CO5370680A1 - Nuevos compuestos - Google Patents

Nuevos compuestos

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Publication number
CO5370680A1
CO5370680A1 CO98075455A CO98075455A CO5370680A1 CO 5370680 A1 CO5370680 A1 CO 5370680A1 CO 98075455 A CO98075455 A CO 98075455A CO 98075455 A CO98075455 A CO 98075455A CO 5370680 A1 CO5370680 A1 CO 5370680A1
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Colombia
Prior art keywords
alkyl
cr10r20
fluorophenyl
aryl
heteroaryl
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CO98075455A
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English (en)
Inventor
Timothy Francis Gallagher
Jeffrey Charles Boehm
Adams Jerry Leroy
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Smithkline Beecham Corp
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Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of CO5370680A1 publication Critical patent/CO5370680A1/es

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    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto que es: 1- Ciclohexil-4-(4-fluorofenil) -5- [(2-fenilamino)pirimidin-4-il]imidazol;1- Ciclohexil-4- (4-fluorofenil)-5-[[2- [N- (3-morfolino)pro-pil]amino]pirimidin-4-il]imidazol;1- Ciclohexil-4- (4-fluorofenil) -5- [ [2- [N- (2-imidazol-4-il)etilamino]pirimidin-4-il]imidazol;1- Ciclohexil-4- (4-fluorofenil) -5- [[2- [N- (3-piridil)metil] amino]pirimidin-4-il]imidazol;1- Ciclohexil-4- (4-fluorofenil) -5- [2- [N- (3,3-difenil)pro-pil] amino]pirimidin-4 - il ]imidazol;( / -) -1-Ciclohexil-4-(4-fluorofenil) -5- [ [2- [N-(1-metil-3-fenil)propil]amino]pirimidin-4-il]imidazol;N-4-[ [ [4- (4-Fluorofenil)] -5- [[2-[(3-trifluorometil)fenil-amino] ]pirimidin-4-il]imidazol-4-il]piperidinil-NAND#39 - [(3-trifluorometil)fenil]urea;N-[2-[4-(4-Fluorofenil) -5-[[2-(3,4-dicloprobencil)pirimidin-4-il] -1H-imidazol-1-il]etil] -3,4-dimetoxibenzamida;N-[2-[4-(4-Fluorofenil) -5-[[2-(4-metoxibencilamino)pirimidin-4-il] -1H-imidazol-1-il]etil]-etoxiacetamida;1-Isopropil-4- (4-fluorofenil) -5- [2-fenilamino-pirimidin-4-il]imidazol;1-Ciclopentil-4- (4-fluorofenil)-5-[2-fenilamino-pirimidin-4-il]imidazol;1- [(1-t-Butoxicarbonil)-4-piperidinil]-4-(4-fluorofenil)-5- [2-(2-metil-4-fluorofenil)amino]pirimidin-4-il] imidazol;1- (4-Piperidinil) -4- (4-fluorofenil) -5- [2-(2-metil-4-fluorofenil)amino]pirimidin-4-il]imidazol;1- (4-Piperidinil) -4- (4-fluorofenil) -5- [2- (2-metil-5-fluorofenil)amino]pirimidin-4-il]imidazol;1- (4-Piperidinil)-4-(4-fluorofenil)-5- [2-(2,6-dimetilfenil) -amino]pirimidin-4-il]imidazol;1- (4-Piperidinil) -4- (4-fluorofenil)-5- [2- (2-metilfenil) -amino]pirimidin-4-il]imidazol;1- (4-Fluorofenil)-4-(4-fluorofenil)-5-[2-fenilaminopirimidin-4-il]imidazol;1- (4-Fluorofenil)-4- (fluorofenil)-5- [2-(4-fluorofenilamino) -pirimidin-4-il]imidazol;1- (4-Fluorofenil) -4- (4-fluorofenil) -5- [2- (4-metilfenilamino)-pirimidin-4-il] imidazol;1- (4-Fluorofenil) -4- (4-fluorofenil) -5- [2-(2-metilfenil-amino)pirimidin-4-il]imidazol;1- (4-Fluorofenil) -4- (4-fluorofenil) -5- [2- (2,6-dimetilfenilamino)pirimidin-4-il]imidazol;1- (4-Fluorofenil) -4- (4-fluorofenil) -5- [2- (4-2-morfolin-fenilamino)pirimidin-4-il]imidazol; ouna de sus sales farmacéuticamente aceptables. - 2 -1Un compuesto de la fórmula <EMI FILE="98075455_1" ID="1" IMF=JPEG >R1 es un anillo de 4-piridazinilo o de 1,2,4-triazin-5-ilo, cuyo anillo está sustituido con NHRa y opcionalmente sustituido con un sustituyente, independiente, adicional, de alquilo C1-C4, halógeno, hidroxilo, alcoxi C1-C4, alquiltio C1-C4, alquilsulfinilo C1-C4, CH2OR12, amino, amino mono- y