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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 96. Отображено 96.
28-07-2016 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATEMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20160213666A1
Принадлежит:

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of the compound or pharmaceutically acceptable salt thereof claim 1 , according to .3. The pharmaceutical composition of claim 2 , wherein the carrier is selected from a parenteral carrier claim 2 , an oral carrier and a topical carrier.4. The pharmaceutical composition according to comprising a further therapeutic agent.5. A method for the treatment claim 1 , or prophylaxis of allergy claim 1 , inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplant rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or interferons claim 1 , comprising administering an amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 , sufficient to effect said treatment claim 1 , or prophylaxis.6. The method according to claim 5 , wherein the compound or pharmaceutically acceptable salt thereof claim 5 , is administered in combination with a further therapeutic agent.7. A method for the treatment ...

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13-10-2016 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20160296530A1
Принадлежит:

A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound according .3. The pharmaceutical composition according to comprising a further therapeutic agent.4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A method for the treatment claim 1 , prevention or prophylaxis of inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 claim 1 , comprising administering an amount of a compound of claim 1 , sufficient to effect said treatment claim 1 , prevention or prophylaxis.9. The method according to claim 8 , wherein the said compound is administered in combination with a further therapeutic agent.10. The pharmaceutical composition according to claim 2 , wherein the further therapeutic agent is an agent for the treatment claim 2 , prevention or prophylaxis of inflammatory conditions claim 2 , autoimmune diseases claim 2 , proliferative diseases claim 2 , transplantation rejection claim 2 , diseases involving impairment of cartilage turnover claim 2 , congenital cartilage malformations claim 2 , and/or diseases associated with hypersecretion of IL6.11. A method for the treatment claim 2 , prevention or prophylaxis of inflammatory conditions claim 2 , autoimmune ...

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02-03-2017 дата публикации

NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS

Номер: US20170057928A1
Принадлежит:

The present invention discloses compounds according to Formula I: 2. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris Me.6. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris H claim 1 , F claim 1 , or Cl.7. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris H claim 1 , Me claim 1 , or Et.8. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris CN claim 1 , F claim 1 , Cl claim 1 , —SOMe or —SOEt.10. A compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein the compound is (1R claim 1 ,2R)—N-[6-[(6-cyano-4-methyl-3-pyridyl)oxy]-1-methyl-benzimidazol-4-yl]-2-fluoro-cyclopropanecarboxamide.11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , according to .12. The pharmaceutical composition according to comprising a further therapeutic agent.13. (canceled)14. A method for the treatment claim 1 , prevention or prophylaxis of allergic diseases claim 1 , inflammatory diseases claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons claim 1 , said method comprising administering an amount of a compound according to claim 1 , sufficient to effect said treatment claim 1 , prevention or prophylaxis.15. The pharmaceutical composition according to claim 12 , wherein the further therapeutic agent is an agent for the treatment of allergic diseases claim 12 , inflammatory diseases claim 12 , autoimmune diseases claim 12 , proliferative diseases claim 12 , transplantation rejection claim 12 , diseases involving impairment of cartilage ...

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09-02-2017 дата публикации

NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20170035738A1
Принадлежит:

[1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the following: 2. (canceled)3. (canceled)4. The method according to claim 1 , wherein Rand Rare H or Me.5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. The method according to wherein Ris cyclopropyl claim 1 , cyclobutyl claim 1 , or cyclopentyl.11. (canceled)13. (canceled)14. (canceled)15. The method according to claim 1 , wherein Cy1 is phenyl; m2 is 1 claim 1 , 2 or 3; and each Ris independently Cl claim 1 , F claim 1 , Me claim 1 , Et claim 1 , OMe claim 1 , CF claim 1 , CONH claim 1 , CONMe claim 1 , CONHMe claim 1 , CN claim 1 , NHCOMe claim 1 , COOH claim 1 , OH or COOEt.16. The method according to claim 1 , wherein Cy1 is substituted or unsubstituted pyridyl claim 1 , substituted or unsubstituted pyrrolyl claim 1 , substituted or unsubstituted pyrazolyl claim 1 , substituted or unsubstituted imidazolyl claim 1 , substituted or unsubstituted triazolyl claim 1 , substituted or unsubstituted oxazolyl claim 1 , substituted or unsubstituted thiazolyl claim 1 , substituted or unsubstituted indolyl claim 1 , substituted or unsubstituted indazolyl claim 1 , substituted or unsubstituted benzimidazolyl claim 1 , substituted or unsubstituted benzofuranyl claim 1 , substituted or unsubstituted benzodioxanyl claim 1 , substituted or unsubstituted benzoxazolyl claim 1 , substituted or unsubstituted quinolinyl claim 1 , or substituted or unsubstituted isoquinolinyl; and m2 is 0.18. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. (canceled)25. The method according to wherein L1 is selected from - a single bond claim 1 , —O— claim 1 , —N(R)— claim 1 , —C(O)— claim 1 , —C[═N(R)]— claim 1 , —CON(R)— claim 1 , —SON(R)— claim 1 , —S(O)— claim 1 , —N(R)SO— and —N(R)CO—; n1 is 0 claim 1 , 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4; and Ris piperidinyl claim 1 , morpholinyl claim 1 , piperazinyl claim 1 , homopiperazinyl or pyrrolidinyl ...

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07-06-2012 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20120142678A1
Принадлежит:

A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound according .3. The pharmaceutical composition according to comprising a further therapeutic agent.4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A method for the treatment claim 1 , prevention or prophylaxis of inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 claim 1 , comprising administering an amount of a compound of claim 1 , sufficient to effect said treatment claim 1 , prevention or prophylaxis.9. The method according to claim 1 , wherein the compound according to is administered in combination with a further therapeutic agent.10. The pharmaceutical composition according to claim 2 , wherein the further therapeutic agent is an agent for the treatment claim 2 , prevention or prophylaxis of inflammatory conditions claim 2 , autoimmune diseases claim 2 , proliferative diseases claim 2 , transplantation rejection claim 2 , diseases involving impairment of cartilage turnover claim 2 , congenital cartilage malformations claim 2 , and/or diseases associated with hypersecretion of IL6.11. A method for the treatment claim 2 , prevention or prophylaxis of inflammatory conditions claim 2 , ...

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01-11-2012 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20120277247A1
Принадлежит:

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of the compound or pharmaceutically acceptable salt thereof claim 1 , according to .3. The pharmaceutical composition of claim 2 , wherein the carrier is selected from a parenteral carrier claim 2 , an oral carrier and a topical carrier.4. The pharmaceutical composition according to comprising a further therapeutic agent.5. A method for the treatment claim 1 , or prophylaxis of allergy claim 1 , inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplant rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or interferons claim 1 , comprising administering an amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 , sufficient to effect said treatment claim 1 , or prophylaxis.6. The method according to claim 5 , wherein the compound or pharmaceutically acceptable salt thereof claim 5 , is administered in combination with a further therapeutic agent.7. A method for the treatment ...

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06-12-2012 дата публикации

TRIAZOLOPYRIDINE KINASE INHIBITORS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20120309784A1
Принадлежит:

A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the following: 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound according to .3. The pharmaceutical composition of claim 2 , wherein the carrier is a parenteral carrier.4. The pharmaceutical composition of claim 2 , wherein the carrier is an oral carrier.5. The pharmaceutical composition of claim 2 , wherein the carrier is a topical carrier.6. A method of treatment claim 1 , prevention or prophylaxis of diseases involving cartilage degradation claim 1 , bone and/or joint degradation claim 1 , for example osteoarthritis; and/or conditions involving inflammation or immune responses claim 1 , such as Crohn's disease claim 1 , rheumatoid arthritis claim 1 , psoriasis claim 1 , allergic airways disease (e.g. asthma claim 1 , rhinitis) claim 1 , juvenile idiopathic arthritis claim 1 , colitis claim 1 , inflammatory bowel diseases claim 1 , endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure) claim 1 , diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes) claim 1 , congenital cartilage malformations claim 1 , diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) claim 1 , comprising administering to a subject a therapeutically effective amount of a compound according to .7. A method of treatment claim 1 , prevention or prophylaxis of proliferative diseases claim 1 , comprising administering to a subject a therapeutically effective amount of a compound according to .8. The method according to claim 6 , wherein the condition is selected from diseases involving a method of the anabolic stimulation of chondrocytes.9. The method according to claim 6 , wherein the condition is selected ...

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22-08-2013 дата публикации

NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20130217664A1
Принадлежит:

Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. 2. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris Me or Et.5. A compound or pharmaceutically acceptable salt according to claim 4 , wherein Ris Calkyl.6. A compound or pharmaceutically acceptable salt according to claim 4 ,{'sup': '2', 'sub': '1-4', 'wherein Ris Calkyl.'}7. A compound or pharmaceutically acceptable salt according to claim 4 , wherein the compound is according to Formula VId claim 4 , VIe claim 4 , or VIf claim 4 , and Ris H claim 4 , Me or Et.8. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris 4-7 membered heterocycloalkenyl comprising 1 double bond claim 1 , and comprising 1 or 2 heteroatoms independently selected from N claim 1 , O claim 1 , and S claim 1 , substituted with one or more groups independently selected from R.11. A compound or pharmaceutically acceptable salt according to claim 9 , wherein Lis —C(═O)— claim 9 , —C(═O)O— claim 9 , —O— claim 9 , or SO—.12. A compound or pharmaceutically acceptable salt according to claim 9 , wherein Ris Me claim 9 , Et claim 9 , n-Pr claim 9 , i-Pr claim 9 , or t-Bu.13. A compound or pharmaceutically acceptable salt according to claim 9 , wherein Ris —CH—CN claim 9 , —CH—CH—CN claim 9 , —CH—CH—OH—C(OH)H—CH claim 9 , —C(OH)H—CF claim 9 , —CHF claim 9 , —CH—CF claim 9 , —CH—CMe-OH claim 9 , —CMeH—OMe claim 9 , —CH—OH claim 9 , CMe-OH claim 9 , —CH—OMe claim 9 , —CH—C(═O)t-Bu claim 9 , ...

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22-08-2013 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20130217722A1
Принадлежит:

A novel imidazolopyridine according to Formula I, able to inhibit JAK as disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of the compound according to .3. The pharmaceutical composition according to comprising a further therapeutic agent.4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A method for the treatment or prophylaxis of allergic or inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or interferons claim 1 , comprising administering an amount of the compound according to claim 1 , sufficient to effect said treatment or prophylaxis.9. The method according to claim 1 , wherein the compound according to claim 1 , is administered in combination with a further therapeutic agent.10. The pharmaceutical composition according to claim 3 , wherein the further therapeutic agent is an agent for the treatment or prophylaxis of allergic or inflammatory conditions claim 3 , autoimmune diseases claim 3 , proliferative diseases claim 3 , transplantation rejection claim 3 , diseases involving impairment of cartilage turnover claim 3 , congenital cartilage malformations claim 3 , and/or diseases associated with hypersecretion of IL6 or interferons.11. The method according to claim 9 ...

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20-02-2014 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20140051677A1
Принадлежит:

Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. 2. A compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein m is 1.3. A compound or pharmaceutically acceptable salt thereof claim 2 , according to claim 2 , wherein Ris OH claim 2 , CN claim 2 , halo claim 2 , Calkyl optionally substituted with one or more halo claim 2 , or Calkoxy optionally substituted with one or more halo.4. A compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Cy1 is phenyl.5. A compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Cy1 is pyridyl claim 1 , pyrrolyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , triazolyl claim 1 , oxazolyl claim 1 , thiazolyl claim 1 , furanyl claim 1 , indolyl claim 1 , indazolyl claim 1 , benzimidazolyl claim 1 , benzofuranyl claim 1 , benzodioxanyl claim 1 , benzoxazolyl claim 1 , quinolinyl claim 1 , or isoquinolinyl.9. A compound or pharmaceutically acceptable salt thereof according to claim 8 , wherein Ris H claim 8 , halo claim 8 , Calkyl claim 8 , —S(O)Me claim 8 , or —C(═O)OMe.11. A compound or pharmaceutically acceptable salt thereof according to claim 10 , wherein Ris H claim 10 , CN claim 10 , or halo.12. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein X is N claim 1 , CH claim 1 , or CF.13. A compound according to claim 1 , wherein the compound is:N-(4-(4-methoxyphenyl)pyrazolo[1,5-a]pyridin ...

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10-04-2014 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20140100220A1
Принадлежит:

A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound according .3. The pharmaceutical composition according to comprising a further therapeutic agent.4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A method for the treatment claim 1 , prevention or prophylaxis of inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 claim 1 , comprising administering an amount of a compound of claim 1 , sufficient to effect said treatment claim 1 , prevention or prophylaxis.9. The method according to claim 1 , wherein the compound according to is administered in combination with a further therapeutic agent.10. The pharmaceutical composition according to claim 2 , wherein the further therapeutic agent is an agent for the treatment claim 2 , prevention or prophylaxis of inflammatory conditions claim 2 , autoimmune diseases claim 2 , proliferative diseases claim 2 , transplantation rejection claim 2 , diseases involving impairment of cartilage turnover claim 2 , congenital cartilage malformations claim 2 , and/or diseases associated with hypersecretion of IL6.11. A method for the treatment claim 2 , prevention or prophylaxis of inflammatory conditions claim 2 , ...

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01-01-2015 дата публикации

Novel compounds and pharmaceutical compositions thereof for the treatment of cystic fibrosis.

Номер: US20150005275A1
Принадлежит: GALAPAGOS NV

The present invention discloses compounds according to Formula I: wherein R 1 , R 2 , R 3 , L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.

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29-01-2015 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20150031671A1
Принадлежит:

A compound is disclosed that has a formula represented by the following: 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to .3. The pharmaceutical composition according to comprising a further therapeutic agent.4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A method for the treatment or prophylaxis of inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 claim 1 , said method comprising administering an effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to .9. A method according to claim 8 , wherein the inflammatory condition is rheumatoid arthritis.10. A method according to claim 8 , wherein the condition or disease involves inflammation.11. The method according to claim 8 , wherein the compound according to is administered in combination with a further therapeutic agent.12. The pharmaceutical composition according to claim 2 , wherein the further therapeutic agent is an agent for the treatment claim 2 , prevention or prophylaxis of inflammatory conditions claim 2 , autoimmune diseases claim 2 , proliferative diseases claim 2 , transplantation rejection claim 2 , diseases involving impairment of cartilage turnover claim 2 , congenital cartilage malformations claim 2 , and/or diseases associated with hypersecretion of IL6.13. A method for the treatment or prophylaxis of inflammatory conditions claim 2 , autoimmune diseases claim 2 , proliferative diseases claim 2 , transplantation rejection claim 2 , diseases involving impairment of cartilage turnover claim 2 , congenital cartilage malformations claim 2 , and/or ...

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29-01-2015 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20150031706A1
Принадлежит:

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of the compound or pharmaceutically acceptable salt thereof claim 1 , according to .3. The pharmaceutical composition of claim 2 , wherein the carrier is selected from a parenteral carrier claim 2 , an oral carrier and a topical carrier.4. The pharmaceutical composition according to comprising a further therapeutic agent.5. A method for the treatment claim 1 , or prophylaxis of allergy claim 1 , inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplant rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or interferons claim 1 , comprising administering an amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 , sufficient to effect said treatment claim 1 , or prophylaxis.6. The method according to claim 5 , wherein the compound or pharmaceutically acceptable salt thereof claim 5 , is administered in combination with a further therapeutic agent.7. A method for the treatment ...

