公开(公告)号：WO2005035525A3

公开(公告)日：2005-10-20

申请号：PCT/US2004029093

申请日：2004-09-07

Applicant: VERTEX PHARMA ,  PERNI ROBERT B ,  COURT JOHN J ,  BRITT SHAWN D ,  PITLIK JANOS ,  VAN DRIE JOHN H

Inventor： PERNI ROBERT B ,  COURT JOHN J ,  BRITT SHAWN D ,  PITLIK JANOS ,  VAN DRIE JOHN H

IPC: A61K31/4178 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K38/00 ,  A61K38/05 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07K5/02 ,  C07K5/06 ,  C07K5/10 ,  C07K7/02 ,  A61P31/14

CPC classification number: C07K5/1016 ,  A01N43/60 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K38/00 ,  A61K45/06 ,  C04B35/632 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07K5/0202 ,  C07K5/0207 ,  C07K5/1027 ,  C07K7/02 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula I-A and I-B that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Abstract translation: 本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式I-A和I-B化合物。 因此，它们通过干扰丙型肝炎病毒的生命周期起作用，并且也可用作抗病毒剂。 本发明还涉及包含这些化合物的组合物，用于离体使用或用于给予HCV感染患者。 本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。 本发明还涉及制备这些化合物的方法。

公开(公告)号：WO2012006055A3

公开(公告)日：2012-03-01

申请号：PCT/US2011042110

申请日：2011-06-28

Applicant: VERTEX PHARMA ,  GREEN JEREMY ,  WILSON DEAN M ,  KONG LAVAL CHAN CHUN ,  DAS SANJOY KUMAR ,  POISSON CARL ,  COURT JOHN J ,  TANG QING ,  LI PAN ,  COLLIER PHILIP N ,  WAAL NATHAN ,  LAUFFER DAVID J ,  DORSCH WARREN

Inventor： GREEN JEREMY ,  WILSON DEAN M ,  KONG LAVAL CHAN CHUN ,  DAS SANJOY KUMAR ,  POISSON CARL ,  COURT JOHN J ,  TANG QING ,  LI PAN ,  COLLIER PHILIP N ,  WAAL NATHAN ,  LAUFFER DAVID J ,  DORSCH WARREN

IPC: C07D333/40 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4535 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  A61P31/12 ,  C07D409/12 ,  C07D413/12 ,  C07D491/08

CPC classification number: C07D413/12 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4535 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07D333/38 ,  C07D409/12 ,  C07D409/14 ,  C07D491/08 ,  C07D491/10

Abstract: A compound is represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract translation: 化合物由结构式（I）或其药学上可接受的盐表示，其中结构式（I）的变量如说明书和权利要求书中所述。 药物组合物包含由结构式（I）表示的化合物或其药学上可接受的盐和赋形剂的药学上可接受的载体。 治疗受试者HCV感染的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。 抑制或降低受试者或生物体外样品中HCV聚合酶活性的方法包括向受试者或样品施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐 。

公开(公告)号：WO2005103050A3

公开(公告)日：2006-10-05

申请号：PCT/US2005011358

申请日：2005-04-04

Applicant: VERTEX PHARMA ,  GREEN JEREMY ,  MILLER ANDREW ,  JIMENEZ JUAN-MIGUEL ,  MARHEFKA CRAIG ,  CAO JINGRONG ,  COURT JOHN J ,  BANDARAGE UPUL K ,  GAO HUAI ,  NANTHAKUMAR SUGANTHINI

Inventor： GREEN JEREMY ,  MILLER ANDREW ,  JIMENEZ JUAN-MIGUEL ,  MARHEFKA CRAIG ,  CAO JINGRONG ,  COURT JOHN J ,  BANDARAGE UPUL K ,  GAO HUAI ,  NANTHAKUMAR SUGANTHINI

IPC: C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P37/08

CPC classification number: C07D471/04

Abstract: The present invention relates to compounds useful as inhibitors of protein 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：WO2005077969A3

