AR040286A1 - Proceso para la preparacion de pirimidinas sustituidas - Google Patents

Proceso para la preparacion de pirimidinas sustituidas

Info

Publication number
AR040286A1
AR040286A1 ARP030102187A ARP030102187A AR040286A1 AR 040286 A1 AR040286 A1 AR 040286A1 AR P030102187 A ARP030102187 A AR P030102187A AR P030102187 A ARP030102187 A AR P030102187A AR 040286 A1 AR040286 A1 AR 040286A1
Authority
AR
Argentina
Prior art keywords
independently selected
monocyclic
saturated
substituted
optionally
Prior art date
Application number
ARP030102187A
Other languages
English (en)
Inventor
Jean-Damien Charrier
Francesca Mazzei
David Kay
William 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 AR040286A1 publication Critical patent/AR040286A1/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)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un proceso sencillo para la preparación de pirimidinas tri y tetra-sustituidas. El proceso es útil para preparar inhibidores de cinasas de proteínas, especialmente, cinasa Aurora. Estos inhibidores son de utilidad para el tratamiento o disminución de la gravedad de condiciones o enfermedades reguladas por Aurora. Compuestos seleccionados a partir de los que poseen la fórmula (1), composición farmacéutica que contiene dichos compuestos y un método de inhibición de Aurora-1. Reivindicación 1: Un método de preparación de un compuesto de fórmula (1) en donde: Q y T son, cada uno en forma independiente, seleccionados entre O, S, o N (R); cada R se selecciona en forma independiente entre H o un grupo alifático C1-6 opcionalmente sustituido, en donde; dos R ligados al mismo átomo de N en forma opcional se toman junto con el N para formar un anillo opcionalmente sustituido, de 3 a 7 miembros, monocíclico, o de 8 a 10 miembros bicíclico, saturado, parcialmente insaturado o completamente insaturado, que tiene 0-3 heteroátomos, además del N ligado al mismo, seleccionados de manera independiente entre N, O, o S; Rx es U-R5; R5 se selecciona entre halógeno, NO2, CN, R, o Ar; cada U se selecciona de manera independiente entre un enlace de valencia o una cadena alquilideno C1-4, en donde; hasta dos unidades metileno de U son en forma opcional e independiente reemplazados con -O-, -S-, -SO-, -SO2-, -N(R)SO2-, -SO2N(R)-, -N(R)-, -C(O)-, -CO2-, -N(R)C(O)-, -N(R)C(O)O-, -N(R)CON(R)-, -N(R)SO2N(R)-, -N(R)N(R)-, -C(O)N(R)-, -OC(O)N(R)-, C(R)=NN(R)-, o -C(R)=N-O-; cada Ar se selecciona en forma independiente entre un anillo opcionalmente sustituido seleccionado entre un anillo de 3 a 7 miembros monocíclico, o uno de 8 a 10 miembros bicíclico, saturado, parcialmente insaturado, o completamente insaturado, que tiene 0 a 4 heteroátomos seleccionados en forma independiente entre N, O, o S; Ry es -N(R1)2, -OR1, o -SR1; cada R1 se selecciona de manera independiente entre R o un anillo 3 a 8 miembros monocíclico, uno de 8 a 10 miembros bicíclico, o uno de 10 a 12 miembros tricíclico, saturado, parcialmente insaturado, o completamente insaturado, que tiene 0 a 4 heteroátomos seleccionados en forma independiente entre N, O ó S; y en donde: cada R1 está opcional o independientemente sustituido con hasta 4 sustituyentes que se seleccionan en forma independiente entre R2; cada R2 se selecciona en forma independiente entre -R3, -OR3, -SR3, -CN, -NO2, oxo, halógeno, -N(R3)2, -C(O)R3, -OC(O)R3, -CO2R3, -SO2R3, -SO2N(R3)2, -N(R3)SO2R3, -C(O)NR(R3), -C(O)N(R3)2, -OC(O)NR(R3), -OC(O)N(R3)2, -NR3C(O)R3, -NR3C(O)N(R3)2, o -NR3CO2(R3); cada R3 se selecciona de manera independiente entre R o Ar; Rz1 se selecciona entre un grupo alifático C1-6, o un anillo 3 a 8 miembros monocíclico, uno de 8 a 10 miembros bicíclico, o uno de 10 a 12 miembros tricíclico, saturado, parcialmente insaturado, o completamente insaturado, que tiene 0 a 4 heteroátomos seleccionados en forma independiente entre N, O ó S; en donde; Rz1 está sustituido con 0 a 4 grupos R2 seleccionados en forma independiente; Rz2 es un grupo alifático C1-6, o un anillo 3 a 8 miembros monocíclico, o uno de 8 a 10 miembros bicíclico, saturado, parcialmente insaturado, o completamente insaturado, que tiene 0 a 4 heteroátomos seleccionados en forma independiente entre N, O ó S; en donde; Rz2 está sustituido con 0 a 4 sustituyentes seleccionados en forma independiente entre oxo o U-R5; dicho proceso comprende la etapa de combinar un compuesto de fórmula (2) y un compuesto de fórmula Ry-H en un medio adecuado; en donde dicho medio adecuado comprende; i) un solvente apropiado y ii) en forma opcional, una base apropiada; y L3 es un grupo de salida adecuado.
ARP030102187A 2002-06-20 2003-06-19 Proceso para la preparacion de pirimidinas sustituidas AR040286A1 (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
AR040286A1 true AR040286A1 (es) 2005-03-23