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28-02-2019 дата публикации

Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Номер: US20190062325A1
Принадлежит: GALAPAGOS NV

The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions, pain, neuroinflammatory conditions, neurodegenerative conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, cardiovascular diseases, leukemia, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

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22-03-2018 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATEMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20180078547A1
Принадлежит:

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of the compound or pharmaceutically acceptable salt thereof claim 1 , according to .3. The pharmaceutical composition of claim 2 , wherein the carrier is selected from a parenteral carrier claim 2 , an oral carrier and a topical carrier.4. The pharmaceutical composition according to comprising a further therapeutic agent.5. A method for the treatment claim 1 , or prophylaxis of allergy claim 1 , inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplant rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or interferons claim 1 , comprising administering an amount of a compound or pharmaceutically acceptable salt thereof according to claim 1 , sufficient to effect said treatment claim 1 , or prophylaxis.6. The method according to claim 5 , wherein the compound or pharmaceutically acceptable salt thereof claim 5 , is administered in combination with a further therapeutic agent.7. A method for the treatment ...

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12-03-2020 дата публикации

NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20200078365A1
Принадлежит:

A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound according .3. The pharmaceutical composition according to comprising a further therapeutic agent.4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A method for the treatment claim 1 , prevention or prophylaxis of inflammatory conditions claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 claim 1 , comprising administering an amount of a compound of claim 1 , sufficient to effect said treatment claim 1 , prevention or prophylaxis.9. The method according to claim 8 , comprising administering a further therapeutic agent.10. The method according to claim 9 , wherein the further therapeutic agent is an agent for the treatment claim 9 , prevention or prophylaxis of inflammatory conditions claim 9 , autoimmune diseases claim 9 , proliferative diseases claim 9 , transplantation rejection claim 9 , diseases involving impairment of cartilage turnover claim 9 , congenital cartilage malformations claim 9 , and/or diseases associated with hypersecretion of IL6.11. The method of claim 8 , wherein the autoimmune disease is obstructive airway disease claim 8 , COPD claim 8 , asthma claim 8 , bronchitis claim 8 , systemic lupus ...

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13-04-2017 дата публикации

NOVEL COMPOUNDS FOR TREATMENT OF CYSTIC FIBROSIS

Номер: US20170100386A1
Принадлежит:

A corrector agent capable of stabilizing a newly synthesized cystic fibrosis transmembrane conductance regulator (CFTR) protein, useful in the treatment of cystic fibrosis. 1. A corrector agent for the treatment of Cystic Fibrosis , wherein the corrector agent is capable of stabilizing a newly synthesized Cystic fibrosis transmembrane conductance regulator (CFTR) protein.2. The corrector agent of claim 1 , wherein the CFTR protein is a mutant CFTR protein.3. The corrector agent of claim 1 , wherein the CFTR protein is a wild-type CFTR protein.4. The corrector agent of claim 1 , wherein the CFTR protein comprises a mutation selected from a group consisting of Class II claim 1 , Class III claim 1 , Class IV claim 1 , Class V and Class VI mutations.5. The corrector agent of claim 1 , wherein the CFTR comprises a Class I mutation or Class III mutation.6. The corrector agent of claim 5 , wherein the CFTR comprises a CFTRΔF508 mutation.7. The corrector agent of claim 1 , wherein said CFTR comprises a CFTRΔF508 mutation and the plasma membrane levels of said CFTR in the presence of said agent are at least 300% of the level obtainable with a type I corrector with said CFTR protein.8. The corrector agent of claim 7 , wherein said level is measured in a Cell Surface Expression assay.9. The corrector agent of claim 1 , wherein the CFTR comprises a CFTRΔF508 mutation and activity of said CFTR protein in the presence of said agent in combination with type I corrector and potentiator are at least 50% of the level of wild-type CFTR in healthy cells.10. The corrector agent of claim 1 , wherein said corrector agent directly binds to CFTR protein.11. The corrector agent of claim 11 , wherein said binding is measured using patch clamp and Back scattering technology.12. The corrector agent of claim 1 , wherein the CFTR protein is synthesized in full length and prior to post-translational modifications.13. The corrector agent of claim 13 , wherein the post-translation modification is ...

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13-04-2017 дата публикации

N-SULFONYLATED PYRAZOLO[3,4-b]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE

Номер: US20170101405A1
Принадлежит: AbbVie SARL, GALAPAGOS NV

The present invention provides for compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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13-04-2017 дата публикации

SUBSTITUTED PYRAZOLO[3,4-b]PYRIDIN-6-CARBOXYLIC ACIDS AND METHOD OF USE

Номер: US20170101406A1
Принадлежит:

The present invention provides for compounds of formula (I) 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '1A', '1B', '1C, 'sub': 1', '6', '1', '6, 'Ris G, -G-G, C-Chaloalkyl, or C-Calkyl.'}3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '1A, 'Ris G.'}4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '1B', '1C, 'Ris -G-G.'}5. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 2', '2xa', '2A, 'sub': 2', '4', '1', '6', '1', '6, 'Ris C-Calkenyl, C-Calkyl, C-Chaloalkyl, —OR, or G.'}6. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 2', '2A, 'sub': 1', '6', '1', '6, 'Ris C-Calkyl, C-Chaloalkyl, or G.'}7. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 3', '3A', '3B', '1', '3C', '3a', '3a', '3b, 'Ris G, -G-L-G, —OR, or —N(R)(R).'}8. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '1A', '1B', '1C, 'Ris Gor -G-G; and'}{'sup': 2', '2xa', '2A, 'sub': 2', '4', '1', '6', '1', '6, 'Ris C-Calkenyl, C-Calkyl, C-Chaloalkyl, —OR, or G.'}9. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '1A', '1B', '1C, 'Ris Gor G-G; and'}{'sup': 3', '3A', '3B', '1', '3C', '3a', '3a', '3b, 'Ris G, -G-L-G, —OR, or —N(R)(R).'}10. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '1A', '1B', '1C, 'Ris Gor -G-G;'}{'sup': 2', '2xa', '2A, 'sub': 2', '4', '1', '6', '1', '6, 'Ris C-Calkenyl, C-Calkyl, C-Chaloalkyl, —OR, or G; and'}{'sup': 3', '3A', '3B', '1', '3C', '3a', '3a', '3b, 'Ris G, -G-L-G, —OR, or —N(R)(R).'}11. The compound of or a pharmaceutically acceptable salt thereof claim 10 , wherein{'sup': '1A', 'Gis optionally substituted phenyl or optionally substituted 5-6 membered monocyclic heteroaryl;'}{'sup': '2', 'sub': 1', '6, ...

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19-04-2018 дата публикации

N-SULFONYLATED PYRAZOLO[3,4-b]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE

Номер: US20180105522A1
Принадлежит:

The present invention provides for compounds of formula (I) 1. A compound , which is 3-cyclobutyl-N-(dimethylsulfamoyl)-1-(4-fluorophenyl)-4-(4-methoxy[1 ,4′-bipiperidin]-1′-yl)-1H-pyrazolo[3 ,4-b]pyridine-6-carboxamide , wherein one or more hydrogen atoms are replaced by deuterium; or a pharmaceutically acceptable salt thereof.2. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a therapeutically effective amount of a potentiator or a therapeutically effective amount of one or more correctors.3. The pharmaceutical composition of claim 1 , wherein the potentiator can be selected from the group consisting of:Ivacaftor (VX-770, N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide);CTP-656;NVS-QBW251;FD1860293;PTI-808;GLPG1837;GLPG2451;2-(2-fluorobenzamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;N-(3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-5-carboxamide;2-(2-hydroxybenzamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;2-(1-hydroxycyclopropanecarboxamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;5,5,7,7-tetramethyl-2-(2-(trifluoromethyl)benzamido)-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;2-(2-hydroxy-2-methylpropanamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;2-(1-(hydroxymethyl)cyclopropanecarboxamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;2-(3-hydroxy-2,2-dimethylpropanamido)-5, 5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;N-(3-carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-5-methyl-1H-pyrazole-3-carboxamide;N-(3-carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-5-cyclopropyl-1H-pyrazole-3-carboxamide;N-(3-carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-5-isopropyl-1H-pyrazole-3-carboxamide;N-(3- ...

