CA2499874A1 - Novel imidazopyrazines as cyclin dependent kinase inhibitors - Google Patents

Novel imidazopyrazines as cyclin dependent kinase inhibitors Download PDF

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Publication number
CA2499874A1
CA2499874A1 CA002499874A CA2499874A CA2499874A1 CA 2499874 A1 CA2499874 A1 CA 2499874A1 CA 002499874 A CA002499874 A CA 002499874A CA 2499874 A CA2499874 A CA 2499874A CA 2499874 A1 CA2499874 A1 CA 2499874A1
Authority
CA
Canada
Prior art keywords
nr5r6
compound
alkyl
group
aryl
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
CA002499874A
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English (en)
French (fr)
Inventor
Kamil Paruch
Timothy J. Guzi
Michael P. Dwyer
Ronald J. Doll
Viyyoor M. Girijavallabhan
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 LLC
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Individual
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 Individual filed Critical Individual
Publication of CA2499874A1 publication Critical patent/CA2499874A1/en
Abandoned legal-status Critical Current

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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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA002499874A 2002-09-23 2003-09-19 Novel imidazopyrazines as cyclin dependent kinase inhibitors Abandoned CA2499874A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41290602P 2002-09-23 2002-09-23
US60/412,906 2002-09-23
PCT/US2003/029456 WO2004026310A1 (en) 2002-09-23 2003-09-19 Novel imidazopyrazines as cyclin dependent kinase inhibitors

Publications (1)

Publication Number Publication Date
CA2499874A1 true CA2499874A1 (en) 2004-04-01

Family

ID=32030939

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002499874A Abandoned CA2499874A1 (en) 2002-09-23 2003-09-19 Novel imidazopyrazines as cyclin dependent kinase inhibitors

Country Status (13)

