JP2014531449A5 - - Google Patents
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- JP2014531449A5 JP2014531449A5 JP2014531222A JP2014531222A JP2014531449A5 JP 2014531449 A5 JP2014531449 A5 JP 2014531449A5 JP 2014531222 A JP2014531222 A JP 2014531222A JP 2014531222 A JP2014531222 A JP 2014531222A JP 2014531449 A5 JP2014531449 A5 JP 2014531449A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkenyl
- alkynyl
- substituted
- different
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 34
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 26
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 25
- 229910052736 halogen Inorganic materials 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052799 carbon Inorganic materials 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 229920006395 saturated elastomer Polymers 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 2
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 2
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- QEKADNOVOXTAIF-UHFFFAOYSA-N 2-methyl-n-[3-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound CC(=C)C(=O)NC1=CC=CC(CN2C3=NC(NC4=CN(C)N=C4)=NC=C3C=N2)=C1 QEKADNOVOXTAIF-UHFFFAOYSA-N 0.000 claims 1
- -1 3-((6-((1-methyl-1H-pyrazol-4-yl) amino) -1H-pyrazolo [3,4-d] pyrimidin-1-yl) methyl) phenyl Chemical group 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical group C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 208000037765 diseases and disorders Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 230000001900 immune effect Effects 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical group C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 1
- DIQANUOZZBWOIF-UHFFFAOYSA-N n-[2-fluoro-5-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=NN2CC=3C=C(NC(=O)C=C)C(F)=CC=3)C2=N1 DIQANUOZZBWOIF-UHFFFAOYSA-N 0.000 claims 1
- XYEGFIKUSACDAB-UHFFFAOYSA-N n-[3-[[2-[(1-methylpyrazol-4-yl)amino]pyrrolo[2,3-d]pyrimidin-7-yl]methyl]phenyl]ethenesulfonamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=CN2CC=3C=C(NS(=O)(=O)C=C)C=CC=3)C2=N1 XYEGFIKUSACDAB-UHFFFAOYSA-N 0.000 claims 1
- KSHMJJCPYXRKEN-UHFFFAOYSA-N n-[3-[[2-[(1-methylpyrazol-4-yl)amino]pyrrolo[2,3-d]pyrimidin-7-yl]methyl]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=CN2CC=3C=C(NC(=O)C=C)C=CC=3)C2=N1 KSHMJJCPYXRKEN-UHFFFAOYSA-N 0.000 claims 1
- PRKZDXYTQMDRPI-UHFFFAOYSA-N n-[3-[[6-[(1-methylpyrazol-3-yl)amino]pyrazolo[4,3-c]pyridin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound CN1C=CC(NC=2N=CC=3C=NN(CC=4C=C(NC(=O)C=C)C=CC=4)C=3C=2)=N1 PRKZDXYTQMDRPI-UHFFFAOYSA-N 0.000 claims 1
- ZDCSHVQCKQGMMD-UHFFFAOYSA-N n-[3-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]ethenesulfonamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=NN2CC=3C=C(NS(=O)(=O)C=C)C=CC=3)C2=N1 ZDCSHVQCKQGMMD-UHFFFAOYSA-N 0.000 claims 1
- OVIYRHXLFVAREZ-UHFFFAOYSA-N n-[3-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC1=NC=C(C=NN2CC=3C=C(NC(=O)C=C)C=CC=3)C2=N1 OVIYRHXLFVAREZ-UHFFFAOYSA-N 0.000 claims 1
- ZYRCGZXXJZYGPD-UHFFFAOYSA-N n-[3-[[6-[(1-methylpyrazol-4-yl)amino]pyrazolo[4,3-c]pyridin-1-yl]methyl]phenyl]prop-2-enamide Chemical compound C1=NN(C)C=C1NC(N=C1)=CC2=C1C=NN2CC1=CC=CC(NC(=O)C=C)=C1 ZYRCGZXXJZYGPD-UHFFFAOYSA-N 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 150000003852 triazoles Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11182020 | 2011-09-20 | ||
| EP11182020.5 | 2011-09-20 | ||
| PCT/EP2012/068504 WO2013041605A1 (en) | 2011-09-20 | 2012-09-20 | Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014531449A JP2014531449A (ja) | 2014-11-27 |
| JP2014531449A5 true JP2014531449A5 (enExample) | 2015-11-05 |
Family
ID=46924422
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014531222A Pending JP2014531449A (ja) | 2011-09-20 | 2012-09-20 | キナーゼ阻害剤としてのピラゾロ［４，３―ｃ］ピリジン誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20140323504A1 (enExample) |
| EP (1) | EP2760863A1 (enExample) |
| JP (1) | JP2014531449A (enExample) |
| KR (1) | KR20140063700A (enExample) |
| CN (1) | CN103874699A (enExample) |
| AU (1) | AU2012311504B2 (enExample) |
| CA (1) | CA2849340A1 (enExample) |
| RU (1) | RU2014115476A (enExample) |
| WO (1) | WO2013041605A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MD20140023A2 (ro) * | 2011-09-22 | 2014-06-30 | Pfizer Inc. | Derivaţi de pirolpirimidină şi purină |
| WO2014022569A1 (en) * | 2012-08-03 | 2014-02-06 | Principia Biopharma Inc. | Treatment of dry eye |
| SMT201900344T1 (it) | 2012-09-10 | 2019-07-11 | Principia Biopharma Inc | Composti di pirazolopirimidina come inibitori di chinasi |
| NZ715838A (en) * | 2013-07-31 | 2020-05-29 | Merck Patent Gmbh | Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof |
| WO2015038417A1 (en) * | 2013-09-10 | 2015-03-19 | Asana Biosciences, Llc | Compounds for regulating fak and/or src pathways |
| KR20160117614A (ko) | 2014-02-21 | 2016-10-10 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| MX381283B (es) | 2014-12-18 | 2025-03-12 | Principia Biopharma Inc | Tratamiento de pénfigo. |
| TW201718572A (zh) | 2015-06-24 | 2017-06-01 | 普林斯匹亞生物製藥公司 | 酪胺酸激酶抑制劑 |
| CN106831779B (zh) * | 2015-11-28 | 2019-07-19 | 南昌弘益药业有限公司 | 一类jak激酶抑制剂的新化合物 |
| US20190231784A1 (en) | 2016-06-29 | 2019-08-01 | Principia Biopharma Inc. | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| KR20190026902A (ko) | 2016-07-14 | 2019-03-13 | 화이자 인코포레이티드 | 바닌-1 효소의 억제제로서의 신규 피리미딘 카르복스아미드 |
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| CN110885331B (zh) * | 2018-09-11 | 2021-07-09 | 中国药科大学 | 一种6-氨基-1H-吡唑并[3，4-d]嘧啶类JAK激酶抑制剂的制备与应用 |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| KR20220052859A (ko) * | 2019-05-08 | 2022-04-28 | 비말란 바이오사이언스즈, 인크. | Jak 억제제 |
| TWI899080B (zh) * | 2019-05-27 | 2025-10-01 | 大陸商迪哲（江蘇）醫藥股份有限公司 | Ｄｎａ依賴性蛋白激酶抑制劑 |
| IL291994A (en) | 2019-10-14 | 2022-06-01 | Principia Biopharma Inc | Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine- 1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| US11697648B2 (en) | 2019-11-26 | 2023-07-11 | Theravance Biopharma R&D Ip, Llc | Fused pyrimidine pyridinone compounds as JAK inhibitors |
| CN115244055B (zh) * | 2020-01-21 | 2024-09-03 | 江苏先声药业有限公司 | 嘧啶并五元环类衍生物及其应用 |
| PH12022551787A1 (en) | 2020-01-22 | 2024-02-12 | Principia Biopharma Inc | Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| CN117412971A (zh) * | 2021-05-12 | 2024-01-16 | 微境生物医药科技(上海)有限公司 | 含吡嗪结构的吡咯并嘧啶衍生物 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020192228A1 (en) | 1997-02-12 | 2002-12-19 | Samir M. Hanash | Protein markers for lung cancer and use thereof |
| GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
| KR100838617B1 (ko) | 1999-02-10 | 2008-06-16 | 아스트라제네카 아베 | 혈관형성 억제제로서의 퀴나졸린 유도체 |
