof claim 1 , wherein A is O.4. The compound of or a pharmacologically acceptable salt thereof claim 1 , wherein A is N—R.8. The compound of or a pharmacologically acceptable salt thereof claim 1 , wherein Ris chosen from:1: a hydrogen atom;2: a cyano group;{'sub': 1-6', '1-6', '3-10', '6-10, '3: a Calkyl group optionally substituted with one to three groups chosen from a fluorine atom, an hydroxyl group, a Calkoxy group, a Ccycloalkyl group, a Caryl group, and a 3- to 8-membered cyclic amino group;'}{'sub': 1-6', '1-6', '1-6', '3-10', '6-10', '1-6, '4: a Calkylcarbonyl group, wherein the alkyl group is optionally substituted with one to three groups chosen from a halogen atom, an hydroxyl group, an amino group optionally substituted with one or two Calkyl groups, a Calkoxy group, a Ccycloalkyl group, a Caryl group, and a 5- to 12-membered monocyclic or polycyclic heterocycle group optionally substituted with one to three Calkyl groups;'}{'sub': 6-10', '1-6', '1-6, '5: a Caryl group optionally substituted with one to three groups chosen from a halogen atom, an hydroxyl group, a Calkyl group, and a Calkoxy group ...

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Номер записи: 84
16-01-2020 дата публикации

N3-CYCLICALLY SUBSTITUTED THIENOURACILS AND USE THEREOF

Номер: US20200016159A1
Автор: Cancho Grande Yolanda, Delbeck Martina, HAERTER Michael, KALTHOF Bernd, Kosemund Dirk, LUSTIG Klemens, SUESSMEIER Frank
Принадлежит:

The present application relates to novel thieno[2,3-d]pyrimidine-2,4-dione (“thienouracil”) derivatives having cyclic substituents in the 3 position, to processes for the preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of pulmonary and cardiovascular disorders and of cancer. 7. The compound as defined in for treatment and/or prevention of one or more diseases.8. The compound as defined in for use in a method for treatment and/or prevention of idiopathic pulmonary fibrosis claim 1 , pulmonary hypertension claim 1 , Bronchiolitis obliterans syndrome claim 1 , chronic-obstructive pulmonary disease claim 1 , asthma claim 1 , cystic fibrosis claim 1 , myocardial infarction claim 1 , heart failure claim 1 , sickle cell anaemia and/or cancer.9. A product comprising a compound as defined in for production of a medicament for treatment and/or prevention of idiopathic pulmonary fibrosis claim 1 , pulmonary hypertension claim 1 , Bronchiolitis obliterans syndrome claim 1 , chronic-obstructive pulmonary disease claim 1 , asthma claim 1 , cystic fibrosis claim 1 , myocardial infarction claim 1 , heart failure claim 1 , sickle cell anaemia and/or cancer.10. Medicament comprising a compound as defined in in combination with one or more inert claim 1 , nontoxic claim 1 , pharmaceutically suitable excipients.11. Medicament comprising a compound as defined in in combination with one or more further active ingredients selected from the group consisting of PDE 5 inhibitors claim 1 , sGC activators claim 1 , sGC stimulators claim 1 , prostacyclin analogues claim 1 , IP receptor agonists claim 1 , endothelin antagonists claim 1 , antifibrotic agents claim 1 , antiinflammatory claim 1 , immunomodulating claim 1 , immunosuppressive and/or cytotoxic agents and/or compounds that inhibit the ...

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Номер записи: 85
21-01-2021 дата публикации

PROTEASE INHIBITORS

Номер: US20210017140A1
Автор: Grabowska Urszula, Kahnberg Pia, NILSSON MAGNUS, ODEN Lourdes Salvador, Samuelsson Bertil
Принадлежит:

Compounds of the formula II: 112.-. (canceled)1422. The compound according to claim , comprising the N-Boc and dimethylacetal protecting groups depicted in Formula Ih′″. This application is a Continuation of pending application Ser. No. 16/449,850 filed on Jun. 24, 2019, which is a Continuation of application Ser. No. 15/667,292 filed on Aug. 2, 2017, now U.S. Pat. No. 10,329,266, which is a Continuation of abandoned application Ser. No. 15/247,804 filed on Aug. 25, 2016, which is a Continuation of Ser. No. 14/940,817 filed on Nov. 13, 2015, now U.S. Pat. No. 9,428,517, which is a Divisional of application Ser. No. 14/249,332 filed on Apr. 9, 2014, now U.S. Pat. No. 9,200,006, which is a Continuation of Ser. No. 13/831,267 filed on Mar. 14, 2013, now U.S. Pat. No. 8,735,395, which is a Continuation of Ser. No. 13/541,519 filed on Jul. 3, 2012, now U.S. Pat. No. 8,426,421, which is a Divisional of application Ser. No. 12/739,489 filed on Oct. 26, 2010, now U.S. Pat. No. 8,242,119 and for which priority is claimed under 35 U.S.C. § 120. Application Ser. No. 12/739,489 is the National Phase of PCT International Application No. PCT/EP2009/062406 filed on Sep. 24, 2009 under 35 U.S.C. § 371. This application also claims priority of Application No. 0817424.5 filed in Great Britain on Sep. 24, 2008 under 35 U.S.C. § 119. The entire contents of each of the above-identified applications are hereby incorporated by reference in their entirety.This invention relates to inhibitors of cysteine proteases, especially those of the papain superfamily. The invention provides novel compounds useful in the prophylaxis or treatment of disorders stemming from misbalance of physiological proteases such as cathepsin K.The papain superfamily of cysteine proteases is widely distributed in diverse species including mammals, invertebrates, protozoa, plants and bacteria. A number of mammalian cathepsin enzymes, including cathepsins B, F, H, K, L, O and S, have been ascribed to this superfamily, ...

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Номер записи: 86
21-01-2021 дата публикации

SOLID STATE FORMS OF RELUGOLIX

Номер: US20210017188A1
Автор: Gabriel Roman, JEGOROV Alexandr, Kantor Hana, Kolesa Pavel
Принадлежит:

The present disclosure provides solid state forms of Relugolix, crystalline forms of Relugolix, pharmaceutical compositions thereof, and pharmaceutical formulations thereof. Methods for producing these forms of Relugolix, pharmaceutical compositions, and pharmaceutical formulations are also provided. 1. Crystalline Form F of Relugolix , characterized by data selected from one or more of the following:{'figref': [{'@idref': 'DRAWINGS', 'FIG. 1'}, {'@idref': 'DRAWINGS', 'FIG. 7'}], 'a. an X-ray powder diffraction pattern substantially as depicted in or in ;'}b. an X-ray powder diffraction pattern having peaks at 6.9, 7.5, 9.5, 13.9 and 18.1 degrees 2-theta±0.2 degrees 2-theta;{'sup': −1', '−1, 'c. an FT-IR spectrum having peaks at 1720, 1680, 1626, 1595, 1528, 1460, 1412, 1313, 1237 and 1095 cm±4 cm;'}{'figref': {'@idref': 'DRAWINGS', 'i': 'a', 'FIG. 6'}, 'b': '6', 'i': 'b', 'd. an FT-IR spectrum as depicted in and/or ; and'}e. combinations of these data.2. The crystalline Form F of Relugolix according to claim 1 , characterized by an X-ray powder diffraction pattern having peaks at 6.9 claim 1 , 7.5 claim 1 , 9.5 claim 1 , 13.9 and 18.1 degrees 2-theta±0.2 degrees 2-theta claim 1 , and also having any one claim 1 , two claim 1 , three claim 1 , four or five additional peaks selected from the group consisting of 10.2 claim 1 , 12.9 claim 1 , 19.1 claim 1 , 21.1 and 23.2 degrees 2-theta±0.2 degrees 2-theta.3. The crystalline Form F of Relugolix according to claim 1 , characterized by an FT-IR spectrum having peaks at 3477 claim 1 , 3298 claim 1 , 3223 claim 1 , 3069 claim 1 , 2991 claim 1 , 2952 claim 1 , 2862 claim 1 , 2827 claim 1 , 2782 claim 1 , 1720 claim 1 , 1680 claim 1 , 1626 claim 1 , 1595 claim 1 , 1528 claim 1 , 1460 claim 1 , 1412 claim 1 , 1384 claim 1 , 1350 claim 1 , 1313 claim 1 , 1237 claim 1 , 1212 claim 1 , 1180 claim 1 , 1149 claim 1 , 1113 claim 1 , 1095 claim 1 , 1032 claim 1 , 1014 claim 1 , 973 claim 1 , 936 claim 1 , 836 claim 1 , 808 claim 1 , ...

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Номер записи: 87
16-01-2020 дата публикации

Thienopyridine Carboxamides as Ubiquitin-Specific Protease Inhibitors

Номер: US20200017525A1
Автор: Bair Kenneth W., CARAVELLA Justin A., Guerin David Joseph, Ioannidis, JR. David R., Jr. Stephanos, Lancia, LI Hongbin, MISCHKE Steven, Ng Pui Yee, RICHARD David, Schiller Shawn E.R., SHELEKHIN Tatiana, Wang Zhongguo
Принадлежит:

