JP2011527683A5 - - Google Patents
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- 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 (https=) | 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 (https=) |
| EP (1) | EP2326641B1 (https=) |
| JP (1) | JP5592884B2 (https=) |
| CA (1) | CA2730231C (https=) |
| ES (1) | ES2537480T3 (https=) |
| WO (1) | WO2010005876A2 (https=) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007030680A2 (en) * | 2005-09-07 | 2007-03-15 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| EP2114955B1 (en) | 2006-12-29 | 2013-02-13 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| ES2672172T3 (es) * | 2006-12-29 | 2018-06-12 | Rigel Pharmaceuticals, Inc. | Triazoles N3-heteroarilsustituidos y triazoles N5-heteroarilsustituidos útiles como inhibidores de Axl |
| EP2079736B1 (en) | 2006-12-29 | 2017-10-18 | Rigel Pharmaceuticals, Inc. | Substituted triazoles useful as axl inhibitors |
| WO2008083353A1 (en) | 2006-12-29 | 2008-07-10 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| EP2078010B1 (en) | 2006-12-29 | 2014-01-29 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| WO2009054864A1 (en) * | 2007-10-26 | 2009-04-30 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| US8309566B2 (en) | 2008-02-15 | 2012-11-13 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases |
| US8431594B2 (en) | 2008-07-09 | 2013-04-30 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as AXL inhibitors |
| CA2730231C (en) | 2008-07-09 | 2016-10-18 | Rigel Pharmaceuticals, Inc. | Polycyclic 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 |
| SG172997A1 (en) | 2009-01-16 | 2011-08-29 | 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 |
| RS55728B1 (sr) | 2012-01-31 | 2017-07-31 | Daiichi Sankyo Co Ltd | Derivat piridona |
| JP6527513B2 (ja) | 2013-11-20 | 2019-06-05 | シグナルケム・ライフサイエンシーズ・コーポレイションＳｉｇｎａｌｃｈｅｍ Ｌｉｆｅｓｃｉｅｎｃｅｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｔａｍファミリーキナーゼ阻害剤としてのキナゾリン誘導体 |
| JP6496731B2 (ja) | 2013-11-27 | 2019-04-03 | シグナルケム・ライフサイエンシーズ・コーポレイションＳｉｇｎａｌｃｈｅｍ Ｌｉｆｅｓｃｉｅｎｃｅｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｔａｍファミリーキナーゼ阻害剤としてのアミノピリジン誘導体 |
| TWI690525B (zh) | 2014-07-07 | 2020-04-11 | 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 |
| WO2017027717A1 (en) | 2015-08-12 | 2017-02-16 | Incyte Corporation | Bicyclic fused pyrimidine compounds as tam inhibitors |
| US10053465B2 (en) | 2015-08-26 | 2018-08-21 | 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 |
| MD3436461T2 (ro) | 2016-03-28 | 2024-05-31 | Incyte Corp | Compuși pirolotriazină ca inhibitori TAM |
| 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 |
| JP7156287B2 (ja) | 2017-08-23 | 2022-10-19 | 小野薬品工業株式会社 | Ａｘｌ阻害剤を有効成分として含むがん治療剤 |
| SI3687996T1 (sl) | 2017-09-27 | 2022-04-29 | Incyte Corporation | Soli pirolotriazinskih derivatov, ki so uporabne kot zaviralci TAM |
| EP3695839A4 (en) | 2017-10-13 | 2021-07-14 | ONO Pharmaceutical Co., Ltd. | THERAPEUTIC AGENT WITH AXL INHIBITOR AS AN ACTIVE INGREDIENT FOR SOLID TUMORS |
| MD3813800T2 (ro) | 2018-06-29 | 2025-10-31 | Incyte Corp | Formulări de inhibitor al AXL/MER |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | 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 |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| JP2023527242A (ja) * | 2020-05-29 | 2023-06-27 | 南京正大天晴制薬有限公司 | Ａｘｌ阻害剤であるピリミジン系化合物 |
| JPWO2022220227A1 (https=) * | 2021-04-14 | 2022-10-20 | ||