公开(公告)日：2005-12-01

申请号：PCT/US2005003381

申请日：2005-02-04

Applicant: VERTEX PHARMA ,  COTTRELL KEVIN M ,  COURT JOHN J ,  DEININGER DAVID D ,  FARMER LUC J ,  PITLIK JANOS ,  PERNI ROBERT B

Inventor： COTTRELL KEVIN M ,  COURT JOHN J ,  DEININGER DAVID D ,  FARMER LUC J ,  PITLIK JANOS ,  PERNI ROBERT B

IPC: A61K38/00 ,  A61K38/04 ,  A61K38/05 ,  C07K5/02 ,  C07K5/04 ,  C07K7/02 ,  C07K14/18 ,  A61K38/07 ,  A61K38/08

CPC classification number: C07K5/10 ,  A61K38/00 ,  A61K38/07 ,  A61K45/06 ,  C07K5/0202 ,  C07K7/02 ,  C07K14/005 ,  C12N2770/24222

Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Abstract translation: 本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的式（I）化合物或其药学上可接受的盐或其混合物。 因此，它们通过干扰丙型肝炎病毒的生命周期起作用，也可用作抗病毒剂。 本发明还涉及包含用于离体使用或用于给予HCV感染患者的这些化合物的组合物和制备该化合物的方法。 本发明还涉及通过施用包含本发明化合物的组合物来治疗患者HCV感染的方法。 本发明还涉及制备这些化合物的方法。

公开(公告)号：AR113753A2

公开(公告)日：2020-06-10

申请号：ARP180102912

申请日：2018-10-09

Applicant: VERTEX PHARMA

Inventor： WANNAMAKER M WOODS ,  WANG TIANSHENG ,  PEROLA EMANUELE ,  MALTAIS FRANCOIS ,  LEDFORD BRIAN ,  LEDEBOER MARK W ,  KENNEDY JOSEPH M ,  JACOBS DYLAN H ,  GU WENXIN ,  GAO HUAI ,  FARMER LUC J ,  DUFFY JOHN P ,  DRUTU IOANA ,  DENG HONGBO ,  COURT JOHN J ,  BETHIEL RANDY S ,  CLARK MICHAEL P ,  CHARIFSON PAUL

IPC: A61K31/437 ,  A61P31/16 ,  C07D471/04

Abstract: Métodos de inhibición de la replicación del virus de la gripe en una muestra biológica o un paciente, de reducción de la cantidad del virus de la gripe en una muestra biológica o un paciente y de tratamiento de gripe en un paciente, que comprende la administración a dicha muestra biológica o paciente de una cantidad efectiva de un compuesto representado por la fórmula estructural (1), o una de sus sales farmacéuticamente aceptables, en donde los valores de la fórmula estructural (1) son como se describen en la presente. Un compuesto está representado por la fórmula estructural (1) o una de sus sales farmacéuticamente aceptables, en donde los valores de la fórmula estructural (1) son como se describen en la presente. Una composición farmacéutica comprende una cantidad efectiva de tal compuesto o su sal farmacéuticamente aceptable y un portador, adyuvante o vehículo farmacéuticamente aceptable.

公开(公告)号：ME03336B

公开(公告)日：2019-10-20

申请号：MEP201955

申请日：2014-03-12

Applicant: VERTEX PHARMA

Inventor： CHARIFSON PAUL ,  DENG HONGBO ,  GU WENXIN ,  GIROUX SIMON ,  JACKSON KATRINA LEE ,  LI PAN ,  XU JINWANG ,  MAXWELL JOHN PATRICK ,  TANG QING ,  RONKIN STEVEN M ,  PIERCE ALBERT CHARLES ,  LAUFFER DAVID J ,  MORRIS MARK A ,  COURT JOHN J ,  COTTRELL KEVIN M ,  WAAL NATHAN D

IPC: A61K31/517 ,  A61P35/00 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D417/12 ,  C07D491/052

