JP5393489B2 - 蛋白キナーゼの阻害剤として有用なアミノピリミジン - Google Patents

蛋白キナーゼの阻害剤として有用なアミノピリミジン Download PDF

Info

Publication number
JP5393489B2
JP5393489B2 JP2009552930A JP2009552930A JP5393489B2 JP 5393489 B2 JP5393489 B2 JP 5393489B2 JP 2009552930 A JP2009552930 A JP 2009552930A JP 2009552930 A JP2009552930 A JP 2009552930A JP 5393489 B2 JP5393489 B2 JP 5393489B2
Authority
JP
Japan
Prior art keywords
treating
disease
composition
pharmaceutically acceptable
compound
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
JP2009552930A
Other languages
English (en)
Japanese (ja)
Other versions
JP2010520889A5 (enExample
JP2010520889A (ja
Inventor
アルバート ピアース，
ジョン カム，
ジョン コート，
ホワイ ガオ，
グレゴリー ヘンケル，
マイケル リュー，
ティモシー ニューバーガー，
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2010520889A publication Critical patent/JP2010520889A/ja
Publication of JP2010520889A5 publication Critical patent/JP2010520889A5/ja
Application granted granted Critical
Publication of JP5393489B2 publication Critical patent/JP5393489B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
JP2009552930A 2007-03-09 2008-03-10 蛋白キナーゼの阻害剤として有用なアミノピリミジン Expired - Fee Related JP5393489B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US90592907P 2007-03-09 2007-03-09
US60/905,929 2007-03-09
US95302407P 2007-07-31 2007-07-31
US60/953,024 2007-07-31
PCT/US2008/056433 WO2008112651A2 (en) 2007-03-09 2008-03-10 Aminopyrimidines useful as inhibitors of protein kinases

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2013165986A Division JP2013227348A (ja) 2007-03-09 2013-08-09 蛋白キナーゼの阻害剤として有用なアミノピリミジン

Publications (3)

Publication Number Publication Date
JP2010520889A JP2010520889A (ja) 2010-06-17
JP2010520889A5 JP2010520889A5 (enExample) 2011-04-21
JP5393489B2 true JP5393489B2 (ja) 2014-01-22

Family

ID=39745397

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2009552930A Expired - Fee Related JP5393489B2 (ja) 2007-03-09 2008-03-10 蛋白キナーゼの阻害剤として有用なアミノピリミジン
JP2013165986A Withdrawn JP2013227348A (ja) 2007-03-09 2013-08-09 蛋白キナーゼの阻害剤として有用なアミノピリミジン

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2013165986A Withdrawn JP2013227348A (ja) 2007-03-09 2013-08-09 蛋白キナーゼの阻害剤として有用なアミノピリミジン

Country Status (15)

Country Link
US (1) US8518953B2 (enExample)
EP (1) EP2137183B1 (enExample)
JP (2) JP5393489B2 (enExample)
KR (1) KR20090120510A (enExample)
CN (1) CN101668760B (enExample)
AT (1) ATE526328T1 (enExample)
AU (1) AU2008226466B2 (enExample)
CA (1) CA2680029A1 (enExample)
ES (1) ES2374335T3 (enExample)
IL (1) IL200793A0 (enExample)
MX (1) MX2009009591A (enExample)
NZ (1) NZ579485A (enExample)
RU (1) RU2009137390A (enExample)
WO (1) WO2008112651A2 (enExample)
ZA (1) ZA200906264B (enExample)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6638926B2 (en) 2000-09-15 2003-10-28 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7601718B2 (en) 2003-02-06 2009-10-13 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
WO2007056163A2 (en) 2005-11-03 2007-05-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
DE602007004750D1 (de) 2006-11-02 2010-03-25 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyridine und aminopyrimidine
WO2008077086A1 (en) 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
NZ577798A (en) 2006-12-21 2012-04-27 Vertex Pharma 5-cyano-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
MX2009009590A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
NZ579485A (en) 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
NZ580343A (en) 2007-04-13 2012-03-30 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
CA2694381A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
JP5389785B2 (ja) 2007-05-02 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用なチアゾールおよびピラゾール
AU2008282156B2 (en) * 2007-07-31 2014-07-17 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1H-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
KR20100108390A (ko) 2007-12-19 2010-10-06 버텍스 파마슈티칼스 인코포레이티드 ＪＡＫ２ 억제제로서 유용한 피라졸로［１，５－ａ］피리미딘
WO2009145814A2 (en) * 2008-03-10 2009-12-03 Vertex Pharmaceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
GEP20207129B (en) 2009-06-17 2020-07-10 Vertex Pharma Inhibitors of influenza viruses replication
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
CN103492381A (zh) 2010-12-16 2014-01-01 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
SMT201800608T1 (it) 2012-04-24 2019-01-11 Vertex Pharma Inibitori di dna-pk
AU2014244555B2 (en) 2013-03-12 2018-06-28 Vertex Pharmaceuticals Incorporated DNA-PK inhibitors
HUE041877T2 (hu) 2013-10-17 2019-06-28 Vertex Pharma (S)-N-Metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propán-2-il)kinolin-4-karboxamid kokristályai és deuterált származékai DNS-PK inhibitorokként
HRP20191525T1 (hr) 2013-11-13 2019-11-29 Vertex Pharma Inhibitori replikacije virusa influence
EP3421468B1 (en) 2013-11-13 2020-11-04 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
WO2016183120A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
JP6704416B2 (ja) 2015-05-13 2020-06-03 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ インフルエンザウイルスの複製の阻害剤を調製する方法
US11110108B2 (en) 2016-09-27 2021-09-07 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors

Family Cites Families (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133081A (en) 1964-05-12 J-aminoindazole derivatives
US3935183A (en) 1970-01-26 1976-01-27 Imperial Chemical Industries Limited Indazole-azo phenyl compounds
BE754242A (fr) 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3998951A (en) 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
DE2458965C3 (de) 1974-12-13 1979-10-11 Bayer Ag, 5090 Leverkusen 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel
MA18829A1 (fr) 1979-05-18 1980-12-31 Ciba Geigy Ag Derives de la pyrimidine,procedes pour leur preparation,compositions pharmaceutiques contenant ces composes et leur utilisation therapeutique
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102194L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
SE8102193L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
JPS58124773A (ja) 1982-01-20 1983-07-25 Mitsui Toatsu Chem Inc ５−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤
DE3725638A1 (de) 1987-08-03 1989-02-16 Bayer Ag Neue aryloxy (bzw. thio)aminopyrimidine
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
JPH10509708A (ja) 1994-11-10 1998-09-22 コア セラピューティクス，インコーポレイティド プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物
IL117659A (en) 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
US6716575B2 (en) 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
US6267952B1 (en) 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
JP2000026421A (ja) 1998-01-29 2000-01-25 Kumiai Chem Ind Co Ltd ジアリ―ルスルフィド誘導体及び有害生物防除剤
KR20010041015A (ko) 1998-02-17 2001-05-15 윌리엄 제이. 리플린 항바이러스성 피리미딘 유도체
ATE274510T1 (de) 1998-06-19 2004-09-15 Chiron Corp Glycogen synthase kinase 3 inhibitoren
CA2339188A1 (en) 1998-08-21 2000-03-02 Dupont Pharmaceuticals Company Isoxazolo¬4,5-d|pyrimidines as crf antagonists
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
WO2000058360A2 (en) 1999-03-29 2000-10-05 Uutech Limited Analogs of gastric inhibitory peptide and their use for treatment of diabetes
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
IL145757A (en) 2000-02-05 2007-12-03 Vertex Pharma History of pyrazole and pharmaceutical preparations containing them
WO2001060816A1 (en) 2000-02-17 2001-08-23 Amgen Inc. Kinase inhibitors
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
MXPA02011974A (es) 2000-06-28 2004-09-06 Astrazeneca Ab Derivados de quinazolina sustituidos y su uso como inhibidores.
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
NZ525016A (en) 2000-09-15 2004-10-29 Vertex Pharma Isoxazoles and their use as inhibitors of ERK
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6638926B2 (en) * 2000-09-15 2003-10-28 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
DE10061863A1 (de) 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
US6716851B2 (en) 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
WO2002050079A1 (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)
CA2432799C (en) 2000-12-21 2008-08-19 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
CA2441733A1 (en) 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
EP1389206B1 (en) 2001-04-13 2006-09-13 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
EP1383771A1 (en) 2001-04-20 2004-01-28 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives as inhibitors of gsk-3
US6884804B2 (en) 2001-05-16 2005-04-26 Vertex Pharmaceuticals Incorporated Inhibitors of Src and other protein kinases
US6825190B2 (en) 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
US6689778B2 (en) 2001-07-03 2004-02-10 Vertex Pharmaceuticals Incorporated Inhibitors of Src and Lck protein kinases
US6698980B2 (en) 2001-07-30 2004-03-02 Stewart Mining Products Inc. Rock stabilizing apparatus and method
EP1474147B1 (en) 2001-12-07 2010-05-05 Vertex Pharmaceuticals Incorporated Pyrimidine-based compounds useful as gsk-3 inhibitors
AU2003225800A1 (en) 2002-03-15 2003-09-29 Hayley Binch Azolylaminoazine as inhibitors of protein kinases
ES2289279T3 (es) 2002-03-15 2008-02-01 Vertex Pharmaceuticals Incorporated Composiciones utiles como inhibidores de proteinquinasas.
US7863282B2 (en) 2003-03-14 2011-01-04 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
ATE468336T1 (de) 2002-03-15 2010-06-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
EP1485100B1 (en) 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azinylaminoazoles as inhibitors of protein kinases
US20030207873A1 (en) 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
US7304061B2 (en) 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
JP4570955B2 (ja) 2002-07-09 2010-10-27 バーテクス ファーマスーティカルズ インコーポレイテッド プロテインキナーゼ阻害活性を持つイミダゾール類
PT1532145E (pt) 2002-08-02 2007-01-31 Vertex Pharma Composiçoes de pirazole úteis como inibidores de gsk-3
AU2003286711A1 (en) 2002-10-25 2004-05-13 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
DE602004022187D1 (de) 2003-10-17 2009-09-03 Astrazeneca Ab 4-(pyrazol-3-ylamino)pyrimidinderivate zur verwendung bei der behandlung von krebs
JP2009504771A (ja) 2005-08-18 2009-02-05 バーテックス ファーマシューティカルズ インコーポレイテッド ピラジンキナーゼ阻害剤
WO2007023382A2 (en) 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
CA2622352C (en) 2005-09-30 2014-05-27 Miikana Therapeutics, Inc. Substituted pyrazole compounds
WO2007056163A2 (en) 2005-11-03 2007-05-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
CN101360740A (zh) 2005-11-16 2009-02-04 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶
DE602007004750D1 (de) 2006-11-02 2010-03-25 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyridine und aminopyrimidine
WO2008077086A1 (en) 2006-12-19 2008-06-26 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
NZ579485A (en) 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
MX2009009590A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
JP2010522194A (ja) 2007-03-20 2010-07-01 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害薬として有用なアミノピリミジン
EP2148931A2 (en) 2007-04-17 2010-02-03 Vertex Pharmaceuticals Incorporated Drug discovery methods for aurora kinase inhibitors
JP5389785B2 (ja) 2007-05-02 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用なチアゾールおよびピラゾール
CA2688584A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
CA2694381A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008257044A1 (en) 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors

Also Published As

Publication number Publication date
WO2008112651A3 (en) 2008-11-27
ES2374335T3 (es) 2012-02-15
US8518953B2 (en) 2013-08-27
EP2137183B1 (en) 2011-09-28
EP2137183A2 (en) 2009-12-30
WO2008112651A2 (en) 2008-09-18
US20110020377A1 (en) 2011-01-27
KR20090120510A (ko) 2009-11-24
IL200793A0 (en) 2010-05-17
CN101668760A (zh) 2010-03-10
HK1138572A1 (en) 2010-08-27
JP2013227348A (ja) 2013-11-07
AU2008226466B2 (en) 2013-06-13
NZ579485A (en) 2012-02-24
CN101668760B (zh) 2013-07-24
JP2010520889A (ja) 2010-06-17
ZA200906264B (en) 2010-11-24
MX2009009591A (es) 2009-11-10
ATE526328T1 (de) 2011-10-15
AU2008226466A1 (en) 2008-09-18
CA2680029A1 (en) 2008-09-18
RU2009137390A (ru) 2011-04-20

Similar Documents

Publication Publication Date Title
JP5393489B2 (ja) 蛋白キナーゼの阻害剤として有用なアミノピリミジン
JP5520057B2 (ja) 蛋白キナーゼの阻害剤として有用なアミノピリミジン
JP2011513483A (ja) タンパク質キナーゼの阻害剤として有用なピリミジンおよびピリジン
JP2010520887A (ja) 蛋白キナーゼの阻害剤として有用なアミノピリジン
KR102212923B1 (ko) 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
JP5406039B2 (ja) タンパク質キナーゼ阻害剤として有用な５−シアノ−４−（ピロロ［２，３ｂ］ピリジン−３−イル）−ピリミジン誘導体
RU2627712C2 (ru) Соединение как ингибитор передачи сигналов wnt, его композиции и применение
JP5406725B2 (ja) タンパク質キナーゼ阻害剤として有用な化合物
JP2010513567A (ja) プロテインキナーゼの阻害剤として有用なアミノピリミジン
JP6039683B2 (ja) ピラジンキナーゼ阻害剤
CA3093138C (en) Heteroaryl compounds as kinase inhibitor
JP2014141529A (ja) キナーゼのインヒビターとして有用なチアゾールおよびピラゾール
WO2014040555A1 (zh) 作为酪氨酸激酶抑制剂的含氮杂芳环衍生物
JP2007513172A (ja) 複素環式プロテインキナーゼインヒビターおよびその使用
JP2014510154A (ja) 神経変性疾患の治療方法及び治療用組成物
JP2013014632A (ja) ピラジンキナーゼ阻害剤
JP2010509231A (ja) プロテインキナーゼの阻害剤として有用なアミノピリジンおよびアミノピリミジン
CN104470363A (zh) 1,2,4-三嗪-6-甲酰胺激酶抑制剂
JP2010522210A (ja) Ｊａｋ阻害薬として有用なｎ−複素環式化合物
JP2008535874A (ja) 受容体チロシンキナーゼの活性阻害剤としてのプリン誘導体
AU2018359413A1 (en) Kinase inhibitors for the treatment of central and peripheral nervous system disorders
HK1138572B (en) Aminopyrimidines useful as inhibitors of protein kinases

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110222

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20110222

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120209

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130411

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130710

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130718

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130809

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: 20130919

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20131015

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees