JP2011527683A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2011527683A5 JP2011527683A5 JP2011517493A JP2011517493A JP2011527683A5 JP 2011527683 A5 JP2011527683 A5 JP 2011527683A5 JP 2011517493 A JP2011517493 A JP 2011517493A JP 2011517493 A JP2011517493 A JP 2011517493A JP 2011527683 A5 JP2011527683 A5 JP 2011527683A5
- Authority
- JP
- Japan
- Prior art keywords
- benzo
- cyclohepta
- pyridazin
- triazole
- dihydro
- 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.)
- Granted
Links
- -1 6,7-dihydro -5H- benzo [6,7] cyclohepta [1, 2-c] pyridazin-3-yl Chemical group 0.000 claims 90
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 125000003342 alkenyl group Chemical group 0.000 claims 13
- 125000003710 aryl alkyl group Chemical group 0.000 claims 13
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 13
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 11
- 125000001475 halogen functional group Chemical group 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 9
- 125000002947 alkylene group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 3
- 125000006311 cyclobutyl amino group Chemical group [H]N(*)C1([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000006312 cyclopentyl amino group Chemical group [H]N(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- QCYJCZJMOAWVPC-UHFFFAOYSA-N 1-phenyl-1,2,4-triazole-3,5-diamine Chemical compound N1=C(N)N=C(N)N1C1=CC=CC=C1 QCYJCZJMOAWVPC-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 102000003929 Transaminases Human genes 0.000 claims 1
- 108090000340 Transaminases Proteins 0.000 claims 1
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 150000004985 diamines Chemical class 0.000 claims 1
- 125000004914 dipropylamino group Chemical group C(CC)N(CCC)* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000006308 propyl amino group Chemical group 0.000 claims 1
- HEOQXHNKRXRCTO-UHFFFAOYSA-N C(CC1)CCc2c1cccc2 Chemical compound C(CC1)CCc2c1cccc2 HEOQXHNKRXRCTO-UHFFFAOYSA-N 0.000 description 1
- 0 CC1(CC=C(CCC(C)(*)CCC2)C2=CC1)*(C(*=C1*N=C)=**1C(**1)=CC2=C1c1cccnc1CCC2)=C Chemical compound CC1(CC=C(CCC(C)(*)CCC2)C2=CC1)*(C(*=C1*N=C)=**1C(**1)=CC2=C1c1cccnc1CCC2)=C 0.000 description 1
- XCOVHMKZKNATLH-UHFFFAOYSA-N CNc(nc1N)n[n]1-c1cc(CCCc2ncccc2-2)c-2nn1 Chemical compound CNc(nc1N)n[n]1-c1cc(CCCc2ncccc2-2)c-2nn1 XCOVHMKZKNATLH-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7940308P | 2008-07-09 | 2008-07-09 | |
| US61/079,403 | 2008-07-09 | ||
| PCT/US2009/049617 WO2010005876A2 (en) | 2008-07-09 | 2009-07-02 | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011527683A JP2011527683A (ja) | 2011-11-04 |
| JP2011527683A5 true JP2011527683A5 (enExample) | 2012-08-16 |
| JP5592884B2 JP5592884B2 (ja) | 2014-09-17 |
Family
ID=41152113
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011517493A Expired - Fee Related JP5592884B2 (ja) | 2008-07-09 | 2009-07-02 | Ａｘｌ阻害剤として有用な多環式ヘテロアリール置換トリアゾール |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US8349838B2 (enExample) |
| EP (1) | EP2326641B1 (enExample) |
| JP (1) | JP5592884B2 (enExample) |
| CA (1) | CA2730231C (enExample) |
| ES (1) | ES2537480T3 (enExample) |
| WO (1) | WO2010005876A2 (enExample) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1922310A2 (en) * | 2005-09-07 | 2008-05-21 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| PT2114955E (pt) | 2006-12-29 | 2013-04-18 | Rigel Pharmaceuticals Inc | Triazoles substituídos com arilo bicíclico em ponte ou heteroarilo bicíclico em ponte úteis como inibidores de axl |
| US7872000B2 (en) | 2006-12-29 | 2011-01-18 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as Axl inhibitors |
| JP2010514810A (ja) | 2006-12-29 | 2010-05-06 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ａｘｌインヒビターとして有用な置換トリアゾール |
| ES2607065T3 (es) * | 2006-12-29 | 2017-03-29 | Rigel Pharmaceuticals, Inc. | Triazoles N3-heteroaril sustituidos y triazoles N5-heteroaril sustituidos útiles como inhibidores de axl |
| PL2078010T3 (pl) | 2006-12-29 | 2014-07-31 | Rigel Pharmaceuticals Inc | Triazole podstawione policyklicznym heteroarylem użyteczne jako inhibitory Axl |
