CN104302646B - 可用作Raf激酶抑制剂的2-氨基, 6-苯基取代的吡啶并[2,3-d]嘧啶衍生物 - Google Patents
可用作Raf激酶抑制剂的2-氨基, 6-苯基取代的吡啶并[2,3-d]嘧啶衍生物 Download PDFInfo
- Publication number
- CN104302646B CN104302646B CN201380012913.9A CN201380012913A CN104302646B CN 104302646 B CN104302646 B CN 104302646B CN 201380012913 A CN201380012913 A CN 201380012913A CN 104302646 B CN104302646 B CN 104302646B
- Authority
- CN
- China
- Prior art keywords
- raf
- methyl
- cancer
- cells
- ras
- 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.)
- Expired - Fee Related
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261607702P | 2012-03-07 | 2012-03-07 | |
| US61/607702 | 2012-03-07 | ||
| PCT/US2013/029084 WO2013134243A1 (en) | 2012-03-07 | 2013-03-05 | 2-amino, 6-phenyl substituted pyrido [2, 3 - d] pyrimidine derivatives useful as raf kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104302646A CN104302646A (zh) | 2015-01-21 |
| CN104302646B true CN104302646B (zh) | 2016-05-04 |
Family
ID=47884613
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380012913.9A Expired - Fee Related CN104302646B (zh) | 2012-03-07 | 2013-03-05 | 可用作Raf激酶抑制剂的2-氨基, 6-苯基取代的吡啶并[2,3-d]嘧啶衍生物 |
Country Status (39)
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR090151A1 (es) * | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| KR20190017767A (ko) * | 2016-06-10 | 2019-02-20 | 노파르티스 아게 | C-raf 억제제의 치료적 용도 |
| EP3878850A1 (en) | 2016-12-22 | 2021-09-15 | Boehringer Ingelheim International GmbH | Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors |
| CN110545853A (zh) * | 2017-04-28 | 2019-12-06 | 石英治疗有限公司 | Raf降解偶联化合物 |
| PH12020550786A1 (en) | 2017-12-21 | 2021-04-12 | Boehringer Ingelheim Int | Novel benzylamino substituted pyridopyrimidinones and derivatives as sos1 inhibitors |
| JP7161849B2 (ja) * | 2018-01-24 | 2022-10-27 | 株式会社クラレ | 第一級アミンの製造方法 |
| JP2021512105A (ja) | 2018-01-31 | 2021-05-13 | デシフェラ・ファーマシューティカルズ，エルエルシー | 消化管間質腫瘍の治療のための併用療法 |
| JP7523351B2 (ja) | 2018-01-31 | 2024-07-26 | デシフェラ・ファーマシューティカルズ，エルエルシー | 肥満細胞症の治療のための併用療法 |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| LT3902547T (lt) | 2018-12-28 | 2024-01-25 | Deciphera Pharmaceuticals, Llc | Csf1r inhibitoriai, skirti panaudoti vėžio gydymui |
| MX2021009396A (es) | 2019-02-06 | 2021-09-10 | Lilly Co Eli | Derivados de 1 - ((2- (2,2,2-trifluoroetoxi) piridin-4-yl) metil) urea como potenciadores kcnq. |
| AR118119A1 (es) * | 2019-02-18 | 2021-09-22 | Genentech Inc | Compuestos de pirido-pirimidinilo y métodos de uso |
| WO2020227020A1 (en) * | 2019-05-03 | 2020-11-12 | Kinnate Biopharma Inc. | Inhibitors of raf kinases |
| HUE065486T2 (hu) | 2019-05-10 | 2024-05-28 | Deciphera Pharmaceuticals Llc | Fenilaminopirimidinamid autophágia inhibitorok és azok felhasználási eljárásai |
| PL3966206T3 (pl) | 2019-05-10 | 2024-01-29 | Deciphera Pharmaceuticals, Llc | Heteroaryloaminopirymidynoamidowe inhibitory autofagii i sposoby ich zastosowania |
| AU2020297422B2 (en) | 2019-06-17 | 2024-03-21 | Deciphera Pharmaceuticals, Llc | Aminopyrimidine amide autophagy inhibitors and methods of use thereof |
| NZ784949A (en) | 2019-08-12 | 2025-09-26 | Deciphera Pharmaceuticals Llc | Ripretinib for treating gastrointestinal stromal tumors |
| TWI878335B (zh) | 2019-08-12 | 2025-04-01 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| US11098031B1 (en) | 2019-10-24 | 2021-08-24 | Kinnate Biopharma Inc. | Inhibitors of RAF kinases |
| AU2020419197B2 (en) | 2019-12-30 | 2023-08-31 | Deciphera Pharmaceuticals, Llc | Amorphous kinase inhibitor formulations and methods of use thereof |
| NZ789199A (en) | 2019-12-30 | 2025-07-25 | Deciphera Pharmaceuticals Llc | Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea |
| KR20230019462A (ko) | 2020-06-02 | 2023-02-08 | 베링거 인겔하임 인터내셔날 게엠베하 | 암 치료용 고리형 2-아미노-3-시아노 티오펜 및 유도체 |
