AU2015273217B2 - Pyrazolopyrimidine derivatives useful as inhibitors of Bruton's tyrosine kinase - Google Patents

Pyrazolopyrimidine derivatives useful as inhibitors of Bruton's tyrosine kinase Download PDF

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Publication number
AU2015273217B2
AU2015273217B2 AU2015273217A AU2015273217A AU2015273217B2 AU 2015273217 B2 AU2015273217 B2 AU 2015273217B2 AU 2015273217 A AU2015273217 A AU 2015273217A AU 2015273217 A AU2015273217 A AU 2015273217A AU 2015273217 B2 AU2015273217 B2 AU 2015273217B2
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amino
phenyl
methyl
mmol
pyrimidin
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AU2015273217A1 (en
Inventor
Mathew CALDER
Nicolas E. S. GUISOT
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Redx Pharma Ltd
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Redx Pharma Ltd
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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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2015273217A 2014-06-11 2015-06-11 Pyrazolopyrimidine derivatives useful as inhibitors of Bruton's tyrosine kinase Active AU2015273217B2 (en)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
AU2015273217A1 AU2015273217A1 (en) 2017-01-05
AU2015273217B2 true AU2015273217B2 (en) 2019-07-18

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015273217A Active AU2015273217B2 (en) 2014-06-11 2015-06-11 Pyrazolopyrimidine derivatives useful as inhibitors of Bruton's tyrosine kinase

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
CN114685516A (zh) * 2015-09-16 2022-07-01 洛克索肿瘤学股份有限公司 用于治疗癌症的作为btk抑制剂的吡唑并嘧啶衍生物
PT3390395T (pt) 2015-12-16 2020-11-03 Loxo Oncology Inc Compostos úteis como inibidores de quinase
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
PH12018501390B1 (en) * 2015-12-23 2022-06-10 Arqule Inc Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
IL260691B (en) * 2016-01-21 2022-07-01 Zibo Biopolar Changsheng Pharmaceutical Co Ltd Bruton's tyrosine kinase inhibitors
KR102327917B1 (ko) * 2016-07-07 2021-11-17 주식회사 대웅제약 신규한 4-아미노피라졸로[3,4-d]피리미디닐아자바이사이클로 유도체 및 이를 포함하는 약학 조성물
BR112019003504A2 (pt) 2016-08-24 2019-05-21 Arqule, Inc. compostos de amino-pirrolopirimidinona e métodos de uso dos mesmos
WO2019130229A1 (en) * 2017-12-28 2019-07-04 Mylan Laboratories Ltd Methods and intermediates for preparing rucaparib
US20220362357A1 (en) 2018-08-31 2022-11-17 Stichting Radboud Universitair Medisch Centrum Synergistic Combinations of Amino Acid Depletion Agent Sensitizers (AADAS) and Amino Acid Depletion Agents (AADA), and Therapeutic Methods of Use Thereof
EP4069689A4 (en) * 2019-12-04 2023-12-20 Henan Zhiwei Biomedicine Co., Ltd. SUBSTITUTED IMIDAZOLECARBOXAMIDE AS BRUTON TYROSINKINASE INHIBITORS
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
EP4118086A1 (en) * 2020-03-12 2023-01-18 Fochon Biosciences, Ltd. Compounds useful as kinase inhibitors
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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US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
US20030225098A1 (en) 2002-03-21 2003-12-04 Hirst Gavin C. Kinase inhibitors
SG166093A1 (en) * 2006-09-22 2010-11-29 Pharmacyclics Inc Inhibitors of brutonæs tyrosine kinase
US8987233B2 (en) 2006-11-03 2015-03-24 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
CN101674834B (zh) * 2007-03-28 2013-06-12 环状药物公司 布鲁顿氏酪氨酸激酶(Bruton's tyrosine kinase)抑制剂
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
NZ624345A (en) 2008-06-27 2016-07-29 Celgene Avilomics Res Inc 2,4-disubstituted pyrimidines useful as kinase inhibitors
CA2730930C (en) * 2008-07-16 2015-01-13 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
JP5385382B2 (ja) 2008-07-24 2014-01-08 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ プロテインキナーゼ阻害剤としての3,4−ジアリールピラゾール
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CN114685516A (zh) 2015-09-16 2022-07-01 洛克索肿瘤学股份有限公司 用于治疗癌症的作为btk抑制剂的吡唑并嘧啶衍生物
PT3390395T (pt) 2015-12-16 2020-11-03 Loxo Oncology Inc Compostos úteis como inibidores de quinase

Also Published As

Publication number Publication date
CA2951504C (en) 2023-10-03
CN106661035A (zh) 2017-05-10
US20170129897A1 (en) 2017-05-11
JP2017519754A (ja) 2017-07-20
EP3154978A1 (en) 2017-04-19
US10538524B2 (en) 2020-01-21
US9975897B2 (en) 2018-05-22
CN106661035B (zh) 2019-11-19
US20190119281A1 (en) 2019-04-25
CA2951504A1 (en) 2015-12-17
AU2015273217A1 (en) 2017-01-05
GB201410430D0 (en) 2014-07-23
WO2015189620A1 (en) 2015-12-17
ES2732897T3 (es) 2019-11-26
EP3154978B1 (en) 2019-04-03
JP6721521B2 (ja) 2020-07-15

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