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(11)    Patent No :    AP 1922   
(21)    Application No :    AP/P/2004/003083   
(22)    Filing Date :    20.12.2002   
(24)    Date of Grant &    21.11.2008   
(45)    Publication :

(30)  Priority Data       
(33) Country    (31) Number    (32) Date
EP    01205115.7    21.12.2001

(84)    Designated State

BW    GM    GH    KE    LS    MW  MZ   NA   SL
SD    SZ    T Z    UG    ZM    ZW

(73) Applicant(s)



(72) Inventors

VENDEVILLE Sandrine Marie Hèlène, Belgium

VERSCHUEREN Wim Gaston, Belgium

TAHRI Abdellah, Belgium

et al

(74) Representative


(51)  International  Classification   A61K 31/41 (2006.01)    A61K 31/415 (2006.01)
C07D 233/64 (2006.01)   

(54)    Title

Broadspectrum heterocylclic substituted phenyl containing sulfonamide HIV protease inhibitors.

(57)    Abstract

The present invention concerns the compounds having the formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by

C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, -(R7a)n-M-R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and -A-R6; and on (ii) a nitrogen atom if present by hydroxy or -A-R6. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

(56)    Documents Cited : Database CA 'Online! Chem Abstr Service, Columbus, Ohio, US, Kamijo, Tetsukiyo et al:

Database Accession No. 127:34116    WO 96 33184 A    WO 99 67254 A


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