CA2951504C - 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
CA2951504C
CA2951504C CA2951504A CA2951504A CA2951504C CA 2951504 C CA2951504 C CA 2951504C CA 2951504 A CA2951504 A CA 2951504A CA 2951504 A CA2951504 A CA 2951504A CA 2951504 C CA2951504 C CA 2951504C
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Canada
Prior art keywords
amino
pyrazolo
compound
methyl
pyrimidin
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CA2951504A
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English (en)
French (fr)
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CA2951504A1 (en
Inventor
Mathew CALDER
Nicolas E. S. GUISOT
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Loxo Oncology Inc
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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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
CA2951504A 2014-06-11 2015-06-11 Pyrazolopyrimidine derivatives useful as inhibitors of bruton's tyrosine kinase Active CA2951504C (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
CA2951504A1 CA2951504A1 (en) 2015-12-17
CA2951504C true CA2951504C (en) 2023-10-03

Family

ID=51267088

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2951504A Active CA2951504C (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 (ref)
EP (1) EP3154978B1 (ref)
JP (1) JP6721521B2 (ref)
CN (1) CN106661035B (ref)
AU (1) AU2015273217B2 (ref)
CA (1) CA2951504C (ref)
ES (1) ES2732897T3 (ref)
GB (1) GB201410430D0 (ref)
WO (1) WO2015189620A1 (ref)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
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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
ES2828431T3 (es) 2015-12-16 2021-05-26 Loxo Oncology Inc Compuestos útiles como inhibidores de cinasa
HRP20230379T1 (hr) * 2015-12-23 2023-06-23 Arqule, Inc. TETRAHIDROPIRANIL AMINO-PIROLOPIRIMIDINON ZA PRIMJENU U LIJEČENJU POREMEĆAJA POSREDOVANIH BTK-om
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
CA3009669C (en) * 2016-01-21 2023-08-08 Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. Bruton's tyrosine kinase inhibitors
US10399988B2 (en) 2016-07-07 2019-09-03 Daewoong Pharmaceutical Co., Ltd. 4-aminopyrazolo[3,4-d]pyrimidinylazabicyclo derivatives and pharmaceutical composition comprising the same
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
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
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
KR20020088406A (ko) 1999-09-17 2002-11-27 애보트 게엠베하 운트 콤파니 카게 치료제로서의 피라졸로피리미딘
US20030225098A1 (en) 2002-03-21 2003-12-04 Hirst Gavin C. Kinase inhibitors
PL2526933T3 (pl) * 2006-09-22 2015-08-31 Pharmacyclics Llc Inhibitory kinazy tyrozynowej Brutona
ES2403546T3 (es) 2006-11-03 2013-05-20 Pharmacyclics, Inc. Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización
SG10201508035TA (en) * 2007-03-28 2015-10-29 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
CA2730930C (en) * 2008-07-16 2015-01-13 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
PL2324008T3 (pl) 2008-07-24 2012-09-28 Nerviano Medical Sciences Srl 3,4-diarylopirazole jako inhibitory kinazy białkowej
US8426428B2 (en) 2008-12-05 2013-04-23 Principia Biopharma, Inc. EGFR kinase knockdown via electrophilically enhanced inhibitors
US7741330B1 (en) 2009-10-12 2010-06-22 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
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EA025496B1 (ru) 2011-05-17 2016-12-30 Принсипиа Биофарма Инк. Ингибиторы тирозинкиназы
HUE048834T2 (hu) 2011-05-17 2020-08-28 Univ California Kináz inhibitorok
EA201490265A1 (ru) * 2011-07-13 2014-12-30 Фармасайкликс, Инк. Ингибиторы тирозинкиназы брутона
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
US8377946B1 (en) * 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase 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
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GB201309085D0 (en) * 2013-05-20 2013-07-03 Redx Pharma Ltd Compounds
RS60934B1 (sr) 2013-09-30 2020-11-30 Guangzhou Innocare Pharma Tech Co Ltd Supstituisani nikotinimidni inhibitori btk i njihova priprema i upotreba u lečenju karcinoma, inflamatorne i autoimune bolesti
EP3082809B1 (en) 2013-12-20 2021-01-20 Merck Sharp & Dohme Corp. Btk inhibitors
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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
ES2828431T3 (es) 2015-12-16 2021-05-26 Loxo Oncology Inc Compuestos útiles como inhibidores de cinasa

Also Published As

Publication number Publication date
US9975897B2 (en) 2018-05-22
US20190119281A1 (en) 2019-04-25
JP2017519754A (ja) 2017-07-20
CN106661035B (zh) 2019-11-19
JP6721521B2 (ja) 2020-07-15
GB201410430D0 (en) 2014-07-23
WO2015189620A1 (en) 2015-12-17
CA2951504A1 (en) 2015-12-17
US20170129897A1 (en) 2017-05-11
AU2015273217B2 (en) 2019-07-18
AU2015273217A1 (en) 2017-01-05
EP3154978A1 (en) 2017-04-19
EP3154978B1 (en) 2019-04-03
CN106661035A (zh) 2017-05-10
US10538524B2 (en) 2020-01-21
ES2732897T3 (es) 2019-11-26

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