CN113924301A - 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途 - Google Patents

一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途 Download PDF

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Publication number
CN113924301A
CN113924301A CN202080027882.4A CN202080027882A CN113924301A CN 113924301 A CN113924301 A CN 113924301A CN 202080027882 A CN202080027882 A CN 202080027882A CN 113924301 A CN113924301 A CN 113924301A
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radical
amino
group
hydroxy
mercapto
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CN202080027882.4A
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English (en)
Inventor
戴丽光
祝力
张慧
吴伟
杨艳青
胡伟
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Beijing Puqi Medicine Technology Co ltd
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Beijing Puqi Medicine Technology Co ltd
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Publication of CN113924301A publication Critical patent/CN113924301A/zh
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    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

一种如通式(AI)和(Ⅰ)所示的吡唑并吡嗪衍生的化合物或其药学上可接受的盐、溶剂化物、活性代谢物、多晶型物、同位素标记物或异构体，提供了包含其的药物组合物以及所述化合物、药物组合物在制备用于治疗JAK激酶介导的疾病的药物中的用途。提供的化合物及其药物组合物具有显著的JAK激酶抑制活性，尤其是具备较高的Tyk2酶抑制活性和对JAK2的选择性，因而非常具备应用潜力。

Description

PCT国内申请，说明书已公开。

Claims (17)

  1. PCT国内申请，权利要求书已公开。
CN202080027882.4A 2019-04-12 2020-04-10 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途 Pending CN113924301A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910294408 2019-04-12
CN2019102944087 2019-04-12
PCT/CN2020/084243 WO2020207476A1 (zh) 2019-04-12 2020-04-10 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途

Publications (1)

Publication Number Publication Date
CN113924301A true CN113924301A (zh) 2022-01-11

Family

ID=72750940

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080027882.4A Pending CN113924301A (zh) 2019-04-12 2020-04-10 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途

Country Status (10)

Country Link
US (1) US20220204513A1 (zh)
EP (1) EP3954689B1 (zh)
JP (1) JP7256291B2 (zh)
KR (1) KR20210149151A (zh)
CN (1) CN113924301A (zh)
AU (1) AU2020256720B2 (zh)
BR (1) BR112021020339A2 (zh)
CA (1) CA3136468A1 (zh)
MX (1) MX2021012487A (zh)
WO (1) WO2020207476A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112592345A (zh) * 2020-12-07 2021-04-02 嘉兴特科罗生物科技有限公司 一种三氮唑并吡嗪类化合物及其用途
WO2023076161A1 (en) 2021-10-25 2023-05-04 Kymera Therapeutics, Inc. Tyk2 degraders and uses thereof
CA3237632A1 (en) * 2021-11-12 2023-05-19 Changqing WEI Pyrazolo fused ring compound and use thereof

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080312258A1 (en) * 2007-06-13 2008-12-18 Incyte Corporation METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE
WO2011101161A1 (en) * 2010-02-18 2011-08-25 Almirall, S.A. Pyrazole derivatives as jak inhibitors
WO2011130146A1 (en) * 2010-04-14 2011-10-20 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
WO2013055645A1 (en) * 2011-10-12 2013-04-18 Array Biopharma Inc. 5,7-substituted-imidazo[1,2-c]pyrimidines
WO2016090285A1 (en) * 2014-12-05 2016-06-09 Array Biopharma Inc. 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS
CN109071546A (zh) * 2016-02-24 2018-12-21 辉瑞大药厂 作为jak抑制剂的吡唑并[1,5-a]吡嗪-4-基衍生物

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11254668B2 (en) 2017-08-14 2022-02-22 Pfizer Inc. Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080312258A1 (en) * 2007-06-13 2008-12-18 Incyte Corporation METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE
WO2011101161A1 (en) * 2010-02-18 2011-08-25 Almirall, S.A. Pyrazole derivatives as jak inhibitors
WO2011130146A1 (en) * 2010-04-14 2011-10-20 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
WO2013055645A1 (en) * 2011-10-12 2013-04-18 Array Biopharma Inc. 5,7-substituted-imidazo[1,2-c]pyrimidines
WO2016090285A1 (en) * 2014-12-05 2016-06-09 Array Biopharma Inc. 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS
CN109071546A (zh) * 2016-02-24 2018-12-21 辉瑞大药厂 作为jak抑制剂的吡唑并[1,5-a]吡嗪-4-基衍生物

Also Published As

Publication number Publication date
CA3136468A1 (en) 2020-10-15
AU2020256720B2 (en) 2022-09-01
WO2020207476A1 (zh) 2020-10-15
BR112021020339A2 (pt) 2021-12-07
AU2020256720A1 (en) 2022-02-17
EP3954689A1 (en) 2022-02-16
EP3954689A4 (en) 2023-01-04
KR20210149151A (ko) 2021-12-08
EP3954689B1 (en) 2024-04-24
JP7256291B2 (ja) 2023-04-11
MX2021012487A (es) 2021-11-12
JP2022526599A (ja) 2022-05-25
US20220204513A1 (en) 2022-06-30

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