JP5814467B2 - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP5814467B2 JP5814467B2 JP2014519977A JP2014519977A JP5814467B2 JP 5814467 B2 JP5814467 B2 JP 5814467B2 JP 2014519977 A JP2014519977 A JP 2014519977A JP 2014519977 A JP2014519977 A JP 2014519977A JP 5814467 B2 JP5814467 B2 JP 5814467B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- compound
- imidazo
- phenyl
- amino
- 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.)
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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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2014519977A JP5814467B2 (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 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2012127079 | 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 |
| JP2014519977A JP5814467B2 (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 |
|---|---|
| JP5814467B2 true JP5814467B2 (ja) | 2015-11-17 |
| JPWO2013183578A1 JPWO2013183578A1 (ja) | 2016-01-28 |
Family
ID=49711970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014519977A Active JP5814467B2 (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 |
Country Status (32)
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS53350B (sr) | 2008-09-22 | 2014-10-31 | Array Biopharma, Inc. | Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze |
| HRP20140309T1 (hr) | 2008-10-22 | 2014-05-09 | Array Biopharma, Inc. | SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIMIDINA KAO INHIBITORI TRK KINAZE |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| KR102015402B1 (ko) | 2010-05-20 | 2019-08-28 | 어레이 바이오파마 인크. | Trk 키나제 저해제로서의 매크로시클릭 화합물 |
| AU2013268400B2 (en) | 2012-05-30 | 2017-07-13 | Nippon Shinyaku Co., Ltd. | Aromatic heterocyclic derivative and pharmaceutical |
| EP3126366B1 (en) * | 2014-03-27 | 2018-06-06 | Janssen Pharmaceutica, N.V. | 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 |
| BR112016022105B1 (pt) * | 2014-03-27 | 2023-01-31 | Janssen Pharmaceutica Nv | Derivados de 4,5,6,7-tetra-hidro-pirazolo[1,5- a]pirazina substituídos e derivados de 5,6,7,8-tetrahidro-4h-pirazolo[1,5-a][1,4]diazepina como inibidores do ros1 e composição farmacêutica que os compreende |
| EP3906921A1 (en) * | 2014-04-25 | 2021-11-10 | Exelixis, Inc. | Method of treating lung adenocarcinoma |
| JP6914834B2 (ja) | 2014-11-16 | 2021-08-04 | アレイ バイオファーマ インコーポレイテッド | （Ｓ）−Ｎ−（５−（（Ｒ）−２−（２，５−ジフルオロフェニル）−ピロリジン−１−イル）−ピラゾロ［１，５−ａ］ピリミジン−３−イル）−３−ヒドロキシピロリジン−１−カルボキサミド硫酸水素塩の結晶形 |
| KR20180021745A (ko) | 2015-06-01 | 2018-03-05 | 록쏘 온콜로지, 인코포레이티드 | 암을 진단하고 치료하는 방법 |
| MX379846B (es) | 2015-06-18 | 2025-03-11 | 89Bio Ltd | Derivados de 4-bencil y 4-benzoil piperidina sustituidos. |
| WO2016205633A1 (en) | 2015-06-18 | 2016-12-22 | Cephalon, Inc. | 1, 4-substituted piperidine derivatives |
| HUE053067T2 (hu) | 2015-07-16 | 2021-06-28 | Array Biopharma Inc | Helyettesített pirazolo[1,5-A]piridin vegyületek, mint RET kináz inhibitorok |
| TN2018000138A1 (en) | 2015-10-26 | 2019-10-04 | Array Biopharma Inc | 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 |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| ES2987501T3 (es) | 2016-04-04 | 2024-11-15 | Loxo Oncology Inc | Métodos de tratamiento de cánceres pediátricos |
| AU2017246554B2 (en) | 2016-04-04 | 2022-08-18 | Loxo Oncology, Inc. | Liquid formulations of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| KR102566858B1 (ko) | 2016-05-18 | 2023-08-11 | 어레이 바이오파마 인크. | (s)-n-(5-((r)-2-(2,5-디플루오로페닐)피롤리딘-1-일)-피라졸로[1,5-a]피리미딘-3-일)-3-히드록시피롤리딘-1-카르복사미드의 제조 방법 |
| 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 |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 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 |
| 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 |
| US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
| RS64354B1 (sr) * | 2017-03-14 | 2023-08-31 | Daiichi Sankyo Co Ltd | Postupak za proizvodnju derivata 3, 6-disupstituisanog imidazo[1, 2-b]piridazina |
| 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 |
