公开(公告)号：JP2013253114A

公开(公告)日：2013-12-19

申请号：JP2013196681

申请日：2013-09-24

Applicant: VERTEX PHARMA

Inventor： LEDEBOER MARK W ,  WANNAMAKER MARION W ,  FARMER LUC J ,  WANG TIANSHENG ,  PIERCE ALBERT C ,  MARTINEZ-BOTELLA GABRIEL ,  BETHIEL RANDY S ,  BEMIS GUY W ,  WANG JIAN ,  SALITURO FRANCESCO G ,  ARNOST MICHAEL J ,  COME JON H ,  GREEN JEREMY ,  STEWART MICHELLE ,  MARHEFKA CRAIG

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61K31/551 ,  A61K45/00 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P15/06 ,  A61P15/10 ,  A61P17/06 ,  A61P17/14 ,  A61P19/00 ,  A61P19/10 ,  A61P21/00 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D519/00 ,  C12N9/99 ,  C12Q1/48

Abstract: PROBLEM TO BE SOLVED: To provide pyrrolopyridine compounds useful as inhibitors of protein kinase.SOLUTION: The present invention relates to compounds of formula (I) (wherein Q, Z, R, Rand Rare described in specification), useful as inhibitors of protein kinases, particularly of JAK family and ROCK family kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：WO2004058769A3

公开(公告)日：2004-09-30

申请号：PCT/US0339990

申请日：2003-12-17

Applicant: VERTEX PHARMA ,  GREEN JEREMY ,  GREY RONALD JR ,  PIERCE ALBERT C

Inventor： GREEN JEREMY ,  GREY RONALD JR ,  PIERCE ALBERT C

IPC: A61K31/495 ,  A61K31/503 ,  A61K31/5377 ,  A61K31/541 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K31/495 ,  A61K31/503 ,  A61K31/5377 ,  A61K31/541

Abstract: The present invention provides a compound of formula (I), or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of PIM-1, CDK-2, GSK-3, and SRC mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.

Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐。 这些化合物是蛋白激酶的抑制剂，特别是PIM-1，CDK-2，GSK-3和SRC哺乳动物蛋白激酶的抑制剂。 本发明还提供包含本发明化合物的药学上可接受的组合物和利用这些化合物和组合物治疗各种蛋白激酶介导的病症的方法。

公开(公告)号：WO02102800A9

公开(公告)日：2004-05-06

申请号：PCT/US0219186

申请日：2002-06-14

Applicant: VERTEX PHARMA ,  MOON YOUNG CHOON ,  GREEN JEREMY ,  DAVIES ROBERT ,  CHOQUETTE DEB ,  PIERCE ALBERT ,  LEDEBOER MARK

Inventor： MOON YOUNG CHOON ,  GREEN JEREMY ,  DAVIES ROBERT ,  CHOQUETTE DEB ,  PIERCE ALBERT ,  LEDEBOER MARK

IPC: A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/635 ,  A61L27/00 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/06 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D413/04 ,  C07D413/14 ,  A61K31/505 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D413/04 ,  C07D413/14

Abstract: Described herein are benzisoxazole compounds of formula I or a pharmaceutically acceptable derivative or prodrug thereof, wherein A-B is N-O or O-N; Ar is an optionally substituted C5-10 aryl group; R is hydrogen or an optionally substituted group selected from C1-I0 aliphatic, C5-10 aryl, C6-12 aralkyl, C3-10 heterocyclyl, or C4-12 heterocyclylalkyl; and T, n, R and R are as described in the specification. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3 and JAK mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various -, protein kinase mediated disorders.

Abstract translation: 本文描述的是式I的苯并异恶唑化合物或其药学上可接受的衍生物或前药，其中A-B是N-O或O-N; Ar是任选取代的C 5-10芳基; R 1是氢或选自C 1-10脂族，C 5-10芳基，C 6-12芳烷基，C 3-10杂环基或C 4-12杂环基烷基的任选取代的基团; 和T，n，R 2和R 3如说明书中所述。 这些化合物是蛋白激酶的抑制剂，特别是GSK-3和JAK哺乳动物蛋白激酶的抑制剂。 本发明还提供包含本发明化合物的药学上可接受的组合物以及利用这些化合物和组合物治疗各种蛋白激酶介导的病症的方法。

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：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：WO2012024363A3

公开(公告)日：2012-05-31

申请号：PCT/US2011048027

申请日：2011-08-17

Applicant: VERTEX PHARMA ,  GREEN JEREMY ,  KONG LAVAL CHAN CHUN ,  DAS SANJOY KUMAR ,  POISSON CARL ,  NANTHAKUMAR SUGANTHINI ,  WAAL NATHAN ,  LI PAN ,  RONKIN STEVEN ,  LAUFFER DAVID J ,  WILSON DEAN M

Inventor： GREEN JEREMY ,  KONG LAVAL CHAN CHUN ,  DAS SANJOY KUMAR ,  POISSON CARL ,  NANTHAKUMAR SUGANTHINI ,  WAAL NATHAN ,  LI PAN ,  RONKIN STEVEN ,  LAUFFER DAVID J ,  WILSON DEAN M

IPC: C07D333/38 ,  A61K31/381 ,  A61P31/12 ,  C07D333/40 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: A61K31/427 ,  A61K31/381 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/4436 ,  A61K31/4535 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/7056 ,  A61K38/212 ,  C07D333/38 ,  C07D333/40 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 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 selected from the structural formulae depicted in FIG. 1 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 selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.

Abstract translation: 化合物选自图1中所示的结构式。 1或其药学上可接受的盐。 药物组合物包含选自图1中描绘的结构式的化合物。 1或其药学上可接受的盐和赋形剂的药学上可接受的载体。 治疗受试者的HCV感染的方法包括向受试者施用治疗有效量的选自图1中描述的结构式的治疗有效量的化合物。 1或其药学上可接受的盐。 抑制或降低受试者中或生物体外样品中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选自图1中描述的结构式的治疗有效量。 1或其药学上可接受的盐。

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：WO2004072029A3

公开(公告)日：2004-12-16

申请号：PCT/US2004003061

申请日：2004-02-04

Applicant: VERTEX PHARMA ,  GREEN JEREMY ,  GREY RONALD ,  PIERCE ALBERT C

Inventor： GREEN JEREMY ,  GREY RONALD ,  PIERCE ALBERT C

IPC: A61K31/5025 ,  A61K31/503 ,  A61K31/5377 ,  A61K31/541 ,  A61P3/10 ,  A61P25/28 ,  C07D20060101 ,  C07D487/02 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors of GSK-3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐或其混合物。 这些化合物是蛋白激酶的抑制剂，特别是GSK哺乳动物蛋白激酶的抑制剂，特别是GSK-3哺乳动物蛋白激酶的抑制剂。 本发明还提供包含本发明化合物的药学上可接受的组合物和利用这些化合物和组合物治疗各种蛋白激酶介导的病症的方法。

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：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 。