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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 39. Отображено 39.
15-11-2012 дата публикации

NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES

Номер: US20120289496A1
Принадлежит: Rhizen Pharmaceuticals SA

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. 2. A compound of claim 1 , wherein R is independently selected from halogen claim 1 , cyano claim 1 , substituted or unsubstituted Calkyl claim 1 , substituted or unsubstituted alkoxy claim 1 , substituted or unsubstituted Calkenyl claim 1 , substituted or unsubstituted Calkynyl claim 1 , substituted or unsubstituted Ccycloalkyl claim 1 , and substituted or unsubstituted heterocyclic group.3. A compound of claim 2 , wherein R is fluoro claim 2 , methyl claim 2 , methoxy or morpholine.4. A compound of claim 1 , wherein Cyis selected from substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl.6. A compound of claim 1 , wherein Rand Rindependently represent hydrogen or substituted or unsubstituted Calkyl.7. A compound of claim 1 , wherein Lis absent or selected from S(═O)— or —NR—.8. A compound of claim 7 , wherein q is 0 claim 7 , Lis absent or Lis —NH—.9. A compound of claim 1 , wherein Cyis selected from substituted or unsubstituted heterocyclic group and substituted or unsubstituted heteroaryl.15. A compound of claim 10 , wherein Ris hydrogen claim 10 , halogen claim 10 , cyano claim 10 , substituted or unsubstituted alkyl claim 10 , substituted or unsubstituted alkynyl claim 10 , substituted or unsubstituted heterocyclyl claim 10 , substituted or unsubstituted aryl claim 10 , or substituted or unsubstituted heteroaryl.18. A compound of claim 13 , wherein each of R′ and R″ is selected from hydrogen or Calkyl claim 13 , or —NR′R″ together are joined to form a substituted or unsubstituted claim 13 , saturated or unsaturated 3-10 membered ring claim 13 , which may optionally include heteroatoms which may be the same or different and are selected from O claim 13 , NR(wherein Ris hydrogen or substituted or ...

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04-02-2021 дата публикации

NOVEL GLUTAMINASE INHIBITORS

Номер: US20210032236A1
Принадлежит:

The present disclosure provides compounds of formula (I) to (III) as glutaminase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders involving glutamine. 9. A compound of claim 1 , wherein P and Q are each independently selected from —NRC(═O)—(CRR)— claim 1 , —(CRR)—C(═O)—NR— claim 1 , —C(═O)NR—(CRR)— claim 1 , —(CRR)—NR—C(═O)— claim 1 , —NH—C(═O)—C(RR)— claim 1 , —(CRR)—C(═O)—NH— claim 1 , —NRC(═O)— claim 1 , —NRC(═S)— claim 1 , —NRS(═O)— claim 1 , —C(═O)NR— claim 1 , —C(═S)NR— claim 1 , or —NR—.10. A compound of claim 1 , wherein P and Q are each independently selected from —NRC(═O)—(CRR)— claim 1 , —(CRR)—C(═O)—NRC(═O)— or —NR— claim 1 , wherein Rand R are independently selected from hydrogen claim 1 , substituted or unsubstituted Calkyl claim 1 , halogen claim 1 , hydroxy and substituted or unsubstituted Calkoxy.11. A compound of claim 1 , wherein P and Q are each independently selected from —NH—C(═O)—(CRR)— claim 1 , —(CRR)—C(═O)—NH— claim 1 , —NH—C(═O)— or —NH— claim 1 , wherein Rand Rare hydrogen.12. A compound of claim 1 , wherein{'sub': 2', '2, '(i) each of P and Q are independently —NH—C(═O)—(CH)—, —(CH)—C(═O)—NH—, —NH—C(═O)— or —NH—;'}{'sub': 2', '2, '(ii) P is —(CH)—C(═O)—NH— and Q is —NH—C(═O)—CH—, —NH—C(═O)— or —NH—;'}{'sub': 2', '2, '(iii) P is —(CH)—C(═O)—NH—, —NH—C(═O)— or —NH— and Q is —NH—C(═O)—CH—; or'}{'sub': 2', '2, '(iv) P is —(CH)—C(═O)—NH— and Q is —NH—C(═O)—CH—.'}13. A compound of claim 1 , wherein both P and Q are independently selected from —NH—C(═O)—CH— or —CH—C(═O)—NH—.15. A compound of claim 1 , wherein{'sub': 1', '1-6', '1-3, 'sup': x', 'x, 'Lis absent, substituted or unsubstituted Calkyl or NR, wherein Ris hydrogen or Calkyl;'}{'sub': '2', 'Lis substituted or unsubstituted 3 to 10 membered heterocyclyl; and'}{'sub': 3', '1-6', '1-3, 'sup': x', 'x, 'Lis absent, substituted or unsubstituted Calkyl or NR, wherein Ris hydrogen ...

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04-02-2021 дата публикации

DUAL SELECTIVE PI3 DELTA AND GAMMA KINASE INHIBITORS

Номер: US20210032248A1
Принадлежит:

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them. 121-. (canceled)22. A method of treating T-cell lymphoma in a patient in need thereof , the method comprising administering to the patient an effective amount of 2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof.23. A method of treating T-cell lymphoma in a patient in need thereof , the method comprising administering to the patient an effective amount of (S)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof.24. A method of treating T-cell lymphoma in a patient in need thereof , the method comprising administering to the patient an effective amount of a compound that is (S)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof , wherein the compound contains less than about 5% by weight of (R)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof.25. The method of claim 24 , wherein the compound contains less than about 2.5% by weight of (R)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof.26. The method of claim 24 , wherein the compound contains less than about 1% by weight of (R)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof.27. The method of claim 24 , wherein the compound contains less than about 0.1% by weight of (R)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof.28. The method of claim 22 , wherein the patient is a human patient.29. The ...

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26-02-2015 дата публикации

NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5- DISUBSTITUTED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF C-MET PROTEIN, ETC

Номер: US20150057309A1
Принадлежит:

The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them. 145-. (canceled)48. A compound of claim 46 , wherein Cyis substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.51. A compound of claim 46 , wherein Lis —CRR—.52. A compound of claim 51 , wherein Lis —CH— claim 51 , —CH(OH)— claim 51 , —CHF— claim 51 , —CF— claim 51 , —CH(CH)— or —C(CH)—.53. A compound of claim 46 , wherein Lis —CH.56. A compound of claim 47 , wherein Xand Xare CRand Xis independently selected from —CR═CRand —S—.57. A compound of claim 56 , wherein Xis CH claim 56 , Xis CRand Xis —CR═CR claim 56 , wherein Ris hydrogen claim 56 , halogen or substituted or unsubstituted Calkyl.62. A compound of claim 60 , wherein each occurrence of Ris selected from hydrogen claim 60 , halogen and substituted or unsubstituted alkyl.63. A compound of claim 54 , wherein each occurrence of Ris selected from hydrogen claim 54 , fluoro claim 54 , chloro claim 54 , methyl and CFand each occurrence of Ris selected from hydrogen and fluoro.64. A compound of claim 46 , wherein each of Rand Ris hydrogen claim 46 , alkyl or halogen claim 46 , X is N or CRand Ris H claim 46 , substituted or unsubstituted Calkyl claim 46 , NH claim 46 , OH claim 46 , CN or CONH.65. A compound of claim 46 , wherein(a) X is N;{'sup': '2', '(b) Ris H;'}{'sup': a', 'b, 'claim-text': [{'sup': a', 'b, '(ii) Ris methyl and Ris hydrogen,'}, {'sup': a', 'b, '(iii) Ris fluoro and Ris hydrogen,'}, {'sup': a', 'b, '(iv) Rand Rboth are fluoro, or'}, {'sup': a', 'b, '(v) Rand Rboth are methyl; and'}], '(c) (i) both Rand Rare hydrogen,'}{'sup': 'c', '(d) Z is CR, N, S, O, HC═CH— or —N═CH—;'}{'sub': '1', '(e) Zis CH or N;'}{'sub': '2', '(f) Zis C; and'}{'sub': '3', '(g) Zis C or N.'}66. A compound of claim 54 , wherein{'sub': ...

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01-03-2018 дата публикации

NOVEL GLUTAMINASE INHIBITORS

Номер: US20180057487A1
Принадлежит:

The present disclosure provides compounds of formula (I) to (III) as glutaminase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders involving glutamine. 9. (canceled)10. A compound of claim 1 , wherein P and Q are each independently selected from —NRC(═O)—(CRR)— claim 1 , —(CRR)—C(═O)—NR— claim 1 , —NRC(═O)— or —NR— claim 1 , wherein Rand Rare independently selected from hydrogen claim 1 , substituted or unsubstituted Calkyl claim 1 , halogen claim 1 , hydroxy and substituted or unsubstituted Calkoxy.11. A compound of claim 1 , wherein P and Q are each independently selected from —NH—C(═O)—(CRR)— claim 1 , —(CRR)—C(═O)—NH— claim 1 , —NH—C(═O)— or —NH— claim 1 , wherein Rand Rare hydrogen.12. A compound of claim 1 , wherein{'sub': 2', '2, '(i) each of P and Q are independently —NH—C(═O)—(CH)—, —(CH)—C(═O)—NH—, —NH—C(═O)— or —NH—;'}{'sub': 2', '2, '(ii) P is —(CH)—C(═O)—NH— and Q is —NH—C(═O)—CH—, —NH—C(═O)— or —NH—;'}{'sub': 2', '2, '(iii) P is —(CH)—C(═O)—NH—, —NH—C(═O)— or —NH— and Q is —NH—C(═O)—CH—; or'}{'sub': 2', '2, '(iv) P is —(CH)—C(═O)—NH— and Q is —NH—C(═O)—CH—.'}13. A compound of claim 1 , wherein both P and Q are independently selected from —NH—C(═O)—CH— or —CH—C(═O)—NH—.15. A compound of claim 1 , wherein{'sub': 1', '1-6', '1-3, 'sup': x', 'x, 'Lis absent, substituted or unsubstituted Calkyl or NR, wherein Ris hydrogen or Calkyl;'}{'sub': '2', 'Lis substituted or unsubstituted 3 to 10 membered heterocyclyl; and'}{'sub': 3', '1-6', '1-3, 'sup': x', 'x, 'Lis absent, substituted or unsubstituted Calkyl or NR, wherein Ris hydrogen or Calkyl.'}16. A compound of claim 1 , wherein{'sub': 1', '1-6, 'Lis absent or substituted or unsubstituted Calkyl;'}{'sub': '2', 'Lis substituted or unsubstituted 3 to 10 membered heterocyclyl; and'}{'sub': 3', '1-6, 'Lis absent or substituted or unsubstituted Calkyl.'}17. (canceled)18. (canceled)19. A compound of ...

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15-03-2018 дата публикации

NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5-DISUBSTITUTED-3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF C-MET PROTEIN KINASES

Номер: US20180072721A1
Принадлежит:

The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them. 3. A compound of claim 1 , wherein Cyis substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.5. (canceled)6. A compound of claim 1 , wherein Lis —CRR—.7. A compound of claim 6 , wherein Lis —CH— claim 6 , —CH(OH)— claim 6 , —CHF— claim 6 , —CF— claim 6 , —CH(CH)— or —C(CH)—.8. (canceled)11. A compound of claim 2 , wherein Xand Xare CRand Xis independently selected from —CR═CRand —S—.12. (canceled)14. (canceled)1719-. (canceled)20. A compound of claim 9 , wherein{'sup': a', 'b, 'each of Rand Ris hydrogen, alkyl or halogen; and'}{'sup': 'c', 'Ris hydrogen or fluoro.'}21. (canceled)22. A compound of claim 9 , wherein{'sup': 'c', 'Z is CR, N, S, O, —HC═CH— or —N═CH—;'}{'sub': '1', 'Zis CH or N;'}{'sub': '2', 'Zis C; and'}{'sub': '3', 'Zis C or N.'}2324-. (canceled)25. A compound of claim 9 , wherein X is N or CRand Ris H claim 9 , substituted or unsubstituted Calkyl claim 9 , NH claim 9 , OH claim 9 , CN or CONH.2630-. (canceled)31. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.32. The pharmaceutical composition of claim 31 , further comprising one or more additional therapeutic agents and mixtures thereof.33. The pharmaceutical composition of claim 32 , wherein the one or more additional therapeutic agent is an anti-cancer agent claim 32 , anti-inflammatory agent claim 32 , immunosuppressive agent claim 32 , steroid claim 32 , non-steroidal anti-inflammatory agent claim 32 , antihistamine claim 32 , analgesic claim 32 , or a mixture thereof.3435-. (canceled)36. A method of inhibiting the HGF/c-Met kinase signaling pathway in a cell comprising contacting said cell with a compound of .37. A method of inhibiting the proliferative ...

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11-04-2019 дата публикации

SUBSTITUTED CHROMENONES AS MODULATORS OF PROTEIN KINASES

Номер: US20190105324A9
Принадлежит:

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. 2. A compound of claim 1 , wherein R is independently selected from halogen claim 1 , cyano claim 1 , substituted or unsubstituted Calkyl claim 1 , substituted or unsubstituted alkoxy claim 1 , substituted or unsubstituted Calkenyl claim 1 , substituted or unsubstituted Calkynyl claim 1 , substituted or unsubstituted Ccycloalkyl claim 1 , and substituted or unsubstituted heterocyclic group.3. A compound of claim 2 , wherein R is fluoro claim 2 , methyl claim 2 , methoxy or morpholine.4. A compound of claim 1 , wherein Cyis selected from substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl.6. A compound of claim 1 , wherein Rand Rindependently represent hydrogen or substituted or unsubstituted Calkyl.7. A compound of claim 1 , wherein Li is absent or selected from S(═O)— or —NR—.8. A compound of claim 7 , wherein q is 0 claim 7 , Lis absent or Lis —NH—.9. A compound of claim 1 , wherein Cyis selected from substituted or unsubstituted heterocyclic group and substituted or unsubstituted heteroaryl.15. A compound of claim 10 , wherein Ris hydrogen claim 10 , halogen claim 10 , cyano claim 10 , substituted or unsubstituted alkyl claim 10 , substituted or unsubstituted alkynyl claim 10 , substituted or unsubstituted heterocyclyl claim 10 , substituted or unsubstituted aryl claim 10 , or substituted or unsubstituted heteroaryl.18. A compound of claim 13 , wherein each of R′ and R″ is selected from hydrogen or Calkyl claim 13 , or —NR′R″ together are joined to form a substituted or unsubstituted claim 13 , saturated or unsaturated 3-10 membered ring claim 13 , which may optionally include heteroatoms which may be the same or different and are selected from O claim 13 , NR(wherein Ris hydrogen or substituted or ...

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26-04-2018 дата публикации

NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES

Номер: US20180110783A1
Принадлежит:

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. 2. A compound of claim 1 , wherein R is independently selected from halogen claim 1 , cyano claim 1 , substituted or unsubstituted Calkyl claim 1 , substituted or unsubstituted alkoxy claim 1 , substituted or unsubstituted Calkenyl claim 1 , substituted or unsubstituted Calkynyl claim 1 , substituted or unsubstituted Ccycloalkyl claim 1 , and substituted or unsubstituted heterocyclic group.3. A compound of claim 2 , wherein R is fluoro claim 2 , methyl claim 2 , methoxy or morpholine.4. A compound of claim 1 , wherein Cyis selected from substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl.6. A compound of claim 1 , wherein Rand Rindependently represent hydrogen or substituted or unsubstituted Calkyl.7. A compound of claim 1 , wherein Li is absent or selected from S(═O)— or —NR—.8. A compound of claim 7 , wherein q is 0 claim 7 , Lis absent or Lis —NH—.9. A compound of claim 1 , wherein Cyis selected from substituted or unsubstituted heterocyclic group and substituted or unsubstituted heteroaryl.15. A compound of claim 10 , wherein Ris hydrogen claim 10 , halogen claim 10 , cyano claim 10 , substituted or unsubstituted alkyl claim 10 , substituted or unsubstituted alkynyl claim 10 , substituted or unsubstituted heterocyclyl claim 10 , substituted or unsubstituted aryl claim 10 , or substituted or unsubstituted heteroaryl.18. A compound of claim 13 , wherein each of R′ and R″ is selected from hydrogen or Calkyl claim 13 , or —NR′R″ together are joined to form a substituted or unsubstituted claim 13 , saturated or unsaturated 3-10 membered ring claim 13 , which may optionally include heteroatoms which may be the same or different and are selected from O claim 13 , NR(wherein Ris hydrogen or substituted or ...

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20-07-2017 дата публикации

SELECTIVE DUAL INHIBITORS OF PI3 DELTA AND GAMMA PROTEIN KINASES

Номер: US20170204106A1
Принадлежит:

The present invention relates to a selective dual delta (δ) and gamma (γ) PI3K protein kinase modulator (S)-N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them. 126-. (canceled)27. A method of inhibiting a catalytic activity of a PI3 δ kinase in a cell , comprising contacting the cell with an effective amount of (S)-N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-3-y1)-2-methoxyphenyl)methanesulfonamide or a pharmaceutically acceptable salt thereof.28. A method of inhibiting a catalytic activity of a PI3 γ kinase in a cell , comprising contacting the cell with an effective amount of (S)-N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-3-y1)-2-methoxyphenyl)methanesulfonamide or a pharmaceutically acceptable salt thereof.29. A method of inhibiting a catalytic activity of a PI3δ kinase and PI3γ kinase in a cell , comprising contacting the cell with an effective amount of (S)-N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-3-y1)-2-methoxyphenyl)methanesulfonamide or a pharmaceutically acceptable salt thereof.30. The method of claim 27 , wherein the inhibition takes place in a subject suffering from a disease claim 27 , disorder or condition selected from a proliferative disease claim 27 , a bone disorder claim 27 , an inflammatory disease claim 27 , an immune disease claim 27 , a nervous system disease claim 27 , a metabolic disease claim 27 , a respiratory disease claim 27 , thrombosis claim 27 , and cardiac disease.31. A method of treating leukemia in a patient in need thereof claim 27 , comprising administering to the ...

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25-06-2020 дата публикации

SELECTIVE DUAL INHIBITORS OF PI3 DELTA AND GAMMA PROTEIN KINASES

Номер: US20200199133A1
Принадлежит:

The present invention relates to a selective dual delta (δ) and gamma (γ) PI3K protein kinase modulator (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them. 126-. (canceled)30. A pharmaceutical composition comprising a compound according to and at least one pharmaceutically acceptable carrier.31. A pharmaceutical composition comprising a compound according to and at least one pharmaceutically acceptable carrier.32. A pharmaceutical composition comprising a compound according to and at least one pharmaceutically acceptable carrier.33. A method of treating asthma or chronic obstructive pulmonary disease in a patient in need thereof claim 27 , the method comprising administering to the patient an effective amount of a compound of .34. A method of treating asthma or chronic obstructive pulmonary disease in a patient in need thereof claim 28 , the method comprising administering to the patient an effective amount of a compound of .35. A method of treating asthma or chronic obstructive pulmonary disease in a patient in need thereof claim 29 , the method comprising administering to the patient an effective amount of a compound of .36. A method of treating rheumatoid arthritis claim 27 , psoriasis claim 27 , lupus or experimental autoimmune encephalomyelitis (EAE) in a patient in need thereof claim 27 , the method comprising administering to the patient an effective amount of a compound of .37. A method of treating rheumatoid arthritis claim 28 , psoriasis claim 28 , lupus or experimental autoimmune encephalomyelitis (EAE) in a patient in need thereof claim 28 , the method comprising administering to the patient an effective amount of a compound of .38. A method of treating rheumatoid arthritis ...

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04-07-2019 дата публикации

SELECTIVE DUAL INHIBITORS OF PI3 DELTA AND GAMMA PROTEIN KINASES

Номер: US20190202836A1
Принадлежит:

The present invention relates to a selective dual delta (δ) and gamma (γ) PI3K protein kinase modulator (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them. 126-. (canceled)27. A method of inhibiting a catalytic activity of a PI3 δ kinase in a cell comprising contacting the cell with an effective amount of (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-3-yl)-2-methoxyphenyl)methanesulfonamide or a pharmaceutically acceptable salt thereof.28. A method of inhibiting a catalytic activity of a PI3 γ kinase in a cell comprising contacting the cell with an effective amount of (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-3-yl)-2-methoxyphenyl)methanesulfonamide or a pharmaceutically acceptable salt thereof.29. A method of inhibiting a catalytic activity of a PI3 δ kinase and PI3 γ kinase in a cell comprising contacting the cell with an effective amount of (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-3-yl)-2-methoxyphenyl)methanesulfonamide or a pharmaceutically acceptable salt thereof.30. The method of claim 27 , wherein the inhibition takes place in a subject suffering from a disease claim 27 , disorder or condition selected from a proliferative disease claim 27 , a bone disorder claim 27 , an inflammatory disease claim 27 , an immune disease claim 27 , a nervous system disease claim 27 , a metabolic disease claim 27 , a respiratory disease claim 27 , thrombosis claim 27 , cardiac disease claim 27 , and any combination thereof.31. The method of claim 28 , wherein the inhibition takes place in a subject ...

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11-12-2014 дата публикации

DUAL SELECTIVE PI3 DELTA AND GAMMA KINASE INHIBITORS

Номер: US20140364447A1
Принадлежит:

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them. 1. A compound selected from 2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one and pharmaceutically acceptable salts thereof.2. A compound selected from (S)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one and pharmaceutically acceptable salts thereof.3. The compound according to claim 2 , wherein the compound is substantially free of (R)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one claim 2 , and pharmaceutical acceptable salts thereof.4. The compound of claim 2 , wherein the compound has an enantiomeric excess greater than about 95%.5. (S)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one.6. The compound of claim 5 , wherein the compound is substantially free of (R)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one.7. The compound of claim 5 , wherein the compound has an enantiomeric excess greater than about 95%.8. A pharmaceutical composition comprising a compound of and at least one pharmaceutically acceptable carrier.9. A method of inhibiting a catalytic activity of a PI3 δ kinase present in a cell claim 2 , comprising contacting the cell with an effective amount of a compound of .10. A method of inhibiting a catalytic activity of a PI3 γ kinase present in a cell claim 2 , comprising contacting the cell with an effective amount of a compound of .11. A method of inhibiting a catalytic activity of a PI3 δ kinase and PI3 γ kinase present in a cell claim 2 , comprising contacting the cell with an effective amount of a compound of .12. The method of claim 9 , wherein the inhibition takes place in a subject suffering from a disease claim 9 , disorder or condition selected from cancer claim 9 , a ...

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19-09-2019 дата публикации

NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES

Номер: US20190282581A1
Принадлежит:

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. 137-. (canceled)38. A method of inhibiting a catalytic activity of a phosphoinositol 3-kinase present in a cell comprising contacting the cell with an effective amount of a compound selected from 2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3 ,4-d]pyrimidin-1-yl)ethyl)-5-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt , N-oxide or tautomer thereof.39. The method of claim 38 , wherein the inhibition takes place in a subject suffering from a disease or disorder selected from cancer claim 38 , a bone disorder claim 38 , an inflammatory disease claim 38 , an immune disease claim 38 , a nervous system disease claim 38 , a metabolic disease claim 38 , a respiratory disease claim 38 , thrombosis claim 38 , and a cardiac disease.40. A method of treating asthma in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a compound selected from 2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3 claim 38 ,4-d]pyrimidin-1-yl) ethyl)-5-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt claim 38 , N-oxide or tautomer thereof.41. A method of treating chronic obstructive pulmonary disease in a subject claim 38 , comprising administering to the subject in need thereof a therapeutically effective amount of a compound selected from 2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3 claim 38 ,4-d]pyrimidin-1-yl) ethyl)-5-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt claim 38 , N-oxide or tautomer thereof.42. A method of inhibiting a catalytic activity of a phosphoinositol 3-kinase present in a cell claim 38 , comprising contacting the cell with an effective amount of a ...

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12-11-2015 дата публикации

NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES

Номер: US20150320752A1
Принадлежит:

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. 124-. (canceled)26. The method of claim 25 , wherein the inhibition takes place in a subject suffering from a disease or disorder which is cancer claim 25 , bone disorder claim 25 , inflammatory disease claim 25 , immune disease claim 25 , nervous system disease claim 25 , metabolic disease claim 25 , respiratory disease claim 25 , thrombosis claim 25 , or cardiac disease.2728-. (canceled)30. A method of claim 29 , further comprising the step of administering simultaneously or sequentially to a subject in need thereof at least one other anti-cancer agent claim 29 , anti-inflammatory agent claim 29 , immunosuppressive agent claim 29 , steroid claim 29 , non-steroidal anti-inflammatory agent claim 29 , antihistamine claim 29 , analgesic claim 29 , or a mixture thereof.31. A method of claim 29 , wherein the PI3K associated disease claim 29 , disorder or condition is an immune system-related disease claim 29 , a disease or disorder involving inflammation claim 29 , cancer or other proliferative disease claim 29 , a hepatic disease or disorder claim 29 , or a renal disease or disorder.32. A method of claim 29 , wherein the PI3K associated disease claim 29 , disorder or condition is selected from inflammation claim 29 , glomerulonephritis claim 29 , uveitis claim 29 , hepatic diseases or disorders claim 29 , renal diseases or disorders claim 29 , chronic obstructive pulmonary disease claim 29 , rheumatoid arthritis claim 29 , inflammatory bowel disease claim 29 , vasculitis claim 29 , dermatitis claim 29 , osteoarthritis claim 29 , inflammatory muscle disease claim 29 , allergic rhinitis claim 29 , vaginitis claim 29 , interstitial cystitis claim 29 , scleroderma claim 29 , osteoporosis claim 29 , eczema claim 29 , allogeneic or ...

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03-11-2016 дата публикации

NOVEL GLUTAMINASE INHIBITORS

Номер: US20160318921A1
Принадлежит:

The present disclosure provides compounds of formula (I) to (III) as glutaminase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders involving glutamine. 9. A compound of claim 1 , wherein P and Q are each independently selected from —NRC(═O)—(CRR)— claim 1 , —(CRR)—C(═O)—NR— claim 1 , —C(═O)NR—(CRR)— claim 1 , —(CRR)—NR—C(═O)— claim 1 , —NH—C(═O)—C(RR)— claim 1 , —(CRR)—C(═O)—NH— claim 1 , —NRC(═O)— claim 1 , —NRC(═S)— claim 1 , —NRS(═O)— claim 1 , —C(═O)NR— claim 1 , —C(═S)NR— claim 1 , or —NR—.10. A compound of claim 1 , wherein P and Q are each independently selected from —NRC(═O)—(CRR)— claim 1 , —(CRR)—C(═O)—NR claim 1 , —NRC(═O)— or —NR— claim 1 , wherein Rand Rare independently selected from hydrogen claim 1 , substituted or unsubstituted Calkyl claim 1 , halogen claim 1 , hydroxy and substituted or unsubstituted Calkoxy.11. A compound of claim 1 , wherein P and Q are each independently selected from —NH—C(═O)—(CRR)— claim 1 , —(CRR)—C(═O)—NH— claim 1 , —NH—C(═O)— or —NH— claim 1 , wherein Rand Rare hydrogen.12. A compound of claim 1 , wherein{'sub': 2', '2, '(i) each of P and Q are independently —NH—C(═O)—(CH)—, —(CH)—C(═O)—NH—, —NH—C(═O)— or —NH—;'}{'sub': 2', '2, '(ii) P is —(CH)—C(═O)—NH— and Q is —NH—C(═O)—CH—, —NH—C(═O)— or —NH—;'}{'sub': 2', '2, '(iii) P is —(CH)—C(═O)—NH—, —NH—C(═O)— or —NH— and Q is —NH—C(═O)—CH—; or'}{'sub': 2', '2, '(iv) P is —(CH)—C(═O)—NH— and Q is —NH—C(═O)—CH—.'}13. A compound of claim 1 , wherein both P and Q are independently selected from —NH—C(═O)—CH— or —CH—C(═O)—NH—.15. A compound of claim 1 , wherein{'sub': 1', '1-6', '1-3, 'sup': x', 'x, 'Lis absent, substituted or unsubstituted Calkyl or NR, wherein Ris hydrogen or Calkyl;'}{'sub': '2', 'Lis substituted or unsubstituted 3 to 10 membered heterocyclyl; and'}{'sub': 3', '1-6', '1-3, 'sup': x', 'x, 'Lis absent, substituted or unsubstituted Calkyl or NR, wherein ...

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23-11-2017 дата публикации

DUAL SELECTIVE PI3 DELTA AND GAMMA KINASE INHIBITORS

Номер: US20170334914A1
Принадлежит:

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them. 1. A compound selected from 2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one and pharmaceutically acceptable salts thereof.2. A compound selected from (S)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one and pharmaceutically acceptable salts thereof.3. The compound according to claim 2 , wherein the compound is substantially free of (R)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one claim 2 , and pharmaceutical acceptable salts thereof.4. The compound of claim 2 , wherein the compound has an enantiomeric excess greater than about 95%.5. (S)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one.6. The compound of claim 5 , wherein the compound is substantially free of (R)-2-(1-(9H-purin-6-ylamino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one.7. The compound of claim 5 , wherein the compound has an enantiomeric excess greater than about 95%.8. A pharmaceutical composition comprising a compound of and at least one pharmaceutically acceptable carrier.9. A method of inhibiting a catalytic activity of a P13 δ kinase present in a cell claim 2 , comprising contacting the cell with an effective amount of a compound of .10. A method of inhibiting a catalytic activity of a P13 γ kinase present in a cell claim 2 , comprising contacting the cell with an effective amount of a compound of .11. A method of inhibiting a catalytic activity of a PI3 δ kinase and PI3 γ kinase present in a cell claim 2 , comprising contacting the cell with an effective amount of a compound of .12. The method of claim 9 , wherein the inhibition takes place in a subject suffering from a disease claim 9 , disorder or condition selected from cancer claim 9 , a ...

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31-12-2015 дата публикации

SELECTIVE DUAL INHIBITORS OF PI3 DELTA AND GAMMA PROTEIN KINASES

Номер: US20150376188A1
Принадлежит:

The present invention relates to a selective dual delta (δ) and gamma (γ) PI3K protein kinase modulator (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them. 1. A compound selected from N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-3-yl)-2-methoxyphenyl)methanesulfonamide and pharmaceutically acceptable salts thereof.3. A compound selected from (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-3-yl)-2-methoxyphenyl)methanesulfonamide and pharmaceutically acceptable salts thereof.4. The compound according to claim 3 , wherein the compound is substantially free of (R)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 claim 3 ,4-d]pyrimidin-3-yl)-2-methoxyphenyl)methanesulfonamide and pharmaceutically acceptable salt thereof.5. The compound of claim 3 , wherein the compound has an enantiomeric excess greater than about 95%.6. (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 claim 3 ,4-d]pyrimidin-3-yl)-2-methoxyphenyl)methanesulfonamide.7. The compound of claim 6 , wherein the compound is substantially free of (R)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3 claim 6 ,4-d]pyrimidin-3-yl)-2-methoxyphenyl)methanesulfonamide.8. The compound of claim 6 , wherein the compound has an enantiomeric excess greater than about 95%.9. A pharmaceutical composition comprising a compound according to and at least one pharmaceutically acceptable carrier.10. A method of inhibiting a catalytic activity of a PI3 δ kinase in a cell claim 1 , comprising contacting ...

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28-09-2021 дата публикации

New 3,5-disubstituted-3H-imidazo [4,5-B] biridine and 3,5-disubstituida-3H- [1,2,3] triazolo [4,5-B] pyridine compounds as protein kinase modulators C-MET

Номер: ES2856848T3
Принадлежит: Rhizen Pharmaceuticals Ag

Un compuesto de fórmula (IA-1) **(Ver fórmula)** o un tautómero, un estereoisómero, un enantiómero, diastereómero, una sal farmacéuticamente aceptable o un N- óxido del mismo; en donde X es CR1 o N; D es arilo monocíclico sustituido o heteroarilo monocíclico sustituido; en donde D está sustituido con un grupo E que se selecciona entre: **(Ver fórmula)** ; y además D puede estar opcionalmente sustituido con uno o más de Rz; L2 se selecciona entre -O-, -S(=O)q-, -NRa-, -(CRaRb)n-, -C(=Y)-, -C(=Y)-C(=Y)-, -CRaRb-C(=Y)-CRaRb-, -CRaRb-Y- CRaRb-, -C(=Y)-NRa-, -NRa-C(=Y)-NRa-, -S(=O)q-NRa-, -NRa-S(=O)q-NRa-, -NRa-NRa-; Cy2 se selecciona independientemente entre cicloalquilo sustituido o sin sustituir, grupo heterocíclico sustituido o sin sustituir, arilo sustituido o sin sustituir y heteroarilo sustituido o sin sustituir; cada aparición de R1 y R2 puede ser igual o diferente y se selecciona independientemente entre hidrógeno, nitro, hidroxi, ciano, halógeno, -ORa, -S(=O)q-Ra, -NRaRb, -C(=Y)-Ra, -CRaRb-C(=Y)-Ra, -CRaRb-Y-CRaRbRb, -C(=Y)- NRaRb, -NRaRb-C(=Y)-NRaRb, -S(=O)q-NRaRb-, -NRaRb-S(=O)q-NRaRb, -NRaRb-NRaRb, alquilo C1-6 sustituido o sin sustituir, alquenilo C2-6 sustituido o sin sustituir, alquinilo C2-6 sustituido o sin sustituir, cicloalquilo C3-6 sustituido o sin sustituir, cicloalquilalquilo C3-6 sustituido o sin sustituir y cicloalquenilo C3-6 sustituido o sin sustituir; cada aparición de Y se selecciona independientemente entre O, S y NRa; cada aparición de Ra y Rb puede ser igual o diferente y se seleccionan independientemente entre hidrógeno, nitro, hidroxi, ciano, halógeno, alquilo C1-6 sustituido o sin sustituir, alquenilo C2-6 sustituido o sin sustituir, alquinilo C2-6 sustituido o sin sustituir, cicloalquilo C3-6 sustituido o sin sustituir, cicloalquilalquilo C3-6 sustituido o sin sustituir y cicloalquenilo C3-6 sustituido o sin sustituir o cuando dos sustituyentes Ra y/o Rb están unidos directamente a un átomo de carbono, estos pueden estar unidos para ...

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22-10-2015 дата публикации

Novel 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of c-met protein kinases.

Номер: MX2014011750A
Принадлежит: Rhizen Pharmaceuticals SA

La presente invención proporciona compuestos útiles como moduladores de C-met proteína cinasa, métodos para prepararlos, composiciones farmacéuticas conteniéndolos y métodos de tratamiento, prevención y/o mejoramiento de enfermedades o desórdenes mediados por C-met cinasa con los mismos.

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15-01-2019 дата публикации

Selective dual inhibitors of PI3 delta and gamma protein kinases

Номер: US10179786B2
Принадлежит: Rhizen Pharmaceuticals SA

The present invention relates to a selective dual delta (δ) and gamma (γ) PI3K protein kinase modulator (S)-N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them.

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10-05-2018 дата публикации

Dual selective PI3 delta and gamma kinase inhibitors

Номер: AU2014276476B2
Принадлежит: Rhizen Pharmaceuticals SA

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

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18-06-2019 дата публикации

Substituted chromenones as modulators of protein kinases

Номер: US10322130B2
Принадлежит: Rhizen Pharmaceuticals SA

The present invention provides PI3K protein kinase modulators of formula wherein R, Cy 1 , R 1 , R 2 , L 1 and Cy 2 are as defined herein. The present invention also relates to methods of preparing compounds of formula (I) to pharmaceutical compositions containing them and to methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

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11-12-2014 дата публикации

Dual selective pi3 delta and gamma kinase inhibitors

Номер: WO2014195888A1
Принадлежит: Rhizen Pharmaceuticals SA

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

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17-10-2017 дата публикации

Dual selective PI3 delta and gamma kinase inhibitors

Номер: US9790224B2
Принадлежит: Rhizen Pharmaceuticals SA

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

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14-03-2016 дата публикации

Dual selective pi3 delta and gamma kinase inhibitors

Номер: PH12015502698A1
Принадлежит: Rhizen Pharmaceuticals SA

The present invention relates to dual delta (d) and gamma (?) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

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22-09-2020 дата публикации

Novel 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of c-met protein kinases

Номер: CA2865719C
Принадлежит: Rhizen Pharmaceuticals SA

The present invention provides compounds useful as C-met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of C-met kinase mediated diseases or disorders with them.

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03-01-2023 дата публикации

Dual selective pi3 delta and gamma kinase inhibitors

Номер: CA2913226C
Принадлежит: Rhizen Pharmaceuticals SA

The present invention relates to dual delta (.delta.) and gamma (.gamma.) PI3K protein kinase modulators, as reproduced below, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them: (see above formula)

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24-12-2019 дата публикации

compound, compound for use and pharmaceutical composition

Номер: BR112015030385A8
Принадлежит: Rhizen Pharmaceuticals S A

a presente invenção refere-se a moduladores de proteína quinase delta (d) e gama (¿) pi3k duplos, métodos de preparação dos mesmos, composições farmacêuticas que contêm os mesmos e métodos de tratamento, prevenção e/ou melhora de doenças ou distúrbios mediados por pi3k quinase com os mesmos. the present invention relates to double delta (d) and gamma (¿) pi3k protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treating, preventing and / or ameliorating mediated diseases or disorders by pi3k kinase with them.

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03-10-2013 дата публикации

Novel 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of c-met protein kinases

Номер: CA2865719A1
Принадлежит: Rhizen Pharmaceuticals SA

The present invention provides compounds useful as C-met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of C-met kinase mediated diseases or disorders with them.

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10-11-2011 дата публикации

Novel immunomodulator and anti-inflammatory compounds

Номер: US20110275603A1

The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.

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11-10-2022 дата публикации

Dual selective PI3 delta and gamma kinase inhibitors

Номер: US11466006B2
Принадлежит: Rhizen Pharmaceuticals Ag

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

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01-04-2014 дата публикации

Immunomodulator and anti-inflammatory compounds

Номер: US8686048B2
Принадлежит: Rhizen Pharmaceuticals SA

The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.

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01-06-2023 дата публикации

Purine derivatives as sik-3 inhibitors

Номер: US20230167116A1
Принадлежит: Rhizen Pharmaceuticals Ag

The present invention relates to novel inhibitors of salt-inducible kinase-3 (SIK3), methods of preparing them, pharmaceutical compositions containing them and methods for the treatment and/or prevention of kinase mediated diseases or disorders using them.

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10-08-2022 дата публикации

Derivados de purina como inhibidores del sik-3

Номер: AR122086A1
Принадлежит: Rhizen Pharmaceuticals Ag

Se proveen derivados de purina como inhibidores de la actividad catalítica de la quinasa inducible por sal 3 (SIK-3), una composición farmacéutica que comprende a uno de éstos compuestos y el empleo de éstos para el tratamiento de una enfermedad, trastorno o afección asociada con SIK-3 tales como cáncer, diversos tipos de leucemia y enfermedades neurodegenerativas. Reivindicación 1: Un compuesto seleccionado de (RS)-3-(3-fluorofenil)-2-(1-((8-hidroxi-9H-purin-6-il)amino)propil)-4H-cromen-4-ona y sales farmacéuticamente aceptable de estos. Reivindicación 5: Un compuesto que se selecciona de (RS)-3-(3-fluorofenil)-2-(1-((8-hidroxi-9H-purin-6-il)amino)propil)-4H-cromen-4-ona, (S)-3-(3-fluorofenil)-2-(1-((8-hidroxi-9H-purin-6-il)amino)propil)-4H-cromen-4-ona, y (R)-3-(3-fluorofenil)-2-(1-((8-hidroxi-9H-purin-6-il)amino)propil)-4H-cromen-4-ona, y sales farmacéuticamente aceptables de estos.

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14-11-2017 дата публикации

3,5-disubstituted-3H-imidazo[4,5-B]pyridine and 3,5-disubstituted-3H-[1,2,3]triazolo[4,5-B] pyridine compounds as modulators of c-Met protein kinases

Номер: US09815831B2
Принадлежит: Rhizen Pharmaceuticals SA

The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.

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10-10-2017 дата публикации

Glutaminase inhibitors

Номер: US09783533B2
Принадлежит: Rhizen Pharmaceuticals SA

The present disclosure provides compounds of formula (I) to (III) as glutaminase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders involving glutamine.

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12-09-2017 дата публикации

Immunomodulator and anti-inflammatory compounds

Номер: US09758474B2

The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.

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18-07-2017 дата публикации

Selective dual inhibitors of PI3 delta and gamma protein kinases

Номер: US09708329B2
Принадлежит: Rhizen Pharmaceuticals SA

The present invention relates to a selective dual delta (δ) and gamma (γ) PI3K protein kinase modulator (S)—N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them.

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