ECSP055561A - Procesos para la preparación de pirimidinas sustituidas y derivados de pirimidina como inhibidores de las proteínas quinasas - Google Patents

Procesos para la preparación de pirimidinas sustituidas y derivados de pirimidina como inhibidores de las proteínas quinasas

Info

Publication number
ECSP055561A
ECSP055561A EC2005005561A ECSP055561A ECSP055561A EC SP055561 A ECSP055561 A EC SP055561A EC 2005005561 A EC2005005561 A EC 2005005561A EC SP055561 A ECSP055561 A EC SP055561A EC SP055561 A ECSP055561 A EC SP055561A
Authority
EC
Ecuador
Prior art keywords
inhibitors
preparation
pyrimidins
pirimidine
derived
Prior art date
Application number
EC2005005561A
Other languages
English (en)
Inventor
Jean Damien Charrier
Francesca Mazzei
David Kay
Andrew Miller
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Publication of ECSP055561A publication Critical patent/ECSP055561A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P19/08—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
    • 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
    • A61P25/18—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
    • A61P25/28—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
    • 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
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención proporciona un método fácil para la preparación de pirimidinas tri y tetra sustituidas. El proceso es útil para preparar inhibidores de proteínas quinasas, especialmente quinasas Aurora. Estos inhibidores son útiles para el tratamiento o disminución de enfermedades o condiciones mediadas por quinasas Aurora
EC2005005561A 2002-06-20 2005-01-20 Procesos para la preparación de pirimidinas sustituidas y derivados de pirimidina como inhibidores de las proteínas quinasas ECSP055561A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39065802P 2002-06-20 2002-06-20
US41160902P 2002-09-18 2002-09-18

Publications (1)

Publication Number Publication Date
ECSP055561A true ECSP055561A (es) 2005-03-10

Family

ID=30003168

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2005005561A ECSP055561A (es) 2002-06-20 2005-01-20 Procesos para la preparación de pirimidinas sustituidas y derivados de pirimidina como inhibidores de las proteínas quinasas

Country Status (27)

Country Link
US (4) US20040049032A1 (es)
EP (4) EP1746093B1 (es)
JP (5) JP4237701B2 (es)
KR (2) KR101141959B1 (es)
CN (1) CN100484934C (es)
AR (1) AR040286A1 (es)
AT (2) ATE556068T1 (es)
AU (1) AU2003245568B2 (es)
BR (1) BR0312443A (es)
CA (1) CA2489824C (es)
CO (1) CO5680433A2 (es)
DE (1) DE60336092D1 (es)
EA (2) EA012869B1 (es)
EC (1) ECSP055561A (es)
ES (1) ES2386781T3 (es)
HK (3) HK1077057A1 (es)
HR (1) HRP20050064A2 (es)
IL (1) IL165849A0 (es)
IS (2) IS7606A (es)
MX (1) MXPA05000068A (es)
MY (1) MY141867A (es)
NO (2) NO331925B1 (es)
NZ (4) NZ537720A (es)
PL (1) PL374953A1 (es)
SG (1) SG170614A1 (es)
TW (2) TWI297684B (es)
WO (1) WO2004000833A1 (es)

