Настройки

Укажите год
-

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год
Применить Всего найдено 8206. 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.

Подробнее
Номер записи: 1
26-01-2012 дата публикации

Process for Preparing Dithiine-tetracarboxy-diimides

Номер: US20120022270A1
Автор: Martin Kaussmann, Thomas Himmler
Принадлежит: Bayer CropScience AG

The present invention relates to a new process for preparing dithiine-tetracarboxy-diimides

Подробнее
Номер записи: 2
01-03-2012 дата публикации

Conjugated compound, and organic thin film and organic thin film element each comprising same

Номер: US20120049174A1
Автор: Makoto Okabe, Masato Ueda, Yoshio Aso, Yutaka Ie
Принадлежит: Osaka University NUC, Sumitomo Chemical Co Ltd

A conjugated compound having a group represented by formula (I) and/or formula (II). [In the formulas, Ar represents an optionally substituted trivalent aromatic hydrocarbon or optionally substituted trivalent heterocyclic group, and A represents hydrogen, a halogen atom or a monovalent group. When multiple A groups are present they may be the same or different, and at least one A represents an electron-withdrawing group. Ar′ represents an optionally substituted C6 or greater divalent aromatic hydrocarbon or optionally substituted C4 or greater divalent heterocyclic group, and R1 and R2 are the same or different and each represents hydrogen, a halogen atom or a monovalent group, while A′ represents hydrogen, a halogen atom or a monovalent group. When multiple A′ groups are present they may be the same or different, and at least one A′ represents an electron-withdrawing group.]

Подробнее
Номер записи: 3
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.

Подробнее
Номер записи: 4
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.

Подробнее
Номер записи: 5
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.

Подробнее
Номер записи: 6
13-09-2012 дата публикации

Organic compound and photovoltaic device comprising the same

Номер: US20120227802A1
Автор: Alexey Nokel, Pavel Ivan Lazarev, Pavel Khokhlov
Принадлежит: Cryscade Solar Ltd

The present invention provides a organic compound of the general structural formula 1 and photovoltaic device and photovoltaic layer comprising thereof Said organic compound forms rod-like supramolecules and absorbs electromagnetic radiation in at least one predetermined spectral subrange within a wavelength range from 400 to 3000 nm with excitation of electron-hole pairs. The polycyclic core Cor 1 , the bridging group B, and the polycyclic core Cor 2 form a molecular system selected from the list comprising donor-bridge-acceptor-bridge-donor and acceptor-bridge-donor-bridge-acceptor in which a dissociation of excited electron-hole pairs is carried out. A solution of the organic compound or its salt forms a solid photovoltaic layer on a substrate.

Подробнее
Номер записи: 7
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).

Подробнее
Номер записи: 8
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.

Подробнее
Номер записи: 9
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 ...

Подробнее
Номер записи: 10
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 ...

Подробнее
Номер записи: 11
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 , ...

Подробнее
Номер записи: 12
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 ...

Подробнее
Номер записи: 13
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) ...

Подробнее
Номер записи: 14
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 ...

Подробнее
Номер записи: 15
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 ...

Подробнее
Номер записи: 16
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 , ...

Подробнее
Номер записи: 17
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 ...

Подробнее
Номер записи: 18
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. ...

Подробнее
Номер записи: 19
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 ...

Подробнее
Номер записи: 20
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 ...

Подробнее
Номер записи: 21
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 ...

Подробнее
Номер записи: 22
18-04-2013 дата публикации

LEAVING SUBSTITUENT-CONTAINING COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL FORMED THEREFROM, ORGANIC ELECTRONIC DEVICE, ORGANIC THIN-FILM TRANSISTOR AND DISPLAY DEVICE USING THE ORGANIC SEMICONDUCTOR MATERIAL, METHOD FOR PRODUCING FILM-LIKE PRODUCT, PI-ELECTRON CONJUGATED COMPOUND AND METHOD FOR PRODUCING THE PI ELECTRON CONJUGATED COMPOUND

Номер: US20130095605A1
Автор: Goto Daisuke, Kato Takuji, Matsumoto Shinji, Mohri Masataka, Sagisaka Toshiya, Shinoda Masato, TANO Takanori, YAMAMOTO Satoshi, Yutani Keiichiro
Принадлежит: RICOH COMPANY, LTD.

A leaving substituent-containing compound represented by General Formula (I), wherein the leaving substituent-containing compound can be converted to a compound represented by General Formula (Ia) and a compound represented by General Formula (II), by applying energy to the leaving substituent-containing compound, in General Formulas (I), (Ia) and (II), X and Y each represent a hydrogen atom or a leaving substituent, where one of X and Y is the leaving substituent and the other is the hydrogen atom; Qto Qeach represent a hydrogen atom, a halogen atom or a monovalent organic group; Qand Qeach represent a hydrogen atom or a monovalent organic group other than the leaving substituent; and among the monovalent organic groups represented by Qto Q, adjacent monovalent organic groups may be linked together to form a ring. 2: The leaving substituent-comprising compound according to claim 1 , wherein the leaving substituent represented by X or Y is a substituted or unsubstituted ether group or acyloxy group comprising a carbon atom.3: The leaving substituent-comprising compound according to claim 1 , wherein in the General Formula (I) claim 1 , at least one pair selected from (Q claim 1 , Q) claim 1 , (Q claim 1 , Q) claim 1 , (Q claim 1 , Q) claim 1 , (Q claim 1 , Q) and (Q claim 1 , Q) forms a ring structure which optionally has a substituent claim 1 , and one pair optionally forms a ring structure with adjacent pair or pairs.4: The leaving substituent-comprising compound according to claim 1 , wherein in the General Formula (I) claim 1 , at least one pair selected from (Q claim 1 , Q) claim 1 , (Q claim 1 , Q) and (Q claim 1 , Q) forms a ring structure which optionally has a substituent.5: The leaving substituent-comprising compound according to claim 3 , wherein the ring structure is an aryl group or a heteroaryl group.614-. (canceled)16: The method according to claim 15 , wherein the leaving substituent represented by X or Y is a substituted or unsubstituted ether group ...

Подробнее
Номер записи: 23
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 ...

Подробнее
Номер записи: 24
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 ...

Подробнее
Номер записи: 25
18-04-2013 дата публикации

ORGANIC SEMICONDUCTIVE MATERIAL PRECURSOR CONTAINING DITHIENOBENZODITHIOPHENE DERIVATIVE, INK, INSULATING MEMBER, CHARGE-TRANSPORTING MEMBER, AND ORGANIC ELECTRONIC DEVICE

Номер: US20130096320A1
Автор: Goto Daisuke, Kato Takuji, Matsumoto Shinji, Mohri Masataka, Okada Takashi, Sagisaka Toshiya, Shinoda Masato, TANO Takanori, YAMAMOTO Satoshi, Yutani Keiichiro
Принадлежит:

An organic semiconductive material precursor containing a dithienobenzodithiophene derivative expressed by General Formula I: in General Formula I, X and Y represent groups bonded together, upon application of external stimulus, to form X—Y which is eliminated from the compound expressed by General Formula I; Rand Reach represent a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aryl group; and Rto Reach represent a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkylthio group, or a substituted or unsubstituted aryl group. 2. The organic semiconductive material precursor according to claim 1 ,wherein a first group of either X or Y is a hydrogen atom, anda second group of either X or Y that is different from the first group is a hydroxyl group or a group having an ether structure, an ester structure, or a thioester structure.67-. (canceled)8. The organic semiconductive material precursor of claim 1 , wherein the precursor is soluble in at least one solvent selected from the group consisting of dichloromethane claim 1 , tetrahydrofuran claim 1 , chloroform claim 1 , toluene claim 1 , mesitylene claim 1 , ethyl benzoate claim 1 , dichlorobenzene claim 1 , and xylene.9. The organic semiconductive material precursor of claim 1 , wherein Rand Rare each independently a substituted or unsubstituted aryl group.10. The ink of claim 4 ,wherein a first group of either X or Y is a hydrogen atom, anda second group of either X or Y that is different from the first group is a hydroxyl group or a group having an ether structure, an ester structure, or a thioester structure.12. The insulating member of claim 5 ,wherein a first group of either X or Y is a hydrogen atom, anda second group of either X or Y that is different from the first group is a hydroxyl group or a group having an ether structure, an ester structure, or a thioester structure. The present invention ...

Подробнее
Номер записи: 26
25-04-2013 дата публикации

METHOD OF MAKING COUPLED HETEROARYL COMPOUNDS VIA REARRANGEMENT OF HALOGENATED HETEROAROMATICS FOLLOWED BY OXIDATIVE COUPLING

Номер: US20130102785A1
Автор: Getmanenko Yulia Alexandrovna, Marder Seth
Принадлежит: GEORGIA TECH RESEARCH CORPORATION

The inventions disclosed and described herein relate to new and efficient generic methods for making a wide variety of compounds having Formulas (I) and (II) as shown below (Formulas (I) and (II)) wherein HAr is an optionally substituted five or six membered heteroaryl ring, and Hal is a halogen, and Y is a bridging radical, such as S, Se, NRC(O), C(O)C(O), Si(R), SO, SO, PR, BR, C(R)or P(O)R. The synthetic methods employ a “Base-Catalyzed Halogen Dance” reaction to prepare a metallated compound comprising a five or six membered heteroaryl ring comprising a halogen atom, and then oxidatively coupling the reactive intermediate compound. The compounds of Formula (II) and/or oligomer or polymers comprising repeat units having Formula (II) can be useful for making semi-conducting materials, and/or electronic devices comprising those materials. 2. The method of wherein Hal is Br or I.3. The method of wherein HAr is an optionally substituted five membered heteroaryl ring.87. The method of any one of - wherein Ris a C-Caryl or heteroaryl optionally substituted by one to four ring substituents independently selected from halides claims 4 , alkyl claims 4 , alkynyl claims 4 , perfluoroalkyl claims 4 , alkoxide claims 4 , perfluoroalkoxide claims 4 , —Sn(R) claims 4 , —Si(R) claims 4 , —Si(OR)or —B(—OR)wherein each Ris an independently selected alkyl or aryl claims 4 , and each Ris an independently selected alkyl or aryl claims 4 , or the Rgroups together form an optionally substituted alkylene group to form a ring bridging the oxygen atoms.1110. The method of any one of - wherein the strongly basic compound is an alkyl lithium compound.1210. The method of any one of - wherein the strongly basic compound is a lithium dialkylamide compound.1310. The method of any one of - wherein the oxidizing agent is a Cu(II) salt.1410. The method of any one of - wherein the bishalo-bisheteroaryl compound is a 2 claims 1 ,2′-bishalo-1 claims 1 ,1′-bisheteroaryl compound.21. The method of ...

Подробнее
Номер записи: 27
02-05-2013 дата публикации

PHOTOINITIATED REACTIONS

Номер: US20130105297A1
Автор: Johnstone Robert A. W., Loureiro Rui Manuel da Silva
Принадлежит: LINTFIELD LIMITED

Disclosed is a method for the photoinitiated transformation of a transformable reactive substrate. The method includes an initial step in which a protected ketone photoinitiator species which is present in the substrate is deprotected to form the corresponding ketone photoinitiator species for use in a subsequent photoinitiated reaction in the method. The ketone group of the photoinitiator is protected by an unsubstituted 1, 3 dioxolane group. Also disclosed are a composition which may be used in the method, the use of the protected ketone photoinitiator in a photoinitiated reaction, as well as the protected ketone photoinitiators themselves. 1. A method for the photoinitiated transformation of a transformable reactive substrate , said method including an initial step in which a protected ketone photoinitiator species which is present in the substrate is deprotected to form the corresponding ketone photoinitiator species for use in a subsequent photoinitiated reaction in the method , wherein the ketone group of the photoinitiator is protected by an unsubstituted 1 , 3 dioxolane group.2. A method according to claim 1 , wherein the reactive substrate is a coating on a surface of a support.3. A method according to claim 1 , wherein the substrate further includes a species capable of forming acid in response to an external stimulus claim 1 , and wherein deprotection of the protected ketone photoinitiator is effected by reaction with acid generated in situ by the said acid forming species in response to exposure of the substrate to an external stimulus.4. A method according to claim 1 , wherein a suitable acid is applied directly to the substrate to deprotect the protected ketone photoinitiator.5. A method according to claim 1 , wherein the subsequent photoinitiated reaction involves exposure of the substrate to electromagnetic radiation of a wavelength or energy which is suitable to generate a reactive species from the deprotected ketone photoinitiator claim 1 , wherein ...