| 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 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 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 |
| WO2019084285A1 (en) | 2017-10-26 | 2019-05-02 | Qian Zhao | 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 |
| WO2019107671A1 (ko) * | 2017-11-29 | 2019-06-06 | 서울대학교 산학협력단 | 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 |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CA3087972C (en) | 2018-01-18 | 2023-01-10 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CA3095366A1 (en) | 2018-03-29 | 2019-10-03 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| SG11202100719YA (en) | 2018-07-24 | 2021-02-25 | Taiho Pharmaceutical Co Ltd | Heterobicyclic compounds for inhibiting the activity of shp2 |
| CA3224985C (en) | 2018-07-31 | 2025-11-18 | Loxo Oncology, Inc. | SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE |
| JP2022500383A (ja) | 2018-09-10 | 2022-01-04 | 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縮合複素環式化合物 |
| 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 |
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| KR20210135521A (ko) | 2019-03-06 | 2021-11-15 | 다이이찌 산쿄 가부시키가이샤 | 피롤로피라졸 유도체 |
| EP3942045A1 (en) | 2019-03-21 | 2022-01-26 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| AU2020270303B2 (en) * | 2019-05-08 | 2023-09-07 | Tyk Medicines, Inc. | Compound used as kinase inhibitor and application thereof |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| 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 |
| TW202200589A (zh) * | 2020-05-28 | 2022-01-01 | 瑞士商諾華公司 | Ｍｌｌ１抑制劑及抗癌劑 |
| 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 |
| CA3223035A1 (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 |
| IL316837A (en) * | 2022-05-18 | 2025-01-01 | Anheart Therapeutics Hangzhou Co Ltd | METHOD FOR PRODUCING 3,6-DISUPTATED-IMIDAZO[1,2-B]PYRIDAZINE COMPOUNDS |
| 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 |
| KR20250056969A (ko) | 2022-09-07 | 2025-04-28 | 수저우 랑루이 바이오파마슈티컬 씨오 엘티디 | 마크로시클릭 이미다조[1,2-b]피리다진 유도체 및 이의 제조 방법과 용도 |
| 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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| JP2003231687A (ja) | 2002-02-04 | 2003-08-19 | Japan Tobacco Inc | ピラゾリル縮合環化合物及びその医薬用途 |
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| JP2007533717A (ja) | 2004-04-21 | 2007-11-22 | アストラゼネカ アクチボラグ | 化合物 |
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| WO2006087538A1 (en) | 2005-02-16 | 2006-08-24 | Astrazeneca Ab | Chemical compounds |
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| 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 |
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| JPWO2012005299A1 (ja) | 2010-07-07 | 2013-09-05 | 日本新薬株式会社 | Ｒｏｓチロシンキナーゼ阻害剤 |
| WO2012125667A1 (en) | 2011-03-17 | 2012-09-20 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
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2013
- 2013-05-31 TW TW102119261A patent/TWI585088B/zh active
- 2013-06-03 WO PCT/JP2013/065328 patent/WO2013183578A1/ja not_active Ceased
- 2013-06-03 DK DK13801320.6T patent/DK2857404T3/en active
- 2013-06-03 SI SI201330798T patent/SI2857404T1/sl unknown
- 2013-06-03 US US14/378,318 patent/US9187489B2/en active Active
- 2013-06-03 RU RU2014153627A patent/RU2635917C2/ru active
- 2013-06-03 PT PT138013206T patent/PT2857404T/pt unknown
- 2013-06-03 SM SM20170539T patent/SMT201700539T1/it unknown
- 2013-06-03 NO NO13801320A patent/NO2857404T3/no 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 RS RS20171198A patent/RS56625B1/sr unknown
- 2013-06-03 MY MYPI2014003346A patent/MY170326A/en unknown
- 2013-06-03 HR HRP20171724TT patent/HRP20171724T1/hr unknown
- 2013-06-03 NZ NZ702574A patent/NZ702574A/en unknown
- 2013-06-03 CA CA2874819A patent/CA2874819C/en active Active
- 2013-06-03 SG SG11201408052WA patent/SG11201408052WA/en unknown
- 2013-06-03 CN CN201380041498.XA patent/CN104520300B/zh active Active
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