CN109890829B - 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物 - Google Patents

作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物 Download PDF

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Publication number
CN109890829B
CN109890829B CN201780065283.XA CN201780065283A CN109890829B CN 109890829 B CN109890829 B CN 109890829B CN 201780065283 A CN201780065283 A CN 201780065283A CN 109890829 B CN109890829 B CN 109890829B
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pyridin
methyl
pyrimidine
pyrazolo
alkyl
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Chinese (zh)
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CN109890829A (zh
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M·C·布赖恩
J·德罗布尼克
J·R·小基弗
A·科列斯尼科夫
N·S·拉贾帕克萨
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F Hoffmann La Roche AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201780065283.XA 2016-11-02 2017-10-31 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物 Expired - Fee Related CN109890829B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662416550P 2016-11-02 2016-11-02
US62/416,550 2016-11-02
US201662417893P 2016-11-04 2016-11-04
US62/417,893 2016-11-04
PCT/EP2017/077886 WO2018083085A1 (en) 2016-11-02 2017-10-31 PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS

Publications (2)

Publication Number Publication Date
CN109890829A CN109890829A (zh) 2019-06-14
CN109890829B true CN109890829B (zh) 2022-07-15

Family

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Application Number Title Priority Date Filing Date
CN201780065283.XA Expired - Fee Related CN109890829B (zh) 2016-11-02 2017-10-31 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物

Country Status (5)

Country Link
US (1) US11434250B2 (https=)
EP (1) EP3535273A1 (https=)
JP (1) JP7059268B2 (https=)
CN (1) CN109890829B (https=)
WO (1) WO2018083085A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202340194A (zh) 2017-02-16 2023-10-16 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
TWI842978B (zh) 2018-07-13 2024-05-21 美商基利科學股份有限公司 衍生物
WO2020036830A1 (en) * 2018-08-13 2020-02-20 Gilead Sciences, Inc. Pyrrolo[1,2-b]pyridazine derivatives as irak4 inhibitors
GB201904373D0 (en) * 2019-03-29 2019-05-15 Galapagos Nv Novel compounds and pharamaceutical compositions thereof for the treatment of inflammatory disorders
CN113402499B (zh) 2021-06-21 2022-05-13 上海勋和医药科技有限公司 一种亚磺酰亚胺取代的吲唑类irak4激酶抑制剂、制备方法及用途

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0329214D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
EP2288260A4 (en) 2008-06-20 2013-10-23 Genentech Inc TRIAZOLOPYRIDINE-JAK HEMMER COMPOUNDS AND METHOD
JP5985473B2 (ja) * 2010-07-13 2016-09-06 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft IRAK4モジュレーターとしてのピラゾロ[1,5a]ピリミジン及びチエノ[3,2b]ピリミジン誘導体
WO2012007855A1 (en) 2010-07-14 2012-01-19 Ecole Polytechnique Federale De Lausanne (Epfl) System and method for 3d gait assessment
DK2649075T3 (en) * 2010-12-08 2018-07-30 Us Health SUBSTITUTED PYRAZOLOPYRIMIDINES AS GLUCOCEREBROSIDASE ACTIVATORS
SI2941432T1 (en) * 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
JP6437452B2 (ja) * 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Pimキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物
JP2017518348A (ja) 2014-06-20 2017-07-06 オーリジーン ディスカバリー テクノロジーズ リミテッドAurigene Discovery Technologies Limited Irak4阻害剤としての置換インダゾール化合物
HRP20240644T1 (hr) 2014-11-06 2024-08-02 Bial-R&D Investments, S.A. Supstituirani pirazolo(1,5-a)pirimidini i njihova uporaba u liječenju medicinskih poremećaja
EP3268003B1 (en) 2015-03-12 2020-07-29 Merck Sharp & Dohme Corp. Thienopyrazine inhibitors of irak4 activity
WO2016144848A1 (en) 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Pyrrolotriazine inhibitors of irak4 activity
EP3267996B1 (en) 2015-03-12 2020-11-11 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
US10155765B2 (en) * 2015-03-12 2018-12-18 Merck Sharp & Dohme Corp. Carboxamide inhibitors of IRAK4 activity
BR112018000624A2 (pt) 2015-07-15 2018-09-18 Aurigene Discovery Technologies Limited compostos de indazol e azaindazol como inibidores de irak-4
JP2018524365A (ja) * 2015-07-15 2018-08-30 アウリジーン ディスカバリー テクノロジーズ リミテッド Irak−4阻害剤としての置換アザ化合物
EP3394066A2 (en) * 2015-12-22 2018-10-31 H. Hoffnabb-La Roche Ag PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS

Also Published As

Publication number Publication date
JP7059268B2 (ja) 2022-04-25
JP2019532974A (ja) 2019-11-14
WO2018083085A1 (en) 2018-05-11
CN109890829A (zh) 2019-06-14
US20200262845A1 (en) 2020-08-20
US11434250B2 (en) 2022-09-06
EP3535273A1 (en) 2019-09-11

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