Families Citing this family (135)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4105948B2 (ja) 2000-09-15 2008-06-25 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 プロテインキナーゼインヒビターとして有用なピラゾール化合物
US7473691B2 (en) * 2000-09-15 2009-01-06 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
KR100909665B1 (ko) * 2000-12-21 2009-07-29 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 약제학적 조성물
RU2004126671A (ru) * 2002-02-06 2005-04-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Гетероарилсоединения, полезные в качестве ингибиторов gsk-3
WO2003078427A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azolylaminoazines as inhibitors of protein kinases
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
NZ538426A (en) 2002-08-02 2007-05-31 Vertex Pharma Pyrazole compositions useful as inhibitors of glycogen synthase kinase-3 (GSK-3)
US7601718B2 (en) * 2003-02-06 2009-10-13 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
AU2004297235A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
EP1694686A1 (en) * 2003-12-19 2006-08-30 Takeda San Diego, Inc. Kinase inhibitors
EP1745034A1 (en) 2004-02-11 2007-01-24 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7456176B2 (en) 2004-04-08 2008-11-25 Targegen, Inc. Benzotriazine inhibitors of kinases
EP1763524A1 (en) * 2004-04-23 2007-03-21 Takeda San Diego, Inc. Indole derivatives and use thereof as kinase inhibitors
US7550598B2 (en) * 2004-08-18 2009-06-23 Takeda Pharmaceutical Company Limited Kinase inhibitors
MX2007002208A (es) 2004-08-25 2007-05-08 Targegen Inc Compuestos hetrociclicos y metodos de uso.
US7285569B2 (en) 2004-09-24 2007-10-23 Hoff Hoffmann-La Roche Inc. Tricycles, their manufacture and use as pharmaceutical agents
AR050948A1 (es) 2004-09-24 2006-12-06 Hoffmann La Roche Derivados de ftalazinona; su obtencion y su utilizacion en la fabricacion de medicamentos para el tratamiento del cancer.
US7713973B2 (en) * 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
CA2587427A1 (en) * 2004-11-17 2006-05-26 Miikana Therapeutics, Inc. Kinase inhibitors
ATE519759T1 (de) 2004-12-30 2011-08-15 Exelixis Inc Pyrimidinderivate als kinasemodulatoren und anwendungsverfahren
WO2006108489A1 (en) 2005-04-14 2006-10-19 F. Hoffmann-La Roche Ag Aminopyrazole derivatives, their manufacture and use as pharmaceutical agents
US8071768B2 (en) * 2005-06-10 2011-12-06 Janssen Pharmaceutica, N.V. Alkylquinoline and alkylquinazoline kinase modulators
US7825244B2 (en) * 2005-06-10 2010-11-02 Janssen Pharmaceutica Nv Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
US20060281788A1 (en) * 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
US20060281768A1 (en) * 2005-06-10 2006-12-14 Gaul Michael D Thienopyrimidine and thienopyridine kinase modulators
CA2616517A1 (en) * 2005-07-26 2007-02-01 Vertex Pharmaceuticals Incorporated Abl kinase inhibition
AU2006279376B2 (en) * 2005-08-18 2011-04-14 Vertex Pharmaceuticals Incoporated Pyrazine kinase inhibitors
ES2535854T3 (es) * 2005-09-30 2015-05-18 Miikana Therapeutics, Inc. Compuestos de pirazol sustituidos
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
WO2007048088A2 (en) 2005-10-18 2007-04-26 Janssen Pharmaceutica N.V. Method of inhibiting flt3 kinase
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
AU2013201630B2 (en) * 2005-11-03 2016-12-01 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
ES2533241T3 (es) 2005-11-03 2015-04-08 Vertex Pharmaceuticals Incorporated Aminopirimidinas útiles como inhibidores de cinasas