di-sustituido con alquilo C1-C6, N(R10)C(O)Rb o NHRa, Ra es arilo, aril-alquilo C1-C6, heterociclilo, heterociclil-alquilo C1-C6, heteroarilo, heteroaril-alquilo C1-C6, en donde cada uno de estos restos puede estar opcionalmente sustituido;Rb es hidrógeno, alquilo C1-C6, cicloalquilo C3-C7, arilo, aril-alquilo C1-C4, heteroarilo, heteroaril-alquilo C1-C4, heterociclilo, o heterociclil-alquilo C1-C4;R4 es fenilo, naft-1-ilo o naft-2-ilo, o un heteroarilo, que está opcionalmente sustituido con uno o dos sustituyentes, cada uno de los cuales se selecciona independientemente, y que, para un sustituyente 4-fenilo, 4-naft-1-ilo, 5-naft-2-ilo o 6-naft-2-ilo, es halógeno, ciano, nitro, C(Z)NR7R17, C(Z)OR16, (CR10R20)vCOR12, SR5, SOR5, OR12, alquilo C1-C4 sustituido con halo, alquilo C1-C4, ZC(Z)R12,NR10C(Z)R16 o (CR10R20)vNR10R20, y que, para otras posiciones de sustitución es halógeno, ciano, C(Z)NR13R14, C(Z)OR3, (CR10R20)m"COR3, S(O)mR3, OR3, alquilo C1-C4 sustituido con halo, alquilo C1-C4, (CR10R20)m"NR10C(Z)R3, NR10S(O)mAND#39R8, NR10S(O)mAND#39R7R17, ZC(Z)R3 o (CR10R20)m"NR13R14;v es 0, o un número entero con un valor de 1 ó 2;m es 0, o el número entero 1 ó 2;mAND#39 es un número entero con un valor de 1 ó 2;m" es 0, o un número entero con un valor de 1 a 5;R2 es - (CR10R20)nAND#39OR9, heterociclilo, heterociclil-alquilo C1-C10, alquilo C1-C10, alquilo C1-C10 sustituido con halo, alquenilo C2-C10, alquinilo C2-C10 cicloalquilo C3-C7, cicloalquil C3-C7-alquilo C1-C10, cicloalquenilo C5-C7, cicloalquenil C5-C7-alquilo C1-C10, arilo, aril-alquilo C1-C10, heteroarilo, heteroaril-alquilo C1-C10, (CR10R20)nOR11, (CR10R20)nS(O)mR18, (CR10R20)nNHS(O)2R18, (CR10R20)nNR13R14, (CR10R20)nNO2, (CR10R20)nCN, (CR10R20)n, SO2R18, (CR10R20)nS(O)mAND#39NR13R14, (CR10R20)nC(Z)R11, (CR10R20)nOC(Z)R11, (CR10R20)nC(Z)OR11, (CR10R20)nC(Z)NR13R14, (CR10R20)nC(Z)NR11OR9, (CR10R20)nNR10C(Z)R11, (CR10R20)nNR10C(Z)NR13R14, (CR10R20)nN(OR6)C(Z)NR13R14, (CR10R20)nN(OR6)C(Z)R11, (CR10R20)nC(=NOR6)R11, (CR10R20)nNR10C(=NR19)NR13R14, (CR10R20)nOC(Z)NR13R14, (CR10R20)nNR10C(Z)NR13R14, (CR10R20)nNR10C(Z)OR10, 5-(R18)-1,2,4-oxadiazol-3-ilo o 4-(R12)-5-(R18R19)-4,5-dihidro-1,2,4-oxadiazol-3-ilo; en donde los grupos arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterociclilo y heterociclilalquilo pueden estar opcionalmente sustituidos;n es un número entero que tiene un valor de 1 a 10;nAND#39 es 0, o un número entero que tiene un valor de 1 a 10;Z es oxígeno o azufre;R3 es heterociclilo, heterociclil-alquilo C1-C10 o R8;R5 es hidrógeno, alquilo C1-C4, alquenilo C2-C4, alquinilo C2-C4 o NR7R17, excluyendo los restos SR5 que son SNR7R17 y los restos SOR5 que son SOH;R6 es hidrógeno, un catión farmacéuticamente aceptable, alquilo C1-C10, cicloalquilo C3-C7, arilo, aril-alquilo C1-C4, heteroarilo, heteroaril-alquilo C1-C4, heterociclilo, aroílo, o alcanoílo C1-C10;R7 y R17, en cada caso, se seleccionan independientemente entre hidrógeno o alquilo C1-C4 o R7 y R17 junto con el nitrógeno al que están unidos forman un anillo heterocíclico de 5 a 7 miembros, el cual contiene opcionalmente un heteroátomo adicional seleccionado entre oxígeno, azufre o NR15;R8 es alquilo C1-C10, alquilo C1-C10 sustituido con halo, alquenilo C2-C10, alquinilo C2-C10, cicloalquilo C3-C7, cicloalquenilo C5-C7, arilo, aril-alquilo C1-C10, heteroarilo, heteroaril-alquilo C1-C10, (CR10R20)nOR11, (CR10R20)nS(O)mR18, (CR10R20)nNHS(O)2R18, (CR10R20)nNR13R14; donde el arilo, arilalquilo, heteroarilo o heteroarilalquilo puede estar opcionalmente sustituido;R9 es hidrógeno, C(Z)R11 o alquilo C1-C10 opcionalmente