| US11407737B2 (en) | 2020-09-18 | 2022-08-09 | Kinnate Biopharma Inc. | Inhibitors of RAF kinases |
| US11377431B2 (en) | 2020-10-12 | 2022-07-05 | Kinnate Biopharma Inc. | Inhibitors of RAF kinases |
| WO2022090481A1 (en) | 2020-11-02 | 2022-05-05 | Boehringer Ingelheim International Gmbh | Substituted 1h-pyrazolo[4,3-c]pyridines and derivatives as egfr inhibitors |
| IL302807A (en) | 2020-11-18 | 2023-07-01 | Deciphera Pharmaceuticals Llc | Gcn2 and perk kinase inhibitors and methods of use thereof |
| CN117396472A (zh) | 2020-12-22 | 2024-01-12 | 上海齐鲁锐格医药研发有限公司 | Sos1抑制剂及其用途 |
| CN117561057A (zh) | 2021-04-23 | 2024-02-13 | 金耐特生物制药公司 | 用raf抑制剂治疗癌症 |
| US12065427B2 (en) | 2021-04-29 | 2024-08-20 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds capable of activating STING |
| CR20240233A (es) | 2021-12-01 | 2024-07-17 | Univ Vanderbilt | Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del cáncer |
| EP4441056A1 (en) | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2023099612A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| TW202340208A (zh) | 2021-12-01 | 2023-10-16 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
| WO2023099592A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| US20250145608A1 (en) | 2021-12-01 | 2025-05-08 | Boehringer Ingelheim Int'l GmbH Corp. | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| TW202337455A (zh) | 2021-12-09 | 2023-10-01 | 美商迪賽孚爾製藥有限公司 | Ｒａｆ激酶抑制劑及其使用方法 |
| CN119585242A (zh) | 2021-12-09 | 2025-03-07 | 德西费拉制药有限责任公司 | Raf激酶抑制剂及其使用方法 |
| EP4452975A1 (en) | 2021-12-23 | 2024-10-30 | Boehringer Ingelheim International GmbH | 8-aza quinazolines as brain-penetrant sos1-inhibitors |
| WO2023173017A1 (en) * | 2022-03-09 | 2023-09-14 | Blossomhill Therapeutics, Inc. | Kras inhibitors for treating disease |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
| TW202432115A (zh) | 2022-10-26 | 2024-08-16 | 德商百靈佳殷格翰國際股份有限公司 | 可活化sting之雜環化合物 |
| US20240174642A1 (en) | 2022-10-26 | 2024-05-30 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds capable of activating sting |
| WO2024088991A1 (en) | 2022-10-26 | 2024-05-02 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds capable of activating sting |
| 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 |
| WO2024246099A1 (en) | 2023-05-30 | 2024-12-05 | Boehringer Ingelheim International Gmbh | Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| GB2631397A (en) | 2023-06-28 | 2025-01-08 | Sevenless Therapeutics Ltd | New treatments for pain |
| 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 |
| GB2633813A (en) | 2023-09-21 | 2025-03-26 | Sevenless Therapeutics Ltd | New treatments for pain |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025083426A1 (en) | 2023-10-20 | 2025-04-24 | Sevenless Therapeutics Limited | New treatments for pain |
| WO2025122952A1 (en) | 2023-12-08 | 2025-06-12 | Deciphera Pharmaceuticals, Llc | Formulations of vimseltinib |
| WO2025137507A1 (en) | 2023-12-22 | 2025-06-26 | Regor Pharmaceuticals, Inc. | Sos1 inhibitors and uses thereof |
| WO2025146548A1 (en) | 2024-01-04 | 2025-07-10 | Sevenless Therapeutics Limited | Sos1 inhibitors useful to treat pain and cancer |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025210041A1 (en) | 2024-04-03 | 2025-10-09 | Boehringer Ingelheim International Gmbh | Bicyclic benzylamido pyridine derivatives as sos1 inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008034008A2 (en) * | 2006-09-14 | 2008-03-20 | Deciphera Pharmaceuticals, Llc. | Kinase inhibitors useful for the treatment of proliferative diseases |
| WO2011100319A1 (en) * | 2010-02-09 | 2011-08-18 | Exelixis, Inc. | Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1447405A4 (en) * | 2001-10-17 | 2005-01-12 | Kirin Brewery | CHINOLIN OR CHINAZOLINE DERIVATIVES THAT PREVENT THE AUTOPHOSPHORYLATION OF RECEPTORS FOR THE FIBROBLAST GROWTH FACTOR |