The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: 149.-. (canceled)51. The compound of claim 50 , wherein Ris (C-C) alkyl claim 50 , Ris H or (C-C) alkyl claim 50 , or Rand Rtogether form a (C-C) cycloalkyl optionally substituted with one or more R; and Ris H.53. The compound of claim 50 , wherein R claim 50 , R claim 50 , and R are each independently chosen from H or (C-C) alkyl.54. The compound of claim 50 , wherein Rand Rare each independently chosen from H or CH claim 50 , and R is H.55. The compound of claim 50 , wherein Ris —(C-C) alkylene-heterocycloalkyl claim 50 , wherein the heterocycloalkyl is optionally substituted with one or more R.56. The compound of claim 50 , wherein X is CH.57. The compound of claim 52 , wherein Ris (C-C) alkyl claim 52 , Ris H or (C-C) alkyl claim 52 , or Rand Rtogether form a (C-C) cycloalkyl optionally substituted with one or more R; Ris H; R claim 52 , R claim 52 , and R are each independently chosen from H or (C-C) alkyl; and Ris —(C-C) alkylene-heterocycloalkyl claim 52 , wherein the heterocycloalkyl is optionally substituted with one or more R.58. The compound of claim 57 , wherein Ris CH claim 57 , Ris H; Ris H; R claim 57 , R claim 57 , and R are each independently chosen from H or CH; and Ris —(C-C) alkylene-heterocycloalkyl claim 57 , wherein the heterocycloalkyl is optionally substituted with one or more R.59. The compound of claim 58 , wherein R claim 58 , R claim 58 , and R are each H.60. The compound of claim 58 , wherein Ris piperazinyl ring.61. The compound of claim 52 , wherein Rand Rtogether form a (C-C) cycloalkyl optionally substituted with one or more R claim 52 , wherein Ris independently at each occurrence (C-C) alkyl claim 52 , halogen claim 52 , or —OH; Ris H; R claim 52 , R claim 52 , and R are each independently chosen from H or (C-C) alkyl; and Ris —(C) alkylene-heterocycloalkyl. ...

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Номер записи: 88
16-01-2020 дата публикации

METHODS TO ASSESS BINDING AGENT SPECIFICITY

Номер: US20200018763A1
Автор: INNGJERDINGEN Marit, LUND-JOHANSEN Fridtjof, MEHTA Adi, SIKORSKI Krzsysztof
Принадлежит:

The present invention relates to methods for assessing binding agent specificity, in particular antibody specificity. The present invention thus provides a method of analysing a mixture of polypeptides comprising the steps of: (i) separating the polypeptides in the mixture into a plurality of fractions; (ii) contacting a first aliquot of two or more of the fractions with a plurality of different binding agents attached to one or more solid supports and detecting the binding of the polypeptides to the binding agents in each fraction; (iii) assessing the amino acid composition of the polypeptides in a second aliquot of said fractions by mass spectrometry; and (iv) correlating the binding results detected in step (ii) and the mass spectrometry results from step (iii) to assess the specificity of the binding agents for a polypeptide of interest. 1. A method of analysing a mixture of polypeptides comprising the steps of:(i) separating the polypeptides in the mixture into a plurality of fractions;(ii) contacting a first aliquot of two or more of the fractions with a plurality of different binding agents attached to one or more solid supports and detecting the binding of the polypeptides to the binding agents in each fraction;(iii) assessing the amino acid composition of the polypeptides in a second aliquot of said fractions by mass spectrometry; and(iv) correlating the binding results detected in step (ii) and the mass spectrometry results from step (iii) to assess the specificity of the binding agents for a polypeptide of interest.2. The method of further comprising the steps of:(v) determining one or more fractions which are enriched for a particular polypeptide of interest;(vi) contacting the one or more fractions with a binding agent to said polypeptide of interest attached to one or more solid supports;(vii) disrupting the binding agents of step (vi) from the associated polypeptides; and(viii) contacting the released polypeptides with a plurality of binding agents ...

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Номер записи: 89
17-01-2019 дата публикации

COMPOUND FOR PHOTOACTIVE ORGANIC ELECTRONIC COMPONENTS AND PHOTOACTIVE ORGANIC ELECTRONIC COMPONENT CONTAINING THE COMPOUND

Номер: US20190019957A1
Автор: "DSOUZA Daniel", Fitzner Roland, Gerdes Olga, Hildebrandt Dirk, Mattersteig Gunter, Weiss André
Принадлежит:

A compound and method of producing the compound of formula (I) that has high absorption in the short wavelength spectral region of visible light and is capable of being used for an organic electronic component. 2. The compound as claimed in claim 1 , wherein exactly one of the three coefficients o claim 1 , p and q is 1 claim 1 , while the two other coefficients are 0.5. The compound as claimed in wherein the Rand Rradicals are each CN.6. The compound as claimed in claim 3 , wherein the Rto Rand Rand Rradicals are each independently selected from the group of the following radicals: H claim 3 , F claim 3 , linear or branched C-C-alkyl claim 3 , and wherein hydrogens in the alkyl may each independently be replaced by fluorine atoms.9. The compound as claimed in with X=oxygen.11. The compound as claimed in claim 1 ,{'sup': 'a', 'wherein Y, Y′, Z and Z′ are each independently selected from: N or CR, and'}{'sup': 'a', 'sub': 1', '5', '1', '5', '2', '5', '2', '5', '2', '5', '2', '5, 'wherein Ris selected from the group of the following radicals: H, F, C-C-alkyl, C-C—O-alkyl, C-C-alkenyl, C-C—O-alkenyl, C-C—S-alkenyl, C-C-alkynyl, phenyl, wherein hydrogen atoms in the alkyl, O-alkyl, S-alkyl, alkenyl, O-alkenyl, S-alkenyl, alkynyl and phenyl radicals may each independently be substituted.'}12. The compound as claimed in claim 1 , wherein Y claim 1 , Y′ claim 1 , Z claim 1 , Z′ are each independently selected from: N claim 1 , CH claim 1 , C—F claim 1 , C—CH claim 1 , C—CF claim 1 , C—CH claim 1 , C—CH claim 1 , C—OCH claim 1 , C—OCH claim 1 , C—SCH claim 1 , C—SCH.13. The compound as claimed in claim 1 , wherein Y claim 1 , Y′ claim 1 , Z claim 1 , Z′ are each CH.16. The compound as claimed in claim 1 , wherein X″=S.23. The A method of using one or more of the compounds as claimed in in a photoactive organic electronic component.24. The method of use as claimed in claim 23 , wherein the component is an organic solar cell.25. A photoactive organic electronic component ...

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Номер записи: 90
28-01-2016 дата публикации

THIENO[3,2-d]PYRIMIDINE, FURO[3,2-d]PYRIMIDINE, AND PYRROLO[3,2-D]PYRIMIDINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS

Номер: US20160024107A1
Автор: "Clarke Michael ONeil Hanrahan", Mackman Richard L., Siegel Dustin
Принадлежит:

Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds. 2. A compound of wherein X is S claim 1 , or a pharmaceutically acceptable salt thereof.3. A compound of claim 1 , wherein Ris selected from the group of CN claim 1 , OR claim 1 , C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , —CH—O—C-Calkyl claim 1 , —CH—S—C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , azido claim 1 , halogen claim 1 , C-Cchloroalkyl claim 1 , C-Cbromoalkyl claim 1 , and C-Cfluoroalkyl; or a pharmaceutically acceptable salt thereof.4. A compound of claim 1 , wherein Ris selected from the group of H claim 1 , CH claim 1 , F claim 1 , Cl claim 1 , and NH; Ris selected from the group of OH claim 1 , F claim 1 , Cl claim 1 , N claim 1 , NH claim 1 , and CN; and Ris selected from the group of CN claim 1 , N claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , vinyl claim 1 , propenyl claim 1 , ethynyl claim 1 , CHF claim 1 , CHF claim 1 , CHCl claim 1 , CHSMe claim 1 , and CHOMe; or a pharmaceutically acceptable salt thereof.8. A compound of wherein X is S claim 7 , or a pharmaceutically acceptable salt thereof.10. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris H.11. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris F12. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris F.13. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris Cl.14. A compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein Ris N.15. A compound of claim 9 , or a ...

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Номер записи: 91
26-01-2017 дата публикации

Compounds for Eradicating or Inhibiting Proliferation of Cancer Stem Cells

Номер: US20170022215A1
Автор: Athavale Maithili, More Gayatri, Shukre Kedar, Srivastava Sangeeta
Принадлежит:

The present invention provides compounds of formula (I), compositions, uses thereof and methods for eradicating or inhibiting proliferation of cancer stem cells which includes killing; and/or inducing apoptosis in cancer stem cells. Included within the scope of such compounds, compositions, uses thereof and methods are those in which proliferation of cancer stem cells are selectively eradicated or inhibited. 514-. (canceled) The present invention relates to compounds for eradicating or inhibiting proliferation of cancer stem cells and uses thereof in eradicating or inhibiting proliferation of cancer stem cells. The present invention also relates to a method of eradicating or inhibiting proliferation of cancer stem cells.Cancer is considered to be the most dreadful disease until today and recurrence or relapse of cancer still remains challenging with the most of the conventional cancer therapies. Radiotherapy is believed to reduce the rate of recurrence to some extent, but it also damages the normal rapidly dividing cells in the area being treated and has never been found to increase overall survival but rather increase mortality. It is also known that though many types of cancer can initially be targeted with chemotherapy using currently available drugs. However, often resistance to treatment with such a drug can occur and recurrence or relapse of cancer is common.In recent years, a new model for genesis of cancer has gained wide acceptance, it is hypothesized that only a small fraction of cells of the entire tumor mass are responsible for the tumorigenic activities within the tumor. This small fraction of tumorigenic cells, according to the new model, are transformed cells with stem-cell-like qualities and are called “cancer stem cells” (CSCs). In 1990s in vivo presence of CSCs in acute myeloid leukemia (AML) was demonstrated. Later, these CSCs were shown to have the same cellular markers, CD34/CD38″, as that of hematopoietic stem cells. Since then, researchers ...