| 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 |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | 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 |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
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 |
| WO1995003286A1 (en) | 1993-07-23 | 1995-02-02 | The Green Cross Corporation | Triazole derivative and pharmaceutical use thereof |
| GB9918180D0 (en) | 1999-08-02 | 1999-10-06 | Smithkline Beecham Plc | Novel compositions |
| DE60120494T2 (de) | 2000-12-22 | 2006-12-21 | Ortho-Mcneil Pharmaceutical, Inc. | Substituieten triazoldiamin derivaten und ihre verwendung als kinase inhibitoren |
| TW201041580A (en) | 2001-09-27 | 2010-12-01 | Alcon Inc | Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma |
| CN1290893C (zh) | 2002-05-03 | 2006-12-20 | 詹森药业有限公司 | 聚合物微乳状液 |
| US20060293256A1 (en) | 2002-08-06 | 2006-12-28 | Masateru Yamada | Remedy or preventive for kidney disease and method of diagnosing kidney disease |
| AU2003286746A1 (en) | 2002-10-29 | 2004-05-25 | Rigel Pharmaceuticals, Inc. | Modulators of angiogenesis and tumorigenesis |
| CL2003002353A1 (es) | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| WO2005013982A1 (en) | 2003-08-06 | 2005-02-17 | Vertex Pharmaceuticals Incorporated | Aminotriazole compounds useful as inhibitors of protein kinases |
| EP1720843A2 (en) | 2004-02-11 | 2006-11-15 | Janssen Pharmaceutica N.V. | Process for the preparation of substituted triazole compounds |
| WO2007030680A2 (en) | 2005-09-07 | 2007-03-15 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| WO2008045978A1 (en) | 2006-10-10 | 2008-04-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors |
| WO2008080134A2 (en) | 2006-12-22 | 2008-07-03 | Rigel Pharmaceuticals, Inc. | 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors |
| ES2672172T3 (es) | 2006-12-29 | 2018-06-12 | Rigel Pharmaceuticals, Inc. | Triazoles N3-heteroarilsustituidos y triazoles N5-heteroarilsustituidos útiles como inhibidores de Axl |
| WO2008083353A1 (en) | 2006-12-29 | 2008-07-10 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| EP2114955B1 (en) | 2006-12-29 | 2013-02-13 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| EP2078010B1 (en) | 2006-12-29 | 2014-01-29 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| EP2079736B1 (en) | 2006-12-29 | 2017-10-18 | Rigel Pharmaceuticals, Inc. | Substituted triazoles useful as axl inhibitors |
| AU2008266290A1 (en) | 2007-06-15 | 2008-12-24 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| WO2009054864A1 (en) | 2007-10-26 | 2009-04-30 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| US8309566B2 (en) | 2008-02-15 | 2012-11-13 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases |
| US8431594B2 (en) | 2008-07-09 | 2013-04-30 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as AXL inhibitors |
| CA2730231C (en) | 2008-07-09 | 2016-10-18 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| SG172997A1 (en) | 2009-01-16 | 2011-08-29 | Rigel Pharmaceuticals Inc | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
-
2009
- 2009-07-02 CA CA2730231A patent/CA2730231C/en active Active
- 2009-07-02 EP EP09790061.7A patent/EP2326641B1/en not_active Not-in-force
- 2009-07-02 JP JP2011517493A patent/JP5592884B2/ja not_active Expired - Fee Related
- 2009-07-02 US US13/002,487 patent/US8349838B2/en active Active
- 2009-07-02 WO PCT/US2009/049617 patent/WO2010005876A2/en not_active Ceased
- 2009-07-02 ES ES09790061.7T patent/ES2537480T3/es active Active
-
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
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