EA201592287A1 - Замещенные тетрагидрокарбазольные и карбазолкарбоксамидные соединения - Google Patents
Замещенные тетрагидрокарбазольные и карбазолкарбоксамидные соединенияInfo
- Publication number
- EA201592287A1 EA201592287A1 EA201592287A EA201592287A EA201592287A1 EA 201592287 A1 EA201592287 A1 EA 201592287A1 EA 201592287 A EA201592287 A EA 201592287A EA 201592287 A EA201592287 A EA 201592287A EA 201592287 A1 EA201592287 A1 EA 201592287A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- carbazolkarboxamide
- connections
- disclosed
- substituted tetrahydrocarbazole
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
- C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Раскрыты соединения формулы (I)где: обе пунктирные линии отображают либо две одинарные, либо две двойные связи;Q представляет собойилиRпредставляет собой F, Cl, -CN или -СН; Rпредставляет собой С1 или -СН; Rпредставляет собой -С(СН)ОН или -СНСНОН; Rпредставляет собой Н или -СН; каждый Rнезависимо представляет собой F, Cl, -СНи/или -ОСН; и n имеет значения 0, 1 или 2. Также раскрыты способы применения таких соединений в качестве ингибиторов тирозинкиназы Брутона (Btk) и фармацевтических композиций, содержащих такие соединения. Эти соединения являются полезными для лечения, предупреждения или замедления прогрессирования заболеваний или расстройств в различных терапевтических областях, таких как аутоиммунные заболевания и заболевание сосудов.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361839141P | 2013-06-25 | 2013-06-25 | |
| PCT/US2014/043978 WO2014210085A1 (en) | 2013-06-25 | 2014-06-25 | Substituted tetrahydrocarbazole and carbazole carboxamide compounds useful as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201592287A1 true EA201592287A1 (ru) | 2016-06-30 |
| EA026729B1 EA026729B1 (ru) | 2017-05-31 |
Family
ID=51210830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201592287A EA026729B1 (ru) | 2013-06-25 | 2014-06-25 | Замещенные тетрагидрокарбазольные и карбазолкарбоксамидные соединения |
Country Status (31)
| Country | Link |
|---|---|
| US (6) | US9334290B2 (ru) |
| EP (1) | EP3013814B1 (ru) |
| JP (1) | JP6353529B2 (ru) |
| KR (1) | KR102346508B1 (ru) |
| CN (1) | CN105358546B (ru) |
| AR (1) | AR096721A1 (ru) |
| AU (1) | AU2014302548B2 (ru) |
| BR (1) | BR112015030723A8 (ru) |
| CA (1) | CA2916500A1 (ru) |
| CL (1) | CL2015003635A1 (ru) |
| CY (1) | CY1119371T1 (ru) |
| DK (1) | DK3013814T3 (ru) |
| EA (1) | EA026729B1 (ru) |
| ES (1) | ES2636652T3 (ru) |
| HK (1) | HK1223359A1 (ru) |
| HR (1) | HRP20171031T1 (ru) |
| HU (1) | HUE034460T2 (ru) |
| IL (1) | IL243296B (ru) |
| LT (1) | LT3013814T (ru) |
| MA (1) | MA38648B1 (ru) |
| MY (1) | MY176631A (ru) |
| PE (1) | PE20160519A1 (ru) |
| PH (1) | PH12015502630A1 (ru) |
| PL (1) | PL3013814T3 (ru) |
| PT (1) | PT3013814T (ru) |
| RS (1) | RS56371B1 (ru) |
| SI (1) | SI3013814T1 (ru) |
| TN (1) | TN2015000529A1 (ru) |
| TW (1) | TWI648272B (ru) |
| UY (1) | UY35625A (ru) |
| WO (1) | WO2014210085A1 (ru) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105473573B (zh) | 2013-06-25 | 2018-03-16 | 百时美施贵宝公司 | 用作激酶抑制剂的咔唑甲酰胺化合物 |
| DK3461821T3 (da) | 2014-10-24 | 2020-08-17 | Bristol Myers Squibb Co | Indolcarboxamidforbindelser, der er brugbar som kinasehæmmere |
| BR112017007545A2 (pt) * | 2014-10-24 | 2017-12-19 | Bristol Myers Squibb Co | derivados de carbazol |
| WO2016065222A1 (en) | 2014-10-24 | 2016-04-28 | Bristol-Myers Squibb Company | Tricyclic atropisomer compounds |
| CN109414156A (zh) | 2016-07-01 | 2019-03-01 | 布里奥设备有限责任公司 | 具有视频馈送的插管管心针 |
| CN108101905A (zh) * | 2016-11-24 | 2018-06-01 | 中国科学院上海药物研究所 | 嘧啶并[5,4-b]吲嗪或嘧啶并[5,4-b]吡呤化合物、其制备方法及用途 |
| JP2020511462A (ja) | 2016-12-03 | 2020-04-16 | ジュノー セラピューティクス インコーポレイテッド | キナーゼ阻害剤との組み合わせで治療用ｔ細胞を使用するための方法および組成物 |
| WO2018118830A1 (en) | 2016-12-20 | 2018-06-28 | Bristol-Myers Squibb Company | Process for preparing tetrahydrocarbazole carboxamide compound |
| EP3789040A4 (en) | 2018-04-27 | 2022-03-09 | ONO Pharmaceutical Co., Ltd. | PREVENTIVE AND/OR THERAPEUTIC AGENT FOR AUTOIMMUNE DISEASES WITH A COMPOUND WITH BTK INHIBITING ACTIVITY AS AN INGREDIENT |
| CN117281803A (zh) | 2018-07-31 | 2023-12-26 | 罗索肿瘤学公司 | 喷雾干燥的分散体和制剂 |
| WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| WO2022212893A1 (en) | 2021-04-02 | 2022-10-06 | Biogen Ma Inc. | Combination treatment methods of multiple sclerosis |
| AU2023220628A1 (en) * | 2022-02-15 | 2024-05-23 | F. Hoffmann-La Roche Ag | Processes for the preparation of 1,2,3,5,6,7-hexahydro-s-indacene derivatives |
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| US4200750A (en) | 1977-01-07 | 1980-04-29 | Westwood Pharmaceuticals Inc. | 4-Substituted imidazo [1,2-a]quinoxalines |
| CA2140722A1 (en) | 1994-01-24 | 1995-07-25 | Joseph A. Jakubowski | Beta-carboline thromboxane synthase inhibitors |
| WO2005014599A1 (en) | 2003-06-04 | 2005-02-17 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds |
| US7393848B2 (en) | 2003-06-30 | 2008-07-01 | Cgi Pharmaceuticals, Inc. | Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds |
| US20050288295A1 (en) | 2003-11-11 | 2005-12-29 | Currie Kevin S | Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof |
| WO2006044687A2 (en) | 2004-10-15 | 2006-04-27 | Takeda San Diego, Inc. | Kinase inhibitors |
| SG159549A1 (en) | 2004-11-10 | 2010-03-30 | Cgi Pharmaceuticals Inc | Imidazo[1,2-a] pyrazin-8-ylamines useful as modulators of kinase activity |
| AR066386A1 (es) | 2004-12-17 | 2009-08-19 | Glenmark Pharmaceuticals Sa | Compuestos heterociclicos condensados, metodos e intermediarios para su preparacion, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por la inhibicion de la pde-4 |
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| US20070078136A1 (en) | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
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| US20090062251A1 (en) | 2007-08-17 | 2009-03-05 | Astrazeneca Ab | Novel Compounds 002 |
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| HRP20220401T3 (hr) | 2008-02-14 | 2022-05-27 | Eli Lilly And Company | Nova vizualizacijska sredstva za detektiranje neurološke disfunkcije |
| GB0809360D0 (en) | 2008-05-22 | 2008-07-02 | Isis Innovation | Calcium modulation |
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| MX2011006171A (es) * | 2008-12-19 | 2011-06-20 | Squibb Bristol Myers Co | Compuestos de carbazol carboxamida utiles como inhibidores de cinasa. |
| CN101475571B (zh) | 2009-01-21 | 2011-06-22 | 中国药科大学 | β-咔啉类细胞周期蛋白依赖性激酶2抑制剂及其用途 |
| US8242260B2 (en) | 2009-08-28 | 2012-08-14 | Novartis Ag | Compounds and compositions as protein kinase inhibitors |
| ES2562183T3 (es) | 2010-03-26 | 2016-03-02 | Merck Patent Gmbh | Benzonaftiridinaminas como inhibidores de la autotaxina |
