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：WO9947545A3

公开(公告)日：1999-11-25

申请号：PCT/US9905919

申请日：1999-03-19

Applicant: VERTEX PHARMA ,  WANNAMAKER MARION W ,  BEMIS GUY W ,  CHARIFSON PAUL S ,  LAUFFER DAVID J ,  MULLICAN MICHAEL D ,  MURCKO MARK A ,  WILSON KEITH P ,  JANETKA JAMES W ,  DAVIES ROBERT J ,  GRILLOT ANNE LAURE ,  SHI ZHAN ,  FORSTER CORNELIA J

Inventor： WANNAMAKER MARION W ,  BEMIS GUY W ,  CHARIFSON PAUL S ,  LAUFFER DAVID J ,  MULLICAN MICHAEL D ,  MURCKO MARK A ,  WILSON KEITH P ,  JANETKA JAMES W ,  DAVIES ROBERT J ,  GRILLOT ANNE-LAURE ,  SHI ZHAN ,  FORSTER CORNELIA J

IPC: C07D207/273 ,  A61K31/47 ,  A61K38/00 ,  A61K38/03 ,  A61K38/04 ,  A61P5/48 ,  A61P7/00 ,  A61P9/00 ,  A61P17/00 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07D401/12 ,  C07K5/02 ,  C07K5/023

CPC classification number: C07K5/0202 ,  A61K38/00 ,  C07D401/12

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1 beta converting enzyme ("ICE") inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1- ("IL-1"), apoptosis-, interferon- gamma inducing factor- (IGIF), or interferon- gamma - ("IFN- gamma ") mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN- gamma production and methods for treating interleukin-1, apoptosis-, and interferon- gamma - mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.

Abstract translation: 本发明涉及新型的化合物，它们是半胱天冬酶抑制剂，特别是白细胞介素-1β转化酶（“ICE”）抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制半胱天冬酶活性，因此可以有利地用作抗白细胞介素-1（“IL-1”），细胞凋亡 - ，干扰素-γ诱导因子 - （IGIF） ，或干扰素-γ-（“IFN-γ”）介导的疾病，包括炎性疾病，自身免疫性疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。 本发明还涉及抑制半胱天冬酶活性并降低IGIF产生和IFN-γ产生的方法以及使用本发明的化合物和组合物治疗白细胞介素-1，细胞凋亡和干扰素-γ介导的疾病的方法。 本发明还涉及制备本发明化合物的方法。

公开(公告)号：WO2011041634A8

公开(公告)日：2011-12-29

申请号：PCT/US2010051053

申请日：2010-10-01

Applicant: VERTEX PHARMA ,  MESSERSMITH DAVID ,  ARONOV ALEX ,  LAUFFER DAVID J ,  GRILLOT ANNE-LAURE ,  DAVIES ROBERT J

Inventor： MESSERSMITH DAVID ,  ARONOV ALEX ,  LAUFFER DAVID J ,  GRILLOT ANNE-LAURE ,  DAVIES ROBERT J

IPC: C07D401/08 ,  A61K31/4439 ,  A61K31/4965 ,  A61P25/28 ,  A61P37/00 ,  C07D401/14 ,  C07D403/08

CPC classification number: C07D401/08 ,  C07D401/14 ,  C07D403/08

Abstract: The present invention relates to compounds 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抑制剂，特别是P13Kα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：WO02060879A3

公开(公告)日：2003-03-27

申请号：PCT/US0148855

申请日：2001-12-12

Applicant: VERTEX PHARMA ,  GRILLOT ANNE-LAURE ,  CHARIFSON PAUL ,  STAMOS DEAN ,  LIAO YUSHENG ,  BADIA MICHAEL ,  TRUDEAU MARTIN

Inventor： GRILLOT ANNE-LAURE ,  CHARIFSON PAUL ,  STAMOS DEAN ,  LIAO YUSHENG ,  BADIA MICHAEL ,  TRUDEAU MARTIN

IPC: C07D235/32 ,  A61K31/00 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  A61P31/00 ,  A61P31/04 ,  A61P43/00 ,  C07D213/00 ,  C07D221/00 ,  C07D235/00 ,  C07D235/30 ,  C07D263/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/14 ,  C07D491/04 ,  C07D491/056 ,  C07D498/04 ,  C07D521/00 ,  C07F9/6558 ,  C07F9/6561

CPC classification number: C07D403/12 ,  A61K31/00 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D231/12 ,  C07D233/56 ,  C07D235/30 ,  C07D249/08 ,  C07D263/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/14 ,  C07D491/04 ,  C07F9/65583 ,  C07F9/6561 ,  A61K2300/00

Abstract: The present invention relates to compounds of the formula (I): or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的衍生物或前药。 该化合物可用作细菌回旋酶活性的抑制剂。 本发明还涉及用于治疗哺乳动物细菌感染的方法。 本发明还涉及生物样品中细菌数量减少的方法。

公开(公告)号：EP1218369A4

公开(公告)日：2005-06-22

申请号：EP00957485

申请日：2000-08-11

Applicant: VERTEX PHARMA

Inventor： GREEN JEREMY ,  BEMIS GUY ,  GRILLOT ANNE-LAURE ,  LEDEBOER MARK ,  SALITURO FRANCIS ,  HARRINGTON EDMUND ,  GAO HUAI ,  BAKER CHRISTOPHER ,  CAO JINGRONG ,  HALE MICHAEL

IPC: A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/02 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D413/04 ,  C07D413/14 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04

CPC classification number: C07D413/04 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  C07D413/14

公开(公告)号：AU2010341573B2

公开(公告)日：2016-10-13

申请号：AU2010341573

申请日：2010-12-21

Applicant: VERTEX PHARMA

Inventor： ARONOV ALEX ,  COME JON H ,  DAVIES ROBERT J ,  PIERCE ALBERT C ,  WANG JIAN ,  NANTHAKUMAR SUGANTHINI ,  CAO JINGRONG ,  BANDARAGE UPUL K ,  KRUEGER ELAINE ,  TIRAN AMAUD LE ,  LIAO YUSHENG ,  MESSERSMITH DAVID ,  COLLIER PHILIP N ,  GREY RONALD ,  O'DOWD HARDWIN ,  HENDERSON JAMES A ,  GRILLOT ANNE-LAURE

IPC: C07D401/04 ,  A61K31/352 ,  A61K31/424 ,  A61K31/429 ,  A61P9/00 ,  A61P29/00 ,  A61P37/00 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/20 ,  C07D491/20

Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. 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：CY1110230T1

公开(公告)日：2015-01-14

申请号：CY091100932

申请日：2009-09-07

Applicant: VERTEX PHARMA

Inventor： CHARIFSON PAUL S ,  DEININGER DAVID D ,  GRILLOT ANNE-LAURE ,  LIAO YUSHENG ,  RONKIN STEVEN M ,  STAMOS DEAN ,  PEROLA EMANUELE ,  WANG TIANSHENG ,  LE TIRAN ARNAUD ,  DRUMM JOSEPH

IPC: C07D491/04 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/506 ,  A61P31/00 ,  A61P31/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: Ηπαρούσαεφεύρεσησχετίζεταιμεενώσειςπουαναστέλλουνβακτηριακήγυράσηκαι/ή Topo IV καιφαρμακευτικώςαποδεκτέςσυνθέσειςπουπεριλαμβάνουντιςπροαναφερθείσεςενώσεις. Αυτέςοιενώσεις, καισυνθέσειςαυτών, είναιχρήσιμεςστηναντιμετώπισηβακτηριακήςλοίμωξης. Σύμφωναμεαυτά, ηπαρούσαεφεύρεσηεπίσηςσχετίζεταιμεμεθόδουςγιατηναντιμετώπισηβακτηριακώνλοιμώξεωνσεθηλαστικά.

公开(公告)号：ZA201305233B

公开(公告)日：2014-11-26

申请号：ZA201305233

申请日：2013-07-11

Applicant: VERTEX PHARMA

Inventor： LE TIRAN ARNAUD ,  GRILLOT ANNE-LAURE ,  CHARIFSON PAUL S ,  BENNANI YOUSSEF LAAFIRET ,  O'DOWD HARDWIN ,  PEROLA EMANUELE

IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101 ,  C07F20060101

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.

公开(公告)号：CA2324226C

公开(公告)日：2012-06-05

申请号：CA2324226

申请日：1999-03-19

Applicant: VERTEX PHARMA

Inventor： WANNAMAKER MARION W ,  BEMIS GUY W ,  CHARIFSON PAUL S ,  LAUFFER DAVID J ,  MULLICAN MICHAEL D ,  MURCKO MARK A ,  WILSON KEITH P ,  JANETKA JAMES W ,  DAVIES ROBERT J ,  GRILLOT ANNE-LAURE ,  SHI ZHAN ,  FORSTER CORNELIA J

IPC: C07D207/273 ,  C07K5/023 ,  A61K31/47 ,  A61K38/00 ,  A61K38/03 ,  A61K38/04 ,  A61P5/48 ,  A61P7/00 ,  A61P9/00 ,  A61P17/00 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00 ,  C07D401/12 ,  C07K5/02

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1.beta. converting enzyme ("ICE") inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-("IL-1"), apoptosis-, interferon-.gamma. inducing factor- (IGIF), or interferon-.gamma.- ("IFN-.gamma.") mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-.gamma. production and methods for treating interleukin-1, apoptosis-, and interferon-.gamma.- mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.

公开(公告)号：NZ592569A

公开(公告)日：2012-05-25

申请号：NZ59256909

申请日：2009-10-20

Applicant: VERTEX PHARMA

Inventor： LAUFFER DAVID ,  LI PAN ,  MCGINTY KIRA ,  RONKIN STEVEN ,  TANG QING ,  GRILLOT ANNE-LAURE ,  WAAL NATHAN

IPC: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D451/06

Abstract: Disclosed are tetrazole piperazine compounds represented by general formula (I), or pharmaceutically acceptable salts thereof, wherein RA is a phenyl or 5-9 membered heteroaryl. The compounds are used to treat a proliferative disorder such as cancer.