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31-07-2014 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: US20140213576A1
Принадлежит: GALAPAGOS NV

A novel compound according to Formula I, able to inhibit JAK as disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

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04-06-2015 дата публикации

NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: US20150150856A1
Принадлежит:

[1,2,4]triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the following: 150-. (canceled)52. The method of wherein said compound is prepared and administered as a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of said compound or a pharmaceutically acceptable salt thereof.53. The method according to wherein the inflammatory bowel disorder is selected from Crohn's disease and colitis.57. A method for the treatment of inflammatory bowel disorders claim 51 , said method comprising administering a therapeutically effective amount of a compound selected fromN-(5-(4-(4-methylpiperazin-1-yl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(3-(morpholinomethyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(biphenyl-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(4-benzoylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,4-(2-(cyclopropanecarboxamido)-[1,2,4]triazolo[1,5-a]pyridin-5-yl)-N-cyclopropylbenzamide,N-(5-(4-(benzyloxy)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(4-(N-cyclopropylsulfamoyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(3-(benzyloxy)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(4-(benzyloxy)-3-fluorophenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(2-(benzyloxy)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(4-(piperidine-1-carbonyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(4-(morpholinomethyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(4-(pyrrolidine-1-carbonyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(5-(4-(thiophen-2-yl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide,N-(4-(2-(cyclopropanecarboxamido)-[1,2,4]triazolo[1,5-a]pyridin- ...

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23-05-2019 дата публикации

NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS

Номер: US20190152922A1
Принадлежит:

The present invention discloses compounds according to Formula I: 2. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris Me.6. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris H claim 1 , F claim 1 , or Cl.7. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris H claim 1 , Me claim 1 , or Et.8. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris CN claim 1 , F claim 1 , Cl claim 1 , —SOMe or —SOEt.10. A compound or pharmaceutically acceptable salt according to claim 1 , wherein the compound is (1R claim 1 ,2R)—N-[6-[(6-cyano-4-methyl-3-pyridyl)oxy]-1-methyl-benzimidazol-4-yl]-2-fluoro-cyclopropanecarboxamide.11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound or pharmaceutically acceptable salt according to .12. The pharmaceutical composition according to claim 11 , comprising a further therapeutic agent.13. (canceled)14. A method for treating or preventing allergic diseases claim 1 , inflammatory diseases claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons comprising administering an effective amount of the compound or pharmaceutically acceptable according to .15. The pharmaceutical composition according to claim 12 , wherein the further therapeutic agent is an agent for the treatment of allergic diseases claim 12 , inflammatory diseases claim 12 , autoimmune diseases claim 12 , proliferative diseases claim 12 , transplantation rejection claim 12 , diseases involving impairment of cartilage turnover claim 12 , congenital cartilage malformations claim 12 , and/or diseases associated with hypersecretion of IL6 or ...

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23-07-2015 дата публикации

NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS

Номер: US20150203455A1
Принадлежит:

The present invention discloses compounds according to Formula I: 2. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris Me.6. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris H claim 1 , F claim 1 , or Cl.7. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris H claim 1 , Me claim 1 , or Et.8. A compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris CN claim 1 , F claim 1 , Cl claim 1 , —SOMe or —SOEt.10. A compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein the compound is (1R claim 1 ,2R)—N-[6-[(6-cyano-4-methyl-3-pyridyl)oxy]-1-methyl-benzimidazol-4-yl]-2-fluoro-cyclopropanecarboxamide.11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , according to .12. The pharmaceutical composition according to comprising a further therapeutic agent.13. (canceled)14. A method for the treatment claim 1 , prevention or prophylaxis of allergic diseases claim 1 , inflammatory diseases claim 1 , autoimmune diseases claim 1 , proliferative diseases claim 1 , transplantation rejection claim 1 , diseases involving impairment of cartilage turnover claim 1 , congenital cartilage malformations claim 1 , and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons claim 1 , said method comprising administering an amount of a compound according to claim 1 , sufficient to effect said treatment claim 1 , prevention or prophylaxis.15. The pharmaceutical composition according to claim 12 , wherein the further therapeutic agent is an agent for the treatment of allergic diseases claim 12 , inflammatory diseases claim 12 , autoimmune diseases claim 12 , proliferative diseases claim 12 , transplantation rejection claim 12 , diseases involving impairment of cartilage ...

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04-07-2019 дата публикации

N-SULFONYLATED PYRAZOLO[3,4-b]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE

Номер: US20190202823A1
Принадлежит:

The present invention provides for compounds of formula (I) 1. A compound , which is 3-cyclobutyl-N-(dimethylsulfamoyl)-1-(4-fluorophenyl)-4-(4-methoxy[1 ,4′-bipiperidin]-1′-yl)-1H-pyrazolo[3 ,4-b]pyridine-6-carboxamide , wherein one or more hydrogen atoms are replaced by deuterium; or a pharmaceutically acceptable salt thereof.2. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a therapeutically effective amount of a potentiator or a therapeutically effective amount of one or more correctors.3. The pharmaceutical composition of claim 1 , wherein the potentiator can be selected from the group consisting of:Ivacaftor (VX-770, N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide);CTP-656;NVS-QBW251 FD1860293;PTI-808;GLPG1837;GLPG2451;2-(2-fluorobenzamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;N-(3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-5-carboxamide;2-(2-hydroxybenzamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;2-(1-hydroxycyclopropanecarboxamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;5,5,7,7-tetramethyl-2-(2-(trifluoromethyl)benzamido)-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;2-(2-hydroxy-2-methylpropanamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;2-(1-(hydroxymethyl)cyclopropanecarboxamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;2-(3-hydroxy-2,2-dimethylpropanamido)-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide;N-(3-carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-5-methyl-1H-pyrazole-3-carboxamide;N-(3-carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-5-cyclopropyl-1H-pyrazole-3-carboxamide;N-(3-carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-5-isopropyl-1H-pyrazole-3-carboxamide;N-(3- ...

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15-09-2016 дата публикации

NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF CYSTIC FIBROSIS

Номер: US20160263084A1
Принадлежит:

The present invention discloses compounds according to Formula I: 3) The method according to claim 2 , wherein Ris Calkyl.5) The method according to claim 4 , wherein Ris phenyl substituted with one or more independently selected R.6) The method according to claim 5 , wherein Ris F claim 5 , Cl claim 5 , or CN.8) The method according to claim 7 , wherein Cy is azetidinyl claim 7 , pyrrolidinyl claim 7 , tetrahydropyranyl claim 7 , piperidinyl claim 7 , morpholinyl 2-oxa-5-aza-bicyclo[2.2.1]heptanyl claim 7 , [1 claim 7 ,4]oxazepanyl claim 7 , 2 claim 7 ,3-dihydro-1H-isoindolyl claim 7 , or 1 claim 7 ,2 claim 7 ,3 claim 7 ,4-tetrahydro-isoquinolinyl.9) The method according to claim 1 , wherein Ris phenyl claim 1 , substituted with one or more independently selected Rgroups.10) The method according to claim 1 , wherein Ris furanyl claim 1 , thiophenyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , thiazolyl claim 1 , oxazolyl claim 1 , pyridinyl claim 1 , pyridazinyl claim 1 , pyrimidyl claim 1 , or pyrazinyl claim 1 , each of which is substituted with one or more independently selected Rgroups.11) The method according to claim 10 , wherein Ris F claim 10 , Cl claim 10 , OH claim 10 , or CN.12) The method according to claim 10 , wherein Ris CH claim 10 , —CH—CH claim 10 , —CH(CH) claim 10 , —OCH claim 10 , or —OCH—CH claim 10 , each of which is optionally substituted with one or more independently selected R.13) The method according to claim 12 , wherein Ris F claim 12 , Cl claim 12 , OH claim 12 , CN claim 12 , or —OCH.14) The method according to claim 1 , wherein Ris —CH(CH) claim 1 , —C(CH) claim 1 , —C(CH)—CH claim 1 , or —C(CH)H—CH(CH) claim 1 , each of which is substituted with one or more independently selected Re groups.15) The method according to claim 14 , wherein Ris F claim 14 , Cl claim 14 , OH claim 14 , or CN.16) The method according to claim 1 , wherein Ris H.17) The method according to claim 1 , wherein Ris —CH.18) The method according to claim 1 ...

