CN112771043A - 取代吡唑稠环类衍生物及其制备方法和应用 - Google Patents
取代吡唑稠环类衍生物及其制备方法和应用 Download PDFInfo
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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- 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
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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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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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
- A61K31/4427—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
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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
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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
- A61K31/495—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
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
-
- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Abstract
涉及药物化学领域,主要涉及式I所示的化合物、其立体异构体、消旋体、互变异构体、同位素标记物、氮氧化物、或其药学上可接受的盐及其制备方法和在制备用于治疗RET激酶介导的疾病的药物中的用途。
Description
PCT国内申请,说明书已公开。
Claims (10)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2018111624971 | 2018-09-30 | ||
CN201811162497 | 2018-09-30 | ||
PCT/CN2019/109502 WO2020064009A1 (zh) | 2018-09-30 | 2019-09-30 | 取代吡唑稠环类衍生物及其制备方法和应用 |
Publications (2)
Publication Number | Publication Date |
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CN112771043A true CN112771043A (zh) | 2021-05-07 |
CN112771043B CN112771043B (zh) | 2023-04-28 |
Family
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CN201910942753.7A Active CN110964008B (zh) | 2018-09-30 | 2019-09-30 | 取代吡唑稠环类衍生物及其制备方法和应用 |
CN201980064157.1A Active CN112771043B (zh) | 2018-09-30 | 2019-09-30 | 取代吡唑稠环类衍生物及其制备方法和应用 |
CN202210125578.4A Active CN114380825B (zh) | 2018-09-30 | 2019-09-30 | 取代吡唑稠环类衍生物及其制备方法和应用 |
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CN201910942753.7A Active CN110964008B (zh) | 2018-09-30 | 2019-09-30 | 取代吡唑稠环类衍生物及其制备方法和应用 |
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CN202210125578.4A Active CN114380825B (zh) | 2018-09-30 | 2019-09-30 | 取代吡唑稠环类衍生物及其制备方法和应用 |
Country Status (6)
Country | Link |
---|---|
US (1) | US20210379056A1 (zh) |
EP (1) | EP3845531A4 (zh) |
JP (1) | JP2022508533A (zh) |
KR (1) | KR20210070286A (zh) |
CN (3) | CN110964008B (zh) |
WO (1) | WO2020064009A1 (zh) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
WO2021023209A1 (zh) * | 2019-08-05 | 2021-02-11 | 北京志健金瑞生物医药科技有限公司 | 含氮多环稠环类化合物,其药物组合物、制备方法和用途 |
WO2021057963A1 (zh) * | 2019-09-29 | 2021-04-01 | 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 |
CN112851664B (zh) * | 2019-11-12 | 2024-03-29 | 浙江海正药业股份有限公司 | 吡唑[1,5-a]吡啶-3-腈化合物及其在医药上的用途 |
US20230095530A1 (en) * | 2019-12-27 | 2023-03-30 | TYK Medicines, Inc | Compound used as ret kinase inhibitor and application thereof |
TW202202501A (zh) * | 2020-04-17 | 2022-01-16 | 美商絡速藥業公司 | 結晶ret抑制劑 |
CA3191183A1 (en) * | 2020-08-20 | 2022-02-24 | Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd. | Heteroaromatic ring compound as ret kinase inhibitor, and preparation and use thereof |
US20230365596A1 (en) * | 2020-09-29 | 2023-11-16 | Guangzhou Baiyunshan Pharmaceutical Holdings Co., Ltd. Baiyunshan Pharmaceutical General Factory | Crystal forms of pyridopyrazole compounds and preparation method therefor |
WO2022083741A1 (zh) * | 2020-10-23 | 2022-04-28 | 上海辉启生物医药科技有限公司 | 吡唑并吡啶类化合物或其盐及其制备方法和用途 |
TWI818424B (zh) * | 2021-02-08 | 2023-10-11 | 大陸商北京志健金瑞生物醫藥科技有限公司 | 含氮多環稠環類化合物,其藥物組合物、製備方法和用途 |
