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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 1237. Отображено 100.
25-04-2013 дата публикации

BIARYL OXYACETIC ACID COMPOUNDS

Номер: US20130102609A1
Автор: Babu Suresh, Dong Guizhen, Duo Jingqi, Ho Koc-Kan, Le Thuy X.H., Mcguinness Brian F., Saionz Kurt W.
Принадлежит: LIGAND PHARMACEUTICALS INC.

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 2. A compound or salt according to wherein R claim 1 , R claim 1 , Rand Rare each independently selected from hydrogen and methyl.3. (canceled)4. A compound or salt according to claim 1 , wherein Ris selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl and isopropyl.5. (canceled)6. A compound or salt according to claim 1 , wherein Ris selected from aryl and heteroaryl claim 1 , each optionally substituted with one to four substituents independently selected from halogen claim 1 , cyano claim 1 , (C-C) haloalkyl claim 1 , (C-C) alkoxy claim 1 , (C-C) haloalkoxy claim 1 , (C-C) alkyl claim 1 , and (C-C) alkylsulfonyl.9. A compound or salt according to claim 8 , wherein Ris selected from hydrogen claim 8 , methyl claim 8 , fluoro claim 8 , chloro claim 8 , cyano claim 8 , —CFand methoxy; and Ris selected from hydrogen claim 8 , fluoro claim 8 , chloro claim 8 , methyl claim 8 , methoxy claim 8 , cyano claim 8 , —CFand —SOCH.10. A compound or salt according to wherein Rand Rare each independently selected from fluoro claim 9 , chloro claim 9 , methoxy and hydrogen.11. (canceled)13. A compound or salt according to wherein Ris selected from naphthyl claim 6 , pyridinyl and quinolinyl claim 6 , each optionally substituted with one to four substituents independently selected from halogen claim 6 , cyano claim 6 , (C-C) haloalkyl claim 6 , (C-C) alkoxy claim 6 , (C-C) haloalkoxy claim 6 , (C-C) alkyl and alkylsulfonyl.14. A compound or salt according to claim 1 , wherein Rand Rare each hydrogen.15. A compound or salt according to claim 1 , wherein A is selected from phenyl claim 1 , pyridinyl claim 1 , benzimidazolyl claim 1 , quinolinyl claim 1 , indolyl claim 1 , pyrimidinyl and imidazopyridinyl.16. A compound ...

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Номер записи: 1
09-05-2013 дата публикации

Triazolium carbene catalysts and processes for asymmetric carbon-carbon bond formation

Номер: US20130116445A1
Автор: Daniel Dirocco, Joseph Guiles, Tomislav Rovis
Принадлежит: COLORADO STATE UNIVERSITY RESEARCH FOUNDATION

Provided herein are chiral triazolium catalysts useful for asymmetric C—C bond formation and processes for their preparation. Also provided are synthetic reactions in which these catalysts are used, in particular, in asymmetric C—C bond formation.

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Номер записи: 2
30-05-2013 дата публикации

HETEROARYL (ALKYL) DITHIOCARBAMATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF

Номер: US20130136794A1
Автор: Cui Jingrong, GE Zemei, LI Runtao, Sun Xingyl, WANG Zhongqing, Yan Xu
Принадлежит: PEKING UNIVERSITY

Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer. 2. The compound according to claim 1 , wherein the group A is substituted or unsubstituted heterocyclic group claim 1 , is the heterocyclic group being selected from pyridyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , furyl claim 1 , oxazolyl claim 1 , pyrazolyl claim 1 , thiazolyl or oxadiazolyl; preferably the group A is substituted or unsubstituted pyridyl claim 1 , or pyridyl fused with benzene or morpholine ring claim 1 , the fused benzene or morpholine ring being unsubstituted or substituted with methyl.3. The compounds according to claim 2 , wherein the Calkyl is methyl claim 2 , the Calkoxy is methoxy claim 2 , the Calkoxycarbonyl is methoxycarbonyl claim 2 , and/or the Calkylamido is pentylamido .4. The compound according to claim 3 , wherein the Rgroup is cyano.5. The compound according to claim 1 , wherein the compound is:3-(furan-2-ylmethyl)-4-hydroxy-1,3-thiazinane-2-thione (compound 1);2-(methoxycarbonyl)ethyl(furan-2-ylmethyl)dithiocarbamate (compound 2);2-cyanoethyl(furan-2-ylmethyl)dithiocarbamate (compound 3);3-(furan-2-ylmethyl)-4-hydroxy-4,5-dimethyl-3,4-dihydro-2H-1,3-thiazine-2-thione (compound 4);2-sulfamoylethyl(furan-2-ylmethyl)dithiocarbamate (compound 5);2-boronoethyl(furan-2-ylmethyl)dithiocarbamate (compound 6);2-(methylsulfinyl)ethyl(furan-2-ylmethyl)dithiocarbamate (compound 7);2-(benzylsulfinyl)ethyl(furan-2-ylmethyl)dithiocarbamate (compound 8);4-hydroxy-3-(pyridin-3-ylmethyl)-1,3-thiazinane-2-thione ( ...

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Номер записи: 3
30-05-2013 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20130137699A1
Автор: Dawson Marcia, Fontana Joseph A., Xia Zebin
Принадлежит:

The invention provides compounds of formula I or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for inducing apoptosis or treating cancer using compounds of formula I. 2. The compound of wherein Zis N claim 1 , Zis CR claim 1 , Zis CRand Zis N.3. The compound of wherein Zis CR claim 1 , Zis CR claim 1 , Zis CRand Zis N.4. The compound of wherein Ris H or halo.56-. (canceled)7. The compound of wherein Zis CR claim 1 , Zis N claim 1 , Zis CRand Zis N.89-. (canceled)10. The compound of wherein Zis CR claim 1 , Zis CR claim 1 , Zis N and Zis N.1112-. (canceled)13. The compound of wherein Zis CR claim 1 , Zis N claim 1 , Zis CRand Zis CR.1416-. (canceled)17. The compound of wherein Zis CR claim 1 , Zis N claim 1 , Zis N and Zis CR.1819-. (canceled)20. The compound of wherein Ris adamantyl wherein any adamantyl of Rmay be optionally substituted with one or more groups selected from —OH and oxo(═O).2123-. (canceled)24. The compound of claim wherein Ris —OH or —OC(═O)R.2527-. (canceled)28. The compound of wherein Ris H or (C-C)alkoxy.2931-. (canceled)32. The compound of wherein Rand Rtogether with the atoms to which they are attached form a alkylenedioxy ring claim 1 , wherein the alkylenedioxy ring is optionally substituted is with one or more (C-C)alkyl.33. (canceled)34. The compound of wherein A is —CR═CR—.35. (canceled)36. The compound of wherein Ris H or (C-C)alkyl.37. (canceled)39. A composition comprising a compound as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable diluent or carrier.40. (canceled)41. A method for inducing apoptosis or cell death in a mammal in need of such treatment comprising administering to the mammal an effective amount of a compound as described in claim 1 , or a ...

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Номер записи: 4
06-06-2013 дата публикации

CO-CRYSTAL INTERMEDIATES OF ROSUVASTATIN AND METHODS OF USING SAME

Номер: US20130143890A1
Автор: Castellin Andrea, De Mier Jordi, Ferrari Clark, Galvagni Marco, Rafecas Llorenç, Tesson Nicolas
Принадлежит: F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.

Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions. 2. The method of claim 1 , wherein Rosuvastatin is a calcium salt.3. The method of wherein step (a) further comprises the addition of a conformer to a solution of Rosuvastatin in Toluene claim 1 , MIK or water.4. The method of wherein step (a) is performed at a temperature below about 40° C.5. A co-crystal of Rosuvastatin selected from the group consisting of:Rosuvastatin 2-aminopyrimidine hemihydrate,Rosuvastatin pyrazine hydrate,Rosuvastatin quinoxaline (1:2).6. The co-crystal of Rosuvastatin of comprising Rosuvastatin 2-aminopyrimidine hemihydrate.7. The co-crystal of Rosuvastatin of having a Powder X-Ray Diffractogram (PXRD) with characteristic peaks expressed in 2 Theta value of: 9.40 (vs) claim 6 , 13.50 (s) claim 6 , 14.08 (m) claim 6 , 15.15 (m) claim 6 , 18.59 (m) claim 6 , 21.67 (m) claim 6 , 22.16 (m) claim 6 , 22.21 (m) claim 6 , 22.66 (m) claim 6 , (+/−) 0.10; wherein (vs)=very strong intensity claim 6 , (s)=strong intensity claim 6 , and (m)=medium intensity.8. The co-crystal of Rosuvastatin of having a melting point of about 109.4° C.9. A method for treating conditions associated with hypercholesterolemia comprising administering a co-crystal of Rosuvastatin according to .10. The method of wherein the co-crystal of Rosuvastatin is the co-crystal Rosuvastatin pyrazine hydrate.11. A pharmaceutical composition comprising the co-crystal of Rosuvastatin according to and one or more pharmaceutically acceptable excipients claim 5 , carriers and/or diluents. This application claims priority to and benefit of European Patent Application No. 11192188.8 filed Dec. 6, 2011, the contents of which are incorporated by reference in their entirety.The present invention ...

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Номер записи: 5
01-08-2013 дата публикации

PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF LEFT VENTRICULAR DIASTOLIC DYSFUNCTION COMPRISING AN APOLIPOPROTEIN PEPTIDE/PHOSPHOLIPID COMPLEX

Номер: US20130197226A1
Автор: Busseuil David, RHÉAUME Eric, TARDIF Jean-Claude
Принадлежит:

The present invention features pharmaceutical compositions and methods of using the pharmaceutical compositions for treating left ventricular diastolic dysfunction. In particular, the pharmaceutical compositions include an apolipoprotein complex comprising a lipid fraction and a protein fraction. 137-. (canceled)38. A pharmaceutical composition comprising Dalcetrapib (Propanethioic acid , 2-methyl- , S-[2-[[[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino]phenyl]ester) for the treatment of LVDD.39. A pharmaceutical composition for the treatment of LVDD comprising a compound selected from the group consisting of:S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2,2-dimethylthiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2-acetylamino-3-phenylthiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]3-pyridinethiocarboxylate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]chlorothioacetate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]methoxythioacetate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]thiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]phenoxy-thioacetate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2-methylthiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]-4-chlorophenoxythioacetate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]cyclopropanethiocarboxylate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2-acetylamino-4-carbamoylthiobutyrate;S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl]2-hydroxy-2-methylthiopropionate;S-[2-(1-isopentylcyclopentanecarbonylamino)phenyl]2,2-dimethylthiopropionate;S-[2-(1-isopentylcyclopentanecarbonylamino)phenyl]thioacetate;S-[4,5-dichloro-2-(1-isopentylcyclohexanecarbonylamino)-phenyl]2,2-dimethylthiopropionate;S-[4,5-dichloro-2-(1-isopentylcyclopentanecarbonylamino)-phenyl]2,2-dimethylthiopropionate;S-[2-(1-isopentylcyclohexanecarbonylamino)-4-trifluoromethylphenyl]2,2-dimethylthiopropionate;O-methyl S-[2-(1-isopentylcyclohexanecarbonylamino)phenyl ...

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Номер записи: 6
15-08-2013 дата публикации

Method for determining odor when using a self-tanning agent

Номер: US20130210159A1
Автор: Masayuki Yabuki, Miki Takahashi
Принадлежит: Kao Corp

A method for evaluating an odor generated when using a self-tanning agent, wherein at least one compound selected from pyrazine compounds represented by the following general formula (1) is used as an indicator substance: wherein R 1 represents a methyl group, an ethyl group or an acetyl group, and R 2 , R 3 and R 4 independently represent a hydrogen atom or a methyl group.

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Номер записи: 7
22-08-2013 дата публикации

NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS

Номер: US20130217660A1
Автор: Clements Matthew J., Debenham John S., Graham Thomas H., Shen Dong-Ming, Zhang Yong
Принадлежит:

Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders. 2. The compound of wherein R claim 1 , R claim 1 , and Rare hydrogen; or a pharmaceutically acceptable salt thereof.4. The compound of wherein Ris phenyl claim 1 , wherein phenyl is unsubstituted or substituted with one to three substituents selected from R; or a pharmaceutically acceptable salt thereof.9. The compound of wherein Ris —C(O)—(CH)N(R)and Ris hydrogen; or Rand Rform a morpholine ring; or a pharmaceutically acceptable salt thereof.10. The compound of wherein q is 0 or 1; or a pharmaceutically acceptable salt thereof.12. The compound of wherein{'sup': '1', 'claim-text': (1) hydrogen,', {'sub': 2', '1-6, '(2) —COCalkyl,'}, {'sub': 2', 'p, '(3) —C(O)—(CH)-halogen,'}, {'sub': 2', 'p', '2, 'sup': 'f', '(4) —C(O)—(CH)N(R),'}, {'sub': 2', 'p', '2-6, '(5) —C(O)—(CH)—Ccycloheteroalkyl,'}, {'sub': 2', 'p, '(6) —C(O)—(CH)-heteroaryl, and'}, {'sub': 2', '2-3', '1-6, '(7) —(CH)—O—Calkyl,'}], 'Ris independently selected from the group consisting of{'sub': '2', 'sup': 'b', 'wherein each CH, alkyl, cycloheteroalkyl, and heteroaryl is unsubstituted or substituted with one to two groups independently selected from R;'}{'sup': '2', 'claim-text': (1) hydrogen,', {'sub': '1-6', '(2) —Calkyl, and'}, {'sub': '1-6', '(3) —Calkoxy,'}], 'Ris selected from the group consisting of{'sup': 'c', 'wherein each alkyl and alkoxy is unsubstituted or substituted with one to four substituents selected from R, or'}{'sup': 1', '2, 'sub': '1-3', 'Rand Rform a morpholine ring, wherein the morpholine ring is unsubstituted or substituted with —Calkyl and oxo;'}{'sup': 3', '4', '5, 'R, R, and Rare hydrogen;'}{'sup': '6', 'claim-text': [{'sub': 2 ...

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Номер записи: 8
05-09-2013 дата публикации

ARYLOXYUREA COMPOUND AND PEST CONTROL AGENT

Номер: US20130231479A1
Автор: Furukawa Hironori, HANAI Daisuke, Nakamura Takehiko, Tamai Tetsuo
Принадлежит:

The present invention provides a pest control agent, acaricide or fungicide that contains, as the active ingredient thereof, at least one type of compound selected from the aryloxyurea compounds represented by formula (V) (wherein Rto Reach independently represents an alkyl group or the like, X is a halogen atom or the like, n is an integer of 0 to 5, and Z is an oxygen atom or sulfur atom) or salts thereof. 3. A pest control agent claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.4. An acaricide claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.5. A fungicide claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.6. A pest control agent claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.7. An acaricide claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.8. A fungicide claim 2 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient. The present invention relates to a novel pest control agent. More specifically, the present invention relates to an aryloxyurea compound, which is superior in acaricidal activity and/or fungicidal activity, superior in properties and safety, and which can be industrially and advantageously synthesized, and an acaricide and/or fungicide including the aryloxyurea compound as an active ingredient.Priority is claimed on Japanese Patent Application No. 2010-229617, filed Oct. 12, 2010, the content of which is incorporated herein by reference.Compounds represented by formulas (A) to (E), which are structurally relevant to the compound of the present invention, are disclosed in Patent documents 1 to 5.In the formula, Rrepresents a C1-6 alkyl group.Rrepresents a hydrogen ...

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Номер записи: 9
19-09-2013 дата публикации

PYRAZINO[2,3-D]ISOXAZOLE DERIVATIVE

Номер: US20130245264A1
Автор: HANAKI Naoyuki, Murakami Takeshi, NAITOU Hiroyuki, NAKAMURA Kouki, WATANABE Katsuyuki
Принадлежит:

The object of the present invention is to provide a compound which is useful as a production intermediate of pyrazine carboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazine carboxamide. The present invention provides a pyrazino[2,3-d]isoxazole derivative represented by the formula (I): 2. The pyrazino[2 claim 1 ,3-d]isoxazole derivative according to claim 1 , wherein Y represents —C(═O)R where R represents an alkoxy group or an amino group claim 1 , and the alkoxy group and amino group may be optionally substituted.3. The pyrazino[2 claim 1 ,3-d]isoxazole derivative according to claim 1 , wherein X represents a hydroxyl group claim 1 , a chlorine atom or a fluorine atom.4. The pyrazino[2 claim 2 ,3-d]isoxazole derivative according to claim 2 , wherein X represents a hydroxyl group claim 2 , a chlorine atom or a fluorine atom.5. The pyrazino[2 claim 1 ,3-d]isoxazole derivative according to claim 1 , wherein X represents a fluorine atom or a chlorine atom claim 1 , and Y represents —C(═O)R where R represents an optionally substituted alkoxy group.6. The pyrazino[2 claim 1 ,3-d]isoxazole derivative according to claim 1 , wherein X represents a fluorine atom or a chlorine atom claim 1 , and Y represents —C(═O)R where R represents a methoxy group claim 1 , an ethoxy group claim 1 , an n-propoxy group claim 1 , an isopropoxy group claim 1 , or an n-butoxy group.10. The production method according to claim 8 , wherein X represents a fluorine atom and Y represents —C(═O)R where R represents an optionally substituted alkoxy group.11. The production method according to claim 9 , wherein X represents a fluorine atom and Y represents —C(═O)R where R represents an optionally substituted alkoxy group.12. The production method according to claim 8 , wherein X represents a fluorine atom and Y represents —C(═O)R where R represents a methoxy group claim 8 , an ethoxy group claim 8 , an n-propoxy group claim 8 , an isopropoxy group claim 8 , or an n-butoxy group.13. The ...

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Номер записи: 10
03-10-2013 дата публикации

PREPARATION OF C-PYRAZINE-METHYLAMINES

Номер: US20130261306A1
Автор: Mao Yunyu, Mulvihill Kristen Michelle, Rechka Josef A., Tavares-Greco Paula A.
Принадлежит: OSI PHARMACEUTICALS, LLC

A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis. 123-. (canceled)25. The process of claim 24 , wherein R1 is a carboxylate.26. The process of claim 24 , wherein R1 is —C(O)OCHor —C(O)OCHCH.27. The process of claim 24 , wherein R1 is H.30. The process of wherein R2 is methyl.31. The process of claim 29 , wherein in which at least about 0.5 mol of formula I is obtained in an overall yield for the process of at least about 50%.32. The process of claim 29 , wherein (a) is carried out in the presence of triethylamine or ethyldiisopropylamine.33. The process of claim 29 , wherein the base in (b) comprises potassium carbonate or cesium carbonate.34. The process of claim 29 , wherein (b) is carried out at a temperature of about 40-60° C.35. The process of claim 29 , wherein (c) is carried out in the presence of potassium hydroxide claim 29 , sodium hydroxide claim 29 , or lithium hydroxide.36. The process of claim 29 , wherein (c) is carried out in the presence of hydrochloric acid claim 29 , trifluoroacetic acid claim 29 , acetic acid claim 29 , or sulfuric acid.38. The process of claim 37 , wherein Reaction 2 is used to prepare the diaryl imine.39. The process of claim 24 , wherein R1 is a heteroaryl group selected from 2- claim 24 , 3- or 4-pyridinyl claim 24 , pyrazinyl claim 24 , 2- claim 24 , 4- claim 24 , or 5-pyrimidinyl claim 24 , pyridazinyl claim 24 , triazolyl claim 24 , tetrazolyl claim 24 , imidazolyl claim 24 , 2- or 3-thienyl claim 24 , 2- or 3-furyl claim 24 , pyrrolyl claim 24 , oxazolyl claim 24 , isoxazolyl claim 24 , thiazolyl claim 24 , isothiazolyl claim 24 , oxadiazolyl claim 24 , thiadiazolyl claim 24 , quinolyl claim 24 , isoquinolyl claim 24 , benzimidazolyl claim 24 , benzotriazolyl claim 24 , benzofuranyl claim 24 , or benzothienyl; and the heteroaryl group is ...

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Номер записи: 11
14-11-2013 дата публикации

HERBICIDAL COMPOUNDS

Номер: US20130303370A1
Автор: Avery Alaric James, DE MESMAEKER Alain, Mulholland Nicholas Phillip, WILLETTS Nigel James, Worthington Paul Anthony
Принадлежит:

The present invention provides a compound of formula (I) wherein Ris of sub-formula (a) or (b) and wherein the other substituents are as defined in the specification. The compounds of formula (I) are potentially useful as herbicides. 2. The compound of formula (I) according to claim 1 , wherein Rand Rare each independently hydrogen claim 1 , halogen claim 1 , C-Calkyl claim 1 , Cfluoroalky claim 1 , C-Calkoxy claim 1 , or Cfluoroalkoxy.3. The compound of formula (I) according to claim 1 , wherein Rand Rare each independently hydrogen claim 1 , fluorine claim 1 , chlorine claim 1 , methyl or ethyl4. The compound of formula (I) according to claim 1 , wherein Rand Rare each independently C-Calkyl claim 1 , C-C-fluoroalkyl claim 1 , C-Calkenyl claim 1 , C-C-fluoroalkenyl claim 1 , Cchloroalkenyl claim 1 , C-Calkynyl claim 1 , C-Ccycloalkyl claim 1 , C-Ccycloalkyl-CH— claim 1 , or phenyl.5. The compound of formula (I) according to claim 1 , wherein Rand Rare each independently methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , Cfluoroalkyl-CH— claim 1 , vinyl claim 1 , allyl claim 1 , Cfluoroalkenyl claim 1 , propargyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclopropyl-methyl- claim 1 , or phenyl.6. The compound of formula (I) according to claim 1 , wherein Ris of sub-formula (a) and claim 1 ,{'sup': 4a', '4e, 'sub': 1', '3', '1', '2', '3', '2', '2', '2, 'Rand Rare independently hydrogen, fluorine, chlorine, bromine, methyl, Cfluoroalkyl (e.g. CF), methoxy, Cfluoroalkoxy (e.g. CHFO, CFO or CHFO, in particular CHFO), or methyl-S(O)—;'}{'sup': 4b', '4c', '4d', '7, 'sub': 1', '4', '1', '2', '2', '2', '3', '5', '1', '3', '1', 'r', '3', '2', '2', '2', '1', '3', '2', '1', '3', '2', '2, 'R, Rand Rare independently hydrogen, halogen, C-Calkyl, Cfluoroalkyl, methoxymethyl-, MeOCHCHOCH—, C-Ccycloalkyl, C-Calkoxy, Cfluoroalkoxy, CCalkyl-S(O)—, HN—S(O)—, C-Calkyl-NH—S(O)—, or (C-Calkyl)N—S(O)—; phenyl or phenyl substituted by ...

