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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 1400. Отображено 196.
10-11-2009 дата публикации

ЗАМЕЩЕННЫЕ ФЕНОКСИУКСУСНЫЕ КИСЛОТЫ, ОБЛАДАЮЩИЕ МОДУЛИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ РЕЦЕПТОРОВ CRTh2

Номер: RU2372330C2
Принадлежит: АстраЗенека АБ (SE)

Изобретение относится к новым замещенным феноксиуксусным кислотам (I), в которых: Х представляет собой галоген, циано, нитро или С1-4алкил, который замещен одним или более чем одним атомом галогена; Y выбран из водорода, галогена или C1-С6алкила, Z представляет собой фенил, нафтил или кольцо А, где А представляет собой шестичленное гетероциклическое ароматическое кольцо, содержащее один или два атома азота, или может представлять собой 6,6- или 6,5-конденсированный бицикл, содержащий один атом О, N или S, или может представлять собой 6,5-конденсированный бицикл, содержащий два атома О, причем фенил, нафтил или кольца А все, возможно, замещены одним или более чем одним заместителем, независимо выбранным из галогена, CN, ОН, нитро, COR9, CO2R6, SO2R9, OR9, SR9, SO2NR10R11, CONR10R11, NR10R11, NHSO2R9, NR9SO2R9, NR6CO2R6, NR9COR9, ! NR6CONR4R5, NR6SO2NR4R5, фенила или C1-6алкила, причем последняя группа, возможно, замещена одним или более чем одним заместителем, независимо выбранным из галогена ...

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18-05-2021 дата публикации

Номер: RU2019127896A3
Автор:
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20-09-2011 дата публикации

ПРОИЗВОДНЫЕ АЗАБИФЕНИЛАМИНОБЕНЗОЙНОЙ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ DHODH

Номер: RU2010108261A
Принадлежит:

... 1. Соединение формулы (I) для применения для лечения или профилактики патологического состояния или заболевания, чувствительного к облегчению путем ингибирования дегидрооротатдегидрогеназы ! ! где ! R1 выбран из группы, состоящей из атомов водорода, атомов галогена, С1-4алкила, C3-4циклоалкила, -CF3 и -OCF3, ! R2 выбран из группы, состоящей из атомов водорода, атомов галогена и C1-4алкильной группы, ! R3 выбран из группы, состоящей из -COOR5, -CONHR5, тетразолила, групп -SO2NHR5 и -CONHSO2R5, где R5 выбран из группы, состоящей из атома водорода и линейных или разветвленных C1-4алкильных групп, ! R4 выбран из группы, состоящей из атома водорода и C1-4алкильной группы; ! R9 выбран из группы, состоящей из атома водорода и фенильной группы, ! G1 представляет собой группу, выбранную из N и CR6, где R6 выбран из группы, состоящей из атомов водорода, атомов галогена, C1-4алкила, C3-4циклоалкила, C1-4алкокси, -CF3, -OCF3, моноциклических N-содержащих С5-7гетероарильных, моноциклических N-содержащих ...

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10-07-1996 дата публикации

НОВЫЕ 2-ЦИАНО-3-ГИДРОКСИПРОПЕНАМИДЫ, МЕТОД ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Номер: RU94000064A
Принадлежит:

Изобретение относится к новым 2-циано-3-гидроксипропенамидам общей формулы, приведенной в описании, обладающим противовоспалительной активностью.

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11-11-2020 дата публикации

Compounds

Номер: GB0002583882A
Принадлежит:

Compounds of general formula (I): wherein R1, R2, R3, R4, R5a, R5b X1, X2, Z and Y are as defined herein are positive modulators of the calcium-activated chloride channel (CaCC), TMEM16A. The compounds are useful for treating diseases and conditions affected by modulation of TMEM16A, particularly respiratory diseases and conditions.

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31-08-2009 дата публикации

Tricyclic compounds and their use as glucocorticoid receptor modulators

Номер: AP0200904942D0
Принадлежит:

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31-07-2013 дата публикации

Heterocyclic compounds

Номер: AP0201508591D0
Принадлежит:

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31-08-2009 дата публикации

Tricyclic compounds and their use as glucocorticoid receptor modulators

Номер: AP0200904942A0
Принадлежит:

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31-07-2013 дата публикации

Heterocyclic compounds

Номер: AP0201508591A0
Принадлежит:

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31-07-2013 дата публикации

Heterocyclic compounds

Номер: AP2015008591A0
Принадлежит:

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31-08-2009 дата публикации

Tricyclic compounds and their use as glucocorticoid receptor modulators

Номер: AP2009004942A0
Принадлежит:

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31-03-1981 дата публикации

Method of preparation of pharmaceutical compounds.

Номер: OA0000005440A
Автор:
Принадлежит:

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15-05-1986 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN PYRIDYLAMINOETHEN-DERIVATEN

Номер: ATA80584A
Автор:
Принадлежит:

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30-06-2011 дата публикации

Phenazopyridine compounds

Номер: AU2009327322A1
Принадлежит:

The present invention is directed to substituted phenazopyridines represented by Formula I. The present invention also relates to the discovery that compounds of Formula I have increased bioavailability as compared to unconjugated phenazopyridine.

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30-07-2015 дата публикации

Heterocyclic compound

Номер: AU2013358112A1
Принадлежит:

The purpose of the invention is to provide a compound or salt thereof that is useful as an agent for the prevention or treatment of epilepsy, neurodegenerative disease, and the like. The invention pertains to compounds represented by formula (I) (in the formula, each symbol is as defined in the specification) or salts thereof.

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10-07-2014 дата публикации

Tricyclic amino containing compounds for treatment or prevention of symptoms associated with endocrine dysfunction

Номер: AU2012335981A1
Принадлежит:

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.

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03-12-2020 дата публикации

Tricyclic amino containing compounds for treatment or prevention of symptoms associated with endocrine dysfunction

Номер: AU2012335981C1
Принадлежит: Davies Collison Cave Pty Ltd

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.

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17-03-1988 дата публикации

HERBICIDAL AMINOPYRIMIDINE DERIVATIVES

Номер: AU0000570413B2
Принадлежит:

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20-01-2000 дата публикации

LIGANDS FOR METALS AND METAL-CATALYZED PROCESSES

Номер: CA0002336691A1
Принадлежит:

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon- heteroatom and carbon-carbon bond-forming reactions. The subject processes provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

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22-08-2019 дата публикации

USE OF 5-FLUORO-4-(4-FLUORO-2-METHOXYPHENYL)-N-{4-[(S-METHYLSULFONIMIDOYL)METHYL]PYRIDIN-2-YL}PYRIDIN-2-AMINE FOR TREATING DIFFUSE LARGE B-CELL LYMPHOMA

Номер: CA0003090843A1
Автор: SCHOLZ ARNE, SCHOLZ, ARNE
Принадлежит: SMART & BIGGAR IP AGENCY CO.

The present invention relates to the use of 5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{4-[(S- methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine (compound A), more particularly (+)5- Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2- amine (compound A´), for treating diffuse large B-cell lymphoma (DLBCL), especially in germinal- centre B-cell type of diffuse large B-cell lymphoma and especially in diffuse large B-cell lymphoma which cells have an amplification or translocation of the MYC gene and/or BCL2 gene and/or an overexpression of MYC and/or BCL2.

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01-08-2019 дата публикации

COMPOUNDS

Номер: CA0003086747A1
Принадлежит: GOWLING WLG (CANADA) LLP

Compounds of general formula (I): wherein R1, R2, R3, R4, R5a, R5b X1, X2, Z and Y are as defined herein are positive modulators of the calcium-activated chloride channel (CaCC), TMEM16A. The compounds are useful for treating diseases and conditions affected by modulation of TMEM16A, particularly respiratory diseases and conditions.

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19-06-2008 дата публикации

ION CHANNEL MODULATORS

Номер: CA0002672223A1
Принадлежит:

The present teachings provide compounds of Formula (I): and pharmaceutica lly acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes fo r producing said compounds and their pharmaceutically acceptable salts, hydr ates and esters, and methods of treating a pathological condition or disorde r, or alleviating a symptom thereof, using said compounds including their ph armaceutically acceptable salts, hydrates and esters. The compounds can be u seful in modulating ion channel activity including treating a variety of con ditions associated with the abnormal modulation of one or more voltage-gated calcium channels.

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16-04-2009 дата публикации

AMIDES USEFUL AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS

Номер: CA0002701766A1
Принадлежит:

The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

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19-02-2009 дата публикации

AZABIPHENYLAMINOBENZOIC ACID DERIVATIVES AS DHODH INHIBITORS

Номер: CA0002695475A1
Принадлежит:

New azabiphenylaminobenzoic acid derivatives having the chemcial structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).

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21-06-2016 дата публикации

INHIBITORS OF FOCAL ADHESION KINASE

Номер: CA0002681015C

The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.

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18-05-2012 дата публикации

SALT(S) OF 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO[2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE AND PROCESSES OF MAKING THEREOF

Номер: CA0002815839A1
Принадлежит:

This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.

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02-08-2012 дата публикации

ARYLALKYL ESTERS OF 4-AMINO-6-(SUBSTITUTED PHENYL)PICOLINATES AND 6-AMINO-2-(SUBSTITUTED PHENYL)-4-PYRIMIDINECARBOXYLATES AND THEIR USE AS HERBICIDES

Номер: CA0002825878A1
Принадлежит:

Arylalkyl esters of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are herbicides for control of weeds especially those species common to rice and wheat cropping systems and in pasture management programs.

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01-05-2014 дата публикации

HETEROARYL INHIBITORS OF PDE4

Номер: CA0002886263A1
Принадлежит: MBM INTELLECTUAL PROPERTY LAW LLP

The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.

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18-05-2021 дата публикации

5-FLUORO-N-(PYRIDIN-2-YL)PYRIDIN-2-AMINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP

Номер: CA2891358C

... 81787492 Abstract The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I): R3 5 R ¨N 0 N N R1 N R2 (1) and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of .. cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). CA 2891358 2020-03-19 ...

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15-05-1986 дата публикации

CHLORACETAMIDE.

Номер: CH0000655717A5
Принадлежит: SANDOZ AG

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31-07-2018 дата публикации

ANALYSIS OF MODULATORS

Номер: EA0201890080A1
Автор:
Принадлежит:

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31-07-2018 дата публикации

EPITOPE ANTIBODIES

Номер: EA0201890082A1
Автор:
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30-04-2013 дата публикации

PROTEIN KINASE INHIBITORS

Номер: EA0201201274A1
Автор:
Принадлежит:

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25-07-2011 дата публикации

ТРЕХЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ ГЛЮКОКОРТИКОИДНОГО РЕЦЕПТОРА

Номер: UA0000095332C2

Заявленное изобретение касается соединения формулы I: (I) или ее соли, которые являются модуляторами глюкокортикоидного рецептора. Соединения и соли изобретения являются полезными в лечении состояний, опосредованных активностью глюкокортикоидного рецептора.

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25-05-2011 дата публикации

ТРИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ КАК МОДУЛЯТОРОВ ГЛЮКОКОРТИКОИДНОГО РЕЦЕПТОРА

Номер: UA0000094639C2

Изобретение касается соединений формулы I или их солей, которые являются модуляторами рецептора глюкокортикоида. Соединения и соли изобретения могут быть использованы в лечении состояний, опосредованных активностью рецептора глюкокортикоида.

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30-12-2009 дата публикации

ТРИЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ И ЕГО ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ

Номер: EA200970642A1
Принадлежит:

Настоящее изобретение предоставляет соединение, представленное формулой где R1 представляет собой углеводородную группу, необязательно имеющую заместитель(и), аминогруппу, необязательно имеющую заместитель(и), гидроксигруппу, необязательно имеющую заместитель, или гетероциклическую группу, необязательно имеющую заместитель(и), R2 представляет собой атом водорода или углеводородную группу, необязательно имеющую заместитель(и), R3 представляет собой атом водорода, атом галогена, углеводородную группу, необязательно имеющую заместитель(и), аминогруппу, необязательно имеющую заместитель(и), гидроксигруппу, необязательно имеющую заместитель, или меркаптогруппу, необязательно имеющую заместитель, каждый из Xa, Xb, Xc и Xd представляет собой атом углерода или атом азота, при условии, что любой один или любые два из Ха, Xb, Хс и Xd, представляет(ют) собой атом(ы) азота, m равно от 0 до 2 и каждое из колец А-С представляет собой кольцо, необязательно имеющее заместитель(и), или его соль, которое ...

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23-05-2012 дата публикации

Tricyclic compounds and their use as glucocorticoid receptor modulators

Номер: CN0101616925B
Принадлежит:

The present invention is directed to compounds of Formula (I), or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.

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14-01-1942 дата публикации

Method of preparation of derived from sulphamides

Номер: FR0000868714A
Автор:
Принадлежит:

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20-07-2016 дата публикации

METHOD FOR SYNTHESIZING AZOMETHIN YLIDE DERIVATIVES HAVING EXCELLENT STABILITY AND METHOD FOR SYNTHESIZING 1,4-DIAZEPINE DERIVATIVES VIA MULTICOMPONENT [5+2] CYCLOADDITION REACTION

Номер: KR1020160086725A
Принадлежит:

The present invention relates to a method for synthesizing an azomethine ylide derivative represented by Formula 3, wherein the method comprises a step for reacting: a substituted pyridine, represented by Formula 1; and substituted 1-sulfonyl-1,2,3-triazole, represented by Formula 2, in the presence of a metal catalyst. Also, the present invention relates to a method for synthesizing a 1,4-diazepine derivative, represented by Formula 5, wherein the method comprises a step for reacting: a substituted pyridine, represented by Formula 1; substituted 1-sulfonyl-1,2,3-triazole, represented by Formula 2; and an alkyne, represented by Formula 4, in the presence of a metal catalyst and via a multicomponent [5+2] cycloaddition reaction. COPYRIGHT KIPO 2016 ...

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01-08-2013 дата публикации

Stabilized silver catalysts and methods

Номер: TW0201331411A
Принадлежит:

Zero-valent silver compositions include 4-dimethylaminopyridine as stabilizers. The zero-valent silver and the 4-dimethylaminopyridine form stabilized nano-particles in solution. The zero-valent silver compositions may be used as catalysts in the metallization of non-conductive substrates.

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03-10-2016 дата публикации

PEST CONTROL AGENT

Номер: TN2015000246A1
Принадлежит:

Objects of the present invention are to provide a compound which is highly active against pests, to provide a pest control agent comprising the compound, and to provide a method for controlling a pest by applying the compound. The present invention provides a 4-(arylethynyl)pyridine or a sait thereof, a pest control agent which comprises the 4-(arylethynyl)pyridine or sait thereof as an active ingredient, and a method for controlling a pest by applying the 4-(arylethynyl)pyridine or sait thereof in an effective amount.

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06-02-2014 дата публикации

NOVEL AZO COMPOUND, USE THEREOF AND METHOD FOR PREPARING SAME

Номер: WO2014021680A1
Принадлежит:

The present invention provides a novel azo compound having a quenching ability for the material that exhibits a luminescent phenomenon at an excited energy level, a quencher comprising the novel azo compound, a use of the quencher and a method for preparing the azo compound. The quencher according to the present invention may exhibit excellent characteristics in a wavelength absorption region.

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12-05-1987 дата публикации

2-acetyl- and 2-propionylpyridine selenosemicarbazones

Номер: US0004665173A1
Принадлежит:

This invention relates to novel 2-acetyl- and 2-propionylpyridine selenosemicarbazones. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures used to prepare the selenosemicarbazones.

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11-06-2013 дата публикации

Processes for producing phenyl-6-(1-(phenyl)ureido)nicotinamides)

Номер: US0008461345B2

The present invention relates to processes for the preparation of compounds useful as inhibitors of p38 kinase. The processes of the present invention are amenable for large scale preparation and produce stable phenyl-6-(1-(phenyl)ureido)nicotinamides in high purity and yields.

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26-06-2014 дата публикации

New Inhibitors of Cyclophilins and Uses Thereof

Номер: US20140179687A1

The present invention relates to a compound of formula (I): 112-. (canceled)15. A pharmaceutical composition comprising the compound according to claim 13 , in association with a pharmaceutically acceptable vehicle.16. The pharmaceutical composition of claim 13 , wherein said compound is the compound according to . The present invention concerns new inhibitors of cyclophilins, as well as uses thereof.Cyclophilins (or Cyp) are members of the immunophilin class of proteins, comprising in particular cyclophilin A (CypA), cyclophilin B (CypB), and cyclophilin D (CypD). These ubiquitous cellular proteins possess cis-trans prolyl isomerase (PPlase) activities (Fischer, G., H. Bang, and C. Mech. 1984. Determination of enzymatic catalysis for the cis-trans-isomerization of peptide binding in proline-containing peptides. Biomed. Biochim. Acta 43:1101-1111) and are assumed to be involved in protein folding and to function as chaperones in intracellular transport (Snyder, S. H., and D. M. Sabatini. 1995. Immunophilins and the nervous system. Nat. Med. 1:32-37). Cyclophilins are also known to be the intracellular receptor molecules for cyclosporines (Handschumacher, R. E., M. W. Harding, J. Rice, R. J. Drugge, and D. W. Speicher. 1984. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science 226:544-546), a class of cyclic undecapeptides produced by (Dreyfuss, M., E. Harri, H. Hoffmann, H. Kobel, W. Pache, and H. Tscherter. 1976. Cyclosporin A and C. New metabolites from . Eur. J. Appl. Microbiol, 3:125-133). Binding of cyclosporines to cyclophilins leads to the blockade of the isomerase activity.These cyclophilins are known as drug targets for a number of diseases including HIV infection (J. Luban et al., Cell, 1993, 73, 1067-1078; Daelemans et al., Antiviral Res. 2009 Oct. 24), malaria (Bell et al., 2005) and ischemic (Yang Y, Moir E, Kontopidis G, Taylor P, Wear M A, Malone K, Dunsmore C J, Page A P, Turner N J, Walkinshaw M D. Biochem Biophys Res Commun. ...

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29-07-2010 дата публикации

SYNTHESIS OF THIOHYDANTOINS

Номер: US20100190991A1
Принадлежит:

A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.

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15-10-2014 дата публикации

New crystalline forms of the sodium salt of (4- {4- [5- ( 6 - trifluoromethyl - pyridin- 3 - ylamino ) - pyridin- 2 -yl]-phenyl} - cyclohexyl) -acetic acid

Номер: EP2781516A3
Принадлежит:

The present invention relates to novel crystalline forms of (4-{4-[5-(6-Trifluoromethylpyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid, sodium and their use in the treatment or prevention of a condition or a disorder associated with DGAT1 activity in animals, particularly humans. It also relates processes for making such novel crystalline forms.

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23-04-2014 дата публикации

INHIBITORS OF FOCAL ADHESION KINASE

Номер: EP2134689B1
Принадлежит: The Scripps Research Institute

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27-08-1986 дата публикации

Preparation of 4-substituted pyridines and quaternary pyridine salts useful therefor

Номер: EP0000192003A1
Автор: Nummy, Laurence J.
Принадлежит:

A process for preparing a 4-substitued pyridine product from a starting pyridine substituted in the 4-position by a leaving group susceptible to nucleophilic displacement when the starting pyridine is in quaternized form, comprises, quaternizing the starting pyridine under effective acidic conditions with acrylamide, N-monoalkylacrylamide or N-dialkylacrylamide, subjecting the resultant, corresponding quaternized starting pyridine, to a nucleophilic displacement reaction with a reagent which reacts with it to produce the corresponding quaternary salt of the 4-substituted pyridine product, and dequaternizing the latter under effective basic conditions to liberate the 4-substituted pyridine product.