公开(公告)号：HRP20190373T1

公开(公告)日：2019-04-19

申请号：HRP20190373

申请日：2019-02-26

Applicant: VERTEX PHARMA

Inventor： MAXWELL JOHN PATRICK ,  CHARIFSON PAUL S ,  TANG QING ,  RONKIN STEVEN M ,  JACKSON KATRINA LEE ,  PIERCE ALBERT CHARLES ,  LAUFFER DAVID J ,  LI PAN ,  GIROUX SIMON ,  XU JINWANG ,  MORRIS MARK A ,  COURT JOHN J ,  COTTRELL KEVIN M ,  DENG HONGBO ,  WAAL NATHAN D ,  GU WENXIN

IPC: C07D403/12 ,  A61K31/517 ,  A61P35/00 ,  C07D405/12 ,  C07D413/04 ,  C07D417/12 ,  C07D491/052

公开(公告)号：AU2014244555B2

公开(公告)日：2018-06-28

申请号：AU2014244555

申请日：2014-03-12

Applicant: VERTEX PHARMA

Inventor： MAXWELL JOHN PATRICK ,  CHARIFSON PAUL S ,  TANG QING ,  RONKIN STEVEN M ,  JACKSON KATRINA LEE ,  PIERCE ALBERT CHARLES ,  LAUFFER DAVID J ,  LI PAN ,  GIROUX SIMON ,  XU JINWANG ,  COTTRELL KEVIN M ,  MORRIS MARK A ,  WAAL NATHAN D ,  COURT JOHN J ,  GU WENXIN ,  DENG HONGBO

IPC: C07D403/12 ,  A61K31/517 ,  A61P35/00 ,  C07D405/12 ,  C07D413/04 ,  C07D417/12 ,  C07D491/052

Abstract: The present invention relates to compounds (I) useful as inhibitors of DNA-PK. 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.

公开(公告)号：CA2764177C

公开(公告)日：2018-06-05

申请号：CA2764177

申请日：2010-06-17

Applicant: VERTEX PHARMA

Inventor： CHARIFSON PAUL ,  CLARK MICHAEL P ,  BANDARAGE UPUL K ,  BETHIEL RANDY S ,  COURT JOHN J ,  DENG HONGBO ,  DRUTU IOANA ,  DUFFY JOHN P ,  FARMER LUC J ,  GAO HUAI ,  GU WENXIN ,  JACOBS DYLAN H ,  KENNEDY JOSEPH M ,  LEDEBOER MARK W ,  LEDFORD BRIAN ,  MALTAIS FRANCOIS ,  PEROLA EMANUELE ,  WANG TIANSHENG ,  WANNAMAKER M WOODS ,  BYRN RANDAL ,  ZHOU YI ,  LIN CHAO ,  JIANG MIN ,  JONES STEVEN ,  GERMANN URSULA A ,  SALITURO FRANCESCO G ,  KWONG ANN DAK-YEE

IPC: C07D471/04 ,  A61K31/506 ,  A61P31/16

Abstract: Methods of inhibiting the replica-tion 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 in-fluenza 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 (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically ac-ceptable salt thereof, wherein the values of Struc-tural Formula (IA) are as described herein. A phar-maceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically ac-ceptable carrier, adjuvant or vehicle.

公开(公告)号：HRP20161577T1

公开(公告)日：2017-01-27

申请号：HRP20161577

申请日：2016-11-28

Applicant: VERTEX PHARMA

Inventor： CHARIFSON PAUL ,  CLARK MICHAEL P ,  BANDARAGE UPUL K ,  BETHIEL RANDY S ,  COURT JOHN J ,  DENG HONGBO ,  DRUTU IOANA ,  DUFFY JOHN P ,  FARMER LUC ,  GAO HUAI ,  GU WENXIN ,  JACOBS DYLAN H ,  KENNEDY JOSEPH M ,  LEDEBOER MARK W ,  LEDFORD BRIAN ,  MALTAIS FRANCOIS ,  PEROLA EMANUELE ,  WANG TIANSHENG ,  WANNAMAKER M WOODS ,  BYRN RANDAL ,  ZHOU YI ,  LIN CHAO ,  JIANG MIN ,  GERMANN URSULA A ,  JONES STEVEN ,  SALITURO FRANCESCO G ,  KWONG ANN DAK-YEE

IPC: A61K31/506 ,  A61P31/16