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(11)    Patent No :    AP 2111   
(21)    Application No :    AP/P/2004/003151   
(22)    Filing Date :    12.03.2003   
(24)    Date of Grant &    03.03.2010   
(45)    Publication :

(30)  Priority Data       
(33) Country    (31) Number    (32) Date
EP    02075999.9    12.03.2002

(84)    Designated State

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

(73) Applicant(s)



(72) Inventors

SURLERAUX Dominique Louis Nestor Ghislain,


WIGERINCK Piet Tom Bert Paul, Belgium

VOETS Marieke Christiane Johanna, Belgium

et al

(74) Representative


(51)  International  Classification   C07C 217/34 (2006.01)    C07C 217/36 (2006.01)
C07C 229/00 (2006.01)   

(54)    Title

Broadspectrum substituted benzimidazole sulfonamide HIV protease inhibitors.

(57)    Abstract

The present invention concerns the compounds having the formula (1), wherein 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 radical of formula (R11AR11b)NC(R10aR10b)CR9 -;t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(=O) -, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanediyl-C(=O) -, -S(=O)2-,-O-S(=O)2-,-NR8-S(=O)2 ; R3 is C1-6 alkyl, 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), C3-7cycloakyl, C2 -6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, -C(=O)-, -C(=S)-, -S(=O)2-, C1 -6alkanediyl-C(=O)-, C1 -6 alkanediyl-C(=S)- or

C1-6akanediyl-S(=O)2 -; is H, OH, C1 -6alkyl, Het1C1-6alkyl, Het2C1 -6alkyl, optionally substituted amino-C1-6alkyl; R6 is C1-6O, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other then C1 -6alkanediyl then R6 may also be C1 -6alkyl,

Het1C1 -4alkyl,Het1OC1-4alkyl,Het2C1 -4alkyl, arylC1-4alkyl, arylOC1 -4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2, R12, is H, -NH2, -NR5AR6, -C1-6alkyl or alkyl -W -R14, wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het1, Het2, or amino wherein said amino is optionally mono- or di-substituted with C1-4alkyl and R13 is H, C1-6-alkyl, optionally substituted by aryl, Het1, Het2, hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with C1 -4alkyl.

(56)    Documents Cited :    WO 99 65870 A    WO 99 59989 A    WO 96 28465 A


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