| AU2003280599A1 (en) * | 2002-10-29 | 2004-05-25 | Kirin Beer Kabushiki Kaisha | QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF Flt3 AND MEDICINAL COMPOSITIONS CONTAINING THE SAME |
| US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| US7897762B2 (en) | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| AR090151A1 (es) * | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
-
2013
- 2013-02-26 AR ARP130100576A patent/AR090151A1/es unknown
- 2013-02-27 TW TW102107122A patent/TW201348233A/zh unknown
- 2013-03-05 US US13/785,575 patent/US8741911B2/en not_active Expired - Fee Related
- 2013-03-05 RS RS20160416A patent/RS54840B1/sr unknown
- 2013-03-05 CN CN201380012913.9A patent/CN104302646B/zh not_active Expired - Fee Related
- 2013-03-05 US US14/383,799 patent/US9334267B2/en not_active Expired - Fee Related
- 2013-03-05 EP EP13712005.1A patent/EP2850082B1/en active Active
- 2013-03-05 AP AP2014007899A patent/AP2014007899A0/xx unknown
- 2013-03-05 WO PCT/US2013/029098 patent/WO2013134252A1/en not_active Ceased
- 2013-03-05 PE PE2014001381A patent/PE20142338A1/es not_active Application Discontinuation
- 2013-03-05 AU AU2013230146A patent/AU2013230146B2/en not_active Ceased
- 2013-03-05 IN IN1575MUN2014 patent/IN2014MN01575A/en unknown
- 2013-03-05 BR BR112014018528A patent/BR112014018528A8/pt not_active IP Right Cessation
- 2013-03-05 ES ES13712005.1T patent/ES2584387T3/es active Active
- 2013-03-05 SG SG11201404969YA patent/SG11201404969YA/en unknown
- 2013-03-05 KR KR1020147024732A patent/KR20140129087A/ko not_active Abandoned
- 2013-03-05 HR HRP20160654TT patent/HRP20160654T1/hr unknown
- 2013-03-05 HK HK15103082.6A patent/HK1202541A1/xx unknown
- 2013-03-05 WO PCT/US2013/029084 patent/WO2013134243A1/en not_active Ceased
- 2013-03-05 DK DK13712005.1T patent/DK2850082T3/en active
- 2013-03-05 CA CA2863673A patent/CA2863673A1/en not_active Abandoned
- 2013-03-05 MX MX2014010701A patent/MX2014010701A/es unknown
- 2013-03-05 LT LTEP13712005.1T patent/LT2850082T/lt unknown
- 2013-03-05 MA MA37316A patent/MA37316B1/fr unknown
- 2013-03-05 JP JP2014561029A patent/JP2015509536A/ja not_active Ceased
- 2013-03-05 HU HUE13712005A patent/HUE028095T2/en unknown
- 2013-03-05 ME MEP-2016-124A patent/ME02423B/me unknown
- 2013-03-05 SI SI201330188A patent/SI2850082T1/sl unknown
- 2013-03-05 PT PT137120051T patent/PT2850082T/pt unknown
- 2013-03-05 NZ NZ627454A patent/NZ627454A/en not_active IP Right Cessation
- 2013-03-05 EA EA201491456A patent/EA024824B1/ru not_active IP Right Cessation
- 2013-05-03 UA UAA201409109A patent/UA112340C2/uk unknown
-
2014
- 2014-07-24 CO CO14161404A patent/CO7010837A2/es unknown
- 2014-08-11 IL IL234052A patent/IL234052A/en not_active IP Right Cessation
- 2014-08-12 CR CR20140378A patent/CR20140378A/es unknown
- 2014-08-21 CL CL2014002220A patent/CL2014002220A1/es unknown
- 2014-09-03 TN TNP2014000375A patent/TN2014000375A1/fr unknown
- 2014-09-04 DO DO2014000200A patent/DOP2014000200A/es unknown
- 2014-09-05 EC ECIEPI201417584A patent/ECSP14017584A/es unknown
- 2014-09-05 PH PH12014501986A patent/PH12014501986B1/en unknown
-
2016
- 2016-07-22 CY CY20161100719T patent/CY1117846T1/el unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008034008A2 (en) * | 2006-09-14 | 2008-03-20 | Deciphera Pharmaceuticals, Llc. | Kinase inhibitors useful for the treatment of proliferative diseases |
| WO2011100319A1 (en) * | 2010-02-09 | 2011-08-18 | Exelixis, Inc. | Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors |
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Granted publication date: 20160504 Termination date: 20170305 |