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01-10-2015 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: US20150274722A1
Принадлежит: GALAPAGOS NV

A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

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25-10-2018 дата публикации

6-[5-AMINO-6-(2-ETHOXYETHOXY)-IMIDAZO[4,5-B]PYRIDIN-3-YL]-NICOTINONITRILE DERIVATIVES AND THEIR USE AS IRAK INHIBITORS

Номер: US20180305351A1
Принадлежит:

The present invention discloses compounds according to Formula I: 2. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Cy is monocyclic Ccycloalkyl substituted with one or two independently selected R.3. A compound or pharmaceutically acceptable salt thereof according to or claim 1 , wherein Cy is tetrahydropyranyl or tetrahydrothiopyranyl claim 1 , each of which is optionally substituted with one or two independently selected R.4. A compound or pharmaceutically acceptable salt thereof according to any one of - claim 1 , wherein Ris selected from OH claim 1 , ═O claim 1 , F claim 1 , and —CH.6. A compound or pharmaceutically acceptable salt thereof according to any one of - claim 1 , wherein Ris H claim 1 , —CH claim 1 , —SOH claim 1 , or —P(═O)(OH).7. A compound or pharmaceutically acceptable salt thereof according to any one of - claim 1 , wherein Ris —C(═O)Calkyl claim 1 , which Calkyl is substituted with one or two independently selected R.8. A compound or pharmaceutically acceptable salt thereof according to any one of - claim 1 , wherein Ris —C(═O)Calkyl claim 1 , which Calkyl is substituted with one or two independently selected —C(═O)OH claim 1 , —NH claim 1 , —NHCH claim 1 , or —N(CH).9. A compound or pharmaceutically acceptable salt thereof according to any one of - claim 1 , wherein Ris H or —CH.10. A compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is selected from:6-[6-[2-(2-hydroxy-ethoxy)-ethoxy]-5-(tetrahydro-pyran-4-ylamino)-imidazo[4,5-b]pyridin-3-yl]-nicotinonitrile, and(S)-2-amino-3-methyl-butyric acid 2-{2-[3-(5-cyano-pyridin-2-yl)-5-(tetrahydro-pyran-4-ylamino)-3H-imidazo[4,5-b]pyridin-6-yloxy]-ethoxy}-ethyl ester.11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound or pharmaceutically acceptable salt thereof claim 1 , according to any one of -.12. A pharmaceutical composition ...

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26-12-2019 дата публикации

NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROSIS

Номер: US20190388421A1
Принадлежит:

The present invention discloses compounds according to Formula I: 4) A compound or a pharmaceutically acceptable salt thereof according to , or , wherein Ris —CH , —CHCH , or —(CH)CH , each of which is substituted with one , two or three independently selected halo , —CN , —Calkoxy , or —NRR.5) A compound or a pharmaceutically acceptable salt thereof according to , or , wherein Ris Cmonocyclic cycloalkyl.7) A compound or a pharmaceutically acceptable salt thereof according to any one of - , wherein Ris Calkyl.8) A compound or a pharmaceutically acceptable salt thereof according to any one of - , wherein Cyis pyridinyl.9) A compound or a pharmaceutically acceptable salt thereof according to any one of - , wherein the subscript m is 1 , 2 , 3 , or 4.10) A compound or a pharmaceutically acceptable salt thereof according to any one of - , wherein Ris Calkyl substituted with one or more independently selected Rgroups.11) A compound or a pharmaceutically acceptable salt thereof according to claim 10 , wherein Ris F claim 10 , —CN claim 10 , —OH claim 10 , —OCH claim 10 , —OCF claim 10 , —OCHCH claim 10 , —OCHCF claim 10 , —OCHCHOH claim 10 , or —OCHCHOCH.12) A compound or a pharmaceutically acceptable salt thereof according to any one of - claim 10 , wherein Ris Calkoxy.13) A pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof according to any one of - claim 10 , and a pharmaceutically acceptable carrier.14) A pharmaceutical composition according to comprising a further therapeutic agent.15) A compound or a pharmaceutically acceptable salt thereof claim 13 , according to any one of - claim 13 , or a pharmaceutical composition according to or for use in medicine.16) A compound or a pharmaceutically acceptable salt thereof according to any one of - claim 13 , or a pharmaceutical composition according to or for use in the prophylaxis and/or treatment of fibrotic diseases claim 13 , inflammatory diseases claim 13 , autoimmune ...

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31-01-2018 дата публикации

6,7-Dihydropyrid [2,1-a] isoquinolin-2-one derivatives as gpr84 receptor antagonists, and compositions containing them

Номер: CO2017011093A2
Принадлежит: GALAPAGOS NV

Un compuesto de acuerdo con la Fórmula I: (VER IMAGEN ADJUNTA) en donde R1, LA, CyA, RA, R2, R3 y R4 son como se describe en la presente. La presente invención se refiere a compuestos novedosos de acuerdo con la Fórmula I que antagonizan GPR84, un receptor conectado a la proteína G que está involucrado en afecciones inflamatorias, y métodos para la producción de estos nuevos compuestos, composiciones farmacéuticas que comprenden estos compuestos, y métodos para la prevención y/o el tratamiento de afecciones inflamatorias, dolor, afecciones neuroinflamatorias, afecciones neurodegenerativas, enfermedades infecciosas, enfermedades autoinmunes, enfermedades endocrinas y/o metabólicas, enfermedades cardiovasculares, leucemia y/o enfermedades que involucran deterioro de las funciones celulares inmunológicas, mediante la administración de un compuesto de la invención. A compound according to Formula I: (SEE ATTACHED IMAGE) wherein R1, LA, CyA, RA, R2, R3 and R4 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a receptor connected to the G protein that is involved in inflammatory conditions, and methods for the production of these new compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and / or treatment of inflammatory conditions, pain, neuroinflammatory conditions, neurodegenerative conditions, infectious diseases, autoimmune diseases, endocrine and / or metabolic diseases, cardiovascular diseases, leukemia and / or diseases that involve impairment of immune cellular functions , by administering a compound of the invention.

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28-01-2010 дата публикации

Novel compounds useful for the treatment of degenerative and inflammatory diseases.

Номер: AU2009273144A1
Принадлежит: GALAPAGOS NV

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17-09-2019 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: CA2833963C
Принадлежит: GALAPAGOS NV

Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

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03-07-2012 дата публикации

NOVEL COMPOUND USED TO TREAT DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: MA33447B1
Принадлежит: GALAPAGOS NV

L'invention concerne un composé représenté par la formule (I). Ce composé peut être préparé comme une composition pharmaceutique, et peut être utilisé pour prévenir et traiter une variété d'états chez les mammifères, en particulier chez l'homme, comprenant à titre d'exemple notamment et de manière non restrictive, les états inflammatoires, les maladies auto-immunes, les maladies prolifératives, les rejets de transplantation, les maladies impliquant l'incapacité de renouvellement du cartilage, les malformations congénitales du cartilage, et/ou les maladies associées à l'hypersécrétion de IL6. The invention relates to a compound represented by formula (I). This compound can be prepared as a pharmaceutical composition, and can be used to prevent and treat a variety of conditions in mammals, in particular in humans, including by way of example, in particular and in a non restrictive manner, inflammatory conditions , autoimmune diseases, proliferative diseases, transplant rejections, diseases involving cartilage turnover failure, congenital malformations of cartilage, and / or diseases associated with hypersecretion of IL6.

