JP4790265B2 - サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン - Google Patents

サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン Download PDF

Info

Publication number
JP4790265B2
JP4790265B2 JP2004537708A JP2004537708A JP4790265B2 JP 4790265 B2 JP4790265 B2 JP 4790265B2 JP 2004537708 A JP2004537708 A JP 2004537708A JP 2004537708 A JP2004537708 A JP 2004537708A JP 4790265 B2 JP4790265 B2 JP 4790265B2
Authority
JP
Japan
Prior art keywords
cancer
alkyl
group
compound
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.)
Expired - Fee Related
Application number
JP2004537708A
Other languages
English (en)
Japanese (ja)
Other versions
JP2006502184A (ja
JP2006502184A5 (US07544672-20090609-C00177.png
Inventor
ティモシー ジェイ． グジ，
カミル パルク，
マイケル ピー． ドワイヤー，
ロナルド ジェイ． ドール，
ビッヨール ムーピル ギリジャヴァラバーン，
カルメン エス． アルバレツ，
ティン−ヤウ チャン，
チャド ナットソン，
ヴィンセント マディソン，
シェリー オー． フィッシュマン，
ローレンス ダブリュー． ディラード，
ヴィン ディー． トラン，
ゼン ミン ヘー，
レイ アンソニー ジェームス，
ヘンスーン パーク，
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 Corp
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 Corp filed Critical Schering Corp
Publication of JP2006502184A publication Critical patent/JP2006502184A/ja
Publication of JP2006502184A5 publication Critical patent/JP2006502184A5/ja
Application granted granted Critical
Publication of JP4790265B2 publication Critical patent/JP4790265B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

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
    • 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
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • 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
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P7/06—Antianaemics
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • 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

Landscapes

  • 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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
JP2004537708A 2002-09-04 2003-09-03 サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン Expired - Fee Related JP4790265B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40802902P 2002-09-04 2002-09-04
US60/408,029 2002-09-04
PCT/US2003/027491 WO2004026229A2 (en) 2002-09-04 2003-09-03 Pyrazolo[1,5-a]pyrimidines compounds as cyclin dependent kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2010088212A Division JP2010180235A (ja) 2002-09-04 2010-04-06 サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン

Publications (3)

Publication Number Publication Date
JP2006502184A JP2006502184A (ja) 2006-01-19
JP2006502184A5 JP2006502184A5 (US07544672-20090609-C00177.png) 2006-09-21
JP4790265B2 true JP4790265B2 (ja) 2011-10-12

Family

ID=32030632

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2004537708A Expired - Fee Related JP4790265B2 (ja) 2002-09-04 2003-09-03 サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン
JP2010088212A Withdrawn JP2010180235A (ja) 2002-09-04 2010-04-06 サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2010088212A Withdrawn JP2010180235A (ja) 2002-09-04 2010-04-06 サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン

Country Status (19)

