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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 105. Отображено 105.
08-12-2009 дата публикации

N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide and other modulators of chemokine receptor activity, crystalline forms and process

Номер: US0007629351B2

The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8,R9, R10, and are as described herein. Compounds that are useful intermediates ...

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01-01-2019 дата публикации

Substituted bicyclic compounds

Номер: US0010166249B2

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rcare defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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21-11-2019 дата публикации

TRICYCLIC SULFONE COMPOUND AS A ROR GAMMA MODULATOR

Номер: US20190352261A1
Принадлежит: Bristol Myers Squibb Co

or stereoisomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof. Also provided are pharmaceutical compositions comprising the same. The compound of the invention may be useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

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14-03-2017 дата публикации

Imide and acylurea derivatives as modulators of the glucocorticoid receptor

Номер: US0009593113B2

Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF- K B activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification.

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14-07-2020 дата публикации

Substituted bicyclic compounds

Номер: US0010709719B2

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rcare defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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06-03-2007 дата публикации

Pyridyl-substituted spiro-hydantoin compounds and use thereof

Номер: US0007186727B2

A class of substituted spiro-hydantoin compounds (II) having the formula: its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group, as defined herein, is provided. Pharmaceutical compositions and methods of treating anti-inflammatory and/or immune diseases with the pyridyl-substituted spiro-hydantoin compounds are also objectives of this invention.

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31-01-2008 дата публикации

CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

Номер: US20080027080A1
Принадлежит: Bristol-Myers Squibb Company

This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.

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14-06-2018 дата публикации

PHOSPHINE OXIDE ALKYL AMIDE SUBSTITUTED HETEROARYL COMPOUNDS AS MODULATORS OF IL-12, IL-23, AND/OR IFN ALPHA RESPONSES

Номер: US20180162889A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

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06-07-2006 дата публикации

Pyridyl-substituted spiro-hydantoin compounds and use thereof

Номер: US20060148836A1
Принадлежит:

A class of substituted spiro-hydantoin compounds (II) having the formula: its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group, as defined herein, is provided. Pharmaceutical compositions and methods of treating anti-inflammatory and/or immune diseases with the pyridyl-substituted spiro-hydantoin compounds are also objectives of this invention.

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13-06-2024 дата публикации

SUBSTITUTED HETEROCYCLIC COMPOUNDS

Номер: US20240190829A1
Принадлежит: Bristol Myers Squibb Co

There are disclosed compounds of the following formula I:or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

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04-02-2021 дата публикации

HETEROCYCLIC COMPOUNDS COMPRISING PYRIDINE USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES

Номер: US20210032220A1
Принадлежит:

Compounds having the following formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, where R, R, R, R, and Rare as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. 12. A compound which is{'sup': '2', 'sub': '3', '6-cyclopropaneamido-4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methylpyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', '4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methyl-6-[(pyridin-2-yl)amino]pyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', '6-cyclobutaneamido-4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methylpyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', '4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methyl-6-[2-(morpholin-4-yl)acetamido]pyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', '6-acetamido-4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methylpyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', '6-[(5-fluoropyridin-2-yl)amino]-4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methylpyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', '6-butanamido-4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methylpyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', '4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methyl-6-propanamidopyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', 'methyl N-(5-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-6-[(H)methylcarbamoyl]pyridazin-3-yl)carbamate,'}{'sup': '2', 'sub': '3', '6-(2-cyclopropylacetamido)-4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methylpyridazine-3-carboxamide,'}{'sup': '2', 'sub': '3', '4-{[3-methoxy-4-(1-methyl-1H-1,2,4-triazol-3-yl)pyridin-2-yl]amino}-N—(H)methyl-6-[(4-methylpyridin-2-yl)amino]pyridazine-3-carboxamide,'}{'sup': ' ...

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31-01-2008 дата публикации

MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY CRYSTALLINE FORMS AND PROCESS

Номер: US20080027083A1
Принадлежит: Bristol-Myers Squibb Company

The present invention provides a novel antagonist or partial agonists/antagonists of MCP-1 receptor activity: N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein. Compounds that are ...

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30-06-2016 дата публикации

IMIDE AND ACYLUREA DERIVATIVES AS MODULATORS OF THE GLUCOCORTICOID RECEPTOR

Номер: US20160185776A1
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-B activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification. 4. The compound as defined in claim 3 , or an enantiomer claim 3 , diastereomer claim 3 , tautomer claim 3 , or a pharmaceutically-acceptable salt thereof claim 3 , wherein:{'sub': 11', '1-6', '3-7', '15', '16, 'Rat each occurrence is independently selected from Calkyl, Ccycloalkyl, and —NRR; and'}{'sub': 15', '16', '1-8', '1-8', '1-4', '3-7', '3-7', '15', '16, 'R, and Rare the same or different and at each occurrence are independently selected from (i) hydrogen, Calkyl, substituted Calkyl wherein the substituent is selected from OH and aryl optionally substitute with Calkoxy, Ccycloalkyl, Ccycloalkenyl, aryl, heteroaryl, and heterocyclo; or (ii) where possible, Ris taken together with Rto form a heteroaryl or heterocyclo ring.'}5. A compound as defined in claim 4 , or an enantiomer claim 4 , diastereomer claim 4 , tautomer claim 4 , or a pharmaceutically-acceptable salt thereof claim 4 , wherein:{'sub': 1', '1-6', '12', '12', '13', '12', '12', '12', '13', '12', '13', '2', '14', '12', '2', '14', '1-3, 'Ris phenyl, pyridyl or pyrimidinyl, each of which is substituted with zero to three substituents independently selected from halogen, Chydroxyalkyl, —OR, —NRR, —C(═O)R, —C(═O)OR, —C(═O)NR, R, —NRC(═O)R, —S(O)R, —NRSOR, and 5- to 6-membered heteroaryl substituted with Calkyl group.'}7. The compound as defined in or an enantiomer claim 3 , diastereomer claim 3 , tautomer claim 3 , or a pharmaceutically-acceptable salt thereof claim 3 , wherein:{'sub': 1', '1-6', '12', '12', '13', '12', '12', '12', '13', '12', '13', '2', '14', '12', ...

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14-07-2016 дата публикации

IMIDAZOLE-DERIVED MODULATORS OF THE GLUCOCORTICOID RECEPTOR

Номер: US20160200728A1
Принадлежит: Bristol Myers Squibb Co

Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-kB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification.

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30-03-2010 дата публикации

Cyclic derivatives as modulators of chemokine receptor activity

Номер: US0007687508B2

This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.

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13-07-2021 дата публикации

Substituted bicyclic compounds

Номер: US0011058696B2

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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10-05-2018 дата публикации

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

Номер: US20180127368A1
Принадлежит:

There are described RORγ modulators of the formula (I), 17. A compound selected from the following:1-(4-((3R,3aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carbonyl)piperazin-1-yl)ethan-1-one,(3R,3aS,9bS)—N-((1,1-dioxidotetrahydrothiophen-3-yl)methyl)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide (diastereomeric mixture),methyl 4-((3R,3aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamido)tetrahydro-2H-thiopyran-4-carboxylate 1,1-dioxide,(3R,3 aS,9bS)—N-(2,3-dihydroxy-3-methylbutyl)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-N-(2-hydroxy-2-methylpropyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-N-((1r,4R)-4-hydroxycyclohexyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(1,1-dioxidothiomorpholino)((3R,3aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalen-3-yl)methanone,(3R,3 aS,9bS)-9b-((4-fluorophenyl)sulfonyl)-N—((R)-2-hydroxypropyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS, 9bS)-9b-((4-fluorophenyl)sulfonyl)-N-((1-hydroxycyclopentyl)methyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS, 9bS)-9b-((4-fluorophenyl)sulfonyl)-N-((1-hydroxycyclobutyl)methyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS, 9bS)-9b-((4-fluorophenyl)sulfonyl)-N-((1-hydroxy cyclopropyl)methyl)-7-(perfluoropropan-2-yl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalene-3-carboxamide,(3R,3 aS, ...

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08-10-2019 дата публикации

Tricyclic sulfones as ROR gamma modulators

Номер: US0010435369B2

There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

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01-06-2021 дата публикации

Sulfone pyridine alkyl amide-substituted heteroaryl compounds

Номер: US0011021462B2

Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

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19-08-2021 дата публикации

SULFONE PYRIDINE ALKYL AMIDE-SUBSTITUTED HETEROARYL COMPOUNDS

Номер: US20210253554A1
Принадлежит:

Compounds having the following formula I: 2. The method of wherein the inflammatory or autoimmune disease is psoriasis.3. The method of wherein the inflammatory or autoimmune disease is psoriatic arthritis.4. The method of wherein the inflammatory or autoimmune disease is systemic lupus erythematosus. This application is a divisional application of U.S. patent application Ser. No. 16/195,951, filed Nov. 20, 2018, which claims priority to U.S. Provisional Application Ser. No. 62/589,165, filed Nov. 21, 2017, the contents of which are specifically incorporated fully herein by reference.This invention relates to compounds useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition. Provided herein are amide-substituted heterocyclic compounds, compositions comprising such compounds, and methods of their use. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention that are useful for the treatment of conditions related to the modulation of IL-12, IL-23 and/or IFNα in a mammal.The heterodimeric cytokines interleukin (IL)-12 and IL-23, which share a common p40 subunit, are produced by activated antigen-presenting cells and are critical in the differentiation and proliferation of Th1 and Th17 cells, two effector T cell lineages which play key roles in autoimmunity. IL-23 is composed of the p40 subunit along with a unique p19 subunit. IL-23, acting through a heterodimeric receptor composed of IL-23R and IL-12Rβ1, is essential for the survival and expansion of Th17 cells which produce pro-inflammatory cytokines such as IL-17A, IL-17F, IL-6 and TNF-α (McGeachy, M. J. et al., “The link between IL-23 and Th17 cell-mediated immune pathologies”, 19:372-376 (2007)). These cytokines are critical in mediating the pathobiology of a number of autoimmune diseases, including rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease, and lupus. IL-12, in ...

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31-01-2008 дата публикации

MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY CRYSTALLINE FORMS AND PROCESS

Номер: US20080027084A1
Принадлежит: Bristol-Myers Squibb Company

The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4 -ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein. Compounds that are useful intermediates ...

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23-05-2019 дата публикации

SULFONE PYRIDINE ALKYL AMIDE-SUBSTITUTED HETEROARYL COMPOUNDS

Номер: US20190152948A1
Принадлежит:

Compounds having the following formula I: 11. A compound which is{'sup': '2', 'sub': '3', '6-cyclopropaneamido-4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '6-[(5-fluoropyridin-2-yl)amino]-4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '4-[(3-methanesulfonylpyridin-2-yl)amino]-6-[(6-methoxypyridazin-3-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methyl-6-[(1-methyl-1H-pyrazol-3-yl)amino]pyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '6-[(6-cyclopropyl-2-methylpyrimidin-4-yl)amino]-4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '6-{[5-(2-hydroxypropan-2-yl)pyridin-2-yl]amino}-4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '6-[(6-cyclopropylpyrimidin-4-yl)amino]-4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '6-[(6-cyclopropylpyridazin-3-yl)amino]-4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '6-[(1,5-dimethyl-1H-pyrazol-3-yl)amino]-4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methyl-6-{[5-(trifluoromethyl)pyridin-2-yl]amino}pyridine-3-carboxamide;'}{'sup': '2', 'sub': '3', '4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methyl-6-{[6-(trifluoromethyl)pyridazin-3-yl]amino}pyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '4-[(3-methanesulfonylpyridin-2-yl)amino]-6-[(2-methoxypyrimidin-4-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '6-{[5-fluoro-4-(2-hydroxypropan-2-yl)pyridin-2-yl]amino}-4-[(3-methanesulfonylpyridin-2-yl)amino]-N-(H)methylpyridazine-3-carboxamide;'}{'sup': '2', 'sub': '3', '6-{[5-(2-aminopropan-2-yl) ...