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30-07-2015 дата публикации

Benzimidazole derivatives and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Номер: CA2941474A1
Принадлежит: GALAPAGOS NV

The present invention discloses compounds according to Formula (I) wherein Cy, R1, L1 R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

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06-03-2013 дата публикации

Novel compounds useful for the treatment of degenerative and inflammatory diseases.

Номер: EP2346864B1
Принадлежит: GALAPAGOS NV

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29-09-2017 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: PL2792677T3
Принадлежит: GALAPAGOS NV

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31-10-2018 дата публикации

Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Номер: EP3395802A1
Принадлежит: GALAPAGOS NV

The present invention discloses compounds according to Formula I: Wherein Cy, R 1 , L 1 , R 3 , R 4 , R 5 , L a , and R a are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

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29-01-2018 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: HUE034205T2
Принадлежит: GALAPAGOS NV

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21-03-2011 дата публикации

Novel compounds useful for the treatment of degenerative and inflammatory diseases.

Номер: MX2011000756A
Принадлежит: GALAPAGOS NV

Se describe un nuevo compuesto de [1,2,4]Triazolo[1,5-a]piridina que tiene la fórmula representada por la fórmula (I). Este compuesto puede prepararse como un composición farmacéutica, y puede utilizarse para la prevención o tratamiento de una variedad de afecciones en mamíferos incluyendo humanos, incluyendo a manera de ejemplo no limitante, enfermedades que involucran degradación de cartílago, degradación de hueso y/o articulaciones, por ejemplo osteoartritis; y/o afecciones que involucran inflamación o respuestas inmunitarias, tales como enfermedad de Crohn, artritis reumatoide, psoriasis, enfermedad alérgica de las vías respiratorias, (por ejemplo, asma, rinitis), artritis idiopática juvenil, colitis, enfermedades inflamatorias del intestino, estados de enfermedad conducidos por endotoxina (por ejemplo, complicaciones después de cirugía de baipás o estados de endotoxina crónicos que contribuyen a, por ejemplo, falla cardiaca crónica), enfermedades que involucran la disfunción de la funcionalidad de los cartílagos (por ejemplo, enfermedades que involucran estimulación anabólica de condrocitos), malformaciones de cartílago congénitas, enfermedades asociadas con la hipersecreción de 1L6 y rechazo al trasplante (por ejemplo, rechazo al trasplante de órgano) y enfermedades proliferativas.

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29-12-2010 дата публикации

Cyclopropanecarboxylic acid {5[-4-(3,3-dimethyl-azetidine-1-carbonyl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide useful for the inhibition of janus kinase (jak)

Номер: CA2765988A1
Принадлежит: GALAPAGOS NV

A compound is disclosed that has a formula represented by the following: (see formula I) This compound is an inhibitor of JAK, may be prepared as a pharmaceutical composition, and may be useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

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25-11-2011 дата публикации

Novel compounds useful for the treatment of degenerative and inflammatory diseases

Номер: NZ590646A
Принадлежит: GALAPAGOS NV

Disclosed are substituted [1,2,4]triazolo[1 ,5-a]pyridines of formula VIa useful as Janus tyrosine kinase inhibitors for the treatment of degenerative, inflammatory, proliferative and other diseases. The application also relates to the synthesis of these compounds as well as to their pharmaceutical compositions.

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28-01-2010 дата публикации

Substituted [1,2,4]triazolo[1,5-a]pyridine compounds useful for the inhibition of janus kinase (jak)

Номер: CA2730762A1
Принадлежит: GALAPAGOS NV

A novel compound able to inhibit JAK is disclosed, (see formula VIa) This compound may be prepared as a pharmaceutical composition, and may be useful for the prevention and treatment of conditions in mammals including humans, such as, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

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22-10-2014 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: EP2792677A1
Принадлежит: GALAPAGOS NV

A compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

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19-02-2015 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: AU2012247484B2
Принадлежит: GALAPAGOS NV

Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

Подробнее
21-11-2017 дата публикации

Substituted [1,2,4]triazolo[1,5-a]pyridine compounds useful for the inhibition of janus kinase (jak)

Номер: CA2730762C
Принадлежит: GALAPAGOS NV

A novel compound able to inhibit JAK is disclosed, (see formula VIa) This compound may be prepared as a pharmaceutical composition, and may be useful for the prevention and treatment of conditions in mammals including humans, such as, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6 and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

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28-02-2020 дата публикации

5-phenyl-(1,2,4)triazolo(1,5-a)pyridin-2-yl carboxamides as jak inhibitors

Номер: SI3178819T1
Принадлежит: GALAPAGOS NV

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13-05-2013 дата публикации

NEW RELATIONSHIPS USED TO TREAT DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: DK2346864T3
Принадлежит: GALAPAGOS NV

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31-05-2018 дата публикации

PYRAZOLO [3,4-b] PYRIDIN-6-CARBOXAMIDES N-SULFONYLATES AND METHOD OF USE

Номер: ECSP18032223A
Принадлежит: AbbVie SARL, GALAPAGOS NV

La presente invención proporciona compuestos de fórmula (I) (consta fórmula) (I) en donde R1, R2, R3, R4, R5 y R6 tiene cualquiera de los valores definidos en la memoria descriptiva, y sales farmacéuticamente aceptables de los mismos, que son útiles como agentes en el tratamiento de enfermedades y afecciones mediadas y moduladas por CFTR, que incluyen fibrosis quística, síndrome de Sjögren, insuficiencia pancreática, enfermedad pulmonar obstructiva crónica y enfermedad obstructiva crónica de las vías aéreas. También se proporcionan composiciones farmacéuticas comprendidas por uno o más compuestos de fórmula (I).

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04-06-2015 дата публикации

5-phenyl-[1,2,4 ]triazolo[1,5-a]pyridin-2-yl carboxamides as JAK inhibitors

Номер: AU2010264633B2
Принадлежит: GALAPAGOS NV

A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. (I)

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27-01-2020 дата публикации

5-phenyl-[1,2,4]triazolo[1,5-a]pyridin-2-yl-carboxamider som jak-inhibitorer

Номер: DK3178819T3
Принадлежит: GALAPAGOS NV

Подробнее
05-03-2015 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: AU2012247482B2
Принадлежит: GALAPAGOS NV

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed,as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolite thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hyper secretion of IL6.

Подробнее
05-03-2014 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: EP2702059A1
Принадлежит: GALAPAGOS NV

Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

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15-08-2018 дата публикации

N-sulfonylated pyrazolo[3,4-b]pyridin-6-carboxamides and method of use

Номер: EP3359541A1
Принадлежит: AbbVie SARL, GALAPAGOS NV

The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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17-09-2015 дата публикации

5-phenyl-[1,2,4 ]triazolo[1,5-a]pyridin-2-yl carboxamides as JAK inhibitors

Номер: AU2015218544A1
Принадлежит: GALAPAGOS NV

H:\ dx~ jlnavlveroaRPorthl\DCC\RBR2651_,Ldocx:-27/08/2015 A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of 5 conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. />-N H s o

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31-07-2012 дата публикации

5-PHENYL- (1,2,4) TRIAZOLO (1,5-A) PIRIDIN - 2 IL CARBOXAMIDE AS JAK INHIBITOR

Номер: CO6491040A2
Принадлежит: GALAPAGOS NV

Se revela un nuevo compuesto capaz de inhibir JAK; este compuesto puede prepararse como una composición farmacéutica, y puede usarse para la prevención y el tratamiento de una diversidad de afecciones en mamíferos, que incluyen humanos, que abarcan, a modo de ejemplo, sin limitación, afecciones inflamatorias, enfermedades auto inmunitarias, enfermedades proliferativas, rechazo de trasplantes, enfermedades que involucran el deterioro del recambio de cartílago, malformaciones congénitas del cartílago y enfermedades asociadas con la hipersecreción de IL6.

