EA027968B1 - Гетероциклические карбоксамиды в качестве модуляторов активности киназ - Google Patents
Гетероциклические карбоксамиды в качестве модуляторов активности киназ Download PDFInfo
- Publication number
- EA027968B1 EA027968B1 EA201400736A EA201400736A EA027968B1 EA 027968 B1 EA027968 B1 EA 027968B1 EA 201400736 A EA201400736 A EA 201400736A EA 201400736 A EA201400736 A EA 201400736A EA 027968 B1 EA027968 B1 EA 027968B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- amino
- carboxamide
- group
- quinazoline
- title compound
- Prior art date
Links
- -1 Heterocyclic carboxamides Chemical class 0.000 title claims abstract description 155
- 230000000694 effects Effects 0.000 title description 10
- 108091000080 Phosphotransferase Proteins 0.000 title description 8
- 102000020233 phosphotransferase Human genes 0.000 title description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 29
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- 230000003463 hyperproliferative effect Effects 0.000 claims abstract description 10
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- 238000000034 method Methods 0.000 claims description 129
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- IXLVUUFUDRJUSL-RPBOFIJWSA-N 5-[[4-(3-acetamidophenyl)phenyl]methyl]-n-[(1s,2r)-2-phenylcyclopropyl]-1,3-oxazole-4-carboxamide Chemical compound CC(=O)NC1=CC=CC(C=2C=CC(CC3=C(N=CO3)C(=O)N[C@@H]3[C@H](C3)C=3C=CC=CC=3)=CC=2)=C1 IXLVUUFUDRJUSL-RPBOFIJWSA-N 0.000 claims description 27
- GYBHRTQLUQOYID-UHFFFAOYSA-N quinazoline-8-carboxamide Chemical compound N1=CN=C2C(C(=O)N)=CC=CC2=C1 GYBHRTQLUQOYID-UHFFFAOYSA-N 0.000 claims description 24
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 20
- 125000006413 ring segment Chemical group 0.000 claims description 18
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- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- RFPUAYMRJMGCAD-UHFFFAOYSA-N 5-[[4-[3-(trifluoromethoxy)phenyl]pyrrolidin-3-yl]amino]quinoline-8-carboxamide Chemical compound C12=CC=CN=C2C(C(=O)N)=CC=C1NC1CNCC1C1=CC=CC(OC(F)(F)F)=C1 RFPUAYMRJMGCAD-UHFFFAOYSA-N 0.000 claims description 3
- ZIRLUWNUUJIIGT-UHFFFAOYSA-N 5-[[4-[4-(trifluoromethoxy)phenyl]pyrrolidin-3-yl]amino]quinazoline-8-carboxamide Chemical compound C12=CN=CN=C2C(C(=O)N)=CC=C1NC1CNCC1C1=CC=C(OC(F)(F)F)C=C1 ZIRLUWNUUJIIGT-UHFFFAOYSA-N 0.000 claims description 3
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161579377P | 2011-12-22 | 2011-12-22 | |
| PCT/US2012/070085 WO2013096194A1 (en) | 2011-12-22 | 2012-12-17 | Novel heterocyclic carboxamides as modulators of kinase activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201400736A1 EA201400736A1 (ru) | 2015-01-30 |
| EA027968B1 true EA027968B1 (ru) | 2017-09-29 |
Family
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| Application Number | Title | Priority Date | Filing Date |
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| EA201400736A EA027968B1 (ru) | 2011-12-22 | 2012-12-17 | Гетероциклические карбоксамиды в качестве модуляторов активности киназ |
| EA201791073A EA201791073A1 (ru) | 2011-12-22 | 2012-12-17 | Новые гетероциклические карбоксамиды в качестве модуляторов активности киназ |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
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| EA201791073A EA201791073A1 (ru) | 2011-12-22 | 2012-12-17 | Новые гетероциклические карбоксамиды в качестве модуляторов активности киназ |
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| JP (2) | JP6193880B2 (https=) |
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| CN (1) | CN104169258B (https=) |
| AU (2) | AU2012355494B2 (https=) |
| BR (1) | BR112014015327B1 (https=) |
| CA (1) | CA2856448C (https=) |
| DK (1) | DK2794571T3 (https=) |
| EA (2) | EA027968B1 (https=) |
| ES (1) | ES2614232T3 (https=) |
| HR (1) | HRP20170099T1 (https=) |
| HU (1) | HUE032918T2 (https=) |
| IL (1) | IL233199B (https=) |
| LT (1) | LT2794571T (https=) |
| MX (1) | MX353062B (https=) |
| PL (1) | PL2794571T3 (https=) |
| PT (1) | PT2794571T (https=) |
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| SG (2) | SG11201402387WA (https=) |
| SI (1) | SI2794571T1 (https=) |
| WO (1) | WO2013096194A1 (https=) |
| ZA (1) | ZA201403517B (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9586938B2 (en) | 2010-07-29 | 2017-03-07 | Merck Patent Gmbh | Cyclic amine azaheterocyclic carboxamides |
| SG11201402387WA (en) * | 2011-12-22 | 2014-09-26 | Merck Patent Gmbh | Novel heterocyclic carboxamides as modulators of kinase activity |
| SG11201505999VA (en) | 2013-03-11 | 2015-08-28 | Merck Patent Gmbh | 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| JP2021515767A (ja) | 2018-03-07 | 2021-06-24 | バイエル・アクチエンゲゼルシヤフト | Erk5阻害剤の同定及び使用 |
| CN115073369A (zh) * | 2022-05-31 | 2022-09-20 | 汉瑞药业(荆门)有限公司 | 一种5-溴喹啉-8-甲醛的制备方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0308897A1 (en) * | 1987-09-24 | 1989-03-29 | Ss Pharmaceutical Co., Ltd. | Quinoline derivatives |
| WO2010093419A1 (en) * | 2009-02-11 | 2010-08-19 | Merck Patent Gmbh | Novel amino azaheterocyclic carboxamides |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1465651A (en) * | 1974-04-19 | 1977-02-23 | Wyeth John & Brother Ltd | Carbocyclic-fused ring pyridine derivatives |
| JPH01156960A (ja) * | 1987-09-24 | 1989-06-20 | Ss Pharmaceut Co Ltd | キノリン誘導体 |
| TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| TW200407324A (en) * | 2002-05-17 | 2004-05-16 | Bristol Myers Squibb Co | Bicyclic modulators of androgen receptor function |
| WO2004092154A1 (en) | 2003-04-03 | 2004-10-28 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| AU2004278413B2 (en) | 2003-09-30 | 2008-07-31 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| JP4800216B2 (ja) | 2003-10-24 | 2011-10-26 | エグゼリクシス, インコーポレイテッド | p70S6キナーゼモジュレーターおよび使用方法 |
| DE602004014969D1 (de) | 2003-11-21 | 2008-08-21 | Novartis Ag | 1h-imidazochinolinderivate als proteinkinaseinhibitoren |
| CN1889958A (zh) | 2003-12-09 | 2007-01-03 | 美国政府健康及人类服务部 | 抑制免疫应答或治疗增生性疾病的方法 |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| CA2590961C (en) | 2004-12-28 | 2013-11-26 | Exelixis, Inc. | [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| EP1902032A1 (en) | 2005-06-22 | 2008-03-26 | Astex Therapeutics Limited | Pharmaceutical compounds |
| SG11201402387WA (en) * | 2011-12-22 | 2014-09-26 | Merck Patent Gmbh | Novel heterocyclic carboxamides as modulators of kinase activity |
| JP6223563B2 (ja) * | 2013-10-14 | 2017-11-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 選択的に置換されたキノリン化合物 |
| CN105636945B (zh) * | 2013-10-14 | 2017-11-17 | 卫材R&D管理有限公司 | 选择性取代的喹啉化合物 |
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2012
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- 2012-12-17 PL PL12808640T patent/PL2794571T3/pl unknown
- 2012-12-17 CN CN201280063286.7A patent/CN104169258B/zh not_active Expired - Fee Related
- 2012-12-17 CA CA2856448A patent/CA2856448C/en active Active
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- 2012-12-17 AU AU2012355494A patent/AU2012355494B2/en not_active Ceased
- 2012-12-17 DK DK12808640.2T patent/DK2794571T3/en active
- 2012-12-17 EA EA201400736A patent/EA027968B1/ru not_active IP Right Cessation
- 2012-12-17 EA EA201791073A patent/EA201791073A1/ru unknown
- 2012-12-17 US US14/359,937 patent/US9139568B2/en not_active Expired - Fee Related
- 2012-12-17 WO PCT/US2012/070085 patent/WO2013096194A1/en not_active Ceased
- 2012-12-17 RS RS20170071A patent/RS55621B1/sr unknown
- 2012-12-17 KR KR1020147017395A patent/KR102098358B1/ko not_active Expired - Fee Related
- 2012-12-17 HR HRP20170099TT patent/HRP20170099T1/hr unknown
- 2012-12-17 LT LTEP12808640.2T patent/LT2794571T/lt unknown
- 2012-12-17 EP EP12808640.2A patent/EP2794571B1/en active Active
- 2012-12-17 BR BR112014015327-2A patent/BR112014015327B1/pt not_active IP Right Cessation
- 2012-12-17 ES ES12808640.2T patent/ES2614232T3/es active Active
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- 2012-12-17 JP JP2014549176A patent/JP6193880B2/ja not_active Expired - Fee Related
- 2012-12-17 MX MX2014007364A patent/MX353062B/es active IP Right Grant
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- 2014-05-15 ZA ZA2014/03517A patent/ZA201403517B/en unknown
- 2014-06-17 IL IL233199A patent/IL233199B/en active IP Right Grant
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- 2015-09-08 US US14/847,561 patent/US20160058763A1/en not_active Abandoned
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- 2016-08-03 US US15/227,017 patent/US10080753B2/en active Active
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- 2017-08-10 JP JP2017155667A patent/JP6553686B2/ja not_active Expired - Fee Related
- 2017-10-06 AU AU2017239625A patent/AU2017239625B2/en not_active Ceased
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0308897A1 (en) * | 1987-09-24 | 1989-03-29 | Ss Pharmaceutical Co., Ltd. | Quinoline derivatives |
| WO2010093419A1 (en) * | 2009-02-11 | 2010-08-19 | Merck Patent Gmbh | Novel amino azaheterocyclic carboxamides |
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| AU2017239625B2 (en) | Novel heterocyclic carboxamides as modulators of kinase activity | |
| HK1201829B (en) | Novel heterocyclic carboxamides as modulators of kinase activity |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |