JP7075399B2 - Retキナーゼ阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物 - Google Patents
Retキナーゼ阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物 Download PDFInfo
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- JP7075399B2 JP7075399B2 JP2019519331A JP2019519331A JP7075399B2 JP 7075399 B2 JP7075399 B2 JP 7075399B2 JP 2019519331 A JP2019519331 A JP 2019519331A JP 2019519331 A JP2019519331 A JP 2019519331A JP 7075399 B2 JP7075399 B2 JP 7075399B2
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- 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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662406275P | 2016-10-10 | 2016-10-10 | |
| US62/406,275 | 2016-10-10 | ||
| US201762447849P | 2017-01-18 | 2017-01-18 | |
| US62/447,849 | 2017-01-18 | ||
| US201762491180P | 2017-04-27 | 2017-04-27 | |
| US62/491,180 | 2017-04-27 | ||
| US201762531690P | 2017-07-12 | 2017-07-12 | |
| US62/531,690 | 2017-07-12 | ||
| US201762566030P | 2017-09-29 | 2017-09-29 | |
| US62/566,030 | 2017-09-29 | ||
| PCT/US2017/055993 WO2018071454A1 (en) | 2016-10-10 | 2017-10-10 | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019533670A JP2019533670A (ja) | 2019-11-21 |
| JP2019533670A5 JP2019533670A5 (https=) | 2020-11-12 |
| JP7075399B2 true JP7075399B2 (ja) | 2022-05-25 |
Family
ID=60153576
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019519331A Expired - Fee Related JP7075399B2 (ja) | 2016-10-10 | 2017-10-10 | Retキナーゼ阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物 |
Country Status (35)
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| PL3371171T3 (pl) | 2015-11-02 | 2024-03-25 | Blueprint Medicines Corporation | Inhibitory RET |
| 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 |
| 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 |
| EP3541784B1 (en) * | 2016-11-18 | 2023-09-13 | Integrative Research Laboratories Sweden AB | Novel azetidine derivatives useful as modulators of cortical catecholaminergic neurotransmission |
| US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
| 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 |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CN111615514B (zh) | 2018-01-18 | 2022-10-11 | 奥瑞生物药品公司 | 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物 |
| WO2019143991A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| SI3773589T1 (sl) | 2018-04-03 | 2024-03-29 | Blueprint Medicines Corporation | Inhibitor RET za uporabo pri zdravljenju raka, ki ima RET spremembo |
| EP3849986B1 (en) | 2018-09-10 | 2022-06-08 | Array Biopharma, Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| TW202028209A (zh) * | 2018-09-27 | 2020-08-01 | 大陸商重慶複創醫藥研究有限公司 | 作為RET激酶抑制劑的取代的咪唑[1,2-a]吡啶和[1,2,4]三唑[1,5-a]吡啶化合物 |
| KR102558308B1 (ko) | 2018-09-27 | 2023-07-24 | 주식회사 엘지화학 | 3-아자바이사이클로[3,1,1]헵탄 유도체 및 이를 포함하는 약제학적 조성물 |
| EP3845531A4 (en) * | 2018-09-30 | 2021-11-24 | Applied Pharmaceutical Science, Inc. | SUBSTITUTED PYRAZOLE-CONDENSED RING DERIVATIVES, METHOD FOR THEIR PRODUCTION AND USE THEREOF |
| WO2020094084A1 (zh) * | 2018-11-07 | 2020-05-14 | 南京明德新药研发有限公司 | 作为ret抑制剂的三并环衍生物 |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| AU2019394519B2 (en) * | 2018-12-07 | 2025-02-13 | Sunshine Lake Pharma Co., Ltd. | RET inhibitors, pharmaceutical compositions and uses thereof |
