CN103781780B - 作为jak抑制剂的杂环基嘧啶类似物 - Google Patents

作为jak抑制剂的杂环基嘧啶类似物 Download PDF

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Publication number
CN103781780B
CN103781780B CN201280043720.5A CN201280043720A CN103781780B CN 103781780 B CN103781780 B CN 103781780B CN 201280043720 A CN201280043720 A CN 201280043720A CN 103781780 B CN103781780 B CN 103781780B
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amino
base
pyrimidine
chloro
pyrazoles
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CN103781780A (zh
Inventor
J.弗里曼
V.里德
G.阿迪森
N.拉姆斯登
J.E.斯坎隆
R.J.哈里森
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Cellzome Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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]
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201280043720.5A 2011-07-28 2012-07-24 作为jak抑制剂的杂环基嘧啶类似物 Expired - Fee Related CN103781780B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP11175807.4 2011-07-28
EP11175807 2011-07-28
US201261635921P 2012-04-20 2012-04-20
US61/635,921 2012-04-20
PCT/EP2012/064515 WO2013014162A1 (en) 2011-07-28 2012-07-24 Heterocyclyl pyrimidine analogues as jak inhibitors

Publications (2)

Publication Number Publication Date
CN103781780A CN103781780A (zh) 2014-05-07
CN103781780B true CN103781780B (zh) 2015-11-25

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Country Link
US (1) US20140179664A1 (enExample)
EP (1) EP2736901A1 (enExample)
JP (1) JP2014521623A (enExample)
KR (1) KR20140047092A (enExample)
CN (1) CN103781780B (enExample)
AU (1) AU2012288892B2 (enExample)
BR (1) BR112014000360A2 (enExample)
CA (1) CA2843195A1 (enExample)
WO (1) WO2013014162A1 (enExample)

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WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
WO2017156493A1 (en) 2016-03-11 2017-09-14 Denali Therapeutics Inc. Compounds, compositions, and methods
JP6491202B2 (ja) 2013-10-18 2019-03-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
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US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
HK1245260A1 (zh) 2014-12-23 2018-08-24 Dana-Farber Cancer Institute, Inc. 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂
JP6861166B2 (ja) 2015-03-27 2021-04-21 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼの阻害剤
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
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CN113214230B (zh) * 2017-09-21 2022-10-04 北京赛特明强医药科技有限公司 2-取代吡唑氨基-4-取代氨基-5-嘧啶甲酰胺类化合物、组合物及其应用
JP7117029B2 (ja) * 2017-09-21 2022-08-12 北京賽特明強医薬科技有限公司 ２－置換ピラゾールアミノ－４－置換アミノ－５－ピリミジンホルムアミド系化合物、組成物およびその使用
EP3810132A4 (en) 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
CN110734427B (zh) * 2018-07-20 2021-01-15 北京赛特明强医药科技有限公司 含烯基的嘧啶甲酰胺类化合物、组合物及其应用
CN110845476B (zh) * 2018-08-21 2022-11-18 上海和誉生物医药科技有限公司 一种高选择性csf1r抑制剂、其制备方法和在药学上的应用
EP3876939A4 (en) 2018-11-07 2022-08-10 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
WO2020118683A1 (en) * 2018-12-14 2020-06-18 Lynk Pharmaceuticals Co. Ltd. Benzamides of pyrazolyl-amino-pyrimidinyl derivatives, and compositions and methods thereof
CA3124422A1 (en) 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
IL287795B2 (en) 2019-05-10 2025-05-01 Deciphera Pharmaceuticals Llc Heteroarylaminopyrimidine amides as autophagy inhibitors and methods of using them
CN118878519A (zh) 2019-05-10 2024-11-01 德西费拉制药有限责任公司 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法
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WO2013014162A1 (en) 2013-01-31
CA2843195A1 (en) 2013-01-31
BR112014000360A2 (pt) 2017-02-14
KR20140047092A (ko) 2014-04-21
JP2014521623A (ja) 2014-08-28
CN103781780A (zh) 2014-05-07
AU2012288892A1 (en) 2014-02-20
EP2736901A1 (en) 2014-06-04
AU2012288892B2 (en) 2016-04-21
US20140179664A1 (en) 2014-06-26

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