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27-10-2015 дата публикации

СЛОЖНЫЕ АРИЛАЛКИЛОВЫЕ ЭФИРЫ 4-АМИНО-6-(ЗАМЕЩЕННЫЙ ФЕНИЛ)ПИКОЛИНАТОВ И 6-АМИНО-2-(ЗАМЕЩЕННЫЙ ФЕНИЛ)-4-ПИРИМИДИНКАРБОКСИЛАТОВ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ГЕРБИЦИДОВ

Номер: RU2566760C2

Изобретение относится к новым сложным арилалкиловым эфирам 4-аминопиколиновых кислот формулы IB, которые обладают гербицидным действием и могут быть использованы для борьбы с нежелательной растительностью (сорняками). Соединения обладают избирательным действием и особенно применимы для борьбы на послевсходовой стадии с теми видами, которые, как правило, встречаются в системах для выращивания риса, пшеницы или кормовых растений. В формуле IB:X представляет собой Н или F; Y представляет собой фенил, замещенный 1-4 заместителями, независимо выбранными из галогена, С-Сциклоалкила, C-Cалкокси, C-Cгалогеналкила, C-Cгалогеналкокси; Z представляет собой галоген; Rи Rпредставляют собой Н; Rпредставляет собой арилалкил, выбранный из нафтил-(С)алкила или фенил-(С)алкила, который может быть незамещенным или замещенным 1-2 заместителями, независимо выбранными из галогена, нитро, циано, С-Салкила, С-Салкокси, галогенированного С-Салкила, галогенированной С-Салкокси, С-Салкилтио, С(О)OC-Салкила, или где ...

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17-01-2018 дата публикации

СРЕДСТВО ДЛЯ БОРЬБЫ С ВРЕДИТЕЛЯМИ

Номер: RU2641295C2

FIELD: chemistry. SUBSTANCE: invention relates to a compound of the general formula (I) , where R 1 represents a halogen atom, an amino group, a hydroxyl group, a mercapto group, a cyano group, a nitro group, a (C 1 -C 6 ) alkyl group, a (C 2 -C 6 ) alkenyl group, a (C 2 -C 6 ) alkynyl group, a (C 3 -C 6 ) cycloalkyl group, a (C 1 -C 6 ) a halogen alkyl group, a (C 1 -C 6 ) alkoxy group, a (C 2 -C 6 ) alkenyloxy group, a (C 2 -C 6 ) alkynyloxy group, a (C 3 -C 6 ) cycloalkoxy group, a (C 1 -C 6 ) halogen alkoxy group, a (C 1 -C 6 ) alkylthio group, a (C 2 -C 6 ) alkenylthio group, a (C 2 -C 6 ) alkynylthio group, a (C 3 -C 6 ) cycloalkylthio group, a (C 1 -C 6 ) halogen alkylthio group, a (C 1 -C 6 ) alkylamino group, a (C 2 -C 6 ) alkenylamino group, a (C 2 -C 6 ) alkynylamino group, a di (C 1 -C 6 ) alkylamino group, a di (C 2 -C 6 ) alkenylamino group, a di (C 2 -C 6 ) alkynylamino group, a (C 1 -C 6 ) alkylsulfinyl group, a (C 2 -C 6 ) alkenylsulfinyl group, a (C 2 -C 6 ) alkynylsulfinyl group, a (C 3 -C 6 ) cycloalkylsulfinyl group, a (C 1 -C 6 ) halogen alkylsulfinyl group, a (C 1 -C 6 ) alkylsulfonyl group, a (C 2 -C 6 ) alkenylsulfonyl group, a (C 2 -C 6 ) alkynylsulfonyl group, a carboxyl group, a (C 1 -C 6 ) alkylcarbonyl group, a (C 1 -C 6 ) alkoxycarbonyl group, a (C 1 -C 6 ) alkylaminocarbonyl group, a di (C 1 -C 6 ) alkylaminocarbonyl group, a (C 1 -C 6 ) alkylcarbonyloxy group, a (C 1 -C 6 ) alkylcarbonylamino group, or a (C 1 -C 6 ) alkylcarbonyl group, a (C 1 -C 6 ) alkylamino group; R 2 is a halogen atom, a hydroxyl group, a mercapto group, a nitro group, a (C 1 -C 6 ) alkyl group, a (C 2 -C 6 ) alkenyl group, a (C 2 -C 6 ) alkynyl group, a (C 1 - C 6 ) halogen alkyl group, a (C 1 -C 6 ) alkoxy group, a (C 2 -C 6 ) alkenyloxy group, a (C 2 -C 6 ) alkynyloxy group, a (C 1 -C 6 ) alkylthio group, a (C 2 -C 6 ) alkenylthio group, a (C 2 -C 6 ) alkynylthio group, a (C 1 -C 6 ) alkylamino group, a (C 2 -C 6 ) alkenylamino group, a (C 2 -C 6 ) ...

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02-11-2020 дата публикации

Номер: RU2019113229A3
Автор:
Принадлежит:

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10-02-1998 дата публикации

СПОСОБ КАТАЛИТИЧЕСКОГО ОКИСЛЕНИЯ ТИОЛА ИЛИ ЕГО СОЛИ ИЛИ ДИТИОКАРБАМИНОВОЙ КИСЛОТЫ ИЛИ ЕЕ СОЛЕЙ

Номер: RU2104275C1
Принадлежит: Монсанто Компани (US)

Каталитическое окисление тиолов или тиоловых солей, дитиокарбаминовых кислот или их солей с использованием кислорода, необязательно в присутствии первичного или вторичного амина проводят с использованием угольного катализатора, свободного от металлического порфиразина или производного порфиразина. 1 с. и 11 з.п. ф-лы.

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20-11-2014 дата публикации

НОВЫЕ КРИСТАЛЛИЧЕСКИЕ ФОРМЫ НАТРИЕВОЙ СОЛИ(4-{4-[5-(6-ТРИФТОРМЕТИЛ-ПИРИДИН-3-ИЛАМИНО) ПИРИДИН-2-ИЛ] ФЕНИЛ} ЦИКЛОГЕКСИЛ) УКСУСНОЙ КИСЛОТЫ

Номер: RU2013120549A
Принадлежит:

... 1. Кристаллическая форма натриевой соли (4-{4-[5-(6-трифторметил-пиридин-3-иламино)пиридин-2-ил]фенил}циклогексил)уксусной кислоты формулы (II)в форме Модификации B, C, D, F, I, L, N или O.2. Кристаллическая форма по п. 1 в форме Модификации C, N или O.3. Кристаллическая форма по п. 2 в форме Модификации C.4. Кристаллическая форма по п.1, которая остается сухой при 25°C и при относительной влажности в пределах от 0% до 70%.5. Кристаллическая форма по п.4, которая остается сухой при 25°C и при относительной влажности в пределах от 0% до 80%.6. Кристаллическая форма по п.1, включающая по меньшей мере 80, 85, 90, 95% или 99% мас. указанной Модификации.7. Кристаллическая форма по п.6, включающая по меньшей мере 95% или 99% мас. указанной Модификации.8. Кристаллическая форма по любому из п.п. 3-7 в форме Модификации C, характеризующаяся рентгеновской порошковой дифрактограммой с пиками при 5,9 и 17,0 градусах два тета (±0,1 градус) (CuKα λ=1,5418 Å) или рентгеновской порошковой дифрактограммой ...

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10-03-2015 дата публикации

СЛОЖНЫЕ АРИЛАЛКИЛОВЫЕ ЭФИРЫ 4-АМИНО-6-(ЗАМЕЩЕННЫЙ ФЕНИЛ)ПИКОЛИНАТОВ И 6-АМИНО-2-(ЗАМЕЩЕННЫЙ ФЕНИЛ)-4-ПИРИМИДИНКАРБОКСИЛАТОВ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ГЕРБИЦИДОВ

Номер: RU2013139370A
Принадлежит:

... 1. Соединение формулы IA:где Y представляет собой C-Cалкил, C-Cциклоалкил или фенил, замещенный 1-4 заместителями, независимо выбранными из галогена, C-Cалкила, C-Cциклоалкила, C-Cалкокси, C-Cгалогеналкила, C-Cгалогеналкокси, циано, нитро, NRR, или где два смежных заместителя, взятые вместе, представляют собой -O(CH)O- или -O(CH)-, где n=1 или 2;Z представляет собой галоген, C-Cалкокси или C-Cалкенил;Rи Rнезависимо представляют собой H, C-Cалкил, C-Cалкенил, C-Cалкинил, гидрокси, C-Cалкокси, амино или C-Cацил;Rпредставляет собой незамещенный или замещенный C-Cарилалкил.2. Соединение по п.1, где Y представляет собой замещенный фенил.3. Соединение по п.1, где Z представляет собой Cl, -CH=CHили OCH.4. Соединение по п.1, где Rи Rпредставляют собой H.5. Соединение по п.1, где Rпредставляет собой бензил.6. Соединение по п.1, где Rпредставляет собой незамещенный или орто-, мета- или пара-монозамещенный бензил.7. Соединение формулы IB:где X представляет собой H или F;Y представляет собой галоген ...

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27-10-2013 дата публикации

КОНЪЮГАТЫ И ИНГИБИТОРЫ ПРОТЕИНКИНАЗЫ

Номер: RU2012114902A
Принадлежит:

... 1. Конъюгат протеинкиназы, который имеет формулуX-M-S-CH-Prot,где Prot представляет собой протеинкиназу или ее часть, которая содержит цистеиновый остаток, выбранный из группы, состоящей из CYS1, CYS5, CYS6, CYS7, CYS8, CYS9, CYS 10, CYS 11, CYS 12 и CYS 13;S-CHпредставляет собой атом серы и метиленовую группу из боковой цепи указанного цистеинового остатка;М представляет собой фрагмент модификатора, который образован путем ковалентного связывания активной группы с боковой цепью указанного цистеинового остатка; иХ представляет собой химический фрагмент, который связывается в АТФ-связывающем участке протеинкиназы или около него.2. Конъюгат по п.1, в котором активная группа представляет собой -L-Y, гдеL представляет собой ковалентную связь или двухвалентную Cнасыщенную или ненасыщенную, прямую или разветвленную углеводородную цепь, где одна, две или три метиленовые единицы L необязательно и независимо заменены на циклопропилен, -NR-, -N(R)C(O)-, -C(O)N(R)-, -N(R)SO-, -SON(R)-, -O-, -C(O)- ...

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18-01-2017 дата публикации

СПОСОБ ПОЛУЧЕНИЯ 4-АМИНО-5-ФТОР-3-ХЛОР-6-(ЗАМЕЩЕННЫХ)ПИКОЛИНАТОВ

Номер: RU2015127993A

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2015 127 993 A (51) МПК C07D 213/79 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2015127993, 12.12.2013 (71) Заявитель(и): ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи (US) Приоритет(ы): (30) Конвенционный приоритет: 13.12.2012 US 61/736,835 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 13.07.2015 R U (43) Дата публикации заявки: 18.01.2017 Бюл. № 02 (72) Автор(ы): РЕНГА Джеймс М. (US), УАЙТЕКЕР Грегори Т. (US), ДЖОНСОН Питер Ли (US), ГЭЛЛИФОРД Кристофер (US) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2014/093588 (19.06.2014) A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" R U (57) Формула изобретения 1. Способ получения 4-амино-5-фтор-3-хлор-6-(замещенных)пиколинатов формулы I A 2 0 1 5 1 2 7 9 9 3 (54) СПОСОБ ПОЛУЧЕНИЯ 4-АМИНО-5-ФТОР-3-ХЛОР-6-(ЗАМЕЩЕННЫХ)ПИКОЛИНАТОВ 2 0 1 5 1 2 7 9 9 3 US 2013/074600 (12.12.2013) в которой R1 представляет собой С1-С4алкил, циклопропил, С2-С4алкенил или фенил, замещенный 1-4 заместителями, независимо выбранными из галогена, С1-С4алкила, С1-С4галогеналкила, С1-С4алкокси или С1-С4галогеналкокси, и R2 представляет собой С1-С12алкил или незамещенный или замещенный С7-С11арилалкил, включающий следующие стадии: а) контактирование трифторуксусной кислоты с п-метоксианилином в присутствии триарилфосфина и триалкиламинового основания в растворителе четыреххлористый Стр.: 1 углерод для образования ацетимидоилхлорида формулы А b) контактирование ацетимидоилхлорида формулы А с 3,3-диалкоксипроп-1-ином (формула В) A 2 0 1 5 1 2 7 9 9 3 R U в которой R1 и R3 являются такими, как определено ранее; d) хлорирование 4-(4-метоксифенил)амино-5-фтор-6-(замещенный)пиридин-2диалкилацеталя формулы Е посредством 1,3-дихлор-5,5-диметилимидазолидин-2,4диона (формулы F) Стр.: 2 A в которой R1 является таким, как определено ранее, в присутствии неорганического основания щелочного металла в ...

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27-05-2011 дата публикации

ПРОИЗВОДНЫЕ ТРИАЗОЛОПИРИДИНКАРБОКСАМИДОВ, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ В ТЕРАПИИ

Номер: RU2009142430A

1. Соединение, соответствующее формуле (I) ! , ! где ! X означает атом водорода, атом галогена, (C1-C6)алкил, (C1-C6)алкокси, галоген(C1-C6)алкил, S(O)mR", гидрокси- или цианогруппу; ! A отсутствует или означает связь, атом кислорода, атом серы, NR, C(O)NR', SO2NR', (C1-C2)алкилен или (C2)алкенил; ! R1 и R2 независимо друг от друга означают одну или несколько групп, выбранных из атома водорода, (C1-C6)алкила, (C1-C6)алкокси, (C3-C7)циклоалкила, (C3-C7)циклоалкил(C1-C6)алкила, (C3-C7)циклоалкил(C1-C6)алкокси, атома галогена, цианогруппы, C(O)R', C(O)OR', C(O)NR10R20, NO2, NR10R20, NR10C(O)-R20, (C1-C6)алкила и (C1-C6)алкокси, при необходимости имеющих в качестве заместителей один или несколько атомов или групп, выбранных независимо друг от друга из атомов галогенов, гидроксильных групп, аминогрупп и NR10R20; ! R означает группу, выбранную из атома водорода, (C1-C6)алкила, (C3-C7)циклоалкила, (C3-C7)циклоалкил(C1-C6)алкила, C(O)R', SO2R", CO2R", C(O)NR10R20; ! R' означает группу, выбранную из атома водорода, (C1-C6)алкила, (C3-C7)циклоалкила, (C3-C7)циклоалкил(C1-C6)алкила; ! R" означает группу, выбранную из (C1-C6)алкила, (C3-C7)циклоалкила, (C3-C7)циклоалкил(C1-C6)алкила; ! R10 и R20 независимо друг от друга означают одну или несколько групп, выбранных из атома водорода, (C1-C6)алкила, (C3-C7)циклоалкила, (C3-C7)циклоалкил(C1-C6)алкила, или R10 и R20 могут образовывать насыщенный или частично ненасыщенный цикл, содержащий от 5 до 7 атомов углерода и содержащий при необходимости гетероатом, выбранный из O, N или S(O)m; ! m означает 0, 1 или 2; ! в виде основания или кислотно-аддитивной соли, а также в виде гидрата или сольвата. ! 2. Соединение формулы (I) по п.1, отличающееся тем, что ! X означает атом водорода или галогена; ! A отсутствует или означает связь, атом кислорода, атом серы, NR, C(O)NR', SO2NR', (C1-C2) РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2009 142 430 (13) A (51) МПК C07D 471/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ...

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20-12-2014 дата публикации

СОЛЬ (СОЛИ) ДИМЕТИЛАМИДА 7-ЦИКЛОПЕНТИЛ-2-(5-ПИПЕРАЗИН-1-ИЛ-ПИРИДИН-2-ИЛАМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-6-КАРБОНОВОЙ КИСЛОТЫ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ

Номер: RU2013126112A
Принадлежит:

... 1. Сукцинатная соль диметиламида 7-циклопентил-2-(5-пиперазин-1-ил-пиридин-2-иламино)-7H-пирроло[2,3-d]пиримидин-6-карбоновой кислоты.2. Соль по п. 1, представленная формулой (II):3. Соль по п. 1 в негидратной форме.4. Соль по п. 1 в гидратной форме.5. Фармацевтическая композиция, содержащая:(a) терапевтически эффективное количество соли по любому из пп. 1-4; и(b) по меньшей мере один фармацевтически приемлемый носитель, разбавитель, растворитель или эксципиент.6. Способ лечения заболевания, которое ослабляется ингибированием активности циклинзависимых киназ, включающий стадию введения пациенту, нуждающемуся в таком лечении, терапевтически эффективного количества соли по любому из пп. 1-4.7. Способ получения соединения формулы (I), включающий:(1) взаимодействиеис получениеми(2) преобразованиев.8. Способ по п. 7, в котором стадию (1) осуществляют в присутствии Pd(OAc), BINAP и CsCO.9. Способ по п. 7, в котором стадию (2) осуществляют в присутствии водного раствора HCl и толуола.10. Способ ...

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15-08-1994 дата публикации

FUNGICIDES PYRIDYL CYCLOPROPANCARBOXAMIDE ONES.

Номер: AT0000109469T
Принадлежит:

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10-11-1978 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW CYANO PYRIDYLGUANIDINEN AS WELL AS THEIR SALTS WITH NON--TOXIC, PHARMACEUTICAL ACCEPTABLE ACIDS

Номер: AT0000346357B
Автор:
Принадлежит:

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12-07-2012 дата публикации

Trpv1 antagonists including amide substituent and uses thereof

Номер: US20120177570A1
Автор: Laykea Tafesse
Принадлежит: Purdue Pharma LP

The invention relates to compounds of formula IA″ and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA″ or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA″ or a pharmaceutically acceptable derivative thereof.

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26-07-2012 дата публикации

Process for the preparation of 4-amino-3-chloro-5-fluoro-6-(substituted) picolinates

Номер: US20120190858A1
Принадлежит: DOW AGROSCIENCES LLC

4-Amino-3-chloro-5-fluoro-6-(substituted)picolinates are conveniently prepared from 3,4,5,6-tetrachloropicolinonitrile by a series of steps involving fluorine exchange, amination, reaction with hydrazine, halogenation, hydrolysis and esterification, and transition metal assisted coupling.

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23-05-2013 дата публикации

NOVEL TRPV3 MODULATORS

Номер: US20130131036A1
Принадлежит: AbbVie Inc.

Disclosed herein are modulators of TRPV3 of formula (II): 2. The compound according to claim 1 , or a salt thereof claim 1 , wherein u is 0.3. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': '1', 'Gis optionally substituted heteroaryl or optionally substituted cycloalkyl;'}{'sup': 2', '2d, 'Gis G; and'}{'sup': '2d', 'Gis optionally substituted aryl or optionally substituted heteroaryl.'}4. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': '1', 'Gis optionally substituted pyridinyl, pyrimidinyl, thiazolyl, oxazolyl, or pyrazolyl;'}{'sup': 2', '2d, 'Gis G; and'}{'sup': '2d', 'Gis optionally substituted phenyl or optionally substituted pyridinyl.'}5. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': 1', 'gc, 'sub': 1', '6', '1', '6', '2, 'Gis pyridinyl or pyrimidinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and N(R);'}{'sup': 'gc', 'sub': 1', '6, 'Ris hydrogen or C-C-alkyl;'}{'sup': 2', '2d, 'Gis G;'}{'sup': 2d', 'f, 'sub': 1', '6', '1', '6, 'Gis phenyl, pyridinyl, or pyrimidinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, —CN, C-C-alkyl, C-C-haloalkyl, and —OR; and'}{'sup': 'f', 'sub': 1', '6', '1', '6, 'Ris C-C-alkyl or C-C-haloalkyl.'}6. The compound according to claim 2 , or a salt thereof claim 2 , wherein:{'sup': 1', 'gc, 'sub': 1', '4', '1', '4', '2, 'Gis pyridinyl which is optionally substituted with 1 or 2 substituents independently selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, and N(R);'}{'sup': 'gc', 'sub': 1', '4, 'Ris hydrogen or C-C-alkyl;'}{'sup': 2', '2d, 'Gis G;'}{'sup': 2d', 'f, 'sub': 1', '4', '1', '4, 'Gis phenyl or pyridinyl; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group ...

