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(11)    Patent No :    AP 1927   
(73) Applicant(s)       
(21)    Application No :    AP/P/2005/003334    TIBOTEC PHARMACEUTICALS LTD., Little Island , Co Cork,       
(22)    Filing Date :    14.11.2003           
(24)    Date of Grant &    10.12.2008           
(45)    Publication :

(30)  Priority Data    (72) Inventors

    (33) Country    (31) Number    (32) Date    KESTELEYN Bart Rudolf Romanie, Belgium   
    EP            02079783.3    15.11.2002    VAN DE VREKEN Wim, Belgium   
    US            60/434,950        20.12.2002       
                            KINDERMANS Natalie Maria Francisca, 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    A61P 31/12 (2006.01)    A61P 31/00 (2006.01)   
                            C07D 471/04 (2006.01)       

(54)    Title

Substituted indolepyridinium as anti-infective compounds

(57)    Abstract

The present invention concerns the compounds of formula (1) (R3)n P(I) N O R1 R2 their N-oxides, salts, stercoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1. 2 or 3; R1 is H, CN, halo, aminoC(=O),

C(=O)OH, C1 -4alkyloxyC(=O), C1 -4alkylC(=O), mono- or di(C1-4alkyl)aminoC(=O), arylaminoC(=O),

N-(aryl)-N'-(C1-4alkyl)aminoC(=O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methaninudamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2 -10allkenyl, C3-7cycloalkyl, wherein said

C1-10alkyl,C2 -10alkenyl and C3 -7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxyC1-4alkyloxy, hydroxyC(=O), aminoC(=O), C1-4alkyloxyC(=O), mono- or di(C1 -4alkyl)aminoC(=O)

C1-4alkylC(=O), methanimidaimidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy methanimidamidyl or Ilet; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of


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