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 (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 (43)
| 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 |
| CA2710043C (en) | 2006-12-29 | 2016-02-09 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| 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 |
| PL2114955T3 (pl) | 2006-12-29 | 2013-06-28 | Rigel Pharmaceuticals Inc | Triazole podstawione mostkowanym bicyklicznym arylem oraz mostkowanym bicyklicznym heteroarylem użyteczne jako inhibitory Axl |
| CN101622252B (zh) | 2006-12-29 | 2015-04-22 | 里格尔制药公司 | 用作axl抑制剂的取代三唑 |
| ME01832B (me) | 2006-12-29 | 2014-12-20 | Rigel Pharmaceuticals Inc | Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori |
| JP5635909B2 (ja) * | 2007-10-26 | 2014-12-03 | 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アリール置換トリアゾール及び多環ヘテロアリール置換トリアゾール |
| HRP20170317T1 (hr) | 2008-02-15 | 2017-04-21 | Rigel Pharmaceuticals, Inc. | Spojevi pirimidin-2-amina i njihova uporaba kao inhibitora jak kinaza |
| CA2730231C (en) | 2008-07-09 | 2016-10-18 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| CA2730251C (en) | 2008-07-09 | 2016-08-09 | 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 |
| BRPI1007046B1 (pt) | 2009-01-16 | 2019-07-16 | Rigel Pharmaceuticals, Inc. | Inibidores axl para uso em terapia de combinação para evitar, tratar ou controlar o câncer metastático. |
| 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 |
| PT2810937T (pt) | 2012-01-31 | 2017-03-03 | Daiichi Sankyo Co Ltd | Derivado de piridona |
| CN105916506B (zh) | 2013-11-20 | 2020-01-07 | 圣诺康生命科学公司 | 作为tam家族激酶抑制剂的喹唑啉衍生物 |
| WO2015081257A2 (en) | 2013-11-27 | 2015-06-04 | Signalchem Lifesciences Corporation | Aminopyridine derivatives as tam family kinase inhibitors |
| 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 |
| 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 |
| ES2896079T3 (es) | 2016-02-26 | 2022-02-23 | Ono Pharmaceutical Co | Fármaco para la terapia del cáncer, caracterizado por la administración de la combinación entre un inhibidor de Axl y un inhibidor del punto de control inmunitario |
| WO2017172596A1 (en) | 2016-03-28 | 2017-10-05 | Incyte Corporation | Pyrrolotriazine compounds as tam inhibitors |
| 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 |
| CA3077308A1 (en) | 2017-09-27 | 2019-04-04 | Incyte Corporation | Salts of pyrrolotriazine derivatives useful as tam inhibitors |
| US11826363B2 (en) | 2017-10-13 | 2023-11-28 | Ono Pharmaceutical Co., Ltd. | Therapeutic agent for solid cancers, which comprises Axl inhibitor as active ingredient |
| PL3813800T3 (pl) | 2018-06-29 | 2025-08-18 | Incyte Corporation | Formulacje inhibitora axl/mer |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| AU2021230385A1 (en) | 2020-03-06 | 2022-09-22 | Incyte Corporation | Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors |
| AU2021280113B2 (en) * | 2020-05-29 | 2023-12-21 | Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. | Pyrimidine compound as AXL inhibitor |
| JPWO2022220227A1 (enExample) * | 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 |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of 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 |
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 |
| US5750545A (en) | 1993-07-23 | 1998-05-12 | The Green Cross Corporation | Triazole derivative and pharmaceutical use thereof |
| GB9918180D0 (en) | 1999-08-02 | 1999-10-06 | Smithkline Beecham Plc | Novel compositions |
| BR0116792A (pt) | 2000-12-22 | 2004-02-17 | Ortho Mcneil Pharm Inc | Derivados de diamina de triazol substituìdos como inibidores de quinase |
| TWI335221B (en) | 2001-09-27 | 2011-01-01 | Alcon Inc | Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma |
| MXPA04010778A (es) | 2002-05-03 | 2005-03-07 | Janssen Pharmaceutica Nv | Microemulsiones polimericas. |
| CN100345593C (zh) | 2002-08-06 | 2007-10-31 | 东丽株式会社 | 用于制备肾脏疾病的治疗或预防药物中的用途 |
| US8574827B2 (en) | 2002-10-29 | 2013-11-05 | Rigel Pharmaceuticals, Inc. | Modulators of angiogenesis and tumorigenesis |
| AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| AR045731A1 (es) | 2003-08-06 | 2005-11-09 | Vertex Pharma | Compuestos de aminotriazol utiles como inhibidores de quinasas de proteinas |
| KR20070036025A (ko) | 2004-02-11 | 2007-04-02 | 얀센 파마슈티카 엔.브이. | 치환된 트리아졸 화합물의 제조방법 |
| 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 |
| CN101622252B (zh) | 2006-12-29 | 2015-04-22 | 里格尔制药公司 | 用作axl抑制剂的取代三唑 |
| ME01832B (me) | 2006-12-29 | 2014-12-20 | Rigel Pharmaceuticals Inc | Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori |
| 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 |
| CA2710043C (en) | 2006-12-29 | 2016-02-09 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| PL2114955T3 (pl) | 2006-12-29 | 2013-06-28 | Rigel Pharmaceuticals Inc | Triazole podstawione mostkowanym bicyklicznym arylem oraz mostkowanym bicyklicznym heteroarylem użyteczne jako inhibitory Axl |
| WO2008157131A1 (en) | 2007-06-15 | 2008-12-24 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| JP5635909B2 (ja) * | 2007-10-26 | 2014-12-03 | 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アリール置換トリアゾール及び多環ヘテロアリール置換トリアゾール |
| HRP20170317T1 (hr) | 2008-02-15 | 2017-04-21 | Rigel Pharmaceuticals, Inc. | Spojevi pirimidin-2-amina i njihova uporaba kao inhibitora jak kinaza |
| CA2730231C (en) | 2008-07-09 | 2016-10-18 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| CA2730251C (en) | 2008-07-09 | 2016-08-09 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| BRPI1007046B1 (pt) | 2009-01-16 | 2019-07-16 | Rigel Pharmaceuticals, Inc. | Inibidores axl para uso em terapia de combinação para evitar, tratar ou controlar o câncer metastático. |
-
2009
- 2009-07-02 CA CA2730231A patent/CA2730231C/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
- 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 EP EP09790061.7A patent/EP2326641B1/en not_active Not-in-force
-
2012
- 2012-12-21 US US13/725,407 patent/US9079898B2/en active Active
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2015
- 2015-04-16 US US14/688,843 patent/US9173882B2/en not_active Expired - Fee Related