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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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)
  • 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)
  • 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)

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

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

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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)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
UA127863C2 (uk) 2015-12-16 2024-01-31 Локсо Онколоджі, Інк. Сполуки, які можна застосовувати як інгібітори кінази
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
FI3882250T3 (fi) * 2015-12-23 2023-04-27 Arqule Inc TETRAHYDROPYRANYYLIAMINO-PYRROLOPYRIMIDINONI KÄYTETTÄVÄKSI HOIDETTAESSA BTK-VÄLITTEISiÄ HÄIRIÖITÄ
KR102699906B1 (ko) * 2016-01-21 2024-08-29 즈보 바이오폴라 창쉥 파마수티컬 컴퍼니 리미티드 브루톤 티로신 키나제 억제제
ES2965081T3 (es) 2016-07-07 2024-04-11 Daewoong Pharmaceutical Co Ltd Derivados 4-aminopirazolo[3,4-d]pirimidinil-azabiciclo y composición farmacéutica que comprende dichos derivados
SG11201901197PA (en) 2016-08-24 2019-03-28 Arqule Inc Amino-pyrrolopyrimidinone compounds and methods of use thereof
WO2019130229A1 (en) * 2017-12-28 2019-07-04 Mylan Laboratories Ltd Methods and intermediates for preparing rucaparib
WO2020043321A1 (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
WO2021110142A1 (en) * 2019-12-04 2021-06-10 Henan Normal University Substituted imidazolecarboxamide as bruton's tyrosine kinase 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
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

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
WO2014188173A1 (en) * 2013-05-20 2014-11-27 Redx Pharma Limited Pyrazolopyrimidine derivatives useful as inhibitors of bruton's tyrosine kinase

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL148718A0 (en) 1999-09-17 2002-09-12 Abbott Gmbh & Co Kg Pyrazolopyrimidines as therapeutic agents
US20030225098A1 (en) 2002-03-21 2003-12-04 Hirst Gavin C. Kinase inhibitors
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
SG10201510696RA (en) 2008-06-27 2016-01-28 Celgene Avilomics Res Inc Heteroaryl compounds and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AU2009273197B2 (en) 2008-07-24 2014-01-16 Nerviano Medical Sciences S.R.L. 3,4-diarylpyrazoles as protein kinase inhibitors
US8426428B2 (en) 2008-12-05 2013-04-23 Principia Biopharma, Inc. EGFR kinase knockdown via electrophilically enhanced inhibitors
CA3007787C (en) 2010-06-03 2020-03-10 Pharmacyclics Llc The use of inhibitors of bruton's tyrosine kinase (btk)
PL2710007T3 (pl) 2011-05-17 2020-06-01 The Regents Of The University Of California Inhibitory kinazy
US8962831B2 (en) 2011-05-17 2015-02-24 Principia Biopharma Inc. Tyrosine kinase inhibitors
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
DK2861599T3 (da) 2012-06-18 2020-03-02 Principia Biopharma Inc Reversible kovalente pyrrolo- eller pyrazolopyrimidiner, der er nyttige til behandling af cancer og autoimmunsygdomme
US9572811B2 (en) 2012-08-03 2017-02-21 Principia Biopharma Inc. Treatment of dry eye
BR112015009624A2 (pt) 2012-11-02 2017-11-14 Pfizer inibidores de tirosina cinase de bruton
CN103848810A (zh) 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
CN104341388B (zh) 2013-10-16 2017-03-22 北京诺诚健华医药科技有限公司 芳香族酰胺类衍生物、其制备方法及其在医药上的应用
EP3082809B1 (en) 2013-12-20 2021-01-20 Merck Sharp & Dohme Corp. Btk inhibitors
KR20160117614A (ko) 2014-02-21 2016-10-10 프린시피아 바이오파마, 인코퍼레이티드 Btk 억제제의 염 및 고체 형태
GB201404987D0 (en) 2014-03-20 2014-05-07 Redx Pharma Ltd Compounds
CN105085474B (zh) 2014-05-07 2018-05-18 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
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
UA127863C2 (uk) 2015-12-16 2024-01-31 Локсо Онколоджі, Інк. Сполуки, які можна застосовувати як інгібітори кінази

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

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

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