sustituido, S(O)2R18, arilo opcionalmente sustituido o aril-alquilo C1-C4 opcionalmente sustituido;R10 y R20, en cada caso, se seleccionan independientemente entre hidrógeno o alquilo C1-C4;R11 es hidrógeno, alquilo C1-C10, cicloalquilo C3-C7, heterociclilo, heterociclil-alquilo C1-C10, arilo, aril-alquilo C1-C10, heteroarilo o heteroaril-alquilo C1-C10;R12 es hidrógeno o R16;R13 y R14, en cada caso, se seleccionan independientemente entre hidrógeno o alquilo C1-C4 opcionalmente sustituido, arilo opcionalmente sustituido o aril-alquilo C1-C4 opcionalmente sustituido, o junto con el - 3 -nitrógeno al que están unidos forman un anillo heterocíclico de 5 a 7 miembros, el cual contiene opcionalmente un heteroátomo adicional seleccionado entre oxígeno, azufre o NR9;R15 es R10 o C(Z) -alquilo C1-C4;R16 es alquilo C1-C4, alquilo C1-C4 sustituido con halo o cicloalquilo C3-C7;R18 es alquilo C1-C10, cicloalquilo C3-C7, heterociclilo, arilo, aril-alquilo C1-C10, heterociclilo, heterociclil-alquilo C1-C10, heteroarilo o heteroaril-alquilo C1-C10;R19 es hidrógeno, ciano, alquilo C1-C4, cicloalquilo C3-C7 o arilo;o una de sus sales farmacéuticamente aceptables.1 Un procedimiento para preparar un compuesto de Formula (A): <EMI FILE="98075455_2" ID="2" IMF=JPEG >R1 es un anillo de 4-pirimidinilo, cuyo anillo está sustituido con NHRa y opcionalmente sustituido con un sustituyente, independiente, adicional, de alquilo C1-C4, halógeno, hidroxilo, alcoxi C1-C4, alquiltio C1-C4, alquilsulfinilo C1-C4, CH2OR12, amino, amino mono- y di-sustituido con alquilo C1-C6, N(R10)C(O)Rb o NHRa;Ra es hidrógeno, alquilo, alquilo opcionalmente sustituido, arilo, aril-alquilo C1-C6, heterociclilo, heterociclil-alquilo C1-C6, heteroarilo, heteroaril-alquilo C1-C6, en donde cada uno de estos restos arilo, heteroarilo o heterociclilo puede estar opcionalmente sustituido; Rb es hidrógeno, alquilo C1-C6, cicloalquilo C3-C7, arilo, aril-alquilo C1-C4, heteroarilo, heteroaril-alquilo C1-C4, heterociclilo, o heterociclil-alquilo C1-C4;R4 es fenilo, naft-1-ilo o naft-2-ilo, o un heteroarilo, que está opcionalmente sustituido con uno o dos sustituyentes, cada uno de los cuales se selecciona independientemente, y que, para un sustituyente 4-fenilo, 4-naft-1-ilo, 5-naft-2-ilo o 6-naft-2-ilo, es halógeno, ciano, nitro, C(Z)NR7R17, C(Z)OR16, (CR10R20)vCOR12, SR5, SOR5, OR12, alquilo C1-C4 sustituido con halo, alquilo C1-C4, ZC(Z)R12, NR10C(Z)R16 o (CR10R20)vNR10R20, y que, para otras posiciones de sustitución es halógeno, ciano, C(Z)NR13R14, C(Z)OR3, (CR10R20)m"COR3, S(O)mR3, OR3, alquilo C1-C4 sustituido con halo, alquilo C1-C4, (CR10R20)m"NR10C(Z)R3, NR10S(O)mAND#39R8, NR10S(O) mAND#39 R7R17,ZC(Z)R3 o (CR10R20)m"NR13R14;v es 0, o un número entero con un valor de 1 ó 2;m es 0, o el número entero 1 ó 2;mAND#39 es un número entero con un valor de 1 ó 2;m" es 0 , o un número entero con un valor de 1 a 5;R2 es -(CR10R20)nAND#39OR9, heterociclilo, heterociclil-alquilo C1-C10, alquilo C1-C10, alquilo C1-C10 sustituido con halo, alquenilo C2-C10, alquinilo C2-C10, cicloalquilo C3-C7, cicloalquil C3-C7-alquilo C1-C10, cicloalquenilo C5-C7, cicloalquenil C5-C7-alquilo C1-C10, arilo, aril-alquilo C1-C10, heteroarilo, heteroaril-alquilo C1-C10, (CR10R20)nOR11, (CR10R20)nS(O)mR18, (CR10R20)nNHS(O)2R18, (CR10R20)nNR13R14, (CR10R20)nNO2,(CR10R20)nCN, (CR10R20)nAND#39SO2R18,(CR10R20)nS(O)mAND#39NR13R14, (CR10R20)nC(Z)R11,(CR10R20)nOC(Z)R11, (CR10R20)nC(Z)OR11,(CR10R20)nC(Z)NR13R14, (CR10R20)nC(Z)NR11OR9,(CR10R20)nNR10C(Z)R11, (CR10R20)nNR10C(Z)NR13R14,(CR10R20)nN(OR6)C(Z)NR13R14, (CR10R20)nN(OR6)C(Z)R11,(CR10R20)nC(=NOR6)R11, (CR10R20)nNR10C(=NR19)NR13R14,(CR10R20)nOC(Z)NR13R14, (CR10R20)nNR10C(Z)NR13R14,(CR10R20)nNR10C(Z)OR10, 5-(R18)-1,2,4-oxadiazol-3-ilo o 4-(R12)-5-(R18R19)-4,5
CO98075455A 1997-12-19 1998-12-18 Nuevos compuestos CO5370680A1 (es)

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US (2) US6335340B1 (es)
EP (1) EP1037639A4 (es)
JP (1) JP2001526230A (es)
AR (1) AR017219A1 (es)
AU (1) AU1924699A (es)
CA (1) CA2314980A1 (es)
CO (1) CO5370680A1 (es)
WO (1) WO1999032121A1 (es)
ZA (1) ZA9811631B (es)

Families Citing this family (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU7726898A (en) 1997-05-22 1998-12-11 G.D. Searle & Co. Pyrazole derivatives as p38 kinase inhibitors
US6979686B1 (en) 2001-12-07 2005-12-27 Pharmacia Corporation Substituted pyrazoles as p38 kinase inhibitors
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
AU7966198A (en) 1997-06-13 1998-12-30 Smithkline Beecham Corporation Novel pyrazole and pyrazoline substituted compounds
US6610695B1 (en) 1997-06-19 2003-08-26 Smithkline Beecham Corporation Aryloxy substituted pyrimidine imidazole compounds
US6489325B1 (en) 1998-07-01 2002-12-03 Smithkline Beecham Corporation Substituted imidazole compounds
US6562832B1 (en) 1997-07-02 2003-05-13 Smithkline Beecham Corporation Substituted imidazole compounds
US7301021B2 (en) 1997-07-02 2007-11-27 Smithkline Beecham Corporation Substituted imidazole compounds
EP1041989A4 (en) 1997-10-08 2002-11-20 Smithkline Beecham Corp NEW SUBSTITUTED CYCLOALCENYL COMPOUNDS
WO1999032121A1 (en) 1997-12-19 1999-07-01 Smithkline Beecham Corporation Compounds of heteroaryl substituted imidazole, their pharmaceutical compositions and uses
US6858617B2 (en) 1998-05-26 2005-02-22 Smithkline Beecham Corporation Substituted imidazole compounds
US6207687B1 (en) 1998-07-31 2001-03-27 Merck & Co., Inc. Substituted imidazoles having cytokine inhibitory activity
US6846799B1 (en) 1998-08-18 2005-01-25 The Regents Of The University Of California Preventing airway mucus production by administration of EGF-R antagonists
CZ2001584A3 (cs) 1998-08-18 2002-06-12 The Regents Of The University Of California Prevence tvorby hlenu v dýchacích cestách podáváním antagonistů EGF-R
US7354894B2 (en) 1998-08-18 2008-04-08 The Regents Of The University Of California Preventing airway mucus production by administration of EGF-R antagonists
CA2341370A1 (en) 1998-08-20 2000-03-02 Smithkline Beecham Corporation Novel substituted triazole compounds
ATE336484T1 (de) 1998-08-29 2006-09-15 Astrazeneca Ab Pyrimidine verbindungen
DE69933680T2 (de) 1998-08-29 2007-08-23 Astrazeneca Ab Pyrimidine verbindungen
EP1126852B1 (en) * 1998-11-04 2004-01-21 SmithKline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
GB9907658D0 (en) 1999-04-06 1999-05-26 Zeneca Ltd Chemical compounds
JP2003502424A (ja) * 1999-06-17 2003-01-21 シオノギ バイオリサーチ コーポレイション Ｉｌ−１２産生の阻害物質
GB9919778D0 (en) 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
US6759410B1 (en) 1999-11-23 2004-07-06 Smithline Beecham Corporation 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors
JP2003528043A (ja) 1999-11-23 2003-09-24 スミスクライン・ビーチャム・コーポレイション ＣＳＢＰ／ｐ３８キナーゼ阻害剤としての３，４‐ジヒドロ−（１Ｈ）キナゾリン−２−オン化合物
DE60015599T2 (de) 1999-11-23 2005-11-03 Smithkline Beecham Corp. 3,4-DIHYDRO-(1H)CHINAZOLIN-2-ON-VERBINDUNGEN ALS CSBP/p38-KINASE-INHIBITOREN
JP2003514900A (ja) 1999-11-23 2003-04-22 スミスクライン・ビーチャム・コーポレイション ＣＳＢＰ／ｐ３８キナーゼ阻害剤としての３，４−ジヒドロ−（１Ｈ）−キナゾリン−２−オン化合物
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004886D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7235551B2 (en) * 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