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18-07-2013 дата публикации

CRYSTALLINE FORMS OF THE SODIUM SALT OF (4--CYCLOHEXYL)-ACETIC ACID

Номер: US20130184311A1
Принадлежит: NOVARTIS AG

The present invention relates to novel crystalline forms of (4-{4-[5-(6-Trifluoromethyl-pyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid, sodium and their use in the treatment or prevention of a condition or a disorder associated with DGAT1 activity in animals, particularly humans. It also relates to processes for making such novel crystalline forms. 2. A crystalline form according to in the form of Modification C claim 1 , N claim 1 , or O.3. A crystalline form according to in the form of Modification C.4. A crystalline form according to which remains dry at 25° C. and at a relative humidity ranging from 0% to 70%.5. A crystalline form according to which remains dry at 25° C. and at a relative humidity ranging from 0% to 80%.6. A crystalline form according to comprising at least about 80% by weight of said Modification.7. A crystalline form according to comprising at least about 85% by weight of said Modification.8. A crystalline form according to in the form of Modification C claim 1 , characterized by an X-ray powder diffraction pattern with peaks at 5.9 and 17.0 degrees two theta (±0.1 degree) (CuKαλ=1.5418 Å) claim 1 , or an X-ray powder diffraction pattern substantially in accordance with that shown in .9. A crystalline form according to the form of Modification C claim 1 , characterized by a powder x-ray diffraction pattern comprising four or more 2θ values (±0.1 degree) (CuKαλ=1.5418 Å) selected from the group consisting of 5.9 claim 1 , 17.0 claim 1 , 19.6 claim 1 , 22.5 claim 1 , 23.6 claim 1 , 28.4 and 30.0 claim 1 , at a temperature of about 22° C.10. A crystalline form according to claim 9 , in the form of Modification C claim 9 , further characterized by a powder x-ray diffraction pattern comprising five or more 2θ values (±0.1 degree) (CuKαλ=1.5418 Å) selected from the group consisting of 5.9 claim 9 , 17.0 claim 9 , 19.6 claim 9 , 22.5 claim 9 , 23.6 claim 9 , 28.4 and 30.0 claim 9 , at a temperature of about 22° C.11. A crystalline ...

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15-08-2013 дата публикации

SOLUBLE GUANYLATE CYCLASE ACTIVATORS

Номер: US20130210798A1
Принадлежит:

This inventions relates to compounds having the structure Formula I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver. 4. The compound of selected form the group consisting of:1-[6-(4-Chloro-3′-methyl-4′-{[1-(2,2,2-trifluoroethyl)azetidin-3-yl]methoxy}biphenyl-2-yl)pyridin-2-yl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-(6-[4-chloro-4′-(4-cyclopropylpiperidin-1-yl)biphenyl-2-yl]pyridin-2-yl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-{6-[4-chloro-4′-(4,4-difluorocyclohexyl)biphenyl-2-yl]pyridin-2-yl}-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-{6-[4′-(4-cyclopropylpiperidin-1-yl)-4-methylbiphenyl-2-yl]pyridin-2-yl}-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-(6-{4-chloro-4′-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]biphenyl-2-yl}pyridin-2-yl)-5-(trifluoromethyl)-1-pyrazole-4-carboxylic acid;1-[2′-{4-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]phenyl}-5′-(trifluoromethyl)-2,3′-bipyridin-6-yl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-[6-(4-chloro-4′-{4-[(2,2-difluorocyclopropyl)methyl]piperazin-1-yl}biphenyl-2-yl)pyridin-2-yl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-(6-{4-chloro-4′-[1-(methoxycarbonyl)piperidin-4-yl]biphenyl-2-yl}pyridin-2-yl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-(6-{4-chloro-4′-[1-(ethoxycarbonyl)piperidin-4-yl]biphenyl-2-yl}pyridin-2-yl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-(6-{4-chloro-4′-[1-(dimethylcarbamoyl)piperidin-4-yl]-3′-methylbiphenyl-2-yl}pyridin-2-yl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid;1-(6-{(4- ...

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24-10-2013 дата публикации

INHIBITORS OF FOCAL ADHESION KINASE

Номер: US20130281443A1
Принадлежит: The Scripps Research Institute

The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions. 140.-. (canceled)42. The compound of wherein X is a bond.43. The compound of wherein Y comprises in at least one occurrence a 5 or 6-membered heterocyclyl or heteroaryl which is substituted with 0-3 Y substituents.44. The compound of wherein Ror Ror both comprises a phenyl group substituted with 0-3 Y groups.45. The compound of wherein Rcomprises a morpholino-substituted phenyl group substituted with 0-2 additional Y groups.46. The compound of wherein Ris trifluoromethyl.47. The compound of wherein Ris nitro.48. The compound of wherein Ris fluoro.49. The compound of wherein Ris chloro.50. The compound of wherein Ris cyano.52. A method of inhibiting focal adhesion kinase claim 41 , in vitro or in vivo claim 41 , comprising contacting a compound selected from or at an effective concentration with the focal adhesion kinase.53. A method of treating cancer in a mammal that is mediated by abnormal focal adhesion kinase activities claim 41 , comprising administration of the compound of or in a dosage claim 41 , at a frequency claim 41 , and for a duration to produce a beneficial effect on the mammal.54. A pharmaceutical composition comprising a compound of or and a suitable excipient.56. The method of wherein the zero-valent transition metal complex is a zero-valent palladium complex claim 55 , wherein Z is halo claim 55 , or both.57. The method of wherein the zero-valent palladium complex comprises Pd(dba).58. The method of further comprising the ...

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14-11-2013 дата публикации

Organic-Inorganic Hybrid Mesoporous Silica Material Modified by Sulfonic Acid Group for Selective Adsorption of Metal Ions and Method of Manufacturing the Same

Номер: US20130303766A1

A silica precursor having a selective adsorptivity with respect to cobalt ions is disclosed. The silica precursor includes a cross-linked 2,6-diamino pyridine group obtained by using 2,6-diamino pyridine, phosgene and 3-aminopropyltriethoxysilane.

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12-12-2013 дата публикации

COMPOUNDS AND METHODS FOR TREATING DISEASES MEDIATED BY PROTEASE ACTIVATED RECEPTORS

Номер: US20130331411A1
Принадлежит:

The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof. 12-. (canceled)46-. (canceled)821-. (canceled)26. The method of claim 22 , wherein the patient is in need of inhibition of platelet activation.27. The method of claim 22 , wherein the patient is in need of inhibition of thrombus formation.28. The method of claim 22 , wherein the PAR1 disease is particular proliferative diseases of endothelial cells claim 22 , fibroblasts claim 22 , nephrocytes claim 22 , osteosarcoma cells claim 22 , muscle cells claim 22 , cancer cells and/or glia cells.2930-. (canceled)31. The method of claim 22 , wherein said PAR1 mediated disease is selected from acute Myocardial Infarction claim 22 , stable angina claim 22 , unstable angina claim 22 , aortocoronary bypass surgery claim 22 , acute occlusion following coronary angioplasty and or stent placement claim 22 , transient Ischemic attacks claim 22 , cerebrovascular disease claim 22 , peripheral vascular disease claim 22 , placental insufficiency claim 22 , prosthetic heart valves claim 22 , atrial fibrillation claim 22 , anticoagulation of tubing.32. (canceled)33. The method of claim 22 , wherein said disease or disorder is selected from acute myocardial infarction claim 22 , stable angina claim 22 , unstable angina claim 22 , transient ischemic attack claim 22 , cerebrovascular disease claim 22 , peripheral vascular disease claim 22 , placental insufficiency claim 22 , thrombosis subsequent to or associated with a surgical procedure claim 22 , thrombosis associated with atrial fibrillation claim 22 , and inflammation.3436-. (canceled)37. The method of claim 22 , wherein Cyl and Gare aromatic groups and Gis an alkyl group.38. The method of claim 22 , wherein each Gand Gis a group containing at least two carbons independently selected from aliphatic claim 22 , substituted ...

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26-12-2013 дата публикации

INHIBITORS OF PROTEIN KINASES

Номер: US20130345233A1
Принадлежит: Ingenium Pharmaceuticals GmbH

Compounds of general Formula (I): 2. The method of claim 1 , wherein in Formula (I) Ris H.3. The method of wherein in Formula (I) x is 2.4. The method of wherein in Formula (I) Ris halo claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy or Chaloalkoxy.5. The method of claim 4 , wherein in Formula (I) there are two Rgroups claim 4 , one of which is halo and the other of which is methoxy or halomethoxy.6. The method of wherein in Formula (I) Ris Cor Ccarbocyclic claim 4 , Cor Cheterocyclic claim 4 , —Calkyl-phenyl claim 4 , —Calkyl(Cor Cheteroaryl) claim 4 , —Calkyl(Cor Ccarbocyclic) claim 4 , —Calkyl(Cor Cheterocyclic) claim 4 , phenyl or Cor Cheteroaryl claim 4 , wherein any of the aforesaid cyclic groups may optionally be substituted as described in .7. The method of wherein in Formula (I) Ris cyclohexyl claim 4 , cyclopentyl claim 4 , —Calkyl(cyclohexyl) claim 4 , —Calkyl(cyclopentyl); or Ris piperidine claim 4 , piperazine claim 4 , morpholine and pyrrolidine claim 4 , —Calkyl(piperidine) claim 4 , —Calkyl(piperazine) claim 4 , —Calkyl(morpholine) claim 4 , —Calkyl(pyrrolidine); or Ris phenyl or —Calkyl-phenyl; or Ris pyridine claim 4 , thiazole claim 4 , thiophene claim 4 , —Calkyl(pyridine) claim 4 , —Calkyl(thiazole) or —Calkyl(thiophene) claim 4 , wherein any of the aforesaid cyclic groups may optionally be substituted as described in .8. The method of wherein in Formula (I) Ris a —Calkyl(carbocyclic) claim 1 , —Calkyl(heterocyclic) claim 1 , —Calkyl(aryl) or —Calkyl(heteroaryl) group claim 1 , and the —Calkyl linker is:{'sub': '2', '—CH—;'}{'sub': '3', '—CH(CH)—;'}{'sub': 2', '3, '—CHCH(CH)—;'}{'sub': 3', '2, '—CH(CH)CH—; or'}{'sub': 2', '2, '—CHCH—.'}9. The method of claim 1 , wherein in Formula (I) Ris unsubstituted or is substituted claim 1 , with one or more groups chosen from:{'sub': 1', '2, 'halo, OH, N—Hand, for carbocyclic and heterocyclic groups, ═O; or'}{'sub': 1-4', '1-4', '1-4', '1-4, 'Calkyl, —O(Calkyl), —NH(Calkyl), —NHC(O)(Calkyl), any of ...

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03-01-2019 дата публикации

IDO INHIBITORS

Номер: US20190002402A1
Принадлежит:

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. 2. The compound according to wherein Rand Rare independently H claim 1 , Cto Calkyl claim 1 , Cto Calkoxy claim 1 , or join together to form cyclopropyl or cyclobutyl.3. The compound according to wherein Z is —NH— and Ris —SOR claim 1 , halo (C-Calkyl) claim 1 , thiazolyl or oxazolyl claim 1 , wherein Ris Cto Calkyl claim 1 , Cto Ccycloalkyl4. The compound according to wherein Z is O and Ris H.5. The compound according to wherein Ris —COR.6. The compound according to wherein Ris a 5 membered heterocycle containing from 1 to 4 heteroatoms selected from N claim 1 , O claim 1 , and S.7. The compound according to wherein Ris H and Ris —CORor —CONRR; Ris H claim 1 , and Ris phenyl claim 1 , pyridyl claim 1 , isoxazolyl claim 1 , thiadiazolyl claim 1 , indolinyl claim 1 , or benzyl claim 1 , wherein Rmay optionally be substituted with from 1 to 3 substituents selected from the group consisting of halo claim 1 , amino claim 1 , phenoxy claim 1 , benzoxy claim 1 , isoxalyl claim 1 , Cto Calkoxy claim 1 , Cto Calkyl claim 1 , halo-Cto Calkyl claim 1 , and CN.8. The compound according to wherein Ris Cto Ccycloalkyl optionally substituted with halo claim 1 , —OH or Cto Calkoxy; Cto Calkyl optionally substituted with halo claim 1 , —OH or phenyl claim 1 , wherein said phenyl is optionally substituted with Cto Chaloalkyl claim 1 , Cto Calkoxy claim 1 , halo or Cto Calkyl; Cto Calkenyl; Cto Calkoxy; or benzyl optionally substituted with Cto Calkyl claim 1 , halo claim 1 , Cto Calkoxy claim 1 , or haloalkyl.9. The compound according to wherein Ris a Cto Cheterocycloalkyl containing from 1 to 4 heteroatoms selected from O claim 1 , N or S.10. The compound ...

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14-01-2016 дата публикации

METHOD FOR ALKYLATION OF AMINES

Номер: US20160009632A1
Автор: Nara Hideki, Ogata Osamu
Принадлежит:

The present invention provides a simple, efficient, and industrially advantageous method for the alkylation of amines. The present invention relates to a production method for N-alkylamines whereby an amine is reacted with an alcohol in the presence of a ruthenium complex represented by general formula (1): RuXY(CO)(L) (wherein X and Y can be the same or different and represent a monovalent anionic ligand, and L represents a tridentate aminodiphosphine ligand). 3. The production method according to claim 1 , wherein the N-alkylamine has the following general formula (4):{'br': None, 'sup': 'A', 'R—NH—R\u2003\u2003(4)'}wherein, in the general formula (4),{'sup': 'A', 'Rrepresents an alkyl group, a cycloalkyl group, an aryl group, an aralkyl group, a heterocyclic group, an alkenyl group, an alkynyl group, a cycloalkenyl group, an alkyloxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, a hydroxyl group, an alkoxycarbonyl group, a cycloalkyloxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group, an alkenyloxycarbonyl group, an alkynyloxycarbonyl group, a cycloalkenyloxycarbonyl group, a carboxamide group or an alkoxysulfonyl group, which groups may comprise substituent(s); and'}R represents an optionally substituted hydrocarbon group, an optionally substituted aryl group or an optionally substituted heterocyclic group, {'br': None, 'sup': 'A', 'sub': '2', 'R—NH\u2003\u2003(5)'}, 'wherein the amine has the following general formula (5){'sup': 'A', 'wherein, in the general formula (5), Rrepresents the same group as in the definition in the general formula (4), and'} {'br': None, 'R—OH\u2003\u2003(6)'}, 'the alcohol has the following general formula (6)wherein, in the general formula (6), R represents the same group as in the definition in the general formula (4).6. The method according to claim 1 , wherein the alcohol is a primary or secondary alcohol.7. The method according to claim 1 , wherein the alcohol is methanol or ethanol.8. ...

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08-01-2015 дата публикации

SUBSTITUTED 4-PHENYL-PYRIDINES

Номер: US20150011510A1
Принадлежит: HELSINN HEALTHCARE SA

Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK) receptor. The compounds have the general formula (I): 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare each independently selected from the group consisting of hydrogen claim 1 , hydroxy claim 1 , amino claim 1 , alkyl claim 1 , alkenyl claim 1 , cycloalkyl claim 1 , halogen claim 1 , cyano claim 1 , —ORand CF.32. The compound of any of - claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein X is —NRC(O).43. The compound of any of - claims 1 , or a pharmaceutically acceptable salt thereof claims 1 , wherein Y is a heterocycloalkyl or heterocycloalkylalkyl.1110. A method of treating emesis claims 1 , bladder dysfunction claims 1 , depression or anxiety claims 1 , in a patient in need thereof claims 1 , comprising administering to said patient a therapeutically effective amount of a compound of formula (I) according to any of -.12. The method of claim 11 , wherein said emesis comprises chemotherapy induced nausea and vomiting (CINV) claim 11 , radiation therapy induced nausea and vomiting (RINV) claim 11 , or post-operative nausea and vomiting (PONV).1312. The method of either of - claims 11 , wherein said emesis is induced by moderately or highly emetogenic chemotherapy.1413. The method of any of - claims 11 , wherein emesis is acute and delayed emesis induced by moderately or highly emetogenic chemotherapy.1514. The method of - claims 11 , wherein said bladder dysfunction is selected from urgency claims 11 , frequency claims 11 , pollakiuria claims 11 , nocturia claims 11 , low deferment time claims 11 , suboptimal volume threshold claims 11 , and neurogenic bladder claims 11 , or a combination thereof.1615. The method of any of - claims 11 , wherein said compound or a ...

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14-01-2021 дата публикации

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR

Номер: US20210009528A1
Принадлежит:

The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor. 134.-. (canceled) This application is a continuation of U.S. application Ser. No. 16/577,901, filed Sep. 20, 2019, now allowed, which is a divisional application of U.S. application Ser. No. 15/730,728, filed Oct. 11, 2017, now U.S. Pat. No. 10,584,101, which claims priority to, and the benefit of, U.S. Provisional Application No. 62/406,888, filed Oct. 11, 2016, and U.S. Provisional Application No. 62/528,385, filed Jul. 3, 2017, all of which are incorporated by reference in their entirety for all purposes.This invention was made with government support under grant number 1R44CA203199-01 by the National Cancer Institute. The government has certain rights in the invention.U.S. patent application Ser. No. 14/686,640, filed on Apr. 14, 2015, published as U.S. Patent Application Publication No. 2016/0058872; U.S. patent application Ser. No. 14/792,414, filed on Jul. 6, 2015, published as U.S. Patent Application Publication No. 2015/0291562; U.S. patent application Ser. No. 14/371,956, filed on Jul. 11, 2014, published as U.S. Patent Application Publication No. 2014/0356322; U.S. patent application Ser. No. 15/074,820, filed on Mar. 18, 2016, published as U.S. Patent Application Publication No. 2016/0272639, are incorporated herein in their entireties. Furthermore, all references cited herein are incorporated by ...

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19-01-2017 дата публикации

Novel azo compound, use thereof and method for preparing same

Номер: US20170016050A1
Принадлежит: Bioneer Corp

The present invention provides a novel azo compound having a quenching ability for the material that exhibits a luminescent phenomenon at an excited energy level, a quencher comprising the novel azo compound, a use of the quencher and a method for preparing the azo compound. The quencher according to the present invention may exhibit excellent characteristics in a wavelength absorption region.

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10-02-2022 дата публикации

Tricyclic Amino Containing Compounds for Treatment or Prevention of Symptoms Associated with Endocrine Dysfunction

Номер: US20220040174A9
Принадлежит:

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes. 2. A method of claim 1 , wherein the subject is diagnosed with breast cancer.3. A method of claim 1 , wherein the subject is diagnosed with prostate cancer.4. A method of claim 1 , wherein the subject is diagnosed with testicular cancer.5. A method of claim 1 , wherein the subject is diagnosed with thyroid cancer.6. A method of claim 1 , wherein the subject is diagnosed with uterine cancer.7. A method of claim 1 , wherein the subject is diagnosed with adrenocortical carcinoma.8. A method of claim 1 , wherein the subject is diagnosed with a pituitary tumour.9. A method of claim 1 , wherein the subject is diagnosed with a tumour of the endocrine glands.10. A method of claim 1 , wherein the subject is diagnosed with a tumour of the hypothalamus.11. A method of claim 1 , wherein the subject is receiving or has received chemotherapy.12. A method of claim 2 , wherein the compound is administered concomitant with chemotherapy.13. A method of claim 2 , wherein the compound is administered after chemotherapy.14. A method of claim 2 , wherein the compound is administered prior to chemotherapy.15. A method of claim 2 , wherein administration of the compound is maintained after cessation of the chemotherapy.16. A method of claim 14 , wherein the subject is due to receive chemotherapy within 10 days or less of receiving the compound.17. A method of claim 1 , wherein the subject is receiving or has received a hormone replacement or hormone supplement.18. A method of claim 1 , where the compound is administered in combination with another active agent.19. A method of claim 1 , wherein the compound is administered in combination with an agonist or antagonist of an estrogen receptor.20. A method of claim 1 , wherein the compound is administered in combination with tamoxifen. This application is ...

