CN105189498B - 作为janus激酶抑制剂的孪位取代的氰基乙基吡唑并吡啶酮 - Google Patents

作为janus激酶抑制剂的孪位取代的氰基乙基吡唑并吡啶酮 Download PDF

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CN105189498B
CN105189498B CN201480016905.6A CN201480016905A CN105189498B CN 105189498 B CN105189498 B CN 105189498B CN 201480016905 A CN201480016905 A CN 201480016905A CN 105189498 B CN105189498 B CN 105189498B
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amino
pyrazolo
oxo
pyridine
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Chinese (zh)
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CN105189498A (zh
Inventor
M.L.蔡尔德斯
P.富勒
D.盖林
J.D.卡茨
Q.朴
M.E.斯科特
C.F.汤普森
M.马丁内斯
D.法尔孔
L.托雷斯
Y.邓
R.库鲁库拉苏里亚
H.曾
Y.白
N.孔
Y.刘
Z.郑
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Merck Sharp & Dohme LLC
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Merck Sharp & Dohme LLC
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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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Transplantation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201480016905.6A 2013-03-19 2014-03-19 作为janus激酶抑制剂的孪位取代的氰基乙基吡唑并吡啶酮 Expired - Fee Related CN105189498B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201480016905.6A CN105189498B (zh) 2013-03-19 2014-03-19 作为janus激酶抑制剂的孪位取代的氰基乙基吡唑并吡啶酮

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
PCT/CN2013/072873 WO2014146249A1 (en) 2013-03-19 2013-03-19 Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
CNPCT/CN2013/072873 2013-03-19
CN201480016905.6A CN105189498B (zh) 2013-03-19 2014-03-19 作为janus激酶抑制剂的孪位取代的氰基乙基吡唑并吡啶酮
PCT/CN2014/000297 WO2014146491A1 (en) 2013-03-19 2014-03-19 Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors

Publications (2)

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CN105189498A CN105189498A (zh) 2015-12-23
CN105189498B true CN105189498B (zh) 2017-06-27

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CN201480016905.6A Expired - Fee Related CN105189498B (zh) 2013-03-19 2014-03-19 作为janus激酶抑制剂的孪位取代的氰基乙基吡唑并吡啶酮

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US (1) US9957264B2 (enExample)
EP (1) EP2976339B1 (enExample)
JP (1) JP2016514709A (enExample)
CN (1) CN105189498B (enExample)
AU (1) AU2014234907B2 (enExample)
BR (1) BR112015023858A2 (enExample)
CA (1) CA2901765A1 (enExample)
RU (1) RU2664533C2 (enExample)
WO (2) WO2014146249A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014146246A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors
WO2016061751A1 (en) * 2014-10-22 2016-04-28 Merck Sharp & Dohme Corp. Ethyl n-boc piperidinyl pyrazolo pyridones as janus kinase inhibitors
CN110291090A (zh) * 2017-01-20 2019-09-27 利奥制药有限公司 作为新型jak激酶抑制剂的双环胺
DK3915989T3 (da) 2019-01-30 2023-09-18 Felicamed Biotechnology Co Ltd Jak inhibitor and preparation method therefor
EP3982954A4 (en) * 2019-06-14 2024-01-03 The Trustees of Columbia University in the City of New York NT5C2 INHIBITORS FOR THE TREATMENT OF CHEMOTHERAPY-RESISTANT ACUTE LYMPHOBLASTIC LEUKEMIA
CN116322696A (zh) 2020-05-04 2023-06-23 安进公司 作为髓样细胞上表达的触发受体2激动剂的杂环化合物和使用方法
TW202208355A (zh) 2020-05-04 2022-03-01 美商安進公司 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法
JP7023026B1 (ja) 2021-05-18 2022-02-21 株式会社アイビー化粧品 Ｊａｋ阻害剤

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WO2012030924A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Azolopyridine and azolopyrimidine compounds and methods of use thereof

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RU2340611C2 (ru) * 2000-09-15 2008-12-10 Вертекс Фармасьютикалз Инкорпорейтед Производные пиразола, используемые в качестве ингибиторов протеинкиназы
US20100105661A1 (en) 2007-01-12 2010-04-29 Astellas Pharma Inc. Condensed pyridine compound
EA020777B1 (ru) * 2007-11-16 2015-01-30 Инсайт Корпорейшн 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus
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Also Published As

Publication number Publication date
WO2014146249A1 (en) 2014-09-25
US20160272632A1 (en) 2016-09-22
AU2014234907B2 (en) 2017-08-17
CN105189498A (zh) 2015-12-23
WO2014146491A1 (en) 2014-09-25
CA2901765A1 (en) 2014-09-25
BR112015023858A2 (pt) 2017-07-18
RU2015144485A (ru) 2017-04-25
EP2976339B1 (en) 2018-06-27
EP2976339A4 (en) 2016-08-31
AU2014234907A1 (en) 2015-08-13
EP2976339A1 (en) 2016-01-27
JP2016514709A (ja) 2016-05-23
RU2664533C2 (ru) 2018-08-20
US9957264B2 (en) 2018-05-01

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