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
WO2007120339A1 (en) * 2005-12-19 2007-10-25 Genentech, Inc. Pyrimidine kinase inhibitors
KR101332975B1 (ko) 2006-01-23 2013-11-25 암젠 인크 오로라 키나제 조절제 및 사용 방법
US7560551B2 (en) 2006-01-23 2009-07-14 Amgen Inc. Aurora kinase modulators and method of use
EP1978964A4 (en) * 2006-01-24 2009-12-09 Merck & Co Inc JAK2 tyrosine kinase Inhibition
US7868177B2 (en) 2006-02-24 2011-01-11 Amgen Inc. Multi-cyclic compounds and method of use
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
KR101367645B1 (ko) 2006-04-20 2014-02-27 얀센 파마슈티카 엔.브이. Ｃ-ｆｍｓ 키나제의 저해제로서의 복소환식 화합물
US8859602B2 (en) 2006-04-20 2014-10-14 Janssen Pharmaceutica Nv Inhibitors of c-fms kinase
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
US7615627B2 (en) 2006-06-21 2009-11-10 Reliance Life Sciences Pvt. Ltd. RNA interference mediated inhibition of aurorakinase B and its combinations as anticancer therapy
EP2043651A2 (en) 2006-07-05 2009-04-08 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
GB0619343D0 (en) * 2006-09-30 2006-11-08 Vernalis R&D Ltd New chemical compounds
EP2223925A1 (en) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase inhibitors
SG175609A1 (en) 2006-10-09 2011-11-28 Takeda Pharmaceutical Kinase inhibitors
WO2008044045A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
US8236823B2 (en) 2006-10-27 2012-08-07 Amgen Inc. Multi-cyclic compounds and methods of use
DE602007004750D1 (de) * 2006-11-02 2010-03-25 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyridine und aminopyrimidine
JP2010513567A (ja) * 2006-12-19 2010-04-30 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 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
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
MX2009009592A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopiridinas utiles como inhibidores de proteinas cinasas.
NZ579485A (en) * 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
NZ579446A (en) * 2007-03-09 2012-02-24 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
AU2008228963A1 (en) * 2007-03-20 2008-09-25 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
US7776857B2 (en) 2007-04-05 2010-08-17 Amgen Inc. Aurora kinase modulators and method of use
JP2010523700A (ja) * 2007-04-13 2010-07-15 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 キナーゼインヒビターとして有用なアミノピリミジン
MX2009011810A (es) 2007-05-02 2010-01-14 Vertex Pharma Tiazoles y pirazoles utiles como inhibidores de cinasa.
CN101801959A (zh) * 2007-05-02 2010-08-11 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类化合物
AU2008247595A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
CN101687852A (zh) * 2007-05-24 2010-03-31 沃泰克斯药物股份有限公司 可用作激酶抑制剂的噻唑类和吡唑类化合物
US20090029992A1 (en) * 2007-06-11 2009-01-29 Agoston Gregory E Substituted pyrazole compounds
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
NZ584145A (en) 2007-09-14 2012-03-30 Ortho Mcneil Janssen Pharm 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h, 1'h-[1,4'] bipyridinyl-2'-ones
EP2205565B1 (en) 2007-09-14 2013-04-17 Janssen Pharmaceuticals, Inc. 1,3-disubstituted-4-phenyl-1 h-pyridin-2-ones
EA019085B1 (ru) 2007-09-14 2014-01-30 Янссен Фармасьютикалз, Инк. 1',3-двузамещенные 4-(арил-х-фенил)-1н-пиридин-2-оны
JO3240B1 (ar) * 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
MX2010005110A (es) 2007-11-14 2010-09-09 Ortho Mcneil Janssen Pharm Derivados de imidazo[1,2-a]piridina y su uso como moduladores alostericos positivos de los receptores de glutamato metabotropico 2.
