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
thiazolinyl
alkynyl
optionally
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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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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (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)

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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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WO2014022569A1 (en) * 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
HK1211942A1 (en) 2012-09-10 2016-06-03 Principia Biopharma Inc. Pyrazolopyrimidine compounds as kinase inhibitors
KR20160036053A (ko) * 2013-07-31 2016-04-01 메르크 파텐트 게엠베하 Btk 저해제로서 피리딘, 피리미딘, 및 피라진, 및 이들의 용도
WO2015038417A1 (en) * 2013-09-10 2015-03-19 Asana Biosciences, Llc Compounds for regulating fak and/or src pathways
MX372673B (es) 2014-02-21 2020-03-25 Principia Biopharma Inc Un inhibidor de btk para usarse en el tratamiento de penfigo y sales y formas sólidas del mismo.
PT3233103T (pt) 2014-12-18 2021-01-18 Principia Biopharma Inc Tratamento de pênfigo
MA42242A (fr) 2015-06-24 2018-05-02 Principia Biopharma Inc Inhibiteurs de la tyrosine kinase
EA201892836A1 (ru) 2016-06-29 2019-07-31 Принсипиа Биофарма Инк. Составы 2-[3-[4-амино-3-(2-фтор-4-феноксифенил)пиразол[3,4-d]пиримидин-1-ил]пиперидин-1-карбонил]-4-метил-4-[4-(оксетан-3-ил)пиперазин-1-ил]пент-2-еннитрила с модифицированным высвобождением
EP3484876A1 (en) 2016-07-14 2019-05-22 Pfizer Inc Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
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
MX2022004427A (es) 2019-10-14 2022-07-12 Principia Biopharma Inc Metodos para el tratamiento de la trombocitopenia inmunitaria mediante la administracion de (r)-2-[3-[4-amino-3-(2-fluoro-4-feno xi-fenil)pirazolo[3,4-d]pirimidin-1-il]piperidino-1-carbonil]-4-m etil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enonitrilo.
US11697648B2 (en) 2019-11-26 2023-07-11 Theravance Biopharma R&D Ip, Llc Fused pyrimidine pyridinone compounds as JAK inhibitors
MX2022009009A (es) 2020-01-22 2022-08-15 Principia Biopharma Inc Formas cristalinas de 2-[3-[4-amino-3-(2-fluoro-4-fenoxi-fenil)-1h -pirazolo[3,4-d]pirimidin-1-il]piperidin-1-carbonil]-4-metil-4-[4 -(oxetan-3-il)piperazin-1-il]pent-2-enonitrilo.
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors

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Cited By (10)

* 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

Also Published As

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

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Application publication date: 20140618