GB0007371D0 (en) 2000-03-28 2000-05-17 Astrazeneca Uk Ltd Chemical compounds
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
GB0021726D0 (en) 2000-09-05 2000-10-18 Astrazeneca Ab Chemical compounds
US20040253891A1 (en) * 2000-09-12 2004-12-16 Schierenbeck Alan W. Composite structure for protective garment
IL155367A0 (en) 2000-10-23 2003-12-23 Smithkline Beecham Corp NOVEL 2,4,8-TRISUBSTITUTED-8h-PYRIDO[2,3,-d]PYRIMIDIN-7-ONE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME, PROCESSES FOR THE PREPARATION THEREOF, AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR TREATING CSBP/p38 KINASE MEDIATED DISEASES
US7199124B2 (en) 2001-02-02 2007-04-03 Takeda Pharmaceutical Company Limited JNK inhibitor
MY130778A (en) * 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
GB0113041D0 (en) 2001-05-30 2001-07-18 Astrazeneca Ab Chemical compounds
RU2308976C2 (ru) * 2002-02-15 2007-10-27 Си Ви Терапьютикс, Инк. Полимерное покрытие для медицинских устройств
US20040127492A1 (en) * 2002-02-19 2004-07-01 Pharmacia Corporation Cyclic pyrazoles for the inhibition of mitogen activated protein kinase-activated protein kinase-2
GB0205690D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
WO2003076434A1 (en) 2002-03-09 2003-09-18 Astrazeneca Ab 4- imidazolyl substuited pyrimidine derivatives with cdk inhibitiory activity
GB0205693D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
GB0205688D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
AR039241A1 (es) * 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
AU2003245989A1 (en) 2002-07-09 2004-01-23 Boehringer Ingelheim Pharma Gmbh And Co. Kg Pharmaceutical compositions of anticholinergics and p38 kinase inhibitors in the treatment of respiratory diseases
ATE343572T1 (de) * 2002-08-09 2006-11-15 Lilly Co Eli Benzimidazole und benzothiazole als inhibitoren der map-kinase
EP1539121A4 (en) 2002-08-29 2008-08-13 Scios Inc METHOD OF REQUESTING OSTEOGENESIS
UA80295C2 (en) * 2002-09-06 2007-09-10 Biogen Inc Pyrazolopyridines and using the same
US6909001B2 (en) * 2002-12-12 2005-06-21 Pharmacia Corporation Method of making tricyclic aminocyanopyridine compounds
US20040127511A1 (en) * 2002-12-12 2004-07-01 Pharmacia Corporation Tricyclic aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase-2
US20040127519A1 (en) * 2002-12-12 2004-07-01 Pharmacia Corporation Method of using aminocyanopyridine compounds as mitogen activated protein kinase-activated protein kinase-2 inhibitors
US20040142978A1 (en) * 2002-12-12 2004-07-22 Pharmacia Corporation Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase-2
BR0317525A (pt) * 2002-12-20 2005-11-16 Pharmacia Corp Compostos pirazol acìclico, composição terapêutica e farmacêutica, kit, bem como respectivos usos
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
GB0311274D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
US20050143371A1 (en) * 2003-07-23 2005-06-30 Pharmacia Corporation Beta-carboline compounds and analogues thereof as mitogen-activated protein kinase-activated protein kinase-2 inhibitors
US7244441B2 (en) 2003-09-25 2007-07-17 Scios, Inc. Stents and intra-luminal prostheses containing map kinase inhibitors
TW200533357A (en) * 2004-01-08 2005-10-16 Millennium Pharm Inc 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
TWI332003B (en) * 2004-01-30 2010-10-21 Lilly Co Eli Kinase inhibitors
TW200528101A (en) 2004-02-03 2005-09-01 Astrazeneca Ab Chemical compounds
RU2253440C1 (ru) * 2004-03-31 2005-06-10 Открытое Акционерное Общество "Фаберлик" Средство для устранения нарушений нейрогенной и эндокринной регуляции системы капиллярного кровотока