Подробнее
Номер записи: 28
02-05-2013 дата публикации

Conjugated fused thiophenes, methods of making conjugated fused thiophenes, and uses thereof

Номер: US20130109821A1
Автор: Arthur L. Wallace, James Robert Matthews, Jianfeng Li, Mingqian He, Weijun Niu
Принадлежит: Corning Inc

Described herein are compositions including heterocyclic organic compounds based on fused thiophene compounds, polymers based on fused thiophene compounds, and methods for making the monomers and polymer along with uses in thin film-based and other devices.

Подробнее
Номер записи: 29
09-05-2013 дата публикации

HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS

Номер: US20130116235A1
Автор: Crawford James John, Ortwine Daniel Fred, WEI Binqing, Young Wendy B.
Принадлежит: Genentech, Inc.

Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 2. The compound of wherein Xis N.3. The compound of wherein Xis N.4. The compound of wherein Xis N.5. The compound of wherein Xand Xare N claim 1 , Xand Xare N claim 1 , or Xand Xare N.6. The compound of wherein Ris optionally substituted C-Cheteroaryl selected from pyrazolyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , 5-methyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 5-acetyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 6 claim 1 ,7-dihydro-4H-pyrazolo[5 claim 1 ,1-c][1 claim 1 ,4]oxazin-2-yl claim 1 , and 1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2-yl.7. The compound of wherein Ris —(C-Cheteroaryl)-(C-Cheterocyclyl) where heteroaryl is optionally substituted pyridinyl and heterocyclyl is optionally substituted piperazinyl.8. The compound of wherein Ris phenyl claim 1 , optionally substituted with one or more groups selected from F claim 1 , Cl claim 1 , —CH claim 1 , —S(O)CH claim 1 , cyclopropyl claim 1 , azetidinyl claim 1 , oxetanyl claim 1 , and morpholino.11. The compound of wherein Ris CH.12. The compound of wherein Yis CH and Yis N.13. The compound of wherein Yis N and Yis CH.14. The compound of wherein Yand Yare each CH.15. The compound of wherein Yand Yare each CH claim 1 , and Ris CH.16. The compound of selected from Table 1.17. The compound of selected from Table 218. A pharmaceutical composition comprised of a compound of and a pharmaceutically ...

Подробнее
Номер записи: 30
09-05-2013 дата публикации

FUSED POLYHETEROAROMATIC COMPOUND, ORGANIC THIN FILM INCLUDING THE COMPOUND, AND ELECTRONIC DEVICE INCLUDING THE ORGANIC THIN FILM

Номер: US20130116447A1
Автор: Chung Jong Won, Lee Bang Lin, Lee Ji Youl, Park Jeong il
Принадлежит: SAMSUNG ELECTRONICS CO., LTD.

A low-molecular-weight fused polycyclic heteroaromatic compound may have a compact planar structure in which seven or more rings are fused together. The compound may exhibit a relatively high charge mobility and enable the use of a deposition process or a room-temperature solution process when applied to devices, therefore realizing improved processibility. An organic thin film and electronic device may include the fused polycyclic heteroaromatic compound. 2. The fused polycyclic heteroaromatic compound of claim 1 , wherein the R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , or Rthat is not linked to provide the aromatic ring claim 1 , the heteroaromatic ring claim 1 , or the alicyclic ring fused with the X-containing ring or the X-containing ring is a substituted or unsubstituted C10 to C30 alkyl group or a substituted or unsubstituted C10 to C30 alkenyl group.3. The fused polycyclic heteroaromatic compound of claim 1 , wherein X claim 1 , X claim 1 , X claim 1 , and Xare sulfur (S).5. The fused polycyclic heteroaromatic compound of claim 4 , wherein X claim 4 , X claim 4 , X claim 4 , and Xare sulfur (S).7. The fused polycyclic heteroaromatic compound of claim 6 , wherein X claim 6 , X claim 6 , X claim 6 , and Xare sulfur (S).9. The fused polycyclic heteroaromatic compound of claim 8 , wherein X claim 8 , X claim 8 , X claim 8 , X claim 8 , X claim 8 , X claim 8 , X claim 8 , and Xare sulfur (S).11. The fused polycyclic heteroaromatic compound of claim 10 , wherein X claim 10 , X claim 10 , X claim 10 , X claim 10 , X claim 10 , and Xare sulfur (S).12. The fused polycyclic heteroaromatic compound of claim 1 , wherein the compound has an average molecular weight of about 350 to about 3000.13. An organic thin film comprising the fused polycyclic heteroaromatic compound according to .14. An electronic device comprising the fused polycyclic heteroaromatic compound according to .15. The electronic device of claim 14 , wherein the electronic device is a ...

Подробнее
Номер записи: 31
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 ...

Подробнее
Номер записи: 32
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 ...

Подробнее
Номер записи: 33
16-05-2013 дата публикации

BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS

Номер: US20130123291A1
Автор: Nielson Simon Feldbæk
Принадлежит: LEO PHARMA A/S

Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; Rand R, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(0)-; Ris —CHF, —CF, —OCHF, —OCF, —SCHFor —SCF; X is a bond, —CH—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R; and Ris hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders. 2. A compound according to wherein X is —CH— or —NH—;4. A compound according to claim 1 , wherein m and n are both 0.5. A compound according to claim 1 , wherein m and n are both 1.6. A compound according to claim 1 , wherein Ris —OCHFor —OCF.7. A compound according to claim 6 , wherein Ris —OCHF.8. A compound according to claim 1 , wherein Ris —SCHFor —SCF.9. A compound according to claim 1 , wherein Rand R claim 1 , together with the carbon atom to which they are attached claim 1 , form a 4- claim 1 , 5- or 6-membered heterocyclic ring.10. A compound according to claim 9 , wherein the heterocyclic ring is tetrahydropyran claim 9 , oxetane claim 9 , [1 claim 9 ,3]dioxolane claim 9 , [1 claim 9 ,3]dioxane claim 9 , tetrahydrothiopyran claim 9 , tetrahydrothiopyran-1 claim 9 ,1-dioxide claim 9 , tetrahydrothiopyran-1-oxide claim 9 , tetrahydrothiophene claim 9 , [1 claim 9 ,3]-dithiane claim 9 , thietane claim 9 , [1 claim 9 ,3]-dithiane-1 claim 9 ,3-dioxide claim 9 , thietane-1-oxide claim 9 , or thiethane-1 claim 9 ,1-dioxide.11. A compound according to claim 9 , wherein the heterocyclic ring comprises one heteroatom.12. A ...

Подробнее
Номер записи: 34
23-05-2013 дата публикации

Thienopyridine Derivatives for the Treatment and Prevention of Dengue Virus Infections

Номер: US20130129677A1
Автор: Chelsea M. Byrd, Dennis E. Hruby, Dongcheng Dai, James R. Burgeson, Shanthakumar R. Tyavanagimatt
Принадлежит: Siga Technologies Inc

Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.

Подробнее
Номер записи: 35
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 ...

Подробнее
Номер записи: 36
06-06-2013 дата публикации

ORGANIC SEMICONDUCTOR COMPOSITION, ORGANIC THIN FILM, AND ORGANIC THIN FILM TRANSISTOR HAVING SAME

Номер: US20130140548A1
Автор: Kohiro Kenji, Okachi Takayuki
Принадлежит: Sumitomo Chemical Company, Limited

To provide an organic semiconductor composition that can exhibit a high carrier transport property and give uniform characteristics. An organic semiconductor composition characterized by containing a high molecular weight compound having a carrier transport property and a low molecular weight compound, in which the low molecular weight compound has a structure represented by Formula (1) and a content ratio of the low molecular weight compound is from 5 to 95 parts by mass relative to a total of 100 parts by mass of the high molecular weight compound and the low molecular weight compound, 2. The organic semiconductor composition according to claim 1 , wherein the high molecular weight compound has a repeating unit containing at least one kind of structures of an arylamine structure claim 1 , a fluorene structure claim 1 , and a thiophene structure.3. The organic semiconductor composition according to claim 1 , wherein a content ratio of the high molecular weight compound is either from not less than 5 parts by mass to less than 30 parts by mass or from more than 70 parts by mass to not more than 95 parts by mass relative to a total of 100 parts by mass of the high molecular weight compound and the low molecular weight compound.4. The organic semiconductor composition according to claim 1 , wherein the content ratio of the high molecular weight compound is from not less than 5 parts by mass to less than 30 parts by mass relative to a total of 100 parts by mass of the high molecular weight compound and the low molecular weight compound.5. An organic thin film claim 1 , comprising the organic semiconductor composition according to .6. An organic thin film transistor comprising:a source electrode and a drain electrode;an organic semiconductor layer that serves as a current path between these electrodes; anda gate electrode that controls an amount of current flowing through the current path,{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'wherein the organic ...

Подробнее
Номер записи: 37
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 ...

Подробнее
Номер записи: 38
06-06-2013 дата публикации

SEMICONDUCTOR MATERIALS PREPARED FROM BRIDGED BITHIAZOLE COPOLYMERS

Номер: US20130144065A1
Автор: Basuki Johan Sebastian, Doetz Florian, Mishra Ashok Kumar, Noguchi Hiroyoshi, Vaidyanathan Subramanian, ZHU Bo
Принадлежит:

The present invention provides semiconducting compounds, oligomers and polymers of formula wherein Aand Acan be the same or different and are S or Se, E is selected from the group consisting of The compounds, oligomers and polymers of formula of formula (1) are suitable for use in electronic devices such as organic field effect transistors. 2. The compound of claim 1 , wherein Aand Aare S.6. The compound of claim 1 , wherein Rand Rare independently H claim 1 , C-alkyl claim 1 , C-haloalkyl claim 1 , —X—Ror —X—Ar claim 1 ,wherein{'sup': 1', '1', '1', '1, 'sub': a', 'a', 'a, 'claim-text': wherein', {'sup': '1', 'sub': 1-6', '1-6, 'Zis C-alkylene or C-haloalkylene, and'}, 'a is an integer of from 1 to 10,, 'Xis —[Z—O]—, —[Z—S—]—, or —[S—Z]—S—,'}{'sup': '6', 'sub': 1-30', '1-30, 'Ris C-alkyl or C-haloalkyl,'}{'sup': 2', '3', '4', '3', '4, 'sub': 1-30', '1-30, 'claim-text': {'sup': 3', '4, 'sub': 1-6', '1-6, 'wherein Zand Zare independently C-alkylene or C-haloalkylene,'}, 'Xis —Z—O—Z—, —Z—S—Z—, C-alkylene or C-haloalkylene,'}and{'sup': 1', 'a', 'a, 'sub': 6-14', '1-6', '1-6, 'Aris C-aryl, optionally substituted with 1 to 5 substituents R, wherein Ris selected from the group consisting of a halogen, a C-alkyl, and a C-alkoxy.'}7. The compound of claim 1 , wherein Rand Rare independently a C-alkyl.8. The compound of claim 1 , wherein Ris —X—Ar claim 1 , —X—Ar—Ar claim 1 , —X—Ar—Ror —X—Ar—Ar—R claim 1 ,wherein{'sup': '5', 'Xis a covalent bond,'}{'sup': 7', 'e', 'e, 'sub': 6-14', '1-6', '1-6', '1-6, 'Aris C-aryl or monovalent 5 to 14 membered aromatic heterocyclic residue, each optionally substituted with 1 to 5 substituents R, wherein Ris selected from the group consisting of a halogen, a CN, a C-alkyl, a C-alkoxy and a C-haloalkyl,'}{'sup': 8', '9', 'f', 'f, 'sub': 6-14', '1-6', '1-6', '1-6, 'Arand Arare independently C-arylene or bivalent 5 to 14 membered aromatic heterocyclic residue, each optionally substituted with 1 to 4 substituents R, wherein Ris selected from the ...