| CA2704052C (en) * | 2007-10-26 | 2015-04-21 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| CA2715658C (en) | 2008-02-15 | 2016-07-19 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases |
| JP5592884B2 (ja) | 2008-07-09 | 2014-09-17 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ａｘｌ阻害剤として有用な多環式ヘテロアリール置換トリアゾール |
| WO2010005879A1 (en) | 2008-07-09 | 2010-01-14 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| JP4644273B2 (ja) * | 2008-07-15 | 2011-03-02 | 本田技研工業株式会社 | 車両周辺監視装置 |
| EP2387395B1 (en) | 2009-01-16 | 2014-10-15 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
| DE102010030538A1 (de) * | 2010-06-25 | 2011-12-29 | Bayer Schering Pharma Aktiengesellschaft | 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| DE102011087987A1 (de) * | 2011-12-08 | 2013-06-13 | Bayer Intellectual Property Gmbh | 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| PL2810937T3 (pl) | 2012-01-31 | 2017-07-31 | Daiichi Sankyo Company, Limited | Pochodna pirydonu |
| WO2015077375A1 (en) | 2013-11-20 | 2015-05-28 | Signalchem Lifesciences Corp. | Quinazoline derivatives as tam family kinase inhibitors |
| KR102398473B1 (ko) * | 2013-11-27 | 2022-05-16 | 시그널켐 라이프사이언시즈 코포레이션 | Tam 패밀리 키나제 억제제로서의 아미노피리딘 유도체 |
| TWI723572B (zh) | 2014-07-07 | 2021-04-01 | 日商第一三共股份有限公司 | 具有四氫吡喃基甲基之吡啶酮衍生物及其用途 |
| GB201420285D0 (en) * | 2014-11-14 | 2014-12-31 | Bergenbio As | Process |
| US9840503B2 (en) | 2015-05-11 | 2017-12-12 | Incyte Corporation | Heterocyclic compounds and uses thereof |
| US9708333B2 (en) | 2015-08-12 | 2017-07-18 | Incyte Corporation | Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors |
| WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
| WO2017146236A1 (ja) | 2016-02-26 | 2017-08-31 | 小野薬品工業株式会社 | Ａｘｌ阻害剤と免疫チェックポイント阻害剤とを組み合わせて投与することを特徴とする癌治療のための医薬 |
| HUE064656T2 (hu) | 2016-03-28 | 2024-04-28 | Incyte Corp | Pirrolotriazin vegyületek mint TAM inhibitorok |
| CN106083764B (zh) * | 2016-07-11 | 2018-09-18 | 上海皓元生物医药科技有限公司 | 一种用于制备axl抑制剂的高纯度中间体的手性拆分方法 |
| US20200197385A1 (en) | 2017-08-23 | 2020-06-25 | Ono Pharmaceutical Co., Ltd. | Therapeutic agent for cancer containing axl inhibitor as active ingredient |
| SMT202200011T1 (it) | 2017-09-27 | 2022-03-21 | Incyte Corp | Sali di derivati di pirrolotriazina utili come inibitori di tam |
| JP7223998B2 (ja) | 2017-10-13 | 2023-02-17 | 小野薬品工業株式会社 | Ａｘｌ阻害剤を有効成分として含む固形がん治療剤 |
| KR102839002B1 (ko) | 2018-06-29 | 2025-07-29 | 인사이트 코포레이션 | Axl/mer 억제제의 제형 |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
| US20220401436A1 (en) | 2019-11-08 | 2022-12-22 | INSERM (Institute National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| PH12022552347A1 (en) | 2020-03-06 | 2024-01-29 | Incyte Corp | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| US20230227484A1 (en) * | 2020-05-29 | 2023-07-20 | Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. | Pyrimidine compound as axl inhibitor |
| TW202304908A (zh) * | 2021-04-14 | 2023-02-01 | 日商衛材R&D企管股份有限公司 | 四氫吡啶并嘧啶化合物 |
| AR129722A1 (es) | 2022-06-28 | 2024-09-18 | Arcus Biosciences Inc | Compuestos inhibidores de axl |
| WO2024051667A1 (zh) * | 2022-09-05 | 2024-03-14 | 南京正大天晴制药有限公司 | 具有axl抑制活性的取代三唑化合物 |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1403866A (en) * | 1971-12-06 | 1975-08-28 | Wyeth John & Brother Ltd | Derivatives of 3-amino-1,2,4-triazoles |
| EP0710654A4 (en) | 1993-07-23 | 1996-08-28 | Green Cross Corp | TRIAZOLE DERIVATIVE AND ITS PHARMACEUTICAL USE |
| GB9918180D0 (en) | 1999-08-02 | 1999-10-06 | Smithkline Beecham Plc | Novel compositions |
| PT1355889E (pt) | 2000-12-22 | 2006-09-29 | Ortho Mcneil Pharm Inc | Derivados diamina triazole substituidos como inibidores de cinase |
| TWI335221B (en) | 2001-09-27 | 2011-01-01 | Alcon Inc | Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma |
| EA008244B1 (ru) | 2002-05-03 | 2007-04-27 | Янссен Фармацевтика Н.В. | Полимерные микроэмульсии |
| US20060293256A1 (en) * | 2002-08-06 | 2006-12-28 | Masateru Yamada | Remedy or preventive for kidney disease and method of diagnosing kidney disease |
| EP1563094A4 (en) | 2002-10-29 | 2007-04-25 | Rigel Pharmaceuticals Inc | MODULATORS OF ANGIOGENESIS AND TUMORIGENESIS |
| AR042052A1 (es) * | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| TW200514776A (en) | 2003-08-06 | 2005-05-01 | Vertex Pharma | Aminotriazole compounds useful as inhibitors of protein kinases |
| EA200601441A1 (ru) | 2004-02-11 | 2007-02-27 | Янссен Фармацевтика Н.В. | Способ получения соединений замещённого триазола |
| EP1922310A2 (en) | 2005-09-07 | 2008-05-21 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| US8097630B2 (en) * | 2006-10-10 | 2012-01-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as Axl inhibitors |
| US7879856B2 (en) * | 2006-12-22 | 2011-02-01 | Rigel Pharmaceuticals, Inc. | Diaminothiazoles useful as Axl inhibitors |
| PT2114955E (pt) | 2006-12-29 | 2013-04-18 | Rigel Pharmaceuticals Inc | Triazoles substituídos com arilo bicíclico em ponte ou heteroarilo bicíclico em ponte úteis como inibidores de axl |
| JP2010514810A (ja) * | 2006-12-29 | 2010-05-06 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ａｘｌインヒビターとして有用な置換トリアゾール |
| ES2607065T3 (es) | 2006-12-29 | 2017-03-29 | Rigel Pharmaceuticals, Inc. | Triazoles N3-heteroaril sustituidos y triazoles N5-heteroaril sustituidos útiles como inhibidores de axl |
| PL2078010T3 (pl) * | 2006-12-29 | 2014-07-31 | Rigel Pharmaceuticals Inc | Triazole podstawione policyklicznym heteroarylem użyteczne jako inhibitory Axl |
| US7872000B2 (en) * | 2006-12-29 | 2011-01-18 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as Axl inhibitors |
| AU2008266290A1 (en) | 2007-06-15 | 2008-12-24 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| CA2704052C (en) * | 2007-10-26 | 2015-04-21 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| CA2715658C (en) | 2008-02-15 | 2016-07-19 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases |
| WO2010005879A1 (en) | 2008-07-09 | 2010-01-14 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| JP5592884B2 (ja) | 2008-07-09 | 2014-09-17 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ａｘｌ阻害剤として有用な多環式ヘテロアリール置換トリアゾール |
| EP2387395B1 (en) * | 2009-01-16 | 2014-10-15 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
-
2009
- 2009-07-02 JP JP2011517493A patent/JP5592884B2/ja not_active Expired - Fee Related
- 2009-07-02 CA CA2730231A patent/CA2730231C/en active Active
- 2009-07-02 ES ES09790061.7T patent/ES2537480T3/es active Active
- 2009-07-02 WO PCT/US2009/049617 patent/WO2010005876A2/en not_active Ceased
- 2009-07-02 US US13/002,487 patent/US8349838B2/en active Active
- 2009-07-02 EP EP09790061.7A patent/EP2326641B1/en not_active Not-in-force
-
2012
- 2012-12-21 US US13/725,407 patent/US9079898B2/en active Active
-
2015
- 2015-04-16 US US14/688,843 patent/US9173882B2/en not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2011527683A5 (enExample) | ||
| JP7278359B2 (ja) | Ｓｈｐ２の活性を阻害するための化合物および組成物 | |
| EP3094627B1 (en) | 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 | |
| EP3094629B1 (en) | 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2 | |
| CN1151789C (zh) | 芳基(或杂芳基)吡咯基甲醇的衍生物的应用 | |
| AU2012287103B2 (en) | Anti-biofilm compounds | |
| JP2010138190A5 (enExample) | ||
| ES2732442T3 (es) | Compuestos orgánicos | |
| IL200240A (en) | A 6-Amino-8-Hydroxy-Purine-9-Ilbenzyl Pharmaceutical Compound Conjugated with Diolauylphosphatidyl Ethanolamine | |
| CN106413716A (zh) | 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤 | |
| CA2345809A1 (en) | 6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors | |
| JP2007529421A5 (enExample) | ||
| JP2014509659A5 (enExample) | ||
| JP2009504763A5 (enExample) | ||
| JP2009542613A5 (enExample) | ||
| JP2012515225A5 (enExample) | ||
| JP2010241830A5 (enExample) | ||
| JP2011509309A5 (enExample) | ||
| JP2012514655A (ja) | フッ素含有化合物およびその使用法 | |
| JP2020023496A6 (ja) | 有機化合物 | |
| JP2011518202A5 (enExample) | ||
| JP2011505356A5 (enExample) | ||
| JP2007520452A5 (enExample) | ||
| CN104125954A (zh) | 用于抑制bcl2与结合配偶体相互作用的化合物 | |
| EP1682123A1 (en) | Cancer treatment method |