JP6412102B2 - ヤヌスキナーゼ阻害剤としてのシクロアルキルニトリルピラゾロピリドン - Google Patents

ヤヌスキナーゼ阻害剤としてのシクロアルキルニトリルピラゾロピリドン Download PDF

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Publication number
JP6412102B2
JP6412102B2 JP2016503520A JP2016503520A JP6412102B2 JP 6412102 B2 JP6412102 B2 JP 6412102B2 JP 2016503520 A JP2016503520 A JP 2016503520A JP 2016503520 A JP2016503520 A JP 2016503520A JP 6412102 B2 JP6412102 B2 JP 6412102B2
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Prior art keywords
alkyl
dihydro
amino
oxo
pyrazolo
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Expired - Fee Related
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JP2016503520A
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Japanese (ja)
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JP2016518344A5 (enExample
JP2016518344A (ja
Inventor
チルダーズ，マシユー・ロイド
デインスモア，クリストフアー
フラー，ピーター
ゲリン，デイビッド
カツツ，ジエイソン・デイビッド
プウ，チーンリン
スコット，マーク・イー
トンプソン，クリストフアー・エフ
ジヤーン，ホーンジユイン
フアルコン，ダニエル
トーレス，ルイス
ブルベイカー，ジエイソン
ズオン，ホーンボー
ツアイ，ジアチアーン
ドウ，シヤオシーン
ワン，チョーンガーン
バイ，ユインフオン
コーン，ノーマン
リウ，ユイメイ
ジユヨン，ジーシアーン
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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    • 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
    • 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
    • A61K31/41—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)
  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (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)
JP2016503520A 2013-03-19 2014-03-19 ヤヌスキナーゼ阻害剤としてのシクロアルキルニトリルピラゾロピリドン Expired - Fee Related JP6412102B2 (ja)

Applications Claiming Priority (3)

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
PCT/CN2014/000296 WO2014146490A1 (en) 2013-03-19 2014-03-19 Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors

Publications (3)

Publication Number Publication Date
JP2016518344A JP2016518344A (ja) 2016-06-23
JP2016518344A5 JP2016518344A5 (enExample) 2017-04-06
JP6412102B2 true JP6412102B2 (ja) 2018-10-24

Family

ID=51579269

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016503520A Expired - Fee Related JP6412102B2 (ja) 2013-03-19 2014-03-19 ヤヌスキナーゼ阻害剤としてのシクロアルキルニトリルピラゾロピリドン

Country Status (11)

Country Link
US (1) US9725445B2 (enExample)
EP (1) EP2976340B1 (enExample)
JP (1) JP6412102B2 (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)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112014029705A2 (pt) * 2012-06-01 2017-06-27 Takeda Pharmaceuticals Co composto ou sal, medicamento, métodos para inibir quinase de janus em um mamífero, e para a profilaxia ou tratamento de doenças autoimunes, e, uso de um composto ou sal
AU2014234908B2 (en) * 2013-03-19 2017-08-17 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as Janus kinase inhibitors
WO2017157735A1 (de) 2016-03-15 2017-09-21 Bayer Cropscience Aktiengesellschaft Substituierte sulfonylamide zur bekämpfung tierischer schädlinge
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
CN117756789A (zh) 2016-12-14 2024-03-26 英特维特国际股份有限公司 作为选择性Janus激酶抑制剂的氨基吡唑类化合物
KR102857917B1 (ko) * 2019-01-30 2025-09-10 펠리카메드 바이오테크놀로지 컴퍼니 리미티드 Jak 억제제 및 그 제조 방법
WO2021089673A1 (de) 2019-11-07 2021-05-14 Bayer Aktiengesellschaft Substituierte sulfonylamide zur bekämpfung tierischer schädlinge
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
MX2024007863A (es) 2021-12-24 2024-08-30 Intervet Int Bv Uso de compuestos de aminopirazol.
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
CN115141183B (zh) * 2022-07-26 2023-03-21 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
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

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102127078A (zh) * 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
EP2123651A4 (en) 2007-01-12 2011-05-04 Astellas Pharma Inc CONDENSED PYRIDINE COMPOUND
JP2010539080A (ja) * 2007-09-11 2010-12-16 メルク・シャープ・エンド・ドーム・コーポレイション Ｊａｎｕｓキナーゼの阻害剤
TW201105674A (en) 2009-07-08 2011-02-16 Leo Pharma As Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof
SMT201800137T1 (it) * 2010-03-10 2018-07-17 Incyte Holdings Corp Derivati di piperidin-4-il azetidina come inibitori di jak1
EP2688890B1 (en) 2011-03-22 2017-08-30 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
EP2527344A1 (en) * 2011-05-25 2012-11-28 Almirall, S.A. Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases
WO2013017479A1 (en) * 2011-07-29 2013-02-07 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
BR112014029705A2 (pt) * 2012-06-01 2017-06-27 Takeda Pharmaceuticals Co composto ou sal, medicamento, métodos para inibir quinase de janus em um mamífero, e para a profilaxia ou tratamento de doenças autoimunes, e, uso de um composto ou sal
AU2014234908B2 (en) * 2013-03-19 2017-08-17 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as Janus kinase inhibitors
WO2014146249A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
JP6305510B2 (ja) 2013-03-19 2018-04-04 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ヤヌスキナーゼ阻害剤としての非環式シアノエチルピラゾロピリドン

Also Published As

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

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