公开(公告)号：WO2007025307A3

公开(公告)日：2007-04-26

申请号：PCT/US2006033770

申请日：2006-08-28

Applicant: VERTEX PHARMA ,  COTTRELL KEVIN M ,  MAXWELL JOHN ,  TANG QING ,  GRILLOT ANNE-LAURE ,  LE TIRAN ARNAUD ,  PEROLA EMANUELE

Inventor： COTTRELL KEVIN M ,  MAXWELL JOHN ,  TANG QING ,  GRILLOT ANNE-LAURE ,  LE TIRAN ARNAUD ,  PEROLA EMANUELE

IPC: C07D498/10 ,  C07K5/08

CPC classification number: C07D498/10 ,  A61K38/00 ,  C07D498/20 ,  C07D519/00 ,  C07K5/06026 ,  C07K5/06191 ,  C07K5/0804 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0827

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.

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混合物。

公开(公告)号：WO0157022A2

公开(公告)日：2001-08-09

申请号：PCT/US0103911

申请日：2001-02-05

Applicant: VERTEX PHARMA ,  GREEN JEREMY ,  CAO JINGRONG ,  HALE MICHAEL ,  BAKER CHRISTOPHER ,  MALTAIS FRANCOIS ,  JANETKA JAMES ,  MULLICAN MICHAEL ,  BEMIS GUY ,  XIE XIAOLING ,  STRAUB JUDITH ,  TANG QING ,  MASHALL ROBERT

Inventor： GREEN JEREMY ,  CAO JINGRONG ,  HALE MICHAEL ,  BAKER CHRISTOPHER ,  MALTAIS FRANCOIS ,  JANETKA JAMES ,  MULLICAN MICHAEL ,  BEMIS GUY ,  XIE XIAOLING ,  STRAUB JUDITH ,  TANG QING ,  MASHALL ROBERT

IPC: A61B17/00 ,  A61F2/02 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/00 ,  A61L27/00 ,  A61P1/00 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/00 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/04 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D231/38 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D403/00

CPC classification number: C07D401/14 ,  C07D231/38 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: (I) where R , Q, and T are described inthe specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract translation: 本文描述了可用作具有下式的蛋白激酶抑制剂的化合物：其中R 1-4，Q和T在说明书中描述。 该化合物可用于治疗由蛋白激酶抑制剂，特别是诸如癌症，炎症性疾病，再狭窄和心血管疾病等疾病减轻的哺乳动物的疾病状态。

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：WO02064586A2

公开(公告)日：2002-08-22

申请号：PCT/US0203791

申请日：2002-02-08

Applicant: VERTEX PHARMA ,  CAO JINGRONG ,  GREEN JEREMY ,  HALE MICHAEL ,  MALTAIS FRANCOIS ,  STRAUB JUDY ,  TANG QING ,  ARONOV ALEX

Inventor： CAO JINGRONG ,  GREEN JEREMY ,  HALE MICHAEL ,  MALTAIS FRANCOIS ,  STRAUB JUDY ,  TANG QING ,  ARONOV ALEX

IPC: A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/16 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P17/06 ,  A61P19/00 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula (I) wherein Z and Z are each independently nitrogen or CH and Ring A, TmR , QR , UnR , and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

Abstract translation: 本文描述了可用作具有式（I）的蛋白激酶抑制剂的化合物，其中Z 1和Z 2各自独立地为氮或CH，环A，TmR 1，QR 2，UnR 3 >和Sp如说明书中所述。 该化合物特别可用作ERK2的抑制剂，并且用于治疗由蛋白激酶抑制剂，特别是癌症，炎性疾病，再狭窄，糖尿病和心血管疾病等疾病缓解的哺乳动物疾病。

公开(公告)号：WO2009045992A2

公开(公告)日：2009-04-09

申请号：PCT/US2008078239

申请日：2008-09-30

Applicant: VERTEX PHARMA ,  LAUFFER DAVID ,  LI PAN ,  WAAL NATHAN ,  MCGINTY KIRA ,  TANG QING ,  RONKIN STEVEN ,  FARMER LUC ,  SHANNON DEAN ,  JACOBS DYLAN

Inventor： LAUFFER DAVID ,  LI PAN ,  WAAL NATHAN ,  MCGINTY KIRA ,  TANG QING ,  RONKIN STEVEN ,  FARMER LUC ,  SHANNON DEAN ,  JACOBS DYLAN

IPC: A61K31/4439

CPC classification number: C07D401/14 ,  C07D409/14 ,  C07D417/14

Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders. Formula (I).