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Номер записи: 92
17-04-2014 дата публикации

HETEROCYCLE-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES

Номер: US20140107103A1
Автор: ANDERSKEWITZ Ralf, DOLLINGER Horst, Fiegen Dennis, Fox Thomas, GOEGGEL Rolf, HOENKE Christoph, Klinder Klaus, MARTYRES Domnic, NICKOLAUS Peter, Pouzet Pascale
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Dihydrothienopyrimidinesulphoxides of formula 1 5. The method according to claim 1 , wherein in the compound of formula 1:{'sup': '4', 'Ris methyl, ethyl, propyl, or isopropyl,'}and the pharmacologically acceptable salts thereof.20. The method according to claim 19 , wherein the disease is chronic obstructive pulmonary disease (COPD) claim 19 , chronic sinusitis claim 19 , asthma claim 19 , alpha1-antitrypsin deficiency claim 19 , rheumatoid arthritis claim 19 , Crohn's disease claim 19 , and ulcerative colitis.23. The method according to claim 22 , wherein the disease is depression claim 22 , schizophrenia claim 22 , Alzheimer's disease claim 22 , Parkinson's disease claim 22 , acute multiple sclerosis claim 22 , or chronic multiple sclerosis. This application is divisional of U.S. Ser. No. 12/738,429, which is a 371 of International Application No. PCT/EP2008/063983, filed Oct. 16, 2008, which claims priority to European Patent Application No. 07118911.2, filed Oct. 19, 2007, the contents of which are incorporated herein by reference in their entirety.The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof,wherein X is SO or SO, but preferably SO, and wherein Rdenotes an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl and wherein Rand Rhave the meanings stated in claim , as well as pharmaceutical compositions which contain these compounds.These new dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.U.S. Pat. No. 3,318,881 and BE 663693 disclose the preparation of dihydrothieno[3,2-d]pyrimidines which have cardiovascular and sedative ...

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Номер записи: 93
17-04-2014 дата публикации

Thienyl- and Furanyl-Isoquinolinones and Methods for Using Them

Номер: US20140107117A1
Автор: GILBERT ADAM MATTHEW, Hansen Eric Christian, Larkin Peter John, Moroni Flavio, Pellicciari Roberto
Принадлежит:

The present invention relates to substituted thienyl- and furanyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders. 2. The method according to claim 1 , wherein{'sub': 1', '9', '2', '9', '2', '9, 'X is C-Calkylene, C-Calkenylene, or C-Calkynylene;'}Y is S or O;{'sup': '1', 'sub': 2', '1', '6', '1', '6, 'Ris halogen, hydroxy, NH, C-Calkoxy, CN, or C-Cperfluoroalkyl;'}{'sup': 2', '3', '4, 'sub': 2', '1', '6', '1', '6, 'R, R, and Rare each, independently, selected from hydrogen, halogen, hydroxy, NH, C-Calkoxy, CN, and C-Cperfluoroalkyl;'}{'sup': 5', '6, 'sub': 1', '6', '2', '4', '3', '7, 'Rand Rare each, independently, selected from hydrogen, C-Calkyl, C-Calkenyl, C-Ccycloalkyl, phenyl, and benzyl; or'}{'sup': 5', '6, 'Rand Rtogether with the nitrogen to which they are attached form a saturated, partially unsaturated, or unsaturated 3 to 12 membered monocyclic or bicyclic heterocyclic ring optionally comprising from one to three additional ring heteroatoms selected from N, O, and S, the remaining ring atoms are carbon atoms; and'}{'sup': '7', 'sub': 2', '1', '3', '1', '3', '2, 'Ris hydrogen, halogen, hydroxy, NH, C-Calkyl, C-Calkoxy or NO; or a pharmaceutically acceptable salt or zwitterionic form thereof.'}6. The method according to claim 5 , wherein Ris halogen or hydrogen.7. The method according to claim 6 , wherein Ris hydrogen.8. The method according to claim 1 , wherein Y is S.9. The method according to claim 1 , wherein Y is O.10. The method according to claim 1 , wherein Rand Rare each claim 1 , independently claim 1 , C-Calkyl.11. The method according to claim 1 , wherein Rand Rtogether with the nitrogen to which they are attached form a saturated monocyclic heterocyclic ring optionally comprising from one to three additional ring ...