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20-12-2016 дата публикации

Substituted bicyclic compounds

Номер: US0009522888B2

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R 1 is —OH or —OP(O)(OH) 2 , and X 1 , X 2 , X 3 , R 2 , R 2a , R a , R b , and R c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P 1 , and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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24-10-2017 дата публикации

Imidazole-derived modulators of the glucocorticoid receptor

Номер: US0009796720B2

Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification.

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10-09-2020 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20200281952A1
Принадлежит:

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

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21-04-2022 дата публикации

TRIAZOLOPYRIDINYL COMPOUNDS AS KINASE INHIBITORS

Номер: US20220119388A1
Принадлежит: Bristol Myers Squibb Co

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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06-05-2010 дата публикации

MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS

Номер: US20100113489A1
Принадлежит: Bristol-Myers Squibb Company

The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin- 4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein. Compounds that are useful intermediates ...

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26-09-2017 дата публикации

Substituted bicyclic compounds

Номер: US0009770459B2

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R 1 is —OH or —OP(O)(OH) 2 , and X 1 , X 2 , X 3 , R 2 , R 2a , R a , R b , and R c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P 1 , and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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04-04-2024 дата публикации

TRIAZOLOPYRIDINYL COMPOUNDS AS KINASE INHIBITORS

Номер: US20240109888A1
Принадлежит: Bristol Myers Squibb Co

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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21-05-2019 дата публикации

Phosphine oxide alkyl amide substituted heteroaryl compounds as modulators of IL-12, IL-23 and/or IFN alpha responses

Номер: US0010294256B2

Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

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16-02-2017 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20170042917A1
Принадлежит:

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): 111-. (canceled)13. The method according to wherein said autoimmune disease or chronic inflammatory disease is selected from systemic lupus erythematosis claim 12 , multiple sclerosis claim 12 , inflammatory bowel disease claim 12 , ulcerative colitis claim 12 , Crohn's disease claim 12 , rheumatoid arthritis claim 12 , scleroderma claim 12 , giant cell arteritis claim 12 , and Sjögren's syndrome.17. The method according to wherein said autoimmune disease or chronic inflammatory disease is systemic lupus erythematosis.18. The method according to wherein said autoimmune disease or chronic inflammatory disease is ulcerative colitis.19. The method according to wherein said autoimmune disease or chronic inflammatory disease is multiple sclerosis.20. The method according to wherein said autoimmune disease or chronic inflammatory disease is inflammatory bowel disease.21. The method according to wherein said autoimmune disease or chronic inflammatory disease is rheumatoid arthritis.22. The method according to wherein said autoimmune disease or chronic inflammatory disease is Crohn's disease.23. The method according to wherein said autoimmune disease or chronic inflammatory disease is Sjögren's syndrome.24. The method according to wherein said autoimmune disease or chronic inflammatory disease is systemic lupus erythematosis.25. The method according to wherein said autoimmune disease or chronic inflammatory disease is ulcerative colitis.26. The method according to wherein said autoimmune disease or chronic inflammatory disease is multiple sclerosis.27. The method according to wherein said autoimmune disease or chronic inflammatory disease is inflammatory bowel disease.28. The method according to wherein said autoimmune disease or chronic inflammatory disease is rheumatoid arthritis.29. The method according to wherein said autoimmune disease or chronic inflammatory disease is Crohn's disease.30. The method ...

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14-03-2019 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20190076450A1
Принадлежит:

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

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28-04-2020 дата публикации

Tricyclic sulfone compound as a ROR gamma modulator

Номер: US0010633339B2

There is described a RORγ modulator of the formula (I), or stereoisomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof. Also provided are pharmaceutical compositions comprising the same. The compound of the invention may be useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

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26-10-2017 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20170304332A1
Принадлежит:

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

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25-02-2016 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20160052888A1
Принадлежит:

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

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29-12-2022 дата публикации

SUBSTITUTED HETEROCYCLIC COMPOUNDS

Номер: US20220411384A1
Принадлежит:

There are disclosed compounds of the following formula I: 6. A compound or a pharmaceutically acceptable salt thereof , selected from{'sup': '2', '6-cyclopropaneamido-4-{[3-(2-ethyl-2H-1,2,3-triazol-4-yl)-2-methoxyphenyl]amino}-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '4-{[2-methoxy-3-(2-methyl-2H-1,2,3-triazol-4-yl)phenyl]amino}-6-[(6-methoxypyridazin-3-yl)amino]-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '6-cyclopropaneamido-4-{[5-fluoro-2-methoxy-3-(2-methyl-2H-1,2,3-triazol-4-yl)phenyl]amino}-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '4-{[2-methoxy-3-(2-methyl-2H-1,2,3-triazol-4-yl)phenyl]amino}-N-(H3)methyl-6-[(pyridin-2-yl)amino]pyridazine-3-carboxamide,'}{'sup': '2', 'methyl N-(5-{[2-methoxy-3-(2-methyl-2H-1,2,3-triazol-4-yl)phenyl]amino}-6-[(H3)methylcarbamoyl]pyridazin-3-yl)carbamate,'}{'sup': '2', '6-[(1,5-dimethyl-1H-pyrazol-3-yl)amino]-4-{[2-methoxy-3-(2-methyl-2H-1,2,3-triazol-4-yl)phenyl]amino}-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '4-{[2-methoxy-3-(2-methyl-2H-1,2,3-triazol-4-yl)phenyl]amino}-N-(H3)methyl-6-[(1R)-spiro[2.2]pentane-1-amido]pyridazine-3-carboxamide,'}{'sup': '2', '6-cyclopropaneamido-4-{[3-(2-cyclopropyl-2H-1,2,3-triazol-4-yl)-2-methoxyphenyl]amino}-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '6-cyclopropaneamido-4-{[3-(2-cyclopropyl-2H-1,2,3-triazol-4-yl)-5-fluoro-2-methoxyphenyl]amino}-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '6-cyclopropaneamido-4-{[3-(2-ethyl-2H-1,2,3-triazol-4-yl)-4-fluoro-2-methoxyphenyl]amino}-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '6-cyclopropaneamido-4-{[4-(2-cyclopropyl-2H-1,2,3-triazol-4-yl)-3-methoxypyridin-2-yl]amino}-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '6-cyclopropaneamido-4-({3-[2-(2-fluoroethyl)-2H-1,2,3-triazol-4-yl]-2-methoxyphenyl}amino)-N-(H3)methylpyridazine-3-carboxamide,'}{'sup': '2', '6-cyclopropaneamido-4-({3-[2-(2,2-difluoroethyl)-2H-1,2,3-triazol-4-yl]-2-methoxyphenyl}amino)-N-(H3)methylpyridazine-3- ...

