JP2016514709A - ヤヌスキナーゼ阻害剤としてのジェミナル置換シアノエチ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ジェミナル置換シアノエチルピラゾロピリドン Download PDF

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Publication number
JP2016514709A
JP2016514709A JP2016503521A JP2016503521A JP2016514709A JP 2016514709 A JP2016514709 A JP 2016514709A JP 2016503521 A JP2016503521 A JP 2016503521A JP 2016503521 A JP2016503521 A JP 2016503521A JP 2016514709 A JP2016514709 A JP 2016514709A
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JP
Japan
Prior art keywords
oxo
dihydro
amino
pyrazolo
pyridin
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Pending
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JP2016503521A
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Japanese (ja)
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JP2016514709A5 (enExample
Inventor
チルダーズ，マシユー・ロイド
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
マルテイネス，ミシエル
フアルコン，ダニエル
トーレス，ルイス
ドウオン，ヨーンチイ
クルクラスリヤ，ラビ
ズオン，ホーンボー
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 & Dohme LLC
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Merck Sharp & Dohme LLC
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Publication of JP2016514709A publication Critical patent/JP2016514709A/ja
Publication of JP2016514709A5 publication Critical patent/JP2016514709A5/ja
Pending 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
    • 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
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • 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)
  • 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)
  • 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)
JP2016503521A 2013-03-19 2014-03-19 ヤヌスキナーゼ阻害剤としてのジェミナル置換シアノエチルピラゾロピリドン Pending JP2016514709A (ja)

Applications Claiming Priority (3)

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
PCT/CN2014/000297 WO2014146491A1 (en) 2013-03-19 2014-03-19 Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors

Publications (2)

Publication Number Publication Date
JP2016514709A true JP2016514709A (ja) 2016-05-23
JP2016514709A5 JP2016514709A5 (enExample) 2017-04-06

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JP2016503521A Pending JP2016514709A (ja) 2013-03-19 2014-03-19 ヤヌスキナーゼ阻害剤としてのジェミナル置換シアノエチルピラゾロピリドン

Country Status (9)

Country Link
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)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7023026B1 (ja) 2021-05-18 2022-02-21 株式会社アイビー化粧品 Ｊａｋ阻害剤
JP2022518821A (ja) * 2019-01-30 2022-03-16 格格巫（珠海）生物科技有限公司 Ｊａｋ阻害剤及びその製造方法

Families Citing this family (6)

* 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
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

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100105661A1 (en) * 2007-01-12 2010-04-29 Astellas Pharma Inc. Condensed pyridine compound
JP2011503194A (ja) * 2007-11-16 2011-01-27 インサイト・コーポレイション Ｊａｎｕｓキナーゼ阻害剤としての置換複素環
JP2011514909A (ja) * 2008-03-11 2011-05-12 インサイト・コーポレイション Ｊａｋ阻害剤としてのアゼチジン誘導体およびシクロブタン誘導体
WO2012030924A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Azolopyridine and azolopyrimidine compounds and methods of use thereof
JP2013503191A (ja) * 2009-08-27 2013-01-31 バイオクライスト ファーマシューティカルズ， インコーポレイテッド ヤヌスキナーゼインヒビターとしての複素環式化合物
WO2013041042A1 (en) * 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Pyrazole carboxamides as janus kinase inhibitors
JP2013522214A (ja) * 2010-03-10 2013-06-13 インサイト・コーポレイション Ｊａｋ１阻害剤としてのピペリジン−４−イルアゼチジン誘導体
JP2013523884A (ja) * 2010-04-14 2013-06-17 アレイ バイオファーマ、インコーポレイテッド ＪＡＫキナーゼの阻害剤としての５，７置換イミダゾ［１，２−ｃ］ピリミジン
WO2013180265A1 (ja) * 2012-06-01 2013-12-05 武田薬品工業株式会社 複素環化合物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2340611C2 (ru) * 2000-09-15 2008-12-10 Вертекс Фармасьютикалз Инкорпорейтед Производные пиразола, используемые в качестве ингибиторов протеинкиназы
KR20140009259A (ko) * 2010-11-19 2014-01-22 에프. 호프만-라 로슈 아게 피라졸로피리딘 및 tyk2 억제제로서 이의 용도
EP2694060A4 (en) * 2011-04-01 2014-09-10 Univ Utah Res Found SUBSTITUTED 3- (1H-BENZO- {D} -IMIDAZOL-2-YL-) 1H-INDAZOL ANALOGUE AS PDK1 KINASE INHIBITOR
UA111854C2 (uk) * 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013192125A1 (en) * 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100105661A1 (en) * 2007-01-12 2010-04-29 Astellas Pharma Inc. Condensed pyridine compound
JP2011503194A (ja) * 2007-11-16 2011-01-27 インサイト・コーポレイション Ｊａｎｕｓキナーゼ阻害剤としての置換複素環
JP2011514909A (ja) * 2008-03-11 2011-05-12 インサイト・コーポレイション Ｊａｋ阻害剤としてのアゼチジン誘導体およびシクロブタン誘導体
JP2013503191A (ja) * 2009-08-27 2013-01-31 バイオクライスト ファーマシューティカルズ， インコーポレイテッド ヤヌスキナーゼインヒビターとしての複素環式化合物
JP2013522214A (ja) * 2010-03-10 2013-06-13 インサイト・コーポレイション Ｊａｋ１阻害剤としてのピペリジン−４−イルアゼチジン誘導体
JP2013523884A (ja) * 2010-04-14 2013-06-17 アレイ バイオファーマ、インコーポレイテッド ＪＡＫキナーゼの阻害剤としての５，７置換イミダゾ［１，２−ｃ］ピリミジン
WO2012030924A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Azolopyridine and azolopyrimidine compounds and methods of use thereof
WO2013041042A1 (en) * 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Pyrazole carboxamides as janus kinase inhibitors
WO2013040863A1 (en) * 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors
WO2013180265A1 (ja) * 2012-06-01 2013-12-05 武田薬品工業株式会社 複素環化合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SMYTH, L. A. ET AL.，BIOORGANIC & MEDICINAL CHEMISTRY，2011，19(11)，3569-3578，DOI:10.1016/J.BMC.20, JPN6018008441, ISSN: 0003755018 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022518821A (ja) * 2019-01-30 2022-03-16 格格巫（珠海）生物科技有限公司 Ｊａｋ阻害剤及びその製造方法
JP7278649B2 (ja) 2019-01-30 2023-05-22 格格巫（珠海）生物科技有限公司 Ｊａｋ阻害剤及びその製造方法
JP7278649B6 (ja) 2019-01-30 2024-02-15 格格巫（珠海）生物科技有限公司 Ｊａｋ阻害剤及びその製造方法
US12509463B2 (en) 2019-01-30 2025-12-30 Felicamed Biotechnology Co., Ltd. JAK inhibitor and preparation method therefor
JP7023026B1 (ja) 2021-05-18 2022-02-21 株式会社アイビー化粧品 Ｊａｋ阻害剤
JP2022177590A (ja) * 2021-05-18 2022-12-01 株式会社アイビー化粧品 Ｊａｋ阻害剤

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
CN105189498B (zh) 2017-06-27
EP2976339B1 (en) 2018-06-27
EP2976339A4 (en) 2016-08-31
AU2014234907A1 (en) 2015-08-13
EP2976339A1 (en) 2016-01-27
RU2664533C2 (ru) 2018-08-20
US9957264B2 (en) 2018-05-01

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