Abstract translation: 本发明涉及用于抑制c-Met蛋白激酶的式I化合物。 本发明还提供了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增殖性疾病的方法。 公式（I）。

公开(公告)号：WO03011855A3

公开(公告)日：2003-09-25

申请号：PCT/US0224725

申请日：2002-08-02

Applicant: VERTEX PHARMA ,  HALE MICHAEL ROBIN ,  JANETKA JAMES WALTER ,  MALTAIS FRANCOIS ,  TANG QING

Inventor： HALE MICHAEL ROBIN ,  JANETKA JAMES WALTER ,  MALTAIS FRANCOIS ,  TANG QING

IPC: A61K31/4155 ,  A61K45/00 ,  A61L27/00 ,  A61P1/16 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P17/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D403/04

CPC classification number: C07D403/04

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula (I) wherein B, R , n, R , Q and R are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract translation: 本文描述了可用作具有式（I）的蛋白激酶抑制剂的化合物，其中B，R 1，n，R 3，Q和R 4在说明书中描述。 该化合物可用于治疗由蛋白激酶抑制剂，特别是诸如癌症，炎症性疾病，再狭窄和心血管疾病等疾病减轻的哺乳动物的疾病状态。

公开(公告)号：WO2006071644A8

公开(公告)日：2006-08-24

申请号：PCT/US2005046177

申请日：2005-12-20

Applicant: VERTEX PHARMA ,  ARONOV ALEX ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  MARTINEZ-BOTELLA GABRIEL ,  STRAUB JUDITH ,  TANG QING

Inventor： ARONOV ALEX ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  MARTINEZ-BOTELLA GABRIEL ,  STRAUB JUDITH ,  TANG QING

IPC: C07D403/04 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D403/04

Abstract: Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferate disorders such as cancer.

Abstract translation: 本文描述的是可用作ERK2抑制剂的化合物。 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病症（包括增殖性疾病如癌症）的严重性。

公开(公告)号：WO2006065820A2

公开(公告)日：2006-06-22

申请号：PCT/US2005045079

申请日：2005-12-13

Applicant: VERTEX PHARMA ,  MARTINEZ-BOTELLA GABRIEL ,  ARONOV ALEX ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  STRAUB JUDITH ,  TANG QING

Inventor： MARTINEZ-BOTELLA GABRIEL ,  ARONOV ALEX ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  STRAUB JUDITH ,  TANG QING

CPC classification number: C07D239/48

Abstract: Described herein are compounds that are useful as protein kinase inhibitors of formula (I); or a pharmaceutically acceptable salt thereof, wherein Ring A, Z 1 , Z 2 , U, Q, R 1 , R 2 , and L 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 proliferative disorders such as cancer.

Abstract translation: 本文描述的是可用作式（I）的蛋白激酶抑制剂的化合物; 或其药学上可接受的盐，其中环A，Z 1，Z 2，U，Q，R 1，R 2， 和/或L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病症（包括增殖性疾病如癌症）的严重性。

公开(公告)号：HUE067936T2

公开(公告)日：2024-11-28

申请号：HUE22161962

申请日：2019-04-23

Applicant: MERCK PATENT GMBH ,  VERTEX PHARMA

Inventor： KULKARNI SHASHANK ,  YU HENRY ,  CLARK MICHAEL ,  BEMIS GUY ,  BOYD MICHAEL ,  CHANDUPATLA KISHAN ,  COLLIER PHILIP ,  DENG HONGBO ,  DONG HUIJUN ,  DORSCH WARREN ,  HOOVER RUSSELL ,  JOHNSON MAC ,  PENNEY MARINA ,  RONKIN STEVEN ,  TAKEMOTO DARIN ,  TANG QING ,  WAAL NATHAN ,  WANG TIANSHENG ,  LAUFFER DAVID J ,  LI PAN

IPC: C07D413/14 ,  A61P35/00 ,  C07D403/04 ,  C07D409/14 ,  C07D413/04

公开(公告)号：AU2021247285A1

公开(公告)日：2022-10-27

申请号：AU2021247285

申请日：2021-04-02

Applicant: VERTEX PHARMA

Inventor： GIROUX SIMON ,  NUHANT PHILIPPE MARCEL ,  BANDARAGE UPUL KEERTHI ,  GARCIA BARRANTES PEDRO MANUEL ,  LIAO YUSHENG ,  GALE-DAY ZACHARY ,  GU WENXIN ,  KARNS ALEXANDER S ,  ZHANG HU ,  ALLEN EMILY ELIZABETH ,  XU JINWANG ,  DENINNO MICHAEL PAUL ,  TANG QING ,  BOUCHER DIANE MARIE ,  FANNING LEV T D ,  HALL AMY B ,  HURLEY DENNIS JAMES ,  JOHNSON JR MAC ARTHUR ,  MAXWELL JOHN PATRICK ,  SWETT REBECCA JANE ,  TAPLEY TIMOTHY LEWIS ,  THOMSON STEPHEN A ,  DAMAGNEZ VERONIQUE ,  COTTRELL KEVIN MICHAEL

IPC: C07D471/04 ,  A61K31/4745 ,  A61P1/00 ,  A61P1/14 ,  A61P1/16 ,  A61P11/00 ,  A61P11/08 ,  A61P11/10 ,  A61P17/00 ,  A61P31/00 ,  A61P31/02 ,  A61P35/00

Abstract: 1H-pyrazolo[4,3-g]isoquinoline and 1H-pyrazolo[4,3-g]quinoline derivatives as alpha-1-antitrypsin modulators for treating alpha-1- antitrypsin deficiency (AATD).