Подробнее
Номер записи: 39
13-06-2013 дата публикации

Compounds Having Semiconducting Properties and Related Compositions and Devices

Номер: US20130146851A1
Автор: Denti Mitchell, Facchetti Antonio, Huang Chun, Newman Christopher, Usta Hakan, Wang Jingqi
Принадлежит: POLYERA CORPORATION

Disclosed are new compounds having semiconducting properties. Such compounds can be processed into thin film semiconductors that exhibit high carrier mobility and/or good current modulation characteristics. 4. The compound of claim 1 , wherein M comprises a thieno[3 claim 1 ,2-b]thiophene moiety.7. The compound of claim 1 , wherein Rand Rindependently are selected from the group consisting of a branched Calkyl and haloalkyl group.8. The compound of claim 1 , wherein Rand Rindependently are a branched Calkyl group.9. The compound of claim 1 , wherein each of Rand Ris CHR′R″ claim 1 , wherein R′ is selected from a linear Calkyl group and a linear Chaloalkyl group; and R″ is selected from CH claim 1 , CF claim 1 , CH claim 1 , CHCF claim 1 , CFCH claim 1 , and CF.10. A thin film semiconductor comprising a compound of .11. A composite comprising a substrate and the thin film semiconductor of deposited on the substrate.12. An electronic device claim 10 , an optical device claim 10 , or an optoelectronic device comprising the thin film semiconductor of .13. A field effect transistor comprising a source electrode claim 10 , a drain electrode claim 10 , a gate electrode claim 10 , and the thin film semiconductor of in contact with a dielectric material.14. The field effect transistor of claim 13 , wherein the field effect transistor has a structure selected from top-gate bottom-contact structure claim 13 , bottom-gate top-contact structure claim 13 , top-gate top-contact structure claim 13 , and bottom-gate bottom-contact structure.15. The field effect transistor of claim 13 , wherein the dielectric material comprises an organic dielectric material.16. The field effect transistor of claim 13 , wherein the dielectric material comprises an inorganic dielectric material or a hybrid organic/inorganic dielectric material.17. An electroluminescent display device comprising a plurality of field effect transistors according to .18. An organic light-emitting transistor comprising a ...

Подробнее
Номер записи: 40
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 ...

Подробнее
Номер записи: 41
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 ...

Подробнее
Номер записи: 42
20-06-2013 дата публикации

FUSED TRICYCLIC ETHER CARBAMATES AND THEIR USE

Номер: US20130158094A1
Автор: Ghosh Arun K., Mitsuya Hiroaki, Parham Garth, Xu Chun-Xiao
Принадлежит: PURDUE RESEARCH FOUNDATION

Tricylic ether carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are describes. Methods of using the disclosed compounds for treating patients infected with HIV are also described. 2. (canceled)4. (canceled)5. The compound of wherein Xis a bond.7. (canceled)9. (canceled)10. The compound of wherein Y is hydrogen.11. The compound of wherein W claim 1 , W claim 1 , and Ware oxygen.14. The compound of wherein Rand Rare each hydrogen.15. The compound of wherein Ris optionally substituted arylalkyl claim 1 , Xis a bond claim 1 , Ris hydrogen claim 1 , Xis S(O) claim 1 , Ris optionally substituted aryl claim 1 , and Ris iso-butyl.16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. The compound of wherein Ris optionally substituted arylalkyl.22. The compound of wherein Wis oxygen.23. The compound of wherein Wor Wis oxygen.24. The compound of wherein Wand one of Wor Wis oxygen.25. The compound of wherein Wand Ware oxygen.26. The compound of wherein each of W claim 1 , W claim 1 , and W3 is oxygen.27. The compound of wherein Wis optionally substituted methylene.28. (canceled)29. A pharmaceutical composition comprising one or more compounds of and further comprising one or more carriers claim 1 , diluents claim 1 , or excipients claim 1 , or a combination thereof for treating HIV infection.30. (canceled)31. A method for treating a patient in need of relieve of an HIV infection claim 1 , the method comprising the step of administering to a patient in need of relief from the HIV infection a therapeutically effective amount of one or more compounds of or a pharmaceutical composition thereof. This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Application Ser. No. 61/379,414 filed on Sep. 2, 2010, the entire disclosure of which is hereby incorporated by reference.This invention relates to compounds that inhibit HIV proteolytic enzymes and processes for preparing the compounds. The invention also ...

Подробнее
Номер записи: 43
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 ...

Подробнее
Номер записи: 44
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- ...

Подробнее
Номер записи: 45
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 ...

Подробнее
Номер записи: 46
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 ...

Подробнее
Номер записи: 47
27-06-2013 дата публикации

Benzodithiophene organic semiconductive material and its preparation method and use

Номер: US20130165655A1
Автор: Erjian Xu, Jie Huang, Minjie Zhou
Принадлежит: Oceans King Lighting Science and Technology Co Ltd

The present invention relates to optoelectronic materials field, and it discloses a benzodithiophene organic semiconductive material with the following structural formula (P): wherein, x+y=2; 1≦x<2, 0<y≦1; 1<n≦100; R 1 , R 2 are C 1 -C 20 alkyl; R 3 is selected from C 1 -C 20 alkyl; R 4 , R 5 are hydrogen, phenyl, C 1 -C 20 alkyl or phenyl substituted by C 1 -C 20 alkoxy. The present invention is also provided with preparation method and use of the benzodithiophene organic semiconductive material. The benzodithiophene containing bisphenyl siloles unit has good dissolution property, high carrier mobility, strong absorbance, wide optical absorption range, and improved utilization of sunlight, and its preparation process is simple, with high yield, and easy to operate and control.

Подробнее
Номер записи: 48
04-07-2013 дата публикации

EVAPORABLE ORGANIC SEMICONDUCTIVE MATERIAL AND USE THEREOF IN AN OPTOELECTRONIC COMPONENT

Номер: US20130167930A1
Автор: Gerdes Olga, Hildebrandt Dirk, Mattersteig Gunter, Vetter Serge, Weiss André
Принадлежит: HELIATEK GMBH

The invention relates to compounds of general formula IIIa and their use in optoelectronic components. 2. A compound according to claim 1 , wherein said compounds of the formula IIIa have point or mirror symmetry at least in relation to the main chain.11. A compound according to where o and p=0 and W═C—R.14. A compound according to where X═S claim 13 , and Y═S and W═C—R.16. A compound according to claim 15 , where additionally p=0.17. A compound according to wherein R9 and R10 form a 5 membered or 6-membered ring.18. A compound according to claim 1 , in which W is selected from: C(CN) claim 1 , CHCN claim 1 , and R1 and R6 are each selected from: H and CN.194. An optoelectronic component having an electrode and a counterelectrode and at least one organic light-sensitive layer between the electrode and the counterelectrode claim 1 , wherein the organic light-sensitive layer () comprises at least one compound according to .20. (canceled)21. A compound according to wherein R′ is selected from C(CN)and CHCN. The invention relates to an organic semiconductive material of the general formulae I and II, and also IIIa.Research and development in organic solar cells has increased significantly, particularly in the last ten years. The maximum efficiency reported to date for what are called “small molecules” is 5.7% [Jiangeng Xue, Soichi Uchida, Barry P. Rand, and Stephen R. Forrest, Appl. Phys. Lett. 85 (2004) 5757]. Small molecules are understood in the context of the present invention to mean nonpolymeric organic monodisperse molecules in the mass range between 100 and 2000 grams/mol. These have to date been unable to achieve the efficiencies of 10-20% typical of inorganic solar cells. Organic solar cells, however, are subject to the same physical limitations as inorganic solar cells, and therefore, at least theoretically, similar efficiencies are to be expected after corresponding development work.Organic solar cells consist of a sequence of thin layers (each typically of ...

Подробнее
Номер записи: 49
04-07-2013 дата публикации

OPTOELECTRONIC COMPONENT WITH ORGANIC LAYERS

Номер: US20130167931A1
Автор: Gerdes Olga, Hildebrandt Dirk, Mattersteig Gunter, Pfeiffer Martin, Uhrich Christian, Vetter Serge, Weiss André
Принадлежит:

The present disclosure relates to an optoelectronic component having an electrode (), a counter electrode () and at least one organic light-sensitive layer () between the electrode and counter electrode. The organic light-sensitive layer () contains at least one compound of the general formula EWG (electron withdrawing group)-D (donor block)-EWG with at least one substituent on the extended donor block D. 1. An optoelectronic component having an electrode and a counterelectrode and at least one organic light-sensitive layer between the electrode and the counterelectrode , said layer comprising a compound EWG-D-EWG as the main component , in which EWG has electron-withdrawing properties with respect to the extensive donor block D , wherein the extensive donor block D has not more than 9 conjugated double bonds in linear succession and is formed from heterocyclic 5-membered rings and/or from vinylene and/or systems of the same type or mixed types which are fused thereto , and in that the donor block D has at least one substituent.2. The component according to claim 1 , wherein the heterocyclic 5-membered rings of the extensive donor block D are each independently selected from thiophene claim 1 , selenophene claim 1 , furan and pyrrole and/or from systems of the same kind or mixed kinds fused thereto.3. The component according to claim 1 , wherein the at least one substituent of the extensive donor block D has π electrons claim 1 , for example as a free electron pair or in a multiple bond.4. The component according to claim 1 , wherein the at least one substituent of the extensive donor block D is selected from the group of the ethers claim 1 , thioethers claim 1 , amines claim 1 , or from substituted or unsubstituted aromatics or heteroaromatics having 4 to 10 atoms claim 1 , or from alkenyl having at least one double bond in the α position claim 1 , or claim 1 , in the case of 2 adjacent substituents claim 1 , form a heterocyclic 5- claim 1 , 6- or 7-membered ring.5 ...

Подробнее
Номер записи: 50
04-07-2013 дата публикации

LIGHT EMITTING ELEMENT, LIGHT EMITTING DEVICE AND ELECTRONIC APPARATUS

Номер: US20130168654A1
Автор: Fujita Tetsuji, Yamamoto Hidetoshi
Принадлежит: SEIKO EPSON CORPORATION

The light emitting element of the embodiment includes an anode; a cathode; a visible light emitting layer provided between the anode and the cathode and emitting visible light; and a carrier trapping layer containing a thiadiazole based compound represented by the following formula (1). 5. The light emitting element according to claim 1 , wherein the carrier trapping layer is positioned at an anode side relative to the light emitting layer.6. The light emitting element according to claim 5 ,wherein the carrier trapping layer further contains a host material in addition to the thiazole based compound, andwherein the host material is at least one type from among amine based material, anthracene based material, and napthacene based material.7. The light emitting element according to claim 1 , wherein the carrier trapping layer is positioned at a cathode side relative to the light emitting layer.8. The light emitting element according to claim 7 ,wherein the carrier trapping layer further contains a host material in addition to the thiazole based compound, andwherein the host material is at least one type from among anthracene based material, napthacene based material, and a quinolinolato based metal complex.9. The light emitting element according to claim 1 , wherein the light emitting layer is a single layer.10. The light emitting element according to claim 9 , wherein the light emitting layer emits a blue luminescent color as visible light.11. The light emitting element according to claim 9 , wherein the light emitting layer emits a yellow luminescent color as visible light.12. The light emitting element according to claim 1 , wherein the light emitting layer is formed of at least two layers.13. A light emitting device comprising the light emitting element according to .14. A light emitting device comprising the light emitting element according to .15. A light emitting device comprising the light emitting element according to .16. A light emitting device comprising ...