US7672268B2 (en) 2004-06-18 2010-03-02 Kenneth Stanwood Systems and methods for implementing double wide channels in a communication system
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
TW200633990A (en) 2004-11-18 2006-10-01 Takeda Pharmaceuticals Co Amide compound
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
EP1676574A3 (en) 2004-12-30 2006-07-26 Johnson &amp; Johnson Vision Care, Inc. Methods for promoting survival of transplanted tissues and cells
PE20100737A1 (es) 2005-03-25 2010-11-27 Glaxo Group Ltd Nuevos compuestos
AR053450A1 (es) 2005-03-25 2007-05-09 Glaxo Group Ltd Derivados de 3,4-dihidro-pirimido(4,5-d)pirimidin-2-(1h)-ona 1,5,7 trisustituidos como inhibidores de la quinasa p38
EP1865959A2 (en) * 2005-03-25 2007-12-19 Glaxo Group Limited Process for preparing pyridoý2,3-d¨pyrimidin-7-one and 3,4-dihydropyrimidoý4,5-d¨pyrimidin-2(1h)-one derivatives
EP1934213A1 (en) 2005-09-30 2008-06-25 Astra Zeneca AB Imidazo [1,2-a] pyridine having anti-cell-proliferation activity
EP1992344A1 (en) 2007-05-18 2008-11-19 Institut Curie P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation
WO2016149756A1 (en) 2015-03-23 2016-09-29 The University Of Melbourne Treatment of respiratory diseases
EP3518898A4 (en) * 2016-10-03 2020-06-17 The Children's Medical Center Corporation PREVENTION AND TREATMENT OF DIABETIC NEPHROPATHY
CN110753688A (zh) * 2017-05-03 2020-02-04 墨尔本大学 用于治疗呼吸系统疾病的化合物
US10047071B1 (en) 2018-01-15 2018-08-14 King Saud University Dihydropyrimidinone derivatives
EP3877383A4 (en) * 2018-11-07 2022-09-21 The University of Melbourne COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF RESPIRATORY DISEASES

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2833779A (en) 1956-10-29 1958-05-06 American Cyanamid Co Substituted pyrazoles
US3707475A (en) 1970-11-16 1972-12-26 Pfizer Antiinflammatory imidazoles
US3940486A (en) 1971-05-10 1976-02-24 Ciba-Geigy Corporation Imidazole derivatives in the treatment of pain
US3929807A (en) 1971-05-10 1975-12-30 Ciba Geigy Corp 2-Substituted-4(5)-(aryl)-5(4)-(2,3 or -4-pyridyl)-imidazoles
US4058614A (en) 1973-12-04 1977-11-15 Merck & Co., Inc. Substituted imidazole compounds and therapeutic compositions therewith
US4199592A (en) 1978-08-29 1980-04-22 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl-2-nitroimidazoles
DD201677A5 (de) 1980-07-25 1983-08-03 Ciba Geigy Verfahren zur herstellung von trisubstituierten imidazolderivaten
WO1983002613A1 (en) 1981-07-20 1983-08-04 Sallmann, Alfred Trisubstituted oxazo compounds
US4503065A (en) 1982-08-03 1985-03-05 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl 1-2-halo imidazoles
JPS60226882A (ja) 1984-04-24 1985-11-12 Nippon Zoki Pharmaceut Co Ltd 新規ピリミドピリミジン誘導体
US4565875A (en) 1984-06-27 1986-01-21 Fmc Corporation Imidazole plant growth regulators
US4686231A (en) 1985-12-12 1987-08-11 Smithkline Beckman Corporation Inhibition of 5-lipoxygenase products
IL83467A0 (en) 1986-08-15 1988-01-31 Fujisawa Pharmaceutical Co Imidazole derivatives,processes for their preparation and pharmaceutical compositions containing the same
EP0533837A4 (en) 1990-06-12 1994-11-17 Smithkline Beecham Corp Inhibition of 5-lipoxygenase and cyclooxygenase pathway mediated diseases
FR2665898B1 (fr) 1990-08-20 1994-03-11 Sanofi Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
AU9169991A (en) 1990-12-13 1992-07-08 Smithkline Beecham Corporation Novel csaids
EP0565582A4 (en) 1990-12-13 1995-01-11 Smithkline Beecham Corp NOVEL CYTOKINE SUPPRESSIVE ANTI-INFLAMMATORY DRUGS.
WO1992012154A1 (en) 1990-12-31 1992-07-23 Fujisawa Pharmaceutical Co., Ltd. Imidazotriazine derivatives
US5656644A (en) 1994-07-20 1997-08-12 Smithkline Beecham Corporation Pyridyl imidazoles
US5716972A (en) 1993-01-13 1998-02-10 Smithkline Beecham Corporation Pyridyl substituted imidazoles
IL104369A0 (en) 1992-01-13 1993-05-13 Smithkline Beecham Corp Novel compounds and compositions
DE69322254T2 (de) 1992-01-13 1999-04-29 Smithkline Beecham Corp Pyridyl-substituierte imidazole
US6008235A (en) 1992-01-13 1999-12-28 Smithkline Beecham Corporation Pyridyl substituted imidazoles
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
GB9303993D0 (en) 1993-02-26 1993-04-14 Fujisawa Pharmaceutical Co New heterocyclic derivatives
US5670527A (en) * 1993-07-16 1997-09-23 Smithkline Beecham Corporation Pyridyl imidazole compounds and compositions
IL110296A (en) * 1993-07-16 1999-12-31 Smithkline Beecham Corp Imidazole compounds process for their preparation and pharmaceutical compositions containing them
US5593991A (en) 1993-07-16 1997-01-14 Adams; Jerry L. Imidazole compounds, use and process of making
US5593992A (en) * 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
WO1995003297A1 (en) 1993-07-21 1995-02-02 Smithkline Beecham Corporation Imidazoles for treating cytokine mediated disease
JP3377529B2 (ja) 1993-09-17 2003-02-17 スミスクライン・ビーチャム・コーポレイション 薬物結合タンパク質
US5783664A (en) 1993-09-17 1998-07-21 Smithkline Beecham Corporation Cytokine suppressive anit-inflammatory drug binding proteins
US5869043A (en) 1993-09-17 1999-02-09 Smithkline Beecham Corporation Drug binding protein
KR100330553B1 (ko) 1993-10-01 2002-11-27 노파르티스 아게 약물학적활성피리딘유도체및그의제조방법
US5543520A (en) 1993-10-01 1996-08-06 Ciba-Geigy Corporation Pyrimidine derivatives
EP0672035A1 (en) 1993-10-01 1995-09-20 Novartis AG Pyrimidineamine derivatives and processes for the preparation thereof
JP3588116B2 (ja) 1993-10-01 2004-11-10 ノバルティス アクチェンゲゼルシャフト 薬理活性のピリミジンアミン誘導体およびその製造方法
JPH09505055A (ja) 1993-11-08 1997-05-20 スミスクライン・ビーチャム・コーポレイション サイトカイン媒介疾患治療用オキサゾール
US5559137A (en) 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
US5545669A (en) 1994-06-02 1996-08-13 Adams; Jerry L. Anti-inflammatory compounds
JPH10512264A (ja) 1995-01-12 1998-11-24 スミスクライン・ビーチャム・コーポレイション 新規化合物
US5658903A (en) 1995-06-07 1997-08-19 Smithkline Beecham Corporation Imidazole compounds, compositions and use
US5739143A (en) 1995-06-07 1998-04-14 Smithkline Beecham Corporation Imidazole compounds and compositions
WO1997005877A1 (en) 1995-08-10 1997-02-20 Merck & Co., Inc. 2-substituted aryl pyrroles, compositions containing such compounds and methods of use
CA2228050A1 (en) 1995-08-10 1997-02-20 Harold G. Selnick 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
IL123950A (en) 1995-10-06 2001-04-30 Merck & Co Inc Transformed imidazoles with anti-cancer and cytokine-inhibiting activity and pharmaceutical preparations containing them
AU702887B2 (en) 1995-10-31 1999-03-11 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
AU7529096A (en) 1995-10-31 1997-05-22 Merck & Co., Inc. Substituted aryl pyrroles, compositions containing such compounds and methods of use
WO1997016441A1 (en) 1995-10-31 1997-05-09 Merck & Co., Inc. Substituted aryl pyrroles, compositions containing such compounds and methods of use
ZA9610687B (en) 1995-12-22 1997-09-29 Smithkline Beecham Corp Novel synthesis.
JP2000503302A (ja) 1996-01-11 2000-03-21 スミスクライン・ビーチャム・コーポレイション 新規置換イミダゾール化合物
ZA97175B (en) 1996-01-11 1997-11-04 Smithkline Beecham Corp Novel substituted imidazole compounds.
AP9700912A0 (en) 1996-01-11 1997-01-31 Smithkline Beecham Corp Novel cycloalkyl substituted imidazoles
WO1997025047A1 (en) 1996-01-11 1997-07-17 Smithkline Beecham Corporation Novel cycloalkyl substituded imidazoles
JP2000507224A (ja) 1996-03-08 2000-06-13 スミスクライン・ビーチャム・コーポレイション Ｃｓａｉｄ化合物の血管形成の抑制物質としての使用
EP0888335A4 (en) 1996-03-13 2002-01-02 Smithkline Beecham Corp NEW PYRIMIDINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CYTOKININ MEDIATOR DISEASES
EP0889887A4 (en) 1996-03-25 2003-06-11 Smithkline Beecham Corp TREATMENT OF CENTRAL NERVOUS SYSTEM INJURIES
EP0889888A4 (en) 1996-03-25 2003-01-08 Smithkline Beecham Corp NEW TREATMENT OF LESIONS IN THE CENTRAL NERVOUS SYSTEM
WO1997036587A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. A method of treating cancer
JP3418624B2 (ja) * 1996-06-10 2003-06-23 メルク エンド カンパニー インコーポレーテッド サイトカイン阻害活性を有する置換イミダゾール類
DK0912518T3 (da) 1996-07-18 2003-12-08 Merck Frosst Canada Inc Substituerede pyridiner som selektive cyclooxygenase-2 inhibitorer
EP0922042A1 (en) 1996-08-09 1999-06-16 Smithkline Beecham Corporation Novel piperazine containing compounds
EP0956018A4 (en) 1996-08-21 2000-01-12 Smithkline Beecham Corp IMIDAZOLE COMPOUNDS, COMPOSITIONS CONTAINING THEM AND THEIR USE
AU5147598A (en) 1996-10-17 1998-05-11 Smithkline Beecham Corporation Methods for reversibly inhibiting myelopoiesis in mammalian tissue
DK0948495T3 (da) 1996-11-19 2004-06-01 Amgen Inc Aryl- og heteroarylsubstitueret, kondenseret pyrrol som antiinflammatoriske midler
WO1998022109A1 (en) 1996-11-20 1998-05-28 Merck & Co., Inc. Triaryl substituted imidazoles as glucagon antagonists
CZ9902016A3 (cs) 1996-12-05 1999-11-17 Amgen Inc. Substituované pyrimidinonové a pyridonové sloučeniny a způsoby jejich použití
ZA9711092B (en) 1996-12-11 1999-07-22 Smithkline Beecham Corp Novel compounds.
US6147080A (en) 1996-12-18 2000-11-14 Vertex Pharmaceuticals Incorporated Inhibitors of p38
WO1998028292A1 (en) 1996-12-23 1998-07-02 Smithkline Beecham Corporation Novel piperidine containing compounds
US5929076A (en) 1997-01-10 1999-07-27 Smithkline Beecham Corporation Cycloalkyl substituted imidazoles
AU7138298A (en) 1997-04-24 1998-11-13 Ortho-Mcneil Corporation, Inc. Substituted imidazoles useful in the treatment of inflammatory diseases
MA26487A1 (fr) 1997-04-29 2004-12-20 Smithkline Beecham Corp Heterocyclecetohydrazides inhibiteurs de proteases, procede pour leur preparation et compositions pharmaceutiques les contenant .
PT1019040E (pt) 1997-05-23 2005-01-31 Bayer Pharmaceuticals Corp Inibicao da actividade de p38-quinase por meio de arilureias
EP1041989A4 (en) 1997-10-08 2002-11-20 Smithkline Beecham Corp NEW SUBSTITUTED CYCLOALCENYL COMPOUNDS
WO1999032121A1 (en) 1997-12-19 1999-07-01 Smithkline Beecham Corporation Compounds of heteroaryl substituted imidazole, their pharmaceutical compositions and uses
JP3593035B2 (ja) 1998-10-23 2004-11-24 エフ．ホフマン−ラ ロシュ アーゲー 二環式窒素複素環化合物

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