CN115594678A (zh) * | 2021-07-09 | 2023-01-13 | 北京志健金瑞生物医药科技有限公司(Cn) | 含氮多环稠环类化合物的制备方法及其中间体和用途 |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
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US20180133207A1 (en) * | 2016-10-10 | 2018-05-17 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
TW201825488A (zh) * | 2016-10-10 | 2018-07-16 | 美商亞雷生物製藥股份有限公司 | 作為pet激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
WO2018136661A1 (en) * | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
CN108349969A (zh) * | 2015-07-16 | 2018-07-31 | 阵列生物制药公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡啶化合物 |
WO2019075108A1 (en) * | 2017-10-10 | 2019-04-18 | Metcalf Andrew T | CRYSTALLINE FORMS |
WO2019075114A1 (en) * | 2017-10-10 | 2019-04-18 | Mark Reynolds | FORMULATIONS COMPRISING 6- (2-HYDROXY-2-METHYLPROPOXY) -4- (6- (6 - ((6-METHOXYPYRIDIN-3-YL) METHYL) -3,6-DIAZABICYCLO [3.1.1] HEPTAN-3- YL) PYRIDIN-3-YL) PYRAZOLO [1,5-A] pYRIDINE-3-carbonitrile |
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AR086042A1 (es) * | 2011-04-28 | 2013-11-13 | Galapagos Nv | Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica |
CN103814020B (zh) * | 2011-06-17 | 2017-07-14 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
CN102827073A (zh) * | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
TWI783057B (zh) * | 2017-10-10 | 2022-11-11 | 美商絡速藥業公司 | 製備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-甲腈的方法 |
-
2019
- 2019-09-30 EP EP19865058.2A patent/EP3845531A4/en active Pending
- 2019-09-30 CN CN201910942753.7A patent/CN110964008B/zh active Active
- 2019-09-30 CN CN201980064157.1A patent/CN112771043B/zh active Active
- 2019-09-30 US US17/281,567 patent/US20210379056A1/en active Pending
- 2019-09-30 WO PCT/CN2019/109502 patent/WO2020064009A1/zh unknown
- 2019-09-30 JP JP2021542252A patent/JP2022508533A/ja active Pending
- 2019-09-30 KR KR1020217009429A patent/KR20210070286A/ko active Search and Examination
- 2019-09-30 CN CN202210125578.4A patent/CN114380825B/zh active Active
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CN108349969A (zh) * | 2015-07-16 | 2018-07-31 | 阵列生物制药公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡啶化合物 |
US20180133207A1 (en) * | 2016-10-10 | 2018-05-17 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
TW201825488A (zh) * | 2016-10-10 | 2018-07-16 | 美商亞雷生物製藥股份有限公司 | 作為pet激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
WO2018136661A1 (en) * | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
WO2019075108A1 (en) * | 2017-10-10 | 2019-04-18 | Metcalf Andrew T | CRYSTALLINE FORMS |
WO2019075114A1 (en) * | 2017-10-10 | 2019-04-18 | Mark Reynolds | FORMULATIONS COMPRISING 6- (2-HYDROXY-2-METHYLPROPOXY) -4- (6- (6 - ((6-METHOXYPYRIDIN-3-YL) METHYL) -3,6-DIAZABICYCLO [3.1.1] HEPTAN-3- YL) PYRIDIN-3-YL) PYRAZOLO [1,5-A] pYRIDINE-3-carbonitrile |
Non-Patent Citations (1)
Title |
---|
《STN REGISTER》: "RN 2222758-45-2,RN 2222758-41-8, RN 2222758-39-4,RN 2222758-12-3,RN 2222758-09-8,RN 2222758-07-6,RN 2222758-02-1", 《STN REGISTER》 * |
Also Published As
Publication number | Publication date |
---|---|
KR20210070286A (ko) | 2021-06-14 |
CN112771043B (zh) | 2023-04-28 |
US20210379056A1 (en) | 2021-12-09 |
EP3845531A1 (en) | 2021-07-07 |
CN114380825A (zh) | 2022-04-22 |
CN114380825B (zh) | 2024-02-13 |
CN110964008B (zh) | 2021-12-21 |
JP2022508533A (ja) | 2022-01-19 |
WO2020064009A1 (zh) | 2020-04-02 |
CN110964008A (zh) | 2020-04-07 |
EP3845531A4 (en) | 2021-11-24 |
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