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10-03-2022 дата публикации

ANTIBODY EPITOPE

Номер: US20220074947A1
Принадлежит:

It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Antibodies which selectively bind to complexes of such compounds with TNF superfamily members are disclosed. These antibodies may be used to detect further compounds with the same activity, and as target engagement biomarker. 1. An antibody which binds to an epitope comprising at least one residue selected from L94 , P113 and Y115 of TNFα of SEQ ID NO: 36.2. An antibody according to claim 1 , which binds to trimeric TNFα.4. An antibody according to any one of to claim 1 , which binds to an epitope comprising all three of L94 claim 1 , P113 and Y115 claim 1 , wherein L94 is present on the A chain of a TNFα trimer and P113 and Y115 are present on the C chain of a TNFα trimer.5. An antibody according to any one of the preceding claims claim 1 , which binds to an epitope further comprising one or more residues selected from the following residues of TNFα of SEQ ID NO: 36 claim 1 , which residues are present on the A chain of a TNFα trimer:(a) T77;(b) T79;(c) Y87;(d) T89;(e) K90;(f) V91;(g) N92;(h) L93;(i) S95;(j) A96;(l) 197;(m) E135;(n) 1136; and(o) R138.6. An antibody according to any one of the preceding claims claim 1 , which binds to an epitope further comprising one or more residues selected from the following residues of TNFα of SEQ ID NO: 36 claim 1 , which residues are present on the C chain of a TNFα trimer:(a) L63;(b) D143;(c) F144;(d) S147; and(e) Q149.7. An antibody according to any one of the preceding claims claim 1 , which binds to an epitope further comprising one or more residues selected from the following residues of TNFα of SEQ ID NO: 36 claim 1 , which residues are present on the A chain of a TNFα trimer:(a) L75;(b) S81;(c) R82;(d) 183;(e) 197; and(f) D140.8. An antibody according to any one of the preceding claims claim 1 , which binds to an epitope further comprising one or more residues selected from the ...

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21-02-2019 дата публикации

HETEROARYL INHIBITORS OF PDE4

Номер: US20190055269A1
Принадлежит:

The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. 3. The method of claim 2 , wherein Ris either benzoxaborole claim 2 , or is phenyl which is para-substituted with a substituent of the form R-R-(R)(R) claim 2 , and is optionally substituted with a substituent R.4. The method of claim 2 , wherein Ris phenyl which is para-substituted with a substituent of the form R-R-(R)(R).5. The method of claim 2 , wherein Ris —C(O)N—; Ris chosen from lower hydroxyalkyl and hydrogen; and Ris hydrogen.6. The method of claim 4 , wherein Ris lower alkyl; Ris C(O)OH; and Ris null.7. The method of claim 4 , wherein Ris lower hydroxyalkyl.8. The method of claim 7 , wherein Ris chosen from methanol claim 7 , ethanol claim 7 , isopropanol claim 7 , N-propanol claim 7 , and t-butanol.9. The method of claim 8 , wherein Ris chosen from ethanol and N-propanol.10. The method of claim 4 , wherein Ris chosen from 5-6 membered monocyclic heterocycloalkyl claim 4 , and 5-6 membered monocyclic heteroaryl.13. The method of claim 4 , wherein Ris a bond.14. The method of claim 4 , wherein Ris lower alkyl.15. The method of claim 14 , wherein Ris methyl.16. The method of claim 10 , wherein Ris benzoxaborole.17. The method of claim 14 , wherein X is N.18. The method of claim 17 , wherein Ris chosen from 3-chlorophenyl and 5-chloro-2-thienyl.19. The method of claim 19 , wherein Ris 3-chlorophenyl.20. The method of claim 19 , wherein Ris 5-chloro-2-thienyl.21. The method of claim 18 , wherein Ris chosen from 3-chlorophenyl and 5-chloro-2-thienyl.22. The method of claim 21 , wherein Ris 3-chlorophenyl.23. The method of claim 22 , wherein Ris 5-chloro-2-thienyl.24. The method of claim 2 , wherein Ris chosen from cyclopentyl optionally substituted with one or two R claim 2 , and cyclopentoxy optionally ...

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05-03-2015 дата публикации

NEW COMPOUNDS

Номер: US20150065517A1
Принадлежит: NOVARTIS AG

The present invention provides organic compounds of the following structure; 137-. (canceled)39. The compound according to claim 38 , wherein the divalent residue —[R]—[R]—[C(O)]—[N(R)]—[R]—[R]— is selected from the group consisting of:a divalent alkyl group having from 1 to 4 carbon atomsa divalent alkenyl group having from 2 to 3 carbon atomsa —C(O)— group{'sup': 4', '5, 'sub': 'e', 'claim-text': [{'sup': '5', 'sub': 1', '4', '4', '8, 'e is 0 and Ris selected from the group consisting of a divalent substituted or unsubstituted C-Calkyl group, C-Ccycloalkyl group, phenyl group or 5- or 6-membered heterocyclyl group, or'}, {'sup': 4', '5, 'sub': 1', '4', '4', '8, 'e is 1, Ris a divalent substituted or unsubstituted C-Calkyl group, and Ris a divalent substituted or unsubstituted C-Ccycloalkyl cycloalkyl group, phenyl group or 5- or 6-membered heterocyclyl group,'}], 'a —C(O)—[R]—R— group wherein'}{'sup': 1', '2', '1', '2, 'sub': 1', '4', '4', '8, 'a —R—R— group, wherein Ris a divalent substituted or unsubstituted C-Calkyl group and Ris a divalent substituted or unsubstituted C-Ccycloalkyl group, phenyl group or 5- or 6-membered heterocyclyl group,'}a —C(O)—NH— group,{'sub': 2', '1-3', '2', '1-3, 'a —(CH)—C(O)—NH—(CH)— group,'}{'sup': 4', '4, 'sub': '1-7', 'a —C(O)—NH—R— group, wherein Ris selected from a divalent substituted or unsubstituted Calkyl group, cyclohexyl group or cyclopentyl group,'}{'sup': 3', '4', '3', '4, 'a —C(O)—N(R)—R— group, wherein Rand Rand the N-atom together form a pyrrolidine ring or a piperidine ring, or a pharmaceutically acceptable salt thereof.'}40. The compound according to claim 38 , wherein the alkylidenyl group is ═CH— claim 38 , or a pharmaceutically acceptable salt thereof.41. The compound according to claim 38 , wherein the L1 group is an amine group —NH— claim 38 , or a pharmaceutically acceptable salt thereof.42. The compound according to claim 38 , wherein the L1 group is an amide group —C(O)NH— or —NHC(O)— claim 38 , or a ...

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28-02-2019 дата публикации

HETEROCYCLE AND CARBOCYCLE DERIVATIVES HAVING TRKA INHIBITORY ACTIVITY

Номер: US20190062282A1
Принадлежит: Shionogi & Co., Ltd.

The present invention relates to a compound represented by Formula (I): 135-. (canceled)37. The compound according to claim 36 ,{'sup': 5', '5A, 'wherein ═X is ═O and Rand Rare hydrogen atoms,'}or its pharmaceutically acceptable salt.38. The compound according to claim 36 ,{'sup': '1', 'wherein Ris substituted or unsubstituted alkyl,'}or its pharmaceutically acceptable salt.39. The compound according to claim 36 ,{'sup': 3', '4, 'wherein Ris substituted or unsubstituted alkyl and Ris a hydrogen atom,'}or its pharmaceutically acceptable salt.41. The compound according to claim 36 ,wherein Ring C is a substituted or unsubstituted aromatic heterocycle,or its pharmaceutically acceptable salt.42. The compound according to claim 41 ,wherein Ring C is substituted or unsubstituted pyrazole,or its pharmaceutically acceptable salt.44. The compound according to claim 43 ,{'sup': 13', '14', '15, 'wherein Ris a hydrogen atom, or substituted or unsubstituted aromatic carbocyclyl, Ris substituted or unsubstituted aromatic heterocyclyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted aromatic carbocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl, and Ris substituted or unsubstituted alkyl,'}or its pharmaceutically acceptable salt.48. A pharmaceutical composition comprising the compound according to claim 36 , or its pharmaceutically acceptable salt. The present invention relates to a compound that has a TrkA inhibitory activity and is useful in the treatment and/or prevention of TrkA mediated disorders, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising thereof.The tropomyosin receptor kinase (Trk) is a family of receptor tyrosine kinases and has a function as a receptor of neurotrophin (NT). Three major subtypes of Trk receptors are TrkA high-affinity receptor for nerve growth factor (NGF), TrkB high-affinity receptor for brain-derived neutrophic factor (BDNF) and NT-4/5, and TrkC high-affinity receptor ...

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10-03-2016 дата публикации

Novel compounds as diacylglycerol acyltransferase inhibitors

Номер: US20160068487A1
Принадлежит: GlaxoSmithKline LLC

This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.

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15-03-2018 дата публикации

ANTIMICROBIAL PYRIDINOHYDRAZIDE AND HYDRAZOMETHYLPYRIDINE-BASED AGENTS

Номер: US20180072675A1
Принадлежит:

A class of modified salicylaldehyde derivatives has also been synthesized and a series of modified pyridine-based hydrazones identified that have potent antimicrobial activity against multiple spp. These compounds have been characterized using fungal growth inhibition assays, mammalian cell toxicity assays, time-kill assays and synergy studies of these novel pyridine-based hydrazones on both azole-susceptible and azole-resistant fungal species. Effectiveness of these compounds in inhibiting the growth of protozoal parasites was also found. 2. The compound of claim 1 , wherein Ris an ester having the forty OCOX claim 1 , wherein X is selected from the group consisting of: methyl claim 1 , ethyl claim 1 , cyclopentane cycloheptane claim 1 , CHCH claim 1 , phenyl claim 1 , 3 claim 1 ,4 claim 1 ,5-trimethoxyphenyl 2-acetyloxphenyl claim 1 , 2-pyridinyl claim 1 , 3-pyridiyl claim 1 , and 4-pyridinyl.3. The compound of claim 1 , wherein Ris selected from the group consisting of: phenyl claim 1 , 4-methylphenyl claim 1 , 4-methoxyphenyl 4-t-butyiphenyl claim 1 , 4-hydroxyphenyl claim 1 , 4-nitrophenyl claim 1 , 4-chlorophenyl claim 1 , 4-bromophenyl claim 1 , 4-iodophenyl claim 1 , 3 claim 1 ,4-dichlorophenyl claim 1 , 3 claim 1 ,4-dimethylphenyl claim 1 , 2-pyridinyl claim 1 , 3-pyridinyl claim 1 , 2-hydroxy-3 pyridinyl claim 1 , 4-pyridinyl claim 1 , 1-oxidopyridin-2-yl claim 1 , 1-oxidopyridin-3-yl claim 1 , and 1-oxidopyridin-4-yl.5. The compound of . wherein Ris an ester eying the formula OCOX claim 4 , wherein X is selected from the group consisting of: methyl claim 4 , ethyl claim 4 , oyclopentane claim 4 , cycloheptane claim 4 , CHCH claim 4 , phenyl claim 4 , 3 claim 4 ,4 claim 4 ,5-trimethoxyphenyl claim 4 , 2-acetyloxyphenyl claim 4 , 2-pyridinyl claim 4 , 3-pyridinyl claim 4 , and 4-pyridinyl.6. The compound of claim 4 , wherein Ris selected from the group consisting of: phenyl claim 4 , 4-methylphenyl claim 4 , 4-methoxyphenyl claim 4 , 4-t-butylphenyl claim 4 ...

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05-03-2020 дата публикации

Compounds and Methods of Use

Номер: US20200071296A1
Принадлежит:

This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies. 2. The method of claim 1 , wherein the individual is diagnosed with a cancer selected from the group consisting of breast cancer claim 1 , prostate cancer claim 1 , ovarian cancer claim 1 , lung cancer claim 1 , colon cancer claim 1 , brain tumors claim 1 , gastric cancer claim 1 , liver cancer claim 1 , thyroid cancer claim 1 , endometrial cancer claim 1 , gallbladder cancer claim 1 , kidney cancer claim 1 , adrenocortical cancer claim 1 , sarcoma claim 1 , skin cancer claim 1 , head and neck cancer claim 1 , leukemia claim 1 , bladder cancer claim 1 , colorectal cancer claim 1 , hematopoietic cancer claim 1 , and pancreatic cancer.3. The method of claim 1 , wherein the individual is diagnosed with breast cancer.4. The method of claim 3 , wherein the breast cancer is selected from the group consisting of ER negative breast carcinoma claim 3 , ER positive breast carcinoma claim 3 , primary breast ductal carcinoma claim 3 , mammary adenocarcinoma claim 3 , ER positive mammary ductal carcinoma claim 3 , ER negative mammary ductal carcinoma claim 3 , HER2 positive mammary ductal carcinoma claim 3 , HER2 positive breast cancer claim 3 , luminal breast cancer claim 3 , triple negative breast cancer (TNBC) claim 3 , and unclassified breast cancer.5. The method of claim 4 , wherein the breast cancer is TNBC claim 4 , and the TNBC is selected from the group consisting of basal-like TNBC claim 4 , mesenchymal TNBC claim 4 , mesenchymal stem-like TNBC claim 4 , immunomodulatory TNBC claim 4 , and a luminal androgen receptor TNBC.6. The method of claim 4 , wherein the breast cancer is a luminal breast cancer.7. The method of claim 1 , wherein the ...

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31-03-2022 дата публикации

MODULATORS OF TMEM16A FOR TREATING RESPIRATORY DISEASE

Номер: US20220098164A1
Принадлежит:

Compounds of general formula (I): 126.-. (canceled)30. The compound according to claim 27 , wherein Y is —CH—.31. The compound according to claim 27 , wherein:{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a 6- to 11-membered aryl group selected from phenyl, naphthyl, indanyl, 1,2,3,4-tetrahydronaphthyl and benzocycloheptanyl, any of which is unsubstituted or substituted as defined in ; or'}{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a 5- to 10-membered heteroaryl group selected from pyridyl, quinolinyl, quinoxalinyl, indazolyl, indolyl, benzoxazolyl, dihydrobenzofuranyl, furyl and thienyl, any of which is unsubstituted or substituted as defined in ; or'}{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a carbocyclyl group selected from cyclohexyl and adamantyl, any of which is unsubstituted or substituted as defined in .'}34. The compound according to claim 32 , wherein:{'sup': ['11a', '11b'], 'sub': ['1-4', '1-4'], '#text': 'the compound is a compound of formula (Iai), (Ibi), (Ici), (Idi), (Iei), (Ifi) or (Igi) and either Ris H, halo, Calkyl or C(O)O(Calkyl) and Ris H; or'}{'sup': ['11a', '11b'], '#text': 'both Rand Rare halo; or'}{'sup': '11a', '#text': 'the compound is a compound of formula (Iaii), (Ibii), (Icii), (Idii), (Ieii), (Ifii) or (Igii) and Ris H; and'}{'sup': '11b', 'sub': ['1-4', '1-4', '1-4'], '#text': 'Ris Calkyl, Calkyl substituted with OH or Chaloalkyl; and'}{'sup': '11c', '#text': 'Ris H, halo, methyl or ethyl.'}36. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable excipient.37. A method for the treatment or prophylaxis of diseases and conditions affected by modulation of TMEM16A claim 27 , the method comprising administering to a patient in need of such treatment an effective amount of a compound according to .38. The method of claim 37 , wherein the diseases and conditions affected ...

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25-03-2021 дата публикации

NOVEL TNFa STRUCTURE FOR USE IN THERAPY

Номер: US20210088530A1
Принадлежит:

A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy. 171-. (canceled)73. (canceled)74. A method for identifying a candidate inhibitor that interacts with a binding pocket at the centre of an apo TNFα trimer , comprising the steps of:(a) obtaining a TNFα trimer crystal with Space Group P 21 21 21, P 21 21 2, or P 1 21 1;(b) obtaining the structural coordinates of amino acids of the crystal of step a);(c) generating a 3-D model of a TNFα trimer using the structural coordinates of the amino acids generated in step b),(d) determining a binding pocket at the centre of the TNFα trimer from the 3-D model;(e) performing computer fitting analysis to design or identify the candidate inhibitor which interacts with the binding pocket; and(f) contacting the designed or identified candidate inhibitor with an apo TNFα trimer in vitro to determine the effect of the inhibitor on TNFα activity.7576-. (canceled)77. The method of claim 72 , wherein the designing or selecting of step (d) comprises determining deformation energy of binding of the candidate inhibitor with the binding pocket.78. The method of claim 77 , wherein the deformation energy of binding is not greater than 10 kcal/mole.79. The method of claim 78 , wherein the deformation energy of binding is not greater than 7 kcal/mole.80. The method of claim 72 , wherein the designing or selecting of step (d) comprises reducing the repulsive electrostatic interaction with the TNFα trimer and with surrounding water molecules.81. The method of claim 80 , wherein the repulsive electrostatic interaction is zero.82. The ...

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19-06-2014 дата публикации

Process for the preparation of 4-amino-5-fluoro-3-chloro-6-(substituted)picolinates

Номер: US20140171653A1
Принадлежит: DOW AGROSCIENCES LLC

4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a 3,3-dialkoxyprop-1-yne and a substituted methylene amine by a series of steps.

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07-04-2016 дата публикации

NOVEL HISTONE DEACETYLASE INHIBITORS

Номер: US20160096804A1
Принадлежит:

The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors. 3. A compound according to claim 2 , wherein W is —CONHOH.4. A compound of claim 3 , wherein each L is independently selected from a 5 or 6-membered nitrogen-containing heteroaryl claim 3 , which is optionally fused to a benzene.5. A compound of claim 1 , wherein in both L groups claim 1 , the atom that is directly bonded to the N is a carbon claim 1 , and at least one nitrogen atom is directly bonded to said carbon.6. A compound of claim 1 , wherein L is independently selected from pyridinyl claim 1 , pyrimidinyl claim 1 , pyridazinyl claim 1 , oxadiazolyl claim 1 , pyrazolyl claim 1 , thiadiazolyl claim 1 , pyrazinyl claim 1 , benzofused thiazolyl claim 1 , benzofused oxazolyl or benzofused imidazolyl claim 1 , preferably claim 1 , L is independently selected from pyridyl and pyrazinyl.7. A compound of claim 1 , wherein at least one L group is pyridyl or pyrazinyl.8. A compound of claim 1 , wherein Ris phenylene or phenylene substituted with a halogen.9. A compound of claim 1 , wherein at least one claim 1 , preferably both Rare H.10. A compound of claim 1 , wherein R′ that is attached to L is independently selected from the group consisting of H claim 1 , C-Calkyl or O—(C-Calkyl) claim 1 , halogen claim 1 , C-Cheterocycloalkyl claim 1 , aryl claim 1 , trifluoromethyl or heteroaryl.11. A compound of claim 1 , wherein at least one R′ is selected from the group consisting of H claim 1 , halogen claim 1 , CF claim 1 , C-Calkyl claim 1 , aryl optionally substituted with halogen claim 1 , heteroaryl optionally substituted with halogen or heterocycloalkyl.12. A compound of claim 1 , wherein at least one of the R′ that is attached to L is heterocycloalkyl.13. A compound according to claim 12 , wherein R′ attached to Ris hydrogen or halogen.14. A compound according to claim 12 , wherein at least one R′ is C-Calkyl optionally ...

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26-03-2020 дата публикации

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR

Номер: US20200095205A1
Принадлежит:

The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor. 134.-. (canceled)40. The method of claim 35 , wherein the composition further comprises an effective amount of at least one additional anti-cancer agent.41. The method of claim 36 , wherein the composition further comprises an effective amount of at least one additional anti-cancer agent.42. The method of claim 37 , wherein the composition further comprises an effective amount of at least one additional anti-cancer agent.43. The method of claim 38 , wherein the composition further comprises an effective amount of at least one additional anti-cancer agent.44. The method of claim 39 , wherein the composition further comprises an effective amount of at least one additional anti-cancer agent.45. The method of claim 40 , wherein the anti-cancer agent is estramustine claim 40 , docetaxel claim 40 , ketoconazole claim 40 , goserelin claim 40 , histrelin claim 40 , triptorelin claim 40 , buserelin claim 40 , cyproterone claim 40 , flutamide claim 40 , bicalutamide claim 40 , nilutamide claim 40 , pamidronate claim 40 , or zolendronate.46. The method of claim 41 , wherein the anti-cancer agent is estramustine claim 41 , docetaxel claim 41 , ketoconazole claim 41 , goserelin claim 41 , histrelin claim 41 , triptorelin claim 41 , buserelin claim 41 , cyproterone claim 41 , flutamide claim 41 , bicalutamide claim 41 , ...