Подробнее
Номер записи: 51
04-07-2013 дата публикации

Pyrrolopyrrole derivatives, their manufacture and use

Номер: US20130172575A1
Автор: AEBISCHER OLIVER FREDERIC, BIENEWALD FRANK, BUDRY JEAN-LUC, Duggeli Mathias, FONDRODONA TURON MARTA, Fontana Margherita, HAO ZHIMIN, Hayoz Pascal, Schmidhalter Beat, TURBIEZ MATHEIU G.R.
Принадлежит: BASF SE

The present invention relates to compounds of the formula I 9. A semiconductor device according to comprising as a semiconducting effective means a compound of the formula I as defined in with the proviso that at least one of R , R , R , Rand Ris different from hydrogen.10. A semiconductor device according to in the form of a diode claim 8 , a photodiode claim 8 , a sensor claim 8 , an organic field effect transistor claim 8 , a transistor for flexible displays claim 8 , or a heterojunction solar cell.11. A p-type transistor comprising the compound of formula I as defined in . The present invention relates to 1,4-diketopyrrolo[3,4-c]pyrrole (DPP) derivatives of the below formula I, wherein the substituents are as defined herein below, to their manufacture; to their use as organic semiconductors, e.g. in semiconductor devices, especially a sensor, a diode, a photodiode, an organic field effect transistor, a transistor for flexible displays, and/or a solar cell (photovoltaic cell); to such semiconductor devices comprising diketopyrrolopyrrol derivatives of the formula I as a semiconducting effective means, and to devices containing said semiconductor devices.JP 2006117591-A to Toyo Ink Manufacturing Co. discloses diketopyrrolopyrrol derivatives for use in organic electroluminescent elements, like flat panel displays and liquid crystal displays, but not for use as organic semiconductors.WO 2004/090046 A1 to Ciba discloses fluorescent diketopyrrolopyrrol (DPP) derivatives, mainly for use in inks, toners, colorants, pigmented plastics, color changing media, solid dye lasers and electroluminescent devices. Said DPP derivatives have a smaller or shorter side chain on both sides of the diketopyrrolopyrrol moiety than the diketopyrrolopyrrol derivatives claimed per se in the present specification. In addition, specifically disclosed, i.e. individualized, compounds include only those derivatives wherein the DPP nitrogen atoms are substituted by alkyl groups having no more ...

Подробнее
Номер записи: 52
11-07-2013 дата публикации

BENZO-FUSED THIOPHENE / TRIPHENYLENE HYBRID MATERIALS

Номер: US20130175510A1
Автор: Kwong Raymond, LIN Chun, Ma Bin, WU Yonggang
Принадлежит: UNIVERSAL DISPLAY CORPORTION

Triphenylene containing benzo-fused thiophene compounds are provided. Additionally, triphenylene containing benzo-fused furan compounds are provided. The compounds may be useful in organic light emitting devices, particularly as hosts in the emissive layer of such devices, or as materials for enhancement layers in such devices, or both. 1. A compound comprising a triphenylene containing benzo-fused thiophene or benzo-fused furan , wherein any substituent in the compound is an unfused substituent independently selected from the group consisting of CH , OCH , OAr , N(CH) , N(Ar)(Ar) , CH═CH—CH , C≡CHCH , Ar , Ar—Ar , CH—Ar , or no substitution , wherein n is 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , or 10 , and wherein Arand Arare independently selected from the group consisting of benzene , biphenyl , naphthalene , triphenylene , carbazole , and heteroaromatic analogs thereof.3. The compound of claim 2 , wherein X is S.4. The compound of claim 2 , wherein X is O.6. The compound of claim 5 , wherein X is S.7. The compound of claim 5 , wherein X is O.9. The compound of claim 8 , wherein X is S.10. The compound of claim 8 , wherein X is O.12. The compound of claim 11 , wherein X is S.13. The compound of claim 11 , where X is O.1419-. (canceled)20. The compound of claim 1 , wherein Arand Arare independently selected from the group consisting of benzene claim 1 , biphenyl claim 1 , naphthalene claim 1 , triphenylene claim 1 , and carbazole.21. An organic light emitting device claim 1 , comprising:an anode;a cathode; and{'sub': n', '2n+1', 'n', '2n+1', '1', 'n', '2n+1', '2', '1', '2', 'n', '2n+1', 'n', '2n+1', '1', '1', '2', 'n', '2n', '1', '1', '2, 'an organic layer disposed between the anode and the cathode, wherein the organic layer comprises a compound comprising a triphenylene containing benzo-fused thiophene or benzo-fused furan, wherein any substituent in the compound is an unfused substituent independently selected from the group consisting of CH, OCH, OAr, N(CH), N(Ar)( ...

Подробнее
Номер записи: 53
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 ...

Подробнее
Номер записи: 54
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 ...

Подробнее
Номер записи: 55
25-07-2013 дата публикации

NOVEL ORGANIC COMPOUND AND ELECTROCHROMIC ELEMENT HAVING THE SAME

Номер: US20130190513A1
Автор: Okada Shinjiro, Yamada Kenji
Принадлежит: CANON KABUSHIKI KAISHA

An organic compound represented by the following general formula [1] is provided. In the general formula [1], Ato Aare each independently selected from the group consisting of a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, an alkoxy group having 1 to 20 carbon atoms, and an aryl group. However, at least one of Ato Arepresents the alkyl group, the alkoxy group, or the aryl group. 2. The organic compound according to claim 1 ,{'sub': 1', '4, 'wherein at least one of Ato Arepresents an alkoxy group having 1 to 20 carbon atoms.'}3. The organic compound according to claim 2 ,{'sub': 1', '4, 'wherein the least one of Ato Arepresents a methoxy group or an isopropoxy group.'} 1. Field of the InventionThe present invention relates to a novel organic compound and an electrochromic element having the same.2. Description of the Related ArtAs electrochromic (hereinafter abbreviated to as “EC” in some cases) materials, the optical absorption properties (colored state, light transmittance, and the like) of which are changed by an electrochemical oxidation-reduction reaction, various materials have been reported. As inorganic EC materials, a compound using a metal oxide, such as WO, has been known.As organic EC materials, for example, a conductive polymer used in an EC element described in Japanese Patent Laid-Open No. 56-67881 and an EC material using an organic low molecular weight compound, such as an oligothiophene, disclosed in M. G. Hill, J. F. Penneau, B. Zinger, K. R. Mann, L. L. Miller, Chemistry of Materials, 4 (1992) 1106 have been known.When the conductive polymer described in Japanese Patent Laid-Open No. 56-67881 is electrochemically oxidized or reduced, the π-conjugated chain length of its main chain is changed, and as a result, the absorption wavelength is changed.When being in a neutral state, these conductive polymers have absorption in the visible light region and hence are colored, and when the polymers are in an oxidized state, the absorption ...

Подробнее
Номер записи: 56
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 ...

Подробнее
Номер записи: 57
08-08-2013 дата публикации

CRYSTAL OF TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVE

Номер: US20130203989A1
Автор: Kajino Hisaki, Kobayashi Keijiro, Matuura Shinji, Nagai Tomoyuki
Принадлежит: Daiichi Sankyo Company, Limited

To provide a hydrochloride of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90 and a crystal thereof. The present invention provides a hydrochloride of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a crystal thereof, a medicament comprising the same, an anticancer agent comprising the same, and the like. 2. A crystal of a dihydrochloride of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2 claim 1 ,7-dihydro-6-thia-1 claim 1 ,2 claim 1 ,3 claim 1 ,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide represented by formula (1) according to .3. A crystal according to which has the X-ray diffraction pattern shown in claim 2 , in an X-ray powder diffraction pattern obtained by irradiation with copper Kα radiation (wavelength λ=1.54 angstroms).4. A crystal according to which shows characteristic peaks at angles of diffraction 2θ of 7.73 claim 2 , 24.70 claim 2 , 26.01 and 27.29 claim 2 , in an X-ray powder diffraction pattern obtained by irradiation with copper Kα radiation (wavelength λ=1.54 angstroms).5. A crystal according to which shows principal peaks at angles of diffraction 2θ of 7.73 claim 2 , 9.78 claim 2 , 12.58 claim 2 , 14.36 claim 2 , 15.84 claim 2 , 16.71 claim 2 , 17.17 claim 2 , 18.40 claim 2 , 19.58 claim 2 , 21.31 claim 2 , 22.85 claim 2 , 23.62 claim 2 , 24.13 claim 2 , 24.70 claim 2 , 26.01 claim 2 , 27.29 claim 2 , 28.58 claim 2 , 29.37 claim 2 , 30.65 claim 2 , 31.38 claim 2 , 33.52 claim 2 , 35.25 and 36.87 claim 2 , in an X-ray powder diffraction pattern obtained by irradiation with copper Kα radiation (wavelength λ=1.54 angstroms).6. A crystal of a monohydrochloride of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2 claim 1 ,7-dihydro-6-thia-1 claim 1 ,2 claim 1 ,3 claim 1 ,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide ...

Подробнее
Номер записи: 58
15-08-2013 дата публикации

ORGANIC SEMICONDUCTOR DEVICE AND ITS PRODUCTION METHOD, AND COMPOUND

Номер: US20130207081A1
Автор: ADACHI Chihaya, KAKIZOE Hayato, Mieno Hiroyuki, Yasuda Takuma, Yu Seok Yang
Принадлежит: KYUSHU UNIVERSITY NATIONAL UNIVERSITY CORPORATION

An organic semiconductor device which has an organic semiconductor layer formed by crystallizing a compound represented by the following formula (1) from a solution of the compound: 5. The organic semiconductor device according to claim 2 , wherein at least one of Rand Ris a group having a chainlike structure in which the number of the carbon atoms constituting the main chain is from 4 to 20.6. The organic semiconductor device according to claim 2 , wherein at least one of Rand Ris a group having a chainlike structure in which the number of the carbon atoms constituting the main chain is from 8 to 20.7. The organic semiconductor device according to claim 1 , wherein X claim 1 , Xand Xare the same atoms.8. The organic semiconductor device according to claim 7 , wherein X claim 7 , Xand Xare sulfur atoms.9. The organic semiconductor device according to claim 1 , wherein Xand Xare sulfur atoms and Xis a selenium atom or a tellurium atom.10. The organic semiconductor device according to claim 1 , which is a field-effect transistor.13. The method for producing an organic semiconductor device according to claim 11 , wherein the solution is a solution in a halogen solvent.14. The method for producing an organic semiconductor device according to claim 11 , wherein the solvent is an aromatic solvent.18. The compound according to claim 15 , wherein at least one of Rand Ris a group having a chainlike structure in which the number of the carbon atoms constituting the main chain is from 4 to 20.19. The compound according to claim 15 , wherein at least one of Rand Ris a group having a chainlike structure in which the number of the carbon atoms constituting the main chain is from 8 to 20.20. The compound according to claim 15 , wherein X claim 15 , Xand Xare the same atoms.21. The compound according to claim 20 , wherein X claim 20 , Xand Xare sulfur atoms.22. The compound according to claim 15 , wherein Xand Xare sulfur atoms and Xis a selenium atom or a tellurium atom.23. An ...

Подробнее
Номер записи: 59
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 ...

Подробнее
Номер записи: 60
15-08-2013 дата публикации

FREE CRYSTAL OF TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVE

Номер: US20130211084A1
Автор: Ohki Hitoshi, Suzuki Nobuyuki, Ueda Yasusi
Принадлежит: Daiichi Sankyo Company, Limited

To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like. 2. The crystal of which shows principal peaks at angles of diffraction 2θ of 3.10 claim 1 , 4.02 claim 1 , 6.22 claim 1 , 8.54 claim 1 , 9.62 claim 1 , 11.58 claim 1 , 11.84 claim 1 , 12.16 claim 1 , 12.56 claim 1 , 14.46 claim 1 , 15.02 claim 1 , 15.26 claim 1 , 17.86 claim 1 , 22.14 claim 1 , 22.96 claim 1 , 23.10 claim 1 , 23.82 claim 1 , 24.26 and 26.82 claim 1 , in an X-ray powder diffraction pattern obtained by irradiation with copper Kα radiation (wavelength λ=1.54 angstroms).3. A crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2 claim 1 ,7-dihydro-6-thia-1 claim 1 ,2 claim 1 ,3 claim 1 ,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide represented by formula (1) as defined in which has the diffraction pattern shown in claim 1 , in an X-ray powder diffraction pattern obtained by irradiation with copper Kα radiation (wavelength λ=1.54 angstroms).4. The crystal of which shows principal peaks at angles of diffraction 2θ of 5.04 claim 3 , 6.78 claim 3 , 7.72 claim 3 , 10.14 claim 3 , 11.16 claim 3 , 13.24 claim 3 , 13.66 claim 3 , 15.32 claim 3 , 18.50 claim 3 , 20.40 claim 3 , 22.36 claim 3 , 22.90 claim 3 , 25.16 claim 3 , 26.66 claim 3 , 27.92 claim 3 , 30.92 and 31.78 claim 3 , in an X-ray powder diffraction pattern obtained by irradiation with copper Kα radiation (wavelength λ=1.54 angstroms).5. A crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2 claim 1 ,7-dihydro-6-thia-1 claim 1 ,2 claim 1 ,3 claim 1 ,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide represented by ...

Подробнее
Номер записи: 61
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 ...

Подробнее
Номер записи: 62
29-08-2013 дата публикации

THIADIAZOLE, COMPOUND FOR LIGHT-EMITTING ELEMENTS, LIGHT-EMITTING ELEMENT, LIGHT-EMITTING APPARATUS, AUTHENTICATION APPARATUS, AND ELECTRONIC DEVICE

Номер: US20130221334A1
Автор: Fujita Tetsuji, Yamamoto Hidetoshi
Принадлежит: SEIKO EPSON CORPORATION

The thiadiazole represented by formula (1), when used as a light-emitting material in a light-emitting element, allows the light-emitting element to emit near-infrared light. 4. The compound for light-emitting elements according to used as a light-emitting material.8. The light-emitting element according to claim 5 , further comprising an electron transport layer claim 5 , which is a layer having the capability of transporting electrons claim 5 , provided between the cathode and the light-emitting layer so as to be in contact with the light-emitting layer claim 5 ,wherein the electron transport layer contains a compound having an azaindolizine skeleton and an anthracene skeleton in the molecule as an electron transport material.12. The light-emitting element according to claim 9 , further comprising an electron transport layer claim 9 , which is a layer having the capability of transporting electrons claim 9 , provided between the cathode and the light-emitting layer so as to be in contact with the light-emitting layer claim 9 ,wherein the electron transport layer contains a compound having an azaindolizine skeleton and an anthracene skeleton in the molecule as an electron transport material.14. A light-emitting apparatus comprising the light-emitting element according to .15. A light-emitting apparatus comprising the light-emitting element according to .16. A light-emitting apparatus comprising the light-emitting element according to .17. An authentication apparatus comprising the light-emitting element according to .18. An authentication apparatus comprising the light-emitting element according to .19. An authentication apparatus comprising the light-emitting element according to .20. An electronic device comprising the light-emitting element according to .21. An electronic device comprising the light-emitting element according to .22. An electronic device comprising the light-emitting element according to . The present application claims priority to Japanese ...

Подробнее
Номер записи: 63
05-09-2013 дата публикации

QUINOLINO[3,2,1-KL]PHENOXAZINE COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT USING THE SAME

Номер: US20130228768A1
Автор: Abe Shigemoto, Kamatani Jun, Kishino Kengo, Kosuge Tetsuya
Принадлежит: CANON KABUSHIKI KAISHA

Provided is an excellent organic light emitting element having high emission efficiency and a low drive voltage. The organic light emitting element includes an anode, a cathode, and an organic compound layer disposed between the anode and the cathode, in which the organic compound layer includes a quinolino[3,2,1-kl]phenoxazine compound represented by the following general formula [1]: 3. An organic light emitting element comprising:an anode;a cathode; andan organic compound layer disposed between the anode and the cathode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the organic compound layer comprises the quinolino[3,2,1-kl]phenoxazine compound according to .'}4. The organic light emitting element according to claim 3 , wherein:the organic compound layer comprises an emission layer and a hole transport layer adjacent to the emission layer; andthe hole transport layer comprises the quinolino[3,2,1-kl]phenoxazine compound.5. The organic light emitting element according to claim 4 , wherein:the emission layer comprises a host and a guest;the host comprises the quinolino[3,2,1-kl]phenoxazine compound; andthe guest comprises a phosphorescent light emitting material.6. The organic light emitting element according to claim 5 , wherein the phosphorescent light emitting material comprises an iridium complex.7. A display device comprising multiple pixels claim 3 , wherein the pixels each comprise the organic light emitting element according to and a switching element connected to the organic light emitting element.8. An image input device comprising:a display unit for displaying an image; andan input unit for inputting image information,wherein:the display unit comprises multiple pixels; and{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'the pixels each comprise the organic light emitting element according to and a switching element connected to the organic light emitting element.'}9. A display device comprising multiple pixels claim 4 , wherein the pixels ...

Подробнее
Номер записи: 64
05-09-2013 дата публикации

INDOLOPHENOXAZINE COMPOUND AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME

Номер: US20130228770A1
Автор: Abe Shigemoto, Kamatani Jun, Kishino Kengo, Kosuge Tetsuya
Принадлежит: CANON KABUSHIKI KAISHA

Provided is an organic light emitting device having high emission efficiency and excellent driving durability. The organic light emitting device includes an anode, a cathode, and an organic compound layer disposed between the anode and the cathode, in which the organic compound layer includes an indolophenoxazine compound represented by the following general formula [1]: 2. The indolophenoxazine compound according to claim 1 , wherein each of Rto Rrepresents a hydrogen atom.4. An organic light emitting device comprising:an anode;a cathode; andan organic compound layer disposed between the anode and the cathode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the organic compound layer comprises the indolophenoxazine compound according to .'}5. The organic light emitting device according to claim 4 , wherein the indolophenoxazine compound is contained in one of a hole injection layer and a hole transport layer.6. The organic light emitting device according to claim 5 , wherein:the organic compound layer comprises a light emitting layer; andthe light emitting layer comprises a phosphorescent light emitting material.7. The organic light emitting device according to claim 6 , wherein the phosphorescent light emitting material comprises an iridium complex.8. An image display apparatus comprising:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'the organic light emitting device according to ; and'}a switching element connected to the organic light emitting device.9. An image display apparatus comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'the organic light emitting device according to ; and'}a switching element connected to the organic light emitting device.10. An image display apparatus comprising:{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'the organic light emitting device according to ; and'}a switching element connected to the organic light emitting device.11. An image display apparatus comprising:{'claim-ref': {'@idref': 'CLM-00007', ...

Подробнее
Номер записи: 65
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 ...

Подробнее
Номер записи: 66
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 ...

Подробнее
Номер записи: 67
05-09-2013 дата публикации

COMPOUNDS HAVING PHOTOCHEMICALLY REMOVABLE PROTECTING GROUPS BASED ON AN ELECTROCYCLIC REACTION BETWEEN A CHROMOPHORE ATTACHED VIA AN ANILIDE GROUP TO A BENZOTHIOPHENE RING

Номер: US20130231484A1
Автор: Sarker Majher I., Shahrin Tasnuva, Steinmetz Mark G.
Принадлежит: Marquette University

Disclosed herein are compounds having photoremovable protecting groups which are removed after the compounds absorbs light of a given wavelength and undergo an electrocyclic reaction between a chromophore in the compound attached via an anilide to a benzothiophene ring. 3. The compound of claim 1 , wherein A is a thioxanthene-type chromophore claim 1 , a xanthene-type fluorophore (such as a fluorescein-type chromophore or a rhodamine-type chromophore) claim 1 , a naphthalene-type chromophore claim 1 , a carbocyanine-type chromophore claim 1 , a dipyrromethene boron-type chromophore claim 1 , a coumarin-type chromophore claim 1 , an acridine-type chromophore claim 1 , a pyrene-type chromophore claim 1 , a DANSYL-type chromophore claim 1 , and a lanthanide chelate-type chromophore.4. The compound of claim 1 , wherein A is thioxanthene-type chromaophore.6. The compound of claim 5 , wherein Z is S.7. The compound of claim 5 , wherein W is hydrogen and X is a carboxyl group.8. The compound of claim 5 , wherein Ris halogen.9. The compound of claim 8 , wherein Ris bromine.10. The compound of claim 5 , wherein LG is chlorine.14. The compound of claim 1 , wherein the compound has an absorption maxima of about 350-400 nm.15. The compound of claim 1 , wherein the compound has an absorption maxima of about 400-450 nm.17. The method of claim 16 , wherein claim 16 , the photolytic reaction has a yield of greater than about 90%.19. The method of claim 18 , wherein LG is Cl.20. The method of claim 18 , further comprising subjecting the reaction product to light. The present application claims the benefit of priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 61/605,406, filed on Mar. 1, 2013, the content of which is incorporated herein by reference in its entirety.This invention was made with government support under CHE 1055339 awarded by the National Science Foundation. The government has certain rights in the invention.The field of the invention relates ...

Подробнее
Номер записи: 68
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- ...

Подробнее
Номер записи: 69
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.

Подробнее
Номер записи: 70
26-09-2013 дата публикации

INERT SOLUTION-PROCESSABLE MOLECULAR CHROMOPHORES FOR ORGANIC ELECTRONIC DEVICES

Номер: US20130247989A1
Автор: Bazan Guillermo C., Love John, Nguyen Thuc-Quyen, Van Der Poll Thomas S.
Принадлежит: The Regents of the University of California

Small organic molecule chromophores containing a benzo[c][1,2,5]thiadiazole with an electron-withdrawing substituent W in the 5-position (5BTH), benzo[c][1,2,5]oxadiazole with an electron-withdrawing substituent W in the 5-position (5BO), 2H-benzo[d][1,2,3]triazole (5BTR) with an electron-withdrawing substituent W in the 5-position (5BTR), 5-fluorobenzo[c][1,2,5]thiadiazole (FBTH), 5-fluorobenzo[c][1,2,5]oxadiazole (FBO), or 5-fluoro-2H-benzo[d][1,2,3]triazole (FBTR) core structure are disclosed. Such compounds can be used in organic heterojunction devices, such as organic small molecule solar cells and transistors. 2. The electronic or optoelectronic device according to claim 1 ,wherein the non-polymeric compound is used in an active layer of said device.3. The electronic or optoelectronic device according to claim 1 ,wherein said device is a solar cell.4. The electronic or optoelectronic device according to claim 1 ,wherein M is sulfur and W is F.7. The electronic or optoelectronic device according to claim 6 , wherein Ais independently selected from substituted or unsubstituted thiophene claim 6 , pyrrole claim 6 , furan claim 6 , phenyl claim 6 , phosphole claim 6 , benzodithiophene claim 6 , spirofluorene claim 6 , spirothiophene claim 6 , bithiophene claim 6 , terthiophene claim 6 , thienothiophene claim 6 , dithienothiophene claim 6 , benzothiophene claim 6 , isobenzothiophene claim 6 , benzodithiophene claim 6 , cyclopentadithiophene claim 6 , silacyclopentadiene claim 6 , silacyclopentadienebithiophene claim 6 , indole claim 6 , benzene claim 6 , naphthalene claim 6 , anthracene claim 6 , perylene claim 6 , indene claim 6 , fluorene claim 6 , pyrene claim 6 , azulene claim 6 , pyridine claim 6 , oxazole claim 6 , thiazole claim 6 , thiazine claim 6 , pyrimidine claim 6 , pyrazine claim 6 , imidazole claim 6 , benzoxazole claim 6 , benzoxadiazole claim 6 , benzothiazole claim 6 , benzimidazole claim 6 , benzofuran claim 6 , isobenzofuran claim 6 , ...

Подробнее
Номер записи: 71
26-09-2013 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING METABOLISM

Номер: US20130252331A1
Автор: Bradner James Elliott, Brown Jonathan, Plutzky Jorge
Принадлежит:

The invention provides compositions comprising an effective amount of an agent that inhibits a BET protein (e.g., Brd2, Brd3, Brd4), and methods of using such compositions for treating or preventing metabolic syndrome, obesity, type II diabetes, insulin resistance, and related disorders characterized by undesirable alterations in metabolism or fat accumulation. 1. A method of inhibiting adipogenesis , the method comprising contacting an adipocyte or pre-adipocyte with an effective amount of an agent that inhibits a bromodomain and extra-terminal (BET) protein.2. The method of claim 1 , wherein the method inhibits adipocyte differentiation claim 1 , proliferation claim 1 , or hypertrophy.3. A method of inhibiting adipocyte biological function claim 1 , the method comprising contacting an adipocyte with an effective amount of an agent that inhibits a bromodomain and extra-terminal (BET) protein.4. The method of claim 3 , wherein the method reduces fatty acid synthesis claim 3 , lipogenesis claim 3 , lipid droplet accumulation.5. A method for treating or preventing metabolic syndrome in a subject claim 3 , the method comprising administering to the subject an effective amount of an agent that inhibits a bromodomain and extra-terminal (BET) protein claim 3 , thereby treating or preventing metabolic syndrome in the subject.6. The method of claim 5 , wherein the method reduces abdominal obesity claim 5 , atherogenic dyslipidemia claim 5 , elevated blood pressure claim 5 , insulin resistance claim 5 , or type II diabetes.7. A method for treating or preventing obesity or weight gain in a subject claim 5 , the method comprising administering to the subject an effective amount of an agent that inhibits a bromodomain and extra-terminal (BET) protein claim 5 , thereby treating or preventing obesity or weight gain in the subject.8. A method of inhibiting hepatic steatosis in a subject claim 5 , the method comprising administering to the subject an effective amount of an agent ...

Подробнее
Номер записи: 72
03-10-2013 дата публикации

COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC LIGHT EMITTING DIODE INCLUDING THE SAME AND DISPLAY INCLUDING THE ORGANIC LIGHT EMITTING DIODE

Номер: US20130256644A1
Автор: Chae Mi-Young, Kim Hyung-Sun, MIN Soo-Hyun, Yu Eun-Sun
Принадлежит:

A compound for an organic optoelectronic device, the compound being represented by the following Chemical Formula 1: 3. The compound for an organic optoelectronic device as claimed in claim 1 , wherein the ETU is a substituted or unsubstituted imidazolyl group claim 1 , a substituted or unsubstituted triazolyl group claim 1 , a substituted or unsubstituted tetrazolyl group claim 1 , a substituted or unsubstituted oxadiazolyl group claim 1 , a substituted or unsubstituted oxatriazolyl group claim 1 , a substituted or unsubstituted thiatriazolyl group claim 1 , a substituted or unsubstituted benzimidazolyl group claim 1 , a substituted or unsubstituted benzotriazolyl group claim 1 , a substituted or unsubstituted pyridinyl group claim 1 , a substituted or unsubstituted pyrimidinyl group claim 1 , a substituted or unsubstituted triazinyl group claim 1 , a substituted or unsubstituted pyrazinyl group claim 1 , a substituted or unsubstituted pyridazinyl group claim 1 , a substituted or unsubstituted purinyl group claim 1 , a substituted or unsubstituted quinolinyl group claim 1 , a substituted or unsubstituted isoquinolinyl group claim 1 , a substituted or unsubstituted phthalazinyl group claim 1 , a substituted or unsubstituted naphpyridinyl group claim 1 , a substituted or unsubstituted quinazolinyl group claim 1 , a substituted or unsubstituted acridinyl group claim 1 , a substituted or unsubstituted phenanthrolinyl group claim 1 , a substituted or unsubstituted phenazinyl group claim 1 , or a combination thereof.5. The compound for an organic optoelectronic device as claimed in claim 4 , wherein the Aris a substituted or unsubstituted pyridinylene group claim 4 , a substituted or unsubstituted pyrimidinylene group claim 4 , a substituted or unsubstituted triazinylene group claim 4 , or a combination thereof.6. The compound for an organic optoelectronic device as claimed in claim 4 , wherein the Aris a substituted or unsubstituted pyridinylene group claim 4 , and X is ...

Подробнее
Номер записи: 73
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 ...

Подробнее
Номер записи: 74
03-10-2013 дата публикации

Organic Compound, Benzoxazole Derivative, and Light-Emitting Element, Light-Emitting Device, and Electronic Device Using the Benzoxazole Derivative

Номер: US20130261304A1
Автор: Kadoma Hiroshi, KAWAKAMI Sachiko, Nomura Hiroko, SEO Satoshi, USHIKUBO Takahiro
Принадлежит: SEMICONDUCTOR ENERGY LABORATORY CO., LTD.

Novel benzoxazole derivatives are provided to reduce driving voltage of light-emitting elements, and to reduce power consumption of light-emitting elements, light-emitting devices, and electronic devices. A benzoxazole derivative represented by the general formula (G1) is provided. Since the benzoxazole derivative represented by the general formula (G1) has an electron-injecting property, the benzoxazole derivative can be suitably used for light-emitting elements, light-emitting devices, and electronic devices. 120-. (canceled)22. The method for synthesizing the benzoxazole derivative according to claim 21 , wherein the halogen is one selected from the group consisting of chlorine claim 21 , bromine claim 21 , and iodine.24. The method for synthesizing the benzoxazole derivative according to claim 21 , wherein the reaction is performed with the Suzuki-Miyaura coupling method.26. The method for synthesizing a compound according to claim 25 , wherein the boronic acid and the organoboron compound each comprises a benzoxazole skeleton. 1. Field of the InventionThe present invention relates to organic compounds and benzoxazole derivatives. Further, the present invention relates to light-emitting elements, light-emitting devices and electronic devices using the benzoxazole derivatives.2. Description of the Related ArtAn organic compound can take a wider variety of structures compared with an inorganic compound, and it is possible to synthesize a material having various functions by appropriate molecular-design of an organic compound. Owing to these advantages, photo electronics and electronics which use a functional organic material have been attracting attention in recent years.For example, a solar cell, a light-emitting element, an organic transistor, and the like are exemplified as electronic devices utilizing an organic compound as a functional material. These are devices taking advantage of electric properties and optical properties of the organic compound. Among ...

Подробнее
Номер записи: 75
10-10-2013 дата публикации

SUBSTITUTED HYDROGENATED THIENO-PYRROLO[3,2-C]PYRIDINE, LIGANDS, A PHARMACEUTICAL COMPOSITION AND A METHOD FOR USING THE ABOVE

Номер: US20130267551A1
Автор: Ivachtchenko Alexandre Vasilievich, Mitkin Oleg Dmitrievich
Принадлежит: ALLA CHEM, LLC

The present invention relates to novel substituted tetrahydro-4H-thieno-pyrrolo[3,2-c]pyridines of the general formula 1, geometrical isomers, mixtures of geometrical isomers, and pharmaceutically acceptable salts thereof, 4. The compound of claim 1 , selected from the group consisting of2,7-dimethyl-4-(pyridyl-4-yl)-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.4(1),4-benzyl-2,7-dimethyl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.5(1),2,7-dimethyl-4-phenethyl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.6(1),(7-methyl-4-phenethyl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine-2-yl)-methanol 2.6(2),2,7-dimethyl-4-(3-fluorophenyl)-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.4(3),4-(3-methylbenzyl)-3-methyl-7-benzyl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.5(3),3,5,7-trimethyl-4-[2-(pyridin-3-yl)ethyl]-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.6(4),2-(2,7-dimethyl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridin-4-yl)-1-phenyl-ethanol 2.7(1),(E)-2,7-dimethyl-4-styryl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.8(1),(Z)-2,7-dimethyl-4-styryl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.9(1),2-(2,5,7-trimethyl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridin-4-yl)-1-(6-methylpyridin-3-yl)-ethanol 2.7(3),(E)-2-methyl-7-ethyl-4-(3-fluorostyryl)-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.8(3),(Z)-2-methyl-7-ethyl-4-(3-fluorostyryl)-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.9(3),2,7-dimethyl-4-phenylethyl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.10(1),2-methyl-7-(3-fluorobenzyl)-4-cinnamyl-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.11(1)(E)-3,7-dimethyl-4-[3-(n-tolyl)allyl]-5,6,7,8-tetrahydro-4H-thieno[2′,3′:4,5]pyrrolo[3,2-c]pyridine 2.11(2),(E)-2,7-dimethyl-4-[3-(3-chlorophenyl)allyl]-5,6, ...

Подробнее
Номер записи: 76
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, ...

Подробнее
Номер записи: 77
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 ...

Подробнее
Номер записи: 78
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. ...

Подробнее
Номер записи: 79
24-10-2013 дата публикации

Fused polycyclic heteroaromatic compound, organic thin film including the compound and electronic device including the organic thin film

Номер: US20130277657A1
Автор: Bang Lin Lee, Jeong Il Park, Ji Young Jung, Jong Won Chung
Принадлежит: SAMSUNG ELECTRONICS CO LTD

A low-molecular-weight fused polycyclic heteroaromatic compound, an organic thin film and an electronic device including the fused polycyclic heteroaromatic compound, include a compact planar structure in which six or more rings are fused together, and thereby exhibits high charge mobility, and furthermore, enables the use of a deposition process or a room-temperature solution process when applied to devices, therefore realizing improved processibility.

Подробнее
Номер записи: 80
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- ...

Подробнее
Номер записи: 81
24-10-2013 дата публикации

FUSED TRICYCLIC INHIBITORS OF MAMMALIAN TARGET OF RAPAMYCIN

Номер: US20130281474A1
Автор: Meng Zhaoyang, Reddy Panduranga Abdulla, Siddiqui M. Arshad
Принадлежит: Merck Sharp & Dohme Corp.

This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders. 2. The compound of wherein W is CRR; X is CRR claim 1 , NRor SO; Y is CRR claim 1 , CRNHRor NR; or a pharmaceutically acceptable salt thereof.3. The compound of wherein Ris hydrogen; or a pharmaceutically acceptable salt thereof.4. The compound of wherein Ris hydrogen; or a pharmaceutically acceptable salt thereof.5. The compound of wherein Ris heteroaryl wherein said heteroaryl is optionally substituted with one to three substituents independently selected from the group consisting of R claim 4 , halo and Calkyl; or a pharmaceutically acceptable salt thereof.6. The compound of wherein Ris pyridinyl or quinolinyl wherein said pyridinyl and quinolinyl groups are optionally substituted with one to three substituents independently selected from the group consisting of R claim 5 , halo and Calkyl; or a pharmaceutically acceptable salt thereof.7. The compound of wherein Ris aryl or heteroaryl claim 5 , wherein said heteroaryl group is optionally substituted with Calkyl; or a pharmaceutically acceptable salt thereof.9. A pharmaceutical composition comprising a pharmaceutically effective amount of the compound according to claim 1 , and a pharmaceutically acceptable carrier.10. A method for the treatment or prevention of proliferative disorders or cancer in a patient comprising the step of administering a therapeutically effective amount of the compound of to the patient. This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.The mammalian target ...

