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Title:
INHIBITORS OF ASPARTYL PROTEASE
Document Type and Number:
WIPO Patent Application WO2000047551
Kind Code:
A3
Abstract:
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Inventors:
HALE MICHAEL R (US)
BAKER CHRISTOPHER T (US)
STAMMERS TIMOTHY A (CA)
SHERRILL RONALD G (US)
SPALTENSTEIN ANDREW (US)
FURFINE ERIC S (US)
MALTAIS FRANCOIS (US)
ANDREWS CLARENCE WEBSTER III (US)
MILLER JOHN F (US)
SAMANO VICENTE (US)
Application Number:
PCT/US2000/003288
Publication Date:
August 16, 2001
Filing Date:
February 09, 2000
Export Citation:
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Assignee:
VERTEX PHARMA (US)
HALE MICHAEL R (US)
BAKER CHRISTOPHER T (US)
STAMMERS TIMOTHY A (CA)
SHERRILL RONALD G (US)
SPALTENSTEIN ANDREW (US)
FURFINE ERIC S (US)
MALTAIS FRANCOIS (US)
ANDREWS CLARENCE WEBSTER III (US)
MILLER JOHN F (US)
SAMANO VICENTE (US)
International Classes:
A61K9/20; A61K9/48; A61K31/27; A61K31/275; A61K31/34; A61K31/341; A61K31/357; A61K31/36; A61K31/5377; A61K31/662; A61P31/14; A61P31/18; C07D317/28; A61P43/00; C07B53/00; C07C271/20; C07C271/22; C07C311/19; C07C311/29; C07C311/42; C07C311/46; C07C317/18; C07D307/20; C07D317/62; C07D319/06; C07D409/12; C07D493/04; C07F9/6561; (IPC1-7): C07D493/04; C07C311/29; C07C311/42; C07D317/62; C07D307/20; C07D319/06; C07D407/12; C07F9/6561; A61K31/34; A61K31/36; A61K31/18; A61K31/665
Domestic Patent References:
WO1994004492A11994-03-03
WO1994010136A11994-05-11
Foreign References:
US4629724A1986-12-16
EP0159156A11985-10-23
Other References:
A.C. NAIR ET AL, BIOCHEM. BIOPHYS. RES. COMMUN., vol. 242, no. 3, 1998, pages 545 - 551, XP002162562
A.K. GHOSH ET AL, BIOORG. MED. CHEM. LETT., vol. 8, no. 6, 1998, pages 687 - 690, XP004136945
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