CA2706075A1 (en) * 2007-11-20 2009-05-28 University Health Network Cancer diagnostic and therapeutic methods that target plk4/sak
WO2009073224A1 (en) * 2007-12-07 2009-06-11 Ambit Biosciences Corp. Methods of treating certain diseases using pyrimidine derivatives
WO2009086012A1 (en) * 2007-12-20 2009-07-09 Curis, Inc. Aurora inhibitors containing a zinc binding moiety
WO2009117157A1 (en) 2008-03-20 2009-09-24 Amgen Inc. Aurora kinase modulators and method of use
US9126935B2 (en) 2008-08-14 2015-09-08 Amgen Inc. Aurora kinase modulators and methods of use
ES2439291T3 (es) 2008-09-02 2014-01-22 Janssen Pharmaceuticals, Inc. Derivados de 3-azabiciclo[3.1.0]hexilo como moduladores de receptores de glutamato metabotrópicos
EP2323622A1 (en) * 2008-09-03 2011-05-25 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical formulations comprising the same
NZ621143A (en) * 2008-09-05 2016-08-26 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
US8697689B2 (en) 2008-10-16 2014-04-15 Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
TWI491605B (zh) 2008-11-24 2015-07-11 Boehringer Ingelheim Int 新穎化合物
MX2011005242A (es) 2008-11-28 2011-09-06 Ortho Mcneil Janssen Pharm Derivados de indol y benzoxazina como moduladores de los receptores de glutamato metabotropicos.
ES2468391T3 (es) 2008-12-22 2014-06-16 Millennium Pharmaceuticals, Inc. Combinación de inhibidores de cinasas Aurora y anticuerpos anti-CD20
MY161325A (en) 2009-05-12 2017-04-14 Janssen Pharmaceuticals Inc 1, 2, 4-triazolo[4,3-a]pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
CA2760259C (en) 2009-05-12 2018-05-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
IN2012DN02534A (es) 2009-09-16 2015-08-28 Avila Therapeutics Inc
AU2010339456A1 (en) 2009-12-30 2012-07-05 Celgene Avilomics Research, Inc. Ligand-directed covalent modification of protein
WO2012059932A1 (en) 2010-11-01 2012-05-10 Aurigene Discovery Technologies Limited 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors
WO2012060847A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
ES2536433T3 (es) 2010-11-08 2015-05-25 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
CN103298809B (zh) 2010-11-08 2016-08-31 杨森制药公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途
JP5852664B2 (ja) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド １，２，４−トリアゾロ［４，３−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体のポジティブアロステリックモジュレーターとしてのそれらの使用
US9382229B2 (en) * 2011-02-15 2016-07-05 The Johns Hopkins University Compounds and methods of use thereof for treating neurodegenerative disorders
CN104024246B (zh) * 2012-03-27 2016-03-02 广东东阳光药业有限公司 作为欧若拉激酶抑制剂的取代嘧啶衍生物
WO2013163190A1 (en) 2012-04-24 2013-10-31 Vertex Pharmaceutical Incorporated Dna-pk inhibitors
WO2013177367A2 (en) 2012-05-23 2013-11-28 The Johns Hopkins University Compounds and methods of use thereof for treating neurodegenerative disorders
AU2013271731A1 (en) * 2012-06-07 2014-12-18 Georgia State University Research Foundation, Inc. SecA inhibitors and methods of making and using thereof
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
ES2608628T3 (es) 2012-08-07 2017-04-12 Janssen Pharmaceutica Nv Procedimiento para la preparacion de derivados de ester heterociclicos
JP6407504B2 (ja) 2012-09-21 2018-10-17 アログ・ファーマシューティカルズ・インコーポレイテッドＡｒｏｇ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 恒常的に活性であるリン酸化型ｆｌｔ３キナーゼの阻害方法
CN104955459B (zh) 2012-11-05 2019-02-01 南特知识产权控股有限责任公司 取代的吲哚-5-酚衍生物及其治疗应用