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15-02-2012 дата публикации

NEW USEFUL COMPOUND FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: DOP2011000378A
Принадлежит: GALAPAGOS NV

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28-05-2009 дата публикации

Novel compounds useful for the treatment of degenerative & inflamatory diseases

Номер: US20090137549A1
Принадлежит: Biofocus DPI Ltd, GALAPAGOS NV

The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation.

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27-07-2016 дата публикации

NEW UNIONS USEFUL FOR TREATMENT OF DISEASES AND INFLAMMATORY DISEASES

Номер: CY1113945T1
Принадлежит: GALAPAGOS N.V.

Παρουσιάζεται μια νέα ένωση [1,2,4]τριαζολο[1,5-α]πυριδίνης, η οποία έχει έναν τύπο που αναπαριστάται από τον τύπο (I). Αυτή η ένωση μπορεί να παρασκευαστεί ως μια φαρμακευτική σύνθεση και μπορεί να χρησιμοποιηθεί για την πρόληψη και την αντιμετώπιση ενός πλήθους καταστάσεων στα θηλαστικά, συμπεριλαμβανόμενων των ανθρώπων, συμπεριλαμβανόμενων ως μη περιοριστικό παράδειγμα των νόσων που εμπλέκουν τον εκφυλισμό του χόνδρου, τον εκφυλισμό των οστών και/ή των αρθρώσεων, για παράδειγμα της οστεοαρθρίτιδας, και/ή καταστάσεων που εμπλέκουν την φλεγμονή ή φλεγμονώδεις αποκρίσεις, όπως η νόσος του Crohn, η ρευματοειδής αρθρίτιδα, η ψωρίαση, η αλλεργική νόσος των αεραγωγών (π.χ. άσθμα, ρινίτιδα), η νεανική ιδιοπαθής αρθρίτιδα, η κολίτιδα, η φλεγμονώδης νόσος των εντέρων, οι καταστάσεις νόσων που προκαλούνται από ενδοτοξίνη (π.χ. επιπλοκές μετά από χειρουργική επέμβαση bypass ή χρόνιες καταστάσεις ενδοτοξίνης, οι οποίες συμβάλλουν π.χ. στην χρόνια καρδιακή ανεπάρκεια), νόσων που αφορούν την εξασθένιση της ανανέωσης του χόνδρου (π.χ. νόσων που εμπλέκουν την αναβολική διέγερση των χονδροκυττάρων), των συγγενών δυσπλασιών χόνδρου, των νόσων που σχετίζονται με την υπερέκκριση της IL6 και την απόρριψη μεταμόσχευσης (π.χ. απόρριψη μεταμόσχευσης οργάνου) και των πολλαπλασιαστικών νόσων. A novel compound [1,2,4] triazolo [1,5-a] pyridine is introduced, having a formula represented by formula (I). This compound can be prepared as a pharmaceutical composition and can be used to prevent and treat a variety of conditions in mammals, including humans, including as a non-limiting example of diseases involving cartilage degeneration, bone degeneration and / or or joints, for example osteoarthritis, and / or conditions that involve inflammation or inflammatory responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic air disease fever (eg asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel disease, endotoxin-induced disease states (eg ...

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08-09-2017 дата публикации

Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis

Номер: CA3016185A1
Принадлежит: GALAPAGOS NV

The present invention discloses compounds according to Formula I, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6a, X, Cy1, Cy2, and the subscript n and m are as defined herein. The present invention relates to antagonists compounds of sphingosine 1-phosphate (SIP) receptor, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, inflammatory diseases, autoimmune diseases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering the compound of the invention.

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18-07-2012 дата публикации

5-Phenyl-[1,2,4] triazolo[1,5-A]pyridin-2-yl carboxamides as jak inhibitors

Номер: GB2483424B
Принадлежит: GALAPAGOS NV

Подробнее
28-01-2010 дата публикации

Novel compounds useful for the treatment of degenerative and inflammatory diseases

Номер: CA2730757A1
Принадлежит: GALAPAGOS NV

[1,2,4]Triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non- limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6, transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

Подробнее
27-04-2017 дата публикации

5-phenyl-[1,2,4 ]triazolo[1,5-a]pyridin-2-yl carboxamides as JAK inhibitors

Номер: AU2015218544B2
Принадлежит: GALAPAGOS NV

H:\ dx~ jlnavlveroaRPorthl\DCC\RBR2651_,Ldocx:-27/08/2015 A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of 5 conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. />-N H s o

Подробнее
05-03-2014 дата публикации

Novel compound useful for the treatment of degenerative and inflammatory diseases

Номер: EP2702058A1
Принадлежит: GALAPAGOS NV

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed,as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolite thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hyper secretion of IL6.

Подробнее
30-07-2015 дата публикации

Benzimidazole derivatives and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Номер: WO2015110378A1
Принадлежит: GALAPAGOS NV

The present invention discloses compounds according to Formula (I) wherein Cy, R 1 , L 1 R 3 , R 4 , R 5 , L a, and R a are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

Подробнее
08-05-2012 дата публикации

5-phenyl-[1,2,4 ]triazolo[1,5-a]pyridin-2-yl carboxamides as jak inhibitors.

Номер: MX2011013450A
Принадлежит: GALAPAGOS NV

Se revela un nuevo compuesto capaz de inhibir JAK; este compuesto puede prepararse como una composición farmacéutica, y puede usarse para la prevención y el tratamiento de una diversidad de afecciones en mamíferos, que incluyen humanos, que abarcan, a modo de ejemplo, sin limitación, afecciones inflamatorias, enfermedades autoinmunitarias, enfermedades proliferativas, rechazo de trasplantes, enfermedades que involucran el deterioro del recambio de cartílago, malformaciones congénitas del cartílago y enfermedades asociadas con la hipersecreción de IL6.

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09-02-2012 дата публикации

NEW USEFUL COMPOUND FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES

Номер: CR20120016A
Принадлежит: GALAPAGOS NV, Heinz Co H J

Se revela un nuevo compuesto capaz de inhibir JAK; este compuesto puede prepararse como una composición farmacéutica, y puede usarse para la prevención y el tratamiento de una diversidad de afecciones en mamíferos, que incluyen humanos, que abarcan, a modo de ejemplo, sin limitación, afecciones inflamatorias, enfermedades autoinmunitarias, rechazo de trasplantes, etc.

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15-02-2024 дата публикации

Compounds for the treatment of pain, in particular neuropathic pain, and/or other diseases or disorders that are associated with at2r and/or at2r mediated signaling

Номер: AU2022318349A1
Принадлежит: Confo Therapeutics N V

The present invention relates to compounds that can be used for the prevention, treatment and/or management of pain, in particular chronic pain, such as neuropathic pain, and/or other diseases or disorders that are associated with AT2R and/or AT2R-mediated signaling.

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16-01-2024 дата публикации

COMPOSTOS PIRAZOLO[3,4-b]PIRIDIN-6-CARBOXAMIDA N-SULFONILADA, COMPOSIÇÃO FARMACÊUTICA CONTENDO OS DITOS COMPOSTOS E USOS DOS MESMOS PARA TRATAR FIBROSE CÍSTICA

Номер: BR112018007161B1
Принадлежит: Abbvie Global Enterprises Ltd, GALAPAGOS NV

pirazolo[3,4-b]piridin-6-carboxamidas n-sulfoniladas e métodos de uso. a presente invenção proporciona compostos de fórmula (i) (i) caracterizado. pelo fato de que r1, r2, r3, r4, r5, e r6 têm qualquer um dos valores definidos no relatório descritivo, e os seus sais farmaceuticamente aceitáveis, que são úteis como agentes no tratamento de doenças e condições mediadas e moduladas por cftr, incluindo fibrose cística, síndrome de sjögren, insuficiência pancreática, doença pulmonar obstrutiva crônica, e doença obstrutiva crônica das vias aéreas. são também proporcionadas composições farmacêuticas compostas por um ou mais compostos de fórmula (i).

