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公开(公告)号：WO0170695A8
公开(公告)日：2001-11-29
申请号：PCT/US0109256
申请日：2001-03-22
Applicant: VERTEX PHARMA , SALITURO FRANCESCO , BEMIS GUY , EVINDAR GHOTAS
Inventor： SALITURO FRANCESCO , BEMIS GUY , EVINDAR GHOTAS
IPC: C07D487/04 , A61K31/4418 , A61K31/519 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/02 , A61P7/04 , A61P7/06 , A61P7/10 , A61P9/00 , A61P9/04 , 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 , A61P29/02 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D213/75 , C07D489/04 , A61K31/4402 , A61K31/5025
CPC classification number: C07D213/75 , C07D489/04
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli, having the formula (III), or tautomers thereof or pharmaceutically acceptable salts thereof, wherein: each of Q1 and Q2 are independently selected from 5-6 membered aromatic carbocyclic or heterocyclic ring systems, or 8-10 membered bicyclic ring systems comprising aromatic carbocyclic rings, aromatic heterocyclic rings or a combination of an aromatic carbocyclic ring and an aromatic heterocyclic ring. 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.
Abstract translation: 本发明涉及p38的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应，具有式（III）或其互变异构体或其药学上可接受的盐，其中：Q1和Q2各自独立地 选自5-6元芳族碳环或杂环系统，或包含芳族碳环，芳族杂环或芳族碳环和芳族杂环的组合的8-10元双环体系。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。
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2.发明申请
公开(公告)号：WO2008116139A3
公开(公告)日：2008-12-18
申请号：PCT/US2008057797
申请日：2008-03-21
Applicant: VERTEX PHARMA , WANNAMAKER MARION , SALITURO FRANCESCO , PIERCE ALBERT , ARONOV ALEXANDER , MARTINEZ-BOTELLA GABRIEL , WANG JIAN , FARMER LUC , LEDEBOER MARK , WANG TIANSHENG , BETHIEL RANDY , LEDFORD BRIAN , PORTER EMILIE
Inventor： WANNAMAKER MARION , SALITURO FRANCESCO , PIERCE ALBERT , ARONOV ALEXANDER , MARTINEZ-BOTELLA GABRIEL , WANG JIAN , FARMER LUC , LEDEBOER MARK , WANG TIANSHENG , BETHIEL RANDY , LEDFORD BRIAN , PORTER EMILIE
IPC: C07D213/74 , A61K31/506 , C07D239/42 , C07D401/04 , C07D403/04 , C07D403/12 , C07D405/04 , C07D417/04 , C07D417/12 , C07D471/04
CPC classification number: C07D401/14 , C07D213/74 , C07D239/42 , C07D401/04 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Abstract translation: 本发明涉及可用作蛋白激酶抑制剂，特别是JAK家族激酶的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。
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公开(公告)号：WO2007084557A3
公开(公告)日：2007-09-27
申请号：PCT/US2007001225
申请日：2007-01-17
Applicant: VERTEX PHARMA , FARMER LUC , MARTINEZ-BOTELLA GABRIEL , PIERCE ALBERT , SALITURO FRANCESCO , WANG JIAN , WANNAMKER MARION , WANG TIANSHENG
Inventor： FARMER LUC , MARTINEZ-BOTELLA GABRIEL , PIERCE ALBERT , SALITURO FRANCESCO , WANG JIAN , WANNAMKER MARION , WANG TIANSHENG
IPC: C07D471/04 , A61K31/506 , A61K31/517 , A61K31/53 , A61P25/00 , A61P29/00 , A61P37/00 , C07D519/00
CPC classification number: A61K31/506 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D495/10 , C07D519/00 , C12N9/12 , C12Y207/10002
Abstract: The present invention relates to azaindole compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Abstract translation: 本发明涉及可用作蛋白激酶抑制剂，尤其是JAK家族激酶抑制剂的氮杂吲哚化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。
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公开(公告)号：WO2007041130A3
公开(公告)日：2010-01-21
申请号：PCT/US2006037593
申请日：2006-09-28
Applicant: VERTEX PHARMA , SALITURO FRANCESCO , FARMER LUC , WANG TIANSHENG , WANG JIAN , BETHIEL RANDY , WANNAMAKER MARION , MARTINEZ-BOTELLA GABRIEL , DUFFY JOHN , ARONOV ALEXANDER , LAUFFER DAVID , PIERCE ALBERT
Inventor： SALITURO FRANCESCO , FARMER LUC , WANG TIANSHENG , WANG JIAN , BETHIEL RANDY , WANNAMAKER MARION , MARTINEZ-BOTELLA GABRIEL , DUFFY JOHN , ARONOV ALEXANDER , LAUFFER DAVID , PIERCE ALBERT
IPC: C07D487/04 , A61K31/495 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07D519/00
CPC classification number: C07D487/04
Abstract: The present invention relates to compounds of formula (I) useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Abstract translation: 本发明涉及用作蛋白激酶抑制剂，特别是JAK家族激酶的抑制剂的式（I）化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。
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5.发明申请
公开(公告)号：WO2008079521A2
公开(公告)日：2008-07-03
申请号：PCT/US2007083134
申请日：2007-10-31
Applicant: VERTEX PHARMA , BENNANI YOUSSEFF , WANG TIANSHENG , SALITURO FRANCESCO , DUFFY JOHN
Inventor： BENNANI YOUSSEFF , WANG TIANSHENG , SALITURO FRANCESCO , DUFFY JOHN
CPC classification number: C07D471/16 , C07D471/22 , C07D487/16
Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Abstract translation: 本发明涉及用作蛋白激酶抑制剂，特别是JAK家族激酶抑制剂的化合物。 本发明还提供了包含所述化合物的药学上可接受的组合物以及使用该组合物治疗各种疾病，病症或障碍的方法。
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Patent Agency Ranking
公开(公告)号：ES2401192T8
公开(公告)日：2013-05-10
申请号：ES06815526
申请日：2006-09-28
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , FARMER LUC , WANG TIANSHENG , WANG JIAN , BETHIEL RANDY , WANNAMAKER MARION , MARTINEZ-BOTELLA GABRIEL , DUFFY JOHN , ARONOV ALEXANDER , LAUFFER DAVID , PIERCE ALBERT
IPC: C07D487/04 , A61K31/495 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07D519/00
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公开(公告)号：HRP20110566T8
公开(公告)日：2012-12-31
申请号：HRP20110566
申请日：2011-07-29
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , FARMER LUC , BETHIEL RANDY , HARRINGTON EDMUND , GREEN JEREMY , COURT JOHN , COME JON , LAUFFER DAVID , ARONOV ALEX , BINCH HAYLEY , BOYALL DEAN , CHARRIER JEAN-DAMIEN , EVERITT SIMON , FRAYSSE DAMIEN , MORTIMORE MICHAEL , PIERARD FRANCOISE , ROBINSON DANIEL , PINDER JOANNE , WANG TIANSHENG , PIERCE ALBERT , WANG JIAN
IPC: C07D471/04 , C07D519/00
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公开(公告)号：AU2012203382A1
公开(公告)日：2012-06-28
申请号：AU2012203382
申请日：2012-06-08
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , FARMER LUC , BETHIEL RANDY , HARRINGTON EDMUND , GREEN JEREMY , COURT JOHN , COME JON , LAUFFER DAVID , ARONOV ALEX , BINCH HAYLEY , BOYALL DEAN , CHARRIER JEAN-DAMIEN , EVERITT SIMON , FRAYSSE DAMIEN , MORTIMORE MICHAEL , PIERARD FRANCOISE , ROBINSON DANIEL , WANG JIAN , PINDER JOANNE , WANG TIANSHEN , PIERCE ALBERT
IPC: C07D471/04 , C07D519/00
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：AU2007207533B8
公开(公告)日：2012-06-28
申请号：AU2007207533
申请日：2007-01-17
Applicant: VERTEX PHARMA
Inventor： WANNAMAKER MARION , SALITURO FRANCESCO , MARTINEZ-BOTELLA GABRIEL , WANG TIANSHENG , PIERCE ALBERT , FARMER LUC , WANG JIAN
IPC: C07D471/04 , A61K31/506 , A61K31/517 , A61K31/53 , A61P25/00 , A61P29/00 , A61P37/00 , C07D495/10 , C07D519/00
Abstract: The present invention relates to azaindole compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
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公开(公告)号：ES2364340T3
公开(公告)日：2011-08-31
申请号：ES05756052
申请日：2005-03-30
Applicant: VERTEX PHARMA
Inventor： SALITURO FRANCESCO , FARMER LUC , BETHIEL RANDY , HARRINGTON EDMUND , GREEN JEREMY , COURT JOHN , COME JON , LAUFFER DAVID , ARONOV ALEX , BINCH HAYLEY , BOYALL DEAN , CHARRIER JEAN-DAMIEN , EVERITT SIMON , FRAYSSE DAMIEN , MORTIMORE MICHAEL , PIERARD FRANCOISE , ROBINSON DANIEL , PINDER JOANNE , WANG TIANSHENG , PIERCE ALBERT
IPC: C07D471/04 , C07D519/00
Abstract: Un compuesto de formula (IB): **Fórmula** o sales farmaceuticamente aceptables del mismo, en la que: R1 es T-R' o es -Si(R')3; cada uno de R2, R3 y R4 es independientemente halogeno, -CN, -NO2 o V-R'; x es 1, 2 o 3; en cada aparicion, R5 es independientemente halogeno, -CN, -NO2 o U-R', en el que al menos un R5 es distinto de H; cada uno de T, V y U es independientemente un enlace o una cadena de alquilideno-C1-C6 opcionalmente sustituida, en la que hasta dos unidades de metileno de la cadena estan opcionalmente e independientemente sustituidas con -NR'-, -S-, -O- -CS-, -CO2-, -OCO-, -CO-, -COCO-, -CONR'-, -NR'CO-, - NR'CO2-, -SO2NR'-, - NR'SO2-, -CONR'NR'-, -NR'CONR'-, -OCONR'-, -NR'NR'-, - NR'SO2NR'-, -SO-, -SO2-, -PO-, -PO2- o -POR'-; y en cada aparicion, R es independientemente hidrogeno o un grupo opcionalmente sustituido seleccionado entre un grupo alifatico-C1-C6, un anillo monociclico saturado, parcialmente insaturado o totalmente insaturado de 3-8 miembros que tiene 0-3 heteroatomos seleccionados independientemente entre nitrogeno, oxigeno o azufre, o un sistema de anillos biciclico saturado, parcialmente insaturado o totalmente insaturado de 8-12 miembros que tiene 0-5 heteroatomos seleccionados independientemente entre nitrogeno, oxigeno o azufre; o dos apariciones de R se toman junto con el atomo o atomos a los que estan unidas para formar un anillo monociclico o biciclico, opcionalmente sustituido, saturado, parcialmente insaturado o totalmente insaturado de 3-12 miembros que tiene 0-4 heteroatomos seleccionados independientemente entre nitrogeno, oxigeno o azufre, con la condicion de que: a) si R2, R3 y R4 son simultaneamente H, entonces R1 no sea Si(R')3; y b) si R1, R2 y R4 son simultaneamente H entonces R3 no sea fenilo o fenilo sustituido con O-fenilo o N(Me)2.
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