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(11)    Patent No :    AP 2585    (73) Applicant(s)       
(21)    Application No :    AP/P/2008/004306    TIBOTEC PHARMACEUTICALS LTD., Eastgate Village,       
            Eastgate, Little Island, Co Cork,       
(22)    Filing Date :    28.07.2006    Ireland       
(24)    Date of Grant &        MEDIVIR AB, Lunastigen 7, S-141 44 Huddinge,       
        04.02.2013    Sweden       
(45)    Publication :

(30)  Priority Data    (72) Inventors

    (33) Country    (31) Number    (32) Date    RABOISSON Pierre Jean-Marie Bernard, Belgium   
    EP            05107057.1    29.07.2005    DE KOCK Herman Augustinus, Belgium   
    EP            06113097.7    25.04.2006       
                        HU Lili, Belgium   
                                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    C07K 5/00 (2006.01)    C07D 419/00 (2006.01)   
(54)    Title

Macrocyclic inhibitors of hepatitis C virus

(57)    Abstract

Compounds of the formula (I), and N-oxides, salts, and stereoisomers thereof wherein A is OR1 , NHS(=O)PR2 ; wherein; R1 is hydrogen, C1 -C6alkyl,

Co-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl,

Co-C3alkylenecarbocyclyl, Co-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; - - - deonotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1 -C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino,

Co-C3alkylenecarbocyclyl and Co-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen,

C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylenecarbocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV

(56)    Documents Cited :    WO 2004/037855 A    WO 03/053349 A    WO 2005/028501 A


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