Country Link
US (2) US7067661B2 (US07544672-20090609-C00177.png)
EP (1) EP1534712B1 (US07544672-20090609-C00177.png)
JP (2) JP4790265B2 (US07544672-20090609-C00177.png)
KR (1) KR20050033659A (US07544672-20090609-C00177.png)
CN (1) CN1701073B (US07544672-20090609-C00177.png)
AR (1) AR041133A1 (US07544672-20090609-C00177.png)
AT (1) ATE362474T1 (US07544672-20090609-C00177.png)
AU (1) AU2003298571B2 (US07544672-20090609-C00177.png)
CA (1) CA2497544C (US07544672-20090609-C00177.png)
DE (1) DE60313872T2 (US07544672-20090609-C00177.png)
ES (1) ES2283868T3 (US07544672-20090609-C00177.png)
HK (1) HK1071572A1 (US07544672-20090609-C00177.png)
MX (1) MXPA05002572A (US07544672-20090609-C00177.png)
MY (2) MY145332A (US07544672-20090609-C00177.png)
NZ (1) NZ539161A (US07544672-20090609-C00177.png)
PE (1) PE20041000A1 (US07544672-20090609-C00177.png)
TW (1) TWI329645B (US07544672-20090609-C00177.png)
WO (1) WO2004026229A2 (US07544672-20090609-C00177.png)
ZA (1) ZA200501846B (US07544672-20090609-C00177.png)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1386922B1 (en) * 1996-12-03 2012-04-11 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereof, analogues and uses thereof
EP1388541A1 (en) * 2002-08-09 2004-02-11 Centre National De La Recherche Scientifique (Cnrs) Pyrrolopyrazines as kinase inhibitors
WO2004018478A2 (en) 2002-08-23 2004-03-04 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
ATE362474T1 (de) * 2002-09-04 2007-06-15 Schering Corp Pyrazolo(1,5-a)pyrimidine als hemmstoffe cyclin- abhängiger kinasen
US7601724B2 (en) * 2002-09-04 2009-10-13 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7205308B2 (en) * 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
CA2516824A1 (en) * 2003-02-28 2004-09-10 Teijin Pharma Limited Pyrazolo[1,5-a]pyrimidine derivatives
WO2004087707A1 (en) * 2003-03-31 2004-10-14 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
EP1671962A1 (en) * 2003-10-10 2006-06-21 Ono Pharmaceutical Co., Ltd. Novel fused heterocyclic compound and use thereof
WO2005112936A1 (en) * 2004-05-14 2005-12-01 The Regents Of The University Of Michigan Compositions and methods relating to protein kinase inhibitors
WO2006027346A2 (en) * 2004-09-06 2006-03-16 Altana Pharma Ag Novel pyrazolopyrimidines
FR2876582B1 (fr) * 2004-10-15 2007-01-05 Centre Nat Rech Scient Cnrse Utilisation de derives de pyrrolo-pyrazines pour la fabrication de medicaments pour le traitement de la mucoviscidose et de maladies liees a un defaut d'adressage des proteines dans les cellules
ATE433454T1 (de) * 2004-12-21 2009-06-15 Schering Corp Pyrazoloä1,5-aüpyrimidine als antagonisten des adenosin-a2a-rezeptors
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
ATE478852T1 (de) 2005-09-09 2010-09-15 Schering Corp Neue 4-cyano-, 4-amino-, und 4- aminomethylderivative von pyrazoloä1,5- aüpyridinen, pyrazoloä1,5-cüpyrimidinen und 2h- indazolverbindungen und 5-cyano-, 5-amino- und 5- aminomethylderivative von imidazoä1,2-aüpyridinen,und imidazoä1,5-aüpyrazinverbindungen als inhibitoren der cyclinabhänggen kinase
CA2625153A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
WO2007118844A1 (de) * 2006-04-13 2007-10-25 Basf Se Substituierte pyrazolopyrimidine, verfahren zu ihrer herstellung und ihre verwendung zur bekämpfung von schadpilzen sowie sie enthaltende mittel
EP2377531A2 (en) 2006-05-09 2011-10-19 Braincells, Inc. Neurogenesis by modulating angiotensin
EP2027127A1 (en) * 2006-05-22 2009-02-25 Shering Corporation Pyrazolo [1, 5-a]pyrimidines as cdk inhibitors
US8008307B2 (en) 2006-08-08 2011-08-30 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
SG177128A1 (en) * 2006-12-05 2012-01-30 Arena Pharm Inc Processes for preparing (r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine and intermediates thereof
CN102056925A (zh) * 2008-04-07 2011-05-11 Irm责任有限公司 作为激酶抑制剂的化合物和组合物
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
US8993535B2 (en) 2009-09-04 2015-03-31 Merck Sharp & Dohme Corp. Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors
CN102762208A (zh) * 2009-12-04 2012-10-31 赛林药物股份有限公司 作为ck2抑制剂的吡唑嘧啶和相关杂环
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
US10953012B2 (en) 2011-04-26 2021-03-23 Bioenergenix Llc Heterocyclic compounds for the inhibition of pask
EP2723746A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
AU2012340200B2 (en) 2011-11-17 2017-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-Terminal Kinase (JNK)
EP3536692B1 (en) 2012-02-17 2021-04-07 Millennium Pharmaceuticals, Inc. Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
CN102633803A (zh) * 2012-05-03 2012-08-15 盛世泰科生物医药技术(苏州)有限公司 一种5,7-二氯吡唑并[1,5-a]嘧啶的合成方法
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014066743A1 (en) 2012-10-25 2014-05-01 Bioenergenix Heterocyclic compounds for the inhibition of pask
WO2014066795A1 (en) 2012-10-25 2014-05-01 Bioenergenix Heterocyclic compounds for the inhibition of pask
ES2946360T3 (es) 2012-12-07 2023-07-17 Vertex Pharma Pirazolo[1,5-a]pirimidinas útiles como inhibidores de ATR quinasa para el tratamiento de enfermedades de cáncer
BR112015022545A2 (pt) 2013-03-13 2017-07-18 Constellation Pharmaceuticals Inc compostos de pirazolo e os usos disso
US8969360B2 (en) 2013-03-15 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
WO2014143241A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN105492429A (zh) 2013-07-02 2016-04-13 米伦纽姆医药公司 Sumo活化酶的杂芳基抑制剂
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
JP6491202B2 (ja) 2013-10-18 2019-03-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤
RU2687276C2 (ru) 2013-12-06 2019-05-13 Вертекс Фармасьютикалз Инкорпорейтед Соединения, пригодные для использования в качестве ингибиторов atr киназы
WO2015097121A1 (en) 2013-12-23 2015-07-02 Norgine B.V. Compounds useful as ccr9 modulators
CN106061975B (zh) * 2014-01-22 2019-09-24 库洛维公司 作为抗病毒化合物的吡唑并[1,5-a]嘧啶
LT3152212T (lt) 2014-06-05 2020-05-11 Vertex Pharmaceuticals Inc. Radioaktyviai žymėti 2-amino-6-fluor-n-[5-fluor-piridin-il]- pirazolo[1,5-a]pirimidin-3-karboksamido junginio dariniai, naudingi kaip atr kinazės inhibitoriai, minėto junginio gamybos būdas ir jo skirtingos kietos formos
SG11201610500WA (en) 2014-06-17 2017-01-27 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
JP6603712B2 (ja) 2014-07-01 2019-11-06 ミレニアム ファーマシューティカルズ， インコーポレイテッド Ｓｕｍｏ活性化酵素の阻害薬として有用なヘテロアリール化合物
CN105294655B (zh) * 2014-07-26 2019-03-15 广东东阳光药业有限公司 Cdk类小分子抑制剂的化合物及其用途
EP3236959A4 (en) 2014-12-23 2018-04-25 Dana Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2978518C (en) * 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CA3000684A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
AU2016357720A1 (en) 2015-11-18 2018-07-05 Genzyme Corporation Biomarker of polycystic kidney disease and uses thereof
TWI703149B (zh) * 2017-11-16 2020-09-01 美商美國禮來大藥廠 用於抑制cdk7之化合物
EP3849981B1 (en) 2018-09-10 2023-02-01 Eli Lilly and Company Pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives useful in the treatment of psoriasis and systemic lupus erythematosus
CN112996790B (zh) 2018-10-30 2023-11-03 克洛诺斯生物公司 用于调节cdk9活性的化合物、组合物和方法
AR121251A1 (es) 2020-02-12 2022-05-04 Lilly Co Eli Compuestos de 7-(metilamino)pirazolo[1,5-a]pirimidina-3-carboxamida
CN116396298A (zh) * 2023-06-06 2023-07-07 四川维亚本苑生物科技有限公司 CDK Ligand-1的中间体XII及CDK Ligand-1的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH03204877A (ja) * 1989-10-25 1991-09-06 Otsuka Pharmaceut Factory Inc ピラゾロ［１，５―ａ］ピリミジン誘導体
JPH0570353A (ja) * 1991-04-22 1993-03-23 Otsuka Pharmaceut Factory Inc 抗炎症剤

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US626096A (en) * 1899-05-30 Dust-pan
JPS4116288Y1 (US07544672-20090609-C00177.png) 1964-11-07 1966-07-28
JPS6157587A (ja) 1984-08-29 1986-03-24 Shionogi & Co Ltd 縮合複素環誘導体および抗潰瘍剤
JP2811020B2 (ja) 1990-04-17 1998-10-15 日本特殊陶業株式会社 セラミックスと鋼の接合体及びその製造方法
US5571813A (en) * 1993-06-10 1996-11-05 Beiersdorf-Lilly Gmbh Fused pyrimidine compounds and their use as pharmaceuticals
EP0628559B1 (en) 1993-06-10 2002-04-03 Beiersdorf-Lilly GmbH Pyrimidine compounds and their use as pharmaceuticals
CN1046730C (zh) 1994-06-21 1999-11-24 株式会社大塚制药工场 吡唑并[1,5-a]嘧啶衍生物
US5919815A (en) * 1996-05-22 1999-07-06 Neuromedica, Inc. Taxane compounds and compositions
US6191131B1 (en) 1997-07-23 2001-02-20 Dupont Pharmaceuticals Company Azolo triazines and pyrimidines
US6040321A (en) * 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6262096B1 (en) * 1997-11-12 2001-07-17 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6413974B1 (en) * 1998-02-26 2002-07-02 Aventis Pharmaceuticals Inc. 6,9,-disubstituted 2-[trans-(4-aminocyclohexyl) amino] purines
US6190131B1 (en) * 1999-08-31 2001-02-20 General Electric Co. Non-integral balanced coverplate and coverplate centering slot for a turbine
FR2805160B1 (fr) 2000-02-23 2002-04-05 Oreal Compositions pour la teinture d'oxydation des fibres keratiniques comprenant un n(2-hydroxybenzene)-carbramate ou un n-(2-hydroxybenzene)-uree et une pyrazolopyrimidine, et procedes de teinture
US7067520B2 (en) 2000-11-17 2006-06-27 Ishihara Sangyo Kaisha, Ltd. Preventive or therapeutic medicines for diabetes containing fused-heterocyclic compounds or their salts
FR2817469B1 (fr) * 2000-12-04 2003-04-18 Oreal Composition de coloration, procede d'obtention et utilisation pour la coloration de fibres keratiniques
CA2432417A1 (fr) 2000-12-20 2002-06-27 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R .A.S.) Inhibiteurs de kinases dependantes des cylines (cdk) et de la glycogene synthase kinase-3 (gsk-3)
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
MXPA04010441A (es) 2002-04-23 2005-02-14 Shionogi & Co Derivado de pirazolo[1,5-a]pirimidina e inhibidor de nad(p)h oxidasa que contiene el mismo.
DE10223917A1 (de) 2002-05-29 2003-12-11 Bayer Cropscience Ag Pyrazolopyrimidine
CN1310918C (zh) * 2002-09-04 2007-04-18 先灵公司 作为细胞周期蛋白依赖激酶抑制剂的吡唑并嘧啶
ATE362474T1 (de) * 2002-09-04 2007-06-15 Schering Corp Pyrazolo(1,5-a)pyrimidine als hemmstoffe cyclin- abhängiger kinasen