| WO2011159857A1 (en) * | 2010-06-16 | 2011-12-22 | Bristol-Myers Squibb Company | Carboline carboxamide compounds useful as kinase inhibitors |
| EP2455378A1 (en) | 2010-11-03 | 2012-05-23 | Philip Morris Products S.A. | Carbazole and carboline derivatives, and preparation and therapeutic applications thereof |
| CN103429595B (zh) | 2010-11-15 | 2015-10-21 | Viiv保健英国有限公司 | Hiv复制的抑制剂 |
| JP5859640B2 (ja) | 2011-05-17 | 2016-02-10 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ブルトンチロシンキナーゼ阻害剤 |
| WO2013054185A1 (en) | 2011-10-13 | 2013-04-18 | Pfizer, Inc. | Pyrimidine and pyridine derivatives useful in therapy |
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2014
- 2014-06-24 UY UY0001035625A patent/UY35625A/es unknown
- 2014-06-24 TW TW103121681A patent/TWI648272B/zh not_active IP Right Cessation
- 2014-06-24 AR ARP140102388A patent/AR096721A1/es unknown
- 2014-06-25 PT PT147400949T patent/PT3013814T/pt unknown
- 2014-06-25 PE PE2015002665A patent/PE20160519A1/es active IP Right Grant
- 2014-06-25 RS RS20170904A patent/RS56371B1/sr unknown
- 2014-06-25 EP EP14740094.9A patent/EP3013814B1/en active Active
- 2014-06-25 DK DK14740094.9T patent/DK3013814T3/en active
- 2014-06-25 JP JP2016523869A patent/JP6353529B2/ja active Active
- 2014-06-25 MY MYPI2015704738A patent/MY176631A/en unknown
- 2014-06-25 WO PCT/US2014/043978 patent/WO2014210085A1/en active Application Filing
- 2014-06-25 AU AU2014302548A patent/AU2014302548B2/en not_active Ceased
- 2014-06-25 LT LTEP14740094.9T patent/LT3013814T/lt unknown
- 2014-06-25 PL PL14740094T patent/PL3013814T3/pl unknown
- 2014-06-25 SI SI201430268T patent/SI3013814T1/sl unknown
- 2014-06-25 HU HUE14740094A patent/HUE034460T2/en unknown
- 2014-06-25 ES ES14740094.9T patent/ES2636652T3/es active Active
- 2014-06-25 BR BR112015030723A patent/BR112015030723A8/pt not_active Application Discontinuation
- 2014-06-25 MA MA38648A patent/MA38648B1/fr unknown
- 2014-06-25 EA EA201592287A patent/EA026729B1/ru not_active IP Right Cessation
- 2014-06-25 KR KR1020167001632A patent/KR102346508B1/ko active IP Right Grant
- 2014-06-25 TN TN2015000529A patent/TN2015000529A1/en unknown
- 2014-06-25 CN CN201480035611.8A patent/CN105358546B/zh active Active
- 2014-06-25 CA CA2916500A patent/CA2916500A1/en not_active Abandoned
- 2014-06-25 US US14/314,602 patent/US9334290B2/en active Active
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2015
- 2015-11-26 PH PH12015502630A patent/PH12015502630A1/en unknown
- 2015-12-15 CL CL2015003635A patent/CL2015003635A1/es unknown
- 2015-12-22 IL IL243296A patent/IL243296B/en active IP Right Grant
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2016
- 2016-03-11 US US15/067,915 patent/US20160194338A1/en not_active Abandoned
- 2016-10-04 HK HK16111549.5A patent/HK1223359A1/zh not_active IP Right Cessation
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2017
- 2017-06-16 US US15/625,417 patent/US9850258B2/en active Active
- 2017-07-05 HR HRP20171031TT patent/HRP20171031T1/hr unknown
- 2017-09-06 CY CY20171100943T patent/CY1119371T1/el unknown
- 2017-11-10 US US15/809,437 patent/US10106559B2/en active Active
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2018
- 2018-09-25 US US16/140,750 patent/US10435415B2/en active Active
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2019
- 2019-08-22 US US16/547,675 patent/US20190382416A1/en not_active Abandoned
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