公开(公告)号：WO2007056164A3

公开(公告)日：2007-12-13

申请号：PCT/US2006042994

申请日：2006-11-03

Applicant: VERTEX PHARMA ,  BINCH HAYLEY ,  MORTIMORE MICHAEL ,  FRAYSSE DAMIEN ,  DAVIS CHRIS ,  O'DONNELL MICHAEL ,  EVERITT SIMON ,  ROBINSON DANIEL ,  PINDER JOANNE ,  MILLER ANDREW

Inventor： BINCH HAYLEY ,  MORTIMORE MICHAEL ,  FRAYSSE DAMIEN ,  DAVIS CHRIS ,  O'DONNELL MICHAEL ,  EVERITT SIMON ,  ROBINSON DANIEL ,  PINDER JOANNE ,  MILLER ANDREW

IPC: A61K31/66 ,  A01N43/54 ,  A01N57/00

CPC classification number: C07D403/12 ,  C07D239/38 ,  C07D401/14 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

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

Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物以及使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。

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：WO02057259A3

公开(公告)日：2003-04-24

申请号：PCT/US0149401

申请日：2001-12-19

Applicant: VERTEX PHARMA ,  BEBBINGTON DAVID ,  CHARRIER JEAN-DAMIEN ,  GOLEC JULIAN ,  MILLER ANDREW ,  KNEGTEL RONALD

Inventor： BEBBINGTON DAVID ,  CHARRIER JEAN-DAMIEN ,  GOLEC JULIAN ,  MILLER ANDREW ,  KNEGTEL RONALD

IPC: C12N9/99 ,  A61K20060101 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/00 ,  A61P20060101 ,  A61P1/00 ,  A61P3/08 ,  A61P3/10 ,  A61P3/14 ,  A61P5/00 ,  A61P5/18 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P17/14 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/00 ,  A61P21/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P31/20 ,  A61P31/22 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D20060101 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D521/00

CPC classification number: C07D403/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

Abstract: This invention describes novel pyrazole compounds of formula (IIIa), wherein R is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R , R , R , and R are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract translation: 本发明描述了式（IIIa）的新型吡唑化合物，其中R 1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环 ; R x，R y，R 2和R 2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。

公开(公告)号：WO02094263A3

公开(公告)日：2003-03-27

申请号：PCT/US0216353

申请日：2002-05-23

Applicant: VERTEX PHARMA ,  MORTIMORE MICHAEL ,  MILLER ANDREW ,  STUDLEY JOHN ,  CHARRIER JEAN-DAMIEN

Inventor： MORTIMORE MICHAEL ,  MILLER ANDREW ,  STUDLEY JOHN ,  CHARRIER JEAN-DAMIEN

IPC: A61K31/404 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/407 ,  A61K31/435 ,  A61K31/45 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/538 ,  A61K31/54 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/00 ,  A61P3/10 ,  A61P7/00 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/00 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P27/00 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P39/02 ,  A61P43/00 ,  C07D209/86

CPC classification number: A61K31/55 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/407 ,  A61K31/435 ,  A61K31/45 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/538 ,  A61K31/54

Abstract: This invention provides compounds of formula (I): wherein Z is oxygen or sulfu; R is hydrogen, -CHN2, R, CH2OR, CH2SR, or -CH2Y; --- next to R represents a single or double bond; Y is an electronegative leaving group; R is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R is a group capable of fitting into the S2 subsite or a caspase enzyme; R is hydrogen or C1-6alkyl or R and R taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1 beta secretion.

Abstract translation: 本发明提供式（I）化合物：其中Z是氧或磺基; R 1是氢，-CHN 2，R 1，CH 2 OR，CH 2 SR或-CH 2 Y; --- R 3独立表示单键或双键; Y是电负离子团; R 2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体异构体; R 3是能够适合S2亚位点或胱天蛋白酶的基团; R 4是氢或C 1-6烷基或R 3和R 4一起形成环; 环A和环B各自为杂环，R和R 5如说明书所述。 这些化合物是凋亡和IL-1β分泌的有效抑制剂。

公开(公告)号：EP1948193A4

公开(公告)日：2011-11-09

申请号：EP06836890

申请日：2006-11-03

Applicant: VERTEX PHARMA

Inventor： BINCH HAYLEY ,  MORTIMORE MICHAEL ,  FRAYSSE DAMIEN ,  DAVIS CHRIS ,  O'DONNELL MICHAEL ,  EVERITT SIMON ,  ROBINSON DANIEL ,  PINDER JOANNE ,  MILLER ANDREW

IPC: C07D401/14 ,  A61K31/505 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D403/12 ,  C07D239/38 ,  C07D401/14 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

公开(公告)号：HK1215256A1

公开(公告)日：2016-08-19

申请号：HK16103327

申请日：2016-03-22

Applicant: VERTEX PHARMA

Inventor： BOYALL DEAN ,  DAVIS CHRISTOPHER ,  DODD JAMES ,  EVERITT SIMON ,  MILLER ANDREW ,  WEBER PETER ,  WESTCOTT JAMES ,  YOUNG STEPHEN ,  SETTIMO LUCA

IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101

公开(公告)号：AU2013348167A1

公开(公告)日：2015-05-28

申请号：AU2013348167

申请日：2013-11-19

Applicant: VERTEX PHARMA

Inventor： BOYALL DEAN ,  DAVIS CHRISTOPHER ,  DODD JAMES ,  EVERITT SIMON ,  MILLER ANDREW ,  WEBER PETER ,  WESTCOTT JAMES ,  YOUNG STEPHEN ,  SETTIMO LUCA

IPC: C07D403/12 ,  A61K31/4192 ,  A61P35/00 ,  C07D249/10 ,  C07D401/12 ,  C07D413/12

Abstract: The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications.. The compounds of this invention have formula I-A; wherein the variables are as defined herein.

公开(公告)号：AU2014203289A1

公开(公告)日：2014-07-17

申请号：AU2014203289

申请日：2014-06-18

Applicant: VERTEX PHARMA

Inventor： JIMENEZ JUAN-MIGUEL ,  MILLER ANDREW ,  GREEN JEREMY ,  GAO HUAI ,  HENKEL GREGORY ,  LIU MICHAEL ,  NEUBERGER TIMOTHY

IPC: C07D403/12 ,  A61K31/506 ,  A61P3/10 ,  A61P25/00 ,  C07D471/04

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

公开(公告)号：NZ606259A

公开(公告)日：2014-06-27

申请号：NZ60625906

申请日：2006-11-03

Applicant: VERTEX PHARMA

Inventor： ROBINSON DANIEL ,  BINCH HAYLEY ,  DAVIS CHRIS ,  MILLER ANDREW ,  RUTHERFORD ALISTAIR ,  EVERITT SIMON ,  O’DONNELL MICHAEL ,  FRAYSSE DAMIEN ,  PINDER JOANNE ,  STUDLEY JOHN ,  BOYALL DEAN ,  MORTIMORE MICHAEL ,  RAMAYA SHARN

IPC: A01N57/00 ,  A01N43/54 ,  A61K31/66

Abstract: Disclosed is N-(5-(4-(3-methyl-1H-pyrazol-5-ylamino)-6-(3-cyclopropyl-3-fluoroazetidin-2-yl)pyrimidin-2-ylthio)pyridin-2-yl)-3,3,3- trifluoropropanamide represented by structural formula (I-21) or a pharmaceutically acceptable salt thereof, which inhibit Aurora protein kinase activity and are suitable for treating a proliferative disorder is selected from melanoma, myeloma, leukemia, lymphoma, neuroblastoma, or a cancer selected from colon, breast, gastric, ovarian, cervical, lung, central nervous system, renal, prostate, bladder, pancreatic, brain, head and neck, kidney, liver, melanoma, sarcoma, or thyroid cancer.

公开(公告)号：ES2435997T3

公开(公告)日：2013-12-26

申请号：ES08731830

申请日：2008-03-10

Applicant: VERTEX PHARMA

Inventor： JIMENEZ JUAN-MIGUEL ,  MILLER ANDREW ,  GREEN JEREMY ,  GAO HUAI ,  HENKEL GREGORY ,  LIU MICHAEL ,  NEUBERGER TIMOTHY

IPC: C07D403/12 ,  A61K31/506 ,  A61P3/10 ,  A61P25/00 ,  C07D471/04

Abstract: Un compuesto de fórmula I:**Fórmula** o una de sus sales farmacéuticamente aceptables, donde: Ht es**Fórmula** donde cualquier carbono sustituible de Ht está independiente y opcionalmente sustituido con -R10; el anillo D es un cicloalifático o heterociclilo de 3 a 10 miembros; donde dicho heterociclilo contiene 1 a 2heteroátomos elegidos entre O, N o S; y donde el cicloalifático o heterociclilo está independiente y opcionalmentesustituido con 1 a 5 -R5; el anillo D está enlazado a la pirimidina a través de un átomo de carbono; Z1 es N, CH o CR10; RX es H, halo o C1-6alquilo, donde el alquilo está independiente y opcionalmente sustituido con 1 a 5 grupos elegidosentre halo, -CN y -OR; RY es H, halo, C1-6alquilo o un anillo heterociclilo de 5 a 6 miembros que contiene 1 a 2 heteroátomos elegidos entreO, N o S; donde dicho RY está independiente y opcionalmente sustituido con 1 a 4 halo, CN, OR o C1-6alquilo; cada R10 se elige independientemente entre C1-6alquilo, haloC1-6alquilo, halo, OR, C(>=O)R, CO2R, COCOR, NO2, CN,S(O)R, SO2R, SR, N(R4)2, CON(R4)2, SO2N(R4)2, OC(>=O)R, N(R4) COR o N(R4)CO2R; cada R4 se elige independientemente entre H, C1-6alquilo o haloC1-6alquilo; cada R5 se elige independientemente entre halo, haloC1-6alquilo o C1-6alquilo; y cada R se elige independientemente entre H, C1-6 alquilo o haloC1-6 alquilo; siempre que el compuesto no sea**Fórmula**