Подробнее
Номер записи: 82
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- ...

Подробнее
Номер записи: 83
07-11-2013 дата публикации

Use of Dithiine Derivatives in Crop Protection and the Protection of Materials

Номер: US20130296315A1
Автор: Benting Jurgen, SEITZ Thomas, Wachendorff-Neumann Urike
Принадлежит:

The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives. 3. (canceled)4. (canceled)5. (canceled)6. A method for protecting plants or materials from unwanted phytopathogenic fungi comprising administering a dithiine derivative of formula (I) according to to the plants claim 1 , parts of the plants claim 1 , or the materials in need of such protection claim 1 , or a combination thereof.7. A method for protecting plants or materials from unwanted microorganisms comprising administering a dithiine derivative of formula (I) according to to the plants claim 1 , parts of the plants claim 1 , or the materials in need of such protection claim 1 , or a combination thereof.8. A process for producing a composition for controlling unwanted microorganisms claim 1 , comprising mixing a dithiine derivative of formula (I) according to with extenders claim 1 , surface-active substances or a combination thereof.9. A method for treating a transgenic plant claim 1 , comprising applying a compound of formula (I) according to to the transgenic plant in need of such treatment.10. A composition comprising at least one dithiine derivative of formula (I) according to and at least one other active compound selected from the group consisting of insecticides claim 1 , attractants claim 1 , sterilants claim 1 , bactericides claim 1 , acaricided claim 1 , nematicides claim 1 , fungicides claim 1 , growth regulators claim 1 , herbicides claim 1 , fertilizers claim 1 , safeners and semiochemicals. The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly ...

Подробнее
Номер записи: 84
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- ...

Подробнее
Номер записи: 85
07-11-2013 дата публикации

C-17 bicyclic amines of triterpenoids with hiv maturation inhibitory activity

Номер: US20130296554A1
Автор: Alicia Regueiro-Ren, Jacob Swidorski, Jie Chen, Nicholas A. Meanwell, Ny Sin, Sing-Yuen Sit, Yan Chen, Zheng Liu
Принадлежит: Bristol Myers Squibb Co

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.

Подробнее
Номер записи: 86
14-11-2013 дата публикации

Photoelectric conversion device, photoelectric conversion device material, photosensor and imaging device

Номер: US20130299799A1
Автор: Katsuyuki Yofu, Kimiatsu Nomura, Mitsumasa Hamano, Tetsuro Mitsui
Принадлежит: Fujifilm Corp

A photoelectric conversion device comprising an electrically conductive film, an organic photoelectric conversion film, and a transparent electrically conductive film, wherein the organic photoelectric conversion film contains a compound represented by the following formula (1) and an n-type organic semiconductor: wherein each of R 1 and R 2 independently represents a substituted aryl group, an unsubstituted aryl group, a substituted heteroaryl group or an unsubstituted heteroaryl group, each of R 3 to R 11 independently represents a hydrogen atom or a substituent provided that an acidic group is excluded, m represents 0 or 1, n represents an integer of 0 or more, R 1 and R 2 , R 3 and R 4 , R 3 and R 5 , R 5 and R 6 , R 6 and R 8 , R 7 and R 8 , R 7 and R 9 , or R 10 and R 11 may be combined each other to form a ring, and when n is an integer of 2 or more, out of a plurality of R 7 's and R 8 's, a pair of R 7 's, a pair of R 8 's, or a pair of R 7 and R 8 may be combined each other to form a ring.

Подробнее
Номер записи: 87
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 ...

Подробнее
Номер записи: 88
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'} [{' ...

Подробнее
Номер записи: 89
28-11-2013 дата публикации

Charge Transporting Material, Organic Electroluminescent Element, Light Emitting Device, Display Device And Illumination Device

Номер: US20130313532A1
Автор: Sotoyama Wataru, WATANABE Kousuke, YAMAMOTO Yosuke
Принадлежит: UDC IRELAND LIMITED

[Problem] To provide a charge transporting material which allows for a low driving voltage and is superior in luminous efficiency and durability. 2. The charge transporting material according to claim 1 , which comprises a compound represented by the general formula (1-1) or the general formula (1-2).6. The charge transporting material according to claim 1 , wherein at least one of Lto Land Arto Arin the general formulae (1-1) to (1-3) contains an m-phenylene group.7. An organic electroluminescent element comprising a substrate; a pair of electrodes including an anode and a cathode claim 1 , disposed on the substrate; and an organic layer disposed between the electrodes claim 1 , wherein the organic layer contains the charge transporting material of .8. The organic electroluminescent element according to claim 7 , wherein the organic layer includes a light emitting layer containing a phosphorescence emitting material.9. The organic electroluminescent element according to claim 8 , wherein the light emitting layer contains the compound represented by any one of the general formula (1-1) to the general formula (1-3).12. A light emitting device comprising the organic electroluminescent element of .13. A display device comprising the organic electroluminescent element of .14. An illumination device comprising the organic electroluminescent element of . the present invention relates to a charge transporting material, an organic electroluminescent element, a light emitting device, a display device and an illumination device.Since organic electroluminescent elements (which may hereinafter also be referred to as “elements” or “organic EL elements”) are capable of high-luminance light emitting using low voltage driving, they have been actively researched and developed. The organic electroluminescent elements have a pair of electrodes and an organic layer between the pair of electrodes, and utilize, for light emitting, energy of the exciton generated as a result of ...

Подробнее
Номер записи: 90
28-11-2013 дата публикации

INHIBITORS OF BETA-SECRETASE

Номер: US20130317014A1
Автор: Dillard Lawrence W., Jia Lanqi, YUAN Jing, ZHENG Yajun
Принадлежит:

The present invention is directed to a compound represented by the following structural formula: 156-. (canceled)58. The method of claim 57 , wherein the disorder is selected from the group consisting of Alzheimer's disease claim 57 , cognitive impairment claim 57 , Down's Syndrome claim 57 , HCHWA-D claim 57 , cognitive decline claim 57 , senile dementia claim 57 , cerebral amyloid angiopathy claim 57 , degenerative dementia claim 57 , other neurodegenerative disorders claim 57 , and glaucoma.5963-. (canceled)66. The method of claim 65 , wherein X is —O— and Ris —H claim 65 , —Br claim 65 , —F claim 65 , (C-C)alkyl claim 65 , (C-C)cycloalkyl claim 65 , aryl claim 65 , heteroaryl claim 65 , phenoxy claim 65 , or benzyloxy claim 65 , each optionally substituted with 1 to 3 substituents independently selected from the group consisting of —F claim 65 , —Cl claim 65 , —Br claim 65 , —CN claim 65 , —OR claim 65 , —NRR claim 65 , —S(O)R claim 65 , —NRS(═O)R claim 65 , —C(═O)OR claim 65 , —C(═O)NRR claim 65 , —NRC(═O)R claim 65 , —C(═S)NRR claim 65 , —C(═O)R claim 65 , (C-C)alkyl claim 65 , (C-C)cycloalkyl claim 65 , (C-C)alkenyl claim 65 , halo(C-C)alkyl claim 65 , (C-C)alkylsulfonylaminoalkyl claim 65 , hydroxy(C-C)alkyl claim 65 , cyano(C-C)alkyl claim 65 , (C-C)alkylcarbonylamino(C-C)alkyl claim 65 , (C-C)alkoxy claim 65 , halo(C-C)alkoxy claim 65 , (C-C)alkoxy(C-C)alkyl and a heteroaryl group.68. The method of claim 67 , wherein ring A is tetrahydrofuran claim 67 , tetrahydropyran claim 67 , cyclopentane claim 67 , cyclohexane claim 67 , cycloheptane claim 67 , oxepane claim 67 , 1 claim 67 ,3-dioxane claim 67 , piperidine claim 67 , 6 claim 67 ,7 claim 67 ,8 claim 67 ,9-tetrahydro-5H-benzo[7]annulene claim 67 , 2 claim 67 ,3-dihydro-1H-indene claim 67 , tetrahydronaphthalene claim 67 , decahydronaphthalene claim 67 , 5 claim 67 ,6 claim 67 ,7 claim 67 ,8-tetrahydroquinoline claim 67 , 5 claim 67 ,6 claim 67 ,7 claim 67 ,8-tetrahydroisoquinoline claim 67 , 2- ...

Подробнее
Номер записи: 91
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, ...

Подробнее
Номер записи: 92
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': ...

Подробнее
Номер записи: 93
05-12-2013 дата публикации

DICHALCOGENOBENZODIPYRROLE COMPOUND

Номер: US20130323913A1
Автор: Matsumoto Mitsuhiro, Miyata Yasuo
Принадлежит: Sumitomo Chemical Company, Limited

A dichalcogenobenzodipyrrole compound represented by the formula (1): 2. The dichalcogenobenzodipyrrole compound according to claim 1 , wherein X and Y are a sulfur atom in said formula (1).3. The dichalcogenobenzodipyrrole compound according to claim 1 , wherein Rand Rare a hydrogen atom or a halogen atom and Rand Rare an alkyl group having 1 to 30 carbon atoms claim 1 , an aryl group having 7 to 30 carbon atoms or a heteroaryl group having 5 to 30 carbon atoms claim 1 , wherein the aryl group and the heteroaryl group have an alkyl group optionally substituted by a fluorine atom or an alkoxy group optionally substituted by a fluorine atom in said formula (1).4. The dichalcogenobenzodipyrrole compound according to claim 1 , wherein Rand Rare a hydrogen atom in said formula (1).5. The dichalcogenobenzodipyrrole compound according to claim 1 , wherein Rto Rare a hydrogen atom or a halogen atom in said formula (1).6. The dichalcogenobenzodipyrrole compound according to claim 1 , wherein Rand Rare an aryl group having 7 to 26 carbon atoms having an alkyl group optionally substituted by a fluorine atom in said formula (1).7. The dichalcogenobenzodipyrrole compound according to claim 1 , wherein Rand Rare an alkyl group having 1 to 20 carbon atoms optionally having a fluorine atom in said formula (1).8. A film containing the dichalcogenobenzodipyrrole compound according to .9. A film composed of the dichalcogenobenzodipyrrole compound according to .10. An organic transistor containing the film according to .11. An organic semiconductor device containing the film according to .13. A composition containing the dichalcogenobenzodipyrrole compound according to and an organic solvent.14. A process for producing a film claim 13 , comprising a step of coating the composition according to on a substrate or an insulation layer and a step of drying the coated film coated on the substrate or insulation layer. The present invention relates to a dichalcogenobenzodipyrrole compound, a ...

Подробнее
Номер записи: 94
05-12-2013 дата публикации

NITROGEN-CONTAINING CONDENSED RING COMPOUND, NITROGEN-CONTAINING CONDENSED RING POLYMER, ORGANIC THIN FILM, AND ORGANIC THIN FILM ELEMENT

Номер: US20130324685A1
Автор: Aso Yoshio, Ie Yutaka, Ueda Masato, Ueta Masashi
Принадлежит:

It is an object of the present invention to provide a nitrogen-containing condensed ring compound, which can be used as an organic n-type semiconductor having an excellent electron transport property and which is also excellent in terms of solubility in an organic solvent. The nitrogen-containing condensed ring compound of the present invention has a structural unit represented by the following formula (1-1) or formula (1-2): 2. The nitrogen-containing condensed ring compound according to claim 1 , wherein claim 1 , in the formula (1-1) and the formula (1-2) claim 1 , Yand Yeach represent a single bond.3. The nitrogen-containing condensed ring compound according to claim 1 , wherein claim 1 , in the formula (1-1) and the formula (1-2) claim 1 , Arrepresents a benzene ring or a thiophene ring.4. The nitrogen-containing condensed ring compound according to claim 1 , wherein claim 1 , in the formula (1-1) and the formula (1-2) claim 1 , Zand Zeach represent a group represented by the formula (ii).5. The nitrogen-containing condensed ring compound according to claim 1 , wherein claim 1 , in the formula (1-1) and the formula (1-2) claim 1 , Wand Weach represent a group represented by —N═.8. The nitrogen-containing condensed ring polymer according to claim 7 , wherein claim 7 , in the formula (1-1) and the formula (1-2) claim 7 , Yand Yeach represent a single bond.9. The nitrogen-containing condensed ring polymer according to claim 7 , wherein claim 7 , in the formula (1-1) and the formula (1-2) claim 7 , Arrepresents a benzene ring or a thiophene ring.10. The nitrogen-containing condensed ring polymer according to claim 7 , wherein claim 7 , in the formula (1-1) and the formula (1-2) claim 7 , Zand Zeach represent a group represented by the formula (ii).11. The nitrogen-containing condensed ring polymer according to claim 7 , wherein claim 7 , in the formula (1-1) and the formula (1-2) claim 7 , Wand Weach represent a group represented by —N═.12. The nitrogen-containing ...