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH03204877A (ja) * 1989-10-25 1991-09-06 Otsuka Pharmaceut Factory Inc ピラゾロ［１，５―ａ］ピリミジン誘導体
JPH0570353A (ja) * 1991-04-22 1993-03-23 Otsuka Pharmaceut Factory Inc 抗炎症剤

Also Published As

Publication number Publication date
JP2010180235A (ja) 2010-08-19
MY137843A (en) 2009-03-31
WO2004026229A2 (en) 2004-04-01
EP1534712B1 (en) 2007-05-16
TWI329645B (en) 2010-09-01
PE20041000A1 (es) 2004-12-29
EP1534712A2 (en) 2005-06-01
MY145332A (en) 2012-01-31
TW200413376A (en) 2004-08-01
AR041133A1 (es) 2005-05-04
DE60313872D1 (de) 2007-06-28
AU2003298571B2 (en) 2006-10-19
JP2006502184A (ja) 2006-01-19
WO2004026229A3 (en) 2004-06-17
US7514442B2 (en) 2009-04-07
CA2497544C (en) 2010-11-02
ATE362474T1 (de) 2007-06-15
ES2283868T3 (es) 2007-11-01
HK1071572A1 (en) 2005-07-22
US7067661B2 (en) 2006-06-27
ZA200501846B (en) 2005-09-12
KR20050033659A (ko) 2005-04-12
MXPA05002572A (es) 2005-09-08
US20040106624A1 (en) 2004-06-03
CA2497544A1 (en) 2004-04-01
CN1701073A (zh) 2005-11-23
AU2003298571A1 (en) 2004-04-08
DE60313872T2 (de) 2008-01-17
CN1701073B (zh) 2011-06-22
US20060178371A1 (en) 2006-08-10
NZ539161A (en) 2006-05-26

Similar Documents

Publication Publication Date Title
JP4790265B2 (ja) サイクリン依存性キナーゼインヒビターとしての新規ピラゾロピリミジン
JP4700344B2 (ja) サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン
JP4845379B2 (ja) サイクリン依存性キナーゼインヒビターとしてのイミダゾピリジン
JP4571969B2 (ja) キナーゼインヒビターとしてのピラゾロトリアジン
JP4799864B2 (ja) サイクリン依存性キナーゼインヒビターとしてのイミダゾピラジン
US7205308B2 (en) Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
JP2006502184A5 (US07544672-20090609-C00177.png)
US20040102451A1 (en) Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors
JP2011074088A (ja) サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン
JP2006501260A5 (US07544672-20090609-C00177.png)
JP2009511477A (ja) サイクリン依存性キナーゼインヒビターとしての、新規なピラゾロピリミジン
JP2006503838A (ja) サイクリン依存性キナーゼインヒビターとしての新規イミダゾピラジン
JP2009507843A (ja) アザ縮合サイクリン依存性キナーゼ阻害剤
JP2010505838A (ja) サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン
JP4845380B2 (ja) サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン

Legal Events

Date Code Title Description
A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20060802

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20060802

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100125

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100406

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20100406

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100518

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100706

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100730

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100831

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20101210

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110309

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20110524

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110531

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20110620

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110720

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140729

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313115

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R360 Written notification for declining of transfer of rights

Free format text: JAPANESE INTERMEDIATE CODE: R360

R371 Transfer withdrawn

Free format text: JAPANESE INTERMEDIATE CODE: R371

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

LAPS Cancellation because of no payment of annual fees