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Номер записи: 12
09-01-2014 дата публикации

SYNTHESIS AND USE OF ANTI-TUMOR DRUG LQC-Y

Номер: US20140011786A1
Автор: Lei Haimin
Принадлежит:

Disclosed are the general structural formula of LQC-Y as well as the synthesis and use thereof. Pharmacological experiments demonstrated the marked antitumor effect of such compounds. Single day administration of LQC-Y3 to mice at a maximum dose of 6000 mg/kg showed no toxicity response during the 14-day continuous observation period, indicating the high safety of the compounds, and the compounds can be used to prepare medicaments for preventing and treating carcinomas such as liver cancer, lung cancer. In the general structural formula of LQC-Y, R represents steroid compounds such as cholic acid, deoxycholic acid, ursodeoxycholic acid, chenodeoxycholic acid, and hyodeoxycholic acid and so on; triterpenoid compounds such as oleanolic acid, ursolic acid, pachymic acid, glycyrrhetinic acid and glycosides thereof and so on; emodic acid, emodin and other mono-substituted or poly-substituted structures of anthraquinone parent nucleus; baicalein, baicalin and other flavonoid; shikimic acid, mono-substituted shikimic acid or poly-substituted shikimic acid; gardenia acid and other iridoid acid derivatives; paeonol, curcumin and structural derivatives thereof. 2. A method of treating a tumor disease comprising administering to a patient in need thereof an effective amount of a compound according to .4. The compound or the pharmaceutically acceptable salt thereof according to claim 3 , wherein the compound of formula 1 is an ester of R-acid with trimethyl pyrazine methanol claim 3 , and the R-acid is selected from the group consisting of cholic acid claim 3 , deoxycholic acid claim 3 , oleanolic acid claim 3 , glycyrrhetinic acid claim 3 , pachymic acid claim 3 , emodic acid and shikimic acid.5. The compound or the pharmaceutically acceptable salt thereof according to claim 3 , wherein the compound of formula 1 is an ether of R-phenol with trimethyl pyrazine methanol claim 3 , and R-phenol is one of chrysophanol or paeonol.9. The compound or the pharmaceutically acceptable ...

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Номер записи: 13
09-01-2014 дата публикации

Medicine for Treating Ischemic Brain Injury and its Sequelae, and Preparation Method Thereof

Номер: US20140011813A1
Автор: HONG Ying, Lei Haimin
Принадлежит: Haimin Lei

Disclosed in the present invention are a compound of the general structure formula LQC-T as shown below, wherein R represents an aromatic organic acid or phenol or the structural analogue thereof, such as protocatechuic acid, protocatechuic aldehyde, vanillic acid, gallic acid, caffeic acid, ferulic acid etc., and the synthesis and use of the compound. The compounds promote new blood vessel growth in the chick embryo chorioallantoic membrane, wherein LQC-T4 can be used to prepare a medicine for treating ischemic brain injury (stroke) and its sequelae. 2. A method of treating apoplexy caused by ischemic cerebral damage and the sequelae thereof comprising administering to a patient in need thereof an effective amount of a compound according to .4. The compound or the pharmaceutically acceptable salt thereof according to claim 3 , wherein Ris an alkyl which is substituted by pyrazine substituted by multiple methyls claim 3 , Ris an alkyl which is substituted by pyrazine substituted by multiple methyls claim 3 , Ris an alkoxycarbonyl which is substituted by pyrazine substituted by multiple methyls claim 3 , an alkenyl substituted by alkoxycarbonyl which is substituted by pyrazine substituted by multiple methyls claim 3 , or an aldehyde group.5. The compound or the pharmaceutically acceptable salt thereof according to claim 4 , wherein Ris a pyrazine methylene substituted by three methyls claim 4 , Ris a pyrazine methylene substituted by three methyls claim 4 , Ris a pyrazine methyleneoxy carbonyl which is substituted by three methyls claim 4 , an alkenyl substituted by alkoxycarbonyl which is substituted by pyrazine substituted by multiple methyls claim 4 , an aldehyde group.6. The compound according to claim 3 , wherein the compound is selected from the group consisting of:i) (3,5,6-trimethylpyrazin-2-yl)methyl 4-hydroxy-3-methoxybenzoate,ii) (3,5,6-trimethylpyrazine-2-yl)methyl-3,4-bis((3,5,6-trimethylpyrazine-2-yl)methoxy)benzoate,iii) (3,5,6-trimethylpyrazin-2-yl) ...

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Номер записи: 14
23-01-2014 дата публикации

METHOD FOR PRODUCING DICHLOROPYRAZINE DERIVATIVE

Номер: US20140024832A1
Автор: HARA Tamio, KANO Takuya, KURUSHIMA Hiroaki, NORIMATSU Naoki
Принадлежит: NIPPON SODA CO., LTD.

A method for producing a hydroxypyrazine derivative represented by formula (I) (wherein Rrepresents a halogen atom), the method including reacting a pyrazine derivative represented by formula (III) (wherein Rrepresents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group or a carboxyl group, M represents a cation capable of forming a salt, and n represents a number corresponding with the valence of M) with a halogenating agent. Also, a method for producing a dichloropyrazine derivative represented by formula (II) (wherein Rrepresents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group, a carboxyl group, or a group formed as a result of a change in the functional group of Rduring chlorination), the method including reacting the hydroxypyrazine derivative (I) with a chlorinating agent. According to the present invention, a dichloropyrazine derivative can be produced efficiently at low cost, and a hydroxypyrazine derivative that functions as a production intermediate for the dichloropyrazine derivative can be produced efficiently at low cost. 14-. (canceled)6. The method for producing a hydroxypyrazine derivative according to claim 5 , wherein M is a cation formed from a metal element belonging to group I claim 5 , group IIa or group Ma of a periodic table of elements. The present invention relates to a method for producing a dichloropyrazine derivative that is useful as an intermediate for an agrochemical or pharmaceutical product, and a method for producing a hydroxypyrazine derivative that functions as a production intermediate for the dichloropyrazine derivative.Priority is claimed on Japanese Patent Application No. 2009-016221, filed Jan. 28, 2009, the content of which is incorporated herein by reference.Compounds represented by formula (IV) below are known to be very effective against a variety of viruses, and particularly the influenza virus.(wherein Rrepresents a hydrogen atom or a halogen atom, ...

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Номер записи: 15
20-03-2014 дата публикации

Inhibitors of Histone Deacetylase

Номер: US20140080800A1
Автор: Haggarty Stephen, Holson Edward, Tsai Li-Huei, Wagner Florence Fevrier, Weiwer Michel, ZHANG YAN-LING
Принадлежит:

The present invention relates to compounds of formula (I): 5. The compound of or a pharmaceutically acceptable salt claim 4 , hydrate claim 4 , solvate claim 4 , or prodrug thereof claim 4 , wherein Ris selected from phenyl claim 4 , 2-pyridinyl claim 4 , 3-pyridinyl claim 4 , 4-pyridinyl claim 4 , 2-pyrimidinyl claim 4 , 4-pyrimidinyl claim 4 , 5-pyrimidinyl claim 4 , 2-pyrazinyl claim 4 , oxazolyl claim 4 , thiazolyl claim 4 , and isoxazolyl.12. A pharmaceutical composition comprising an effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or prodrug thereof and a pharmaceutical carrier claim 1 , diluent claim 1 , or excipient.13. A method of treating claim 1 , alleviating claim 1 , and/or preventing a condition wherein said condition is associated with histone deacetylase activity in a subject comprising administering to the subject in need thereof an effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate or prodrug thereof.14. The method of claim 13 , wherein the condition is selected from a neurological disorder claim 13 , memory loss or impairment claim 13 , cognitive function disorder or impairment claim 13 , extinction learning disorder claim 13 , fungal disease or infection claim 13 , inflammatory disease claim 13 , hematological disease claim 13 , and neoplastic disease.15. The method of claim 14 , wherein the condition is selected from:a cognitive function disorder or impairment associated with Alzheimer's disease, Huntington's disease, seizure induced memory loss, schizophrenia, Rubinstein Taybi syndrome, Rett Syndrome, Fragile X, Lewy body dementia, vascular dementia, ADHD, dyslexia, bipolar disorder and social, cognitive and learning disorders associated with autism, traumatic head injury, or attention deficit disorder, anxiety disorder, conditioned fear response, panic disorder, obsessive compulsive disorder, posttraumatic stress ...

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Номер записи: 16
03-04-2014 дата публикации

Compounds as S-Nitrosoglutathione Reductase Inhibitors

Номер: US20140094465A1
Автор: Qiu Jian, Stout Adam, Sun Xicheng
Принадлежит:

The present invention is directed to compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same. 1. What is claimed is: {'br': None, 'sub': 1', '2, 'HO-Cy-linker-Cy-acidic moiety\u2003\u2003Formula 1'}, 'A method of inhibiting GSNOR in a patient in need thereof by administering an effective amount of a compound of Formula 1 or a pharmaceutically acceptable salt thereofwherein{'sub': '1', 'Cyis selected from the group consisting of substituted and unsubstituted monocyclic aryl, substituted and unsubstituted bicyclic aryl, substituted and unsubstituted monocyclic heterocycle, substituted and unsubstituted bicyclic heterocycle, substituted and unsubstituted monocyclic heteroaryl, substituted and unsubstituted bicyclic heteroaryl, substituted and unsubstituted monocyclic cycloalkyl, and substituted and unsubstituted bicyclic cycloalkyl;'}{'sub': 2', '5', '6', '7', '2', '3', '2', '3', '2', '3', '5', '6', '1', '6', '1', '6', '1', '6', '7', '1', '6', '1', '6', '1', '6', '2', '3', '2', '3', '2', '3', '1', '3', '1', '3', '1', '3', '1', '8', '1', '8', '1', '8, 'linker is selected from the group consisting of a direct bond, O, S, SO, SO, C═O, CRR, NR, substituted and unsubstituted (C-C) alkyl, substituted and unsubstituted (C-C) heteroalkyl, substituted and unsubstituted (C-C) alkene, substituted and unsubstituted 5 or 6 membered aryl, substituted and unsubstituted 5 or 6 membered heteroaryl, substituted and unsubstituted 3-6 membered cycloalkyl, and substituted and unsubstituted 3-6 membered saturated heterocyclyl; wherein Rand Rare independently selected from the group consisting of hydrogen, (C-C) alkyl, (C-C) heteroalkyl, halogen, (C-C) haloalkyl, cyano, and hydroxyl; Ris selected from the group consisting of hydrogen, (C-C)alkyl, (C-C) haloalkyl, and (C-C) heteroalkyl; substitutions for the (C-C) alkyl, (C-C) heteroalkyl, and (C-C) alkene are selected from the group ...

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Номер записи: 17
15-01-2015 дата публикации

ANTIBACTERIAL AGENTS

Номер: US20150018331A1
Автор: Kaldor Stephen, Kasar Ramesh, Lu Qing, Moser Heinz E., Patten Phillip A., Patterson Brian D., WANG DAN
Принадлежит: Achaogen, Inc.

Antibacterial compounds of formula (I) are provided: 137-. (canceled)39. A compound of wherein A is —C(R claim 38 ,R)N(R claim 38 ,R).40. A compound of wherein A is —C(CH)NH.41. A compound of wherein A is —C(R claim 38 ,R)OR.42. A compound of wherein A is selected from the group consisting of:{'sub': 3', '10, '(1) substituted or unsubstituted C-C-cycloalkyl,'}(2) substituted or unsubstituted heterocyclyl, and(3) substituted or unsubstituted heteroaryl.44. (canceled)45. A compound of wherein G is selected from the group consisting of:(1) —C≡C—,(2) —C≡C—C≡C—,{'sup': 3G', '3G, '(3) —CR═CR—C≡C—, and'}{'sup': 3G', '3G, '(4) —C≡C—CR═CR—.'}46. A compound of wherein G is selected from the group consisting of:(1) —C≡C—,(2) —C≡C—C≡C—,(3) —CH═CH—C≡C—, and(4) —C≡C—CH═CH—.47. A compound of wherein G is —C≡C—.48. A compound of wherein G is —C≡C—C≡C—.49. A compound of wherein G is —CH═CH—C≡C—.50. (canceled)51. A compound of wherein G is —C≡C—CH═CH—.5257-. (canceled)58. A compound of wherein Ris H.59. A compound of wherein Y is substituted or unsubstituted aryl.60. A compound of wherein Y is substituted or unsubstituted phenyl.61. A compound of wherein Y is unsubstituted phenyl.62. (canceled)63. A compound of wherein D is substituted or unsubstituted heteroaryl.6467-. (canceled)68. A compound of wherein D is absent.6972-. (canceled)73. A compound of wherein L is absent.74. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier or diluent.75. A method for treating a subject with a gram-negative bacterial infection comprising administering to the subject in need thereof an antibacterially effective amount of a compound of or a pharmaceutical composition of .76. (canceled) This application is a continuation of U.S. patent application Ser. No. 12/635,551, filed Dec. 10, 2009, now pending, which is a continuation of International PCT Application No. PCT/US2008/066766, filed Jun. 12, 2008, which claims the benefit under 35 U.S.C. §119(e) of U.S. ...

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Номер записи: 18
28-01-2016 дата публикации

HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF

Номер: US20160024019A1
Автор: Beaumont Vahri, Beconi Maria, Bürli Roland W., Dominguez Celia, Haughan Alan F., Luckhurst Christopher A., Muñoz-Sanjuán Ignacio, Raphy Gilles, Thomas Beth, Wall Michael
Принадлежит:

Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein n is 1.5. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein each Ris independently C-Calkyl or C-Chaloalkyl.6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein each Ris independently methyl or trifluoromethyl.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 1.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein at least one Ris halo.10. The compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein at least one Ris fluoro.11. The compound of claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , wherein m is 1 claim 10 , and Ris 2-fluoro.13. A pharmaceutically acceptable composition comprising a pharmaceutically acceptable carrier and at least one compound of claim 1 , or a pharmaceutically acceptable salt thereof.14. A pharmaceutical composition of claim 13 , wherein the composition is formulated in a form chosen from tablets claim 13 , capsules claim 13 , powders claim 13 , liquids claim 13 , suspensions claim 13 , suppositories claim 13 , and aerosols.15. A method for treating a condition or disorder mediated by at least one histone deacetylase in a patient in need of such a treatment which method comprises administering to the patient a therapeutically effective amount of at least one compound of claim 1 , or a pharmaceutically acceptable salt thereof.16. A method for treating a condition or disorder responsive to inhibition of at least one histone deacetylase in a patient in need of such a treatment which method comprises administering to the patient an effective amount of at least one compound of claim 1 , or a pharmaceutically acceptable salt ...

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Номер записи: 19
17-04-2014 дата публикации

Benzamides

Номер: US20140107340A1
Автор: Chen Bin, Eldemenky Eman Mohammed, Hopper Allen T., Jessing Mikkel, Jiang Yu, Kilburn John Paul, Rasmussen Lars Kyhn
Принадлежит: H. Lundbeck A/S

The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor 2. The compound of claim 1 , wherein Ris optionally substituted phenyl.3. The compound of claim 1 , wherein Ris optionally substituted pyridyl.4. The compound of claim 1 , wherein Ris optionally substituted pyrazinyl.5. The compound of claim 1 , wherein Ris optionally substituted pyrimidyl.6. The compound of claim 1 , wherein Ris optionally substituted 5 membered heteroaryl.7. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted piperazinyl.8. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted piperidinyl.9. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted morpholinyl.10. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted pyrrolidinyl.11. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted pyrrolo.12. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted imidazo.13. The compound of anyone of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homomorpholinyl14. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homopiperidinyl15. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homopiperazinyl16. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted azetidinyl.17. The compound of claim 1 , wherein Ris chlorine claim 1 , methyl or trifluorormethyl.18. The compound of claim 1 ...

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Номер записи: 20
10-02-2022 дата публикации

OREXIN 1 RECEPTOR ANTAGONISTS

Номер: US20220041573A1
Автор: Brown Giles Albert, Bucknell Sarah Joanne, Christopher John Andrew, Congreve Miles Stuart, Mills Mark, PATEL ANIL, Stephenson Anne Mary, Swain Nigel Alan, TEHAN Benjamin Gerald
Принадлежит:

The disclosures herein relate to novel compounds of formula (I): and salts thereof, wherein W; X; Y; Z; R; R; Rand Rare defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors. 3. The compound according to or wherein X is CR.4. The compound according to wherein W is N.5. The compound according to or wherein Ris selected from H claim 3 , F claim 3 , OMe claim 3 , OCHF claim 3 , OCDor CHOMe.6. The compound according to or wherein W is CR.7. The compound according to wherein X is N.8. The compound according to or wherein Ris H claim 6 , Me claim 6 , CHOMe or OMe.9. The compound according to any one of - wherein Z is CH.10. The compound according to any one of - wherein Ris H.11. The compound according to any one of - wherein Ris a 1 claim 6 ,2 claim 6 ,3-triazole ring optionally substituted with one or more fluorine atoms; a pyrimidine ring optionally substituted with one or more fluorine atoms; or a pyrazine ring optionally substituted with one or more fluorine atoms.14. The compound according to any one of - wherein Ris H.15. The compound according to any one of - wherein Ris F.16. The compound according to or which is selected from the group consisting of:N-[(1S,2S)-2-[(4-fluorophenoxy)methyl]cyclopentyl]-2-(triazol-2-yl)benzamide;N-[(1S,2S)-2-[(4-fluorophenoxy)methyl]cyclopentyl]-5-methyl-2-pyrimidin-2-yl-benzamide;N-[(1S,2S)-2-[(4-fluorophenoxy)methyl]cyclopentyl]-5-methyl-2-(triazol-2-yl)benzamide;2-fluoro-N-[(1S,2S)-2-[(4-fluorophenoxy)methyl]cyclopentyl]-6-(triazol-2-yl)benzamide;N-[(1S,2S)-2-[(4-fluorophenoxy)methyl]cyclopentyl]-2-methoxy-6-(triazol-2-yl)benzamide;N-[(1S,2S)-2-[(4-chlorophenoxy)methyl]cyclopentyl]-2-methoxy-6-(triazol-2-yl)benzamide;N-[(1S,2S)-2-[dideuterio-(4-fluorophenoxy)methyl]cyclopentyl]-2-methoxy-6-(triazol-2-yl)benzamide;2-(difluoromethoxy)-N-[(1S,2S)-2-[(4-fluorophenoxy)methyl]cyclopentyl]-6-(triazol-2-yl)benzamide;N ...

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Номер записи: 21
23-01-2020 дата публикации

SUBSTITUTED DIHYDROINDENE-4-CARBOXAMIDES AND ANALOGS THEREOF, AND METHODS USING SAME

Номер: US20200024226A1
Автор: Cole Andrew G., DORSEY Bruce D., KAKARLA Ramesh, Kultgen Steven, Quintero Jorge
Принадлежит: Arbutus Biopharma Corporation

The present invention includes novel substituted bicyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention are capsid inhibitors. 2. The compound of claim 1 , wherein each occurrence of Ror Ris independently selected from the group consisting of —(CH)-(optionally substituted heteroaryl) claim 1 , —(CH)-(optionally substituted heterocyclyl) claim 1 , and —(CH)-(optionally substituted aryl).3. The compound of claim 1 , wherein each occurrence of optionally substituted alkyl claim 1 , optionally substituted heterocyclyl claim 1 , or optionally substituted cycloalkyl is independently optionally substituted with at least one substituent selected from the group consisting of C-Calkyl claim 1 , halo claim 1 , —OR claim 1 , optionally substituted phenyl claim 1 , optionally substituted heteroaryl claim 1 , optionally substituted heterocyclyl claim 1 , —N(R)C(═O)R claim 1 , —C(═O)NRR claim 1 , and —N(R)(R) claim 1 , wherein each occurrence of Ris independently H claim 1 , optionally substituted C-Calkyl claim 1 , optionally substituted C-Ccycloalkyl claim 1 , optionally substituted aryl claim 1 , or optionally substituted heteroaryl claim 1 , or two Rgroups combine with the N to which they are bound to form a heterocycle.4. The compound of claim 1 , wherein each occurrence of optionally substituted aryl or optionally substituted heteroaryl is independently optionally substituted with at least one substituent selected from the group consisting of C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Chaloalkoxy claim 1 , halo claim 1 , —CN claim 1 , —OR claim 1 , —N(R)(R) claim 1 , —NO claim 1 , —S(═O)N(R)(R) claim 1 , acyl claim 1 , and C-Calkoxycarbonyl claim 1 , wherein each occurrence of Ris independently H claim 1 , C-Calkyl claim 1 , or C-Ccycloalkyl.5. The compound of claim 1 , wherein each occurrence of optionally ...

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Номер записи: 22
04-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160029635A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

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Номер записи: 23
04-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160029636A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 15-. (canceled)6. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).7. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 38 , 1 claim 38 ,2-dichloropropane claim 38 , 1 claim 38 ,3-dichloropropene claim 38 , 1-methylcyclopropene claim 38 , 1-naphthol claim 38 , 2-(octylthio)ethanol claim 38 , 2 claim 38 ,3 claim 38 ,5-tri-iodobenzoic acid claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-dimethylammonium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-lithium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-potassium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-sodium claim 38 , 2 claim 38 ,4 claim 38 ,5-T claim 38 , 2 claim 38 ,4 claim 38 ,5-T-2-butoxypropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-2-ethylhexyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-3-butoxypropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-TB claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butometyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butotyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isobutyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isoctyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isopropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-methyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-pentyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-sodium claim 38 , 2 claim 38 ,4 claim 38 ,5-T-triethylammonium claim 38 , 2 claim 38 ,4 claim 38 ,5-T-trolamine claim 38 , 2 claim 38 ,4-D claim 38 , 2 claim 38 , ...

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Номер записи: 24
29-01-2015 дата публикации

Volatile dihydropyrazinly and dihydropyrazine metal complexes

Номер: US20150030782A1
Автор: Ivanov Sergei Vladimirovich, Lei Xinjian, Norman John Anthony Thomas
Принадлежит: AIR PRODUCTS AND CHEMICALS, INC.

A composition comprising dihydropyrazinyl anions that can be coordinated as 6 electron ligands to a broad range of different metals to yield volatile metal complexes for ALD and CVD depositions are described herein. Also described herein are undeprotonated dihydropyrazines that can coordinate to metals as stabilizing neutral ligands. In one embodiment, the composition is used for the direct liquid injection delivery of the metal dihydropyrazinyl complex precursor to the chamber of an ALD or CVD chamber for the deposition of metal-containing thin films such as, for example, ruthenium or cobalt metal films. 4. A method for forming a metal oxide film on a substrate wherein the film comprises a thickness , the method comprising:a. introducing a metal dihydopyrazinyl complex comprising at least one selected from a Formula 3A, 3B, 3C, 3D, 3E, 3F, 3G, 3H compound or combinations thereof;b. chemisorbing the metal dihydopyrazinyl complex onto the substrate;c. purging away the a metal dihydopyrazinyl complex using a purge gas;d. providing an oxygen source to the metal dihydopyrazinyl complex onto the heated substrate to react with the sorbed metal dihydopyrazinyl complex containing composition; ande. optionally purging away any unreacted oxygen source.5. The method of wherein steps a. through d. and optional step e. are repeated until the thickness of film is established.6. The method of wherein the method is an atomic layer deposition process.7. The method of wherein the metal dihydopyrazinyl complex comprises at least one selected from ruthenium (pentamethylcyclopentadienyl)(2 claim 4 ,2-dihydro-3 claim 4 ,3-dimethyl-5 claim 4 ,6-diethyl pyrazinyl) claim 4 , cobalt(pentamethylcyclopentadienyl)(2 claim 4 ,2-dihydro-3 claim 4 ,3-dimethyl-5 claim 4 ,6-diethylpyrazine) claim 4 , ruthenium (2 claim 4 ,2-dihydro-3 claim 4 ,3-dimethyl-5 claim 4 ,6-diethylpyrazine)(benzene) claim 4 , and combinations thereof.8. A method for forming a metal film on a substrate wherein the film ...

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Номер записи: 25
04-02-2016 дата публикации

HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF

Номер: US20160031876A1
Автор: Allen Daniel R., Breccia Perla, Bürli Roland W., Dominguez Celia, Haughan Alan F., Hughes Samantha J., Jarvis Rebecca E., Luckhurst Christopher A., Maillard Michel, Muñoz-Sanjuán Ignacio, Penrose Stephen D., Saville-Stones Elizabeth A., Stott Andrew J., Vater Huw D., Wall Michael, Wishart Grant
Принадлежит:

Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. 5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —C(O)NH(OH).6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —N(OH)C(O)R.7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein Ris chosen from hydrogen and lower alkyl.8. The compound of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein Ris lower alkyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 1.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 2.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 3.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein claim 1 , for each occurrence claim 1 , Ris independently chosen from halo and lower alkyl.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl optionally substituted with 1 to 3 substituents independently chosen from halo claim 1 , alkyl claim 1 , cycloalkyl claim 1 , haloalkyl claim 1 , hydroxyl claim 1 , alkoxy claim 1 , and nitrile.15. The compound of claim 14 , or a pharmaceutically acceptable salt thereof claim 14 , wherein Ris phenyl optionally substituted with 1 to 3 substituents independently chosen from halo claim 14 , lower alkyl claim 14 , and haloalkyl.16. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ris chosen from phenyl claim 15 , 2-fluorophenyl claim 15 , 2-methyl claim 15 , 3-fluoro-2-methylphenyl and 2-methylphenyl.17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof ...

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Номер записи: 26
11-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160037778A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 140-. (canceled)41. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).42. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 73 , 1 claim 73 ,2-dichloropropane claim 73 , 1 claim 73 ,3-dichloropropene claim 73 , 1-methylcyclopropene claim 73 , 1-naphthol claim 73 , 2-(octylthio)ethanol claim 73 , 2 claim 73 ,3 claim 73 ,5-tri-iodobenzoic acid claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-dimethylammonium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-lithium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-potassium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-ethylhexyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-3-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-TB claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butomethyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butotyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isobutyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isoctyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isopropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-methyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-pentyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-triethylammonium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-trolamine claim 73 , 2 claim 73 ,4-D claim 73 , 2 claim ...

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Номер записи: 27
11-02-2016 дата публикации

Pesticidal compositions and processes related thereto

Номер: US20160037779A1
Автор: Akshay PATNY, Gerald B. Watson, James E. Hunter, Joshodeep Boruwa, Pravin S. IYER, William C. Lo
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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Номер записи: 28
09-02-2017 дата публикации

TRIAZOLE AGONISTS OF THE APJ RECEPTOR

Номер: US20170035744A1
Автор: Chen Ning, Chen Xiaoqi, CHEN Yinhong, Cheng Alan C., Connors Richard V., DeBenedetto Mikkel V., Deignan Jeffrey, Dransfield Paul John, Du Xiaohui, Farrell Robert P., FU Zice, HEATH Julie Anne, Hedley Simon J., Horne Daniel, HOUZE Jonathan, Judd Ted C., Kaller Matthew R., KAYSER Frank, KHAKOO Aarif Yusuf, Kopecky David John, LAI Su-Jen, Ma Zhihua, McGee Lawrence R., MEDINA Julio C., MIHALIC Jeffrey T., Nishimura Nobuko, OLSON Steven H., Pattaropong Vatee, SWAMINATH Gayathri, Wang Xiaodong, Yang Kevin, YEH Wen-Chen
Принадлежит:

Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: 2. The compound of claim 1 , the salt thereof claim 1 , the tautomer thereof claim 1 , or the salt of the tautomer claim 1 , wherein Q′ is selected from a pyridinyl claim 1 , pyrimidinyl claim 1 , or pyrazinyl group that is unsubstituted or is substituted with 1 claim 1 , or 2 Rsubstituents.5. The compound of claim 4 , the salt thereof claim 4 , the tautomer thereof claim 4 , or the salt of the tautomer claim 4 , wherein R is a —CH6. The compound of claim 5 , the salt thereof claim 5 , the tautomer thereof claim 5 , or the salt of the tautomer claim 5 , wherein Ris a —C-Calkyl7. The compound of claim 6 , the salt thereof claim 6 , the tautomer thereof claim 6 , or the salt of the tautomer claim 6 , wherein R is a —CH8. The compound of claim 5 , the salt thereof claim 5 , the tautomer thereof claim 5 , or the salt of the tautomer claim 5 , wherein Ris a —O—(C-Calkyl).9. The compound of claim 8 , the salt thereof claim 8 , the tautomer thereof claim 8 , or the salt of the tautomer claim 8 , wherein Ris selected from —O—CH claim 8 , —O—CHCH claim 8 , or —O—CH(CH).10. The compound of claim 1 , the salt thereof claim 1 , the tautomer thereof claim 1 , or the salt of the tautomer claim 1 , wherein R is a —CH11. The compound of claim 1 , the salt thereof claim 1 , the tautomer thereof claim 1 , or the salt of the tautomer claim 1 , wherein Ris a —C-Calkyl12. The compound of claim 11 , the salt thereof claim 11 , the tautomer thereof claim 11 , or the salt of the tautomer claim 11 , wherein R is a —CH13. The compound of claim 1 , the salt thereof claim 1 , the tautomer thereof claim 1 , or the salt of the tautomer claim 1 , wherein Ris a —O—(C-Calkyl).14. The compound of ...

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Номер записи: 29
09-02-2017 дата публикации

Metabotropic Glutamate Receptor Positive Allosteric Modulators (PAMS) and Uses Thereof

Номер: US20170036987A1
Автор: COSFORD Nicholas D. P., DHANYA Raveendra Panickar, SHEFFLER Douglas J.
Принадлежит:

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. 3. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sup': '1', 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'Lis absent, —CH—, —CHCH—, —CHCHCH—, or —CHCHCHCH—.'}4. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sup': '1', 'Lis absent.'}5. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sub': 1', '6, 'Z is halogen, or C-Calkyl.'}6. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sub': 3', '2', '3, 'Z is —CH, or —CHCH.'}9. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sup': 1', '4', '5, 'Ris —OH or —N(RR).'}10. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sup': '4', 'sub': 1', '6', '1', '6, 'X is —OH, —OR, C-Calkyl, or C-Cfluoroalkyl.'}11. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sup': 2', '4, 'sub': 1', '6', '1', '6, 'Ris hydrogen, halogen, —CN, —OH, —OR, substituted or unsubstituted C-Calkyl, or substituted or unsubstituted C-Cfluoroalkyl.'}12. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sup': '3', 'sub': 1', '6', '3', '6, 'Ris C-Calkyl, or C-Ccycloalkyl.'}13. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein:{'sup': '3', 'sub': 3', '2', '3', '2', '2', '3', '3', '2', '2', '2', '2', '3', '3', '2', '3', '2', '3', '2', '3', '3, 'Ris —CH, —CHCH, —CHCHCH, —CH(CH), —CHCHCHCH, —CH(CH)CHCH, —CHCH(CH), —C(CH), cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl.'}14. The compound of any one of - , or a pharmaceutically acceptable salt thereof , ...

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Номер записи: 30
18-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160044925A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 140-. (canceled)41. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).42. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 73 , 1 claim 73 ,2-dichloropropane claim 73 , 1 claim 73 ,3-dichloropropene claim 73 , 1-methylcyclopropene claim 73 , 1-naphthol claim 73 , 2-(octylthio)ethanol claim 73 , 2 claim 73 ,3 claim 73 ,5-tri-iodobenzoic acid claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-dimethylammonium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-lithium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-potassium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-ethylhexyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-3-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-TB claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butometyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butotyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isobutyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isoctyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isopropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-methyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-pentyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-triethylammonium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-trolamine claim 73 , 2 claim 73 ,4-D claim 73 , 2 claim ...

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Номер записи: 31
01-05-2014 дата публикации

METHOD FOR PREPARATION OF 5-SUBSTITUTED PYRIMIDINES

Номер: US20140121375A1
Автор: Vartak Ashish P., Vince Robert
Принадлежит: Regents of the University of Minnesota

The present invention provides a method to prepare 5-substituted pyrimidines by reacting a 5-acylpyrimidine with a suitable nucleophile to afford a 5-methanolpyrimidine, such as flurprimidol. 3. The method of wherein X is halo.4. The method of wherein X is Br or Cl.5. The method of wherein M in compound (III) is Mg(II) claim 1 , Zn(II) claim 1 , Mn(II) claim 1 , Cr(I) claim 1 , Sn(IV) or Li(I).6. The method of wherein Y in formula (IV) is methoxy.7. The method of wherein M in compound (V) is Zn.8. The method of wherein Ris aryl or (substituted)aryl.9. The method of wherein Ris (substituted)phenyl.10. The method of wherein the metal in the complexed metal is palladium claim 1 , nickel or iron.11. The method of wherein the metal is complexed with triphenyphosphine or acetylacetone.12. The method of wherein the catalyst is (PhP)Pd claim 11 , (PPh)NiClor Fe(acac).13. The method of wherein the compound of formula (VI) is oxidized with SeO claim 2 , KMnOor CrO.14. The method of wherein the solvate is THF or diethyl ether.15. The method of wherein Ris phenyl claim 1 , 4-trifluorophenyl claim 1 , 4-methoxyphenyl or 4-halophenyl or 4-trifluoromethylphenyl.16. The method of wherein Ris 4-chlorophenyl.17. The method of wherein Ris isopropyl claim 16 , halo-substituted phenyl or cyclopropyl.18. The method of wherein Ris 2-chlorophenyl or 3 claim 17 ,5-dichlorophenyl.19. The method of wherein Ris 4-trifluoromethylphenyl and Ris isopropyl.20. The method of wherein Ris 4-chlorophenyl or 4-fluorophenyl and Ris 2-chlorophenyl.21. The method of wherein Ris 4-methoxyphenyl and Ris cyclopropyl.22. The method of wherein Ris phenyl and Ris 3 claim 2 ,4-dichlorophenyl.24. The compound of wherein Z is FC—.25. The compound of wherein Z is Cl.26. The compound of wherein R is methoxy. This application claims priority to U.S. Provisional Patent Application Ser. No. 61/466,276 filed Mar. 22, 2011, which application is incorporated herein by reference.The 5-pyrimidinemethanol, flurprimidol (1, ...

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Номер записи: 32
25-02-2016 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20160052888A1
Автор: Dhar T.G. Murali, Dyckman Alaric J., Gilmore John L., Marcoux David, Xiao Hai-Yun, Xiao Zili, Yang Michael G.
Принадлежит:

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): 3. The compound according to claim 2 , having the structure of Formula (I) or a salt thereof claim 2 , wherein:{'sub': 1', '2, 'Ris —OH or —OP(O)(OH);'}{'sub': 2', '2a', '2b, 'Ris Ror R;'}{'sub': '2a', 'claim-text': [{'sub': 2', '3', '3', '2', '5', '3', '2', '2', '3', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '2', '2', '4', '2', '2', '4', '3', '2', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3, 'is —(CH)CH, —(CH)CH, —CHCH═CHCHCH, —CHCHCH═CHCHCH, —(CH)CH═CHCH, —(CH)CH═C(CH), —(CH)CH═CH, —(CH)CH═CHCH, —CH═C H(CH)CH, —CH═CH(CH)OCH, —CH═CHCHCHCH(CH), —CH═CHCHCHCHOCH, —CHCH═CHCH═CHCH, —CH═CHCHCHCH═CH, —CH═CH(phenyl) wherein said phenyl is substituted with —CH'}, {'sub': 3', '2', '1-3', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '2', '2', '1-2, 'or —OCH; —CH═CH(tetrahydropyranyl), —(CH)(phenyl) wherein said phenyl is substituted with zero to 2 substituents independently selected from F, I, —CH, —OCH, —OCHCH, —OCH(CH), and —CHC(O)N(CH); —(CH)(methyl imidazolyl), —(CH)(methyl pyrazolyl), —(CH)(pyridinyl) wherein said pyridinyl is substituted with zero to 1 substituent selected'}, {'sub': 3', '2', '2', '2', '2', '2', '2-3', '2', '2', '3-4', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '9', '3', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '3', '3', '2', '1-6', '3', '3', '2', '2', '3', '2', '2', '3', '3', '3', '2', '2', '2', '3, 'from —OCH; —(CH)(pyrimidinyl), —(CH)(quinolinyl), —(CH)(tetrahydropyranyl), —CHO(CH)CH, —CHOCHCHCH(CH), —CHOCHCHC(CH), —CHO(CH)CH, —CHOCHCHCHCF, —CHOCHCH═CHCHCH, —CHOCHCH═C(CH), —CHOCHCH═CHCHCHCH, — ...

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Номер записи: 33
25-02-2016 дата публикации

PYRIDINE- OR PYRAZINE-CONTAINING COMPOUNDS

Номер: US20160052893A1
Автор: Moser William H.
Принадлежит:

Described herein are selective bis-alkynyl pyrazines, bis-alkynyl pyridines, bispyridine substituted ellagic acid derivatives, and pyridine-substituted coumarin derivatives and methods of making thereof. 1(a) bis-alkynyl pyrazine and bis-alkynyl pyridines of the formulas:. A composition comprising a compound selected from the group consisting essentially of:{'sub': '3', 'wherein R is selected from H, CH, or the two adjacent R groups join to form a cyclohexane ring;'}{'sub': '3', 'wherein R is selected from H, CH, or the two adjacent R groups join to form a cyclohexane ring;'}(b) bispyridine substituted ellagic acid derivatives of the formulas:wherein X is a pyridyl group;wherein X is a pyridyl group; andwherein X is selected from a pyridyl group; and(c) pyridine-substituted coumarin derivatives of the formulas:wherein (i) X is a 4-pyridyl group and R″ is methylene, ethylene, or a propylene, or (ii) X is a 3-pyridyl group and R″ is a methylene;wherein X is a 4-pyridyl group and R″ is ethylene; andwherein X is a 4-pyridyl group and R″ is ethylene. Pyridine- or pyrazine-containing compounds are described along with their methods of making.Pyridine- and pyrazine-containing compounds are valued materials in the fields of organic synthesis, supramolecular chemistry, and materials science. The presence of the nitrogen atoms, with their accompanying lone pair of electrons, renders pyridines and pyrazines both basic and nucleophilic, and thus can be used as highly soluble bases or catalysts in a variety of organic transformations. Pyridines and pyrazines are also valuable as synthons in organic synthesis, and are particularly useful in the preparation of pharmaceuticals and agrochemicals due to their propensity towards high biological activity. Pyridines and pyrazines also serve as ligands in the chelation of a variety of metals and metal ions, and the resultant organometallic complexes of pyridines and pyrazines are utilized, for example, as catalysts in asymmetric organic ...

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Номер записи: 34
13-02-2020 дата публикации

COMPOSITIONS AND METHODS FOR MODULATING PROTEASE ACTIVITY

Номер: US20200048227A1
Автор: Chang Fang-Yuan, CLARDY Jon, Fischbach Michael A., Guo Chun-Jun, Voigt Christopher A., Wyche Thomas
Принадлежит:

Disclosed herein, inter alia, are compositions for modulating protease activity and treating cancer. 2. The compound claim 1 , of claim 1 , wherein when Ris —B(OH) claim 1 , Ris independently hydrogen claim 1 , —C(O)R claim 1 , or —C(O)—OR; and{'sup': '1C', 'sub': 3', '3', '3', '3', '2', '2', '2', '2', '2', '2', '2', '2, 'Ris hydrogen, —CF, —Cl, —CI, —CBr, —COOH, —CONH, —CHF, —CHCl, —CHI, —CHBr, —OCHF, —OCHCl, —OCHI, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl.'}312.-. (canceled)14. The compound of claim 1 , wherein Ris —C(O)H.15. The compound claim 1 , of claim 1 , wherein when Ris —C(O)H claim 1 , Ris —C(O)R claim 1 , or —C(O)—OR.1624.-. (canceled)34. The compound claim 1 , of claim 1 , wherein at least one N is N claim 1 , at least one C is C claim 1 , or at least one H is H.35. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable excipient.36. A method of treating cancer claim 1 , said method comprising administering to a subject in need thereof an effective amount of a compound of .37. A method of inhibiting cathepsin activity claim 1 , said method comprising: contacting the cathepsin with a compound of .38. (canceled)39. A method of reducing cathepsin activity claim 1 , said method comprising: contacting the cathepsin with a compound of .40. (canceled)41. (canceled)42. A method of inhibiting protease activity claim 1 , said method comprising: contacting the protease with a compound of .4345.-. (canceled) This application is the national stage filing under USC 371 of international application PCT/US2017/061840, filed Nov. 15, 2017, which claims the benefit of U.S. Provisional Application No. 62/426,012, filed Nov. 23, 2016, which are incorporated herein by reference in their entirety and for all purposes.This invention was made with government support under grant no. ...

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Номер записи: 35
20-02-2020 дата публикации

BENZAMIDES-CONTAINING COMPOUNDS AND THEIR USE IN THE TREATMENT OF DEPRESSION

Номер: US20200054630A1
Автор: Chen Bin, Eldemenky Eman Mohamed, Hopper Allen T., Jessing Mikkel, Jiang Yu, Kilburn John Paul, Rasmussen Lars Kyhn
Принадлежит:

The present invention is directed to benzamide-containing compounds of formula I 118-. (canceled)20. The method of claim 19 , wherein the depression is major depressive disorder (MDD) including mild claim 19 , moderate and severe depression.21. The method of claim 19 , wherein the depression is treatment-resistant depression.22. The method of claim 19 , wherein the depression is catatonic depression claim 19 , melancholic depression claim 19 , atypical depression claim 19 , psychotic depression claim 19 , postpartum depression. bipolar depression claim 19 , mild claim 19 , moderate or severe depression claim 19 , wherein bipolar depression includes bipolar I and bipolar II.23. The method of claim 19 , wherein the depression is associated with inflammatory disease.24. The method of claim 19 , wherein the compound is 2-chloro-N-[3-cyclopropyl-2-[2-(trifluoromethyl)pyrimidin-5-yl]propyl]benzamide or a pharmaceutically acceptable salt thereof.25. The method of claim 24 , wherein the depression is major depressive disorder (MDD) including mild claim 24 , moderate and severe depression.26. The method of claim 24 , wherein the depression is treatment-resistant depression.27. The method of claim 24 , wherein the depression is catatonic depression claim 24 , melancholic depression claim 24 , atypical depression claim 24 , psychotic depression claim 24 , postpartum depression. bipolar depression claim 24 , mild claim 24 , moderate or severe depression claim 24 , wherein bipolar depression includes bipolar I and bipolar II.28. The method of claim 24 , wherein the depression is associated with inflammatory disease.29. The method of claim 19 , wherein the compound is (−)2-chloro-N-[3-cyclopropyl-2-[2-(trifluoromethyl)pyrimidin-5-yl]propyl]benzamide or a pharmaceutically acceptable salt thereof.30. The method of claim 29 , wherein the depression is major depressive disorder (MDD) including mild claim 29 , moderate and severe depression.31. The method of claim 29 , wherein the ...

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Номер записи: 36
02-03-2017 дата публикации

BIPHENYL AND PHENYL-PYRIDINE AMIDES AS P2X3 AND P2X2/3 ANTAGONISTS

Номер: US20170057932A1
Автор: Broka Chris Allen, Hawley Ronald Charles
Принадлежит: Roche Palo Alto LLC

Compounds of the formula I: 2. The compound of wherein R claim 1 , Rand Rare hydrogen.3. The compound of wherein Ris pyrimidin-2-yl substituted at the 5-position with methyl or halo.4. The compound of wherein Ris 5-methyl-pyrimidin-2-yl.5. The compound of wherein Ris pyrimidin-2-yl substituted with halo at the 5-position.6. The compound of wherein Ris hydrogen.7. The compound of wherein Ris methyl.8. The compound of wherein Ris Calkyl claim 2 , hydroxy-Calkyl claim 2 , Calkylsulfanyl-Calkyl claim 2 , Calkylsulfonyl-Calkyl claim 2 , amino-Calkyl claim 2 , N—Calkyl-amino-Calkyl claim 2 , N claim 2 ,N claim 2 ,-di-Calkyl-amino-Calkyl claim 2 , Ccycloalkyl claim 2 , optionally substituted phenyl claim 2 , heteroaryl claim 2 , or heterocyclyl-Calkyl.9. The compound of wherein Ris Calkyloxy-Calkyl claim 8 , hydroxy-Calkyl claim 8 , heteroaryl or heterocyclyl-Calkyl.10. The compound of wherein Ris methoxymethyl.11. The compound of wherein Ris hydroxymethyl.12. The compound of wherein Ris heteroaryl selected from pyridinyl claim 9 , pyrimidinyl claim 9 , or pyrazinyl claim 9 , each of which may be optionally substituted once or twice with methyl.13. The compound of wherein Ris hydroxymethyl claim 9 , methoxymethyl claim 9 , pyrazin-2-yl or 5-methyl-pyrazin-2-yl.14. The compound of wherein Ris pyridazin-3-yl.15. The compound of wherein Ris pyridazin-3-yl substituted at the 6-position with methyl or halo.16. The compound of wherein Ris thienyl.17. A pharmaceutical composition comprising a compound of and at least one pharmaceutical acceptable carrier claim 1 , diluent or excipient.18. A method of modulating P2Xand P2Xreceptor activity in a subject claim 1 , said method comprising administering to a subject in need thereof an effective amount of a compound of .19. A method of wherein the subject suffers from a pain condition selected from the group consisting of poisoning claim 18 , neuritis claim 18 , neuralgias claim 18 , interstitial cystitis claim 18 , nerve injury claim ...

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Номер записи: 37
04-03-2021 дата публикации

GRAPHENE NANOSTRUCTURE

Номер: US20210061774A1
Автор: Tetsuka Hiroyuki
Принадлежит: KABUSHIKI KAISHA TOYOTA CHUO KENKYUSHO

A graphene nanostructure has a nanographene, a π conjugated functional group bonded to the nanographene via a pyrazine skeleton, and at least one Br group and/or at least one CN group introduced into the π conjugated functional group. A graphene nanostructure preferably has an average size of 1 nm or larger to 100 nm or smaller, a band gap of 0.01 eV or higher to 1.2 eV or lower, and/or a HOMO level of −6.0 eV or higher to −4.0 eV or lower. As the π conjugated functional group into which the Br group(s) and/or the CN group(s) are/is introduced, a 4-bromobenzene group, a 4,5-dibromobenzene group, a 5-bromopyridine group, a 5-bromopyrazine group, a benzonitrile group, a phthalonitrile group, or a 2,3-dicyanopyrazine group is desirable. 1. A graphene nanostructure , comprising:a nanographene;a π conjugated functional group bonded to the nanographene via a pyrazine skeleton; andat least one Br group and/or at least one CN group introduced into the π conjugated functional group.2. The graphene nanostructure according to claim 1 , wherein an average size is 1 nm or larger to 100 nm or smaller.3. The graphene nanostructure according to claim 1 , wherein a band gap is 0.01 eV or higher to 1.2 eV or lower.4. The graphene nanostructure according to claim 1 , wherein a HOMO level is −6.0 eV or higher to −4.0 eV or lower.5. The graphene nanostructure according to claim 1 , wherein the π conjugated functional group into which the Br group(s) and/or the CN group(s) are/is introduced is at least a functional group selected from the group consisting of a 4-bromobenzene group claim 1 , a 4 claim 1 ,5-dibromobenzene group claim 1 , a 5-bromopyridine group claim 1 , a 5-bromopyrazine group claim 1 , a benzonitrile group claim 1 , a phthalonitrile group claim 1 , and a 2 claim 1 ,3-dicyanopyrazine group.6. The graphene nanostructure according to used for a broadband optical sensor. The present invention relates to a graphene nanostructure, more specifically, a graphene nanostructure ...

