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(11)    Patent No :    AP 2126   
(21)    Application No :    AP/P/2005/003245   
(22)    Filing Date :    14.08.2003   
(24)    Date of Grant &    03.06.2010   
(45)    Publication :

(30)  Priority Data       
(33) Country    (31) Number    (32) Date
EP    02078384.1    14.08.2002

(84)    Designated State

BW    GM    GH    KE    LS    MW  MZ   NA   SL
SD    SZ    T Z    UG    ZM    ZW
(73) Applicant(s)



(72) Inventors

TAHRI Abdellah, Belgium

WIGERINCK Piet Tom Bert Paul, Belgium

(74) Representative


(51)  International  Classification   A61K    31/4045 (2006.01)    A61K 31/4439 (2006.01)
A61P    31/14 (2006.01)   

(54)    Title

Broadspectrum substituted oxindole 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 R1 and R8 each are H, optionally substituted C1-6alkyl, C2 -6alkenyl,

C3-7cycloalkyl, aryl, Het1, Het2; R1, may also be a radical of formula (R11a ,R11b)NC(R10a, R10b)CR9-; t is 0,1 or 2; R2 is H or

C1-6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6 alkanediyl-C(=O)-, -NR8-C1-6alkanediyl-C(=O)-,S(=O)2-,-O-S(=O)2-,-NR8 -S(=0)2 ; R3 is

C1-6alkyl, aryl, C3-7 cycloalkyl,

C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(=O), carboxyl, aminoC(=O), mono- or

di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1 -6alkyl; formula (II) is formula (III) or formula (IV) ; R5a, and R5b is C2 -6alkenyl, C2 -6 alkynyl,

C3-7cycloalkyl or C1-6alkyl, optionally substituted on one or more atoms; R5a and R5b may also be hydrogen, aryl, Het1, Het2; R6 is hydrogen or C1-6alkyl optionally substituted on one ore more carbon atoms. It further relates to their use as broad spectrum 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 :    WO 96 22287 A    WO 01 72708 A    WO 99 65870 A



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