Family

ID=30003168

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030102187A AR040286A1 (es) 2002-06-20 2003-06-19 Proceso para la preparacion de pirimidinas sustituidas

Country Status (27)

Country Link
US (4) US20040049032A1 (es)
EP (4) EP2277876A1 (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) EA015990B1 (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) NZ576752A (es)
PL (1) PL374953A1 (es)
SG (1) SG170614A1 (es)
TW (2) TWI297684B (es)
WO (1) WO2004000833A1 (es)

Families Citing this family (134)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2422367C (en) 2000-09-15 2010-05-18 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
KR100947185B1 (ko) * 2000-12-21 2010-03-15 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 조성물
SG159380A1 (en) * 2002-02-06 2010-03-30 Vertex Pharma Heteroaryl compounds useful as inhibitors of gsk-3
EP1485380B1 (en) 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
PL374967A1 (en) 2002-08-02 2005-11-14 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
WO2004072029A2 (en) * 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
AU2004297235A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
WO2005061519A1 (en) * 2003-12-19 2005-07-07 Takeda San Diego, Inc. Kinase inhibitors
CA2556239A1 (en) * 2004-02-11 2005-08-25 Amgen Inc. Vanilloid receptor ligands and their use in treatments
KR20070011458A (ko) 2004-04-08 2007-01-24 탈자진 인코포레이티드 키나제의 벤조트리아진 억제제
JP2007533753A (ja) * 2004-04-23 2007-11-22 タケダ サン ディエゴ インコーポレイテッド インドール誘導体及びキナーゼ阻害剤としてのその使用
EP1778669A2 (en) * 2004-08-18 2007-05-02 Takeda San Diego, Inc. Kinase inhibitors
NZ588896A (en) 2004-08-25 2012-05-25 Targegen Inc Heterocyclic compounds and methods of use
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.
DE602005023333D1 (de) * 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
CA2587427A1 (en) 2004-11-17 2006-05-26 Miikana Therapeutics, Inc. Kinase inhibitors
WO2006074057A2 (en) 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
EP1879894A1 (en) 2005-04-14 2008-01-23 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
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
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
AU2006272609A1 (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
KR101487027B1 (ko) * 2005-09-30 2015-01-28 미카나 테라퓨틱스, 인크. 치환된 피라졸 화합물
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
NZ595182A (en) 2005-10-18 2012-12-21 Janssen Pharmaceutica Nv Pharmaceutical uses of 4-cyano-1H-imidazole-2-carboxylic acid { 2-cyclohex-1-enyl-4-[1-(2-dimethylamino-acetyl)-piperidin-4-yl]-phenyl} -amide
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007056221A2 (en) * 2005-11-03 2007-05-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2013201630B2 (en) * 2005-11-03 2016-12-01 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2006315334B2 (en) * 2005-11-16 2011-05-19 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
WO2007120339A1 (en) * 2005-12-19 2007-10-25 Genentech, Inc. Pyrimidine kinase inhibitors
US7560551B2 (en) 2006-01-23 2009-07-14 Amgen Inc. Aurora kinase modulators and method of use
EP1984353B1 (en) 2006-01-23 2015-12-30 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
TWI417095B (zh) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc １，４-二取代之３-氰基-吡啶酮衍生物及其作為ｍＧｌｕＲ２-受體之正向異位性調節劑之用途
EP2021335B1 (en) 2006-04-20 2011-05-25 Janssen Pharmaceutica N.V. Heterocyclic compounds as inhibitors of c-fms kinase
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
UA93085C2 (en) 2006-04-20 2011-01-10 Янссен Фармацевтика Н.В. Inhibitors of c-fms 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
WO2008005538A2 (en) 2006-07-05 2008-01-10 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
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