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Номер записи: 38
15-03-2018 дата публикации

BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOALl AGENTS

Номер: US20180072760A1
Автор: Jacobs Robert T., Plattner Jacob J., Zhang Yong-Kang
Принадлежит:

This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. Formula (I) and (II) 4. A combination comprising the compound of claim 1 , together with at least one additional therapeutic agent.5. A pharmaceutical formulation comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a) the compound of ; and'}b) a pharmaceutically acceptable excipient.6. The pharmaceutical formulation of claim 5 , wherein the pharmaceutical formulation is a unit dosage form.7. The pharmaceutical formulation of claim 5 , wherein the salt of the compound of is a pharmaceutically acceptable salt.8. A method of killing and/or preventing the growth of a protozoa claim 1 , comprising: contacting the protozoa with an effective amount of the compound of claim 1 , thereby killing and/or preventing the growth of the protozoa.9Plasmodium. The method of claim 8 , wherein the protozoa is a member of the genus.10Plasmodium falciparum.. The method of claim 8 , wherein the protozoa is11. A method of treating and/or preventing a disease in an animal claim 1 , comprising: administering to the animal a therapeutically effective amount of the compound of claim 1 , thereby treating and/or preventing the disease.12. The method of claim 11 , wherein the disease is malaria.13. The method of claim 11 , wherein the animal is a human.14. A use of the compound of in the manufacture of a medicament for the treatment and/or prophylaxis of protozoal infection. This application claims the benefit of U.S. Provisional Patent Application No. 62/145,422, filed Apr. 9, 2015 and U.S. Provisional Patent Application No. 62/152,605, filed Apr. 24, 2015, which are incorporated by reference in their entirety for all purpose.The global rise of protozoa resistant to antimicrobials in general, poses a major threat. Deployment of ...

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Номер записи: 39
18-03-2021 дата публикации

SUBSTITUTED 6-MEMBERED ARYL OR HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS

Номер: US20210077511A1
Автор: Bell Ian M., CAMPBELL BRIAN T., Crowley Brendan M., Greshock Thomas J., Harvey Andrew John, Rada Vanessa L.
Принадлежит: Merck Sharp & Dohme Corp.

present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation. 3. The compound of any one of to , or a pharmaceutically acceptable salt thereof , wherein Y is H.4. The compound of any one of to , or a pharmaceutically acceptable salt thereof , wherein A is selected from pyridine , pyrimidine , phenyl , pyridazine , pyrazine , triazine , pyridinone , pyrimidinone , pyrazinone , and pyridazinone each substituted with 1 to 2 R groups independently selected from halogen , CN , (C-C)alkyl , O(C-C)alkyl , NRR , (C-C)cycloalkyl , aryl , heteroaryl and heterocyclyl , wherein said alkyl , NRR , (C-C)cycloalkyl , aryl , heteroaryl and heterocyclyl are optionally substituted with one or more substituents independently selected from halogen , CN , (C-C)alkyl , (C═O)O(C-C)alkyl and phenyl , wherein said alkyl is optionally substituted with one or more halogen.5. The compound of any one of to , or a pharmaceutically acceptable salt thereof , wherein R , R , Rand Rare independently H or methyl.6. The compound of any one of to , or a pharmaceutically acceptable salt thereof , wherein Rand Rare independently H , F , Si(CH)or methyl.7. The compound of any one of to , or a pharmaceutically acceptable salt thereof , wherein Rand Rare independently selected from H , (C-C)alkyl , cyclopentyl and phenyl wherein said alkyl and phenyl are optionally substituted with halogen or phenyl.9. The compound of having the formula Ia claim 8 , or a pharmaceutically acceptable salt thereof claim 8 , wherein;{'sub': 1', '6', '1', '6', '3', '1', '4', '1', '4, 'sup': 7', '8, 'A is selected from pyridine, pyrimidine, phenyl, pyridazine and pyrazine ...

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Номер записи: 40
19-03-2015 дата публикации

PYRIDINYL AMIDES AS P2X3 AND P2X2/3 INHIBITORS

Номер: US20150080408A1
Автор: Broka Chris Allen, Hawley Ronald Charles
Принадлежит: Roche Palo Alto LLC

Compounds of the formula I: 2. The compound of claim 1 , wherein R claim 1 , Rand Rare hydrogen.3. The compound of claim 2 , wherein Ris phenyl substituted at the 4-position with methyl or halo and optionally substituted at the 2-position with halo.4. The compound of claim 2 , wherein Ris 4-methyl-phenyl.5. The compound of claim 2 , wherein Ris pyridin 2-yl substituted with methyl or halo at the 5-position.6. The compound of claim 2 , wherein Ris 5-methyl-pyridin-2-yl.8. The compound of claim 7 , wherein Ris hydrogen.9. The compound of claim 7 , wherein Ris methyl.10. The compound of claim 7 , wherein Ris: Calkyl; Calkyloxy-Calkyl; hydroxy-Calkyl; Calkylsulfanyl-Calkyl; Calkylsulfonyl-Calkyl; amino-Calkyl; N—Calkyl-amino-Calkyl; N claim 7 ,N-di-Calkyl-amino-Calkyl; Ccycloalkyl; optionally substituted phenyl; heteroaryl claim 7 , or heterocyclyl-Calkyl.11. The compound of claim 7 , wherein Ris: Calkyloxy-Calkyl; hydroxy-Calkyl; heteroaryl claim 7 , or heterocyclyl-Calkyl.12. The compound of claim 7 , wherein Ris methoxymethyl.13. The compound of claim 7 , wherein Ris hydroxymethyl.14. The compound of claim 7 , wherein Ris heteroaryl selected from pyridinyl claim 7 , pyrimidinyl claim 7 , or pyrazinyl claim 7 , each of which may be optionally substituted once or twice with methyl.15. The compound of claim 7 , wherein Ris hydroxymethyl claim 7 , methoxymethyl claim 7 , pyrazin-2-yl or 5-methyl-pyrazin-2-yl.16. The compound of claim 7 , wherein Ris Calkyl claim 7 , Ccycloalkyl or Ccycloalkyl-Calkyl.17. The compound of claim 7 , wherein Ris isopropyl claim 7 , isobutyl or tert butyl.18. The compound of claim 1 , wherein said compound is selected from:4-Methyl-thiophene-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;5-Methyl-thiophene-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;Furan-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;Thiophene-2- ...

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Номер записи: 41
14-03-2019 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20190076450A1
Автор: Dhar T.G. Murali, Dyckman Alaric J., Gilmore John L., Marcoux David, Xiao Hai-Yun, Xiao Zili, Yang Michael G.
Принадлежит:

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): 116-. (canceled)19. The compound according to or a salt thereof claim 17 , wherein:{'sub': 2a', '2', '3', '3', '2', '5-6', '3', '2', '2', '3', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '2', '2', '4', '2', '2', '4', '3', '2', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '3', '2', '1-3', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '2', '2', '1-2', '3', '2', '2', '2', '2', '2', '2-3', '2', '2', '3-4', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '9', '3', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '3', '3', '2', '1-6', '3', '3', '2', '2', '3', '2', '2', '3', '3', '3', '2', '2', '2', '3', '3', '2', '3', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '3', '2', '3', '2', '2', '2-4', '3', '2', '3', '2', '2', '2', '3', '2', '2', '2', '3', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '1-2', '3', '2', '2', '2', '3', '2', '2', '3', '3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '2', '4', '3', '2', '2', '4', '3', '3', '2', '4', '3', '2', '3', '2', '5', '3', '2', '2', '4-7', '3', '2', '2', '2', '2-4', '3', '2', '2', '2', '3', '2', '2', '2', '2-3', '3', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2-3', '3', ' ...

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Номер записи: 42
29-03-2018 дата публикации

TREATMENT OF PULMONARY AND OTHER CONDITIONS

Номер: US20180086723A1
Автор: Reddy Raju
Принадлежит:

Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: 5. The method of claim 1 , wherein Xand Xare each optionally-substituted pyrazinyl or optionally-substituted pyrimidinyl.6. The method of claim 1 , wherein Xand Xare each the same.7. The method of claim 1 , wherein Xand Xare each different.8. The method of claim 1 , wherein —S—Ris a N-acetylcysteine moiety claim 1 , a 2-mercaptoethane sulfonate moiety claim 1 , or glutathione moiety.11. The method of claim 1 , wherein the compound is administered to the subject via inhalation.12. The method of claim 1 , wherein the compound is administered via direct pulmonary delivery.13. The method of claim 1 , wherein the pulmonary disease is pulmonary fibrosis claim 1 , chronic obstructive pulmonary disease (COPD) claim 1 , asthma claim 1 , cystic fibrosis claim 1 , acute lung injury (ALI) claim 1 , acute respiratory distress syndrome claim 1 , pulmonary hypertension claim 1 , lung cancer claim 1 , or pulmonary manifestations of cystic fibrosis.14. The method of claim 4 , wherein the pulmonary disease is pulmonary fibrosis claim 4 , chronic obstructive pulmonary disease (COPD) claim 4 , asthma claim 4 , cystic fibrosis claim 4 , acute lung injury (ALI) claim 4 , acute respiratory distress syndrome claim 4 , pulmonary hypertension claim 4 , lung cancer claim 4 , or pulmonary manifestations of cystic fibrosis.15. The method of claim 9 , wherein the compound is administered to the subject via inhalation.17. The method of claim 16 , wherein the ischemia and reperfusion is consequent to transplanting of an organ in the subject.18. The method of claim 16 , wherein the compound is administered to a donor prior to removal of the organ.19. The method of claim 16 , wherein the compound is provided to the transplanted organ between the time of removal from a donor and placement in a recipient.20. The method of claim 16 , wherein the organ is a lung. This application is a divisional of U. ...

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Номер записи: 43
31-03-2016 дата публикации

TREATMENT OF PULMONARY AND OTHER CONDITIONS

Номер: US20160090366A1
Автор: Reddy Raju
Принадлежит:

Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: 18-. (canceled)9. A compound , or a pharmaceutically acceptable salt or ester thereof , comprising an adduct of a hydrophilic thiol and an enone that comprises at least two N-heterocycles.1415-. (canceled)16. The compound of claim 12 , wherein Xand Xare each optionally-substituted pyrazinyl or optionally-substituted pyrimidinyl.17. The compound of claim 16 , wherein Xand Xare each the same.18. The compound of claim 16 , wherein Xand Xare each different.19. The compound of claim 12 , wherein Ris an acylamino-substituted carboxylalkyl claim 12 , a sulfonate-substituted alkyl claim 12 , or an acylamino-substituted amido.20. The compound of claim 12 , wherein —S—Ris a derivative of N-acetylcysteine claim 12 , 2-mercaptoethane sulfonate claim 12 , or glutathione.21. A pharmaceutical composition comprising a compound of claim 10 , and at least one pharmaceutically acceptable excipient.22. The pharmaceutical composition of claim 21 , wherein the composition is in the form of an aerosol.23. The pharmaceutical composition of claim 21 , wherein the composition is in the form of a dry powder.24. A method for treating a pulmonary disease in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a compound claim 21 , or a pharmaceutically acceptable salt or ester thereof claim 21 , {'br': None, 'sup': 1', '2, 'X-L-X'}, 'having a structure ofwherein L is a linking moiety comprising an enone; and{'sup': 1', '2, 'Xand Xare each independently an optionally-substituted N-heterocycle.'}25. The method of claim 24 , wherein the compound is administered to the subject via inhalation.26. The method of claim 24 , wherein the compound is administered via direct pulmonary delivery.27. A method for treating a pulmonary disease in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a ...

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Номер записи: 44
21-03-2019 дата публикации

METHODS FOR PREPARING OLTIPRAZ

Номер: US20190084971A1
Автор: Framroze Bomi P.
Принадлежит: ST IP Holding AG

The invention provides improved methods of synthesizing oltipraz, which result in higher overall yield and better purity of the desired product. 120-. (canceled)21. A method of making oltipraz , comprising the steps of:(i) reacting a quantity of pyrazine-2-carboxylic acid methyl ester with methyl propionate to form methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate, wherein the reaction is carried out in the presence of a base comprising potassium t-butoxide or sodium pentanoate, and a solvent comprising 1,4-dioxane in tetrahydrofuran (THF), wherein the ratio of 1,4-dioxane in the THF is at least about 1:5;(ii) adding at least one aqueous liquid to quench the reaction in Step (i);(iii) adding a nonpolar organic solvent and an ionic salt, thereby forming composition comprising an aqueous component and an organic component, wherein the organic component comprises the nonpolar solvent and methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate;(iv) separating the organic component from the aqueous component;{'sub': 2', '5, '(v) reacting the methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate ester in the organic component with PSin the presence of a nonpolar organic solvent to form 4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione (oltipraz).'}22. The method of claim 21 , wherein the ratio of 1 claim 21 ,4-dioxane to THF in Step (i) is from about 1:5 to about 1:3.23. The method of claim 22 , wherein claim 22 , and the ratio of 1 claim 22 ,4-dioxane to THF is about 4:1.24. The method of claim 21 , wherein the base comprises potassium t-butoxide.25. The method of claim 21 , wherein the mole ratio of the base to methyl propionate is from about 3:1 to about 1:1.26. The method of claim 21 , wherein the nonpolar organic solvent used in Step (iii) comprises toluene.27. The method of claim 21 , wherein the nonpolar organic solvent in Step (v) comprises toluene.28. The method of claim 21 , wherein the nonpolar solvent in Step (iii) is the same nonpolar solvent used in Step (v).29. The ...

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Номер записи: 45
21-03-2019 дата публикации

Antireflective compositions with thermal acid generators

Номер: US20190085173A1
Автор: Jae Bong Lim, Jung-June Lee
Принадлежит: Rohm and Haas Electronic Materials Korea Ltd

New methods and substrates are provided that include antireflective compositions that comprise one or more thermal acid generators.

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Номер записи: 46
30-03-2017 дата публикации

ANTIBACTERIAL AGENTS

Номер: US20170088549A1
Автор: Kaldor Stephen W., Kasar Ramesh Annasaheb, Lu Qing, Moser Heinz Ernst, Patten Phillip A., Patterson Brian D., WANG DAN
Принадлежит:

Antibacterial compounds of formula (I) are provided: 2. A compound of wherein G is selected from the group consisting of:(1) —C≡C—,(2) —C≡C—C≡C—,{'sup': 3G', '3G, '(3) —CR═CR—C≡C—, and'}{'sup': 3G', '3G, '(4) —C≡C—CR═CR—.'}3. A compound of wherein G is selected from the group consisting of:(1) —C≡C—,(2) —C≡C—C≡C—,(3) —CH═CH—C≡C—, and(4) —C≡C—CH═CH—.4. A compound of wherein G is —C≡C—.5. A compound of wherein G is —C≡C—C≡C—.6. A compound of wherein G is —CH═CH—C≡C—.8. A compound of wherein G is —C≡C—CH═CH—.10. A compound of any one of - wherein X is —(C═O)NR—.11. A compound of wherein X is —(C═O)NH—.12. A compound of any one of - wherein Q is —(C═O)N(R claim 10 ,R).13. A compound of wherein Q is —(C═O)NHOH.14. A compound of any one of - wherein n is 0.15. A compound of any one of - wherein Ris H.16. A compound of any one of - wherein Y is substituted or unsubstituted aryl.17. A compound of wherein Y is substituted or unsubstituted phenyl.18. A compound of wherein Y is unsubstituted phenyl.19. A compound of any one of - wherein A is selected from the group consisting of:{'sub': 2', '0-4', '2', '0-4, 'sup': 1a', '2a', '3a, '(1) —(CH)C(R,R)(CH)OR,'}{'sub': 2', '0-4, 'sup': 1a', '2a', '4a', '5a, '(2) —(CH)C(R,R)N(R,R), and'}{'sup': 1a', '2a, '(3) —CH(R,R).'}20. A compound of wherein A is selected from the group consisting of —CH(CH) claim 19 , —CHOH claim 19 , —CHNH claim 19 , —CHCHOH claim 19 , —CHCHNHand —C(CH)OH.21. A compound of wherein A is —C(CH)NH.22. A compound of any one of - wherein A is selected from the group consisting of:{'sub': 3', '10, '(1) substituted or unsubstituted C-C-cycloalkyl,'}(2) substituted or unsubstituted aryl,(3) substituted or unsubstituted heterocyclyl, and(4) substituted or unsubstituted heteroaryl.26. A compound of any one of - wherein D is present.27. A compound of wherein D is substituted or unsubstituted heteroaryl.29. A compound of wherein D is substituted or unsubstituted aryl.30. A compound of wherein D is substituted or ...

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Номер записи: 47
19-06-2014 дата публикации

Pesticidal compositions and processes related thereto

Номер: US20140171309A1
Автор: Akshay PATNY, Gerald B. Watson, James E. Hunter, Joshodeep Boruwa, Pravin S. IYER, William C. Lo
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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Номер записи: 48
19-06-2014 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20140171311A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).3. A composition according to wherein further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 1 , 1 claim 1 ,2-dichloropropane claim 1 , 1 claim 1 ,3-dichloropropene claim 1 , 1-methylcyclopropene claim 1 , 1-naphthol claim 1 , 2-(octylthio)ethanol claim 1 , 2 claim 1 ,3 claim 1 ,5-tri-iodobenzoic acid claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-dimethylammonium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-lithium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-potassium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-ethylhexyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-3-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-TB claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butometyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butotyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isobutyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isoctyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isopropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-methyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-pentyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-triethylammonium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-trolamine claim 1 , 2 claim 1 ,4-D claim 1 , 2 claim 1 ,4-D-2-butoxypropyl claim 1 , 2 claim 1 ,4-D-2-ethylhexyl claim 1 , 2 claim 1 ,4-D-3- ...

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Номер записи: 49
19-06-2014 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20140171313A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).3. A composition according to wherein further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 1 , 1 claim 1 ,2-dichloropropane claim 1 , 1 claim 1 ,3-dichloropropene claim 1 , 1-methylcyclopropene claim 1 , 1-naphthol claim 1 , 2-(octylthio)ethanol claim 1 , 2 claim 1 ,3 claim 1 ,5-tri-iodobenzoic acid claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-dimethylammonium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-lithium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-potassium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-ethylhexyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-3-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-TB claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butometyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butotyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isobutyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isoctyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isopropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-methyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-pentyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-triethylammonium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-trolamine claim 1 , 2 claim 1 ,4-D claim 1 , 2 claim 1 ,4-D-2-butoxypropyl claim 1 , 2 claim 1 ,4-D-2-ethylhexyl claim 1 , 2 claim 1 ,4-D-3- ...

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Номер записи: 50
21-04-2016 дата публикации

Synthesis Method of Organometallic Complex, Synthesis Method of Pyrazine Derivative, 5,6-Diaryl-2-Pyrazyl Triflate, Light-Emitting Element, Light-Emitting Device, Electronic Device, and Lighting Device

Номер: US20160108006A1
Автор: Inoue Hideko, Kanamoto Miki, KUBOTA Tomohiro
Принадлежит: SEMICONDUCTOR ENERGY LABORATORY CO., LTD.

Provided is a 5,6-diaryl-2-pyrazyl triflate, its synthetic method, and a method for synthesizing an organometallic complex having a triarylpyrazine ligand from the 5,6-diaryl-2-pyrazyl triflate. The triflate is readily obtained from the corresponding 5,6-diarylpyrazin-2-ol, and the palladium-catalyzed coupling of the 5,6-diaryl-2-pyrazyl triflate with an arylboronic acid derivative leads to a high yield of a triarylpyrazine derivative having high purity. The use of the triarylpyrazine derivative in the reaction with a metal compound such as a metal chloride results in an ortho-metallated organometallic complex with high purity. The high purity of the organometallic complex contributes to the extremely high durability of a light-emitting element. 1. A compound represented by the following formula:{'sup': 1', '8, 'wherein Rto Reach independently represent any one of hydrogen, an alkyl group having 1 to 6 carbon atoms, a phenyl group, and a phenyl group having, as a substituent, an alkyl group having 1 to 6 carbon atoms.'} This application is a divisional of copending U.S. application Ser. No. 14/551,712, filed on Nov. 24, 2014 which is incorporated herein by reference.1. Field of the InventionOne embodiment of the present invention relates to a novel method for synthesizing an organometallic complex such as an organoiridium complex. Another embodiment of the present invention relates to a novel method for synthesizing a triarylpyrazine derivative. Another embodiment of the present invention relates to 5,6-diaryl-2-pyrazyl triflate used for the above synthesis methods. Another embodiment of the present invention relates to a light-emitting element, a light-emitting device, an electronic device, and a lighting device each including an organometallic complex synthesized by the above synthesis method.Note that one embodiment of the present invention is not limited to the above technical field. Specifically, examples of the technical field of one embodiment of the present ...

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Номер записи: 51
23-04-2015 дата публикации

Pyrazine Derivative, and Light Emitting Element, Display Device, Electronic Device Using the Pyrazine Derivative

Номер: US20150112065A1
Автор: Egawa Masakazu, KAWAKAMI Sachiko, Murata Hiroko, Nakashima Harue, Ohsawa Nobuharu, SEO Satoshi
Принадлежит:

It is an object to provide a novel material having a bipolar property, a light emitting element provided with the novel material, and a display device that includes the light emitting element. It is an object to provide a pyrazine derivative represented by the following general formula (g-1). 1. (canceled) This application is a continuation of copending U.S. application Ser. No. 11/645,286, filed on Dec. 22, 2006 which is incorporated herein by reference.1. Field of the InventionThe present invention relates to a pyrazine derivative. The present invention also relates to a light emitting element containing the pyrazine derivative and a display device that includes a light emitting element containing the pyrazine derivative.2. Description of the Related ArtIn recent years, a light emitting element using a light emitting compound has been attracted attention as a display (a display device) of the next generation because it has a feature of low power consumption and a lightweight and thin type. In addition, the light emitting element using a light emitting compound is a self-luminous type; accordingly, it is considered that the light emitting element using a light emitting compound has superiority in visibility without problems such as a viewing angle as compared with a liquid crystal display (an LCD).A basic structure of a light emitting element is a structure that has a light emitting layer containing a light emitting compound interposed between a pair of electrodes. It is said that, in such a light emitting element, by applying a voltage, holes injected from an anode and electrons injected from a cathode are recombined in an emission center of a light emitting layer to excite a molecule, and the excited molecule discharge energy in returning to a ground state; accordingly light is emitted. It is to be noted that an excited state that is generated by recombination has a singlet excited state and a triplet excited state. Light emission is considered to be possible ...

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Номер записи: 52
10-07-2014 дата публикации

ACYLAMINOCYCLOALKYL COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF DOPAMINE D3 RECEPTOR

Номер: US20140194437A1
Автор: Haupt Andreas
Принадлежит:

The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. 2. The compound of claim 1 , wherein Ris hydrogen or methyl.3. The compound of claim 1 , wherein Ris methyl.4. The compound of claim 1 , wherein Ris hydrogen.5. The compound of claim 1 , wherein Ris hydrogen.6. The compound of claim 1 , wherein m is 2.7. The compound of claim 1 , wherein n is 2.8. The compound of claim 1 , wherein both m and n are 1.9. The compound of claim 1 , wherein Rand Rare hydrogen.10. The compound of claim 1 , wherein either Ris methyl and Ris hydrogen or Ris hydrogen and Ris methyl.11. The compound of claim 1 , wherein A is CH.12. The compound of claim 1 , wherein A is CHCH claim 1 , CHFCHor CFCH.13. The compound of claim 1 , wherein Ris branched C-Calkyl and in particular tert-butyl.14. The compound of claim 1 , wherein Ris selected from the group consisting of C-C-alkoxy-C-C-alkyl claim 1 , fluorinated C-C-alkoxy-C-C-alkyl and hydroxy-C-C-alkyl.15. The compound of claim 14 , wherein Ris selected from the group consisting of methoxymethyl claim 14 , ethoxymethyl claim 14 , 2-methoxyethyl claim 14 , difluoromethoxymethyl claim 14 , 2-(difluoromethoxy)ethyl claim 14 , trifluoromethoxymethyl claim 14 , 2-(trifluoromethoxy)ethyl claim 14 , methoxydifluoromethyl claim 14 , ethoxydifluoromethyl claim 14 , 2-methoxy-1 claim 14 ,1-difluoroethyl claim 14 , hydroxymethyl claim 14 , 2-hydroxyethyl claim 14 , 2-hydroxypropyl and 2-hydroxy-2-methylpropyl.16. The compound of claim 14 , wherein Ris C-C-alkoxy-C-C-alkyl.17. The compound of claim 1 , wherein Ris selected from the group consisting of oxetanyl claim 1 , fluorinated oxetanyl claim 1 , oxolanyl claim 1 , fluorinated oxolanyl claim 1 , and C-Ccycloalkyl claim 1 , ...

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Номер записи: 53
09-04-2020 дата публикации

PYRAZINE COMPOUND

Номер: US20200109128A1
Автор: KIMURA Takahiro, Nakajima Yuji, Nokura Yoshihiko, ORIMOTO Kohei, Tanabe Takamasa
Принадлежит:

Provided is a compound represented by formula (I): This application is a Division of U.S. patent application Ser. No. 15/766,034 filed Apr. 5, 2018, now allowed, which is a Section 371 of International Application No. PCT/JP2016/080410, filed Oct. 13, 2016, which was published in the Japanese language on Apr. 20, 2017, under International Publication No. WO 2017/065228 A1, which claims priority under 35 U.S.C. § 119(b) to Japanese Application No. 2015-204376, filed Oct. 16, 2015, Japanese Application No. 2015-208639, filed Oct. 23, 2015 and Japanese Application No. 2016-149448, filed Jul. 29, 2016, the disclosures of all of which are incorporated herein by reference in their entireties.The present invention is related to a certain class of pyrazine compound and its use for controlling harmful arthropods.To date, some compounds for controlling harmful arthropods have been developed and come into practical use. Also, a certain class of compounds has been known to be effective for controlling harmful organisms (see Patent Document 1).Patent Document 1: JP 2000-26421 AAn object of the present invention is to provide a compound having an excellent efficacy for controlling harmful arthropods.The present invention provides, for example, the following embodiments.[1] A compound represented by formula (I) or its N oxide compound:[whereinArepresents a nitrogen atom or a CR;Rrepresents a hydrogen atom, a OR, a NRR, a cyano group, a nitro group, or a halogen atom;Rrepresents a C2-C10 chain hydrocarbon group having one or more halogen atoms, a (C1-C5 alkoxy)C2-C5 alkyl group having one or more halogen atoms, a (C1-C5 alkylsulfanyl)C2-C5 alkyl group having one or more halogen atoms, a (C1-C5 alkylsulfinyl)C2-C5 alkyl group having one or more halogen atoms, a (C1-C5 alkylsulfonyl)C2-C5 alkyl group having one or more halogen atoms, a (C3-C7 cycloalkyl)C1-C3 alkyl group having one or more substituents selected from Group G, or a C3-C7 cycloalkyl group having one or more substituents ...

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Номер записи: 54
21-05-2015 дата публикации

COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1

Номер: US20150141427A1
Автор: FURET Pascal, GROTZFELD Robert Martin, Jahnke Wolfgang, JONES Darryl Brynley, MANLEY Paul William, MARZINZIK Andreas, MOUSSAOUI Saliha, PELLE Xavier Francois Andre, SALEM Bahaa, SCHOEPFER Joseph
Принадлежит: NOVARTIS AG

The present invention relates to compounds of formula I: in which Y, Y, Y, Y, Y, R, R, Rand Rare defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers. 3. The compound of in which: Y is CH; and Ris selected from hydrogen claim 2 , halo and methyl.4. The compound of in which Ris hydrogen and Ris selected from trifluoro-methoxy claim 3 , trifluoro-methyl-thio and chloro-difluoro-methoxy.6. The compound of in which: Y is CH; and Ris selected from hydroxy claim 2 , Calkoxy claim 2 , methoxy-carbonyl claim 2 , 3 claim 2 ,6-dihydro-2H-pyran-4-yl claim 2 , tetrahydro-2H-pyran-4-yl claim 2 , tetrahydro-2H-pyran-4-yl-oxy and cyclobutyl; wherein said Calkoxy claim 2 , cyclobutyl or tetrahydro-2H-pyran-4-yl of Rcan be unsubstituted or substituted with 1 to 3 groups independently selected from halo claim 2 , hydroxy claim 2 , cyano claim 2 , Calkoxy claim 2 , morpholino claim 2 , piperazinyl and NRR; wherein Ris selected from hydrogen and Calkyl; and Ris selected from hydroxy-ethyl; wherein said piperazinyl substituent of Rcan be unsubstituted or further substituted with Calkyl.7. The compound of in which: Ris selected from methoxy claim 6 , ethoxy claim 6 , morpholino-ethoxy claim 6 , hydroxy-ethoxy claim 6 , pyrrolidinyl-ethoxy claim 6 , hydroxy claim 6 , methoxy-ethoxy claim 6 , (hydroxy-ethyl)amino-ethoxy claim 6 , (tetrahydro-2H-pyran-4-yl)oxy and piperazinyl-ethoxy; wherein said piperazinyl-ethoxy is unsubstituted or substituted with isobutyl.8. The compound of in which: Ris hydrogen and Ris selected from trifluoro-methoxy and chloro-difluoro-methoxy.10. A pharmaceutical composition comprising a compound of claim 1 , admixed with at least one pharmaceutically acceptable excipient selected from corn starch claim ...

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Номер записи: 55
28-05-2015 дата публикации

Synthesis Method of Organometallic Complex, Synthesis Method of Pyrazine Derivative, 5,6-Diaryl-2-Pyrazyl Triflate, Light-Emitting Element, Light-Emitting Device, Electronic Device, and Lighting Device

Номер: US20150147840A1
Автор: Inoue Hideko, Kanamoto Miki, KUBOTA Tomohiro
Принадлежит:

Provided is a 5,6-diaryl-2-pyrazyl triflate, its synthetic method, and a method for synthesizing an organometallic complex having a triarylpyrazine ligand from the 5,6-diaryl-2-pyrazyl triflate. The triflate is readily obtained from the corresponding 5,6-diarylpyrazin-2-ol, and the palladium-catalyzed coupling of the 5,6-diaryl-2-pyrazyl triflate with an arylboronic acid derivative leads to a high yield of a triarylpyrazine derivative having high purity. The use of the triarylpyrazine derivative in the reaction with a metal compound such as a metal chloride results in an ortho-metallated organometallic complex with high purity. The high purity of the organometallic complex contributes to the extremely high durability of a light-emitting element. 2. A synthetic method including:coupling a 5,6-diaryl-2-pyrazyl trifluoromethansulfonate with an arylboronic acid derivative to give a 2,5,6-triarylpyrazine.5. The synthetic method according to claim 2 ,wherein the coupling is conducted in the presence of a palladium catalyst.6. The synthetic method according to claim 2 , further comprising:reacting the 2,5,6-triarylpyrazine with a metal compound to give an ortho-metallated complex.7. The synthetic method according to claim 6 ,wherein the metal compound is iridium chloride.9. The synthetic method according to claim 8 , further comprising:reacting the halogen-bridged complex with a ligand to give an ortho-metallated complex.11. A method for manufacturing a light-emitting element claim 8 , the method comprising:coupling a 5,6-diaryl-2-pyrazyl trifluoromethansulfonate with an arylboronic acid derivative to give a 2,5,6-triarylpyrazine;transforming the 2,5,6-triarylpyrazine to an ortho-metallated complex by using a metal compound;forming a layer including the ortho-metallated complex between a pair of electrodes.14. The method according to claim 11 ,wherein the coupling is conducted in the presence of a palladium catalyst.15. The method according to claim 11 ,wherein the metal ...

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Номер записи: 56
17-05-2018 дата публикации

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

Номер: US20180138416A1
Автор: Hiroki Suzuki, Kanta Abe, Kyoko Takeda, Satoshi Seo, Tatsuyoshi Takahashi
Принадлежит: Semiconductor Energy Laboratory Co Ltd

A light-emitting element with a lower voltage and higher emission efficiency is provided. The light-emitting element includes a first organic compound, a second organic compound, and a guest material. The LUMO level of the first organic compound is lower than the LUMO level of the second organic compound, and a difference between them is larger than 0 eV and smaller than or equal to 0.5 eV. Furthermore, the HOMO level of the first organic compound is lower than the HOMO level of the second organic compound. The guest material has a function of converting triplet excitation energy into light emission. The first organic compound and the second organic compound form an exciplex.

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Номер записи: 57
30-04-2020 дата публикации

FLUORENE DERIVATIVE AND ORGANIC LIGHT EMITTING DEVICE COMPRISING SAME

Номер: US20200131138A1
Автор: HAN Miyeon, HEO Dong Uk, Huh Jungoh, JANG Boonjae, Lee Dong Hoon, YANG Junghoon, YUN Heekyung
Принадлежит:

Provided is a fluorene derivative of Chemical Formula 1: 3. The fluorene derivative of claim 1 , wherein the compound of Chemical Formula 2 is a triazine group substituted or unsubstituted by an aryl group having 6 to 20 carbon atoms.4. The fluorene derivative of claim 1 , wherein L1 to L4 are identical to or different from one another claim 1 , and are each independently a direct bond claim 1 , a substituted or unsubstituted arylene group having 6 to 20 carbon atoms claim 1 , or a substituted or unsubstituted claim 1 , monocyclic or polycyclic heteroarylene group.6. An organic light emitting device comprising:a first electrode;a second electrode facing the first electrode; andat least one organic material layer interposed between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the at least one organic material layer comprises the fluorene derivative of .'}7. The organic light emitting device of claim 6 , wherein the organic material layer comprises a light emitting layer claim 6 ,wherein the light emitting layer comprises the fluorene derivative.8. The organic light emitting device of claim 6 , wherein the organic material layer comprises a hole injection layer or a hole transport layer claim 6 ,wherein the hole injection layer or the hole transport layer comprises the fluorene derivative.9. The organic light emitting device of claim 6 , wherein the organic material layer comprises an electron injection layer claim 6 , an electron transport layer claim 6 , or an electron injection and transport layer claim 6 ,wherein the electron injection layer, the electron transport layer, or the electron injection and transport layer comprises the fluorene derivative.10. The organic light emitting device of claim 6 , wherein the organic material layer comprises an electron control layer claim 6 ,wherein the electron control layer comprises the fluorene derivative. The present specification is a National Stage Application ...

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Номер записи: 58
30-04-2020 дата публикации

CHEMICAL COMPOUNDS

Номер: US20200131141A1
Автор: BOUTARD Nicolas, FABRITIUS Charles-Henry, GALEZOWSKI Michal, HARRISON David, KOWALCZYK Piotr, LEVENETS Oleksandr, WATT Alan Paul, WOYCIECHOWSKI Jakub
Принадлежит:

The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers. 2. The compound of claim 1 , wherein Ris Methyl-Ror Ethyl-R.3. The compound of or claim 1 , wherein Ris a monocyclic aryl claim 1 , optionally substituted with at least one hydroxyl group.4. The compound of or claim 1 , wherein Ris a monocyclic aryl with a cyano substitution.5. The compound of or claim 1 , wherein Ris a 5 or 6 membered monocyclic aryl ring comprising 1 claim 1 , 2 or 3 heteroatoms independently selected from oxygen claim 1 , nitrogen and sulfur.6. The compound of any preceding claim claim 1 , wherein Ris alkyl (C1-C4) or cyclo alkyl (C3-C6).11. A pharmaceutical composition comprising a compound as defined in any of the preceding claims or a pharmaceutically acceptable salt thereof claim 1 , in a mixture with a pharmaceutically acceptable diluent or carrier.12. A method of inhibiting the NLRP3 inflammasome activity in vitro or in vivo claim 1 , said method comprising contacting a cell with an effective amount of a compound according to any preceding claim or a pharmaceutically acceptable salt thereof.13. A method of treating a disease or disorder in which inflammasome activity is implicated in a patient in need of such treatment claim 1 , said method comprising administering to said patient a therapeutically effective amount of a compound according to any preceding claim or a pharmaceutically acceptable salt or composition thereof.14. A method of treating an auto-inflammatory disorder claim 1 , an autoimmune disorder claim 1 , a neurodegenerative disease or cancer in a patient in need of such ...

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Номер записи: 59
26-05-2016 дата публикации

METHOD FOR PREPARING NITROGEN-CONTAINING AROMATIC COMPOUND BY CATALYTIC PYROLYSIS OF ORGANIC MATERIAL

Номер: US20160145217A1
Автор: Xu Lujiang, Yao Qian, ZHANG YING
Принадлежит:

Provided is a method for preparing a nitrogen-containing aromatic compound through catalytic pyrolysis from organic materials. The method comprises: feeding organic materials and a catalyst into a reactor, to enable the organic material to undergo reactions in the presence of nitrogen and under heating conditions, so as to generate a reaction system flow containing one or more nitrogen-containing aromatic compounds. 1. A method for preparing a nitrogen-containing aromatic compound by catalytic pyrolysis of an organic material , comprising:feeding an organic material feed and a catalyst to a reactor; andreacting the organic material feed under the catalysis of the catalyst in the presence of a nitrogen-containing gas and under heating conditions in the reactor, to generate a reaction stream comprising one or more nitrogen-containing aromatic compounds.2. The method of claim 1 , further comprising:separating at least a part of the nitrogen-containing aromatic compounds in the reaction stream, to obtain a product stream comprising the separated nitrogen-containing aromatic compounds and a recycle stream; andfeeding at least a part of the recycle stream to the reactor.3. The method of claim 1 , wherein the catalyst comprises one or more of a zeolite catalyst claim 1 , a non-zeolite catalyst claim 1 , a metal catalyst and/or a metal oxide catalyst.4. The method of claim 1 , wherein the catalyst comprises γ-AlO claim 1 , SiO—AlO claim 1 , WO/ZrO claim 1 , SO/ZrO claim 1 , MCM-41 claim 1 , ZK-5 claim 1 , ZSM-23 claim 1 , SSZ-20 claim 1 , β-zeolite claim 1 , Y-zeolite claim 1 , ZSM-5 and/or HZSM-5.5. The method of claim 1 , wherein the catalyst has a SiO/AlOratio of 15:1 to 200:1.6. The method of claim 1 , wherein the mass ratio of the catalyst to the organic material is 1:100 to 100:1.7. The method of claim 1 , wherein the catalyst comprises a plurality of pores.8. The method of claim 7 , wherein at least about 95% of pores of one or more catalysts have smallest cross- ...

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Номер записи: 60
02-06-2016 дата публикации

USE OF RUTHENIUM COMPLEXES FOR FORMATION AND/OR HYDROGENATION OF AMIDES AND RELATED CARBOXYLIC ACID DERIVATIVES

Номер: US20160152663A1
Автор: Balaraman Ekambaram, Ben-David Yehoshua, Gnanaprakasam Boopathy, Gunanathan Chidambaram, Milstein David, Zhang Jing
Принадлежит:

A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3. 2. The process of claim 1 , wherein the process is conducted either with (a) Ruthenium catalyst A1′ in the absence of a base; or (b) Ruthenium catalyst A2′ or A3′ in the presence of one or two equivalents of base relative to the amount of the Ruthenium catalyst.5. The process of claim 4 , wherein the ester is selected from the group consisting of ethyl acetate claim 4 , butyl butyrate claim 4 , pentyl pentanoate and hexyl hexanoate.6. The process of claim 4 , wherein the amine is selected from the group consisting of pyrrolidine claim 4 , morpholine claim 4 , 1-methyl piperazine claim 4 , piperidine claim 4 , piperazine claim 4 , 1-hexylamine and p-tolylmethanamine.8. The process of claim 7 , wherein the process is conducted either with (a) Ruthenium catalyst A1″ in the absence of a base; or (b) Ruthenium catalyst A2″ or A3″ in the presence of one or two equivalents of base relative to the amount of the Ruthenium catalyst.11. The process of claim 10 , wherein the process is conducted either with (a) Ruthenium catalyst A1 ...

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Номер записи: 61
17-06-2021 дата публикации

COMPOSITIONS AND METHODS FOR DELIVERING PHARMACEUTICAL AGENTS

Номер: US20210179566A1
Автор: Gomez Alexan I., Gu Yali, Mansour Heidi M., Muralidharan Priyardarshini, WANG Jian, Yuan Jason
Принадлежит:

Provided herein are compositions and methods for treating pulmonary arterial hypertension. In particular, provided herein are dry powder formulations of TMP for delivery to the lung. 1. A composition comprising a polymorphic conversion of a crystal of tetramethylpyrazine (TMP).2. The composition of claim 1 , wherein said composition further comprises a pharmaceutically acceptable carrier.3. The composition of claim 1 , wherein said pharmaceutically acceptable carrier is D-mannitol.4. The composition of claim 3 , wherein said TMP and D-mannitol are present at a molar ratio of 75:25 to 25:75 TMP:D-mannitol.5. The composition of claim 1 , wherein said composition is a dry powder.6. The composition of claim 5 , wherein said dry powder is spray dried.7. The composition of claim 1 , wherein said TMP lacks x-ray diffraction peaks in the 2θ region of 30-60°.8. The composition of claim 1 , wherein said TMP crystals have a diameter of 0.8-1.5 μm9. The composition of claim 1 , wherein said TMP crystals are generated by a method claim 1 , comprising:a) preparing a first solution comprising said TMP in an organic solvent; andb) spraying said first solution using a spray drying apparatus.10. The composition of claim 9 , wherein said method further comprises the steps of preparing a second solution comprising said pharmaceutically acceptable carrier in an organic solvent; and co-spraying said first and second solutions.11. The composition of claim 9 , wherein said organic solvent is methanol.12. A system claim 9 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a) the composition of ; and'}b) a dry powder inhaler device.13. A method of treating pulmonary arterial hypertension (PAH) in a subject claim 9 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering the composition of to a subject diagnosed with or having signs or symptoms of PAH under conditions such that said signs or symptoms are reduced.'}14. The method of claim 13 , wherein said ...

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Номер записи: 62
21-08-2014 дата публикации

HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK

Номер: US20140235579A1
Автор: Clare Michael, McCall John M., Romero Donna L.
Принадлежит:

Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. 138.-. (canceled)40. The method as recited in wherein said disease is chosen from cancer and a metabolic disease.41. The method as recited in wherein said disease is a metabolic disease.42. The method as recited in wherein said metabolic disease is chosen from metabolic syndrome claim 41 , diabetes claim 41 , dyslipidemia claim 41 , fatty liver disease claim 41 , non-alcoholic steatohepatitis claim 41 , obesity claim 41 , and insulin resistance.43. The method of wherein said diabetes is Type II diabetes.44. The method of wherein said dyslipidemia is hyperlipidemia.46. The method of wherein said cholesterol is chosen from LDL and VLDL cholesterol.47. The method of wherein said triglycerides are chosen from plasma triglycerides and liver triglycerides. This application claims the benefit of priority of U.S. Provisional Application No. 61/448,552, filed Mar. 2, 2011, the disclosure of which is hereby incorporated by reference as if written herein in its entirety.Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.The regulation of glycogen metabolism is critical for the maintenance of glucose and energy homeostasis in mammals. Glycogen, a large branched polymer of glucose, acts as a reserve of carbon and energy in a variety of organisms. In mammals, the most important stores are found in the liver and skeletal muscle (1). Liver glycogen is required to efficiently buffer blood glucose levels during fasting, whereas muscle glycogen is primarily used ...

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Номер записи: 63
08-06-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170156320A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).3. A composition according to wherein further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 1 , 1 claim 1 ,2-dichloropropane claim 1 , 1 claim 1 ,3-dichloropropene claim 1 , 1-methylcyclopropene claim 1 , 1-naphthol claim 1 , 2-(octylthio)ethanol claim 1 , 2 claim 1 ,3 claim 1 ,5-tri-iodobenzoic acid claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-dimethylammonium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-lithium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-potassium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-ethylhexyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-3-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-TB claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butometyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butotyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isobutyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isoctyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isopropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-methyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-pentyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-triethylammonium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-trolamine claim 1 , 2 claim 1 ,4-D claim 1 , 2 claim 1 ,4-D-2-butoxypropyl claim 1 , 2 claim 1 ,4-D-2-ethylhexyl claim 1 , 2 claim 1 ,4-D-3- ...

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Номер записи: 64
23-05-2019 дата публикации

NITROGEN-CONTAINING HETEROARYL COMPOUND AND PHARMACEUTICAL USE THEREOF

Номер: US20190152926A1
Автор: Mitani Ikuo, Nagamori Hironobu, Nakagawa Yuichi, NISHIMARU Tatsuya, TAKAGI Masaki
Принадлежит: JAPAN TOBACCO INC.

The invention provides a compound having a GLUT9 inhibitory activity. The compound is of Formula [I] 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein -L-COOH is —COOH.3. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0 or 1.4. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 0 or 1.5. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris (1) hydrogen or (2) halogen.6. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '4', 'Ris'}{'sub': '1-8', '(1) Calkyl optionally substituted with 1 to 3 substituents independently selected from the following Group A,'}{'sub': '1-6', '(2) halo Calkyl, or'}{'sup': 41', '42', '41', '42, 'sub': '1-6', '(3) —CON(R)(R) wherein Rand Rare each independently hydrogen or Calkyl, and'}Group A consists of(a) hydroxy,{'sub': 1-3', '1-3, '(b) Calkoxy optionally substituted with one hydroxy or one Calkoxy,'}{'sub': '1-3', '(c) halo Calkoxy,'}{'sub': '3-6', '(d) Ccycloalkyl optionally substituted with one hydroxy, and'}(e) phenyl.18. A pharmaceutical composition comprising the compound according to any one of and - or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.19. (canceled)20. (canceled)21. A method for the inhibition of GLUT9 in a mammal in need of such inhibition claim 1 , which comprises administering a pharmaceutically effective amount of the compound according to any one of and - or a pharmaceutically acceptable salt thereof to the mammal.22. A method for the treatment or prophylaxis of a disease selected from the group consisting of hyperuricemia and gout in a mammal in need of such treatment or prophylaxis claim 1 , which comprises administering a pharmaceutically effective amount of the compound according to any one of and - or a pharmaceutically acceptable salt ...

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Номер записи: 65
08-06-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170158597A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).3. A composition according to wherein further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 1 , 1 claim 1 ,2-dichloropropane claim 1 , 1 claim 1 ,3-dichloropropene claim 1 , 1-methylcyclopropene claim 1 , 1-naphthol claim 1 , 2-(octylthio)ethanol claim 1 , 2 claim 1 ,3 claim 1 ,5-tri-iodobenzoic acid claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-dimethylammonium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-lithium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-potassium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-ethylhexyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-3-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-TB claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butometyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butotyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isobutyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isoctyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isopropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-methyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-pentyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-triethylammonium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-trolamine claim 1 , 2 claim 1 ,4-D claim 1 , 2 claim 1 ,4-D-2-butoxypropyl claim 1 , 2 claim 1 ,4-D-2-ethylhexyl claim 1 , 2 claim 1 ,4-D-3- ...

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Номер записи: 66
08-06-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170158598A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).3. A composition according to wherein further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 1 , 1 claim 1 ,2-dichloropropane claim 1 , 1 claim 1 ,3-dichloropropene claim 1 , 1-methylcyclopropene claim 1 , 1-naphthol claim 1 , 2-(octylthio)ethanol claim 1 , 2 claim 1 ,3 claim 1 ,5-tri-iodobenzoic acid claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-dimethylammonium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-lithium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-potassium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-ethylhexyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-3-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-TB claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butometyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butotyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isobutyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isoctyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isopropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-methyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-pentyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-triethylammonium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-trolamine claim 1 , 2 claim 1 ,4-D claim 1 , 2 claim 1 ,4-D-2-butoxypropyl claim 1 , 2 claim 1 ,4-D-2-ethylhexyl claim 1 , 2 claim 1 ,4-D-3- ...

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Номер записи: 67
15-06-2017 дата публикации

Substituted 5-hydroxy-2-heteroaryl-3-phenylpentanonitrile derivatives, processes for their preparation and their use as herbicides and/or plant growth regulators

Номер: US20170166549A1
Автор: Dietrich Hansjoerg, GATZWEILER ELMAR, Jakobi Harald, MOSRIN Marc, ROSINGER CHRISTOPHER HUGH, SCHMUTZLER Dirk
Принадлежит: BAYER CROPSCIENCE AKTIENGESELLSHAFT

Primarily, the present invention relates to compounds of the formula (I) defined below and to their use as herbicides, in particular for controlling broad-leaved weeds and/or weed grasses in crops of useful plants and/or as plant growth regulators for influencing the growth of crops of useful plants. The present invention also relates to herbicidal or plant growth-regulating compositions comprising one or more compounds of the formula (I). Moreover, the present invention relates to processes for preparing the compounds of the formula (I). 2. The compound of formula (I) and/or salt thereof according to claim 1 , whereinQ represents a mono- or bicyclic heteroaromatic radical having in total 2 to 9 carbon ring atoms, where the heteroaromatic radical Q contains 1, 2, 3 or 4 heteroatoms in the heteroaromatic ring and the heteroatom or the heteroatoms are selected from the group consisting of N, O, and S.3. The compound of formula (I) and/or salt thereof as claimed in claim 1 , whereinQ represents a mono- or bicyclic heteroaromatic radical selected from the group consisting of pyrimidinyl, pyridinyl, pyridazinyl, pyrazinyl, thienyl, furyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazinyl, quinolyl, isoquinolyl, cinnolinyl-, quinazolinyl, quinoxalinyl, pteridinyl, indolyl and phthalazinyl.5. The compound of formula (I) and/or salt thereof as claimed in claim 1 , wherein{'sup': '1', 'Rrepresents hydrogen or a hydrolyzable radical having in total up to 30 carbon atoms, with preference a hydrolyzable radical having in total 1 to 24 carbon atoms, optionally having in total 1 to 20 carbon atoms.'}6. The compound of formula (I) and/or salt thereof as claimed in claim 1 , wherein{'sup': 1', '1, 'claim-text': represents an optionally substituted hydrocarbon radical or an optionally substituted heterocyclyl radical, or', {'sup': b', 'a', 'b', 'c', 'a', 'b, 'Rrepresents a radical of the formula SiRRR, or —NRR,'}, {'sup': a', 'b', 'c', 'a', 'b, 'where each of the radicals Rand ...

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Номер записи: 68
21-05-2020 дата публикации

KCNQ2-5 CHANNEL ACTIVATOR

Номер: US20200157050A1
Автор: Saito Tetsuji, Wakamatsu Daisuke, Yashiro Kentaro
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases. 119.-. (canceled)22. The method according to claim 20 , wherein Ris a hydrogen atom claim 20 , a salt thereof claim 20 , a solvate thereof claim 20 , or a cocrystal thereof.23. The method according to claim 20 , wherein one of Rand Ris a methyl group which may be substituted with halogen claim 20 , and the other is a hydrogen atom or a methyl group which may be substituted with halogen claim 20 , a salt thereof claim 20 , a solvate thereof claim 20 , or a cocrystal thereof.24. The method according to claim 20 , wherein Ris a hydrogen atom or halogen claim 20 , and Ris a hydrogen atom claim 20 , a salt thereof claim 20 , a solvate thereof claim 20 , or a cocrystal thereof.27. The method according to claim 20 , wherein Rand Rare each independently halogen or a methyl group claim 20 , a salt thereof claim 20 , a solvate thereof claim 20 , or a cocrystal thereof.28. The method according to claim 20 , wherein Ris a hydrogen atom or a methyl group claim 20 , a salt thereof claim 20 , a solvate thereof claim 20 , or a cocrystal thereof.29. The method according to claim 20 , wherein the compound claim 20 , a salt thereof claim 20 , a solvate thereof claim 20 , or a cocrystal thereof is:(1) 1-{2,6-dichloro-4-[(2R)-1,1,1-trifluoro-2-hydroxy-2-propanyl]phenyl}-3-{[5-(trifluoromethyl)-2-pyridinyl]methyl}urea,(2) 1-{2,6-dichloro-4-[(2R)-1,1,1-trifluoro-2-hydroxy-2-propanyl]phenyl}-3-{[5-(trifluoromethyl)-2-pyrimidinyl]methyl}urea,(3) 1-{2,6-di chloro-4-[(2R)-1,1,1-trifluoro-2-hydroxy-2-propanyl]phenyl}-3-{[6-(trifluoromethyl)-3-pyridinyl]methyl}urea,(4) 1-[(5-chloro-2-pyridinyl)methyl]-3-{2,6-dichloro-4-[(2R)-1,1,1-trifluoro-2-hydroxy-2-propanyl]phenyl}urea,(5) 1-{2,6-dichloro-4-[(2R)-1,1,1-trifluoro-2- ...

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Номер записи: 69
01-07-2021 дата публикации

SUBSTITUTED 6-MEMBERED ARYL OR HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS

Номер: US20210196734A1
Автор: Bell Ian M., CAMPBELL BRIAN T., Crowley Brendan M., Greshock Thomas J., Harvey Andrew John, Rada Vanessa L.
Принадлежит: Merck Sharp & Dohme Corp.

The present disclosure relates to compounds of formula I that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Y is H.4. The compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein A is phenyl claim 3 , substituted with 1 to 2 R groups independently selected from halogen claim 3 , CN claim 3 , (C-C)alkyl claim 3 , O(C-C)alkyl claim 3 , NRR claim 3 , (C-C)cycloalkyl claim 3 , aryl claim 3 , heteroaryl and heterocyclyl claim 3 , wherein said alkyl claim 3 , NRR claim 3 , (C-C)cycloalkyl claim 3 , aryl claim 3 , heteroaryl and heterocyclyl are optionally substituted with one or more substituents independently selected from halogen claim 3 , CN claim 3 , (C-C)alkyl claim 3 , (C═O)O(C-C)alkyl and phenyl claim 3 , wherein said alkyl is optionally substituted with one or more halogen.5. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein R claim 4 , R claim 4 , Rand Rare independently H or methyl.6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Rand Rare independently H claim 5 , F claim 5 , Si(CH)or methyl.7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein Rand Rare independently selected from H claim 6 , (C-C)alkyl claim 6 , cyclopentyl and phenyl wherein said alkyl and phenyl are optionally substituted with halogen or phenyl.9. The compound of having the formula Ia claim 8 , or a pharmaceutically acceptable salt thereof claim 8 , wherein;{'sub': 1', '6', '1', '6', '3', '1', '4', '1', '4, 'sup': 7', '8, 'A is phenyl ...

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Номер записи: 70
08-07-2021 дата публикации

METHODS FOR PREPARING OLTIPRAZ

Номер: US20210206752A1
Автор: Framroze Bomi P.
Принадлежит:

The invention provides improved methods of synthesizing oltipraz, which result in higher overall yield and better purity of the desired product. 120-. (canceled)21. A method of making a purified oltipraz composition , comprising the steps of:(i) reacting a quantity of pyrazine-2-carboxylic acid methyl ester with methyl propionate to form methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate, wherein the reaction is carried out in the presence of a base and a solvent comprising 1,4-dioxane in tetrahydrofuran (THF), wherein the ratio of 1,4-dioxane in the THF is at least about 1:5;(ii) adding at least one aqueous liquid to quench the reaction in Step (i);(iii) adding a nonpolar organic solvent and an ionic salt, thereby forming a composition comprising an aqueous component and an organic component, wherein the organic component comprises the nonpolar solvent and methyl 2-methyl-3-oxo-3-(pyrazin-2-yl) propanoate;(iv) separating the organic component from the aqueous component;{'sub': 2', '5, '(v) reacting the methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate ester in the organic component with PSin the presence of a nonpolar organic solvent to form 4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione (oltipraz);'}(vi) quenching the reaction with an aqueous composition to yield a composition comprising (i) an aqueous component and (ii) an organic component that comprises oltipraz;(vii) separating the organic component comprising oltipraz to yield an organic composition comprising oltipraz in the nonpolar organic solvent;(viii) reducing the amount of solvent in the organic composition;(ix) precipitating the oltipraz in the organic composition to yield a composition comprising oltipraz;(x) separating the precipitated oltipraz; and(xi) purifying the separated oltipraz precipitate.22. The method according to claim 21 , wherein the step of purifying comprises recrystallization.23. The method according to claim 21 , wherein the step of purifying does not comprise chromatographic ...

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Номер записи: 71
13-06-2019 дата публикации

NEW SOLID FORMS OF CANNABIDIOL AND USES THEREOF

Номер: US20190177258A1
Автор: Andres Mark, Andres Patricia, EMANUELE R. Martin, Gordon Tanise Shattock, Williford Tabitha
Принадлежит: Artelo Biosciences, Inc.

Disclosed herein are cocrystals of cannabidiol and a coformer containing 5-6 membered rings comprised of carbon and nitrogen atoms, wherein the 5-6 membered rings can be unsaturated or saturated and the rings contain 1 to 2 nitrogen atoms. Cocrystals of cannabidiol and a coformer selected from L-proline, D-proline, tetramethylpyrazine, and 4,4′-dipyridyl are also disclosed herein 1. A solid form comprising cannabidiol and the coformer L-proline.2. The solid form of having an x-ray diffraction pattern (XRPD) comprising one or more peaks at 5.3 claim 1 , 5.8 claim 1 , 9.4 claim 1 , 10.7 claim 1 , 11.1 claim 1 , 11.4 claim 1 , 11.7 claim 1 , 12.3 claim 1 , 15.4 claim 1 , 15.8 claim 1 , 16.4 claim 1 , 17.3 claim 1 , 18.7 claim 1 , 19.2 claim 1 , 19.4 claim 1 , 20.0 claim 1 , 20.8 claim 1 , 21.3 claim 1 , 23.1 claim 1 , and 24.5 degrees 2θ±0.2.3. The solid form of having an x-ray powder diffraction pattern substantially similar to .4. The solid form of wherein the molar ratio of cannabidiol to L-proline is about 1:1.5. The solid form of claim 1 , which is crystalline.6. The solid form of claim 1 , which is a cocrystal.7. The solid form of claim 6 , wherein the cocrystal is anhydrous.8. The solid form of having a DSC thermogram with a peak onset of about 146.4° C. or a peak maximum at about 147.8° C.9. The solid form of having a DSC thermogram which is substantially similar to the DSC thermogram of .10. A pharmaceutical composition comprising the solid form of .11. The pharmaceutical composition of claim 10 , further comprising a pharmaceutically acceptable excipient or carrier.12. A solid form comprising cannabidiol and the coformer D-proline.13. The solid form of having an x-ray diffraction pattern comprising one or more peaks at 5.2 claim 12 , 5.8 claim 12 , 9.4 claim 12 , 10.6 claim 12 , 11.2 claim 12 , 11.5 claim 12 , 12.4 claim 12 , 12.7 claim 12 , 15.3 claim 12 , 15.7 claim 12 , 16.4 claim 12 , 17.4 claim 12 , 18.7 claim 12 , 19.2 claim 12 , 19.4 claim 12 , 20.2 ...

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Номер записи: 72
04-06-2020 дата публикации

CLEAVABLE AGENTS

Номер: US20200172493A1
Автор: Chekmenev Eduard Y., Goodson Boyd M., Hou Yuqing, Kidd Bryce E., Limbach Miranda, Mashni Jamil A., Shi Fan
Принадлежит:

The present disclosure is directed to a cleavable agent for enhanced magnetic resonance generally corresponding to the formula Y-L-R, wherein Y represents a catalyst-binding moiety having at least one isotopically labeled heteroatom, L represents a cleavable bond, and R represents a hyperpolarized payload having at least one isotopically labeled carbon. Also disclosed herein is a method of cleaving the cleavable agent for enhanced magnetic resonance. 2. The cleavable agent of claim 1 , wherein Y is bound to a SABRE catalyst.3. The cleavable agent of claim 2 , wherein the SABRE catalyst is an iridium-type catalyst.4. The cleavable agent of claim 1 , wherein Y contains at least one isotopically labeled nitrogen.5. The cleavable agent of claim 1 , wherein R comprises a carboxylic acid or carboxylate thereof claim 1 , urea claim 1 , an amino acid claim 1 , a molecule involved in lipid metabolism claim 1 , a neurotransmitter claim 1 , a sugar claim 1 , a nucleic acid claim 1 , a drug claim 1 , a metabolite claim 1 , or another molecule that binds to or is a substrate of enzymes or other proteins or biomacromolecules6. The cleavable agent of claim 5 , wherein R comprises a carboxylic acid or carboxylate thereof involved in a metabolic cycle claim 5 , an amino acid selected from the group consisting of alanine claim 5 , glutamine claim 5 , and arginine claim 5 , choline or a derivative thereof claim 5 , glucose claim 5 , or fructose.7. The cleavable agent of claim 5 , wherein R is a carboxylic acid or a carboxylate thereof.8. The cleavable agent of claim 5 , wherein R is an amino acid.10. The cleavable agent of claim 9 , wherein Ris methylene.11. The cleavable agent of claim 9 , wherein Ris a bond.12. The cleavable agent of claim 9 , wherein Ris methyl or C(O)OH.13. The cleavable agent of claim 9 , wherein Ris methyl claim 9 , ethenyl claim 9 , pyridyl claim 9 , CF claim 9 , guanidine claim 9 , or acrylic carboxylate.14. A method of cleaving the cleavable agent of for ...

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Номер записи: 73
04-06-2020 дата публикации

METHODS FOR PREPARING OLTIPRAZ

Номер: US20200172522A1
Автор: Framroze Bomi P.
Принадлежит:

The invention provides improved methods of synthesizing oltipraz, which result in higher overall yield and better purity of the desired product. 120-. (canceled)21. A method of making a composition comprising oltipraz , comprising the steps of:(i) reacting a quantity of pyrazine-2-carboxylic acid methyl ester with methyl propionate to form methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate, wherein the reaction is carried out in the presence of a base comprising potassium t-butoxide or sodium pentanoate, and a solvent comprising 1,4-dioxane in tetrahydrofuran (THF), wherein the ratio of 1,4-dioxane in the THF is at least about 1:5;(ii) adding at least one aqueous liquid to quench the reaction in Step (i);(iii) adding a nonpolar organic solvent and an ionic salt, thereby forming a composition comprising an aqueous component and an organic component, wherein the organic component comprises the nonpolar solvent and methyl 2-methyl-3-oxo-3-(pyrazin-2-yl) propanoate;(iv) separating the organic component from the aqueous component;{'sub': 2', '5, '(v) reacting the methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate ester in the organic component with PSin the presence of a nonpolar organic solvent to form 4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione (oltipraz).'}22. A method according to claim 21 , wherein the ratio of 1 claim 21 ,4-dioxane to THF in Step (i) is from about 1:5 to about 1:3.23. A method according to claim 22 , wherein claim 22 , the ratio of 1 claim 22 ,4-dioxane to THF is about 1:4.24. A method according to claim 21 , wherein the base comprises potassium t-butoxide.25. A method according to claim 21 , wherein the mole ratio of the base to methyl propionate is from about 3:1 to about 1:1.26. A method according to claim 21 , wherein the nonpolar organic solvent used in Step (iii) comprises toluene.27. A method according to claim 21 , wherein the nonpolar organic solvent in Step (v) comprises toluene.28. A method according to claim 21 , wherein the nonpolar ...

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Номер записи: 74
07-07-2016 дата публикации

PHENICOL ANTIBACTERIALS

Номер: US20160194342A1
Автор: Curtis Michael, Ewin Richard A, Johnson Timothy Allan, Sheehan Susan M.K.
Принадлежит:

The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds. 124-. (canceled)25. A compound selected from the group consisting of:N-((1R,2S)-1-(4-(6-(1-aminocyclopropyl)pyridin-3-yl)phenyl)-3-fluoro-1-hydroxypropan-2-yl)-2,2-dichloroacetamide;2,2-Difluoro-N-{(1S,2R)-1-fluoromethyl-2-hydroxy-2-[4-(6-pyrrolidin-2-yl-pyridin-3-yl)-phenyl]-ethyl}-acetamide;2,2-dichloro-N-{(1S,2R)-1-(fluoromethyl)-2-hydroxy-2-{4-(6-pyrrolidin-2-ylpyridin-3-yl)phenyl}ethyl}acetamideN-((1R,2S)-1-(4-(6-((S)-1-amino-2-hydroxyethyl)-pyridin-3-yl)phenyl)-3-fluoro-1-hydroxypropan-2-yl)-2,2-difluoroacetamide, its enantiomers, diastereomers, or a pharmaceutically acceptable salt thereof.26. A compound selected from the group consisting of:2,2-dichloro-N-((1R,2S)-3-fluoro-1-hydroxy-1-(4-(6-(methylsulfonamidomethyl)pyridin-3-yl)phenyl)propan-2-yl)acetamide;2,2-dichloro-N-((1R,2S)-3-fluoro-1-hydroxy-1-(4-(6-(1-(methylsulfonyl)pyrrolidin-2-yl)pyridin-3-yl)phenyl)propan-2-yl)acetamide;2,2-dichloro-N-((1R,2S)-3-fluoro-1-hydroxy-1-(4-(6-(1-(methylsulfonamido)ethyl)pyridin-3-yl)phenyl)propan-2-yl)acetamide;2,2-difluoro-N-((1R,2S)-3-fluoro-1-hydroxy-1-(4-(6-(methylsulfonamidomethyl)pyridin-3-yl)phenyl)propan-2-yl)acetamide;N-((1R,2S)-1-(4-(6-(2-aminopropan-2-yl)pyridin-3-yl)phenyl)-3-fluoro-1-hydroxypropan-2-yl)-2,2-difluoroacetamide;N-((1R,2S)-1-(4-(2-(1-aminoethyl)thiazol-5-yl)phenyl)-3-fluoro-1-hydroxypropan-2-yl)-2,2-difluoroacetamide;2,2-Difluoro-N-[(1R,2R)-1-fluoromethyl-2-(4-{6-[(3-fluoro-propylamino)-methyl]-pyridin-3-yl}-phenyl)-2-hydroxy-ethyl]-acetamide;N-((1S,2R)-2-{4-[6-(1-Amino-2,2,2-trifluoro-ethyl)-pyridin-3-yl]-phenyl}-1-fluoromethyl-2-hydroxy-ethyl)-2,2-difluoro-acetamide;2,2-Difluoro-N-((1S,2R)-1-fluoromethyl-2-hydroxy-2-{4-[6-(1-morpholin-4-yl-ethyl)-pyridin-3-yl]-phenyl}-ethyl)-acetamide;2,2-Difluoro-N-((1S,2R)-1- ...

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Номер записи: 75
23-07-2015 дата публикации

ARYLOXYUREA COMPOUND AND PEST CONTROL AGENT

Номер: US20150203448A1
Автор: Furukawa Hironori, HANAI Daisuke, Nakamura Takehiko, Tamai Tetsuo
Принадлежит: NIPPON SODA CO., LTD.

The present invention provides a pest control agent, acaricide or fungicide that contains, as the active ingredient thereof, at least one type of compound selected from the aryloxyurea compounds represented by formula (V) (wherein Rto Reach independently represents an alkyl group or the like, X is a halogen atom or the like, n is an integer of 0 to 5, and Z is an oxygen atom or sulfur atom) or salts thereof 2. A pest control agent claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient.3. An acaricide claim 1 , comprising at least one of the aryloxyurea compound or a salt thereof according to as an active ingredient. This application is a Continuation of U.S. application Ser. No. 13/877,769, which is the National Stage application of PCT/JP2011/073082, filed Oct. 6, 2011, which claims priority from Japanese Patent Application No. 2010-229617, filed Oct. 12, 2010, the contents of which are incorporated herein by reference.The present invention relates to a novel pest control agent. More specifically, the present invention relates to an aryloxyurea compound, which is superior in acaricidal activity and/or fungicidal activity, superior in properties and safety, and which can be industrially and advantageously synthesized, and an acaricide and/or fungicide including the aryloxyurea compound as an active ingredient.Compounds represented by formulas (A) to (E), which are structurally relevant to the compound of the present invention, are disclosed in Patent documents 1 to 5.In the formula, Rrepresents a C1-6 alkyl group.Rrepresents a hydrogen atom.In the formula, Xrepresents a hydrogen atom, chlorine atom or the like.Yrepresents a hydrogen atom, chlorine atom or the like.Rrepresents a phenyl group or the like.Rrepresents a hydrogen atom, lower alkyl group or the like.Rrepresents a hydrogen atom.A represents a carbon atom or nitrogen atom.In the formula, Xrepresents a hydrogen atom, halogen atom, C1-8 alkyl group ...

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Номер записи: 76
22-07-2021 дата публикации

ANTIBODY AGAINST ADVANCED GLYCATION END PRODUCTS AND USE THEREOF

Номер: US20210221879A1
Автор: CHIRIFU Mami, SASAMOTO Kazumi, SHIGETA Tomoaki, TSUCHIDA Shota, Yamamoto Tetsuro
Принадлежит:

The present invention is directed to providing a monoclonal antibody having high selectivity and affinity for AGEs, particularly, AGEs derived from glyceraldehyde or AGEs derived from glycolaldehyde, and an analysis method utilizing the same. Another object of the present invention is to provide methods for diagnosing, treating and preventing a disease using the monoclonal antibody. 6. The monoclonal antibody or the antigen binding fragment thereof according to claim 1 , which is capable of binding to an epitope contained in AGEs derived from glyceraldehyde.7. The monoclonal antibody or the antigen binding fragment thereof according to claim 1 , which is an full-length antibody claim 1 , Fab claim 1 , Fab′ claim 1 , F(ab′) claim 1 , Fv claim 1 , scFv claim 1 , dsFv claim 1 , diabody claim 1 , or sc(Fv).8. The monoclonal antibody or the antigen binding fragment thereof according to claim 1 , which is a mouse antibody claim 1 , a humanized antibody claim 1 , a human antibody claim 1 , a chimeric antibody claim 1 , or an antigen binding fragment thereof.9. The monoclonal antibody or the antigen binding fragment thereof according to claim 1 , which is capable of binding to an epitope of AGEs derived from glyceraldehyde or AGEs derived from glycolaldehyde with a dissociation constant (Kd value) of 1×10M or less.10. A pharmaceutical composition comprising the monoclonal antibody or the antigen binding fragment thereof as defined in .11. The pharmaceutical composition according to claim 10 , for use in diagnosis claim 10 , treatment or prevention of a disease selected from obesity claim 10 , diabetes mellitus claim 10 , diabetic retinopathy claim 10 , diabetic cataract claim 10 , diabetic neuropathy claim 10 , diabetic cardiomyopathy claim 10 , diabetic vascular complications claim 10 , diabetic nephropathy claim 10 , diabetic renal disease claim 10 , diabetic foot claim 10 , diabetic ketoacidosis claim 10 , periodontal disease claim 10 , age-related macular degeneration ...

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Номер записи: 77
29-07-2021 дата публикации

PYRAZINE COMPOUND

Номер: US20210230137A1
Автор: KIMURA Takahiro, Nakajima Yuji, Nokura Yoshihiko, ORIMOTO Kohei, Tanabe Takamasa
Принадлежит:

Provided is a compound represented by formula (I): This application is a Divisional of U.S. patent application Ser. No. 16/710,035, filed Dec. 11, 2019, which is a Divisional of U.S. patent application Ser. No. 15/766,034, filed Apr. 5, 2018 (now issued U.S. Pat. No. 10,577,343), which is a Section 371 of International Application No. PCT/JP2016/080410, filed Oct. 13, 2016, which was published in the Japanese language on Apr. 20, 2017, under International Publication No. WO 2017/065228 A1, which claims priority under 35 U.S.C. § 119(b) to Japanese Application No. 2015-204376, filed Oct. 16, 2015, Japanese Application No. 2015-208639, filed Oct. 23, 2015, and Japanese Application No. 2016-149448, filed Jul. 29, 2016, the disclosures of all of which are incorporated herein by reference in their entireties.The present invention is related to a certain class of pyrazine compound and its use for controlling harmful arthropods.To date, some compounds for controlling harmful arthropods have been developed and come into practical use. Also, a certain class of compounds has been known to be effective for controlling harmful organisms (see Patent Document 1).An object of the present invention is to provide a compound having an excellent efficacy for controlling harmful arthropods.The present invention provides, for example, the following embodiments.[1] A compound represented by formula (I) or its N oxide compound:[whereinArepresents a nitrogen atom or a CR;Rrepresents a hydrogen atom, a OR, a NRR, a cyano group, a nitro group, or a halogen atom;Rrepresents a C2-C10 chain hydrocarbon group having one or more halogen atoms, a (C1-C5 alkoxy)C2-C5 alkyl group having one or more halogen atoms, a (C1-C5 alkylsulfanyl)C2-C5 alkyl group having one or more halogen atoms, a (C1-C5 alkylsulfinyl)C2-C5 alkyl group having one or more halogen atoms, a (C1-C5 alkylsulfonyl)C2-C5 alkyl group having one or more halogen atoms, a (C3-C7 cycloalkyl)C1-C3 alkyl group having one or more ...

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Номер записи: 78
28-07-2016 дата публикации

Production And Use Of Zinc Amides

Номер: US20160215000A1
Автор: Knochel Paul, MOSRIN Marc
Принадлежит:

Compounds, methods of making the compounds and methods of using the compounds are generally described herein. The compounds are generally of formula RRN—ZnY LiY, wherein Rand Rare independently selected from H, aryl, heteroaryl containing one or more heteroatoms, alkyl, alkenyl, alkynyl, and silicon derivatives thereof; and each Y is independently selected from F, Cl, Br, I, CN, SCN, NCO, HalO, HalO, NO, BF, PF, H, an alcoholate of formula OR, a carboxylate of formula RCO; a thiolate of formula SR, RP(O)O, SCOR, SCSR, OSRand NO, wherein n=2 or 3; wherein Ris selected from substituted or unsubstituted aryls or heteroaryls containing 3 to 24 carbon atoms and one or more heteroatoms selected from B, O, N, S, Se, P, linear, branched or cyclic, substituted or unsubstituted alkyls, alkenyls, alkynyls or H; and wherein Hal is a halogen selected from Cl, Br and I. 1. A compound of formula RRN—ZnY LiY wherein{'sup': 1', '2, 'Rand Rare independently selected from H, aryl, heteroaryl containing one or more heteroatoms, alkyl, alkenyl, alkynyl, and silicon derivatives thereof; and'}{'sub': 3', '4', '3', '4', '6', '2', '2', 'n', 'n, 'sup': 5', '5', '5', '5', '5', '5', '5', '5, 'each Y is independently selected from F, Cl, Br, I, CN, SCN, NCO, HalO, HalO, NO, BF, PF, H, an alcoholate of formula OR, a carboxylate of formula RCO; a thiolate of formula SR, RP(O)O, SCOR, SCSR, OSRand NO, wherein n=2 or 3; wherein Ris selected from substituted or unsubstituted aryls or heteroaryls containing 3 to 24 carbon atoms and one or more heteroatoms selected from B, O, N, S, Se, P, linear, branched or cyclic, substituted or unsubstituted alkyls, alkenyls, alkynyls or H; and wherein Hal is a halogen selected from Cl, Br and I.'}2. The compound of claim 1 , wherein Rand Rform together in connection with N to form a cyclic structure.3. The compound of claim 2 , wherein the cyclic structure comprises an amine.4. The compound of claim 2 , wherein the amine comprises piperidine and wherein each Y is ...

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Номер записи: 79
11-08-2016 дата публикации

TETRA-ARYL CYCLOBUTANE INHIBITORS OF ANDROGEN RECEPTOR ACTION FOR THE TREATMENT OF HORMONE REFRACTORY CANCER

Номер: US20160229811A1
Автор: Carlson Kathryn E., Gunther Jillian, Katzenelienbogen John, Martin Teresa, McDonneli Donald, Norris John D, Parent Alexander, Pollock Julie
Принадлежит:

The present disclosure provides tetra-substituted cyclobutane inhibitors of Androgen Receptor Action, and methods of using such inhibitors, for the treatment of hormone-refractory cancers. 18. A compound according to wherein{'sup': 1', '2', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3, 'sub': 1', '8', '3', '8', '2', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '2', '1', '8', '1', '8', '1', '8', '8', '8', '1', '8, 'each of Rand Rare independently selected from (a) F, (b) Cl, (c) —C-Calkyl, (d) —C-Ccycloalkyl, (e) phenyl, (f) a 7 to 10-membered saturated, unsaturated, or aromatic fused bicyclic carbocyle, (g) a 3 to 10-membered saturated, unsaturated, or aromatic heterocycle or fused bicyclic heterocycle containing one or more heteroatoms selected from nitrogen, oxygen, sulfur, and combinations thereof, (h) —OR, (i) —NRR, (j) —CN, (k) —SR, (l) —SOR, (m) —SOR, (n) —COOR, (o) —COR, (p) —CONRR, (q) —NRCOR—, (r) —NRCONRR, (s) —(C-Calkyl)OR, (t) —(C-Calkyl)NRR, (u) —(C-Calkyl)SR, (v) —(C-Calkyl)SOR, (w) —(C-Calkyl)SOR, (x) —(C-Calkyl)COOR, (y) —(C-Calkyl)COR, (z) —(C-Calkyl)CONRR, (aa) —(C-Calkyl)NRCOR, and (bb) —(C-Calkyl)NRCONRR,'}{'sub': 2', '1', '8', '1', '8', '2, 'wherein each of (c) or (d) immediately recited above is optionally substituted with one or more F, Cl, —OH, —SH, —NH, —NH(C-Calkyl), or —N(C-Calkyl)and'}{'sup': 4', '5, 'wherein each of (e) through (g) immediately recited above is optionally substituted with one more Ror R;'}{'sup': '3', 'sub': 1', '8', '3', '8', '1', '8', '1', '8, 'each Ris independently selected from (a) H, (b) —C-Calkyl, (c) —C-Ccycloalkyl, (d) phenyl, (e) naphthyl, (f) —C-Calkyl(phenyl), and (g) —C-Calkyl(naphthyl), wherein each of (b) through (g) immediately recited above is optionally substituted with one or more R5;'}{'sup': 4', '5, 'sub': 1', '8', '3', '8, 'each Ris independently selected from one or more (a) F, (b) Cl, (c) —C- ...

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Номер записи: 80
17-08-2017 дата публикации

NOVEL COMPOUNDS AS ROR GAMMA MODULATORS

Номер: US20170233380A1
Автор: Bajpai Malini, Das Sanjib, Gharat Laxmikant A., Harde Rajendra L., KHAIRATKAR-JOSHI Neelima, Pardeshi Shailesh R., Shah Daisy M., Shelke Sandeep Y., Thomas Abraham
Принадлежит:

The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R, R, R, R, R, R, R, n, m, p and q are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer. 156-. (canceled)58. The compound according to claim 57 , wherein ring B is cyclohexyl claim 57 , phenyl claim 57 , 6-oxo-1 claim 57 ,6-dihydropyridinyl claim 57 , piperidinyl claim 57 , piperazinyl claim 57 , morpholinyl claim 57 , isoxazolyl claim 57 , pyrazolyl claim 57 , thiazolyl claim 57 , pyridinyl or pyrimidinyl.59. The compound according to claim 57 , wherein L is absent.61. The compound according to claim 57 , wherein Ris hydroxyl claim 57 , methyl or methoxy.62. The compound according to claim 57 , wherein ‘n’ is 0.63. The compound according to claim 57 , wherein each Ris independently cyano claim 57 , F claim 57 , Cl claim 57 , methyl claim 57 , ethyl claim 57 , methoxy claim 57 , methoxyethyl claim 57 , trifluoromethyl claim 57 , cyclopropyl claim 57 , C(O)methyl claim 57 , C(O)cyclopropyl or oxetan-3-yl and ‘n’ is 1 or 2.64. The compound according to claim 57 , wherein ‘m’ is 0.65. The compound according to claim 57 , wherein Ris methyl claim 57 , tert-butyl or trifluoromethyl and ‘m’ is 1.66. The compound according to claim 57 , wherein ‘p’ is 0.67. The compound according to claim 57 , wherein one of Rand Ris hydrogen and the other is hydrogen or methyl.68. The compound according to claim 57 , wherein Ris methyl; Ris hydrogen and Ris hydrogen.69. The compound according to claim 57 , wherein Ris hydroxyl; Ris hydrogen and Ris methyl.78. The compound according to ...

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Номер записи: 81
14-10-2021 дата публикации

NOVEL SUBSTITUTED BIARYL COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS

Номер: US20210317091A1
Автор: Achab Abdelghani, Bharathan Indu, Fradera Xavier, Han Yongxin, Li Derun, Sciammetta Nunzio, Yu Wensheng
Принадлежит: Merck Sharp & Dohme Corp.

Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an 1DO-associated disease or disorder. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 ,wherein:n is 1;p is 0 or 1;{'sup': a', 'b', 'a', 'b, 'sub': '1-6', 'M is selected from —O— and —CRR—, each of Rand Ris independently selected from H, halogen, —OH and —Calkyl;'}{'sup': '1', 'claim-text': (1) aryl, and', '(2) heterocyclyl;', (a) halogen,', {'sub': '3-6', '(b) —Ccycloalkyl, optionally substituted with —OH,'}, '(c) —CN,', {'sub': '1-6', '(d) —O—Calkyl, optionally substituted with 1-3 halogens,'}, {'sub': '3-6', '(e) —O—Ccycloalkyl,'}, {'sub': 1-6', '2', '2', '1-6', '1-6', '3-6, 'sup': c', 'c, '(f) —Calkyl, optionally substituted with 1-4 substituents independently selected from halogen, —OH, —NH, NHC(O)R, and —S(O)—Calkyl, wherein Ris selected from —Calkyl and —Ccycloalkyl,'}, {'sub': 2', '1-6', '3-6, 'sup': c', 'c, '(g) —NH—S(O)—R, wherein Ris selected from —Calkyl and —Ccycloalkyl,'}, '(h) —C(O)—OH, and', {'sub': '1-6', '(i) heterocyclyl, optionally substituted with 1-3 substituents independently selected from halogen and —Calkyl;'}], 'wherein each of the aryl of (1) and the heterocyclyl of (2) is optionally substituted with 1-3 substituents independently selected from], 'Ris selected from{'sup': '2', 'claim-text': [{'sub': '1-6', '(1) Calkyl, optionally substituted with 1-3 halogens,'}, {'sub': '3-6', '(2) Ccarbocyclyl,'}, '(3) aryl, and', '(4) heterocyclyl;', {'sub': '3-6', 'claim-text': (a) halogen,', {'sub': '3-6', '(b) —Ccycloalkyl,'}, '(c) —CN,', {'sub': '1-6', '(d) —O—Calkyl, optionally substituted with 1-3 halogens, ...

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Номер записи: 82
06-08-2020 дата публикации

K-RAS MODULATORS

Номер: US20200247762A1
Автор: DYBA Marcin, Kumari Vandana, Maciag Anna E., McCormick Frank, Renslo Adam, Saavedra Joseph, Turner David, VO Elizabeth D.
Принадлежит:

Provided herein, inter alia, are methods and compounds for modulating K-Ras treating cancer. 2. (canceled)5. The compound of claim 1 , wherein the compound is of Formula (I) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:Ring A is phenyl;{'sup': 1', '1', '1', '1', '1D', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1C', '1C', '1A', '1B', '1D', '1A', '1D', '1A', '1C', '1A', '1C', '1A', '1C', '1', '1', '1, 'sub': 3', '2', '2', 'n1', 'v1', 'm1', '2', '3', '2', '2, 'Ris independently halogen, —CX, —CHX, —CHX, —CN, —SOR, —SONRR, —NHNRR, —ONRR, —NHC═(O)NHNRR, —NHC(O)NRR, —N(O), —NRR, —C(O)R, —C(O)—OR, —C(O)NRR, —OR, —NRSOR, —NRC(O)R, —NRC(O)OR, —NROR, —OCX, —OCHX, —OCHX, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl; or'}{'sup': '1', 'two adjacent Rsubstituents may optionally be joined to form a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;'}z1 is an integer from 0 to 4;{'sup': 2', '2', '2', '2', '2A', '2A', '2A', '2B, 'sub': 3', '2', '2, 'Ris independently hydrogen, —CX, —CHX, —CHX, —C(O)R, —C(O)OR, —C(O)NRR, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;'}{'sup': '1', 'Lis a bond, substituted or unsubstituted alkylene, or substituted or unsubstituted cycloalkylene;'}{'sup': 3', '3', '3', '3', '3', '3, 'sub': '2', 'Lis a bond, —S(O)—, —N(R)—, —O—, —S—, —C(O)—, —C(O)N(R)—, —N(R)C(O)—, —N(R)C(O)NH—, —NHC(O)N(R)—, —C(O)O—, —OC(O)—, substituted or unsubstituted alkylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted cycloalkylene, substituted or unsubstituted ...

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Номер записи: 83
06-08-2020 дата публикации

METHODS FOR PREPARING OLTIPRAZ

Номер: US20200247791A1
Автор: Framroze Bomi P.
Принадлежит: ST IP Holding AG

The invention provides improved methods of synthesizing oltipraz, which result in higher overall yield and better purity of the desired product. 120-. (canceled)21. A method of making a composition comprising oltipraz , comprising the steps of:reacting a quantity of pyrazine-2-carboxylic acid methyl ester with methyl propionate to form methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate, wherein the reaction is carried out in the presence of a base comprising potassium t-butoxide or sodium pentanoate, and a solvent comprising 1,4-dioxane in tetrahydrofuran (THF), wherein the ratio of 1,4-dioxane in the THF is at least about 1:5;(ii) adding at least one aqueous liquid to quench the reaction in Step (i);(iii) adding a nonpolar organic solvent and an ionic salt, thereby forming a composition comprising an aqueous component and an organic component, wherein the organic component comprises the nonpolar solvent and methyl 2-methyl-3-oxo-3-(pyrazin-2-yl) propanoate;(iv) separating the organic component from the aqueous component;{'sub': 2', '5, '(v) reacting the methyl 2-methyl-3-oxo-3-(pyrazin-2-yl)propanoate ester in the organic component with PSin the presence of a nonpolar organic solvent to form 4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione (oltipraz).'}22. A method according to claim 21 , wherein the ratio of 1 claim 21 ,4-dioxane to THF in Step (i) is from about 1:5 to about 1:3.23. A method according to claim 22 , wherein claim 22 , the ratio of 1 claim 22 ,4-dioxane to THF is about 1:4.24. A method according to claim 21 , wherein the base comprises potassium t-butoxide.25. A method according to claim 21 , wherein the mole ratio of the base to methyl propionate is from about 3:1 to about 1:1.26. A method according to claim 21 , wherein the nonpolar organic solvent used in Step (iii) comprises toluene.27. A method according to claim 21 , wherein the nonpolar organic solvent in Step (v) comprises toluene.28. A method according to claim 21 , wherein the nonpolar ...

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Номер записи: 84
22-08-2019 дата публикации

NOVEL COMPOUNDS AS ROR GAMMA MODULATORS

Номер: US20190256508A1
Автор: Bajpai Malini, Das Sanjib, Gharat Laxmikant A., Harde Rajendra L., KHAIRATKAR-JOSHI Neelima, Pardeshi Shailesh R., Shah Daisy M., Shelke Sandeep Y., Thomas Abraham
Принадлежит:

The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R, R, R, R, R, R, R, n, m, p and q are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer. 156-. (canceled)59. The process according to claim 57 , wherein the compound of formula (1) is reacted with a compound of formula (2) in the presence of a coupling agent.60. The process according to claim 59 , wherein the coupling agent is selected from 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDCI) claim 59 , propylphosphonic anhydride (TP) claim 59 , N claim 59 ,N′-dicyclohexylcarbodiimide (DCC) and (1-[bis(dimethylamino)methylene]-1H-1 claim 59 ,2 claim 59 ,3-triazolo[4 claim 59 ,5-b]pyridinium 3-oxid hexafluorophosphate) (HATU) or combination thereof.61. The process according to claim 57 , wherein the compound of formula (1) is reacted with a compound of formula (2) in the presence of a base.62. The process according to claim 61 , wherein the base is selected from EtN claim 61 , DIPEA claim 61 , pyridine or DMAP.63. The process according to claim 57 , wherein the compound of formula (1) is reacted with a compound of formula (2) in the presence of a coupling agent and a base.66. The process according to claim 64 , wherein the compound of formula (1) is reacted with a compound of formula (3) in the presence of a coupling agent.67. The process according to claim 66 , wherein the coupling agent is selected from 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDCI) claim 66 , propylphosphonic anhydride (TP) claim 66 , N claim 66 ,N′-dicyclohexylcarbodiimide (DCC) and (1-[ ...

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Номер записи: 85
11-12-2014 дата публикации

COMPOUNDS FOR ORGANIC ELECTROLUMINESCENT DEVICES

Номер: US20140361224A1
Автор: Buesing Arne, Eberle Thomas, Mjuica-Fernaud Teresa, Parham Amir Hossain, Pflumm Christof, Philipp Stoessel
Принадлежит:

The present invention relates to boron compounds for use in electronic devices, especially organic electroluminescent devices, and to a process for preparing these compounds and to electronic devices, especially organic electroluminescent devices, comprising these compounds. 114.-. (canceled)16. The compound according to claim 15 , wherein Arstands claim 15 , identically or differently on each occurrence claim 15 , for an aryl or heteroaryl group having 5 to 10 aromatic ring atoms claim 15 , which may in each case be substituted by one or more radicals R.17. The compound according to claim 15 , wherein Arstands claim 15 , identically or differently on each occurrence claim 15 , for benzene claim 15 , pyridine claim 15 , pyrimidine claim 15 , pyridazine claim 15 , pyrazine claim 15 , furan claim 15 , thiophene claim 15 , pyrrole claim 15 , naphthalene claim 15 , phenanthrene claim 15 , quinoline claim 15 , isoquinoline claim 15 , quinoxaline claim 15 , indole claim 15 , benzofuran or benzothiophene claim 15 , each of which is optionally substituted by one or more radicals R.19. The compound according to claim 15 , wherein Y stands claim 15 , identically or differently on each occurrence claim 15 , for N—R.20. The compound according to claim 15 , wherein Lor Lstands claim 15 , identically or differently on each occurrence claim 15 , for a single bond or a divalent arylene or heteroarylene group having 5 to 10 aromatic ring atoms claim 15 , which may in each case be substituted by one or more radicals R.21. The compound according to claim 15 , wherein Lor Lstands claim 15 , identically or differently on each occurrence claim 15 , for a single bond or a 1 claim 15 ,2- claim 15 , 1 claim 15 ,3- or 1 claim 15 ,4-phenylene claim 15 , pyridine claim 15 , pyrimidine or triazine claim 15 , each of which is optionally substituted by one or more radicals R.22. The compound according to claim 15 , wherein Arand Arare built up from in each case one or more groups selected from ...

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Номер записи: 86
27-09-2018 дата публикации

METHODS OF SELECTIVELY FORMING SUBSTITUTED PYRAZINES

Номер: US20180273492A1
Автор: Coleman, Dube Michael Francis, III William Monroe
Принадлежит:

Methods of selectively forming substituted pyrazines are provided. Methods of the present invention can include receiving a reaction solution including at least one carbon source and at least one nitrogen source, and heating the reaction solution to a reaction temperature and holding the reaction solution at the reaction temperature for a time sufficient to produce a reaction product comprising at least one substituted pyrazine. The carbon source can be selected from the group consisting of hydroxy ketone(s), sugar(s) treated with at least one buffer, and combinations thereof. Tobacco products incorporating substituted pyrazines are also provided. 1. A method of forming pyrazines comprising:receiving a reaction solution comprising at least one alpha-hydroxy ketone and at least one nitrogen source; andheating the reaction solution to a reaction temperature and holding the reaction solution at the reaction temperature for a time sufficient to produce a reaction product comprising at least one substituted pyrazine.2. The method of claim 1 , wherein the at least one hydroxy ketone comprises acetol.3. The method of claim 2 , wherein the at least one substituted pyrazine is selected from the group consisting of: 2 claim 2 ,3-dimethylpyrazine; 2 claim 2 ,6-dimethylpyrazine; 2-ethyl-6-methylpyrazine; 2-ethyl-5-methylpyrazine; trimethylpyrazine; furaneol; 2 claim 2 ,5-dimethyl-3-ethylpyrazine; 2-ethyl-3 claim 2 ,5-dimethylypyrazine; tetramethylpyrazine; 2 claim 2 ,5-dimethyl-3-propenylpyrazine; 2 claim 2 ,3 claim 2 ,5-trimethyl-6-isopropylpyrazine; 2-acetyl-4 claim 2 ,5-dimethylpyrazine; 3 claim 2 ,5-dimethyl-2-methylpropylpyrazine claim 2 , and combinations thereof.4. The method of claim 1 , wherein the at least one hydroxy ketone comprises acetoin.5. The method of claim 4 , wherein the at least one substituted pyrazine is tetramethylpyrazine.6. The method of claim 1 , wherein the at least one hydroxy ketone comprises 1-hydroxy-2-butanone.7. The method of claim 6 , wherein ...

