CN105189508B - 作为janus激酶抑制剂的环烷基腈吡唑并吡啶酮 - Google Patents

作为janus激酶抑制剂的环烷基腈吡唑并吡啶酮 Download PDF

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Publication number
CN105189508B
CN105189508B CN201480016840.5A CN201480016840A CN105189508B CN 105189508 B CN105189508 B CN 105189508B CN 201480016840 A CN201480016840 A CN 201480016840A CN 105189508 B CN105189508 B CN 105189508B
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China
Prior art keywords
dihydro
amino
oxo
pyrazolo
pyridin
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Expired - Fee Related
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CN201480016840.5A
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Chinese (zh)
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CN105189508A (zh
Inventor
M.L.蔡尔德斯
C.丁斯摩尔
P.富勒
D.盖林
J.D.卡茨
Q.朴
M.E.斯科特
C.F.汤普森
H.张
D.法尔孔
L.托雷斯
J.布鲁贝克
H.曾
J.蔡
X.杜
C.王
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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Priority to CN201480016840.5A priority Critical patent/CN105189508B/zh
Publication of CN105189508A publication Critical patent/CN105189508A/zh
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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
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P11/14—Antitussive agents
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (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)
  • Pyridine Compounds (AREA)
CN201480016840.5A 2013-03-19 2014-03-19 作为janus激酶抑制剂的环烷基腈吡唑并吡啶酮 Expired - Fee Related CN105189508B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201480016840.5A CN105189508B (zh) 2013-03-19 2014-03-19 作为janus激酶抑制剂的环烷基腈吡唑并吡啶酮

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CNPCT/CN2013/072867 2013-03-19
PCT/CN2013/072867 WO2014146246A1 (en) 2013-03-19 2013-03-19 Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors
CN201480016840.5A CN105189508B (zh) 2013-03-19 2014-03-19 作为janus激酶抑制剂的环烷基腈吡唑并吡啶酮
PCT/CN2014/000296 WO2014146490A1 (en) 2013-03-19 2014-03-19 Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors

Publications (2)

Publication Number Publication Date
CN105189508A CN105189508A (zh) 2015-12-23
CN105189508B true CN105189508B (zh) 2018-11-23

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CN201480016840.5A Expired - Fee Related CN105189508B (zh) 2013-03-19 2014-03-19 作为janus激酶抑制剂的环烷基腈吡唑并吡啶酮

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US (1) US9725445B2 (enExample)
EP (1) EP2976340B1 (enExample)
JP (1) JP6412102B2 (enExample)
CN (1) CN105189508B (enExample)
AU (1) AU2014234906B2 (enExample)
BR (1) BR112015023891A2 (enExample)
CA (1) CA2901763A1 (enExample)
ES (1) ES2683309T3 (enExample)
MX (1) MX2015013418A (enExample)
RU (1) RU2655380C2 (enExample)
TR (1) TR201811198T4 (enExample)
WO (2) WO2014146246A1 (enExample)

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CA2874987A1 (en) * 2012-06-01 2013-12-05 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP2976338B1 (en) * 2013-03-19 2018-01-03 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors
AU2017233739A1 (en) 2016-03-15 2018-09-20 Bayer Cropscience Aktiengesellschaft Substituted sulfonyl amides for controlling animal pests
CN105859644A (zh) * 2016-04-15 2016-08-17 华东理工大学 烯烃制备新型有机oled试剂的设计及其应用
CN106366089B (zh) * 2016-08-19 2019-06-11 爱斯特（成都）生物制药股份有限公司 二氢异吲哚衍生物及其类似物的制备方法
TW201822637A (zh) 2016-11-07 2018-07-01 德商拜耳廠股份有限公司 用於控制動物害蟲的經取代磺醯胺類
AU2017376398B2 (en) 2016-12-14 2021-07-15 Intervet International B.V. Aminopyrazoles as selective janus kinase inhibitors
DK3915989T3 (da) * 2019-01-30 2023-09-18 Felicamed Biotechnology Co Ltd Jak inhibitor and preparation method therefor
EP4055010A1 (de) 2019-11-07 2022-09-14 Bayer Aktiengesellschaft Substituierte sulfonylamide zur bekämpfung tierischer schädlinge
CN110938028B (zh) * 2019-12-09 2022-03-04 南京杰运医药科技有限公司 一种(1r)-5-溴-2,3-二氢-1-甲基-1h-异吲哚的制备方法
CN113372364B (zh) * 2020-03-10 2024-05-31 明慧医药（上海）有限公司 一类jak激酶抑制剂及其制备和应用
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
WO2023118555A1 (en) 2021-12-24 2023-06-29 Intervet International B.V. Use of aminopyrazole compounds
TW202345806A (zh) 2022-03-31 2023-12-01 美商艾伯維有限公司 噻唑并〔５，４－ｂ〕吡啶ｍａｌｔ－１抑制劑
CN116715656B (zh) * 2022-07-26 2025-05-02 北京先通国际医药科技股份有限公司 心肌灌注显像剂前体的制备方法及其用途
CN117603101B (zh) * 2023-11-03 2026-02-03 荆楚理工学院 一种路易斯酸促进的n-酰基仲磺酰胺非水解脱酰基方法
CN118561689B (zh) * 2024-08-05 2024-11-22 中节能万润股份有限公司 一种3-氧代环丁羧酸酯类化合物的制备方法

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WO2012127506A1 (en) * 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
WO2013180265A1 (ja) * 2012-06-01 2013-12-05 武田薬品工業株式会社 複素環化合物

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US20100105661A1 (en) 2007-01-12 2010-04-29 Astellas Pharma Inc. Condensed pyridine compound
EP2200612B1 (en) * 2007-09-11 2012-08-08 Schering Corporation Inhibitors of janus kinases
CA2792508C (en) * 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
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WO2013017479A1 (en) * 2011-07-29 2013-02-07 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
MX2015013419A (es) * 2013-03-19 2016-07-19 Merck Sharp & Dohme Cianoetilpirazolo piridonas aciclicas como inhibidores de janus quinasa.
WO2014146249A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
EP2976338B1 (en) * 2013-03-19 2018-01-03 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors

Patent Citations (3)

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CN102574857A (zh) * 2009-07-08 2012-07-11 利奥制药有限公司 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物
WO2012127506A1 (en) * 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
WO2013180265A1 (ja) * 2012-06-01 2013-12-05 武田薬品工業株式会社 複素環化合物

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ES2683309T3 (es) 2018-09-26
AU2014234906A1 (en) 2015-08-13
CA2901763A1 (en) 2014-09-25
TR201811198T4 (tr) 2018-08-27
JP2016518344A (ja) 2016-06-23
MX2015013418A (es) 2016-06-24
US9725445B2 (en) 2017-08-08
EP2976340B1 (en) 2018-06-13
EP2976340A4 (en) 2016-08-31
BR112015023891A2 (pt) 2017-07-18
EP2976340A1 (en) 2016-01-27
WO2014146490A1 (en) 2014-09-25
RU2655380C2 (ru) 2018-05-28
US20160280704A1 (en) 2016-09-29
AU2014234906B2 (en) 2017-11-16
JP6412102B2 (ja) 2018-10-24
RU2015144386A (ru) 2017-04-27
WO2014146246A1 (en) 2014-09-25
CN105189508A (zh) 2015-12-23

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