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Номер записи: 94
25-01-2018 дата публикации

METHOD OF PRODUCING BENZO[1,2-B:4,5-B']DITHIOPHENE AND BENZOTHIADIAZOLE-BASED MOLECULAR COMPLEXES

Номер: US20180022717A1
Автор: Earmme Taeshik, Pan Hualong, Woody Kathy, Worfolk Brian
Принадлежит: Phillips 66 Company

A method of forming a molecular complex. The method proceeds by reacting 5-chloro-2,1,3-benzothiadiazole with N-bromosuccinimide to produce 4,7-dibromo-5-chlorobenzo[c][1,2,5]thiadiazole. 4,7-dibromo-5-chlorobenzo[c][1,2,5]thiadiazole is then reacted with trimethyl[4-(2-octyldodecyl)thiophen-2-yl]stannane to produce 5-chloro-4,7-bis(4-(2-octyldodecyl)thiophen-2-yl)benzo[c][1,2,5]thiadiazole. 4, 7-bis(5-bromo-4-(2-octyldodecyl)thiophen-2-yl)-5-chlorobenzo[c][1,2,5]thiadiazole is subsequently synthesized from 5-chloro-4,7-bis(4-(2-octyldodecyl)thiophen-2-yl)benzo[c][1,2,5]thiadiazole. 4,7-bis(5-bromo-4-(2-octyldodecyl)thiophen-2-yl)-5-chlorobenzo[c][1,2,5]thiadiazole with tributyl(thiophen-2-yl)stannane is then reacted to produce 4-bromo-5,6-difluoro-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole. This is followed by reacting 4,7-dibromo-5-chloro-2,1,3-benzothiadiazole with tributyl(thiophen-2-yl)stannane to produce 4-bromo-5-chloro-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole. trimethyl[4-(2-octyldodecyl)thiophen-2-yl]stannane is then reacted with and 4-bromo-5-chloro-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole to produce 5-chloro-4-(4-(2-octyldodecyl)thiophen-2-yl)-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole. 5-chloro-4-(4-(2-octyldodecyl)thiophen-2-yl)-7-(thiophen-2-yl)benzo[c][1,2,5]thiadiazole is then reacted with N-bromosuccinimide to produce the co-monomer 4-(5-bromo-4-(2-octyldodecyl)thiophen-2-yl)-7-(5-bromothiophen-2-yl)-5-chlorobenzo[c][1,2,5]thiadiazole. A 2. The method of claim 1 , wherein the molecular complex is used as photovoltaic material in one or more photovoltaic devices.3. The method of claim 2 , wherein the one or more photovoltaic devices are polymer solar cell devices or photodetector devices.4. The method of claim 1 , wherein the molecular complex is used as an active layer material in one or more electronic devices.5. The method of claim 4 , wherein the one or more electronic devices are field effect transistors claim 4 , light emitting devices ...

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Номер записи: 95
25-01-2018 дата публикации

UNSYMMETRICAL BENZOTHIADIAZOLE-BASED MOLECULAR COMPLEXES

Номер: US20180022718A1
Автор: Earmme Taeshik, Pan Hualong, Woody Kathy, Worfolk Brian
Принадлежит: Phillips 66 Company

A molecular complex comprising 2. The molecular complex of claim 1 , wherein the molecular complex is part of an oligomer.3. The molecular complex of claim 1 , wherein the molecular complex is part of a polymer with a molecular weight ranging from about 1 claim 1 ,000 to about 100 claim 1 ,000 kDa.5. The molecular complex of claim 1 , wherein the molecular complex is used as photovoltaic material in one or more photovoltaic devices.6. The molecular complex of claim 5 , wherein the one or more photovoltaic devices are polymer solar cell devices or photodetector devices.7. The molecular complex of claim 1 , wherein the molecular complex is used as an active layer material in one or more electronic devices.8. The molecular complex of claim 4 , wherein the one or more electronic devices are field effect transistors claim 4 , light emitting devices and sensors claim 4 , electrochromic devices and capacitors.9. The molecular complex of claim 1 , wherein when used as a photovoltaic polymer produces a power conversion efficiency greater than 7.0%.10. The molecular complex of claim 1 , wherein when used as a photovoltaic polymer produces a fill factor greater than 69%.11. The molecular complex of claim 1 , wherein R1 and R1′ are not identical.12. The molecular complex of claim 1 , wherein R2 and R2′ are not identical.13. The molecular complex of claim 1 , wherein both R1 and R1′ are not identical and R2 and R2′ are not identical. This application is a non-provisional application which claims the benefit of and priority to U.S. Provisional Application Ser. No. 62/364,088 filed Jul. 19, 2016, entitled “Unsymmetrical Benzothiadiazole-Based Molecular Complexes,” which is hereby incorporated by reference in its entirety.None.This invention relates to unsymmetrically substituted benzothiadiazole-based molecular complexes.Solar energy using photovoltaic effect requires active semiconducting materials to convert light into electricity. Currently, solar cells based on silicon are the ...

