公开(公告)号：ZA200004652B

公开(公告)日：2002-04-24

申请号：ZA200004652

申请日：2000-09-05

Applicant: VERTEX PHARMA

Inventor： WANNAMAKER MARION W ,  BENNIS GUY W ,  CHARIFSON PAUL S ,  LAUFFER DAVID J ,  MULLICAN MICHAEL D ,  MURCKO MARK A ,  WILSON KEITH P ,  JANETKA JAMES W ,  DAVIES ROBERT J ,  GRILLOT ANNELAURE ,  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 ,  C07K ,  A61K ,  C07D

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1² 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-³ inducing factor-(IGIF), or interferon-³-("IFN-³") 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-³ production and methods for treating interieukin-1, apoptosis-, and interferon-³ 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：HK1061851A1

公开(公告)日：2004-10-08

申请号：HK04104843

申请日：2004-07-06

Applicant: VERTEX PHARMA

Inventor： GRILLOT ANNELAURE ,  CHARIFSON PAUL ,  STAMOS DEAN ,  LIAO YUSHENG ,  BADIA MICHAEL ,  TRUDEAU MARTIN

IPC: C07D20060101 ,  C07D235/32 ,  A01P20060101 ,  A61K20060101 ,  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

Abstract: The present invention relates to compounds of the formula I or a pharmaceutically acceptable derivative 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.