Подробнее
Номер записи: 95
05-12-2013 дата публикации

Organometallic Complex, Light-Emitting Element, Light-Emitting Device, Electronic Device, and Lighting Device

Номер: US20130324721A1
Автор: Inoue Hideko, SEO Hiromi, SEO Satoshi, Yamaguchi Tomoya
Принадлежит: SEMICONDUCTOR ENERGY LABORATORY CO., LTD.

Provided are a light-emitting element including a novel organometallic complex as an emission center, the organometallic complex, a light-emitting device, an electronic device, and a lighting device each using the light-emitting element. One embodiment of the present invention is a light-emitting element including, as an emission center, an organometallic complex in which a benzofuropyrimidine derivative is coordinated to a metal. In particular, another embodiment is a light-emitting element including, as an emission center, an organometallic complex in which a benzofuropyrimidine derivative having an aryl group at the 4-position is coordinated to a metal. Another embodiment is a light-emitting element including, as an emission center, an organometallic complex in which nitrogen at the 3-position of a benzofuropyrimidine derivative having an aryl group at the 4-position is coordinated to a metal and the aryl group is bonded to the metal. 1. A light-emitting element comprising an organometallic complex comprising a benzofuropyrimidine derivative , wherein the benzofuropyrimidine derivative is coordinated to a metal.2. The light-emitting element according to claim 1 , wherein the benzofuropyrimidine derivative has an aryl group at a 4-position.3. The light-emitting element according to claim 1 ,wherein the benzofuropyrimidine derivative has an aryl group at a 4-position,wherein nitrogen at a 3-position of the benzofuropyrimidine derivative is coordinated to the metal, andwherein the aryl group is bonded to the metal.4. The light-emitting element according to claim 1 , wherein the metal is a Group 9 element or a Group 10 element.5. The light-emitting element according to claim 1 , wherein the metal is iridium.6. A display device comprising the light-emitting element according to .7. An electronic device comprising the light-emitting element according to .8. A lighting device comprising the light-emitting element according to .15. A light-emitting element comprising the ...

Подробнее
Номер записи: 96
05-12-2013 дата публикации

Method of Synthesizing Pyrazine Derivative, and Light-Emitting Element, Light-Emitting Device, Electronic Device, and Lighting Device

Номер: US20130324729A1
Автор: Inoue Hideko, Kitano Yasushi, SEO Hiromi, SEO Satoshi, Yamaguchi Tomoya
Принадлежит: Semiconductor Energy Laboratory Co. Ltd.

A novel method in which a pyrazine derivative is synthesized without a synthetic pathway of a pyrazine halide derivative, which is a synthetic intermediate, whose pytazine skeleton is halogenated is provided. Furthermore, a light-emitting element, a light-emitting device, an electronic device, or a lighting device with high emission efficiency by using a pyrazine derivative obtained by the above synthesizing method as an EL material is provided. In the method, a pyrazine derivative is synthesized without a synthetic pathway of a pyrazine halide derivative, which is a synthetic intermediate, whose pytazine skeleton is halogenated. Specifically, a 2-arylpyrazine derivative having an aryl group or a heteroaryl group as a substituent is synthesized. 1. A method of synthesizing a 2-(haloaryl)pyrazine derivative , comprising the step of condensing and cyclizing an α-diketone and a 1-(haloaryl)ethane-1 ,2-diamine derivative.3. The method according to claim 2 , wherein Rand Rare bonded to each other to form a condensed ring.6. A method of synthesizing a 2-arylpyrazine derivative comprising an aryl group or a heteroaryl group claim 1 , comprising the step of coupling the 2-(haloaryl)pyrazine derivative according to and an arylboronic acid or a heteroarylboronic acid.8. The method according to claim 7 , wherein Rand Rare bonded to each other to form a condensed ring.10. A light-emitting device comprising a light-emitting element comprising the 2-arylpyrazine derivative according to .11. An electronic device comprising the light-emitting device according to .12. A lighting device comprising the light-emitting device according to .13. A method of synthesizing a 2-arylpyrazine derivative comprising an aryl group or a heteroaryl group claim 10 , comprising the step of coupling a 2-(haloaryl)pyrazine derivative and an arylboronic acid or a heteroarylboronic acid.15. The method according to claim 14 , wherein Rand Rare bonded to each other to form a condensed ring.17. The method ...

Подробнее
Номер записи: 97
19-12-2013 дата публикации

GERMOLE CONTAINING CONJUGATED MOLECULES AND POLYMERS

Номер: US20130334520A1
Автор: AMB CHAD MARTIN, Reynolds John R., So Franky
Принадлежит: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.

Embodiments of the invention are directed to Ge comprising heterocyclic compounds which can be used for the preparation of homopolymers and copolymers. The copolymers can be donor-acceptor (DA) alternating copolymers where the donor unit is a Ge comprising heterocyclic unit. The polymers can be used as materials in solar cells and other photovoltaic devices, transistors, diodes, light emitting devices (LEDs), conductors, supercapacitors, batteries, and electrochromic devices. 2. A polymer comprising a plurality of Ge comprising heterocyclic units from one or more of the Ge comprising heterocyclic compounds of claim 1 , wherein the Ge comprising heterocyclic unit comprises the Ge comprising heterocyclic compound absent the Z group.3. The polymer of claim 2 , wherein the polymer is a homopolymer having a plurality of the Ge comprising heterocyclic units of identical structure.4. The polymer of claim 2 , wherein the polymer is a copolymer having a plurality of at least two of the Ge comprising heterocyclic units.5. The polymer of claim 2 , wherein the polymer is a copolymer having a plurality of at least one of the Ge comprising heterocyclic units and at least one conjugated repeating unit comprising a substituted or unsubstituted claim 2 , ethenylene claim 2 , ethynylene claim 2 , phenylene claim 2 , naphthylene claim 2 , silacyclopentadithiophene claim 2 , benzothiadiazole claim 2 , thiadiazoloquinoxaline claim 2 , cyclopentadithiophene claim 2 , cyclopentadithiophene oxide claim 2 , benzoisothiazole claim 2 , benzothiazole claim 2 , thiophene oxide claim 2 , thienothiophene claim 2 , thienothiophene oxide claim 2 , dithienothiophene claim 2 , dithienothiophene oxide claim 2 , tetrahydroisoindole claim 2 , fluorene claim 2 , fluorenone claim 2 , thiazole claim 2 , selenophene claim 2 , silole claim 2 , thiazolothiazole claim 2 , cyclopentadithiazole claim 2 , naphthothiadiazole claim 2 , thienopyrazine claim 2 , oxazole claim 2 , imidazole claim 2 , pyrimidine claim ...

Подробнее
Номер записи: 98
19-12-2013 дата публикации

SUBSTITUTED TRICYCLIC COMPOUNDS AS FGFR INHIBITORS

Номер: US20130338134A1
Автор: He Chunhong, Lu Liang, Qian Ding-quan, Sun Yaping, Wu Liangxing, Xu Meizhong, Yao Wenqing, Zhang Colin, Zhuo Jincong
Принадлежит:

The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein W is O.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein W is NR.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H claim 1 , Calkyl claim 1 , Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 membered heterocycloalkyl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , (5-10 membered heteroaryl)-Calkyl claim 1 , or (4-10 membered heterocycloalkyl)-Calkyl claim 1 , wherein said Calkyl claim 1 , Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 membered heterocycloalkyl claim 1 , Caryl-Calkyl claim 1 , Ccycloalkyl-Calkyl claim 1 , (5-10 membered heteroaryl)-Calkyl claim 1 , and (4-10 membered heterocycloalkyl)-Calkyl are each optionally substituted with R.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H claim 1 , Calkyl claim 1 , Ccycloalkyl claim 1 , 4-10 membered heterocycloalkyl claim 1 , Caryl-Calkyl claim 1 , or Ccycloalkyl-Calkyl.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris methyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , where W is CRR.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare each independently selected from H claim 1 , halo claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Chaloalkyl claim 1 , Caryl claim 1 , Ccycloalkyl claim 1 , 5-10 membered heteroaryl claim 1 , 4-10 ...

Подробнее
Номер записи: 99
19-12-2013 дата публикации

THERAPEUTIC THIOPHENE-, FURAN-, AND PYRIDINE-FUSED AZOLOPYRIMIDIN-5-(6H)-ONES

Номер: US20130338139A1
Автор: Allan Amy, Branstetter Bryan, Breitenbucher James, Dyck Brian, Gharbaoui Tawfik, Gomez Laurent, Hudson Andrew Richard, Marrone Tami Jo, Vickers Troy, Weinhouse Michael I.
Принадлежит:

Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. 2. The compound of claim 1 , wherein M=1.3. The compound of claim 1 , wherein M=2.4. The compound of claim 1 , wherein one or more of R claim 1 , R claim 1 , R claim 1 , and Ris halomethyl.5. The compound of claim 1 , wherein{'sup': 1', '2, 'sub': 1', '6', '3, 'Ris H, and Ris C-Calkoxy, more specifically —OCH.'}6. The compound of claim 1 , whereinA is sulfur, and X is N.7. The compound of claim 1 , wherein{'sup': 1', '2, 'sub': 1', '6', '3', '2, 'Ris halo, more specifically F, Cl, or Br, and Ris C-Calkoxy, more specifically, —CFor —CHF.'}8. The compound of claim 1 , wherein{'sup': 3', '4, 'sub': 1', '6, 'Ris C-Calkyl, more specifically methyl, and Ris H; or'}{'sup': 3', '4', '10', '11', '12', '13, 'sub': 1', '6', '1', '3', '0-3, 'Ris C-Calkyl, more specifically C-Calkyl, and Ris —(CRR)NRR; or'}{'sup': 3', '4, 'Rand Rtaken together with the carbons to which they are attached form a six member monocyclic ring system, wherein D is a nitrogen atom.'}9. The compound ofor a pharmaceutically acceptable salt thereof, wherein{'sup': 1', '2, 'sub': 1', '3', '1', '3', '1', '3', '2', '2', '1', '3', '2', '1', '3', '2', '1', '3', '1', '3', '2, 'each occurrence of Rand Ris independently selected from —H, halo, —CN, —C-Calkyl, —C-Chaloalkyl, —OH, —C-Chaloalkoxy, —NO, —SOC-Calkyl, —SON(C-Calkyl), —CONH(C-Calkyl), and —CON(C-Calkyl);'}{'sup': 1', '2, 'or Rand Rare on adjacent carbons and taken together with the carbons to which they are attached form a 5-6 member monocylic ring system comprising one or more oxygen atoms, wherein the ring system is optionally substituted with one or more F;'}{'sup': 3', '4', '10', '11', '12', '13, 'sub': 1', '3', '1', '6', '3', '2', '1', '3', '3', '2', '2', '1', '3', '2 ...

Подробнее
Номер записи: 100