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Номер записи: 96
25-01-2018 дата публикации

BICYCLIC PYRIDINE COMPOUND

Номер: US20180022755A1
Автор: ENJO Kentaro, HIRAMOTO Masashi, INAGAKI Yusuke, ISHIHATA Akihiro, Kanai Akira, Kawaguchi Kenichi, TAKAMATSU Hajime
Принадлежит:

The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. 2: The compound or a salt thereof according to claim 1 , wherein Ris OH claim 1 , NH claim 1 , or —O-lower alkyl and Ris H.3: The compound or a salt thereof according to claim 2 , wherein X is O claim 2 , and a dotted line is a single bond or a double bond; or X is S claim 2 , and a dotted line is a double bond.4: The compound or a salt thereof according to claim 3 , wherein:{'sup': '1', 'Ris lower alkyl which optionally has one to four substituents selected from the group consisting of halogen, OH, and —O-lower alkyl; cycloalkyl which is optionally substituted by one to two lower alkyls; or -lower alkylene-(cycloalkyl which is optionally substituted by one to two lower alkyls);'}{'sup': 3', '3', '3', '3, 'Ris -lower alkylene-X-lower alkyl, -lower alkylene-X-lower alkylene-(cycloalkyl which is optionally substituted by one to two lower alkyls), -lower alkylene-(cycloalkyl which is optionally substituted by one to two lower alkyls), or -lower alkylene-X-(cycloalkyl which is optionally substituted by one to two lower alkyls); and'}{'sup': 2', '5, 'Rand Rare the same or different from each other, and are H or lower alkyl.'}5: The compound or a salt thereof according to claim 4 , wherein:{'sup': '1', 'Ris lower alkyl which optionally has one to four substituents selected from the group consisting of halogen and OH; cycloalkyl; or -lower alkylene-cycloalkyl; and'}{'sup': '3', 'sub': 'n', 'Ris -lower alkylene-S(O)-lower alkyl, -lower alkylene-O-lower alkylene-cycloalkyl, -lower alkylene-S-lower alkylene-cycloalkyl, -lower alkylene-cycloalkyl, or -lower alkylene-S-cycloalkyl.'}6: The compound or a salt thereof according to claim 5 , wherein Ris lower alkyl claim 5 , cycloalkyl claim 5 , or -lower alkylene-cycloalkyl; Ris -lower alkylene-S-lower alkyl claim 5 , -lower alkylene-O-lower ...

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Номер записи: 97
22-01-2015 дата публикации

IRAK INHIBITORS AND USES THEREOF

Номер: US20150025093A1
Автор: Corin Alan Franklin, FRYE Leah Lynn, Greenwood Jeremy Robert, Harriman Geraldine C., Masse Craig E., Robinson Shaughnessy, Romero Donna L., Shelley Mee, Watts Karl Shawn, Wessel Matthew David
Принадлежит: Nimbus Iris, Inc.

The present invention provides compounds, compositions thereof, and methods of using the same. 6. The compound of claim 3 , wherein n is 1 and Ris —N(CH).7. The compound of claim 3 , wherein n is 1 claim 3 , and Ris Cy.9. The compound of wherein L is —O—.10. The compound of wherein L is —N(R)—.11. The compound of wherein L is —NH—.12. The compound of wherein L is —S—.14. (canceled)15. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient claim 1 , carrier or vehicle.16. A method of treating a proliferative disorder comprising administering to a patient the pharmaceutical composition of .17. The method of wherein the proliferative disorder is selected from a benign or malignant tumor claim 16 , lymphomas claim 16 , Hodgkins and Non-Hodgkin's lymphoma claim 16 , Multiple Myeloma claim 16 , Smoldering of Indolent Multiple Myeloma claim 16 , Waldenström's macroglobulinemia claim 16 , carcinoma of the brain claim 16 , kidney claim 16 , liver claim 16 , adrenal gland claim 16 , bladder claim 16 , breast claim 16 , stomach claim 16 , gastric tumors claim 16 , ovaries claim 16 , colon claim 16 , rectum claim 16 , prostate claim 16 , pancreas claim 16 , lung claim 16 , vagina claim 16 , cervix claim 16 , testis claim 16 , genitourinary tract claim 16 , esophagus claim 16 , larynx claim 16 , skin claim 16 , bone or thyroid claim 16 , sarcoma claim 16 , glioblastomas claim 16 , neuroblastomas claim 16 , or gastrointestinal cancer claim 16 , colon carcinoma or colorectal adenoma or a tumor of the neck and head claim 16 , an epidermal hyperproliferation claim 16 , prostate hyperplasia claim 16 , a neoplasia claim 16 , a neoplasia of epithelial character claim 16 , adenoma claim 16 , adenocarcinoma claim 16 , keratoacanthoma claim 16 , epidermoid carcinoma claim 16 , large cell carcinoma claim 16 , non-small-cell lung carcinoma claim 16 , a mammary carcinoma claim 16 , follicular carcinoma claim 16 , undifferentiated carcinoma claim 16 ...