| AU2019392232B2 (en) * | 2018-12-07 | 2025-02-13 | Sunshine Lake Pharma Co., Ltd. | RET inhibitors, pharmaceutical compositions and uses thereof |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| CN111808077B (zh) | 2019-04-12 | 2023-05-02 | 浙江海正药业股份有限公司 | 哌嗪酰胺衍生物,其制备方法及其在医药上的用途 |
| TW202108582A (zh) | 2019-05-14 | 2021-03-01 | 大陸商上海翰森生物醫藥科技有限公司 | 含二並環類衍生物抑制劑、其製備方法和應用 |
| US20220220128A1 (en) * | 2019-06-10 | 2022-07-14 | Js Innopharm (Shanghai) Ltd | Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
| WO2021043209A1 (zh) * | 2019-09-04 | 2021-03-11 | 广东东阳光药业有限公司 | 一种ret抑制剂、其药物组合物及其用途 |
| CN112574235B (zh) * | 2019-09-29 | 2024-01-16 | 广东东阳光药业股份有限公司 | 一种ret抑制剂、其药物组合物及其用途 |
| CN112574236B (zh) * | 2019-09-29 | 2024-08-09 | 广东东阳光药业股份有限公司 | 一种ret抑制剂、其药物组合物及其用途 |
| 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 |
| WO2021088911A1 (zh) * | 2019-11-08 | 2021-05-14 | 杭州邦顺制药有限公司 | 作为ret激酶抑制剂的3、6二氮杂双环[3.1.1]庚烷衍生物 |
| CN113045569B (zh) * | 2019-12-27 | 2022-04-19 | 浙江同源康医药股份有限公司 | 用作ret激酶抑制剂的化合物及其应用 |
| CN113121524B (zh) | 2019-12-31 | 2023-04-25 | 南京创济生物医药有限公司 | 杂环亚砜亚胺化合物及其中间体、制备方法和应用 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN111410662B (zh) * | 2020-03-27 | 2020-12-29 | 苏州信诺维医药科技有限公司 | 一种酪氨酸激酶抑制剂 |
| CN111269229B (zh) * | 2020-03-27 | 2021-02-12 | 苏州信诺维医药科技有限公司 | 一种治疗癌症的化合物 |
| CN111233899B (zh) * | 2020-03-27 | 2020-12-29 | 苏州信诺维医药科技有限公司 | 一种ret抑制剂 |
| CN111285887B (zh) * | 2020-03-27 | 2020-11-17 | 苏州信诺维医药科技有限公司 | 一种螺环化合物 |
| CN113527292B (zh) * | 2020-04-13 | 2025-07-22 | 广东东阳光药业股份有限公司 | 一种ret抑制剂、其药物组合物及其用途 |
| CN113527290B (zh) * | 2020-04-13 | 2025-07-22 | 广东东阳光药业股份有限公司 | 一种ret抑制剂、其药物组合物及其用途 |
| CN113527291B (zh) * | 2020-04-13 | 2025-07-22 | 广东东阳光药业股份有限公司 | Ret抑制剂、其药物组合物及其用途 |
| TW202144348A (zh) | 2020-04-22 | 2021-12-01 | 大陸商深圳晶泰科技有限公司 | 一種吡唑并[1,5-a]吡啶類衍生物及其製備方法,組合物以及用途 |
| CN113620944B (zh) * | 2020-05-07 | 2024-10-15 | 广东东阳光药业股份有限公司 | 新型的ret抑制剂、其药物组合物及其用途 |
| CN113683610B (zh) * | 2020-05-18 | 2025-02-25 | 广东东阳光药业股份有限公司 | 一种ret抑制剂、其药物组合物及其用途 |
| CN113683611B (zh) * | 2020-05-18 | 2025-02-11 | 广东东阳光药业股份有限公司 | 新的ret抑制剂、其药物组合物及其用途 |
| ES3059451T3 (en) * | 2020-05-20 | 2026-03-20 | Tyk Medicines Inc | Compound used as ret kinase inhibitor and application thereof |
| JP2023527412A (ja) | 2020-05-29 | 2023-06-28 | ブループリント メディシンズ コーポレイション | プラルセチニブの固体形態 |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED DEGRADATION OF RET |
| CN116528859A (zh) * | 2020-11-13 | 2023-08-01 | 上海翰森生物医药科技有限公司 | 含二并环类衍生物抑制剂自由碱的晶型及其制备方法和应用 |
| JP2024539137A (ja) | 2021-10-22 | 2024-10-28 | ユニバーシティー オブ ヒューストン システム | 上皮組織の慢性炎症性傷害、化生、異形成、および癌を処置するための方法および組成物 |
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| CN119768394A (zh) * | 2022-08-01 | 2025-04-04 | 江苏豪森药业集团有限公司 | 一种二并环类抑制剂的中间体及其制备方法 |
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| JP2011529032A (ja) | 2008-07-25 | 2011-12-01 | ガラパゴス・ナムローゼ・フェンノートシャップ | 変性及び炎症性疾患の治療に有用な新規化合物 |
| JP2012520867A (ja) | 2009-03-18 | 2012-09-10 | レスバーロジックス コーポレイション | 新規抗炎症剤 |
| JP2014512404A (ja) | 2011-04-28 | 2014-05-22 | ガラパゴス・ナムローゼ・フェンノートシャップ | 変性疾患及び炎症性疾患の治療に有用な新規化合物 |
| JP2015535242A (ja) | 2013-09-30 | 2015-12-10 | コリア リサーチ インスティテュート オブ ケミカル テクノロジー | 新規なトリアゾロピラジン誘導体及びその用途 |
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