CN104520300B - 作为激酶抑制剂的咪唑并[1,2-b]哒嗪衍生物 - Google Patents
作为激酶抑制剂的咪唑并[1,2-b]哒嗪衍生物 Download PDFInfo
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- CN104520300B CN104520300B CN201380041498.XA CN201380041498A CN104520300B CN 104520300 B CN104520300 B CN 104520300B CN 201380041498 A CN201380041498 A CN 201380041498A CN 104520300 B CN104520300 B CN 104520300B
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- Prior art keywords
- compound
- amino
- imidazo
- phenyl
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2012-127079 | 2012-06-04 | ||
| JP2012127079 | 2012-06-04 | ||
| PCT/JP2013/065328 WO2013183578A1 (ja) | 2012-06-04 | 2013-06-03 | キナーゼ阻害剤としてのイミダゾ[１，２－ｂ]ピリダジン誘導体 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104520300A CN104520300A (zh) | 2015-04-15 |
| CN104520300B true CN104520300B (zh) | 2016-12-21 |
Family
ID=49711970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380041498.XA Active CN104520300B (zh) | 2012-06-04 | 2013-06-03 | 作为激酶抑制剂的咪唑并[1,2-b]哒嗪衍生物 |
Country Status (32)
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2350075T3 (da) | 2008-09-22 | 2014-05-26 | Array Biopharma Inc | Substituerede imidazo[1,2b]pyridazinforbindelser som trk-kinase-inhibitorer |
| PT3106463T (pt) | 2008-10-22 | 2018-05-18 | Array Biopharma Inc | Compostos de pirazolo[1,5-]pirimidina substituídos como inibidores de cinase trk |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| RU2735545C2 (ru) | 2010-05-20 | 2020-11-03 | Эррэй Биофарма Инк. | Макроциклические соединения в качестве ингибиторов киназы trk |
| AU2013268400B2 (en) | 2012-05-30 | 2017-07-13 | Nippon Shinyaku Co., Ltd. | Aromatic heterocyclic derivative and pharmaceutical |
| WO2015144801A1 (en) * | 2014-03-27 | 2015-10-01 | Janssen Pharmaceutica Nv | SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AND 2,3-DIHYDRO-1H-IMIDAZO[1,2-b]PYRAZOLE DERIVATIVES AS ROS1 INHIBITORS |
| CN106164076B (zh) | 2014-03-27 | 2019-03-26 | 詹森药业有限公司 | 作为ros1抑制剂的化合物 |
| EP3906921A1 (en) * | 2014-04-25 | 2021-11-10 | Exelixis, Inc. | Method of treating lung adenocarcinoma |
| EP3218380B1 (en) | 2014-11-16 | 2021-03-17 | Array Biopharma, Inc. | Preparation of a crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| PE20180329A1 (es) | 2015-06-01 | 2018-02-13 | Loxo Oncology Inc | Metodos para diagnosticar y tratar el cancer |
| BR112017027339A2 (pt) | 2015-06-18 | 2018-09-04 | Cephalon, Inc. | derivados de piperidina 1,4-substituída |
| US10919875B2 (en) | 2015-06-18 | 2021-02-16 | 89Bio Ltd | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
| PT3322706T (pt) | 2015-07-16 | 2021-03-08 | Array Biopharma Inc | Compostos de pirazolo[1,5-a]piridina substituídos como inibidores da quinase do ret |
| TN2019000271A1 (en) | 2015-10-26 | 2021-01-07 | Univ Colorado Regents | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| CN106854174A (zh) * | 2015-12-08 | 2017-06-16 | 湖南华腾制药有限公司 | 一种4位取代哌啶衍生物的制备方法 |
| IL304018A (en) | 2016-04-04 | 2023-08-01 | Loxo Oncology Inc | Liquid formulations of (S)-N-(5-((R)-2-(5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-A]pyrimidin-3-yl)-3 -hydroxypyrrolidine-1-carboxamide |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| TN2019000332A1 (en) | 2016-04-04 | 2021-05-07 | Loxo Oncology Inc | Methods of treating pediatric cancers |
| ES2952056T3 (es) | 2016-05-18 | 2023-10-26 | Loxo Oncology Inc | Preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