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09-06-2017 дата публикации

Substituted bicyclic compounds

Номер: CO2017002312A2
Принадлежит: Bristol Myers Squibb Co

Compuestos de las Fórmulas (I), (II), (III), (IV) y (V), y/o una sal de estos, en donde R1 es -OH u -OP(O)(OH)2, y X1, X2, X3, R2, R2a, Ra, Rb y Rc se definen en la presente. También se describen métodos para usar estos compuestos como agonistas selectivos del receptor S1P1 acoplado a la proteína G, y composiciones farmacéuticas que comprenden estos compuestos. Estos compuestos son útiles para el tratamiento, la prevención o la ralentización de la progresión de enfermedades o trastornos en varias áreas terapéuticas, tales como enfermedades autoinmunitarias y vasculares. Compounds of Formulas (I), (II), (III), (IV) and (V), and / or a salt thereof, wherein R1 is -OH or -OP (O) (OH) 2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also described are methods of using these compounds as selective agonists of the S1P1 receptor coupled to the G protein, and pharmaceutical compositions comprising these compounds. These compounds are useful for treating, preventing, or slowing the progression of diseases or disorders in various therapeutic areas, such as autoimmune and vascular diseases.

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31-01-2008 дата публикации

Modulators of chemokine receptor activity, crystalline forms and process

Номер: CA2831219A1
Принадлежит: Bristol Myers Squibb Co

The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: (see formula I) wherein R1, R8, R9, R10, and (see formula II) are as described herein. Compounds that are useful intermediates of the process are also provided herein.

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10-09-2020 дата публикации

Imidazopyridazine compounds useful as modulators of il-12, il-23 and/or ifn alpha responses

Номер: WO2020180907A1
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

Compounds having the following formula I: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.

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06-08-2020 дата публикации

Amide-disubstituted pyridine or pyridazine compounds

Номер: CA3128014A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula (I): (Formula (I)) or a stereoisomer or pharmaceutically-acceptable salt thereof, are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition.

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08-10-2010 дата публикации

CYCLE DERIVATIVES AS MODULATORS OF THE ACTIVITY OF THE CHEMIOQUINE RECEIVER.

Номер: ES2346100T3
Принадлежит: Bristol Myers Squibb Co

Un compuesto seleccionado de: (i)N-((1R,2S,5R)-2-((3S)-3-((6-terc-butilpirimido[5,4-d]pirimidin-4-il)amino)-2-oxo-1-pirrolidinil)-5-(isopropil(metil)amino)ciclohexil)acetamida; N-((1R,2S,5R)-5-(metilamino)-2-((3S)-2-oxo-3-((6-(trifluorometil)-4-quinazolinil)amino)-1-pirrolidinil)ciclohexil)acetamida; N-((1R,2S,5R)-5-(isopropil(metil)amino)-2-((3S)-2-oxo-3-((6-(trifluorometil)-4-quinazolinil)amino)-1-pirrolidinil)ciclohexil)formamida; N-((1R,2S,5R)-5-(dimetilamino)-2-((3S)-2-oxo-3-((6-(trifluorometil)-4-quinazolinil)amino)-1-pirrolidinil)ciclohexil)acetamida; N-((3S)-1-((1S,2R,4R)-2-acetamido-4-(isopropil(metil)amino)ciclohexil)-2-oxo-3-pirrolidinil)-6-terc-butil-2-piridincarboxamida; N-((1R,2S,5R)-5-amino-2-((3S)-2-oxo-3-((6-(trifluorometil)-4-quinazolinil)amino)-1-pirrolidinil)ciclohexil)propanamida; 2-terc-butil-N-((3S)-1-((1S,2R,4R)-4-(terc-butilamino)-2-(metanosulfonilamino)ciclohexil)-2-oxo-3-pirrolidinil)-4-pirimidincarboxamida; 2-terc-butil-N-((3S)-1-((1S,2R,4R)-4-(terc-butilamino)-2-(propionilamino)ciclohexil)-2-oxo-3-pirrolidinil)-4-pirimidincarboxamida; N-((1R,2S,5R)-5-(terc-butilamino)-2-((3S)-3-((6-terc-butilpirimido[5,4-d]pirimidin-4-il)amino)-2-oxo-1-pirrolidinil)ciclohexil)metanosulfonamida; y N-(((1S,2S,5R)-5-metoxi-2-((3S)-2-oxo-3-((6-(trifluorometil)-4-quinazolinil)amino)-1-pirrolidinil)ciclohexil)metil)acetamida; N-(((1R,2S,5R)-5-(isopropilamino)-2-((3S)-2-oxo-3-((6-(trifluorometil)-4-quinazolinil)amino)-1-pirrolidinil)ciclohexil)acetamida; N-((1R,2S,5R)-5-amino-2-((3S)-2-oxo-3-((6-(trifluorometil)-4-quinazolinil)amino)-1-pirrolidinil)ciclohexil)acetamida; N-((1R,2S,5R)-5-(isopropilo(metil)amino)-2-((3S)-2-oxo-3-((1-oxido-6-(trifluorometil)-4-quinazolinil)amino)-2-oxo-1-pirrolidinil)ciclohexil)acetamida; N-((1R,2S,5R)-5-(isopropilamino)-2-((3S)-3-((1-oxido-6-(trifluorometil)-4-quinazolinil)amino)-2-oxo-1-pirrolidinil)ciclohexil)acetamida; y N-((1R,2S,5R)-5-(terc-butilamino)-2-((3S)-3-((1-oxido-6-(trifluorometil)-4-quinazolinil)amino-2-oxo-1- ...

