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(11)    Patent No :    AP 1878    (73) Applicant(s)       
(21)    Application No :    AP/P/2005/003242    TIBOTEC PHARMACEUTICALS LTD., Little Island , Co Cork,       
(22)    Filing Date :    04.08.2003           
(24)    Date of Grant &    13.08.2008           
(45)    Publication :

(30)  Priority Data    (72) Inventors

    (33) Country    (31) Number    (32) Date    SURLERAUX Dominique Louis Nestor Ghislain,   
    EP            02078231.4    02.08.2002    Belgium       
    US            60/427,862        20.11.2002    WIGERINCK Piet Tom Bert Paul, Belgium   
                                GETMAN Daniel P., United States of America   
                                et al       
                                (74) Representative   
(84)    Designated State                   
    BW    GM    GH    KE    LS    MW    MZ   NA   SL    HONEY & BLANCKENBERG   
    SD    SZ    T Z    UG    ZM    ZW               
(51)    International    Classification    A61K 31/425 (2006.01)    A61P 31/18 (2006.01)   
                            C07D 277/82 (2006.01)       
(54)    Title

Broadspectrum 2 -amino-benzothiazole sulfonamide HIV protease inhibitors

(57)    Abstract

The present invention relates to the use of 2 -amino-benzothiazoles, having the formula (I) wherein RI is hexahydrofuro[2,3-b]furanyl, tetrahydrofuranyl, oxazolyl, thiazolyl, pyridinyl, or phenyl optionally substituted with one or more substituents independently selected from

C1-6-alkyl, hydroxy, amino, halogen, aminoC1-4-alkyl and mono-or di(C1-4alkyl)amino; R2 is hydrogen or C1-6alkyl; L is a direct bond, -0 -, C1-6alkanediyl-O- or -O-C1-6alkanediyl; R3 is phenylC1 -4alkyl; R4 is

C1-6alkyl; R5 is hydrogen or C1 -6alkyl; R6 is hydrogen or C1-6alkyl; in the manufacture of a medicament useful for inhibiting mutant HIV protease in a mammal infected with said mutant HIV protease. It also relates to novel compounds of formula (I).

(56)    Documents Cited :    WO 95 06030 A    WO 99 67254 A


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