公开(公告)号：WO2012083122A8

公开(公告)日：2013-12-05

申请号：PCT/US2011065389

申请日：2011-12-16

Applicant: VERTEX PHARMA ,  CHARIFSON PAUL S ,  CLARK MICHAEL P ,  BANDARAGE UPUL K ,  DENG HONGBO ,  DAVIES IOANA ,  DUFFY JOHN P ,  FARMER LUC J ,  GAO HUAI ,  GU WENXIN ,  KENNEDY JOSEPH M ,  LEDEBOER MARK W ,  LEDFORD BRIAN ,  MALTAIS FRANCOIS ,  PEROLA EMANUELE ,  WANNAMAKER MARION W ,  WANG TIANSHENG ,  SALITURO FRANCESCO G

Inventor： CHARIFSON PAUL S ,  CLARK MICHAEL P ,  BANDARAGE UPUL K ,  DENG HONGBO ,  DAVIES IOANA ,  DUFFY JOHN P ,  FARMER LUC J ,  GAO HUAI ,  GU WENXIN ,  KENNEDY JOSEPH M ,  LEDEBOER MARK W ,  LEDFORD BRIAN ,  MALTAIS FRANCOIS ,  PEROLA EMANUELE ,  WANNAMAKER MARION W ,  WANG TIANSHENG ,  SALITURO FRANCESCO G

IPC: C07D471/04 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53

CPC classification number: C07D471/04

Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

Abstract translation: 抑制生物样品或患者中流感病毒的复制，减少生物样品或患者中流感病毒的量以及治疗患者中的流感的方法包括向所述生物样品或患者施用有效量的 由结构式（I）表示的化合物或其药学上可接受的盐，其中结构式（I）的值如本文所述。 结构式（I）表示的化合物或其药学上可接受的盐，其中结构式（I）的值如本文所述。 药物组合物包含有效量的这样的化合物或其药学上可接受的盐和药学上可接受的载体，助剂或媒介物。

公开(公告)号：WO0102358A3

公开(公告)日：2001-07-12

申请号：PCT/US0018418

申请日：2000-07-05

Applicant: VERTEX PHARMA ,  LAUFFER DAVID ,  MULLICAN MICHAEL ,  LEDFORD BRIAN

Inventor： LAUFFER DAVID ,  MULLICAN MICHAEL ,  LEDFORD BRIAN

IPC: C07D243/12 ,  A61K31/4015 ,  A61K31/45 ,  A61K31/4545 ,  A61K31/55 ,  A61K31/5513 ,  A61K38/27 ,  A61P19/08 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/16 ,  A61P25/28 ,  C07D207/26 ,  C07D207/273 ,  C07D211/76 ,  C07D223/12 ,  C07D223/16 ,  C07D243/14 ,  C07D243/24 ,  C07D401/06 ,  C07D401/14 ,  A61K31/554 ,  C07D211/72 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D207/273 ,  C07D211/76 ,  C07D223/16 ,  C07D243/24 ,  C07D401/14

Abstract: The present invention relates to cyclized amide derivatives of formula (I) for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract translation: 本发明涉及用于治疗或预防与神经疾病相关的神经元损伤的式（I）的环化酰胺衍生物。 本发明还提供包含本发明化合物的组合物和利用这些组合物治疗或预防神经元损伤的方法。

公开(公告)号：WO2015027005A1

公开(公告)日：2015-02-26

申请号：PCT/US2014051988

申请日：2014-08-21

Applicant: VERTEX PHARMA

Inventor： BRUMMEL CHRISTOPHER LEE ,  MALTAIS FRANCOIS ,  DEININGER DAVID D ,  LEDFORD BRIAN ,  DORSCH WARREN

IPC: C07D239/95 ,  C07B59/00 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07B59/002 ,  C07D239/42 ,  C07D239/95 ,  C07F5/025

Abstract: The present invention relates to a deuterated pyrrolo[2,3-b]pyridinyl compound that is useful for inhibiting Janus kinases. The invention also relates to processes and intermediates useful for preparing such a compound.

Abstract translation: 本发明涉及用于抑制Janus激酶的氘代吡咯并[2,3-b]吡啶基化合物。 本发明还涉及可用于制备这种化合物的方法和中间体。

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。

公开(公告)号：WO2007111904A3

公开(公告)日：2007-12-13

申请号：PCT/US2007007016

申请日：2007-03-21

Applicant: VERTEX PHARMA ,  LAUFFER DAVID J ,  DAVIES ROBERT J ,  STAMOS DEAN ,  ARONOV ALEXANDER ,  DEININGER DAVID D ,  GREY RONALD JR ,  XU JINWANG ,  LI PAN ,  LEDFORD BRIAN ,  FARMER LUC ,  BETHIEL RANDY SCOTT ,  JACOBS DYLAN ,  MCGINTY KIRA

Inventor： LAUFFER DAVID J ,  DAVIES ROBERT J ,  STAMOS DEAN ,  ARONOV ALEXANDER ,  DEININGER DAVID D ,  GREY RONALD JR ,  XU JINWANG ,  LI PAN ,  LEDFORD BRIAN ,  FARMER LUC ,  BETHIEL RANDY SCOTT ,  JACOBS DYLAN ,  MCGINTY KIRA

IPC: C07D401/04 ,  A61K31/4439 ,  A61K31/497 ,  A61K35/00 ,  A61P35/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04

CPC classification number: C07D417/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D407/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D451/02 ,  C07D451/06 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D495/04 ,  C07D498/08 ,  C07D513/04 ,  C12N9/99

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.

Abstract translation: 本发明涉及可用于蛋白激酶抑制剂的化合物。 本发明还提供了制备本发明化合物的方法，包含本发明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的方法。

公开(公告)号：WO0102363A3

公开(公告)日：2001-07-05

申请号：PCT/US0018564

申请日：2000-07-06

Applicant: VERTEX PHARMA ,  LAUFFER DAVID ,  LEDFORD BRIAN ,  MULLICAN MICHAEL

Inventor： LAUFFER DAVID ,  LEDFORD BRIAN ,  MULLICAN MICHAEL

IPC: A61K31/4409 ,  A61K31/444 ,  A61K38/22 ,  A61P9/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  C07D213/40 ,  A61K31/4465

CPC classification number: C07D213/40

Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract translation: 本发明涉及用于治疗或预防与神经疾病相关的神经元损伤的N-取代甘氨酸衍生物。 本发明还提供了包含本发明化合物的组合物和利用这些组合物治疗或预防神经元损伤的方法。

公开(公告)号：WO2008027584A3

公开(公告)日：2008-06-19

申请号：PCT/US2007019261

申请日：2007-09-04

Applicant: VERTEX PHARMA ,  WANG TIANSHENG ,  GREEN JEREMY ,  CORNEBISE MARK ,  LEDFORD BRIAN ,  PARSONS JONATHAN ,  TANNER ADAM ,  WESTCOTT JAMES

Inventor： WANG TIANSHENG ,  GREEN JEREMY ,  CORNEBISE MARK ,  LEDFORD BRIAN ,  PARSONS JONATHAN ,  TANNER ADAM ,  WESTCOTT JAMES

IPC: C07D417/04 ,  A61K31/427 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D417/04

Abstract: The present invention relates to compounds of formula (I) useful as inhibitors of P13K particularly of P13K?. 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P13K特别是P13Kα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。

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。

公开(公告)号：WO2004016597A3

公开(公告)日：2004-04-22

申请号：PCT/US0325333

申请日：2003-08-12

Applicant: VERTEX PHARMA ,  COCHRAN JOHN ,  GREEN JEREMY ,  HALE MICHAEL R ,  LEDFORD BRIAN ,  MALTAIS FRANCOIS ,  NANTHAKUMAR SUGANTHINI

Inventor： COCHRAN JOHN ,  GREEN JEREMY ,  HALE MICHAEL R ,  LEDFORD BRIAN ,  MALTAIS FRANCOIS ,  NANTHAKUMAR SUGANTHINI

IPC: C07D239/00 ,  A61P19/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D213/74 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/505 ,  A61K31/506

CPC classification number: C07D213/74 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formulae (I) and (V) or a pharmaceutically acceptable salt thereof, wherein Ring B, Z , Z U, T, m, n, p, Q, Q', R , R , R , R , and R are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplantation.

Abstract translation: 本文描述了可用作具有式（I）和（V）的蛋白激酶抑制剂或其药学上可接受的盐的化合物，其中环B，Z 1，Z 2 U，T，m，n ，p，Q，Q'，R 1，R 2，R x，R 3和R 6如本文所定义。 这些化合物及其药学上可接受的组合物可用于治疗或减轻各种疾病的严重程度，包括中风，炎性疾病，自身免疫疾病如SLE红斑狼疮和牛皮癣，增殖性疾病如癌症和与器官移植相关的病症 。

公开(公告)号：BR112021011564A2

公开(公告)日：2021-08-31

申请号：BR112021011564

申请日：2019-12-17

Applicant: VERTEX PHARMA

Inventor： MEDEK ALES ,  FORTIER ANNE ,  LEDFORD BRIAN ,  SAYEGH CAMIL ,  ELAINE B KRUEGER ,  WITKOS FAITH ,  DENIS FRANCOIS ,  CAO JINGRONG ,  JON H COME ,  HU KAN-NIAN ,  GAGNON KEVIN ,  LESLIE A DAKIN ,  HAMEL MARTINE ,  BRODNEY MICHAEL ,  SHRESTHA MUNA ,  NICOLAS OLIVIER ,  ROSE PETER ,  SUGANTHINI S NANTHAKUMAR ,  WANG TIANSHENG ,  TIMOTHY J SENTER ,  WARREN A DORSCH ,  SHI YI

IPC: C07D403/12 ,  A61K31/4025 ,  A61P13/12

Abstract: inibidores de apol1 e métodos de uso dos mesmos. trata-se de pelo menos uma entidade escolhida dentre os compostos de fórmula (i), formas de estado sólido dos mesmos, composições que compreendem os mesmos e métodos para usar os mesmos, incluindo o uso no tratamento de glomeruloesclerose segmentar focal (gesf) e/ou doença renal não diabética (ndkd).