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02-02-2023 дата публикации

Compounds for the treatment of pain, in particular neuropathic pain, and/or other diseases or disorders that are associated with at2r and/or at2r mediated signaling

Номер: CA3227194A1
Принадлежит: Confo Therapeutics NV

The present invention relates to compounds that can be used for the prevention, treatment and/or management of pain, in particular chronic pain, such as neuropathic pain, and/or other diseases or disorders that are associated with AT2R and/or AT2R-mediated signaling.

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24-03-2022 дата публикации

Ν-σουλφονυλιωμενα πυραζολο[3,4-β]πυριδιν-6-καρβοξαμιδια και μεθοδος χρησης

Номер: CY1123545T1
Принадлежит: Abbvie Overseas S.A R.L.

Η παρούσα εφεύρεση παρέχει ενώσεις του τύπου (Ι) όπου τα R1, R2, R3, R4, R5, και R6 έχουν οποιαδήποτε από τις τιμές ορίζονται στην περιγραφή και φαρμακευτικά αποδεκτά άλατα αυτών, που χρησιμεύουν ως παράγοντες στη θεραπεία νόσων και καταστάσεων που διαμεσολαβούνται και τροποποιούνται από CFTR, όπου συμπεριλαμβάνονται κυστική ίνωση, σύνδρομο Sjögren, παγκρεατική ανεπάρκεια, χρόνια αποφρακτική πνευμονοπάθεια και χρόνια αποφρακτική των αεροφόρων οδών νόσος. Επίσης παρέχονται φαρμακευτικές συνθέσεις που περιλαμβάνουν μία ή περισσότερες ενώσεις του τύπου (Ι).

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29-04-2024 дата публикации

Compuestos para el tratamiento del dolor, en particular el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con at2r y/o señalización mediada por at2r

Номер: CO2024000880A2
Принадлежит: Confo Therapeutics N V

La presente invención se relaciona con compuestos que se pueden usar para la prevención, tratamiento y/o manejo del dolor, en particular el dolor crónico, tal como el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con AT2R y/o señalización mediada por AT2R.

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05-06-2024 дата публикации

Compounds for the treatment of pain, in particular neuropathic pain, and/or other diseases or disorders that are associated with at2r and/or at2r mediated signaling

Номер: EP4377307A1
Принадлежит: Confo Therapeutics NV

The present invention relates to compounds that can be used for the prevention, treatment and/or management of pain, in particular chronic pain, such as neuropathic pain, and/or other diseases or disorders that are associated with AT2R and/or AT2R-mediated signaling.

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30-04-2024 дата публикации

Compuestos para el tratamiento del dolor, en particular el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con at2r y/o señalización mediada por at2r

Номер: ECSP24007288A
Принадлежит: Confo Therapeutics N V

La presente invención se relaciona con compuestos que se pueden usar para la prevención, tratamiento y/o manejo del dolor, en particular el dolor crónico, tal como el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con AT2R y/o señalización mediada por AT2R.

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16-06-2024 дата публикации

Compuestos para el tratamiento del dolor, en particular el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con at2r y/o señalización mediada por at2r

Номер: DOP2024000017A
Принадлежит: Confo Therapeutics NV

La presente invención se relaciona con compuestos que se pueden usar para la prevención, tratamiento y/o manejo del dolor, en particular el dolor crónico, tal como el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con AT2R y/o señalización mediada por AT2R.

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04-06-2024 дата публикации

Compuestos para el tratamiento del dolor, en particular el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con AT2R y/o señalización mediada por AT2R

Номер: CR20240041A
Принадлежит: Confo Therapeutics N V

La presente invención se relaciona con compuestos que se pueden usar para la prevención, tratamiento y/o manejo del dolor, en particular el dolor crónico, tal como el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con AT2R y/o señalización mediada por AT2R.

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01-07-2024 дата публикации

Compuestos para el tratamiento del dolor, en particular el dolor neuropatico, y/u otras enfermedades o trastornos que se asocian con at2r y/o se?alizacion mediada por at2r.

Номер: MX2024001155A
Принадлежит: Confo Therapeutics N V

La presente invención se relaciona con compuestos que se pueden usar para la prevención, tratamiento y/o manejo del dolor, en particular el dolor crónico, tal como el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con AT2R y/o señalización mediada por AT2R.

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23-08-2024 дата публикации

Compuestos para el tratamiento del dolor, en particular el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con at2r y/o señalización mediada por at2r.

Номер: CL2024000230A1
Принадлежит: Confo Therapeutics N V

La presente invención se relaciona con compuestos que se pueden usar para la prevención, tratamiento y/o manejo del dolor, en particular el dolor crónico, tal como el dolor neuropático, y/u otras enfermedades o trastornos que se asocian con AT2R y/o señalización mediada por AT2R.

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23-07-2024 дата публикации

Compound useful for the treatment of degenerative and inflammatory diseases

Номер: US12042498B2
Принадлежит: Alfasigma Spa

A novel compound able to inhibit JAK is disclosed, that comprises a compound of Formula I:The compound may be prepared as a pharmaceutical composition, and may be used for the treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

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05-06-2018 дата публикации

Compound useful for the treatement of degenerative and inflammatory diseases

Номер: US09987272B2
Принадлежит: GALAPAGOS NV

A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

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13-02-2018 дата публикации

N-sulfonylated pyrazolo[3,4-b]pyridin-6-carboxamides and method of use

Номер: US09890158B2
Принадлежит: AbbVie SARL, GALAPAGOS NV

The present invention provides for compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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16-01-2018 дата публикации

Compounds and pharmaceutical compositions thereof for the treatment of cystic fibrosis

Номер: US09867806B2
Принадлежит: GALAPAGOS NV

The present invention discloses compounds according to Formula I: wherein R 1 , R 2 , R 3 , L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.

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24-10-2017 дата публикации

Substituted pyrazolo[3,4-b]pyridin-6-carboxylic acids and method of use

Номер: US09796711B2
Принадлежит: AbbVie SARL, GALAPAGOS NV

The present invention provides for compounds of formula (I) wherein R 1 , R 2 , R 3 , and R 4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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18-07-2017 дата публикации

Compound useful for the treatment of degenerative and inflammatory diseases

Номер: US09707237B2
Принадлежит: GALAPAGOS NV

A novel compound able to inhibit JAK is disclosed, that comprises a compound according to Formula I: or a pharmaceutically acceptable salt thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

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29-11-2016 дата публикации

Compound useful for the treatment of degenerative and inflammatory diseases

Номер: US09505754B2
Принадлежит: GALAPAGOS NV

A compound is disclosed that has a formula represented by the following: This compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.

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07-11-2024 дата публикации

Compounds for the Treatment of Pain, in Particular, Neuropathic Pain, and/or Other Diseases or Disorders that are Associated with AT2R and/or AT2R Mediated Signaling

Номер: US20240368133A1
Принадлежит: Confo Therapeutics NV

The present invention relates to compounds that can be used for the prevention, treatment and/or management of pain, in particular chronic pain, such as neuropathic pain, and/or other diseases or disorders that are associated with AT2R and/or AT2R-mediated signaling.

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13-09-2016 дата публикации

Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Номер: US09440929B2
Принадлежит: GALAPAGOS NV

The present invention discloses compounds according to Formula I: wherein Cy, R 1 , L 1 , R 3 , R 4 , R 5 , L a , and R a are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

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