CA2706946A1 - 2-fluoropyrazolo[1,5-a] pyrimidines en tant qu'inhibiteurs de proteine kinase - Google Patents

2-fluoropyrazolo[1,5-a] pyrimidines en tant qu'inhibiteurs de proteine kinase Download PDF

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Publication number
CA2706946A1
CA2706946A1 CA2706946A CA2706946A CA2706946A1 CA 2706946 A1 CA2706946 A1 CA 2706946A1 CA 2706946 A CA2706946 A CA 2706946A CA 2706946 A CA2706946 A CA 2706946A CA 2706946 A1 CA2706946 A1 CA 2706946A1
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CA
Canada
Prior art keywords
compound
alkyl
group
heteroaryl
substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2706946A
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English (en)
Inventor
Kamil Paruch
Timothy J. Guzi
Michael P. Dwyer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme Corp
Original Assignee
Schering Corporation
Kamil Paruch
Timothy J. Guzi
Michael P. Dwyer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corporation, Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer filed Critical Schering Corporation
Publication of CA2706946A1 publication Critical patent/CA2706946A1/fr
Abandoned legal-status Critical Current

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Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
CA2706946A 2007-11-28 2008-11-25 2-fluoropyrazolo[1,5-a] pyrimidines en tant qu'inhibiteurs de proteine kinase Abandoned CA2706946A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US99073607P 2007-11-28 2007-11-28
US60/990,736 2007-11-28
PCT/US2008/084643 WO2009070567A1 (fr) 2007-11-28 2008-11-25 2-fluoropyrazolo[1,5-a] pyrimidines en tant qu'inhibiteurs de protéine kinase

Publications (1)

Publication Number Publication Date
CA2706946A1 true CA2706946A1 (fr) 2009-06-04

Family

ID=40343608

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2706946A Abandoned CA2706946A1 (fr) 2007-11-28 2008-11-25 2-fluoropyrazolo[1,5-a] pyrimidines en tant qu'inhibiteurs de proteine kinase

Country Status (6)

Country Link
EP (1) EP2225247A1 (fr)
JP (1) JP2011504931A (fr)
CN (1) CN101970440A (fr)
CA (1) CA2706946A1 (fr)
MX (1) MX2010005950A (fr)
WO (1) WO2009070567A1 (fr)

Families Citing this family (33)

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UY32192A (es) 2008-10-22 2011-05-31 Array Biopharma Inc COMPUESTOS PIRAZOLO[1,5-a]PIRIMIDINA SUSTITUIDA COMO INHIBIDORES DE TRK CINASA
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
HUE035337T2 (en) 2010-05-20 2018-05-02 Array Biopharma Inc Macrocyclic compounds as TRK kinase inhibitors
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
DK3486245T3 (da) 2012-12-07 2021-07-19 Vertex Pharma 2-amino-n-(piperidin-1-yl-pyridin-3-yl) pyrazolo[1,5alpha]pyrimidin-3-carboxamid som hæmmer for atr kinase
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2970289A1 (fr) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Composés utiles en tant qu'inhibiteurs de la kinase atr
EP2970288A1 (fr) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Composés utiles en tant qu'inhibiteurs de la kinase atr
SI3077397T1 (sl) 2013-12-06 2020-02-28 Vertex Pharmaceuticals Inc. 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)pirazolo(1,5-A)pirimidin-3- karboksamidna spojina, koristna kot inhibitor kinaze ATR, njena priprava, različne trdne oblike in njeni radioaktivno označeni derivati
EP3087069B1 (fr) 2013-12-23 2019-01-30 Norgine B.V. Composés utiles en tant que modulateurs du ccr9
SG10201902206QA (en) 2014-06-05 2019-04-29 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
HUE044280T2 (hu) 2014-06-17 2019-10-28 Vertex Pharma Rosszindulatú daganatok kezelése Chk1- és ATR-gátlók kombinációjával
US10118930B2 (en) 2014-11-03 2018-11-06 Bayer Pharma Aktiengesellschaft Piperidinylpyrazolopyrimidinones and their use
WO2016073891A1 (fr) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Pyrrolo[1,2-a]pyrimidines substituées et leur utilisation dans le traitement de troubles médicaux
ES2958391T3 (es) 2014-11-06 2024-02-08 Bial R&D Invest S A Imidazo[1,5-a]pirimidinas sustituidas y su uso en el tratamiento de trastornos médicos
MX2017005940A (es) 2014-11-06 2018-01-11 Lysosomal Therapeutics Inc Pyrazolo [1, 5-a] pirimidinas sustituidas y su uso en el tratamiento de trastornos médicos.
KR102649887B1 (ko) 2014-11-16 2024-03-22 어레이 바이오파마 인크. (s)-n-(5-((r)-2-(2,5-디플루오로페닐)-피롤리딘-1-일)-피라졸로[1,5-a]피리미딘-3-일)-3-히드록시피롤리딘-1-카르복스아미드 히드로겐 술페이트의 결정질 형태
SI3233839T1 (sl) * 2014-12-19 2019-12-31 Janssen Pharmaceutica Nv Heterociklil vezani derivati imidazopiridazina kot inhibitorji PI3Kbeta
KR20180054657A (ko) 2015-09-30 2018-05-24 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제 및 atr 저해제의 병용물을 사용한 암 치료 방법
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX2018012163A (es) 2016-04-04 2019-07-08 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirr olidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina- 1-carboxamida.
JP7046827B2 (ja) 2016-04-06 2022-04-04 リソソーマル・セラピューティクス・インコーポレイテッド イミダゾ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
CA3020310A1 (fr) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Composes pyrrolo[1,2-a]pyrimidinyl carboxamide et leur utilisation dans le traitement de troubles medicaux
JP7038063B2 (ja) 2016-04-06 2022-03-17 リソソーマル・セラピューティクス・インコーポレイテッド ピラゾロ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
WO2017192931A1 (fr) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. Imidazo[1,2-a]pyridines substituées, imidazo[1,2-a]pyrazines substituées, composés apparentés et leur utilisation dans le traitement de troubles médicaux
SG11201809693SA (en) 2016-05-05 2018-11-29 Lysosomal Therapeutics Inc SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
JP7443057B2 (ja) 2016-05-18 2024-03-05 ロクソ オンコロジー， インコーポレイテッド （Ｓ）－Ｎ－（５－（（Ｒ）－２－（２，５－ジフルオロフェニル）ピロリジン－１－イル）－ピラゾロ［１，５－ａ］ピリミジン－３－イル）－３－ヒドロキシピロリジン－１－カルボキサミドの調製
US10611779B2 (en) 2016-09-19 2020-04-07 Bayer Cropscience Aktiengesellschaft Fused bicyclic heterocycle derivatives as pesticides
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CA3174507A1 (fr) * 2020-03-06 2021-09-10 Bayer Aktiengesellschaft Imidazotriazines agissant sur le cancer par inhibition de cdk12
EP4163282A1 (fr) * 2020-06-01 2023-04-12 Unimatec Co., Ltd. Composé pyrimidine à cycle condensé contenant du fluor et son procédé de production

Family Cites Families (3)

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Publication number Priority date Publication date Assignee Title
AU2003299651A1 (en) * 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
AU2004215481B2 (en) * 2003-02-28 2010-11-11 Teijin Pharma Limited Pyrazolo(1,5-A)pyrimidine derivatives
EP1856122A2 (fr) * 2005-03-02 2007-11-21 Basf Aktiengesellschaft 7-amino-azolopyrimidine 2-substituee, son procede de fabrication et son utilisation pour lutter contre les champignons nuisibles, et agents renfermant ce compose

Also Published As

Publication number Publication date
WO2009070567A1 (fr) 2009-06-04
EP2225247A1 (fr) 2010-09-08
JP2011504931A (ja) 2011-02-17
MX2010005950A (es) 2010-06-17
CN101970440A (zh) 2011-02-09

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