CN103874699A - 吡唑并[4,3-c]吡啶衍生物作为激酶抑制剂 - Google Patents

吡唑并[4,3-c]吡啶衍生物作为激酶抑制剂 Download PDF

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Publication number
CN103874699A
CN103874699A CN201280049382.6A CN201280049382A CN103874699A CN 103874699 A CN103874699 A CN 103874699A CN 201280049382 A CN201280049382 A CN 201280049382A CN 103874699 A CN103874699 A CN 103874699A
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alkyl
compound
alkynyl
thiazolinyl
optionally
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CN201280049382.6A
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Chinese (zh)
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N.拉姆斯登
C.达戈斯廷
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Cellzome Ltd
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Cellzome Ltd
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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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201280049382.6A 2011-09-20 2012-09-20 吡唑并[4,3-c]吡啶衍生物作为激酶抑制剂 Pending CN103874699A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11182020 2011-09-20
EP11182020.5 2011-09-20
PCT/EP2012/068504 WO2013041605A1 (en) 2011-09-20 2012-09-20 Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors

Publications (1)

Publication Number Publication Date
CN103874699A true CN103874699A (zh) 2014-06-18

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CN201280049382.6A Pending CN103874699A (zh) 2011-09-20 2012-09-20 吡唑并[4,3-c]吡啶衍生物作为激酶抑制剂

Country Status (9)

Country Link
US (1) US20140323504A1 (enExample)
EP (1) EP2760863A1 (enExample)
JP (1) JP2014531449A (enExample)
KR (1) KR20140063700A (enExample)
CN (1) CN103874699A (enExample)
AU (1) AU2012311504B2 (enExample)
CA (1) CA2849340A1 (enExample)
RU (1) RU2014115476A (enExample)
WO (1) WO2013041605A1 (enExample)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106831779A (zh) * 2015-11-28 2017-06-13 南昌弘益药业有限公司 一类jak激酶抑制剂的新化合物
CN110885331A (zh) * 2018-09-11 2020-03-17 中国药科大学 一种新颖的6-氨基-1H-吡唑并[3，4-d]嘧啶类JAK激酶抑制剂的制备与应用
WO2021147953A1 (zh) * 2020-01-21 2021-07-29 江苏先声药业有限公司 嘧啶并五元环类衍生物及其应用
CN113924305A (zh) * 2019-05-27 2022-01-11 迪哲(江苏)医药股份有限公司 Dna依赖性蛋白激酶抑制剂
CN114269734A (zh) * 2019-05-08 2022-04-01 维玛兰生物科学公司 Jak抑制剂
WO2022237844A1 (zh) * 2021-05-12 2022-11-17 微境生物医药科技(上海)有限公司 含吡嗪结构的吡咯并嘧啶衍生物

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MD20140023A2 (ro) * 2011-09-22 2014-06-30 Pfizer Inc. Derivaţi de pirolpirimidină şi purină
US9572811B2 (en) 2012-08-03 2017-02-21 Principia Biopharma Inc. Treatment of dry eye
AU2013312296B2 (en) 2012-09-10 2017-06-22 Principia Biopharma Inc. Pyrazolopyrimidine compounds as kinase inhibitors
PT3049417T (pt) * 2013-07-31 2019-01-24 Merck Patent Gmbh Piridinas, pirimidinas e pirazinas, como inibidores de btk e utilizações das mesmas
WO2015038417A1 (en) * 2013-09-10 2015-03-19 Asana Biosciences, Llc Compounds for regulating fak and/or src pathways
KR20160117614A (ko) 2014-02-21 2016-10-10 프린시피아 바이오파마, 인코퍼레이티드 Btk 억제제의 염 및 고체 형태
EA036269B1 (ru) 2014-12-18 2020-10-21 Принсипиа Биофарма Инк. Лечение пузырчатки
WO2016210165A1 (en) 2015-06-24 2016-12-29 Principia Biopharma Inc. Tyrosine kinase inhibitors
EP3478273A1 (en) 2016-06-29 2019-05-08 Principia Biopharma Inc. Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
BR112019000589A2 (pt) 2016-07-14 2019-04-24 Pfizer Inc. pirimidina carboxamidas como inibidores da enzima vanina-1
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
EP4045051A1 (en) 2019-10-14 2022-08-24 Principia Biopharma Inc. Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
US11697648B2 (en) 2019-11-26 2023-07-11 Theravance Biopharma R&D Ip, Llc Fused pyrimidine pyridinone compounds as JAK inhibitors
PH12022551787A1 (en) 2020-01-22 2024-02-12 Principia Biopharma Inc Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors

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Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106831779A (zh) * 2015-11-28 2017-06-13 南昌弘益药业有限公司 一类jak激酶抑制剂的新化合物
CN106831779B (zh) * 2015-11-28 2019-07-19 南昌弘益药业有限公司 一类jak激酶抑制剂的新化合物
CN110885331A (zh) * 2018-09-11 2020-03-17 中国药科大学 一种新颖的6-氨基-1H-吡唑并[3，4-d]嘧啶类JAK激酶抑制剂的制备与应用
WO2020052489A1 (zh) * 2018-09-11 2020-03-19 中国药科大学 一种6-氨基-1h-吡唑并[3,4-d]嘧啶类jak激酶抑制剂的制备与应用
CN110885331B (zh) * 2018-09-11 2021-07-09 中国药科大学 一种6-氨基-1H-吡唑并[3，4-d]嘧啶类JAK激酶抑制剂的制备与应用
CN114269734A (zh) * 2019-05-08 2022-04-01 维玛兰生物科学公司 Jak抑制剂
CN113924305A (zh) * 2019-05-27 2022-01-11 迪哲(江苏)医药股份有限公司 Dna依赖性蛋白激酶抑制剂
WO2021147953A1 (zh) * 2020-01-21 2021-07-29 江苏先声药业有限公司 嘧啶并五元环类衍生物及其应用
WO2022237844A1 (zh) * 2021-05-12 2022-11-17 微境生物医药科技(上海)有限公司 含吡嗪结构的吡咯并嘧啶衍生物
CN117412971A (zh) * 2021-05-12 2024-01-16 微境生物医药科技(上海)有限公司 含吡嗪结构的吡咯并嘧啶衍生物
CN117412971B (zh) * 2021-05-12 2026-02-24 微境生物医药科技(上海)有限公司 含吡嗪结构的吡咯并嘧啶衍生物

Also Published As

Publication number Publication date
RU2014115476A (ru) 2015-10-27
CA2849340A1 (en) 2013-03-28
AU2012311504B2 (en) 2016-03-24
KR20140063700A (ko) 2014-05-27
US20140323504A1 (en) 2014-10-30
EP2760863A1 (en) 2014-08-06
WO2013041605A1 (en) 2013-03-28
AU2012311504A1 (en) 2014-04-10
JP2014531449A (ja) 2014-11-27

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Application publication date: 20140618