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12-04-2018 дата публикации

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR

Номер: US20180099940A1
Принадлежит:

The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor. 4. The compound of claim 1 , wherein the CLM comprises a chemical group derived from an imide claim 1 , a thioimide claim 1 , an amide claim 1 , or a thioamide that binds to the cereblon E3 ubiquitin ligase.5. The compound of claim 4 , wherein the chemical group is a phthalimido group claim 4 , or an analog or derivative thereof.6. The compound of claim 1 , wherein the CLM is thalidomide claim 1 , lenalidomide claim 1 , pomalidomide claim 1 , analogs thereof claim 1 , isosteres thereof claim 1 , or derivatives thereof.12. The bifunctional compound of claim 9 , wherein CLM comprises a chemical group derived from an imide claim 9 , a thioimide claim 9 , an amide claim 9 , or a thioamide that binds cereblon E3 ubiquitin ligase.13. The bifunctional compound of claim 12 , wherein the chemical group is a phthalimido group claim 12 , or an analog or derivative thereof.14. The bifunctional compound of claim 9 , wherein the CLM is thalidomide claim 9 , lenalidomide claim 9 , pomalidomide claim 9 , analogs thereof claim 9 , isosteres thereof claim 9 , or derivatives thereof.21. The bifunctional compound according to claim 9 , wherein L is a polyethylene group optionally substituted with aryl or phenyl comprising from 1 to 10 ethylene glycol units.22. The bifunctional compound according to claim 9 , wherein the compound ...

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19-04-2018 дата публикации

Tricyclic Amino Containing Compounds for Treatment or Prevention of Symptoms Associated with Endocrine Dysfunction

Номер: US20180104243A1
Принадлежит:

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes. 2. The method of claim 1 , wherein the subject is menopausal or perimenopausal woman.3. The method of claim 1 , wherein the subject is menstruating or expecting to menstruate with a week.4. The method of claim 1 , wherein the subject is a woman diagnosed with vulvodynia.5. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with another active agent.6. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with an agonist or antagonist of an estrogen receptor.7. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with tamoxifen.8. The method of claim 1 , wherein the pharmaceucial composition is administered in combination with an antiandrogen.9. The method of claim 1 , wherein the subject is a man with prostate cancer.10. The method of Claim claim 1 , wherein the pharmaceutical composition is administered in combination with spironolactone claim 1 , cyproterone claim 1 , flutamide claim 1 , nilutamide claim 1 , bicalutamide claim 1 , finasteride claim 1 , or dutasteride.11. The method of claim 1 , wherein said compound is N-(4-((pyrimidin-2-ylamino)methyl)benzyl)-pyrimidin-2-amine or pharmaceutically acceptable salt thereof12. The method of claim 1 , further comprising the step of administering the pharmaceutical composition to the subject after claim 1 , before claim 1 , or during a surgery selected from a hysterectomy claim 1 , oophorectomy claim 1 , partial oophorectomy claim 1 , unilateral salpingo-oophorectomy claim 1 , bilaterial salpingo-oophorectomy or combination thereof.13. The use of a compound of in the production of a medicament for the treatment or prevention of hot flashes. This application claims priority to U.S. Provisional Application Number 61/ ...

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03-07-2014 дата публикации

Pyridylphenyl compounds for inflammation and immune-related uses

Номер: US20140187586A1
Принадлежит: Synta Phamaceuticals Corp

The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X 1 , X 2 , Z, R 3 , R 4 , and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

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13-05-2021 дата публикации

MECHANISM OF ACTION

Номер: US20210140972A1
Принадлежит:

The invention is in the field of TNF signalling. Compounds have been identified which are capable of modulating signalling of TNF trimers through receptors. Methods of identifying such compounds are therefore provided. The compounds themselves have utility in therapy. 120-. (canceled)22. A complex comprising a trimeric protein that is a tumor necrosis factor (TNF) superfamily member and the compound of .23. (canceled)24. A method of treating and/or preventing a disorder selected from an autoimmune claim 21 , an inflammatory claim 21 , a neurological claim 21 , a neurodegenerative claim 21 , a pain claim 21 , a nociceptive claim 21 , and a cardiovascular disorders in a subject in need thereof claim 21 , comprising administering the compound of to the subject.25. The method of claim 24 , wherein rheumatoid arthritis claim 24 , Crohn's disease claim 24 , psoriasis claim 24 , systemic lupus erythematosus claim 24 , Alzheimer's disease claim 24 , Parkinson's disease or epilepsy is treated and/or prevented.26. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.27. A method of treating and/or preventing a disorder selected from an autoimmune claim 22 , an inflammatory claim 22 , a neurological claim 22 , a neurodegenerative claim 22 , a pain claim 22 , a nociceptive claim 22 , and a cardiovascular disorder in a subject in need thereof claim 22 , comprising administering the complex of to the subject.28. A pharmaceutical composition comprising the complex of and a pharmaceutically acceptable carrier.29. The method of claim 27 , wherein rheumatoid arthritis claim 27 , Crohn's disease claim 27 , psoriasis claim 27 , systemic lupus erythematosus claim 27 , Alzheimer's disease claim 27 , Parkinson's disease or epilepsy is treated and/or prevented. The present invention relates to methods for identifying compounds which modulate signalling of TNF superfamily member trimers through TNF receptors. In particular, the invention relates ...

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25-04-2019 дата публикации

A VERSATILE LIGAND FOR PALLADIUM-CATALYZED META-C-H FUNCTIONALIZATIONS

Номер: US20190119212A1
Автор: YU JIN-QUAN
Принадлежит:

A class of mono-protected 3-amino-2-hydroxypyridine (MPAHP) ligands that enable the meta-C—H arylation of anilines, phenols, phenylacetic acids, and biologically relevant heterocyclic compounds using norbornene as a transient mediator is disclosed. The applicability of this meta-arylation methodology in the pharmaceutical industry is illustrated for heteroaryl substrates and heteroaryl iodide coupling partners, a feat made possible by using the MPAHP ligand. The enabling nature of MPAHP ligands to achieve other meta-C—H functionalization processes is also illustrated by the development of a meta-C—H amination reaction and a meta-C—H alkynylation reaction. 2. The method according to claim 1 , wherein n is 1.3. The method according to claim 2 , wherein Ring B is a heteroaromatic single 6-membered ring and Z is a carbon atom.5. The method according to claim 4 , wherein Ring A is a single ring structure.6. The method according to claim 5 , wherein said single ring structure is a heteroaromatic ring.7. The method according to claim 7 , wherein said single heteroaromatic ring contains a ring hetero atom or a ring substituent in the meta-position rotated counter clock-wise from said 1-position.8. The method according to claim 4 , wherein Ring A is a fused ring structure containing two rings.9. The method according to claim 5 , wherein said single ring structure is a carbocyclic aromatic ring.10. The method according to claim 9 , wherein said carbocyclic aromatic ring contains at least one substituent group.11. The method according to claim 1 , wherein Ris acetyl or 1-adamantoyl.12. The method according to claim 11 , wherein Ris hydrido claim 11 , Ris C-C-hydrocarbyl or trifluoromethyl and Ris hydrido.13. The method according to claim 1 , wherein A is CHand Ris C-C-hydrocarbyl carboxylate in a transient mediator compound of Formula II.14. The method according to claim 13 , wherein the remaining substituent R groups of a transient mediator compound of Formula II are hydrido. ...

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19-05-2016 дата публикации

Heteroaryl inhibitors of pde4

Номер: US20160137672A1
Принадлежит: Tetra Discovery Partners Llc

The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.

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10-06-2021 дата публикации

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR

Номер: US20210171470A1
Принадлежит:

The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor. 10. The compound of claim 1 , wherein the L has 1-25 optionally substituted ethylene glycol units wherein each O is optionally replaced with an optionally substituted N claim 1 , S claim 1 , P claim 1 , or Si atom.11. The bifunctional compound of claim 1 , wherein L has 1-10 optionally substituted ethylene glycol units wherein each O is optionally replaced with an optionally substituted N atom.15. The bifunctional compound according to claim 1 , wherein the compound is a member selected from the group consisting of Examples 1-399 claim 1 , 402 claim 1 , 409-413 claim 1 , and 415-625 from Tables 2-7 claim 1 , a salt claim 1 , a polymorph claim 1 , isostere claim 1 , and a prodrug thereof.16. A composition comprising an effective amount of a bifunctional compound of claim 1 , and a pharmaceutically acceptable carrier.17. The composition of claim 16 , wherein the composition further comprises at least one bioactive agent.18. The composition of claim 17 , wherein the bioactive agent is an anti-cancer agent. This application is a continuation of U.S. patent application Ser. No. 16/577,901, filed 20 Sep. 2019, which is a divisional of U.S. patent application Ser. No. 15/730,728, filed 11 Oct. 2017, now U.S. Pat. No. 10,584,101, which claims priority to and the benefit of U.S. Provisional Application No. 62/406,888, ...

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02-06-2016 дата публикации

Aryl lactam kinase inhibitors

Номер: US20160152621A1
Принадлежит: Bristol Myers Squibb Co

The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

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18-06-2015 дата публикации

Benzene or thiophene derivative and use thereof as vap-1 inhibitor

Номер: US20150166525A1
Принадлежит: R Tech Ueno Ltd

The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.

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04-09-2014 дата публикации

TRICYCLIC AMINO CONTAINING COMPOUNDS FOR TREATMENT OR PREVENTION OF SYMPTOMS ASSOCIATED WITH ENDOCRINE DYSFUNCTION

Номер: US20140248236A1
Принадлежит:

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes. 2. The method of claim 1 , wherein the subject is menopausal or perimenopausal woman.3. The method of claim 1 , wherein the subject is menstruating or expecting to menstruate with a week.4. The method of claim 1 , wherein the subject is a woman diagnosed with vulvodynia.5. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with another active agent.6. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with an agonist or antagonist of an estrogen receptor.7. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with tamoxifen.8. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with an antiandrogen.9. The method of claim 1 , wherein the subject is a man with prostate cancer.10. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with spironolactone claim 1 , cyproterone claim 1 , flutamide claim 1 , nilutamide claim 1 , bicalutamide claim 1 , finasteride claim 1 , or dutasteride.11. The method of claim 1 , wherein said compound is N-(4-((pyrimidin-2-ylamino)methyl)benzyl)-pyrimidin-2-amine or pharmaceutically acceptable salt thereof.12. The method of claim 1 , further comprising the step of administering the pharmaceutical composition to the subject after claim 1 , before claim 1 , or during a surgery selected from a hysterectomy claim 1 , oophorectomy claim 1 , partial oophorectomy claim 1 , unilateral salpingo-oophorectomy claim 1 , bilaterial salpingo-oophorectomy or combination thereof.13. The use of a compound of in the production of a medicament for the treatment or prevention of hot flashes. This application claims priority to U.S. Provisional Application No. 61/556,346 ...

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14-06-2018 дата публикации

Method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate

Номер: US20180162814A1
Принадлежит: DOW AGROSCIENCES LLC

A method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (I) from benzyl 4,5-difluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (II) is described. The method includes the use of amination and chlorination process steps to provide the compound of Formula I.

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15-06-2017 дата публикации

THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE

Номер: US20170166541A1
Принадлежит:

Compounds and compositions comprising compounds useful in the treatment of cancer are described herein. 2. The compound of claim 1 , wherein B and Bare taken together with the carbon atoms to which they are attached to form a carbonyl group.3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein D is a bond and Dis NR.5. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein D is a bond and Dis NR.6. The compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris hydrogen.7. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris heteroaralkyl substituted with 0-3 occurrences of R.8. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein A is phenyl substituted with 1 or 2 occurrences of R.9. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —ORand Ris alkyl.10. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris —ORand Ris alkyl.11. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris alkyl.12. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris alkyl.17. A method of treating a cancer characterized as having an IDH mutation claim 1 , the method comprising administering to a subject a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.18. A method of treating a cancer characterized as having an IDH mutation claim 4 , the method comprising administering to a subject a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.19. The method of claim 17 , wherein the IDH1 mutation is IDH1 R132X.20. The method of claim 18 , wherein the IDH1 mutation is IDH1 R132X. This continuation application claims priority from U.S. Ser. No. 13/492,159, filed Jun. 8, 2012, which is a continuation of International Patent Application PCT/US2010/059778, ...

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21-06-2018 дата публикации

ROR GAMMA (RORY) MODULATORS

Номер: US20180170863A1
Принадлежит:

Compounds according to Formula I: 2. The compound according to where Ais CR.3. The compound according to where Ais NR.4. The compound according to where Ris hydrogen.5. The compound according to wherein R claim 1 , and Rare both H.6. The compound according to where Ris H.7. The compound according to wherein all positions A in A-Aare CR—R claim 1 , and all positions R in R-Rare H.8. The compound according to where Ris according to Formula II wherein:{'sub': 10', '13', '10', '13', '10', '13, 'A-Aare N or CR-CR, respectively, with the proviso that no more than two of the four positions A in A-Acan be simultaneously N;'}{'sub': 10', '13, 'R-Rare independently H, amino, halogen, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl;'}{'sub': '14', 'Xis either C(6)aryl or C(1-5)heteroaryl, with all carbon atoms optionally substituted with halogen, cyano, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-3)alkyl.'}9. The compound according to where Ris according to Formula III wherein:{'sub': 20', '27', '20', '27', '20', '22', '23', '27, 'A-Aare N or CR-CRrespectively, with the proviso that no more than two of the three positions A in A-Acan be simultaneously N and that no more than three of the five positions A in A-Acan be simultaneously N;'}{'sub': 20', '22, 'R-Rare independently H, halogen, amino, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl;'}{'sub': 23', '27, 'R-Rare independently H, halogen, cyano, amino, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-3)alkyl;'}{'sub': '28', 'Xis either C(6)aryl or C(1-5)heteroaryl, with all carbon atoms optionally substituted with halogen, cyano, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-3)alkyl.'}10. The compound according to where Ris according to Formula IV or V wherein:{'sub': '30', 'Ais N or C;'}{'sub': 31', '31', '32, 'Ais O, carbonyl, NRor CR;'}{'sub': '31', 'Ris H or C(1-6)alkyl;'}{'sub': '32', 'Ris H, OH or C(1-6)alkyl, with all alkyl groups optionally substituted with one or more F or OH;'}{'sub': 33', '42', '33', '42', '33', '37', ' ...

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21-06-2018 дата публикации

NOVEL HISTONE DEACETYLASE INHIBITORS

Номер: US20180170876A1
Принадлежит:

The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors. 125-. (canceled)271. The compound of claim , wherein at least one L is pyrazinyl.281. The compound of claim , wherein the R′ attached to Ris hydrogen.291. The compound of claim , wherein L for each occurrence is pyrazinyl.301. The compound of claim , wherein R′ attached to L is independently selected for each occurrence from the group consisting of H , Calkyl , O—(Calkyl) , and halogen.311. A pharmaceutical composition comprising a compound of claim and a pharmaceutically acceptable carrier.32. A compound selected from the group consisting of: N-hydroxy-4-((pyrazin-2-yl(pyridin-2-yl)amino)methyl)benzamide; 4-(((5-fluoropyridin-2-yl)(pyrazin-2-yl)amino)methyl)-N-hydroxybenzamide; N-hydroxy-4-{[(pyrazin-2-yl)(pyrimidin-4-yl)amino]methyl}benzamide; 3-fluoro-N-hydroxy-4-{[(pyrazin-2-yl)(pyrimidin-4-yl)amino]methyl}benzamide; 4-{[bis(pyrazin-2-yl)amino]methyl}-N-hydroxybenzamide; 4-{[bis(pyrazin-2-yl)amino]methyl}-3-fluoro-N-hydroxybenzamide; and pharmaceutically acceptable salts thereof.331. A method of treating breast , ovarian , or prostate cancer in a patient in need thereof , comprising administering a therapeutically effective amount of a compound of claim . The present invention relates to novel compounds which are inhibitors of histone deacetylase (HDAC) and therefore have therapeutic utility.HDACs are zinc metalloenzymes that catalyse the hydrolysis of acetylated lysine residues. In histones, this returns lysines to their protonated state and is a global mechanism of eukaryotic transcriptional control, resulting in tight packaging of DNA in the nucleosome. Additionally, reversible lysine acetylation is an important regulatory process for non-histone proteins. Thus, compounds which are able to modulate HDAC have important therapeutic potential.WO2010/086646 discloses compounds which act as inhibitors of HDAC. The ...

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22-06-2017 дата публикации

Protein Kinase Conjugates and Inhibitors

Номер: US20170174691A1
Принадлежит:

The invention relates to protein conjugates that contain a protein kinase containing a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases. 144.-. (canceled)47. (canceled)4959.-. (canceled) This application claims the benefit of U.S. Patent Application No. 61/242,988, filed on Sep. 16, 2009, the entire teachings of which are incorporated herein by reference.The search for new therapeutic agents has been greatly aided in recent years by a better understanding of the structure of enzymes and other biomolecules associated with diseases. One important class of enzymes that has been the subject of extensive study is protein kinases.Protein kinases constitute a large family of structurally related enzymes that are responsible for the control of a variety of signal transduction processes within the cell. Protein kinases are thought to have evolved from a common ancestral gene due to the conservation of their structure and catalytic function. Almost all kinases contain a similar 250-300 amino acid catalytic domain. The kinases may be categorized into families by the substrates they phosphorylate (e.g., protein-tyrosine, protein-serine/threonine, lipids, etc.).In general, protein kinases mediate intracellular signaling by effecting a phosphoryl transfer from a nucleoside triphosphate to a protein acceptor that is involved in a signaling pathway. These phosphorylation events act as molecular on/off switches that can modulate or regulate the target protein biological function. These phosphorylation events are ultimately triggered in response to a variety of extracellular and other stimuli. Examples of such stimuli include environmental and chemical stress signals (e.g., osmotic shock, heat shock, ultraviolet radiation, bacterial endotoxin, and HO), ...

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21-06-2018 дата публикации

ANTIBODY EPITOPE

Номер: US20180172701A1
Принадлежит:

It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Antibodies which selectively bind to complexes of such compounds with TNF superfamily members are disclosed. These antibodies may be used to detect further compounds with the same activity, and as target engagement biomarker. 23-. (canceled)4. An antibody according to claim 1 , which binds to an epitope comprising all three of L94 claim 1 , P113 and Y115 claim 1 , wherein L94 is present on the A chain of the TNFα trimer and P113 and Y115 are present on the C chain of the TNFα trimer.6. (canceled)8. (canceled)10. An antibody according to claim 1 , which:{'sub': 'D-ab', '(a) has an affinity (K) of 1 nM or less;'}(b) has an affinity of 200 pM or less;(c) is a humanized antibody; or{'sub': '2', '(d) is a Fab, modified Fab, Fab′, modified Fab′, F(ab′), Fv, single domain antibody or an scFv.'}1113-. (canceled)1516-. (canceled)17. An antibody which competes for binding to TNFα with an antibody as defined in .18. An isolated polynucleotide encoding an antibody as defined in .1920-. (canceled)21. Use of an antibody as defined in as a target engagement biomarker for the detection of a compound-trimer complex in a sample obtained from a subject; wherein said antibody is detectable and said complex comprises trimeric TNFα and a compound that is capable of binding to trimeric TNFα claim 1 , whereby the compound-trimer complex binds to the requisite receptor and modulates the signalling induced by the trimer through the receptor.23. Use of an antibody as defined in in screening for a compound that elicits a conformational change in a TNFα trimer claim 1 , wherein said conformational change modulates the signalling of the requisite receptor on binding of the trimeric TNFα.2425-. (canceled)26. A method of identifying a compound that is capable of binding to a TNFα trimer and modulating signalling of the trimer through the requisite receptor claim ...

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09-07-2015 дата публикации

POLYMERIZABLE LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION, POLYMER MATERIAL AND METHOD FOR MANUFACTURING THE SAME, AND FILM

Номер: US20150191651A1
Принадлежит: FUJIFILM Corporation

A polymerizable liquid crystal compound represented by the formula (1); wherein Arepresents a Cmethylene group, one CHor two or more non-adjacent (CH)s in the methylene group may be substituted by —O—; Zrepresents —CO—, —O—CO— or a single bond; Zrepresents —CO— or —CO—CH═CH—; Rrepresents a hydrogen atom or methyl group; Rrepresents hydrogen, Cstraight-chain alkyl group, Cor Cstraight-chain alkoxy group, phenyl group, aryloxy group, vinyl group, acryloylamino group, methacryloylamino group, N-aryloxycarbamoyl group, N-alkyloxycarbamoyl group having a Calkyl group, N-(2-methacryloyloxyethyl)carbamoyloxy group or N-(2-acryloyloxyethyl)carbamoyloxy group; and each of L, L, Land Lindependently represents Calkyl group, Calkoxy group, Calkoxycarbonyl group, Cacyl group, halogen atom or hydrogen atom, at least one of L, L, Land Lrepresents a substituent other than hydrogen atom. 2. The polymerizable liquid crystal compound of claim 1 , wherein in the formula (1) claim 1 , Rrepresents hydrogen atom claim 1 , Cstraight-chain alkyl group claim 1 , Cor Cstraight-chain alkoxy group or phenyl group.3. The polymerizable liquid crystal compound of claim 1 , wherein each of L claim 1 , L claim 1 , Land Lindependently represents a alkyl group or hydrogen atom claim 1 , and at least one of L claim 1 , L claim 1 , Land Lrepresents a Calkyl group.4. The polymerizable liquid crystal compound of claim 1 , wherein each of L claim 1 , L claim 1 , Land Lindependently represents a methyl group or hydrogen atom claim 1 , and at least one of L claim 1 , L claim 1 , Land Lrepresents a methyl group.5. The polymerizable liquid crystal compound of claim 1 , wherein each of L claim 1 , L claim 1 , Land Lindependently represents a methyl group or hydrogen atom claim 1 , one of L claim 1 , L claim 1 , Land Lbeing assigned to a methyl group and three of L claim 1 , L claim 1 , Land Lbeing assigned to hydrogen atoms.6. The polymerizable liquid crystal compound of claim 1 , wherein Zrepresents a single ...

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15-07-2021 дата публикации

PROCESS FOR PREPARATION OF FOSNETUPITANT

Номер: US20210214306A1
Принадлежит: CADILA HEALTHCARE LIMITED

The present invention relates to a process for the preparation of fosnetupitant. The invention further relates to an amorphous fosnetupitant chloride hydrochloride and process for the preparation thereof. 1. A process for the preparation of fosnetupitant , the process comprising:(a) reacting netupitant with chloromethyl di-tert-butyl phosphate in one or more protic solvents; and(b) obtaining fosnetupitant.3. The process according to claim 2 , wherein the fosnetupitant salt is fosnetupitant chloride hydrochloride claim 2 , prepared by the process comprising:(a) reacting netupitant and chloromethyl di-tert-butyl phosphate in one or more protic solvents; and(b) obtaining fosnetupitant chloride hydrochloride by treatment with a hydrogen chloride source.5. The process according to claim 1 , wherein the protic solvent comprises one or more of methanol claim 1 , ethanol claim 1 , propanol claim 1 , isopropanol claim 1 , n-butanol claim 1 , t-butanol claim 1 , pentanol claim 1 , hexanol claim 1 , heptanol claim 1 , decanol claim 1 , dodecanol claim 1 , or mixtures thereof.6. The process according to claim 1 , wherein the reaction of netupitant with chloromethyl di-tert-butyl phosphate is performed in the presence of a base.7. The process according to claim 1 , wherein the method of obtaining fosnetupitant in step (b) comprises one or more of extraction claim 1 , evaporation claim 1 , crystallization claim 1 , filtration claim 1 , recrystallization claim 1 , centrifugation claim 1 , decantation claim 1 , and chromatographic operations.8. The process according to claim 6 , wherein the base comprises one or more of ammonia claim 6 , methylamine claim 6 , ethylamine claim 6 , t-butylamine claim 6 , dimethylamine claim 6 , diethylamine claim 6 , diisopropylamine claim 6 , trimethylamine claim 6 , triethylamine claim 6 , diisopropylmethylamine claim 6 , diisopropylethylamine claim 6 , tributylamine claim 6 , sodium hydroxide claim 6 , potassium hydroxide claim 6 , lithium ...

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15-07-2021 дата публикации

SMALL MOLECULE ANTAGONIST COMPOUND TAC5 SERIES HAVING TOLL-LIKE RECEPTOR 3/7/8/9 INHIBITORY FUNCTION

Номер: US20210214372A1
Автор: CHOI Sangdon, Kim Eunha

A small molecule antagonist compound having a toll-like receptor 3/7/8/9 inhibitory function and its use in inhibiting TLR7, TLR8, TLR9 and TLR3 are disclosed. A novel compound expressed by TAC5 and TAC5-a, TAC5-c, TAC5-d or TAC5-e which are derivatives thereof not only prevents TNFα secretion, NFkB activation, IkB degradation and MAPKs phosphorylation induced by poly(I:C) (TLR3 agonist), IMQ (TLR7 agonist), CL075 (TLR7/8 agonist), R848 (TLR7/8 agonist), TL8 (TLR8 agonist) or CpG ODN (TLR9 agonist), but also inhibits generation of inflammatory cytokine, and thus is highly advantageous for preventive or therapeutic use for TLR3/7/8/9-related autoimmune diseases and inflammatory diseases including systemic lupus erythematosus, psoriasis and the like. 6. A method of preventing or treating an autoimmune disease or an inflammatory disease comprising administering a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof of as an active ingredient to subject in need thereof.8. The method of preventing or treating an autoimmune disease or an inflammatory disease of claim 6 , wherein the autoimmune disease or inflammatory disease is selected from the group consisting of psoriasis claim 6 , systemic lupus erythematosus (SLE) claim 6 , skin rash claim 6 , photosensitivity claim 6 , arthritis claim 6 , oral ulcer claim 6 , nephritis claim 6 , hemocytopenia claim 6 , vasculitis claim 6 , serositis claim 6 , inflammatory bowel disease (IBD) claim 6 , diabetes claim 6 , multiple sclerosis claim 6 , skin sclerosis claim 6 , pemphigus claim 6 , atopic dermatitis claim 6 , urethritis claim 6 , cystitis claim 6 , arteriosclerosis claim 6 , allergic disease claim 6 , rhinitis claim 6 , asthma claim 6 , acute pain claim 6 , chronic pain claim 6 , periodontitis claim 6 , gingivitis claim 6 , gout claim 6 , myocardial infarction claim 6 , congestive heart failure claim 6 , high blood pressure claim 6 , angina pectoris claim 6 , gastric ulcer claim ...

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07-07-2016 дата публикации

P38 mapk inhibitors for the treatment of inflammatory diseases

Номер: US20160194336A1
Принадлежит: ALLINKY BIOPHARMA

The present invention provides new p38 mitogen activated protein (MAP) kinase allosteric inhibitors which are useful for the treatment of p38 mediated diseases such as inflammatory diseases, e.g. rheumatoid arthritis, osteoarthritis, psoriatic arthritis, pain, musculoskeletal system inflammation and musculoskeletal system aging. The present invention thus provides compounds for use in a method for treatment of inflammatory diseases, as well as for use in therapy in general, wherein the compound binds to the region composed of amino acids at positions 170-199 of Mitogen-activated protein kinase 14 (Uniprot accession nr Q16539 or SEQ ID No 1) and/or Mitogen-activated protein kinase 11 (Uniprot accession nr Q15759 or SEQ ID No 2), SEQ ID NO. 1 and SEQ ID NO. 2 being the amino acid sequences of MAPK14 (p38cx) and MAPK11 (p38β), respectively. The specific region composed of amino acids at positions 170-199 is herein disclosed as SEQ ID NO. 4 for Mitogen-activated protein kinase 14 and SEQ ID NO. 5 for Mitogen-activated protein kinase 11 and are believed to be new inhibitory binding sites.

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16-07-2015 дата публикации

Cyclopropanecarboxamido-substitute aromatic compounds as anti-tumor agents

Номер: US20150197511A1

Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.

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26-07-2018 дата публикации

TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF

Номер: US20180208575A1
Автор: TAFESSE Laykea
Принадлежит:

The invention relates to compounds of formula IA 2. The compound of or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , stereoisomer claim 1 , geometric isomer or tautomer thereof claim 1 , wherein X is O.4. The compound of or a pharmaceutically acceptable salt claim 3 , solvate claim 3 , stereoisomer claim 3 , geometric isomer or tautomer thereof claim 3 , wherein X is O.6. The compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein X is O.7. The compounds of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris -halo.8. The compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris —Cl claim 5 , —F claim 5 , or —CF.9. The compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein W is C and the dashed line is absent.10. The compound of claim 1 , wherein the pharmaceutically acceptable salt claim 1 , solvate claim 1 , stereoisomer claim 1 , geometric isomer or tautomer is a pharmaceutically acceptable salt.11. The compound of claim 3 , wherein the pharmaceutically acceptable salt claim 3 , solvate claim 3 , stereoisomer claim 3 , geometric isomer or tautomer is a pharmaceutically acceptable salt.12. A composition comprising the compound of or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , stereoisomer claim 1 , geometric isomer or tautomer thereof and a pharmaceutically acceptable carrier or excipient.13. A composition comprising the compound of or a pharmaceutically acceptable salt claim 3 , solvate claim 3 , stereoisomer claim 3 , geometric isomer or tautomer thereof and a pharmaceutically acceptable carrier or excipient.14. A composition comprising the compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or excipient.15. A method for treating or preventing pain claim 1 , UI claim 1 , an ulcer claim 1 , IBD claim 1 , or IBS in an animal claim 1 , comprising administering to an animal in need thereof claim 1 , an ...

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26-07-2018 дата публикации

Compounds and Methods of Use

Номер: US20180208577A1
Принадлежит:

This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies. 1. A method of treating a tumor in an individual , comprising administering to the individual a therapeutically effective amount of a compound or a pharmaceutically acceptable salt of the compound , wherein the compound is selected from the group consisting of:4-(5-bromo-2-(5-chloro-2-fluorophenyl)pyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyI)-5-isopropylpyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)pyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)pyridin-4-ylamino)-N-(2-hydroxypropyl)pyrimidine-5-carboxamide;4-((4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)pyridin-3-yl)methylamino)propan-2-ol;4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)-N-(1-hydroxypropan-2-yl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)pyridin-4-ylamino)-N-(1-hydroxypropan-2-yl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)pyridin-4-ylamino)-N-(1-hydroxy-2-methylpropan-2-yl)nicotinamide;(4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)pyridin-3-yl)(4-hydroxypiperidin-1-yl)methanone;4-(2-(5-chloro-2-fluorophenyl)-5-vinylpyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-ethylpyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-propylpyridin-4-ylamino)-N-(2-hydroxypropyl)pyrimidine-5-carboxamide;4-(2-(5-chloro-2-fluorophenyl)-5-methoxypyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;N-(2-acetamidoethyl)-4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)nicotinamide;N-(2-amino-2-oxoethyl)- ...

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20-08-2015 дата публикации

Manufacturing process for pyrimidine derivatives

Номер: US20150232446A1
Принадлежит: Individual

The invention relates to processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of such solid forms for the therapeutic treatment of warm-blooded animals.

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16-08-2018 дата публикации

NOVEL TNFalpha STRUCTURE FOR USE IN THERAPY

Номер: US20180231562A1
Принадлежит: Emerald Biostructures Inc, UCB Biopharma SRL

A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy.

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27-11-2014 дата публикации

Compounds and methods for purification of serine proteases

Номер: US20140346397A1
Принадлежит: Portola Pharmaceuticals LLC

Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.

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08-10-2015 дата публикации

INHIBITORS OF SYK

Номер: US20150284367A1
Принадлежит:

The present invention relates to the use of novel compounds of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases. 2. The compound according to claim 1 ,wherein:{'sup': 1', '1′', '1′, 'sub': 2', 'n, 'claim-text': [{'sup': 1′', '1″, 'R is phenyl, pyridyl, cycloalkyl, or lower alkyl, optionally substituted with one or more R;'}, {'sup': '1″', 'each R is independently cyano, amino, amino lower alkyl, halo, lower alkyl, cycloalkyl, or amino cycloalkyl lower alkyl;'}], 'Ris —OR, (CH)R, or oxo;'}{'sup': '2', 'Ris lower alkyl, cycloalkyl, cyano lower alkyl, hydroxy lower alkyl, halo lower alkyl, dialkyl amino, or lower alkoxy;'}R3 is absent, H, lower alkoxy, lower alkyl, or halo;{'sup': '4', 'Ris H or lower alkyl;'}{'sup': '1', 'Xis CH or N;'}{'sup': 2', '2, 'Xis CH, CRor N;'}{'sup': '3', 'Xis CH or N;'}{'sup': '1', 'Yis CH or N; and'}{'sup': '2', 'Yis CH or N;'}{'sup': '3', 'Yis CH or N;'}or a pharmaceutically acceptable salt thereof.3. The compound according to claim 1 , wherein Yand Yare N.4. The compound according to claim 1 , wherein Ris —NR claim 1 , optionally substituted with one or more R.5. The compound according to claim 1 , wherein R is lower alkyl claim 1 , optionally substituted with one or more R.6. The compound according to claim 1 , wherein R is amino lower alkyl.7. The compound according to claim 1 , wherein Xis N.8. The compound according to claim 1 , wherein Xis CRand Xis CH.9. The compound according to claim 1 , wherein Ris H.10. The compound according to claim 1 , wherein Ris lower alkyl.11. The compound according to claim 1 , wherein Ris lower alkoxy or lower alkyl.12. The compound according to claim 1 , wherein Ris absent.13. The compound according to claim 1 , wherein n is 0.14. The compound according to claim 1 , wherein Ris —OR claim 1 , optionally substituted with one or more R.15. The compound according to claim 1 , ...

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15-10-2015 дата публикации

5-FLUORO-N-(PYRIDIN-2-YL)PYRIDIN-2-AMINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP

Номер: US20150291528A1
Принадлежит: BAYER PHARMA AKTIEGESELLSCHAFT

The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). 6. The compound of general formula (I) according to claim 1 , wherein{'sup': '1', 'Rrepresents a methyl, ethyl, 2-hydroxyethyl or 2-aminoethyl group;'}{'sup': '2', 'Rrepresents a 4-fluoro-2-methoxyphenyl or 4-fluoro-2-ethoxyphenyl group;'}{'sup': '3', 'Rrepresents a hydrogen atom, a fluoro atom or a chloro atom, or a methyl, methoxy, difluoromethyl or trifluoromethyl group;'}{'sup': '4', 'Rrepresents a hydrogen atom or a bromo atom;'}{'sup': '5', 'sub': 3', '3', '2', '2', '5, 'Rrepresents a hydrogen atom, or a group selected from cyano, —C(O)CH, —C(O)CF, —C(O)OCH, —C(O)N(H)CH;'}or an enantiomer, diastereomer, salt, solvate or salt of a solvate thereof.7. The compound according to claim 1 , which is(rac)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine;(+)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine;(−)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine;(rac)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{6-methyl-4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine;(rac)-5-Bromo-N-[5-fluoro-4-(4-fluoro-2-methoxyphenyl)pyridin-2-yl]-6-methyl-4-[(S-methylsulfonimidoyl)methyl]pyridin-2-amine;(rac)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{6-methoxy-4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine;(rac)-N-{6-Chloro-4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}-5-fluoro-4-(4-fluoro-2- ...

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05-09-2019 дата публикации

HETEROARYL INHIBITORS OF PDE4

Номер: US20190270759A1
Принадлежит:

The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. 150-. (canceled)52. The pharmaceutical composition of claim 51 , comprising a therapeutically effective amount of between 0.1 mg/kg and 500 mg/kg.53. The pharmaceutical composition of claim 51 , comprising between 5 mg and 500 mg of the compound.54. The pharmaceutical composition of claim 53 , comprising between 10 mg and 200 mg of the compound.55. The pharmaceutical composition of claim 51 , wherein the compound is administered orally.56. The pharmaceutical composition of claim 55 , wherein the compound is administered as a tablet or capsule.57. The pharmaceutical composition of formulated to be administered twice daily.59. The method of claim 58 , wherein the PDE4-mediated disease is chosen from depression claim 58 , anxiety claim 58 , degradation of learning and memory ability claim 58 , Alzheimer's disease claim 58 , dementia claim 58 , Parkinson's disease claim 58 , Huntington's disease claim 58 , late motor disorders claim 58 , mild cognitive impairment claim 58 , stroke claim 58 , ischemia claim 58 , depression secondary to illness claim 58 , major depressive disorder claim 58 , multiple sclerosis claim 58 , chronic inflammatory demyelinating polyneuropathy claim 58 , transverse myelitis claim 58 , amyotrophic lateral sclerosis claim 58 , and arteriosclerotic dementia.60. The method of claim 59 , wherein the PDE4-mediated disease is Alzheimer's disease.61. The method of claim 58 , wherein the therapeutically effective amount is administered orally.62. The method of claim 58 , wherein the therapeutically effective amount is administered once daily.63. The method of claim 58 , wherein the therapeutically effective amount is administered twice daily. This application is a continuation application of U.S. ...

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22-10-2015 дата публикации

Novel compounds as diacylglycerol acyltransferase inhibitors

Номер: US20150299138A1
Принадлежит: GlaxoSmithKline LLC

This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.

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10-11-2016 дата публикации

Compounds and Methods of Use

Номер: US20160326137A1
Принадлежит:

This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies. 313-. (canceled)1624-. (canceled)26. (canceled)2830-. (canceled)31. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound is selected from the group consisting of:4-(5-bromo-2-(5-chloro-2-fluorophenyl)pyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)pyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)pyridin-4-ylamino)-N-(2-hydroxypropyl)pyrimidine-5-carboxamide;1-((4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)pyridin-3-yl)methylamino)propan-2-ol;4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)-N-(1-hydroxypropan-2-yl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)pyridin-4-ylamino)-N-(1-hydroxypropan-2-yl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)pyridin-4-ylamino)-N-(1-hydroxy-2-methylpropan-2-yl)nicotinamide;(4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)pyridin-3-yl)(4-hydroxypiperidin-1-yl)methanone;4-(2-(5-chloro-2-fluorophenyl)-5-vinylpyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-ethylpyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)-N-(2-hydroxypropyl)pyrimidine-5-carboxamide;4-(2-(5-chloro-2-fluorophenyl)-5-methoxypyridin-4-ylamino)-N-(2-hydroxypropyl)nicotinamide;N-(2-acetamidoethyl)-4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)nicotinamide;N-(2-amino-2-oxoethyl)-4-(2-(5-chloro-2-fluorophenyl)-5- ...

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26-11-2015 дата публикации

Compounds and methods for purification of serine proteases

Номер: US20150337285A1
Принадлежит: Portola Pharmaceuticals LLC

Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.

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30-11-2017 дата публикации

HETEROARYL INHIBITORS OF PDE4

Номер: US20170342094A1
Принадлежит:

The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. 5. The compound as recited in claim 4 , wherein Ris either benzoxaborole claim 4 , or is phenyl which is para-substituted with a substituent of the form R—R—(R)(R) claim 4 , and is optionally substituted with a substituent R.6. The compound as recited in claim 5 , wherein Y is chosen from O claim 5 , NH claim 5 , and CH.7. The compound as recited in claim 6 , wherein Y is NH.8. The compound as recited in claim 6 , wherein Y is CH.9. The compound as recited in claim 8 , wherein Ris phenyl which is para-substituted with a substituent of the form R—R—(R)(R).10. The compound as recited in claim 9 , wherein{'sub': '9', 'Ris —C(O)N—;'}{'sub': '10a', 'Ris lower hydrogen; and'}{'sub': '10b', 'Ris null.'}11. The compound as recited in claim 9 , wherein{'sub': '9', 'Ris lower alkyl;'}{'sub': '10a', 'Ris C(O)OH; and'}{'sub': '10b', 'Ris null.'}12. The compound as recited in claim 9 , wherein Ris lower hydroxyalkyl.13. The compound as recited in claim 12 , wherein Ris chosen from methanol claim 12 , ethanol claim 12 , isopropanol claim 12 , N-propanol claim 12 , and t-butanol.14. The compound as recited in claim 13 , wherein Ris chosen from ethanol and N-propanol.15. The compound as recited in claim 9 , wherein Ris chosen from 5-6 membered monocyclic heterocycloalkyl claim 9 , and 5-6 membered monocyclic heteroaryl.18. The compound as recited in claim 10 , wherein Ris a bond.19. The compound as recited in claim 11 , wherein Ris a bond.20. The compound as recited in claim 11 , wherein Ris lower alkyl.21. The compound as recited in claim 20 , wherein Ris methyl.22. The compound as recited in claim 15 , wherein Ris benzoxaborole.23. The compound as recited in claim 18 , wherein X is N.24. The compound as recited in claim 19 , wherein ...

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08-12-2016 дата публикации

TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF

Номер: US20160355499A1
Автор: TAFESSE Laykea
Принадлежит:

The invention relates to compounds of formula IA 2. The compound of or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , stereoisomer claim 1 , geometric isomer or tautomer thereof claim 1 , wherein X is O.4. The compound of or a pharmaceutically acceptable salt claim 3 , solvate claim 3 , stereoisomer claim 3 , geometric isomer or tautomer thereof claim 3 , wherein X is O.6. The compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein X is O.7. The compounds of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris -halo.8. The compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris —Cl claim 5 , —F claim 5 , or —CF.9. The compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein W is C and the dashed line is absent.10. The compound of claim 1 , wherein the pharmaceutically acceptable salt claim 1 , solvate claim 1 , stereoisomer claim 1 , geometric isomer or tautomer is a pharmaceutically acceptable salt.11. The compound of claim 3 , wherein the pharmaceutically acceptable salt claim 3 , solvate claim 3 , stereoisomer claim 3 , geometric isomer or tautomer is a pharmaceutically acceptable salt.12. A composition comprising the compound of or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , stereoisomer claim 1 , geometric isomer or tautomer thereof and a pharmaceutically acceptable carrier or excipient.13. A composition comprising the compound of or a pharmaceutically acceptable salt claim 3 , solvate claim 3 , stereoisomer claim 3 , geometric isomer or tautomer thereof and a pharmaceutically acceptable carrier or excipient.14. A composition comprising the compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or excipient.15. A method for treating or preventing pain claim 1 , UI claim 1 , an ulcer claim 1 , IBD claim 1 , or IBS in an animal claim 1 , comprising administering to an animal in need thereof claim 1 , an ...

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07-12-2017 дата публикации

Process for the preparation of 4-amino-5-fluoro-3-chloro-6-(substituted)picolinates

Номер: US20170349549A1
Принадлежит: DOW AGROSCIENCES LLC

4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a 3,3-dialkoxyprop-1-yne and a substituted methylene amine by a series of steps.

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12-11-2020 дата публикации

HETEROARYL INHIBITORS OF PDE4

Номер: US20200354384A1
Принадлежит:

The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. 150-. (canceled)55. A pharmaceutical composition comprising a compound as recited in claim 51 , together with a pharmaceutically acceptable carrier.56. A method of treatment of a PDE4-mediated disease in a subject comprising the administration of a therapeutically effective amount of a compound as recited in .57. The method as recited in wherein the PDE4 is PDE4B.58. The method as recited in wherein the PDE4B-mediated disease is chosen from depression claim 57 , depression secondary to illness claim 57 , Huntington's disease claim 57 , Alzheimer's Disease claim 57 , cognitive impairment claim 57 , and schizophrenia.59. The method as recited in wherein the PDE4 is PDE4D.60. A method of treatment of disease in a subject comprising the administration of a therapeutically effective amount of a compound as recited in claim 51 , wherein the disease is chosen from depression claim 51 , depression secondary to illness claim 51 , Huntington's disease claim 51 , Alzheimer's Disease claim 51 , cognitive impairment claim 51 , and schizophrenia.61. A method of modulation of a PDE4-mediated function in a subject comprising the administration of a therapeutically effective amount of a compound as recited in claim 51 , wherein:the PDE4 is PDE4D;the modulation is enhancement; andthe function is cognition.62. A method for achieving an effect in a patient comprising the administration of a therapeutically effective amount of a compound as recited in to a patient claim 51 , wherein the effect is cognition enhancement.63. A method for achieving an effect in a patient comprising the administration of a therapeutically effective amount of a compound as recited in to a patient claim 51 , wherein the effect is cognition enhancement.64. A ...

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12-12-2019 дата публикации

Tricyclic Amino Containing Compounds for Treatment or Prevention of Symptoms Associated with Endocrine Dysfunction

Номер: US20190374541A1
Принадлежит:

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes. 2. A method of claim 1 , wherein the subject is diagnosed with breast cancer.3. A method of claim 1 , wherein the subject is diagnosed with prostate cancer.4. A method of claim 1 , wherein the subject is diagnosed with testicular cancer.5. A method of claim 1 , wherein the subject is diagnosed with thyroid cancer.6. A method of claim 1 , wherein the subject is diagnosed with uterine cancer.7. A method of claim 1 , wherein the subject is diagnosed with adrenocortical carcinoma.8. A method of claim 1 , wherein the subject is diagnosed with a pituitary tumour.9. A method of claim 1 , wherein the subject is diagnosed with a tumour of the endocrine glands.10. A method of claim 1 , wherein the subject is diagnosed with a tumour of the hypothalamus.11. A method of claim 1 , wherein the subject is receiving or has received chemotherapy.12. A method of claim 2 , wherein the compound is administered concomitant with chemotherapy.13. A method of claim 2 , wherein the compound is administered after chemotherapy.14. A method of claim 2 , wherein the compound is administered prior to chemotherapy.15. A method of claim 2 , wherein administration of the compound is maintained after cessation of the chemotherapy.16. A method of claim 14 , wherein the subject is due to receive chemotherapy within 10 days or less of receiving the compound.17. A method of claim 1 , wherein the subject is receiving or has received a hormone replacement or hormone supplement.18. A method of claim 1 , where the compound is administered in combination with another active agent.19. A method of claim 1 , wherein the compound is administered in combination with an agonist or antagonist of an estrogen receptor.20. A method of claim 1 , wherein the compound is administered in combination with tamoxifen. This application is ...

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19-12-2019 дата публикации

Tricyclic Amino Containing Compounds for Treatment or Prevention of Symptoms Associated with Endocrine Dysfunction

Номер: US20190381042A1
Принадлежит:

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes. 2. The method of claim 1 , wherein the subject is a menopausal or perimenopausal woman.3. The method of claim 1 , wherein the subject is menstruating or expecting to menstruate within a week.4. The method of claim 1 , wherein the subject is a woman diagnosed with vulvodynia.5. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with another active agent.6. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with an agonist or antagonist of an estrogen receptor.7. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with tamoxifen.8. The method of claim 1 , further comprising the step of administering the pharmaceutical composition to the subject after claim 1 , before claim 1 , or during a surgery selected from a hysterectomy claim 1 , oophorectomy claim 1 , partial oophorectomy claim 1 , unilateral salpingo-oophorectomy claim 1 , bilaterial salpingo-oophorectomy or combination thereof. This application is continuation of U.S. patent application Ser. No. 15/618,814, filed Jun. 9, 2017, which is a continuation of U.S. patent application Ser. No. 14/934,715, filed Nov. 6, 2015, which is a continuation of U.S. patent application Ser. No. 14/356,302, filed May 5, 2014, which is a national phase application under 35 U.S.C. § 371 of International Application No. PCT/US2012/063796, filed on Nov. 7, 2012, which claims priority to U.S. Provisional Application Number 61/556,347 filed Nov. 7, 2011, the entire contents of each application being incorporated herein by reference.The disclosure provides pharmaceutical compositions and methods of use of certain tricyclic amino containing compounds for the prevention or treatment of symptoms associated with endocrine ...

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24-12-2020 дата публикации

Modulator assay

Номер: US20200400678A1
Принадлежит: UCB Biopharma SRL

It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. A new assay for identifying compounds with this mechanism of action is also disclosed.

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21-07-2011 дата публикации

Oligomerization of olefins

Номер: WO2011085951A1

The invention deals with oligomerization, especially tetramerization of olefins by use of a catalyst system comprising an organometalliccomplex of an element of group 3 to 10 of the Periodic Table of the Elements and a didendate nitogen comprising ligand.

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12-09-2017 дата публикации

一类stat3蛋白抑制剂的三元环类化合物

Номер: CN107151232A
Принадлежит: Individual

本发明涉及一类STAT3蛋白抑制剂的三元环类化合物。该化合物为式I化合物及其药学上可接受的盐、前药和溶剂合物,及包含所述化合物的药物组合物,并涉及其合成方法。此外,本发明涉及包含所述化合物的药物组合物,可用于预防或治疗与STAT3蛋白相关疾病的STAT3蛋白抑制剂。本发明公开一类STAT3蛋白抑制剂三元环类新化合物结构为:一种式(I)的新化合物:

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23-10-2001 дата публикации

Ligands for metals and improved metal-catalyzed processes based thereon

Номер: US6307087B1
Принадлежит: Massachusetts Institute of Technology

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

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28-05-2002 дата публикации

Ligands for metals and improved metal-catalyzed processes based thereon

Номер: US6395916B1
Принадлежит: Massachusetts Institute of Technology

One aspect of the present invention relates to novel, electron-rich bidentate ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

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20-09-2005 дата публикации

Ligands for metals and improved metal-catalyzed processes based thereon

Номер: US6946560B2
Принадлежит: Massachusetts Institute of Technology

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

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11-04-2006 дата публикации

Ligands for metals and improved metal-catalyzed processes based thereon

Номер: US7026498B2
Принадлежит: Massachusetts Institute of Technology

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

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25-03-2015 дата публикации

基质化合物和掺杂剂化合物的新颖组合及包含该组合的有机电致发光器件

Номер: CN104471026A

本发明涉及掺杂剂化合物和基质化合物的特定组合以及包括该特定组合的有机电致发光器件。本发明的有机电致发光器件发射黄-绿光,通过提高器件的电流特征降低了器件的驱动电压,并且提高了功率效率和工作寿命。

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04-12-2013 дата публикации

4-氨基-3-氯-5-氟-6-(取代的)吡啶-2-甲酸酯的制备方法

Номер: CN103429082A
Принадлежит: DOW AGROSCIENCES LLC

4-氨基-3-氯-5-氟-6-(取代的)吡啶-2-甲酸酯是通过一系列步骤方便地从3,4,5,6-四氯吡啶-2-甲腈制备的,所述步骤包括氟交换、胺化、与肼反应、卤化、水解和酯化及过渡金属辅助的偶联。

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15-01-2014 дата публикации

류코형 색원체 함유 수용액의 보존 방법

Номер: KR20140005890A
Автор: 하루요 소야
Принадлежит: 교와 메덱스 가부시키가이샤

류코형 색원체 함유 수용액에, 니트로소기 및 아조기로 이루어지는 군에서 선택되는 적어도 하나의 치환기를 갖고, 또한 금속 이온 배위능을 갖는 화합물 또는 그 염을 첨가하는 것을 특징으로 하는, 류코형 색원체 함유 수용액의 보존 방법 ; 류코형 색원체를, 니트로소기 및 아조기로 이루어지는 군에서 선택되는 적어도 하나의 치환기를 갖고, 또한 금속 이온 배위능을 갖는 화합물 또는 그 염을 포함하는 수용액 중에서 공존시키는 것을 특징으로 하는, 류코형 색원체의 안정화 방법 ; 류코형 색원체와, 니트로소기 및 아조기로 이루어지는 군에서 선택되는 적어도 하나의 치환기를 갖고, 또한 금속 이온 배위능을 갖는 화합물 또는 그 염을 함유하는 액상 시약.

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22-07-2015 дата публикации

抗肿瘤药物

Номер: CN103508961B
Принадлежит: Crown Bioscience Inc Taicang

本发明涉及式I的化合物及其药用盐,其中M,L,A,W,X,Y,Z,和R 1 至R 4 如说明书中所定义。本发明还涉及含有这些化合物的药物组合物,它们的制备方法和它们在制备用于治疗癌症的药物的应用。

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27-03-2015 дата публикации

Method of obtaining 4-amino-3-chloro-5-fluoro-6-(substituted)picolinates

Номер: RU2545021C1

FIELD: chemistry. SUBSTANCE: invention relates to a method of obtaining 4-amino-3-chloro-5-fluoro-6-(substituted)picolinate of formula I where R stands for (C 1 -C 4 )alkyl, cyclopropyl, (C 2 -C 4 )alkenyl or phenyl, which contains from 1 to 4 substituents, as such independently selected are: a halogen, (C 1 -C 4 )alkyl, (C 1 -C 4 )halogenalkyl, (C 1 -C 4 )alkoxy or (C 1 -C 4 )halogenalkoxy; R 1 stands for (C 1 -C 12 )alkyl or non-substituted or substituted (C 7 -C 11 )arylalkyl; which includes the following stages: a) fluorination of 3,4,5,6-tetrachloropicolinonitrile by a source of fluoride-ions, b) amination of 3-chloro-4,5,6-trifluoro-2-picolinonitrile with ammonia, c) substitution of fluorine-substituent in position 6 with 4-amino-3-chloro-5,6-difluoropicolinonitrile by means of hydrogen bromide (HBr), hydrogen chloride (HCl) or hydrogen iodide (HI) and nitrile hydrolysis, d) etherification of 4-amino-3-chloro-5-fluoro-6-halogenpicolineamide by a strong acid and alcohol (R 1 OH) and e) combination of 4-amino-3-chloro-5-fluoro-6-halogenpicolinate of formula E with an aryl-, alkyl- or alkenylmetalorganic compound. EFFECT: obtaining the target product with the high output. 2 cl, 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 545 021 C1 (51) МПК C07D 213/79 (2006.01) C07D 213/803 (2006.01) A01N 43/40 (2006.01) A01P 13/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2013139300/04, 24.01.2012 (24) Дата начала отсчета срока действия патента: 24.01.2012 Приоритет(ы): (30) Конвенционный приоритет: (73) Патентообладатель(и): ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи (US) (45) Опубликовано: 27.03.2015 Бюл. № 9 2 5 4 5 0 2 1 (56) Список документов, цитированных в отчете о поиске: RU 2002120923, A, 10.01.2004 . US R U 25.01.2011 US 61/435,966 (72) Автор(ы): АРНДТ Ким Э. (US), РЕНГА Джеймс М. (US), ЧЖУ Юаньмин (US), УАЙТЕКЕР Грегори Т. (US), ЛОУ Кристиан Т. (US) 5710106, A1, 20.01.1998. WO 2001051468, A1, 19.07.2001 (85) ...

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20-01-2000 дата публикации

Ligands for metals and metal-catalyzed processes

Номер: WO2000002887A2
Принадлежит: Massachusetts Institute of Technology

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject processes provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

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20-02-1999 дата публикации

2-cyano-3-hydroxypropeneamides, methods of their synthesis and a pharmaceutical composition based on said

Номер: RU2126387C1
Принадлежит: Руссель Юклаф

FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention relates to 2-cyano-3-hydroxypropeneamides of the formula (I) where each of A, B and E means =CH-group or nitrogen atom; R is C 3 -C 6 -cycloalkyl; R 1 is hydrogen; R 2 and R 3 are similar or distinct - hydrogen, C 1 -C 6 -alkyl, trifluoromethyl, halogen, nitro-group. Invention relates to also methods of synthesis of compounds of the formula (I). The 1-st method: compound of the formula (II) is subjected for interaction with sodium hydride and then with functional derivatives of an acid of the formula Hal-C(O)-R A where Hal is halogen atom; R A has values R or they are R-protected radical. The synthesized compound of the formula (IA) is isolated after protecting group removal if necessary. The 2-d method: compounds of the formula (IV) ДЗ 9СсЬс ПЧ Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ "” 2 126 387. (51) МПК 13) Сл С 070 213/40, А 61 К 31/44 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 94000064/04, 04.01.1994 (30) Приоритет: 05.01.1993 СВ 9300083.4 (46) Дата публикации: 20.02.1999 (56) Ссылки: ЕР 0326107 АЛ, 1989. ЗЦ 5898888, 1978. ЕР 0190683 АЛ, 1986. ЕК 2485008, 1981. Машковский М.Д. Лекарственные средства-- М.: Медицина, 1985, ч.1, с.182-183. (98) Адрес для переписки: 103735 Москва, ул.Ильинка 5/2, Союзпатент (71) Заявитель: Руссель Юклаф (ЕК) (72) Изобретатель: Элизабет Анн Кюо (СВ) (73) Патентообладатель: Руссель Юклаф (ЕК) (54) 2-ЪЦИАНО-3-ГИДРОКСИПРОПЕНАМИДЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ (57) Реферат: Изобретение ОТНОСИТСЯ К 2-циано-3-гидроксипропенамидам формулы | Е Е 2 3 он `, но ри “А и в о 1 сн где А. ВиЕ каждый представляют собой группу =СН или атом азота, причем только один из них является атомом азота, К-С з-Сё-циклоалкил, К\-водород, К и Кз одинаковые или разные - водород, С 1-Св-алкил, трифторметил, галоген, нитрогруппа, которые обладают повышенной противовоспалительной активностью. Изобретение ...

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20-07-2012 дата публикации

New compounds

Номер: RU2456273C2
Принадлежит: НОВАРТИС АГ

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to compounds of formula: wherein B is specified in a group consisting of pyridine, pyridazine, pyrimidine and oxazole which can be optionally substituted by halogen, C 1-7 -alkyl or a C 1-7 -alkoxy group; L1 is specified in a group consisting of -NH-, -C(O)NH- and -NHC(O)-, A means C 3 -C 12 -cycloalkyl, C 6 -C 12 -aryl, a 4-7-member monocyclic heterocyclic group consisting of 1-3 heteroatoms optionally specified in O N and S, or a bicyclic heterocyclyl specified in a group consisting of benzimidazolyl, benzoxazolyl, benzothiazolyl, wherein cycloalkyl, aryl, mono- or bicyclic heterocyclyl can be optionally substituted by one or more substitutes optionally specified in a group consisting of a cyano group, halogen, an oxo group, C 1-7 -alkyl, C 1-7 -halogenalkyl, a C 1-7 -alkoxy group, C 1-7 -halogenalkoxy group, an amino group, a di-C 1-7 -alkylamino group, a C 1-7 -alkylthio group and C 3-8 -cycloalkyl, 1-2- means a bivalent residue specified in a group consisting of: - a bivalent alkyl group consisting of 1 to 4 carbon atoms, a bivalent alkenyl group consisting of 2 to 3 carbon atoms, - -C(O)-, - -C(O)-[R 4 ] c -R 5 - wherein c is equal to 0, and R 5 is specified in a group consisting of a bivalent C 1 -C 4 -alkyl group optionally substituted by another C 1 - 4 -alkyl, a C 4 -C 8 -cycloalkyl group, a phenyl group and a 5- or 6-member heterocyclyl group consisting of N heteroatoms, - -C(O)-NH-, - -(CH 2 ) 1-3 -C(O)-NH-(CH 2 ) 1-3 -, - -C(O)-NH-R 4 - wherein R 4 is specified in a group consisting of a bivalent C 1 -C 7 -alkyl group optionally substituted by another C 1-4 -alkyl, a cyclohexyl group and a cyclopentyl group, and E is specified in a group consisting of: - COOH, - a ester group of carboxylic acid, or to its pharmaceutically acceptable salts. What is also described is a pharmaceutical composition exhibiting DGAT1 modulatory activity, on the basis of the presented compounds, and also a method of ...