WO2008057280A1 (en) 2006-10-27 2008-05-15 Amgen Inc. Multi-cyclic compounds and methods of use
NZ576750A (en) * 2006-11-02 2012-01-12 Vertex Pharma Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
DE602007007985D1 (de) * 2006-12-19 2010-09-02 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyrimidine
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
EP2137183B1 (en) * 2007-03-09 2011-09-28 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
CN101663295B (zh) * 2007-03-09 2014-11-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的氨基嘧啶类化合物
JP2010520887A (ja) * 2007-03-09 2010-06-17 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 蛋白キナーゼの阻害剤として有用なアミノピリジン
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
EP2137177B1 (en) 2007-04-05 2014-05-07 Amgen, Inc Aurora kinase modulators and method of use
CA2683785A1 (en) * 2007-04-13 2008-10-23 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247594A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
MX2009011810A (es) 2007-05-02 2010-01-14 Vertex Pharma Tiazoles y pirazoles utiles como inhibidores de cinasa.
MX2009011811A (es) * 2007-05-02 2010-01-14 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasa.
EP2164842A2 (en) * 2007-05-24 2010-03-24 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
CA2683152A1 (en) * 2007-06-11 2008-12-18 Miikana Therapeutics, Inc. Substituted pyrazole compounds
CN101790532B (zh) * 2007-07-31 2013-11-20 沃泰克斯药物股份有限公司 5-氟-1H-吡唑并[3，4-b]吡啶-3-胺及其衍生物的制备方法
JP5366269B2 (ja) 2007-09-14 2013-12-11 ジャンセン ファーマシューティカルズ， インコーポレイテッド． １，３−二置換４−（アリル−ｘ−フェニル）−１ｈ−ピリジン−２−オン
US9114138B2 (en) 2007-09-14 2015-08-25 Janssen Pharmaceuticals, Inc. 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′] bipyridinyl-2′-ones
CN101801930B (zh) 2007-09-14 2013-01-30 奥梅-杨森制药有限公司 1,3-二取代的-4-苯基-1h-吡啶-2-酮
JO3240B1 (ar) * 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
US8785486B2 (en) 2007-11-14 2014-07-22 Janssen Pharmaceuticals, Inc. Imidazo[1,2-A]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
WO2009065232A1 (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
EP2288611B1 (en) 2008-03-20 2013-05-15 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
WO2010025890A1 (en) 2008-09-02 2010-03-11 Ortho-Mcneil-Janssen Pharmaceuticals, Inc 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
CN102215816A (zh) * 2008-09-03 2011-10-12 沃泰克斯药物股份有限公司 共晶和包含所述共晶的药物制剂
RU2014150660A (ru) * 2008-09-05 2015-07-20 Селджен Авиломикс Рисерч, Инк. Алгоритм разработки необратимо действующих ингибиторов
WO2010043396A1 (en) 2008-10-16 2010-04-22 Ortho-Mcneil-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
WO2010060589A1 (en) 2008-11-28 2010-06-03 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
WO2010074724A1 (en) 2008-12-22 2010-07-01 Millennium Pharmaceuticals, Inc. Combination of aurora kinase inhibitors and anti-cd20 antibodies
MX2011011962A (es) 2009-05-12 2012-02-28 Janssen Pharmaceuticals Inc Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostericos positivos de receptores de glutamato metabotropico (mglur2).
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
SG10201402250TA (en) 2009-05-12 2014-07-30 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
NZ620174A (en) 2009-09-16 2016-08-26 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
WO2011082285A1 (en) 2009-12-30 2011-07-07 Avila Therapeutics, 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
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
ES2552879T3 (es) 2010-11-08 2015-12-02 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
WO2012062750A1 (en) 2010-11-08 2012-05-18 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP2643320B1 (en) 2010-11-08 2015-03-04 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
