CN105189497B - 作为janus激酶抑制剂的n-(2-氰基杂环基)吡唑并吡啶酮 - Google Patents

作为janus激酶抑制剂的n-(2-氰基杂环基)吡唑并吡啶酮 Download PDF

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Publication number
CN105189497B
CN105189497B CN201480016754.4A CN201480016754A CN105189497B CN 105189497 B CN105189497 B CN 105189497B CN 201480016754 A CN201480016754 A CN 201480016754A CN 105189497 B CN105189497 B CN 105189497B
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CN
China
Prior art keywords
alkyl
base
amino
dihydro
pyrazolo
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Expired - Fee Related
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CN201480016754.4A
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English (en)
Chinese (zh)
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CN105189497A (zh
Inventor
C.丁斯摩尔
P.富勒
D.盖林
C.F.汤普森
Q.朴
M.E.斯科特
J.D.卡茨
R.库鲁库拉苏里亚
J.T.克罗斯
D.法尔孔
J.布鲁贝克
H.曾
Y.白
J.傅
N.孔
Y.刘
Z.郑
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Merck Sharp and Dohme LLC
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Schering Corp
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Publication of CN105189497A publication Critical patent/CN105189497A/zh
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Publication of CN105189497B publication Critical patent/CN105189497B/zh
Expired - Fee Related legal-status Critical Current
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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201480016754.4A 2013-03-19 2014-03-19 作为janus激酶抑制剂的n-(2-氰基杂环基)吡唑并吡啶酮 Expired - Fee Related CN105189497B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361803226P 2013-03-19 2013-03-19
US61/803226 2013-03-19
PCT/CN2014/000298 WO2014146492A1 (en) 2013-03-19 2014-03-19 N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors

Publications (2)

Publication Number Publication Date
CN105189497A CN105189497A (zh) 2015-12-23
CN105189497B true CN105189497B (zh) 2019-05-03

Family

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Family Applications (1)

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CN201480016754.4A Expired - Fee Related CN105189497B (zh) 2013-03-19 2014-03-19 作为janus激酶抑制剂的n-(2-氰基杂环基)吡唑并吡啶酮

Country Status (11)

Country Link
US (1) US9957265B2 (enExample)
EP (1) EP2976338B1 (enExample)
JP (1) JP6322275B2 (enExample)
KR (1) KR20150130311A (enExample)
CN (1) CN105189497B (enExample)
AU (1) AU2014234908B2 (enExample)
BR (1) BR112015023878A2 (enExample)
CA (1) CA2901766A1 (enExample)
MX (1) MX2015013414A (enExample)
RU (1) RU2669922C2 (enExample)
WO (1) WO2014146492A1 (enExample)

Families Citing this family (7)

* 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
WO2018111663A1 (en) * 2016-12-14 2018-06-21 Merck Sharp & Dohme Corp. Aminopyrazoles as janus kinase inhibitors
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN111499592B (zh) * 2020-03-14 2023-06-23 江苏省农用激素工程技术研究中心有限公司 5-氨甲基糖精的合成方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1656079A (zh) * 2002-05-31 2005-08-17 卫材株式会社 吡唑化合物和含有该化合物的药物组合物

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2759227B2 (ja) 1990-09-28 1998-05-28 大鵬薬品工業株式会社 ピラゾロピリジン誘導体
CN1636005A (zh) 1999-06-03 2005-07-06 克诺尔股份有限公司 苯并噻嗪酮和苯并噁嗪酮化合物
AU2003217863B9 (en) 2002-02-28 2009-10-29 Biota Scientific Management Pty Ltd Nucleotide mimics and their prodrugs
JP4139185B2 (ja) 2002-10-17 2008-08-27 京セラ株式会社 配線基板の製造方法
NZ601687A (en) * 2006-01-17 2014-03-28 Vertex Pharma Azaindoles useful as inhibitors of janus kinases
JP5287253B2 (ja) 2007-01-12 2013-09-11 アステラス製薬株式会社 縮合ピリジン化合物
US9346809B2 (en) 2009-07-08 2016-05-24 Leo Pharma A/S Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors
PH12015502575A1 (en) 2010-03-10 2017-04-24 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
WO2012127506A1 (en) 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
ES2633793T3 (es) * 2011-09-22 2017-09-25 Merck Sharp & Dohme Corp. Pirazol carboxamidas como inhibidores de quinasa Janus
EP2857400A4 (en) 2012-06-01 2015-12-09 Takeda Pharmaceutical HETEROCYCLIC CONNECTION
WO2014146246A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1656079A (zh) * 2002-05-31 2005-08-17 卫材株式会社 吡唑化合物和含有该化合物的药物组合物

Also Published As

Publication number Publication date
US9957265B2 (en) 2018-05-01
JP2016514710A (ja) 2016-05-23
EP2976338A4 (en) 2016-08-31
AU2014234908A1 (en) 2015-08-13
RU2015144483A (ru) 2017-04-25
RU2669922C2 (ru) 2018-10-17
US20160272633A1 (en) 2016-09-22
BR112015023878A2 (pt) 2017-07-18
CN105189497A (zh) 2015-12-23
EP2976338A1 (en) 2016-01-27
WO2014146492A1 (en) 2014-09-25
CA2901766A1 (en) 2014-09-25
KR20150130311A (ko) 2015-11-23
EP2976338B1 (en) 2018-01-03
AU2014234908B2 (en) 2017-08-17
MX2015013414A (es) 2016-02-26
JP6322275B2 (ja) 2018-05-09

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Granted publication date: 20190503

Termination date: 20200319