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24-08-2021 дата публикации

Amide-disubstituted pyridine or pyridazine compounds.

Номер: MX2021008752A
Принадлежит: Bristol Myers Squibb Co

Compuestos que tienen la siguiente fórmula (I): (Fórmula (I) o un estereoisómero o una sal farmacéuticamente aceptable del mismo, son útiles en la modulación de IL-12, IL-23 y/o IFNa, actuando sobre Tyk-2 para provocar la inhibición de la transducción de señales. (ver Fórmula).

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30-10-2017 дата публикации

Substituted bicyclic compounds

Номер: CL2017000382A1
Принадлежит: Bristol Myers Squibb Co

<p>COMPUESTOS DE LAS FORMULAS (I), (II), (III), (IV) Y (V):</p> <p>* incluir figuras de estructuras de hoja resumen de fecha 15-02-2017, pagina 4</p> <p>Y/O UNA SAL DE ESTOS, EN DONDE R1 ES -OH U OP(O)(OH)2, Y X1, X2, X3, R2, R2A, RA, RB Y RC SE DEFINEN EN LA PRESENTE. TAMBIÉN SE DESCRIBEN MÉTODOS PARA USAR ESTOS COMPUESTOS COMO AGONISTAS SELECTIVOS DEL RECEPTOR S1P1 ACOPLADO A LA PROTEÍNA G, Y COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN ESTOS COMPUESTOS. ESTOS COMPUESTOS SON ÚTILES PARA EL TRATAMIENTO, LA PREVENCIÓN O LA RALENTIZACIÓN DE LA PROGRESIÓN DE ENFERMEDADES O TRASTORNOS EN VARIAS ÁREAS TERAPÉUTICAS, TALES COMO ENFERMEDADES AUTOINMUNITARIAS Y VASCULARES.</p> <p> COMPOUNDS OF FORMULAS (I), (II), (III), (IV) AND (V): </p> <p> * include figures of summary sheet structures dated 15-02-2017, page 4 </p> <p> AND / OR A SALT OF THESE, WHERE R1 IS -OH OR OP (O) (OH) 2, Y X1, X2, X3, R2, R2A, RA, RB AND RC SE DEFINED IN THIS. METHODS ARE ALSO DESCRIBED FOR USING THESE COMPOUNDS AS SELECTIVE AGONISTS OF THE S1P1 RECEPTOR COUPLED TO PROTEIN G, AND PHARMACEUTICAL COMPOSITIONS THAT UNDERSTAND THESE COMPOUNDS. THESE COMPOUNDS ARE USEFUL FOR THE TREATMENT, PREVENTION OR REALENTIZATION OF THE PROGRESSION OF DISEASES OR DISORDERS IN VARIOUS THERAPEUTIC AREAS, SUCH AS AUTOIMMUNITY AND VASCULAR DISEASES. </p>

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07-03-2023 дата публикации

Heterocyclic compounds comprising pyridine useful as modulators of IL-12, IL-23 and/or IFNα responses

Номер: US11597721B2
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, where R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

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15-10-2021 дата публикации

Substituted bicyclic compounds

Номер: HRP20211121T1
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

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27-09-2011 дата публикации

MODULATORS OF THE ACTIVITY OF THE CHEMIOKIN RECEPTOR, CRYSTAL FORMS AND PROCEDURES.

Номер: ES2365264T3
Принадлежит: Bristol Myers Squibb Co

- Un compuesto que es N-((1R,2S,5R)-5-(terc-butilamino)-2-((S)-2-oxo-3-(6-(trifluorometil)quinazolin-4- ilamino)pirrolidin-1-il)ciclohexil)acetamida, o una sal farmacéuticamente aceptable del mismo. - A compound that is N - ((1R, 2S, 5R) -5- (tert-butylamino) -2 - ((S) -2-oxo-3- (6- (trifluoromethyl) quinazolin-4-ylamino) pyrrolidine -1-yl) cyclohexyl) acetamide, or a pharmaceutically acceptable salt thereof.

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31-05-2019 дата публикации

Sulfone pyridine alkyl amide-substituted heteroaryl compounds

Номер: CA3083122A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula (I), or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition.

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26-02-2010 дата публикации

Modulators of chemokine receptor activity, crystalline forms and process

Номер: SG158925A1
Принадлежит: Bristol Myers Squibb Co

The present invention provides a novel antagonist or partial agonists,antagonists of MCP-1 receptor activity: N-((lR,2S,5R)-5- (isopropyl(methyl)amino)-2-((S)-2-0x0-3-(6- (trifluoromethyl)quinazolin-4- ylamino)pyrrolidin-1- yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3- (6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and structure (a) are as described herein. Compounds that are useful intermediates of the process are also provided herein.

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29-01-2009 дата публикации

Modulators of chemokine receptor activity, crystalline forms and process.