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Номер записи: 87
27-09-2018 дата публикации

BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS

Номер: US20180273553A1
Автор: Jacobs Robert T., Plattner Jacob J., Zhang Yong-Kang
Принадлежит:

This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. 3. The compound of claim 2 , wherein the compound is according to formula (Ia).4. The compound of claim 2 , wherein the compound is according to formula (IIa).5. The compound of claim 1 , wherein Y is substituted or unsubstituted C-Calkyl.6. The compound of claim 1 , wherein Y is substituted or unsubstituted methyl.8. The compound of claim 7 , wherein Ris H.9. The compound of claim 7 , wherein Ris unsubstituted C-Calkyl or halosubstituted C-Calkyl or unsubstituted C-Ccycloalkyl.10. The compound of claim 7 , wherein Ris methyl or ethyl or propyl or isopropyl or trifluoromethyl or difluoromethyl or trifluoroethyl or cyclopropyl.11. The compound of claim 7 , wherein Ris H.12. The compound of claim 7 , wherein Ris H.13. The compound of claim 1 , selected from the following group:5-((1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)oxy)-N-(2-hydroxyethyl) pyrazine-2-carboxamide;5-(1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yloxy)-N-(2-methoxyethyl)pyrazine-2-carboxamide;N-(1-hydroxy-2-methylpropan-2-yl)-5-(1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yloxy)pyrazine-2-carboxamide;N-(2-hydroxy-2-methylpropyl)-5-(1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yloxy)pyrazine-2-carboxamide;5-(1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yloxy)-N-(1-hydroxypropan-2-yl)pyrazine-2-carboxamide;5-(1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yloxy)-N,N-bis(2-hydroxyethyl)pyrazine-2-carboxamide;N-(1-hydroxy-3-methylbutan-2-yl)-5-(1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yloxy)pyrazine-2-carboxamide;N-(1-hydroxy-4-methylpentan-2-yl)-5-((1-hydroxy-7-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)oxy)pyrazine-2-carboxamide;5-(1-hydroxy-7-methyl-1,3-dihydrobenzo[c ...

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Номер записи: 88
12-09-2019 дата публикации

Pyrazine derivative, and preparation method and medical use thereof

Номер: US20190276413A1
Автор: Shan Luchen, SUN Yewei, WANG Yuqiang, Yi Peng, YU Pei, ZHANG Gaoxiao, ZHANG Zaijun
Принадлежит: Guangzhou Magpie Pharmaceuticals Co., Ltd.

The present invention relates to a pyrazine derivative, and preparation method and medical use thereof. The pyrazine derivative can remove free radicals and suppress calcium overload and has cytoprotective effects, and can be used for the prevention and treatment of cardiovascular and cerebrovascular diseases, neurodegenerative diseases and other related diseases. 8. A method of preparation of the pyrazine derivative of claim 1 , the method comprising:tetramethylpyrazine is first reacted with NBS to give a ligustrazine mono-bromide as intermediate I; ortetramethylpyrazine is oxidized by activated manganese dioxide to give a para-substituted tetramethylpyrazine dialdehyde derivative, which is subjected to selective reduction, bromination and aldehyde group protection to give a para-substituted tetramethylpyrazine derivative as intermediate II; andthe intermediate I or intermediate II is further reacted to give a respective product of the pyrazine derivative.9. The method according to claim 8 , comprising:the intermediate I or intermediate II is reacted with triethyl phosphate to give intermediate III or intermediate IV, respectively;the tetramethylpyrazine dialdehyde derivative is reacted with ethylene glycol, with one of aldehyde groups being selectively protected, to give a product, which is further reacted respectively with the intermediate III or the intermediate IV to give a respective tetramethylpyrazine coupling compound, which is deprotected under acidic conditions and then reacted with t-butylhydroxylamine to give a product of the pyrazine derivative.10. The method according to claim 8 , comprising:the tetramethylpyrazine dialdehyde derivative is reacted with one or two of aldehyde groups being selectively reduced to give a monohydroxy derivative or a dihydroxy derivative;the monohydroxy derivative or the dihydroxy derivative is each reacted with phosphorus tribromide to give a mono-bromo or dibromo derivative, respectively;the mono-bromo derivative is ...

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Номер записи: 89
23-12-2021 дата публикации

SUBSTITUTED TETRACYCLINE COMPOUNDS

Номер: US20210395189A1
Автор: Abato Paul, Bowser Todd
Принадлежит:

The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms. 1391-. (canceled) This application claims priority to U.S. Provisional Patent Application No. 60/876,313, filed on Dec. 21, 2006 and U.S. Provisional Patent Application No. 60/943,003, filed Jun. 8, 2007. The contents of the foregoing applications are hereby incorporated in their entirety.The development of the tetracycline antibiotics was the direct result of a systematic screening of soil specimens collected from many parts of the world for evidence of microorganisms capable of producing bactericidal and/or bacteriostatic compositions. The first of these novel compounds was introduced in 1948 under the name chlortetracycline. Two years later, oxytetracycline became available. The elucidation of the chemical structure of these compounds confirmed their similarity and furnished the analytical basis for the production of a third member of this group in 1952, tetracycline. A new family of tetracycline compounds, without the ring-attached methyl group present in earlier tetracyclines, was prepared in 1957 and became publicly available in 1967; and minocycline was in use by 1972.Recently, research efforts have focused on developing new tetracycline antibiotic compositions effective under varying therapeutic conditions and routes of administration. New tetracycline analogues have also been investigated which may prove to be equal to or more effective than the originally introduced tetracycline compounds. Examples include U.S. Pat. Nos. 2,980,584; 2,990,331; 3,062,717; 3,165,531; 3,454,697; 3,557,280; 3,674,859; 3,957,980; 4,018,889; 4,024,272; and 4,126,680. These patents are representative of the range of pharmaceutically active tetracycline and tetracycline analogue compositions.Historically, soon after their initial development and ...

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Номер записи: 90
10-09-2020 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20200281952A1
Автор: Dhar T.G. Murali, Dyckman Alaric J., Gilmore John L., Marcoux David, Xiao Hai-Yun, Xiao Zili, Yang Michael G.
Принадлежит:

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): 116-. (canceled)19. The compound according to or a salt thereof claim 17 , wherein:{'sub': 2a', '2', '3', '3', '2', '5-6', '3', '2', '2', '3', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '2', '2', '4', '2', '2', '4', '3', '2', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '3', '2', '1-3', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '2', '2', '1-2', '3', '2', '2', '2', '2', '2', '2-3', '2', '2', '3-4', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '9', '3', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '3', '3', '2', '1-6', '3', '3', '2', '2', '3', '2', '2', '3', '3', '3', '2', '2', '2', '3', '3', '2', '3', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '3', '2', '3', '2', '2', '2-4', '3', '2', '3', '2', '2', '2', '3', '2', '2', '2', '3', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '1-2', '3', '2', '2', '2', '3', '2', '2', '3', '3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '2', '4', '3', '2', '2', '4', '3', '3', '2', '4', '3', '2', '3', '2', '5', '3', '2', '2', '4-7', '3', '2', '2', '2', '2-4', '3', '2', '2', '2', '3', '2', '2', '2', '2-3', '3', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2-3', '3', ' ...

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Номер записи: 91
18-10-2018 дата публикации

Pyrazine compound and arthropod pest control agent containing same

Номер: US20180297978A1
Автор: Kohei ORIMOTO, Takahiro Kimura, Takamasa Tanabe, Yoshihiko Nokura, Yuji Nakajima
Принадлежит: Sumitomo Chemical Co Ltd

Provided is a compound represented by formula (I): or an N-oxide compound thereof, wherein the variable groups are as defined in the specification. Also provided is an arthropod pest control agent containing a compound represented by formula (I) and an inert carrier. The compound represented by formula (I) and arthropod pest control agent exhibit an excellent controlling effect against arthropod pests.

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Номер записи: 92
26-10-2017 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20170304332A1
Автор: Dhar T.G. Murali, Dyckman Alaric J., Gilmore John L., Marcoux David, Xiao Hai-Yun, Xiao Zili, Yang Michael G.
Принадлежит:

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): 116-. (canceled)19. The compound according to or a salt thereof claim 17 , wherein:{'sub': 2a', '2', '3', '3', '2', '5', '3', '2', '2', '3', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '2', '2', '4', '2', '2', '4', '3', '2', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '3', '2', '1-3', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '2', '2', '1-2', '3', '2', '2', '2', '2', '2', '2-3', '2', '2', '3-4', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '9', '3', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '3', '3', '2', '1-6', '3', '3', '2', '2', '3', '2', '2', '3', '3', '3', '2', '2', '2', '3', '3', '2', '3', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '3', '2', '3', '2', '2', '2-4', '3', '2', '3', '2', '2', '2', '3', '2', '2', '2', '3', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '1-2', '3', '2', '2', '2', '3', '2', '2', '3', '3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '2', '4', '3', '2', '2', '4', '3', '3', '2', '4', '3', '2', '3', '2', '5', '3', '2', '2', '4-7', '3', '2', '2', '2', '2-4', '3', '2', '2', '2', '3', '2', '2', '2', '2-3', '3', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2-3', '3', '2 ...

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Номер записи: 93
26-09-2019 дата публикации

Volatile dihydropyrazinly and dihydropyrazine metal complexes

Номер: US20190292659A1
Автор: Ivanov Sergei Vladimirovich, Lei Xinjian, Norman John Anthony Thomas
Принадлежит: Versum Materials US, LLC

A composition comprising dihydropyrazinyl anions that can be coordinated as 6 electron ligands to a broad range of different metals to yield volatile metal complexes for ALD and CVD depositions are described herein. Also described herein are undeprotonated dihydropyrazines that can coordinate to metals as stabilizing neutral ligands. In one embodiment, the composition is used for the direct liquid injection delivery of the metal dihydropyrazinyl complex precursor to the chamber of an ALD or CVD chamber for the deposition of metal-containing thin films such as, for example, ruthenium or cobalt metal films. 2. The composition of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , Rare each independently selected from a C-Clinear claim 1 , or branched alkyl group; Ris hydrogen claim 1 , Q is benzene or an alkylated benzene claim 1 , M is cobalt claim 1 , x is 1 claim 1 , Z is hydrogen.3. The composition of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , Rare each independently selected from a C-Clinear claim 1 , or branched alkyl group; Ris hydrogen claim 1 , Q is benzene or an alkylated benzene claim 1 , M is ruthenium claim 1 , x is 1 claim 1 , Z is hydrogen.4. A method for forming a metal oxide film on a substrate wherein the film comprises a thickness claim 1 , the method comprising:a. introducing a metal dihydropyrazinyl complex comprising Formula 3E;b. chemisorbing the metal dihydropyrazinyl complex onto the substrate;c. purging away the metal dihydropyrazinyl complex using a purge gas;d. providing an oxygen source to the metal dihydropyrazinyl complex onto the heated substrate to react with the sorbed metal dihydropyrazinyl complex containing composition; ande. optionally purging away any unreacted oxygen source.5. The method of wherein steps a. through d. and optional step e. are repeated until the thickness of film is established.6. The method of wherein the method is an atomic layer deposition process.7. The method of claim 4 , wherein R claim 4 , R ...

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Номер записи: 94
26-10-2017 дата публикации

HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF

Номер: US20170305900A1
Автор: Allen Daniel R., Breccia Perla, Bürli Roland W., Dominguez Celia, Haughan Alan F., Hughes Samantha J., Jarvis Rebecca E., Luckhurst Christopher A., Maillard Michel, Muñoz-Sanjuán Ignacio, Penrose Stephen D., Saville-Stones Elizabeth A., Stott Andrew J., Vater Huw D., Wall Michael, Wishart Grant
Принадлежит:

Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. 136.-. (canceled)40. The method of claim 37 , or a pharmaceutically acceptable salt thereof claim 37 , wherein Ris —C(O)NH(OH).41. The method of claim 37 , or a pharmaceutically acceptable salt thereof claim 37 , wherein Ris —N(OH)C(O)R.42. The method of claim 37 , wherein Ris phenyl optionally substituted with 1 to 3 substituents independently selected from halo claim 37 , alkyl claim 37 , cycloalkyl claim 37 , haloalkyl claim 37 , hydroxyl claim 37 , alkoxy claim 37 , and nitrile.43. The method of claim 37 , wherein Ris heteroaryl optionally substituted with 1 to 3 substituents independently selected from halo claim 37 , lower alkyl claim 37 , and haloalkyl.44. The method of claim 37 , wherein Ris hydrogen claim 37 , alkyl claim 37 , cycloalkyl claim 37 , heterocycloalkyl claim 37 , aryl claim 37 , heteroaryl claim 37 , aralkyl claim 37 , or heteroaralkyl claim 37 , each of which is optionally substituted with 1 to 3 substituents independently selected from halo claim 37 , alkyl claim 37 , cycloalkyl claim 37 , haloalkyl claim 37 , hydroxyl claim 37 , alkoxy claim 37 , and nitrile.45. A method for treating a patient suffering from a neurodegenerative condition claim 37 , cancer claim 37 , amyotrophic lateral sclerosis (ALS) claim 37 , diabetes claim 37 , a cardiovascular condition claim 37 , epilepsy claim 37 , depression claim 37 , viral infection claim 37 , or fungal infection claim 37 , wherein the method comprises administering to the patient a therapeutically effective amount of a compound claim 37 , or a pharmaceutically acceptable salt thereof claim 37 , selected from:(R)-1-(3-fluoro-2-methylphenyl)-N-hydroxy-3-phenylcyclopent-2-enecarboxamide;(S)-1-(3-fluoro-2-methylphenyl)-N-hydroxy-3-phenylcyclopent-2-enecarboxamide;(R)-1-(3-fluoro-2-methylphenyl)-N-hydroxy-3-(o-tolyl)cyclopent-2-enecarboxamide;(S)-1-(3-fluoro-2-methylphenyl)-N-hydroxy ...

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Номер записи: 95
05-11-2015 дата публикации

Polycyclic organic compound, optically anisotropic film and method of production thereof

Номер: US20150316695A1
Автор: Alexey Nokel, Valery S. Kuzmin
Принадлежит: Crysoptix KK

The polycyclic organic compounds which are substantially transparent for an electromagnetic radiation in the visible spectral range, an anisotropic optical film comprising at least one polycyclic organic compound and a method of producing thereof are disclosed. The polycyclic organic compounds have a general formula (I) wherein A and B are acid groups; n is the number of phenyl rings in the range from 3 to 10; m is 0, 1, 2 or 3; l is 1, 2, or 3; p is 1, 2, 3, 4, 5 or 6; C is a counterion from a list comprising H + , NH + 4 , Na + , K + , Li + , Cs + , Ca 2+ , Mg 2+ , Sr 2+ , La 3+ , Zn 2+ , Zr 4+ , Ce 3+ , Y 3+ , Yb 3+ , Gd 3+ , and any combination thereof; k is the number of counterions necessary for compensation of the negative electric charge equal to (−p).

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Номер записи: 96
03-10-2019 дата публикации

NEW SOLID FORMS OF CANNABIDIOL AND USES THEREOF

Номер: US20190300466A1
Автор: Andres Mark, Andres Patricia, EMANUELE R. Martin, Shattock-Gordon Tanise, Williford Tabitha
Принадлежит: Artelo Biosciences, Inc.

Disclosed herein are cocrystals of cannabidiol and a coformer containing 5-6 membered rings comprised of carbon and nitrogen atoms, wherein the 5-6 membered rings can be unsaturated or saturated and the rings contain 1 to 2 nitrogen atoms. Cocrystals of cannabidiol and a coformer selected from L-proline, D-proline, tetramethylpyrazine, and 4,4′-dipyridyl are also disclosed herein 130.-. (canceled)31. A solid form comprising cannabidiol and the coformer tetramethylpyrazine.32. The solid form of having an x-ray diffraction pattern comprising one or more peaks at about 9.1 claim 31 , 14.6 claim 31 , 18.3 claim 31 , and 19.6 degrees 2θ±0.2.33. The solid form of having an x-ray powder diffraction pattern substantially similar to .34. The solid form of claim 31 , wherein the molar ratio of cannabidiol to tetramethylpyrazine is about 1:1.35. The solid form of claim 31 , which is crystalline.36. The solid form of claim 31 , which is a cocrystal.37. The solid form of having a DSC thermogram with a peak onset of approximately 89.9° C. or a peak maximum at about 92.8° C.38. The solid form of having a DSC thermogram which is substantially similar to the DSC thermogram of .39. A pharmaceutical composition comprising the solid form of .40. The pharmaceutical composition of claim 39 , further comprising a pharmaceutically acceptable excipient or carrier.41. A method for treating a disease or condition amenable to treatment with cannabidiol comprising administering a pharmaceutical composition according to to a subject in need of treatment.42. The method of claim 40 , wherein the disease or condition is selected from one or more of central nervous system disorders; cardiovascular disorders; neurovascular disorders claim 40 , neuromuscular disorders claim 40 , cancers claim 40 , autoimmune disorders claim 40 , inflammation; pain; sleep disorders claim 40 , posttraumatic stress disorder; posttraumatic stress syndrome; nausea claim 40 , and hypoxia-ischemia (acute stroke).43. The ...

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Номер записи: 97
10-11-2016 дата публикации

COMPOUNDS WITH NEURAL PROTECTIVE EFFECT, AND PREPARATION AND USE THEREOF

Номер: US20160326099A1
Автор: LANG Ming, Liu Wei, SUN Yewei, WANG Yuqiang, Yi Peng, Youdim Moussa B.H., YU Pei, ZHANG Gaoxiao, ZHANG Zaizun
Принадлежит: GUANGZHOU MAGPIE PHARMACEUTICAL CO., LTD

The invention generally relates to compounds of formula (I) with neural protective effect, and preparation and uses thereof. 15-. (canceled)7. (canceled)1011-. (canceled)151. A method of preparation of the compound of claim , comprising:using a compound with a cyclic aryl moiety, which has an aldehyde group and may or may not contain a nitrogen, as a starting material;in case when substitution of a nitronyl group is required, the cyclic aryl moiety is reacted directly with a tertiary butyl hydroxylamine to form the nitronyl group;in case when substitution of a propargyl amino group is required, the cyclic aryl moiety is reacted with a propargyl amine to generate Schiff's base which is then reduced to form the propargyl amino group;in case when substitution of a urethane group is required, the cyclic aryl moiety is reacted with an acyl chloride to cause a hydroxyl group on the cyclic aryl moiety is esterificated to form the urethane group.161. Use of the compound of claim in manufacture of a health supplement or medicament , which is used for prevention or treatment of diseases , the diseases are monoamine oxidase related diseases , cholinesterase related diseases , oxidative stress injury and free radicals related diseases , or neurodegenerative diseases.17. The use of claim 16 , wherein the monoamine oxidase related diseases are Parkinson's disease claim 16 , Alzheimer's disease claim 16 , hypertension claim 16 , diarrhea claim 16 , depression claim 16 , asthma claim 16 , or allergies.18. The use of claim 16 , wherein the cholinesterase related diseases are Alzheimer's disease claim 16 , Parkinson's disease claim 16 , Huntington's claim 16 , amyotrophic lateral sclerosis claim 16 , myasthenia gravis claim 16 , glaucoma claim 16 , thyroid function hyperfunction claim 16 , hypertension claim 16 , bronchial asthma claim 16 , type IV high lipoprotein hematic disease claim 16 , or kidney failure.19. The use of claim 16 , wherein the oxidative stress injury and free ...

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Номер записи: 98
10-11-2016 дата публикации

Anti-Angiogenic Compounds

Номер: US20160326122A1
Автор: "OSULLIVAN Jacintha", BAXTER Andrew Douglas, KENNEDY Breandan, REYNOLDS Alison
Принадлежит:

Compounds and compositions are described which are useful especially for treatment of angiogenesis-related diseases or disorders such as neovascularisation of the eye, age-related macular degeneration, diabetic retinopathy or cancer. 142-. (canceled)43. A pharmaceutical composition comprising a compound of the formula:{'br': None, 'A-X—Y—B'}wherein A is a six membered heteroaryl ring containing 2 nitrogen atoms which is optionally substituted with R1;R1 is H, C1-6 alkyl, CN, CONR2R3;R2 and R3 which may be the same or different and selected from H, C1-6 alkyl or R2 and R3 form a ring;the group X—Y is an alkyne or alkene, in the case wherein X—Y is an alkene the double bond may be cis or trans and optionally substituted with R1B is an aryl; or five or six membered heteroaryl ring containing 1 to 3 heteroatoms, both of which may optionally substituted with one or more R4;R4 is R1 or OR5;R5 is H, COR6 or R6; andR6 is C1-6 alkyland salts thereof.44. The composition as claimed in wherein R1 is H or C1-6 alkyl.45. The composition as claimed in wherein R1 is CH3.46. The composition as claimed in wherein X—Y is an alkyne.47. The composition as claimed in wherein X—Y is an alkene which is optionally substituted with R1.48. The composition as claimed in wherein R1 is CH3.49. The composition as claimed in wherein B is an aryl which may be optionally substituted with one or more R4.50. The composition as claimed in wherein R4 is OR5.51. The composition as claimed in wherein R5 is H.52. The composition as claimed in wherein B is phenol. The invention relates to anti-angiogenic compounds.In many human diseases there is an inappropriate growth of new blood vessels (angiogenesis). Angiogenesis is a physiological process involving the growth of new blood vessels from pre-existing vessels (Ferrara and Kerbel, 2005). Angiogenesis may be a therapeutic target for combating diseases characterised by poor vascularisation or abnormal vasculature (Ferrara and Kerbel, 2005). Targeted ...

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Номер записи: 99
15-11-2018 дата публикации

Volatile Dihydropyrazinly and Dihydropyrazine Metal Complexes

Номер: US20180327900A1
Автор: Ivanov Sergei Vladimirovich, Lei Xinjian, Norman John Anthony Thomas
Принадлежит: Versum Materials US, LLC

A composition comprising dihydropyrazinyl anions that can be coordinated as 6 electron ligands to a broad range of different metals to yield volatile metal complexes for ALD and CVD depositions are described herein. Also described herein are undeprotonated dihydropyrazines that can coordinate to metals as stabilizing neutral ligands. In one embodiment, the composition is used for the direct liquid injection delivery of the metal dihydropyrazinyl complex precursor to the chamber of an ALD or CVD chamber for the deposition of metal-containing thin films such as, for example, ruthenium or cobalt metal films. 3. A method for forming a metal oxide film on a substrate wherein the film comprises a thickness , the method comprising:a. introducing a metal dihydopyrazinyl complex comprising at least one selected from a Formula, 3D, 3E compound or combinations thereof;b. chemisorbing the metal dihydopyrazinyl complex onto the substrate;c. purging away the a metal dihydopyrazinyl complex using a purge gas;d. providing an oxygen source to the metal dihydopyrazinyl complex onto the heated substrate to react with the sorbed metal dihydopyrazinyl complex containing composition; ande. optionally purging away any unreacted oxygen source.4. The method of wherein steps a. through d. and optional step e. are repeated until the thickness of film is established.5. The method of wherein the method is an atomic layer deposition process.6. The method of wherein the metal dihydopyrazinyl complex comprises at least one selected from cobalt(pentamethylcyclopentadienyl)(2 claim 4 ,2-dihydro-3 claim 4 ,3-dimethyl-5 claim 4 ,6-diethylpyrazine) claim 4 , ruthenium (2 claim 4 ,2-dihydro-3 claim 4 ,3-dimethyl-5 claim 4 ,6-diethylpyrazine)(benzene) claim 4 , and combinations thereof.7. A method for forming a metal film on a substrate wherein the film comprises a thickness claim 4 , the method comprising:a. introducing a metal dihydopyrazinyl complex comprising at least one selected from a Formula 3D, ...

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