| CN107400082A (zh) * | 2016-05-19 | 2017-11-28 | 湖南华腾制药有限公司 | 一种取代哌啶衍生物的制备方法 |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| JOP20190072A1 (ar) * | 2016-10-13 | 2019-04-07 | Glaxosmithkline Ip Dev Ltd | مشتقات 1، 3 سيكلوبوتان ثنائي الاستبدال أو آزيتيدين كمثبطات للإنزيم المخلق للبروستاجلاندين d المكون للدم |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JP6888101B2 (ja) | 2017-01-18 | 2021-06-16 | アレイ バイオファーマ インコーポレイテッド | ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物 |
| CA3055504A1 (en) * | 2017-03-14 | 2018-09-20 | Daiichi Sankyo Company, Limited | Method for producing 3,6-disubstituted imidazo[1,2-b]pyridazine derivative |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| US10180422B1 (en) | 2017-08-22 | 2019-01-15 | Scripps Health | Methods of treating a neuroendocrine tumor |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| US20190247398A1 (en) | 2017-10-26 | 2019-08-15 | Array Biopharma Inc. | Formulations of a macrocyclic trk kinase inhibitor |
| CN109748902B (zh) * | 2017-11-02 | 2020-11-06 | 杭州科巢生物科技有限公司 | 一种盐酸安罗替尼的制备方法 |
| KR102078775B1 (ko) | 2017-11-29 | 2020-02-19 | 서울대학교산학협력단 | 항-ros1 항체 및 그의 용도 |
| CN108129288B (zh) * | 2017-12-27 | 2021-01-22 | 上海毕得医药科技股份有限公司 | 一种反式-3-羟基环丁基甲酸的合成方法 |
| JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物 |
| WO2019143977A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| WO2019143991A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| US20210023086A1 (en) | 2018-03-29 | 2021-01-28 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| MX2021000795A (es) | 2018-07-24 | 2021-04-12 | Taiho Pharmaceutical Co Ltd | Compuestos heterociclicos para inhibir la actividad de shp2. |
| JP7286755B2 (ja) | 2018-07-31 | 2023-06-05 | ロクソ オンコロジー， インコーポレイテッド | （ｓ）－５－アミノ－３－（４－（（５－フルオロ－２－メトキシベンズアミド）メチル）フェニル）－１－（１，１，１－トリフルオロプロパン－２－イル）－１ｈ－ピラゾール－４－カルボキサミドの噴霧乾燥分散体および製剤 |
| CA3111984A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| JP2022515198A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物 |
| CN113474337A (zh) | 2018-12-19 | 2021-10-01 | 奥瑞生物药品公司 | 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物 |
| CN113543852A (zh) * | 2019-03-06 | 2021-10-22 | 第一三共株式会社 | 吡咯并吡唑衍生物 |
| 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 |
| WO2020224626A1 (zh) * | 2019-05-08 | 2020-11-12 | 浙江同源康医药股份有限公司 | 用作激酶抑制剂的化合物及其应用 |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| CA3159348A1 (en) | 2019-11-08 | 2021-05-14 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | 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 |
| AR122159A1 (es) * | 2020-05-28 | 2022-08-17 | Novartis Ag | Inhibidores de mll1 y agentes antineoplásicos |
| CN114957259A (zh) * | 2021-02-25 | 2022-08-30 | 南京明德新药研发有限公司 | 氰基取代的芳香双环类化合物及其应用 |
| WO2023272701A1 (en) * | 2021-07-01 | 2023-01-05 | Anheart Therapeutics (Hangzhou) Co., Ltd. | Crystalline forms of 3-{4-[(2r)-2-aminopropoxy]phenyl}-n-[(1r)- 1-(3-fluorophenyl) ethyl]imidazo[1,2-b]pyridazin-6-amine and salts thereof |
| JP2025515952A (ja) * | 2022-05-18 | 2025-05-20 | アンハート セラピューティクス（ハンチョウ）コーポレーション，リミテッド | ３，６－二置換－イミダゾ［１，２－ｂ］ピリダジン化合物の製造方法 |
| CN114989176B (zh) * | 2022-07-08 | 2024-08-27 | 深圳市新樾生物科技有限公司 | 咪唑并哒嗪类衍生物及其应用 |
| CN115197115B (zh) * | 2022-08-25 | 2024-11-08 | 成都金博汇康医药科技有限公司 | 一种手性5-氧代吡咯烷-3-甲酸的制备方法与应用 |