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20-12-2008 дата публикации

2-propen-1-ons as hsp-70 inductors

Номер: RU2341522C2

FIELD: chemistry. SUBSTANCE: described are novel compounds of series 2-propen-1-on of general formula or their tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, pharmaceutically acceptable solvates, where Q stands for heteroaryl cycle, containing up to 2 nitrogen atoms. Compounds I induce HSP-70 and are useful in treatment of diseases accompanying pathologic process in organisms of mammals, including humans. EFFECT: novel compounds possess useful biological properties. 26 cl, 7 tbl, 179 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 341 522 (13) C2 (51) ÌÏÊ C07D 401/04 (2006.01) C07D 401/14 (2006.01) C07D 403/10 (2006.01) C07D 403/12 (2006.01) A61K 31/4375 (2006.01) A61P 9/10 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2006139940/04, 11.04.2005 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 11.04.2005 (30) Êîíâåíöèîííûé ïðèîðèòåò: 12.04.2004 IN 178/KOL/2004 (43) Äàòà ïóáëèêàöèè çà âêè: 20.05.2008 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: WO 00/18390, À, 06.04.2000. WO 03/097574, À, 27.11.2003. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 13.11.2006 Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé, ðåã. ¹ 517 (54) 2-ÏÐÎÏÅÍ-1-ÎÍÛ Â ÊÀ×ÅÑÒÂÅ ÈÍÄÓÊÒÎÐΠHSP-70 (57) Ðåôåðàò: Íàñòî ùåå èçîáðåòåíèå îòíîñèòñ ê íîâûì ñîåäèíåíè ì ð äà 2-ïðîïåí-1-îíà îáùåé ôîðìóëû I R U 2 3 4 1 5 2 2 (87) Ïóáëèêàöè PCT: WO 2005/097746 (20.10.2005) C 2 C 2 (86) Çà âêà PCT: IN 2005/000112 (11.04.2005) ïîëèìîðôàì, ôàðìàöåâòè÷åñêè ïðèåìëåìûì ñîë ì, ôàðìàöåâòè÷åñêè ïðèåìëåìûì ñîëüâàòàì, ãäå Q îçíà÷àåò ãåòåðîàðèëüíûé öèêë, ñîäåðæàùèé äî 2 àòîìîâ àçîòà. Ñîåäèíåíè I èíäóöèðóþò HSP70 è ïîëåçíû ïðè ëå÷åíèè çàáîëåâàíèé, ñîïðîâîæäàþùèõ ïàòîëîãè÷åñêèé ñòðåññ â îðãàíèçìàõ ìëåêîïèòàþùèõ, âêëþ÷à ÷åëîâåêà. Îïèñàíû òàêæå ñïîñîá ëå÷åíè ñ ïîìîùüþ ñîåäèíåíèé I, ôàðìàöåâòè÷åñêèå êîìïîçèöèè ...

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20-01-2015 дата публикации

Method of obtaining 4-amino-3-chloro-5-fluoro-6-(substituted)picolinates

Номер: RU2539578C1

FIELD: chemistry. SUBSTANCE: invention relates to method of obtaining 4-amino-3-chloro-5-fluoro-6-(substituted)picolinate of formula I , where R represents (C1-C4)alkyl, cyclopropyl, (C2-C4)alkenyl or phenyl, which contains from 1 to 4 substituents, as such independently selected are halogen, (C1-C4)alkyl, (C1-C4)haloalkyl, (C1-C4)alkoxy or (C1-C4)haloalkoxy; and R1 represents (C1-C12)alkyl or non-substituted (C7-C11)arylalkyl, which includes fluoride substitution, amination, reaction with hydrazine, halogenation, hydrolysis and etherification, as well as catalised by transition metals combination. EFFECT: method improvement. 4 cl, 6 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 539 578 C1 (51) МПК C07D 213/803 (2006.01) C07D 213/04 (2006.01) A01N 43/40 (2006.01) A01P 13/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2013139346/04, 24.01.2012 (24) Дата начала отсчета срока действия патента: 24.01.2012 Приоритет(ы): (30) Конвенционный приоритет: (73) Патентообладатель(и): ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи (US) (45) Опубликовано: 20.01.2015 Бюл. № 2 2 5 3 9 5 7 8 (56) Список документов, цитированных в отчете о поиске: US 4087431, A1,02.05.1978. US 3755338, R U 25.01.2011 US 61/435,974 (72) Автор(ы): ЧЖУ Юаньмин (US), УАЙТЕКЕР Грегори Т. (US), АРНДТ Ким Э. (US), РЕНГА Джеймс М. (US), ФРОУЭС Роберт Д. (US) A1, 28.08.1973. US 3971799,A1, 27.07.1976. RU 225401, C2, 20.06.2005 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 26.08.2013 (86) Заявка PCT: US 2012/022288 (24.01.2012) (87) Публикация заявки PCT: 2 5 3 9 5 7 8 C 1 C 1 WO 2012/103044 (02.08.2012) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры", А.В. Миц (54) СПОСОБ ПОЛУЧЕНИЯ 4-АМИНО-3-ХЛОР-5-ФТОР-6-(ЗАМЕЩЕННЫХ)ПИКОЛИНАТОВ (57) Реферат: Изобретение относится к способу получения содержащий от 1 до 4 заместителей, в качестве 4-амино-3-хлор-5-фтор-6-(замещенного) которых ...

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01-09-2011 дата публикации

Oligomerization of olefins

Номер: WO2011085951A8

The invention deals with oligomerization, especially tetramerization of olefins by use of a catalyst system comprising an organometalliccomplex of an element of group 3 to 10 of the Periodic Table of the Elements and a didendate nitogen comprising ligand.

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27-12-2012 дата публикации

Method of producing toluidine compound

Номер: RU2470919C2

FIELD: chemistry. SUBSTANCE: invention relates to a method of producing 3-chloro-N-(3-chloro-5-trifluoromethyl-2-pyridyl)-α,α,α-trifluoro-2,6-dinitro-p-toluidine, which involves (1) a step of reacting 2-amino-3-chloro-5-trifluoromethylpyridine and 2,4-dichloro-3,5-dinitrobenzotrifluoride in the presence of an alkali component selected from a group consisting of hydroxides and carbonates of alkali metals and hydroxides and carbonates of alkaline earth metals as an alkaline substance, a solvent selected from a group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water for almost full dissolution of the alkali component, (2) a step of neutralising or acidifying the reaction mixture with an acid and (3) a step of removing the solvent from a mixture containing 3-chloro-N-(3-chloro-5-trifluoromethyl-2-pyridyl)-α,α,α-trifluoro-2,6-dinitro-p-toluidine as the reaction product and the reaction solvent by distillation in order to precipitate crystals of the product, where at step (1), water is present in amount of 20-40% with respect to the total amount of water and solvent. EFFECT: novel method of producing fluazinam with high output using simple operations in industrially preferred reaction systems is described. 17 cl, 13 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 470 919 (13) C2 (51) МПК C07D 213/72 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2010107469/04, 29.07.2008 (24) Дата начала отсчета срока действия патента: 29.07.2008 (45) Опубликовано: 27.12.2012 Бюл. № 36 2 4 7 0 9 1 9 R U (85) Дата начала рассмотрения заявки PCT на национальной фазе: 02.03.2010 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: WO 2007/060662 А2, 31.05.2007. US 4331670, 25.05.1982. JP 57126475 A, 06.08.1982. US 5081133, 14.01.1992. (86) Заявка PCT: JP 2008/063933 (29.07.2008) (87) Публикация заявки РСТ: WO 2009/017241 (05.02.2009) Адрес для переписки: 129090, Москва, ул. Б. Спасская, ...

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21-07-2020 дата публикации

ROR GAMMA (RORγ) MODULATORS

Номер: RU2727191C2

FIELD: medicine; pharmaceuticals. SUBSTANCE: invention relates to compounds of formula I possessing RORγ inhibitor properties activity, and a pharmaceutical composition based thereon for treating RORγ-mediated diseases or conditions. In general formula I A 1 is NR 1 or CR 1 , where R 1 is H or methyl, where methyl, if present, is optionally substituted with one or more F; cyclopropyl part can be optionally substituted with one or more methyl and one or more F; A 2 -A 5 are CR 2 -CR 5 , respectively; R 2 -R 5 are independently H or C(1-6)alkyl; R 6 and R 7 independently are H, methyl or hydroxyl; all alkyl groups, if present, are optionally substituted with one or more F; R 8 is H or C(1-2)alkyl and R 9 is selected from a group comprising formula II, III, IV and V. Other radical values are given in the claim. EFFECT: disclosed are RORγ modulators. 17 cl, 48 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (51) МПК C07D 213/75 C07D 231/12 C07D 333/36 C07D 233/61 C07C 311/20 C07C 317/32 ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 409/04 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 249/08 C07D 263/32 C07D 271/06 (12) (11) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (13) 2 727 191 C2 C07D 277/46 (2006.01) A61K 31/10 (2006.01) A61K 31/18 (2006.01) A61P 29/00 (2006.01) A61P 37/00 (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК (21)(22) Заявка: 2017145929, 03.06.2016 (24) Дата начала отсчета срока действия патента: Дата регистрации: 21.07.2020 (73) Патентообладатель(и): ЛИД ФАРМА ХОЛДИНГ Б.В. (NL), САНОФИ (FR) Приоритет(ы): (30) Конвенционный приоритет: 05.06.2015 EP 15170764.3 (45) Опубликовано: 21.07.2020 Бюл. № 21 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 09.01.2018 (56) Список документов, цитированных в отчете о поиске: WO 2013029338 A1, 07.03.2013. WO 2013171729 A3, 21.11.2013. WO 2014125426 A1, 21.08.2014. RU 2487121 C2, 10.07.2013. WO 2012100734 A1, 02.08.2012. WO 2014179564 A8, 04.12.2014. R U 2 7 2 7 1 9 1 (86) Заявка PCT: EP ...

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17-11-2011 дата публикации

Diagnostic agents for amyloid beta imaging

Номер: WO2011141515A1
Принадлежит: BAYER PHARMA AKTIENGESELLSCHAFT

This invention relates to compounds suitable for labeling or already labeled by F-18, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging.

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29-11-2019 дата публикации

The novel combination of matrix compounds and dopant compound and organic electroluminescence device comprising the combination

Номер: CN110511250A

本发明涉及掺杂剂化合物和基质化合物的特定组合以及包括该特定组合的有机电致发光器件。本发明的有机电致发光器件发射黄‑绿光,通过提高器件的电流特征降低了器件的驱动电压,并且提高了功率效率和工作寿命。

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05-08-2015 дата публикации

Process for the preparation of 4-amino-3-chloro-5-fluoro-6-(substituted)picolinates

Номер: KR101542340B1

본 발명은 불소 교환, 아미노화, 히드라진과의 반응, 할로겐화, 가수분해 및 에스테르화 및 전이 금속 보조 커플링을 비롯한 일련의 단계에 의하여 3,4,5,6-테트라클로로피콜리노니트릴로부터 간편하게 생성된 4-아미노-3-클로로-5-플루오로-6-(치환된)피콜리네이트에 관한 것이다. The present invention is conveniently produced from 3,4,5,6-tetrachloropycolinonitrile by a series of steps including fluorine exchange, amination, reaction with hydrazine, halogenation, hydrolysis and esterification, and transition metal assisted coupling Amino-3-chloro-5-fluoro-6- (substituted) picolinate.

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02-11-2020 дата публикации

COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF THE ANDROGENIC RECEPTOR

Номер: RU2019113229A
Принадлежит: Эрвинэс, Инк.

РОССИЙСКАЯ ФЕДЕРАЦИЯ ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) (19) RU (11) (13) 2019 113 229 A (51) МПК C07D 233/86 (2006.01) C07D 401/04 (2006.01) C07D 491/107 (2006.01) C07D 471/10 (2006.01) A61K 31/4164 (2006.01) A61K 31/4439 (2006.01) A61K 35/00 (2006.01) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2019113229, 11.10.2017 (71) Заявитель(и): ЭРВИНЭС, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет: 11.10.2016 US 62/406,888; 03.07.2017 US 62/528,385 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 29.04.2019 US 2017/056234 (11.10.2017) (87) Публикация заявки PCT: WO 2018/071606 (19.04.2018) A Адрес для переписки: 129090, Москва, пр-кт Мира, 6, ООО "Патентно-правовая фирма "ЮС" R U (57) Формула изобретения 1. Соединение, характеризующееся структурой: ABM-L-CLM, где АВМ представляет собой связывающий андрогенный рецептор (AR) фрагмент, L представляет собой химический линкерный фрагмент, CLM представляет собой связывающий цереблон Е3-убиквитинлигазу фрагмент, где АВМ содержит структуру, выбранную из группы, состоящей из: Стр.: 1 A 2 0 1 9 1 1 3 2 2 9 (54) СОЕДИНЕНИЯ И СПОСОБЫ ДЛЯ НАПРАВЛЕННОЙ ДЕГРАДАЦИИ АНДРОГЕННОГО РЕЦЕПТОРА 2 0 1 9 1 1 3 2 2 9 (86) Заявка PCT: R U (43) Дата публикации заявки: 02.11.2020 Бюл. № 31 (72) Автор(ы): КРЮ, Эндрю, П. (US), ХОРНБЕРГЕР, Кейт, Р. (US), СНАЙДЕР, Лоуренс, Б. (US), ЦИММЕРМАНН, Курт (US), ВАН, Цзин (US), БЕРЛИН, Михаэль (US), КРЮС, Крэйг, М. (US), ДУН, Ханьцин (US) где: A 2 0 1 9 1 1 3 2 2 9 замещенное 0-6 RQ, каждый RQ независимо представляет собой Н, C1-6 алкил (неразветвленный, разветвленный, необязательно замещенный, например, необязательно замещенный 1 или несколькими из галогена, C1-6 алкоксила), галоген, С1-6 алкокси или 2 RQ группы, взятые вместе с атомом, к которому они присоединены, образуют 3-8членную кольцевую систему, содержащую 0-2 гетероатома); R1, R2, Ra, Rb, RY1, RY2 каждый независимо представляет собой Н, C1-6 алкил (неразветвленный, разветвленный, необязательно замещенный; ...

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14-07-2010 дата публикации

Process for producing toluidine compound

Номер: CN101778824A
Принадлежит: Ishihara Sangyo Kaisha Ltd

由于氟啶胺为优异的农药活性成分且高度有用,希望以环境友好方式的低成本的简单操作的合适方式有效制备氟啶胺。所需产物用简单的操作通过使用工业有利的反应体系通过包括如下步骤的方法以良好产率得到:使ACTF和DCDNBTF在碱组分,选自酮、腈、醚和酯的溶剂和其量足以基本溶解碱组分的水存在下反应的步骤,(2)用酸中和或酸化反应混合物的步骤,和(3)通过蒸馏从含有作为反应产物的氟啶胺和反应溶剂的混合物中除去溶剂以沉淀产物晶体的步骤。

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10-05-2013 дата публикации

Azabiphenylaminobenzoic acid derivatives as dhodh inhibitors

Номер: RU2481334C2
Принадлежит: Альмираль, С.А.

FIELD: chemistry.SUBSTANCE: invention describes novel azabiphenylaminobenzoic acid derivatives, having the chemical formula:, where Ris selected from a group consisting of hydrogen atoms, halogen atoms, C-alkyl, C-cycloalkyl and -CF, Ris selected from a group consisting of hydrogen atoms, halogen atoms and C-alkyl group, Ris -COOR, where Ris selected from a group consisting of a hydrogen atom and linear or branched C-alkyl groups, Ris selected from a group consisting of a hydrogen atom and C-alkyl group; Ris selected from a group consisting of a hydrogen atom and a phenyl group, Gis a group selected from N and CR, where Ris selected from a group consisting of hydrogen atoms, halogen atoms, C-alkyl, C-cycloalkyl, -CPand C-aryl group, Gis a group selected from: - a hydrogen atom, hydroxy group, halogen atom, C-cycloalkyl group, C-alkoxy group and -NRR, where Ris C-alkyl group and Ris selected from a group consisting of C-alkyl group and C-alkoxy-C-alkyl group, or Rand Rtogether with the nitrogen atom with which they are bonded, form a saturated 6-8-member heterocyclic ring optionally containing one oxygen atom as an additional heteroatom, -monocyclic or bicyclic 5-10-member heteroatomatic ring containing one or more nitrogen atoms which are optionally substituted with one or more halogen atoms, and a phenyl group which is optionally substituted with one or more substitutes selected from halogen atoms, C-alkyl, hydroxy group, C-alkoxy group, C-cycloalkyl, C-cycloalkoxy group, cyano group, -CF, -OCF, -CONRR, oxadiazolyl, and where Rand Rare independently selected from a hydrogen atom, a linear or branched C-alkyl group, C-cycloalkyl group, or Rand Rtogether with a nitrogen atom with which they are bonded form a group of formula:, where n equals 0-3; or Gtogether with Rform a non-aromatic C-carbocyclic group or a C-aryl group, and pharmaceutically acceptable and N oxides thereof. Also described are pharmaceutical compositions containing said compounds and use thereof in ...

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22-10-2019 дата публикации

Aryl amine alkyl sulfide class compound of class Ruzadolane structure and preparation method thereof

Номер: CN105541702B
Автор: 原庆贺, 朱其明, 陈烨
Принадлежит: Yichun University

一种类卢扎朵仑结构的芳胺基烷基硫类化合物及其制备方法,该化合物是将Ar 1 ‑X 1 、通式Ⅲ所表示的化合物、Ar 2 ‑X 2 及硫源加入到溶剂中,按反应式(1)加热反应完全后得到;或者是将Ar 1 ‑X 1 、通式Ⅲ所表示的化合物及Ar 2 ‑S ‑ M + 加入到溶剂中,按反应式(2)加热反应完全后得到。本方法操作简单高效,反应条件温和,所用到的试剂廉价易得,安全性强,适于工业化大生产。

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03-02-2016 дата публикации

The preparation method of the fluoro-6-of the chloro-5-of 4-amino-3-(replacement) pyridine-2-manthanoate

Номер: CN103874685B
Принадлежит: DOW AGROSCIENCES LLC

4-氨基-3-氯-5-氟-6-(取代的)吡啶-2-甲酸酯是通过一系列步骤方便地从3,4,5,6-四氯吡啶-2-甲腈制备的,所述步骤包括氟交换、胺化、卤素交换和水解、酯化和过渡金属辅助的偶联。

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20-04-2021 дата публикации

5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group

Номер: KR102242871B1

본 발명은 본원에 기재되고 정의된 바와 같은 화학식 I의 술폭시민 기를 함유하는 5-플루오로-N-(피리딘-2-일)피리딘-2-아민 유도체, 및 그의 제조 방법, 장애, 특히 과다증식성 장애 및/또는 바이러스 유발 감염성 질환 및/또는 심혈관 질환의 치료 및/또는 예방을 위한 그의 용도에 관한 것이다. 본 발명은 또한 화학식 I의 상기 화합물의 제조에 유용한 중간체 화합물에 관한 것이다. The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing sulfoximine groups of formula (I) as described and defined herein, and methods of their preparation, disorders, especially hyperproliferative It relates to its use for the treatment and/or prevention of disorders and/or virus-induced infectious diseases and/or cardiovascular diseases. The invention also relates to intermediate compounds useful in the preparation of the above compounds of formula (I).

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04-12-2013 дата публикации

Arylalkyl esters of 4-amino-6-(substituted phenyl)picolinates and 6-amino-2-(substituted phenyl)-4-pyrimidinecarboxylates and their use as herbicides

Номер: EP2667716A1
Принадлежит: DOW AGROSCIENCES LLC

Arylalkyl esters of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are herbicides for control of weeds especially those species common to rice and wheat cropping systems and in pasture management programs.

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