CN106661035B - 用作布鲁顿氏酪氨酸激酶的抑制剂的吡唑并嘧啶衍生物 - Google Patents

用作布鲁顿氏酪氨酸激酶的抑制剂的吡唑并嘧啶衍生物 Download PDF

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CN106661035B
CN106661035B CN201580043155.6A CN201580043155A CN106661035B CN 106661035 B CN106661035 B CN 106661035B CN 201580043155 A CN201580043155 A CN 201580043155A CN 106661035 B CN106661035 B CN 106661035B
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amino
phenyl
methyl
pyrazolo
mmol
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CN106661035A (zh
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马修·考尔德
尼古拉斯·E·S·格伊索特
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Limited By Share Ltd Roxo Oncology
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Redx Pharma Ltd
Loxo Oncology Inc
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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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P43/00—Drugs 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201580043155.6A 2014-06-11 2015-06-11 用作布鲁顿氏酪氨酸激酶的抑制剂的吡唑并嘧啶衍生物 Active CN106661035B (zh)

Applications Claiming Priority (3)

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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

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CN106661035A CN106661035A (zh) 2017-05-10
CN106661035B true CN106661035B (zh) 2019-11-19

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

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GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
EA201890730A1 (ru) * 2015-09-16 2018-10-31 Локсо Онколоджи, Инк. Производные пиразолопиримидина в качестве ингибиторов btk для лечения злокачественного новообразования
WO2017103611A1 (en) 2015-12-16 2017-06-22 Redx Pharma Plc Compounds useful as kinase inhibitors
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
WO2017111787A1 (en) * 2015-12-23 2017-06-29 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
US10662187B2 (en) * 2016-01-21 2020-05-26 Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. Bruton's tyrosine kinase inhibitors
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
TW201811795A (zh) 2016-08-24 2018-04-01 美商亞闊股份有限公司 胺基－吡咯并嘧啶酮化合物及其用途
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
KR102801205B1 (ko) 2019-12-04 2025-04-29 허난 즈웨이 바이오메디슨 씨오., 엘티디. 브루톤 티로신 키나제 억제제인 이미다졸 카복사마이드 유도체
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
WO2021180107A1 (en) * 2020-03-12 2021-09-16 Fochon Pharmaceuticals, 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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WO2008039218A2 (en) * 2006-09-22 2008-04-03 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2008121742A2 (en) * 2007-03-28 2008-10-09 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2011046964A2 (en) * 2009-10-12 2011-04-21 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
CN102159214A (zh) * 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
WO2013010136A2 (en) * 2011-07-13 2013-01-17 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2013102059A1 (en) * 2011-12-30 2013-07-04 Pharmacyclics, Inc. Pyrazolo [3, 4-d] pyrimidine and pyrrolo [2, 3-d] pyrimidine compounds as kinase inhibitors
US8673925B1 (en) * 2013-04-09 2014-03-18 Principia Biopharma Inc. Tyrosine kinase inhibitors
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GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
EA201890730A1 (ru) 2015-09-16 2018-10-31 Локсо Онколоджи, Инк. Производные пиразолопиримидина в качестве ингибиторов btk для лечения злокачественного новообразования
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WO2002080926A1 (en) * 2001-03-22 2002-10-17 Abbott Gmbh & Co. Kg Pyrazolopyrimidines as therapeutic agents
WO2008039218A2 (en) * 2006-09-22 2008-04-03 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2008121742A2 (en) * 2007-03-28 2008-10-09 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
CN102159214A (zh) * 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
WO2011046964A2 (en) * 2009-10-12 2011-04-21 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2013010136A2 (en) * 2011-07-13 2013-01-17 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2013102059A1 (en) * 2011-12-30 2013-07-04 Pharmacyclics, Inc. Pyrazolo [3, 4-d] pyrimidine and pyrrolo [2, 3-d] pyrimidine compounds as kinase inhibitors
US8673925B1 (en) * 2013-04-09 2014-03-18 Principia Biopharma Inc. Tyrosine kinase inhibitors
WO2014188173A1 (en) * 2013-05-20 2014-11-27 Redx Pharma Limited Pyrazolopyrimidine derivatives useful as inhibitors of bruton's tyrosine kinase

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Publication number Publication date
EP3154978B1 (en) 2019-04-03
ES2732897T3 (es) 2019-11-26
US20170129897A1 (en) 2017-05-11
US20190119281A1 (en) 2019-04-25
GB201410430D0 (en) 2014-07-23
AU2015273217A1 (en) 2017-01-05
WO2015189620A1 (en) 2015-12-17
JP2017519754A (ja) 2017-07-20
EP3154978A1 (en) 2017-04-19
US10538524B2 (en) 2020-01-21
JP6721521B2 (ja) 2020-07-15
CA2951504A1 (en) 2015-12-17
AU2015273217B2 (en) 2019-07-18
CA2951504C (en) 2023-10-03
CN106661035A (zh) 2017-05-10
US9975897B2 (en) 2018-05-22

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