| UA72946C2 (uk) | 1999-11-05 | 2005-05-16 | Астразенека Аб | Похідні хіназоліну як інгібітори васкулярного ендотеліального фактора росту (vegf) |
| AU777911B2 (en) | 1999-12-10 | 2004-11-04 | Pfizer Products Inc. | Pyrrolo(2,3-d)pyrimidine compounds |
| CN1329390C (zh) | 2000-02-15 | 2007-08-01 | 苏根公司 | 吡咯取代的2－二氢吲哚酮蛋白激酶抑制剂 |
| DK1713806T3 (da) * | 2004-02-14 | 2013-08-05 | Irm Llc | Forbindelser og sammensætninger som proteinkinaseinhibitorer |
| GB0427604D0 (en) | 2004-12-16 | 2005-01-19 | Novartis Ag | Organic compounds |
| EP1891446B1 (en) | 2005-06-14 | 2013-04-10 | Cellzome GmbH | Process for the identification of novel enzyme interacting compounds |
| GB0605691D0 (en) | 2006-03-21 | 2006-05-03 | Novartis Ag | Organic Compounds |
| EP1862802B1 (en) | 2006-06-01 | 2008-12-10 | Cellzome Ag | Methods for the identification of ZAP-70 interacting molecules and for the purification of ZAP-70 |
| KR20090031787A (ko) | 2006-07-21 | 2009-03-27 | 노파르티스 아게 | Ｊａｋ 키나제 억제제로서의 ２,４-디(아릴아미노)-피리미딘-５-카르복스아미드 화합물 |
| EP2099800A1 (en) | 2006-11-16 | 2009-09-16 | Pharmacopeia, LLC | 7-substituted purine derivatives for immunosuppression |
| US7947698B2 (en) | 2007-03-23 | 2011-05-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| US7834024B2 (en) | 2007-03-26 | 2010-11-16 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| WO2009008992A2 (en) | 2007-07-06 | 2009-01-15 | Osi Pharmaceuticals Inc. | Combination anti-cancer therapy comprising an inhibitor of both mtorc1 and mt0rc2 |
| UY31631A1 (es) | 2008-02-06 | 2009-09-30 | Nuevos derivados de 7-fenil-7h-pirrolo-[2,3d]-pirimidin-2-il-amino, sales de los mismos, procesos para su preparacion, composiciones farmacéuticas que los comprenden y aplicaciones | |
| CL2009001884A1 (es) | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| GB0903759D0 (en) | 2009-03-04 | 2009-04-15 | Medical Res Council | Compound |
| CA2758614A1 (en) | 2009-04-14 | 2010-10-21 | Cellzome Limited | Fluoro substituted pyrimidine compounds as jak3 inhibitors |
| CA2760794C (en) * | 2009-05-05 | 2017-07-25 | Dana Farber Cancer Institute | Egfr inhibitors and methods of treating disorders |
| EP2464647B1 (en) | 2009-08-11 | 2016-09-21 | Bristol-Myers Squibb Company | Azaindazoles as btk kinase modulators and use thereof |
| WO2011048082A1 (en) * | 2009-10-20 | 2011-04-28 | Cellzome Limited | Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors |
| US9040545B2 (en) | 2010-08-20 | 2015-05-26 | Cellzome Limited | Heterocyclyl pyrazolopyrimidine analogues as selective JAK inhibitors |
-
2012
- 2012-09-20 KR KR1020147006956A patent/KR20140063700A/ko not_active Withdrawn
- 2012-09-20 CN CN201280049382.6A patent/CN103874699A/zh active Pending
- 2012-09-20 EP EP12762577.0A patent/EP2760863A1/en not_active Withdrawn
- 2012-09-20 WO PCT/EP2012/068504 patent/WO2013041605A1/en not_active Ceased
- 2012-09-20 RU RU2014115476/04A patent/RU2014115476A/ru not_active Application Discontinuation
- 2012-09-20 JP JP2014531222A patent/JP2014531449A/ja active Pending
- 2012-09-20 US US14/345,512 patent/US20140323504A1/en not_active Abandoned
- 2012-09-20 AU AU2012311504A patent/AU2012311504B2/en not_active Expired - Fee Related
- 2012-09-20 CA CA2849340A patent/CA2849340A1/en not_active Abandoned
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