WO2012112674A2 (en) * 2011-02-15 2012-08-23 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
NZ700928A (en) 2012-04-24 2017-06-30 Vertex Pharma 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
US9957247B2 (en) * 2012-06-07 2018-05-01 Georgia State University Research Foundation, Inc. SecA inhibitors and methods of making and using thereof
JP6359537B2 (ja) 2012-08-07 2018-07-18 ヤンセン ファーマシューティカ エヌ．ベー． 複素環エステル誘導体の調製プロセス
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
KR101738063B1 (ko) 2012-09-21 2017-05-19 아로그 파마슈티칼스, 인코퍼레이티드 구조적으로 활성인 인산화된 ｆｌｔ３ 키나제의 억제 방법
CA2890018A1 (en) 2012-11-05 2014-05-08 Nant Holdings Ip, Llc Substituted indol-5-ol derivatives and their therapeutical applications
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
WO2014134774A1 (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
EP2964221B1 (en) 2013-03-04 2017-12-06 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
LT3527563T (lt) 2013-03-12 2021-12-10 Vertex Pharmaceuticals Incorporated Dnr-pk inhibitoriai
US9550760B2 (en) * 2013-03-15 2017-01-24 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
PT3424920T (pt) 2013-10-17 2020-07-07 Vertex Pharma Co-cristais de (s)-n-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolina-4-carboxamida e derivados deuterados dos mesmos como inibidores de adn-pk
US10463658B2 (en) 2013-10-25 2019-11-05 Videra Pharmaceuticals, Llc Method of inhibiting FLT3 kinase
WO2015085289A1 (en) 2013-12-06 2015-06-11 Millennium Pharmaceuticals, Inc. Combination of aurora kinase inhibitors and anti-cd30 antibodies
HUE053734T2 (hu) 2014-01-21 2021-07-28 Janssen Pharmaceutica Nv 2-es altípusú metabotróp glutamáterg receptor pozitív allosztérikus modulátorait tartalmazó kombinációk és alkalmazásuk
EA201891617A3 (ru) 2014-01-21 2019-04-30 Янссен Фармацевтика Нв Комбинации, содержащие положительные аллостерические модуляторы или ортостерические агонисты метаботропного глутаматергического рецептора 2 подтипа, и их применение
CN107148413B (zh) * 2014-10-30 2020-07-14 富士胶片株式会社 有机胺盐及其制造方法、以及偶氮色素的制造方法
US10752612B2 (en) 2015-04-17 2020-08-25 Ludwig Institute For Cancer Research Ltd PLK4 inhibitors
US10774064B2 (en) 2016-06-02 2020-09-15 Cadent Therapeutics, Inc. 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
US11078541B2 (en) 2016-11-02 2021-08-03 Arog Pharmaceuticals, Inc. Crenolanib for treating FLT3 mutated proliferative disorders associated mutations
SI3571193T1 (sl) 2017-01-23 2022-04-29 Cadent Therapeutics, Inc. Modulatorji kalijevega kanalčka
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
US11874276B2 (en) 2018-04-05 2024-01-16 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
JP2022508945A (ja) 2018-10-22 2022-01-19 カデント セラピューティクス，インコーポレーテッド カリウムチャネルモジュレーターの結晶形態
WO2021041532A1 (en) 2019-08-26 2021-03-04 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.
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
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
ATE325113T1 (de) 1993-10-01 2006-06-15 Novartis Pharma Gmbh Pharmacologisch wirksame pyrimidinderivate und verfahren zu deren herstellung
CA2203517A1 (en) 1994-11-10 1996-05-23 Alan M. Laibelman Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
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
ID19609A (id) 1996-07-13 1998-07-23 Glaxo Group Ltd Senyawa-senyawa heterosiklik
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
DE69732780T2 (de) 1996-10-02 2006-04-06 Novartis Ag Pyrimiderivate und verfahren zu ihrer herstellung
EP0932598A1 (en) 1996-10-11 1999-08-04 Warner-Lambert Company ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME
EA200000409A1 (ru) 1997-10-10 2000-10-30 Сайтовиэ, Инк. Соединение, фармацевтическая композиция, способ ингибирования гибели клетки в одной клетке или ткани, способ лечения или снижения клеточной смерти, способ лечения или профилактики поликистозного заболевания почек или анемии/эритропоэза у животных, способ защиты органа или ткани млекопитающего от гибели клеток, способ снижения или профилактики гибели клеток в органе или ткани донора после их трансплантации, способ снижения или предотвращения гибели спермы или яйцеклеток
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
IL137922A0 (en) 1998-02-17 2001-10-31 Tularik Inc Anti-viral pyrimidine derivatives
CN1297354A (zh) 1998-03-16 2001-05-30 西托维亚公司 二肽卡斯帕酶抑制剂及其用途
DZ2805A1 (fr) 1998-06-02 2005-01-30 Cadus Pharmaceutical Corp Composition à pyrroloÄ2,,3dÜ pyrimidine et leurs usages.
US6489344B1 (en) 1998-06-19 2002-12-03 Chiron Corporation Inhibitors of glycogen synthase kinase 3
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
JP2002527436A (ja) 1998-10-08 2002-08-27 アストラゼネカ アクチボラグ キナゾリン誘導体
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
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
JP2003519143A (ja) * 1999-12-28 2003-06-17 ファーマコピーア，インコーポレーティッド ピリミジン及びトリアジン系キナーゼ阻害剤
SK14082001A3 (sk) 2000-02-05 2002-03-05 Vertex Pharmaceuticals Incorporated Deriváty pyrazolu ako inhibítory ERK a farmaceutická kompozícia, ktorá ich obsahuje
CN1429222A (zh) 2000-02-17 2003-07-09 安姆根有限公司 激酶抑制剂
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
AU4114201A (en) * 2000-04-28 2001-11-12 Tanabe Seiyaku Co Cyclic compounds
US6919338B2 (en) 2000-06-28 2005-07-19 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors of aurora-2 kinase
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE335737T1 (de) 2000-09-15 2006-09-15 Vertex Pharma Isoxazole und ihre verwendung als erk-inhibitoren
CA2422367C (en) 2000-09-15 2010-05-18 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
US7473691B2 (en) 2000-09-15 2009-01-06 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
KR100947185B1 (ko) 2000-12-21 2010-03-15 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 조성물
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
ES2292753T4 (es) 2001-03-29 2009-02-16 Vertex Pharmaceuticals Incorporated Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas.
MXPA03009378A (es) 2001-04-13 2004-01-29 Vertex Pharma Inhibidores de cinasas c-jun n-terminales (jnk) y otras proteinas cinasas.
EP1383771A1 (en) 2001-04-20 2004-01-28 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives as inhibitors of gsk-3
AU2002308748A1 (en) 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as 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
EP1417205B1 (en) 2001-07-03 2006-08-23 Vertex Pharmaceuticals Incorporated Isoxazolyl-pyrimidines as inhibitors of src and lck protein kinases
US6569499B2 (en) 2001-10-02 2003-05-27 Xerox Corporation Apparatus and method for coating photoreceptor substrates
JP2005516005A (ja) 2001-12-07 2005-06-02 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 Ｇｓｋ−３阻害剤として有用なピリミジンベースの化合物
DE60314603T2 (de) 2002-03-15 2008-02-28 Vertex Pharmaceuticals Inc., Cambridge Zusammensetzungen brauchbar als protein-kinase-inhibitoren
EP1485380B1 (en) 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
EP1485381B8 (en) 2002-03-15 2010-05-12 Vertex Pharmaceuticals Incorporated Azolylaminoazine as inhibitors of protein kinases
ATE466580T1 (de) 2002-03-15 2010-05-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
US20030207873A1 (en) 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
AU2003237121A1 (en) 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as 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
PL374967A1 (en) 2002-08-02 2005-11-14 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
KR101487027B1 (ko) 2005-09-30 2015-01-28 미카나 테라퓨틱스, 인크. 치환된 피라졸 화합물
DE602007007985D1 (de) 2006-12-19 2010-09-02 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyrimidine

Also Published As

Publication number Publication date
AU2003245568A1 (en) 2004-01-06
ATE556068T1 (de) 2012-05-15
JP2005320351A (ja) 2005-11-17
ECSP055561A (es) 2005-03-10
IL165849A0 (en) 2006-01-15
JP4662823B2 (ja) 2011-03-30
JP2006501176A (ja) 2006-01-12
HK1081178A1 (en) 2006-05-12
EP1746093A1 (en) 2007-01-24
US8779127B2 (en) 2014-07-15
ES2386781T3 (es) 2012-08-30
WO2004000833A1 (en) 2003-12-31
NZ537720A (en) 2007-01-26
TWI354554B (en) 2011-12-21
US20060270660A1 (en) 2006-11-30
MXPA05000068A (es) 2005-04-11
PL374953A1 (en) 2005-11-14
HK1100081A1 (en) 2007-09-07
BR0312443A (pt) 2005-05-10
NO20110523L (no) 2005-03-21
NZ549142A (en) 2008-04-30
NO331925B1 (no) 2012-05-07
DE60336092D1 (de) 2011-03-31
JP2010202673A (ja) 2010-09-16
EP1517905B1 (en) 2012-05-02
NO20050144D0 (no) 2005-01-11
NZ562953A (en) 2009-06-26
KR101141959B1 (ko) 2012-05-04
CA2489824C (en) 2011-05-03
EA012869B1 (ru) 2009-12-30
HK1077057A1 (en) 2006-02-03
EP2277876A1 (en) 2011-01-26
US20040049032A1 (en) 2004-03-11
IS7661A (is) 2005-01-21
EP2292614A1 (en) 2011-03-09
AU2003245568B2 (en) 2009-12-17
CN100484934C (zh) 2009-05-06
KR20110010794A (ko) 2011-02-07
KR101067254B1 (ko) 2011-09-27
ATE498621T1 (de) 2011-03-15
TW200406210A (en) 2004-05-01
TW200736231A (en) 2007-10-01
EP1517905A1 (en) 2005-03-30
US20130066069A1 (en) 2013-03-14
HRP20050064A2 (en) 2006-07-31
IS7606A (is) 2004-12-20
NZ576752A (en) 2010-11-26
SG170614A1 (en) 2011-05-30
US8268829B2 (en) 2012-09-18
EP1746093B1 (en) 2011-02-16
US7557106B2 (en) 2009-07-07
CO5680433A2 (es) 2006-09-29
JP2010235626A (ja) 2010-10-21
MY141867A (en) 2010-07-16
TWI297684B (en) 2008-06-11
NO20050144L (no) 2005-03-21
JP2014111662A (ja) 2014-06-19
JP4237701B2 (ja) 2009-03-11
KR20050009756A (ko) 2005-01-25
EA200801372A1 (ru) 2008-08-29
EA015990B1 (ru) 2012-01-30
US20090221602A1 (en) 2009-09-03
CN1675199A (zh) 2005-09-28
EA200500053A1 (ru) 2005-08-25
CA2489824A1 (en) 2003-12-31

Similar Documents

Publication Publication Date Title
AR040286A1 (es) Proceso para la preparacion de pirimidinas sustituidas
AR003428A1 (es) Derivados de pirimidindiona o triazindiona como antagonista de los receptores adrenergenicos alfa1, procedimiento para su preparacion, composicion farmaceutica que los contiene y uso de dichos compuestos para la preparacion de medicamentos.
AR038202A1 (es) Compuestos de indazol utiles como inhibidores de la proteina quinasa
AR049333A1 (es) Azaindoles inhibidores de proteinquinasas rock y otras proteinas quinasas. composiciones farmaceuticas.
AR046600A1 (es) Diazaespiroalcanos y su uso como tratamiento para enfermedades mediadas por ccr8
AR032130A1 (es) Un compuesto inhibidor de quinasas proteicas, una composicion farmaceutica que lo incluye, y un metodo para tratar afecciones con dicho compuesto
AR041566A1 (es) Derivados de indol utiles para el tratamiento de enfermedades
AR033678A1 (es) Derivados de quinolina, procedimiento para prepararlos, uso de los mismos para la preparacion de medicamentos y los medicamentos que contienen dichos derivados
UY27503A1 (es) Nuevos derivados de piperazina
AR038259A1 (es) Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p
CO5031253A1 (es) Antagonistas receptores y5 de neuropeptidos composiciones farmaceuticas que las contienen
AR032467A1 (es) Derivados de piridina, procedimiento para prepararlos, el uso de dichos derivados para la preparacion de medicamentos y los medicamentos que contienen dichos derivados
AR049646A1 (es) Derivados de sulfamato y sulfamida utiles para el tratamiento de la epilepsia y trastornos relacionados
AR054035A1 (es) Derivados benzodioxano y benzodioxolano y uso de los mismos
AR049956A1 (es) DERIVADOS DE 1,3 - OXAZOLIDIN - 2 - ONA COMO INHIBIDORES DE CETP Y ELEVADORES DEL NIVEL DE LAD-C; COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN Y SU USO EN LA FABRICACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE LA ATEROSCLEROSIS.
AR042169A1 (es) Compuestos de pirazol utiles como inhibidores de proteinquinasa
AR048501A1 (es) Compuesto de benzoazabicicloheptano dimerico, composicion farmaceutica que lo comprende y su uso para prepararla
AR006720A1 (es) Un compuesto derivado de azahexano heterociclico, su uso para la preparacion de una composicion farmaceutica, procedimiento para prepararlo y una composicion farmaceutica que lo comprende
AR002012A1 (es) Un compuesto, una composicion farmaceutica que lo comprende, su uso, metodo de tratamiento terapeutico, metodo para la preparacion del compuesto.
AR055202A1 (es) Derivados de imidazolcarboxamida como inhibidores de fructosa -1,6- biofosfatasa y composiciones farmaceuticas que los contienen
AR040773A1 (es) Pirazoles utiles como inhibidores de gsk-3
AR049398A1 (es) Derivados de sulfamato y sulfamida; una composicion farmaceutica que los contiene y su uso en la preparacion de un medicamento util para el tratamiento de la epilepsia y trastornos relacionados.
AR050966A1 (es) Derivados de bencimidazol utiles como moduladores selectivos de receptores de androgenos (sarms)
AR086357A1 (es) Derivados de indazol sustituidos activos como inhibidores de quinasas
AR049388A1 (es) Heterociclos como inhibidores de aldosterona sintasa

Legal Events

Date Code Title Description
FB Suspension of granting procedure