| US20260028352A1 (en) | 2022-09-07 | 2026-01-29 | Suzhou Langrui Biopharmaceutical Co., Ltd. | Macrocyclic imidazo [1,2-b] pyridazine derivative, preparation method therefor, and use thereof |
| CN117659020A (zh) * | 2022-09-07 | 2024-03-08 | 苏州朗睿生物医药有限公司 | 一种咪唑并[1,2-b]哒嗪衍生物及其制备方法和用途 |
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2013
- 2013-05-31 TW TW102119261A patent/TWI585088B/zh active
- 2013-06-03 ES ES13801320.6T patent/ES2648228T3/es active Active
- 2013-06-03 NZ NZ702574A patent/NZ702574A/en unknown
- 2013-06-03 NO NO13801320A patent/NO2857404T3/no unknown
- 2013-06-03 PL PL13801320T patent/PL2857404T3/pl unknown
- 2013-06-03 US US14/378,318 patent/US9187489B2/en active Active
- 2013-06-03 CA CA2874819A patent/CA2874819C/en active Active
- 2013-06-03 SI SI201330798T patent/SI2857404T1/sl unknown
- 2013-06-03 JP JP2014519977A patent/JP5814467B2/ja active Active
- 2013-06-03 BR BR112014029851-3A patent/BR112014029851B1/pt active IP Right Grant
- 2013-06-03 EP EP13801320.6A patent/EP2857404B1/en active Active
- 2013-06-03 HR HRP20171724TT patent/HRP20171724T1/hr unknown
- 2013-06-03 HU HUE13801320A patent/HUE037221T2/hu unknown
- 2013-06-03 MY MYPI2014003346A patent/MY170326A/en unknown
- 2013-06-03 LT LTEP13801320.6T patent/LT2857404T/lt unknown
- 2013-06-03 MX MX2014014803A patent/MX357021B/es active IP Right Grant
- 2013-06-03 PT PT138013206T patent/PT2857404T/pt unknown
- 2013-06-03 RS RS20171198A patent/RS56625B1/sr unknown
- 2013-06-03 SG SG11201408052WA patent/SG11201408052WA/en unknown
- 2013-06-03 RU RU2014153627A patent/RU2635917C2/ru active
- 2013-06-03 CN CN201380041498.XA patent/CN104520300B/zh active Active
- 2013-06-03 AU AU2013272701A patent/AU2013272701B2/en active Active
- 2013-06-03 IN IN2497MUN2014 patent/IN2014MN02497A/en unknown
- 2013-06-03 DK DK13801320.6T patent/DK2857404T3/en active
- 2013-06-03 KR KR1020147033351A patent/KR101781255B1/ko active Active
- 2013-06-03 SM SM20170539T patent/SMT201700539T1/it unknown
- 2013-06-03 WO PCT/JP2013/065328 patent/WO2013183578A1/ja not_active Ceased
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2014
- 2014-12-02 ZA ZA2014/08843A patent/ZA201408843B/en unknown
- 2014-12-04 IL IL236075A patent/IL236075A/en active IP Right Grant
- 2014-12-04 PH PH12014502721A patent/PH12014502721B1/en unknown
- 2014-12-30 CO CO14286593A patent/CO7160119A2/es unknown
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2015
- 2015-10-29 US US14/926,973 patent/US9751887B2/en active Active
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2017
- 2017-11-15 CY CY20171101204T patent/CY1119607T1/el unknown
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| US20080167314A1 (en) * | 2004-12-28 | 2008-07-10 | Osamu Uchikawa | Condensed Imidazole Compound And Use Thereof |
| CN101522682A (zh) * | 2006-10-30 | 2009-09-02 | 诺瓦提斯公司 | 作为抗炎剂的杂环化合物 |
| WO2008072682A1 (ja) * | 2006-12-15 | 2008-06-19 | Daiichi Sankyo Company, Limited | イミダゾ［１，２－ｂ］ピリダジン誘導体 |
| JP2009227599A (ja) * | 2008-03-21 | 2009-10-08 | Daiichi Sankyo Co Ltd | イミダゾピリダジン誘導体 |
| CN102056927A (zh) * | 2008-05-13 | 2011-05-11 | Irm责任有限公司 | 作为激酶抑制剂的稠合含氮杂环及其组合物 |
| CN102224153A (zh) * | 2008-09-22 | 2011-10-19 | 阵列生物制药公司 | 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物 |
| WO2011049332A2 (en) * | 2009-10-22 | 2011-04-28 | Korea Institute Of Science And Technology | 2,7-substituted thieno[3,2-d]pyrimidine compounds as protein kinase inhibitors |
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