Номер: MX2009000803A
Принадлежит: Squibb Bristol Myers Co

La presente invención proporciona un antagonista o agonistas/antagonistas parciales novedosos de la actividad del receptor MCP-1: N-((1R,2S,5R)-5-(isopropil(metil)amino)-2-((S)-2-o xo-3-(6-(trifluorometil)quinazolin-4-ilamino)pirrolidin-1-il)cicl ohexil)acetamida, o una sal, solvato o profármaco farmacéuticamente aceptable, de los mismos, que tienen una combinación inesperada de características farmacológicas deseables. También se proporcionan formas cristalinas de la presente invención. Las composiciones farmacéuticas que contienen los mismos y los métodos de uso de las mismas como agentes para el tratamiento de enfermedades inflamatorias, enfermedades alérgicas, autoinmunitarias metabólicas, cáncer y/o cardiovasculares también es un objetivo de esta invención. La presente descripción también proporciona un proceso para preparar los compuestos de la fórmula (I), incluyendo la N-((1R,2S,5R)-5-(isopropil(metil)amino)-2-((S)-2-oxo-3-(6-(triflu orometil)quinazolin-4-ilamino)pirrolidin-1-il)ciclohexil)acetamid a: en donde R1, R8, R9, R10 y la estructura (a) son como se describen en la presente. Los compuestos que son intermediarios útiles del proceso también se proporcionan en la presente.

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10-07-2017 дата публикации

Substituted bicyclic compounds

Номер: PH12017500261A1
Принадлежит: Bristol Myers Squibb Co

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V) and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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29-01-2009 дата публикации

Modulators of chemokine receptor activity, crystalline forms and process.

Номер: MX2009000808A
Принадлежит: Squibb Bristol Myers Co

La presente invención proporciona un antagonistas novedoso o agonista parcial/antagonista del receptor de la actividad de MCP-1; N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-2-oxo-3-(6-(triflu orometil)quinazolin-4-ilamino)pirrolidin-1-il)ciclohexil)acetamid a, o una sal, solvato o profármaco farmacéuticamente aceptable, de los mismos que tiene una combinación inesperada de características farmacológicas deseables. Las formas cristalinas de la presente invención también se proporcionan. Las composiciones farmacéuticas contienen los mismos y los métodos de uso de los mismos como agente para el tratamiento de enfermedades inflamatorias, enfermedades alérgicas, autoinmunes, metabólicos, cáncer y/o cardiovascular también es un objetivo de esta invención. La presente descripción también proporciona un proceso para preparar los compuestos de la fórmula (I), incluyendo N-((1R,S2,5R)-5-(tert-butilamino)-2-((S)-2-oxo-3-(6-(trifluoromet il)quinazolin-4-ilamino)pirrolidin-1-il)ciclohexil)acetamida: (ver fórmula (I)) en donde R1, R8, R9, R10 y HET son como se describen en la presente. Los compuestos que son intermediarios útiles de los procesos también se proporcionan en la presente.

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11-07-2023 дата публикации

Sulfonepyridine alkylamide-substituted heteroaryl compounds

Номер: JP2023098942A
Принадлежит: Bristol Myers Squibb Co

【課題】対象における乾癬を治療するための経口医薬組成物を提供する。【解決手段】下式:TIFF2023098942000149.tif4158で示される化合物を含む、経口医薬組成物とする。【選択図】なし

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29-01-2009 дата публикации

Modulators of chemokine receptor activity, crystalline forms and processes

Номер: NO20090190L
Принадлежит: Bristol Myers Squibb Co

Foreliggende oppfinnelse tilveiebringer en ny antagonist eller partielle agonister/antagonist av MCP-1 reseptor aktivitet: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-okso-3-(6-(trifluormetyl)kinazolin-4-ylamino)pyrrolidin-1-yl)cykloheksyl)acetamid eller et farmasøytisk akseptabelt salt, solvat eller prodroge, derav, som har en uventet kombinasjon av ønskelige farmakologiske karakteristika. Krystallinske former ifølge foreliggende oppfinnelse er også gitt. Farmasøytiske preparater inneholdende disse og metoder for anvendelse av disse som midler for behandling av inflammatoriske sykdommer, allergiske sykdommer, autoimmune sykdommer, metabolske sykdommer, kreft og/eller kardiovaskulære sykdommer er også en hensikt ifølge foreliggende oppfinnelse. Foreliggende beskrivelse tilveiebringer også en fremgangsmåte for fremstilling av forbindelser med formel (I), omfattende N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-okso-3-(6-(trifluormetyl)kinazolin-4-ylamino)pyrrolidin-1-yl)cykloheksyl)acetamid: hvor R1, R8, R9, R10 og er som beskrevet her. Forbindelser som er anvendelige mellomprodukter av fremgangsmåten er også gitt her. 1

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17-05-2018 дата публикации

Tricyclic sulfones as ror gamma modulators

Номер: CA3042877A1
Принадлежит: Bristol Myers Squibb Co

There are described ROR? Gamma modulators of the formula (I), (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders.

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08-05-2023 дата публикации

Triazolopyridinyl compounds as kinase inhibitors

Номер: CO2023004926A2
Принадлежит: Bristol Myers Squibb Co

Compuestos que tienen la Fórmula (I) y enantiómeros y diastereómeros, estereoisómeros, sales farmacéuticamente aceptables de los mismos, (I) son útiles como moduladores de quinasas, incluida la modulación RIPK1. Todas las variables son como se definen en el presente documento. Compounds having Formula (I) and enantiomers and diastereomers, stereoisomers, pharmaceutically acceptable salts thereof, (I) are useful as kinase modulators, including RIPK1 modulation. All variables are as defined in this document.

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20-03-2024 дата публикации

Substituted heterocyclic compounds

Номер: EP4337649A1
Принадлежит: Bristol Myers Squibb Co

There are disclosed compounds of the following formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

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30-01-2024 дата публикации

Compostos heterocíclicos substituídos

Номер: BR112023023425A2
Принадлежит: Bristol Myers Squibb Co

compostos heterocíclicos substituídos. a presente invenção refere-se a compostos da fórmula (i) que segue ou um estereoisômero ou sal farmaceuticamente aceitável dos mesmos, em que todos os substituintes são como definidos na presente invenção, que são úteis na modulação de il-12, il-23 e/ou ifna, através da ação sobre tyk-2 para causar inibição de transdução de sinal. os compostos da invenção podem ser úteis para tratamento de doenças ou distúrbios neurodegenerativos.

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17-10-2023 дата публикации

Sulfone pyridine alkyl amide-substituted heteroaryl compounds

Номер: US11787779B2
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula I:or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

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04-01-2024 дата публикации

Substituted heterocyclic compounds

Номер: AU2022271794A1
Принадлежит: Bristol Myers Squibb Co

There are disclosed compounds of the following formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

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16-11-2023 дата публикации

Sulfone pyridine alkyl amide-substituted heteroaryl compounds

Номер: AU2023255024A1
Принадлежит: Bristol Myers Squibb Co

SULFONE PYRIDINE ALKYL AMIDE-SUBSTITUTED HETEROARYL COMPOUNDS ABSTRACT 5 Compounds having the following formula I: R 4 R 3 0 'N' N H | N N R5 or a stereoisomer or pharmaceutically-acceptable salt thereof, where R', R2, R3 , R4, and 10 R 5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition. - 171-

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04-01-2024 дата публикации

Sulfone pyridine alkyl amide-substituted heteroaryl compounds

Номер: US20240002364A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula I:or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

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16-02-2024 дата публикации

Compuestos de triazolopiridinilo como inhibidores de quinasas

Номер: PE20240219A1
Принадлежит: Bristol Myers Squibb Co

La presente invencion se refiere a un compuesto derivado de triazolopiridinilo de formula (I), o una sal del mismo; en donde R1 es H, alquilo C1-3, alcoxilo C1-3, entre otros; R2 es H o halo; R3 es H, halo o alquiloC1-3 o deuteroalquiloC1-3; R4 es H o F; R5a y R5b son cada uno independientemente H, deuterio, alquiloC1-3 o haloalquiloC1-3 alternativamente; R6a y R6b son cada uno independientemente H, deuterio, OH, F, entre otros; R7a y R7b son cada uno independientemente H, deuterio, OH, OP(O)(OR)2, entre otros; R es H o alquiloC1-3; R8 es H, F, Cl, alquiloC1-3, entre otros; R9 es H o CH3; el anillo Z es fenilo, un anillo heteroarilo de 6 miembros, ciclohexilo, ciclopentilo o ciclobutilo; Y es F, Cl, alquiloC1-3, alcoxiC1-3, entre otros; n es 0 a 3. Un compuesto seleccionado es (S)-5-(2-amino-[1,2,4]triazolo[1,5-?]piridin-7-il)-N-(3-(4-clorofenil)-3-hidroxipropil)-4-fluoro-2-metilbenzamida. Dichos compuestos son inhibidores de quinasas, incluida la modulacion de la actividad de RIPK1. Tambien se refiere a una composicion farmaceutica que comprende dicho compuesto, siendo util en el tratamiento de enfermedades inflamatorias, isquemias, neurodegeneracion y enfermedad de Gaucher.

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22-08-2023 дата публикации

Compostos bicíclicos substituídos, uso dos mesmos e composição farmacêutica

Номер: BR112017002641B1
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

COMPOSTOS BICÍCLICOS SUBSTITUÍDOS. São descritos compostos de fórmulas (I), (II), (III), (IV), e (V): e/ou um sal do mesmo, em que R1 é -OH ou -OP(O)(OH)2, e X1, X2, X3, R2, R2a, Ra, Rb, e Rc são definidos aqui. São também descritos méto-dos de uso de tais compostos como agonistas seletivos para receptor S1P1 de proteína G, e composições farmacêuticas compreendendo tais compostos. Estes compostos são úteis no tratamento, prevenção, ou retardo da progressão de doenças ou distúrbios em uma variedade de áreas terapêuticas, tais como doenças autoimunes e doença vascular.

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22-07-2022 дата публикации

Υποκατεστημενες δικυκλικες ενωσεις

Номер: CY1124355T1
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

Αποκαλύπτονται ενώσεις των Τύπων (Ι), (II), (III), (IV), και (V) ή/και άλας αυτών, όπου το R1 είναι ΟΗ ή ΟΡ{Ο)(ΟΗ)2, και τα Χ1, Χ2, Χ3, R2, R2a, Ra, Rb, και Rc ορίζονται στο παρόν. Επίσης αποκαλύπτονται μέθοδοι χρήσης τέτοιων ενώσεων ως εκλεκτικών αγωνιστών για συνδεδεμένο με G πρωτεΐνη υποδοχέα S1Ρ1, και φαρμακευτικές συνθέσεις που περιλαμβάνουν τέτοιες ενώσεις. Αυτές οι ενώσεις είναι χρήσιμες στη θεραπεία, αποτροπή, ή επιβράδυνση της εξέλιξης ασθενειών ή διαταραχών σε μία ποικιλία θεραπευτικών περιοχών, όπως αυτοάνοσων ασθενειών και αγγειακής ασθένειας.

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23-02-2024 дата публикации

Substituted bicyclic compounds

Номер: NZ730160A
Принадлежит: Bristol Myers Squibb Co

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V) and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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24-03-2021 дата публикации

Tricyclic sulfone compound as a ror gamma modulator

Номер: EP3793978A1
Принадлежит: Bristol Myers Squibb Co

There is described a RORγ modulator of the formula (I), or stereoisomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof. Also provided are pharmaceutical compositions comprising the same. The compound of the invention may be useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

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02-05-2024 дата публикации

Triazolopyridinyl compounds as kinase inhibitors

Номер: AU2021364302A9
Принадлежит: Bristol Myers Squibb Co

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,Formula (I): are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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08-05-2024 дата публикации

Triazolopyridinyl compounds as kinase inhibitors

Номер: EP4364737A2
Принадлежит: Bristol Myers Squibb Co

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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10-05-2023 дата публикации

Compuestos de triazolopiridinilo como inhibidores de cinasas.

Номер: MX2023004492A
Принадлежит: Bristol Myers Squibb Co

La presente invención se refiere a compuestos que tienen la Fórmula (I) y enantiómeros y diastereómeros, estereoisómeros, sales farmacéuticamente aceptables de los mismos, (ver Fórmula) (I) son útiles como moduladores de cinasas, incluida la modulación de RIPK1. Todas las variables son como se definen en el presente documento.

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22-09-2023 дата публикации

Compuestos de triazolopiridinilo como inhibidores de quinasas

Номер: CL2023001123A1
Принадлежит: Bristol Myers Squibb Co

Compuestos que tienen la Fórmula (I) y enantiómeros y diastereómeros, estereoisómeros, sales farmacéuticamente aceptables de los mismos, son útiles como moduladores de quinasas, incluida la modulación RIPK1. Todas las variables son como se definen en el presente documento.

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26-04-2024 дата публикации

Compuestos heterocíclicos sustituidos

Номер: CL2023003308A1
Принадлежит: Bristol Myers Squibb Co

Se describen compuestos de la siguiente fórmula I: o un estereoisómero o sal farmacéuticamente aceptable del mismo, en donde todos los sustituyentes son como se definen aquí, que son útiles en la modulación de IL-12, IL-23 y/o IFN-alfa, actuando sobre Tyk-2 para provocar la inhibición de la transducción de señales. Los compuestos de la invención pueden ser útiles para tratar enfermedades o trastornos neurodegenerativos.

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14-12-2023 дата публикации

Compuestos heterociclicos sustituidos.

Номер: MX2023013445A
Принадлежит: Bristol Myers Squibb Co

La presente invención se refiere a compuestos de la siguiente fórmula I: (ver Fórmula) I o un estereoisómero o sal farmacéuticamente aceptable del mismo, en donde todos los sustituyentes son como se definen aquí, que son útiles en la modulación de IL-12, IL-23 y/o IFNa, actuando sobre Tyk-2 para provocar la inhibición de la transducción de señales. Los compuestos de la invención pueden ser útiles para tratar enfermedades o trastornos neurodegenerativos.

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23-10-2019 дата публикации

Phosphine oxide alkyl amide substituted heteroaryl compounds as modulators of il-12, il-23, and/or ifn alpha responses

Номер: EP3555111A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

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20-11-2023 дата публикации

Compuestos heterocíclicos sustituidos

Номер: CO2023015226A2
Принадлежит: Bristol Myers Squibb Co

Se describen compuestos de la siguiente fórmula I: I o un estereoisómero o sal farmacéuticamente aceptable del mismo, en donde todos los sustituyentes son como se definen aquí, que son útiles en la modulación de IL-12, IL-23 y/o IFNα, actuando sobre Tyk-2 para provocar la inhibición de la transducción de señales. Los compuestos de la invención pueden ser útiles para tratar enfermedades o trastornos neurodegenerativos.

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17-11-2022 дата публикации

Substituted heterocyclic compounds

Номер: CA3217332A1
Принадлежит: Bristol Myers Squibb Co

There are disclosed compounds of the following formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

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20-03-2024 дата публикации

Substituted heterocyclic compounds

Номер: EP4337655A1
Принадлежит: Bristol Myers Squibb Co

There are disclosed compounds of the following formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

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09-01-2024 дата публикации

Substituted heterocyclic compounds

Номер: US11866414B2
Принадлежит: Bristol Myers Squibb Co

There are disclosed compounds of the following formula I: or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

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22-06-2023 дата публикации

Triazolopyridinyl compounds as kinase inhibitors

Номер: AU2021364302A1
Принадлежит: Bristol Myers Squibb Co

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,Formula (I): are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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26-09-2023 дата публикации

Triazolopyridinyl compounds as kinase inhibitors

Номер: US11767322B2
Принадлежит: Bristol Myers Squibb Co

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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07-08-2024 дата публикации

Triazolopyridinyl compounds as kinase inhibitors

Номер: EP4364737A3
Принадлежит: Bristol Myers Squibb Co

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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26-09-2024 дата публикации

Substituted heterocyclic compounds

Номер: US20240317718A1
Принадлежит: Bristol Myers Squibb Co

There are disclosed compounds of the following formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

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26-09-2024 дата публикации

Sulfone pyridine alkyl amide-substituted heteroaryl compounds

Номер: AU2018371010C1
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula (I), or a stereoisomer or pharmaceutically-acceptable salt thereof, where R

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08-10-2024 дата публикации

Triazolopyridinyl compounds as kinase inhibitors

Номер: US12110290B2
Принадлежит: Bristol Myers Squibb Co

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.

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19-09-2024 дата публикации

Method, device, medium and apparatus for controlling running of gantry

Номер: WO2024187319A1
Автор: Jian Xu, Jie LING, Zili Xiao

The present invention provides a method, a device, a medium and an apparatus for controlling running of a gantry. The method comprises: determining road information at the current moment(Sl 10); controlling running of the gantry according to a predicted value of a state parameter at the current moment predicted at the previous moment and the road information at the current moment(S120); determining an actual value of the state parameter at the current moment(S130); calculating a difference value between the predicted value of the state parameter at the current moment predicted at the previous moment and the actual value of the state parameter at the current moment, and using the difference value as a feedback value corresponding to the current moment(S140); and determining a predicted value of the state parameter at the next moment, according to the feedback value corresponding to the current moment and the actual value of the state parameter at the current moment, to control running of the gantry at the next moment according to the predicted value of the state parameter at the next moment(S150). With the present invention, it is possible to improve the rectification precision during running of the gantry.

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