Country Link
US (2) US7186740B2 (enExample)
EP (1) EP1542693A1 (enExample)
JP (1) JP2006503838A (enExample)
KR (1) KR20060010709A (enExample)
CN (1) CN1694706A (enExample)
AR (1) AR041346A1 (enExample)
AU (1) AU2003275031B2 (enExample)
CA (1) CA2499874A1 (enExample)
MX (1) MXPA05003119A (enExample)
NZ (1) NZ538686A (enExample)
TW (1) TW200412967A (enExample)
WO (1) WO2004026310A1 (enExample)
ZA (1) ZA200502380B (enExample)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4579351B2 (ja) 1996-12-03 2010-11-10 スローン−ケッタリング インスティトュート フォア キャンサー リサーチ エポチロンの合成とその中間体及びその類似物並びにその使用
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
IL164703A0 (en) 2002-04-19 2005-12-18 Cellular Genomics Inc ImidazoÄ1,2-AÜpyrazin-8-ylamines method of making and method of use thereof
US6921769B2 (en) 2002-08-23 2005-07-26 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US7649006B2 (en) * 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
CA2496477C (en) 2002-08-23 2012-10-16 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
AU2003270489A1 (en) 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
TW200413378A (en) * 2002-09-23 2004-08-01 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors
US7576085B2 (en) * 2002-09-23 2009-08-18 Schering Corporation Imidazopyrazines as cyclin dependent kinase inhibitors
WO2004072080A1 (en) 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of hsp90 complex activity
US20060183746A1 (en) * 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
WO2005005429A1 (en) 2003-06-30 2005-01-20 Cellular Genomics, Inc. Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds
WO2005019220A2 (en) * 2003-08-11 2005-03-03 Cellular Genomics Inc. Substituted imidazo[1,2-a]pyrazines as modulators of kinase activity
WO2005085252A1 (en) * 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
ES2393741T3 (es) * 2005-01-14 2012-12-27 Gilead Connecticut, Inc. Ureas 1,3-diarilsustituidas como moduladores de la actividad quinasa
US7777040B2 (en) 2005-05-03 2010-08-17 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
JP2009507032A (ja) 2005-09-02 2009-02-19 アボット・ラボラトリーズ 新規なイミダゾ系複素環
CN101300233A (zh) * 2005-09-09 2008-11-05 先灵公司 氮杂稠合的细胞周期蛋白依赖性激酶抑制剂
EP1940395A2 (en) * 2005-09-16 2008-07-09 Schering Corporation Pharmaceutical compositions and methods using temozolomide and a protein kinase inhibitor
EP1945216A1 (en) * 2005-11-10 2008-07-23 Schering Corporation Methods for inhibiting protein kinases
WO2007058942A2 (en) * 2005-11-10 2007-05-24 Schering Corporation Imidazopyrazines as protein kinase inhibitors
US20090018142A9 (en) * 2006-05-02 2009-01-15 Zhengping Zhuang Use of phosphatases to treat tumors overexpressing N-CoR
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
MX2009008347A (es) 2007-02-06 2009-10-19 Lixte Biotechnology Holdings I Oxabicicloheptanos y oxabicicloheptenos, su preparacion y uso.
EP2185173A4 (en) * 2007-08-03 2011-01-12 Lixte Biotechnology Inc USE OF PHOSPHATASES FOR THE TREATMENT OF NEUROBLASTOMES AND MEDULLOGASTOMES
MX2010003417A (es) * 2007-10-01 2010-09-10 Lixte Biotechnology Inc Inhibidores de histona desacetilasa.
NZ587039A (en) 2008-02-13 2013-01-25 Gilead Connecticut Inc 6-aryl-imidazo[1, 2-a]pyrazine derivatives, method of making, and method of use thereof
US8227473B2 (en) * 2008-08-01 2012-07-24 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes, their preparation and use
EP2309853A4 (en) * 2008-08-01 2012-04-25 Lixte Biotechnology Inc METHOD FOR CELL MITITULATING BY INHIBITION OF SERIN / THREONINE PHOSPHATASE
WO2010147612A1 (en) 2009-06-18 2010-12-23 Lixte Biotechnology, Inc. Methods of modulating cell regulation by inhibiting p53
AU2009277086B2 (en) * 2008-08-01 2015-12-10 Lixte Biotechnology, Inc. Neuroprotective agents for the prevention and treatment of neurodegenerative diseases
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
CN104744476B (zh) 2008-12-08 2017-04-12 吉利德康涅狄格公司 咪唑并吡嗪syk抑制剂
SG171993A1 (en) 2008-12-08 2011-07-28 Gilead Connecticut Inc Imidazopyrazine syk inhibitors
EP2473041B1 (en) 2009-09-04 2018-03-07 Merck Sharp & Dohme Corp. Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors
NZ599597A (en) 2009-10-30 2013-05-31 Janssen Pharmaceutica Nv IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
NZ602362A (en) 2010-03-11 2014-11-28 Gilead Connecticut Inc Imidazopyridines syk inhibitors
ES2556458T3 (es) * 2010-12-17 2016-01-18 Bayer Intellectual Property Gmbh 6-Imidazopirazinas sustituidas para uso como inhibidores de Mps-1 y TKK en el tratamiento de trastornos hiperproliferativos
WO2012080236A1 (en) * 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
ES2575092T3 (es) 2011-06-27 2016-06-24 Janssen Pharmaceutica, N.V. Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxalina
RU2657540C2 (ru) 2012-06-26 2018-06-14 Янссен Фармацевтика Нв Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств
KR102171706B1 (ko) 2012-07-09 2020-10-30 얀센 파마슈티카 엔.브이. 포스포디에스테라아제 10 효소의 억제제
BR112015025852A2 (pt) 2013-04-09 2017-07-25 Lixte Biotechnology Inc as formulações de oxabicicloheptanos e oxabicicloheptenos
EA201791873A1 (ru) 2013-07-30 2018-09-28 Джилид Коннектикут, Инк. Полиморф ингибиторов syk
EP3027171B1 (en) 2013-07-30 2020-03-25 Gilead Connecticut, Inc. Formulation of syk inhibitors
KR20180002888A (ko) 2013-12-04 2018-01-08 길리애드 사이언시즈, 인코포레이티드 암을 치료하는 방법
UY35898A (es) 2013-12-23 2015-07-31 Gilead Sciences Inc ?compuestos inhibidores de syk y composiciones que los comprenden?.
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
CN106687139A (zh) 2014-07-14 2017-05-17 吉利德科学公司 用于治疗癌症的组合
EP3377908B1 (en) 2015-11-18 2020-08-05 Genzyme Corporation Biomarker of polycystic kidney disease and uses thereof
US12168008B2 (en) 2016-12-08 2024-12-17 Lixte Biotechnology, Inc. Oxabicycloheptanes for modulation of immune response
CN111051311A (zh) 2017-08-25 2020-04-21 吉利德科学公司 Syk抑制剂的多晶型物
KR20210131372A (ko) 2019-02-22 2021-11-02 크로노스 바이오, 인코포레이티드 Syk 억제제로서의 축합된 피라진의 고체 형태
WO2022061155A1 (en) * 2020-09-17 2022-03-24 The Translational Genomics Research Institute Imidazopyridazine and imidazopyrazine compounds as inhibitors of cdk7
CN114042065B (zh) * 2021-11-26 2024-03-15 长沙拜特生物科技研究所有限公司 一种复方甲苯咪唑透皮溶液剂及其制备方法
WO2025199359A1 (en) * 2024-03-21 2025-09-25 The Translational Genomics Research Institute Methods of modulating cdk7 and flt3 using fused bicyclic compounds

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4797764A (en) * 1986-01-27 1989-01-10 Minnesota Mining And Manufacturing Company Recording disk with low total indicated runout
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
EP0778277B1 (en) 1995-12-08 2003-06-25 Pfizer Inc. Substituted heterocyclic derivatives as CRF antagonists
CA2419626A1 (en) 2000-07-14 2002-01-24 Rajagopal Bakthavatachalam Imidazo¬1,2-a|pyrazines for the treatment of neurological disorders
PL365170A1 (en) 2000-07-26 2004-12-27 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl] carboxamide inhibitors of cyclin dependent kinases
US20040102455A1 (en) * 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
IL164703A0 (en) 2002-04-19 2005-12-18 Cellular Genomics Inc ImidazoÄ1,2-AÜpyrazin-8-ylamines method of making and method of use thereof
TW200413378A (en) * 2002-09-23 2004-08-01 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors

Also Published As

Publication number Publication date
AU2003275031B2 (en) 2006-08-17
AU2003275031A1 (en) 2004-04-08
AR041346A1 (es) 2005-05-11
MXPA05003119A (es) 2005-06-22
EP1542693A1 (en) 2005-06-22
TW200412967A (en) 2004-08-01
KR20060010709A (ko) 2006-02-02
WO2004026310A8 (en) 2005-06-30
US7186740B2 (en) 2007-03-06
NZ538686A (en) 2008-01-31
ZA200502380B (en) 2005-09-27
WO2004026310A1 (en) 2004-04-01
US20070155751A1 (en) 2007-07-05
JP2006503838A (ja) 2006-02-02
CN1694706A (zh) 2005-11-09
US20040072835A1 (en) 2004-04-15

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued