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1.发明申请
公开(公告)号：WO2004046120A3
公开(公告)日：2004-08-12
申请号：PCT/US0336849
申请日：2003-11-17
Applicant: VERTEX PHARMA , PIERCE ALBERT C , ARNOST MICHAEL , DAVIES ROBERT J , FORSTER CORNELIA J , GALULLO VINCENT , GREY RONALD , LEDEBOER MARK , TIAN SHI-KAI , XU JINWANG , BINCH HAYLEY , LEDFORD BRIAN , MESSERSMITH DAVID , NANTHAKUMAR SUGANTHI , JAYARAJ ANDREW
Inventor： PIERCE ALBERT C , ARNOST MICHAEL , DAVIES ROBERT J , FORSTER CORNELIA J , GALULLO VINCENT , GREY RONALD , LEDEBOER MARK , TIAN SHI-KAI , XU JINWANG , BINCH HAYLEY , LEDFORD BRIAN , MESSERSMITH DAVID , NANTHAKUMAR SUGANTHI , JAYARAJ ANDREW
IPC: A61K31/4196 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D249/10 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/02 , C07D417/02 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/14 , C07D487/04 , C07D495/04 , A61K31/41 , C07D498/04 , C07D513/04
CPC classification number: C07D401/04 , C07D249/10 , C07D249/14 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/14 , C07D487/04 , C07D495/04
Abstract: The present invention relates to inhibitors of protein kinases of formula I. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Abstract translation: 本发明涉及式I的蛋白激酶抑制剂。本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：AU2003294329B2
公开(公告)日：2010-04-29
申请号：AU2003294329
申请日：2003-11-17
Applicant: VERTEX PHARMA
Inventor： FORSTER CORNELIA J , JAYARAJ ANDREW , LEDEBOER MARK , PIERCE ALBERT C , DAVIES ROBERT J , BINCH HAYLEY , LEDFORD BRIAN , GREY RONALD , ARNOST MICHAEL , XU JINWANG , MESSERSMITH DAVID , GALULLO VINCENT , NANTHAKUMAR SUGANTHI , TIAN SHI-KAI
IPC: C07D249/14 , A61K31/4196 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D249/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/02 , C07D417/02 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/14 , C07D487/04 , C07D495/04
Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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公开(公告)号：ES2318893T3
公开(公告)日：2009-05-01
申请号：ES99920427
申请日：1999-05-11
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , GALULLO VINCENT , BELLON STEVEN , BEMIS GUY , COCHRAN JOHN
IPC: C07D213/56 , A61K31/17 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , C04B35/01 , C07C275/32 , C07D20060101 , C07D213/00 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/12 , G02B6/02 , G02B6/12
Abstract: Un compuesto de fórmula ** ver fórmula** en la que Q1 se selecciona ** ver fórmula** Q2 se selecciona de: ** ver fórmula** 2-piridilo no sustituido o fenilo no sustituido; R'' se selecciona de hidrógeno, alquilo (C 1-C 3); alquenilo o alquinilo (C 2-C 3); fenilo o fenilo sustituido con 1 a 3 sustituyentes independientemente seleccionados de halógeno, metoxi, ciano, nitro, amino, hidroxi, metilo o etilo; o un sistema anular heterocíclico de 5-6 miembros opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de halógeno, metoxi, ciano, nitro, amino, hidroxi, metilo o etilo; R 3 se selecciona de sistemas anulares carbocíclicos o heterocíclicos aromáticos o no aromáticos de 5-8 miembros; W se selecciona de N(R 2 )SO2-N(R 2 )2; N(R 2 )SO2-N(R 2 )(R 3 ); N(R 2 )C(O)-OR 2 ; N(R 2 )C(O)-N(R 2 )2; N(R 2 )C(O)-N (R 2 )(R 3 ); N(R 2 )C(O)-R 2 ; N(R 2 )2; C(O)-R 2 ; CH(OH)-R 2 ; C(O)-N(R 2 )2; C(O)-OR 2 ; o alquilo (C1-C4) lineal o ramificado opcionalmente sustituido con N(R'')2, OR'', CO2R'', CON(R'')2, R 3 o SO2N(R 2 )2; o un sistema anular carbocíclico o heterocíclico de 5-6 miembros opcionalmente sustituido con N(R'') 2, OR'', CO 2R'', CON(R'') 2 o SO 2N(R 2 ) 2; con la condición de que W no sea un alquilo C 1 sustituido con R 3 ; R 2 se selecciona de hidrógeno, alquilo (C1-C3) o alquenilo (C1-C3); cada uno opcionalmente sustituido con -N (R'')2, -OR'', SR'', -C(O)-N(R'')2, S(O2)-N(R'')2, -C(O)-OR''; cada Y es C, en el que cada R y U unido a Y se selecciona independientemente de hidrógeno o metilo; Z es CH o N; y V es -C(O)NH 2.
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公开(公告)号：PL198352B1
公开(公告)日：2008-06-30
申请号：PL34404699
申请日：1999-05-11
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , GALULLO VINCENT , BELLON STEVEN , BEMIS GUY , COCHRAN JOHN
IPC: C07D213/00 , A61K31/17 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , C04B35/01 , C07C275/32 , C07D20060101 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/12 , G02B6/02 , G02B6/12
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公开(公告)号：MY132496A
公开(公告)日：2007-10-31
申请号：MYPI9901841
申请日：1999-05-10
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCIS , GALULLO VINCENT , BELLON STEVEN , BEMIS GUY , COCHRAN JOHN
IPC: C07D213/56 , A61K31/17 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , C04B35/01 , C07C275/32 , C07D20060101 , C07D213/00 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/12 , G02B6/02 , G02B6/12
Abstract: THE PRESENT INVENTION RELATES TO INHIBITORS OF P38, A MAMMALIAN PROTEIN KINASE INVOLVED CELL PROLIFERATION, CELL DEATH AND RESPONSE TO EXTRACELLULAR STIMULI. THE INVENTION ALSO RELATES TO METHODS FOR PRODUCING THESE INHIBITORS. THE INVENTION ALSO PROVIDES PHARMACEUTICAL COMPOSITIONS COMPRISING THE INHIBITORS OF THE INVENTION AND METHODS OF UTILIZING THOSE COMPOSITIONS IN THE TREATMENT AND PREVENTION OF VARIOUS DISORDERS.
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Patent Agency Ranking
公开(公告)号：DK1077943T3
公开(公告)日：2009-03-16
申请号：DK99920427
申请日：1999-05-11
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , GALULLO VINCENT , BEMIS GUY , BELLON STEVEN , COCHRAN JOHN
IPC: C07D213/56 , A61K31/17 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , C04B35/01 , C07C275/32 , C07D20060101 , C07D213/00 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/12 , G02B6/02 , G02B6/12
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
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公开(公告)号：NO319755B1
公开(公告)日：2005-09-12
申请号：NO20005673
申请日：2000-11-10
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO GERALD , BEMIS GUY W , COCHRAN JOHN E , GALULLO VINCENT , BELLON STEVEN
IPC: A61K31/17 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , C04B35/01 , C07C275/32 , C07D20060101 , C07D213/00 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/12 , G02B6/02 , G02B6/12
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
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公开(公告)号：NO20052888L
公开(公告)日：2005-08-12
申请号：NO20052888
申请日：2005-06-10
Applicant: VERTEX PHARMA
Inventor： ARNOST MICHAEL J , FORSTER CORNELIA J , DAVIES ROBERT J , PIERCE ALBERT , BINCH HAYLEY , LEDEBOER MARK , LEDFORD BRIAN E , GALULLO VINCENT , GREY RONALD , TIAN SHI-KAI , XU JINWANG , MESSERSMITH DAVID , NANTHAKUMAR SUGHANTHI , JAYARAJ ANDREW
IPC: A61K31/4196 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D249/10 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/02 , C07D417/02 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/14 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/41 , A61P3/00 , A61P29/00 , A61P19/00 , A61P25/00 , A61P35/00 , A61P9/00 , A61P37/00
Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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公开(公告)号：BG64533B1
公开(公告)日：2005-06-30
申请号：BG10357599
申请日：1999-07-13
Applicant: VERTEX PHARMA
Inventor： BEMIS GUY , SALITURO FRANCESCO , DUFFY JOHN , COCHRAN JOHN , HARRINGTON EDMUND , MURCKO MARK , WILSON KEITH , SU MICHAEL , GALULLO VINCENT
IPC: A61K31/4375 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/519 , A61K31/5377 , A61P7/02 , A61P9/10 , A61P19/08 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07D213/56 , C07D213/61 , C07D213/70 , C07D213/75 , C07D237/18 , C07D241/12 , C07D241/20 , C07D401/04 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07F9/6561 , A61K31/495 , C07F9/58
Abstract: The invention relates to p38 proteinkinase inhibitors is mammals participating in cellular proliferation, cellular death and extracellular stimulus responses, and to methods for the preparation of these inhihibitors. The invention also relates to pharmaceutical preparation including it, and to methods for the application of these preparation for the prevention and treatment of different diseases.
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公开(公告)号：NZ508653A
公开(公告)日：2003-07-25
申请号：NZ50865399
申请日：1999-05-11
Applicant: VERTEX PHARMA
Inventor： BEMIS GUY , COCHRAN JOHN , SALITURO FRANCESCO , GALULLO VINCENT , BELLON STEVEN
IPC: A61K31/17 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/02 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , C04B35/01 , C07C275/32 , C07D20060101 , C07D213/00 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/06 , C07D401/12 , G02B6/02 , G02B6/12
Abstract: Described are compounds of formulae (Ia), (Ib), (Ic), (Id) and (Ie), wherein; Q1 and Q2 are independently selected from a phenyl or 5-6 membered aromatic heterocyclic ring system, or a 8-10 membered ring system comprising aromatic carbocyclic rings, aromatic heterocyclic rings or a combination of an aromatic carbocyclic ring and an aromatic heterocyclic ring; which may be optionally substituted, V is selected from -C(O)NH2, -P(O)(NH2)2, or -SO2NH2, Y is N or C, wherein when Y is N, then R or U attached thereto is a lone pair of electrons. Also described is the use of the above compounds in inhibiting the p38 mammalian kinase, involved in cell proliferation, cell death and response to extracellular stimuli.
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