JP6721521B2 - ブルトン型チロシンキナーゼのインヒビターとして有用なピラゾロピリミジン誘導体 - Google Patents

ブルトン型チロシンキナーゼのインヒビターとして有用なピラゾロピリミジン誘導体 Download PDF

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JP6721521B2
JP6721521B2 JP2016572754A JP2016572754A JP6721521B2 JP 6721521 B2 JP6721521 B2 JP 6721521B2 JP 2016572754 A JP2016572754 A JP 2016572754A JP 2016572754 A JP2016572754 A JP 2016572754A JP 6721521 B2 JP6721521 B2 JP 6721521B2
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amino
methyl
phenyl
pyrazolo
mmol
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JP2017519754A (ja
JP2017519754A5 (enExample
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マテオ カルダー
マテオ カルダー
イー エス ギゾー ニコラ
イー エス ギゾー ニコラ
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Loxo Oncology Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016572754A 2014-06-11 2015-06-11 ブルトン型チロシンキナーゼのインヒビターとして有用なピラゾロピリミジン誘導体 Active JP6721521B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1410430.1A GB201410430D0 (en) 2014-06-11 2014-06-11 Compounds
GB1410430.1 2014-06-11
PCT/GB2015/051719 WO2015189620A1 (en) 2014-06-11 2015-06-11 Pyrazolopyrimidine derivatives useful as inhibitors of bruton's tyrosine kinase

Publications (3)

Publication Number Publication Date
JP2017519754A JP2017519754A (ja) 2017-07-20
JP2017519754A5 JP2017519754A5 (enExample) 2018-07-26
JP6721521B2 true JP6721521B2 (ja) 2020-07-15

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JP2016572754A Active JP6721521B2 (ja) 2014-06-11 2015-06-11 ブルトン型チロシンキナーゼのインヒビターとして有用なピラゾロピリミジン誘導体

Country Status (9)

Country Link
US (2) US9975897B2 (enExample)
EP (1) EP3154978B1 (enExample)
JP (1) JP6721521B2 (enExample)
CN (1) CN106661035B (enExample)
AU (1) AU2015273217B2 (enExample)
CA (1) CA2951504C (enExample)
ES (1) ES2732897T3 (enExample)
GB (1) GB201410430D0 (enExample)
WO (1) WO2015189620A1 (enExample)

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GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
WO2017046604A1 (en) * 2015-09-16 2017-03-23 Redx Pharma Plc Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer
PE20220507A1 (es) * 2015-12-16 2022-04-07 Loxo Oncology Inc Compuestos utiles como inhibidores de cinasa
PT3882250T (pt) * 2015-12-23 2023-04-21 Arqule Inc Tetrahidropiranil amino-pirrolopirimidinona e métodos de utilização da mesma
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
KR102699906B1 (ko) * 2016-01-21 2024-08-29 즈보 바이오폴라 창쉥 파마수티컬 컴퍼니 리미티드 브루톤 티로신 키나제 억제제
CN109153680B (zh) * 2016-07-07 2021-04-23 株式会社大熊制药 4-氨基吡唑并[3,4-d]嘧啶基氮杂双环衍生物及含其的药物组合物
EP3504213A4 (en) 2016-08-24 2020-01-15 ArQule, Inc. AMINO-PYRROLOPYRIMIDINONE COMPOUNDS AND METHOD FOR USE THEREOF
WO2019130229A1 (en) * 2017-12-28 2019-07-04 Mylan Laboratories Ltd Methods and intermediates for preparing rucaparib
CA3111126A1 (en) 2018-08-31 2020-03-05 Stichting Katholieke Universiteit Synergistic combinations of amino acid depletion agent sensitizers (aadas) and amino acid depletion agents (aada), and therapeutic methods of use thereof
CN114761399B (zh) * 2019-12-04 2024-03-26 河南知微生物医药有限公司 作为布鲁顿酪氨酸激酶抑制剂的咪唑甲酰胺衍生物
JP7011638B2 (ja) * 2019-12-16 2022-02-10 アークル インコーポレイテッド テトラヒドロピラニルアミノ-ピロロピリミジノンおよびその使用の方法
CN113214265B (zh) * 2020-01-21 2023-07-07 江苏先声药业有限公司 嘧啶并五元环类化合物
RU2747991C1 (ru) * 2020-02-18 2021-05-18 Аркьюл, Инк. Тетрагидропиранил амино-пирролопиримидинон и способы его применения
JP2023518006A (ja) * 2020-03-12 2023-04-27 フォチョン・バイオサイエンシーズ・リミテッド キナーゼ阻害剤としての化合物
CN114075190A (zh) * 2020-08-20 2022-02-22 北京诺诚健华医药科技有限公司 杂环类btk抑制剂

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US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
TWI546290B (zh) 2008-06-27 2016-08-21 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
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GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
WO2017046604A1 (en) 2015-09-16 2017-03-23 Redx Pharma Plc Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer
PE20220507A1 (es) 2015-12-16 2022-04-07 Loxo Oncology Inc Compuestos utiles como inhibidores de cinasa

Also Published As

Publication number Publication date
AU2015273217A1 (en) 2017-01-05
JP2017519754A (ja) 2017-07-20
EP3154978A1 (en) 2017-04-19
US20190119281A1 (en) 2019-04-25
GB201410430D0 (en) 2014-07-23
US10538524B2 (en) 2020-01-21
CN106661035B (zh) 2019-11-19
CN106661035A (zh) 2017-05-10
EP3154978B1 (en) 2019-04-03
US9975897B2 (en) 2018-05-22
US20170129897A1 (en) 2017-05-11
AU2015273217B2 (en) 2019-07-18
CA2951504C (en) 2023-10-03
WO2015189620A1 (en) 2015-12-17
ES2732897T3 (es) 2019-11-26
CA2951504A1 (en) 2015-12-17

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