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Номер записи: 98
10-02-2022 дата публикации

THIENO-INDENO-MONOMERS AND POLYMERS

Номер: US20220041617A1
Автор: Chen Hu, Hayoz Pascal, HURHANGEE Michael, KAELBLEIN Daniel, MCCULLOCH Iain, Zhang Weimin
Принадлежит:

Polymers comprising at least one unit of formulae 2. The polymer according to claim 1 , wherein:{'sup': 2', '2′', '2″, 'sub': '1-36', 'R, R and R are at each occurrence hydrogen, and R is at each occurrence C-alkyl.'}7: The polymer of claim 1 , wherein m is 0 claim 1 , 1 or 2.8: An electronic device claim 1 , comprising the polymer of .9: The electronic device of claim 8 , wherein the electronic device is an organic field effect transistor. The present invention relates to new monomers and polymers made thereof, in particular thieno-indeno-monomers and polymers, to a process for the preparation of these monomers and polymers, to intermediates, to electronic devices comprising these polymers, as well as to the use of these polymers as semiconducting material.Organic semiconducting materials can be used in electronic devices such as organic photovoltaic devices (OPVs), organic field-effect transistors (OFETs), organic light emitting diodes (OLEDs), organic photodiodes (OPDs) and organic electrochromic devices (ECDs).It is desirable that the organic semiconducting materials are compatible with liquid processing techniques such as spin coating as liquid processing techniques are convenient from the point of processability, and thus allow the production of low cost organic semiconducting material-based electronic devices. In addition, liquid processing techniques are also compatible with plastic substrates, and thus allow the production of light weight and mechanically flexible organic semiconducting material-based electronic devices.For application in organic photovoltaic devices (OPVs), organic field-effect transistors (OFETs), and organic photodiodes (OPDs), it is further desirable that the organic semiconducting materials show high charge carrier mobility.For application in organic photovoltaic devices (OPVs) and organic photodiodes (OPDs), the organic semiconducting materials should also show a strong absorption of the visible light.It was the object of the present ...

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Номер записи: 99
10-02-2022 дата публикации

SYNTHESIS OF FUNCTIONALIZABLE OR FUNCTIONALIZED POLY(3,4-ETHYLENEDIOXYTHIPHENE)-BASED POLYMERS AND MONOMERS THEREFOR

Номер: US20220041618A1
Автор: Cao Bin, Cui Xinyan
Принадлежит:

A method of forming a compound having the formula: 3. The method of wherein the reaction takes place under conditions to limit nucleophilic addition reactions by the base.4. The method of wherein the base is a non-nucleophilic base.5. The method of wherein the base comprises potassium iert-butoxide and sodium tert-butoxide.6. The method of wherein the base comprises potassium tert-butoxide.7. The method of wherein the reaction take place at room temperature.8. The method of wherein the reaction occurs at a temperature in the range of approximately 0° C. to 100° C.9. The method of wherein the reaction proceeds to quantitative conversion.10. The method of wherein the base comprises sodium hydroxide and potassium hydroxide.11. The method of wherein the reaction has a yield of at least 95%.12. The method of wherein X is Cl.13. A method of forming a polymer claim 1 , comprising; polymerizing monomers comprising at least one of exomethylene functionalized 3 claim 1 ,4-ethylenedioxythiophene or the reaction product of exomethylene functionalized 3 claim 1 ,4-ethylenedioxythiophene and a compound including a group reactive with the exomethylene group of exomethylene functionalized 3 claim 1 ,4-ethylenedioxythiophene via a polymerization reaction claim 1 , wherein the monomers have a purity of at least 90% in the polymerization reaction.14. The method of wherein the monomers have a purity of at least 95%.15. The method of wherein the polymerization reaction is an electropolymerization reaction and the method further comprises functionalization of the polymer after synthesis by reacting a compound with an exomethylene group.16. The method of wherein the monomers have a concentration of at least 20 mM in the polymerization reaction.17. The method of wherein the group reactive with the exomethylene group is a thiol group.18. The method of wherein the compound including the group reactive with the exomethylene group is selected from the group consisting of 3-mercaptopropionic ...

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Номер записи: 100