CN103202843B (zh) * 2012-12-31 2015-04-29 刘强 一种嘧啶衍生物在制备预防和/或治疗和/或辅助治疗癌症的药物中的用途
BR112015016282A2 (pt) 2013-01-07 2017-07-11 Arog Pharmaceuticals Inc crenolanibe para tratamento de distúrbios proliferativos de flt3 mutado
US9440952B2 (en) 2013-03-04 2016-09-13 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2014134774A1 (en) 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2014134776A1 (en) 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2014134772A1 (en) * 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
LT2970218T (lt) 2013-03-12 2019-03-12 Vertex Pharmaceuticals Incorporated Dna-pk inhibitoriai
CA2906185A1 (en) * 2013-03-15 2014-09-18 Nantbioscience, Inc. Substituted indol-5-ol derivatives and their therapeutic applications
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
SG11201602962PA (en) 2013-10-17 2016-05-30 Vertex Pharma Co-crystals of (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as dna-pk inhibitors
US10463658B2 (en) 2013-10-25 2019-11-05 Videra Pharmaceuticals, Llc Method of inhibiting FLT3 kinase
US10335494B2 (en) 2013-12-06 2019-07-02 Millennium Pharmaceuticals, Inc. Combination of aurora kinase inhibitors and anti-CD30 antibodies
WO2015110435A1 (en) 2014-01-21 2015-07-30 Janssen Pharmaceutica Nv Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use
ME03518B (me) 2014-01-21 2020-04-20 Janssen Pharmaceutica Nv Kombinacije koje obuhvataju pozitivne alosterične modulatore ili ortosterične agoniste metabotropnog glutamatergičnog receptora podtipa 2 i njihova primjena
JP6434530B2 (ja) * 2014-10-30 2018-12-05 富士フイルム株式会社 有機アミン塩及びその製造方法、並びに、アゾ色素の製造方法
EP3283482B1 (en) * 2015-04-17 2022-04-06 Ludwig Institute for Cancer Research Ltd Plk4 inhibitors
EP3324976A4 (en) 2015-07-21 2019-03-27 Millennium Pharmaceuticals, Inc. ADMINISTRATION OF KINASE AURORA INHIBITOR AND CHEMOTHERAPEUTIC AGENTS
AU2017275657B2 (en) 2016-06-02 2021-08-19 Novartis Ag Potassium channel modulators
KR20190062485A (ko) 2016-09-27 2019-06-05 버텍스 파마슈티칼스 인코포레이티드 Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법
EP3359155A4 (en) 2016-11-02 2019-05-22 Arog Pharmaceuticals, Inc. CRENOLANIB FOR THE TREATMENT OF MUTATIONS ASSOCIATED WITH FLT3-MUTED PROLIFERATIVE DISEASES
RS62899B1 (sr) 2017-01-23 2022-03-31 Cadent Therapeutics Inc Modulatori kalijumovih kanala
CN108250191B (zh) * 2018-03-15 2020-10-20 兰州大学 一种3,5-二取代的2-氨基-吡嗪化合物及其制备工艺与应用
WO2019195658A1 (en) 2018-04-05 2019-10-10 Dana-Farber Cancer Institute, Inc. Sting levels as a biomarker for cancer immunotherapy
WO2020049208A1 (es) 2018-09-09 2020-03-12 Fundacio Privada Institut De Recerca De La Sida - Caixa Aurora cinasa como diana para tratar, prevenir o curar una infección por vih o sida
CA3116339A1 (en) 2018-10-22 2020-04-30 Cadent Therapeutics, Inc. Crystalline forms of potassium channel modulators
US20220305048A1 (en) 2019-08-26 2022-09-29 Dana-Farber Cancer Institute, Inc. Use of heparin to promote type 1 interferon signaling
US11969420B2 (en) 2020-10-30 2024-04-30 Arog Pharmaceuticals, Inc. Combination therapy of crenolanib and apoptosis pathway agents for the treatment of proliferative disorders
WO2023196959A1 (en) 2022-04-07 2023-10-12 Eli Lilly And Company Process for making a kras g12c inhibitor
WO2023196887A1 (en) 2022-04-08 2023-10-12 Eli Lilly And Company Method of treatment including kras g12c inhibitors and aurora a inhibitors
WO2024006424A1 (en) 2022-06-30 2024-01-04 Eli Lilly And Company Kras g12c inhibitor for treating cancer

Family Cites Families (83)

* 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
US3939183A (en) * 1973-10-05 1976-02-17 Chevron Research Company Purification of maleic anhydride
US3998951A (en) 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
GB1446126A (en) 1974-05-16 1976-08-18 Res Inst For Medicine Chemistr Photolytic preparation of diol mononitrates
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
DE2922436A1 (de) 1979-06-01 1980-12-18 Sueddeutsche Kalkstickstoff Verfahren zur gewinnung von harnstoffkoernern mit verbesserten eigenschaften
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102193L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
SE8102194L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
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
US4477450A (en) * 1983-03-03 1984-10-16 Riker Laboratories, Inc. Triazolo [4,3-c]pyrimidines substituted by nitrogen-containing heterocyclic rings
EP0136976A3 (de) 1983-08-23 1985-05-15 Ciba-Geigy Ag Verwendung von Phenylpyrimidinen als Pflanzenregulatoren
NO157836C (no) 1985-04-19 1988-05-25 Jacobsen As J Anordning ved asymmetrisk belysning.
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
US5597920A (en) 1992-04-30 1997-01-28 Neurogen Corporation Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes
JPH0665237A (ja) 1992-05-07 1994-03-08 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
HU212308B (en) * 1992-06-09 1996-05-28 Richter Gedeon Vegyeszet Process for producing novel pregnane steroids and pharmaceutical compositions containing the same
DE69434721T2 (de) 1993-10-01 2006-11-09 Novartis Ag Pharmacologisch wirksame pyrimidinderivate und verfahren zu deren herstellung
ES2219670T3 (es) 1994-11-10 2004-12-01 Millennium Pharmaceuticals, Inc. Utilizacion de compuestos de pirazola para el tratamiento de la glomerulonefritis, cancer, ateroesclerosis o restenosis.
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
US5935966A (en) 1995-09-01 1999-08-10 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
WO1997009325A1 (en) 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US6716575B2 (en) 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
DK0912559T3 (da) 1996-07-13 2003-03-10 Glaxo Group Ltd Kondenserede heterocykliske forbindelser som proteintyrosinkinaseinhibitorer
JPH10130150A (ja) 1996-09-05 1998-05-19 Dainippon Pharmaceut Co Ltd 酢酸アミド誘導体からなる医薬
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
WO1998014450A1 (en) 1996-10-02 1998-04-09 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
EP0932598A1 (en) 1996-10-11 1999-08-04 Warner-Lambert Company ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME
CA2306692C (en) 1997-10-10 2010-09-21 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
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
EA200000840A1 (ru) 1998-02-17 2001-02-26 Туларик, Инк. Антивирусные производные пиримидина
CA2323439A1 (en) 1998-03-16 1999-09-23 Cytovia, Inc. Dipeptide caspase inhibitors and the use thereof
BR9911612A (pt) 1998-06-02 2001-02-06 Osi Pharm Inc Composições de pirrolo[2,3d]pirimidina e seus usos
JP4533534B2 (ja) 1998-06-19 2010-09-01 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド グリコーゲンシンターゼキナーゼ３のインヒビター
WO2000011003A1 (en) 1998-08-21 2000-03-02 Du Pont 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
CN1161352C (zh) 1998-10-08 2004-08-11 阿斯特拉曾尼卡有限公司 喹唑啉衍生物
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
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
AU2735201A (en) * 1999-12-28 2001-07-09 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
NZ514583A (en) 2000-02-05 2004-05-28 Vertex Pharma Pyrazole compositions useful as inhibitors of ERK
HUP0301117A3 (en) 2000-02-17 2004-01-28 Amgen Inc Thousand Oaks Imidazole derivatives kinase inhibitors, their use, process for their preparation and pharmaceutical compositions containing them
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
KR100711042B1 (ko) * 2000-04-28 2007-04-24 다나베 세이야꾸 가부시키가이샤 환상 화합물
US6919338B2 (en) 2000-06-28 2005-07-19 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors of aurora-2 kinase
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
JP4105948B2 (ja) * 2000-09-15 2008-06-25 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 プロテインキナーゼインヒビターとして有用なピラゾール化合物
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
HUP0302991A3 (en) 2000-09-15 2009-10-28 Vertex Pharma Isoxazoles and their use as inhibitors of erk and pharmaceutical compositions containing the compounds
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6641579B1 (en) 2000-09-29 2003-11-04 Spectrasonics Imaging, Inc. Apparatus and method for ablating cardiac tissue
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
KR100909665B1 (ko) * 2000-12-21 2009-07-29 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 약제학적 조성물
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
JP4160401B2 (ja) 2001-03-29 2008-10-01 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 Ｃ−ｊｕｎｎ末端キナーゼ（ｊｎｋ）および他のタンパク質キナーゼのインヒビター
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
CA2446864C (en) 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
ATE432929T1 (de) 2001-06-15 2009-06-15 Vertex Pharma 5-(2-aminopyrimidin-4-yl)benzisoxazole als proteinkinasehemmer
ES2271283T3 (es) 2001-07-03 2007-04-16 Vertex Pharmaceuticals Incorporated Isoxazolil-pirimidinas como inhibidores de las proteinas quinasas src y lck.
US6569499B2 (en) 2001-10-02 2003-05-27 Xerox Corporation Apparatus and method for coating photoreceptor substrates
EP2198867A1 (en) 2001-12-07 2010-06-23 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as GSK-3 inhibitors
WO2003077921A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
AU2003225800A1 (en) 2002-03-15 2003-09-29 Hayley Binch Azolylaminoazine as inhibitors of protein kinases
WO2003078427A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azolylaminoazines as inhibitors of protein kinases
WO2003078423A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Compositions useful 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
EP1554269A1 (en) 2002-07-09 2005-07-20 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
NZ538426A (en) 2002-08-02 2007-05-31 Vertex Pharma Pyrazole compositions useful as inhibitors of glycogen synthase kinase-3 (GSK-3)
ES2535854T3 (es) 2005-09-30 2015-05-18 Miikana Therapeutics, Inc. Compuestos de pirazol sustituidos
JP2010513567A (ja) 2006-12-19 2010-04-30 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 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

Also Published As

Publication number Publication date
MXPA05000068A (es) 2005-04-11
JP2014111662A (ja) 2014-06-19
KR101067254B1 (ko) 2011-09-27
US8268829B2 (en) 2012-09-18
CN100484934C (zh) 2009-05-06
EA200801372A1 (ru) 2008-08-29
EA015990B1 (ru) 2012-01-30
PL374953A1 (en) 2005-11-14
IS7661A (is) 2005-01-21
MY141867A (en) 2010-07-16
KR101141959B1 (ko) 2012-05-04
EP2292614A1 (en) 2011-03-09
NO20110523L (no) 2005-03-21
SG170614A1 (en) 2011-05-30
EA012869B1 (ru) 2009-12-30
IS7606A (is) 2004-12-20
WO2004000833A1 (en) 2003-12-31
NO20050144D0 (no) 2005-01-11
US20060270660A1 (en) 2006-11-30
NZ537720A (en) 2007-01-26
DE60336092D1 (de) 2011-03-31
NZ549142A (en) 2008-04-30
HK1081178A1 (en) 2006-05-12
BR0312443A (pt) 2005-05-10
JP2006501176A (ja) 2006-01-12
TW200406210A (en) 2004-05-01
US20090221602A1 (en) 2009-09-03
EA200500053A1 (ru) 2005-08-25
EP1517905B1 (en) 2012-05-02
US7557106B2 (en) 2009-07-07
ATE498621T1 (de) 2011-03-15
JP4237701B2 (ja) 2009-03-11
CN1675199A (zh) 2005-09-28
EP1746093B1 (en) 2011-02-16
KR20110010794A (ko) 2011-02-07
HK1100081A1 (en) 2007-09-07
CA2489824A1 (en) 2003-12-31
CO5680433A2 (es) 2006-09-29
NZ576752A (en) 2010-11-26
NO20050144L (no) 2005-03-21
US20040049032A1 (en) 2004-03-11
HK1077057A1 (en) 2006-02-03
EP2277876A1 (en) 2011-01-26
AU2003245568A1 (en) 2004-01-06
ATE556068T1 (de) 2012-05-15
JP2010235626A (ja) 2010-10-21
EP1517905A1 (en) 2005-03-30
NZ562953A (en) 2009-06-26
ES2386781T3 (es) 2012-08-30
NO331925B1 (no) 2012-05-07
JP2010202673A (ja) 2010-09-16
AU2003245568B2 (en) 2009-12-17
JP2005320351A (ja) 2005-11-17
US20130066069A1 (en) 2013-03-14
EP1746093A1 (en) 2007-01-24
TWI297684B (en) 2008-06-11
US8779127B2 (en) 2014-07-15
IL165849A0 (en) 2006-01-15
HRP20050064A2 (en) 2006-07-31
TWI354554B (en) 2011-12-21
TW200736231A (en) 2007-10-01
JP4662823B2 (ja) 2011-03-30
AR040286A1 (es) 2005-03-23
KR20050009756A (ko) 2005-01-25
CA2489824C (en) 2011-05-03

Similar Documents

Publication Publication Date Title
ECSP055561A (es) Procesos para la preparación de pirimidinas sustituidas y derivados de pirimidina como inhibidores de las proteínas quinasas
UY27224A1 (es) Inhibidores de la rho-quinasa
JOP20210154B1 (ar) مثبطات kif18a
MX2021007104A (es) Inhibidores de kif18a.
EA200900779A1 (ru) Производные дигидропиридина, полезные как ингибиторы протеинкиназы
ECSP12008540A (es) PIRROL[2,3-b]PIRIDINAS Y PIRROL[2,3-b]PIRIMIDINAS HETEROARILO SUSTITUIDAS COMO INHIBIDORES DE QUINASAS JANUS
ES2354824T3 (es) Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas.
MX2022001181A (es) Inhibidores de kif18a.
ATE451376T1 (de) Zusammensetzungen, die sich als inhibitoren von proteinkinasen eignen
BR0318383A (pt) derivados de pirazoloisoquinolina como inibidores de cinase
ATE450530T1 (de) Zusammensetzungen zur verwendung als protein- kinase-inhibitoren
DE602004014117D1 (de) Thiazole zur verwendung als inhibitoren von protein-kinasen
BRPI0410117A (pt) composto, composição farmacêutica, método para o tratamento de uma doença ou condição mediada por jak3, e, processo para a preparação de um composto
ATE348828T1 (de) Beta-carbolin-derivate als ptp-inhibitoren
UY27225A1 (es) Inhibidores de la rho-quinasa
ECSP055640A (es) Composiciones de pirazol útiles como inhibidores de gsk-3
GT201000082A (es) Derivados de pirrolo [2,3-d] pirimidina como inhibidores de proteinas quinasas b
ATE419253T1 (de) Inhibitoren von thienopyridin- und furopyridinkinase
MX2008011258A (es) Derivados de quinazolina como inhibidores de fosfodiesterasa 10.
ATE389651T1 (de) Als inhibitoren von c-met geeignete pyrrolzusammensetzungen
BR112021026531A2 (pt) Composto, composição farmacêutica, e, método para prevenir ou tratar uma doença mediada pela tirosina cinase 2
CL2022001887A1 (es) Pirazolo-pirimidinas sustituidas y usos de las mismas
ATE367380T1 (de) Zur behandlung von zns-erkrankungen geeignete piperazinylchinolinderivate
DE60222286D1 (de) Verfahren zur erhöhung des testosteronspiegels
DE60323533D1 (de) Methode zur stimulierung von haarwuchs auf der basis von benzopyranen