Patent ID: 6825231
Filing Date: 2004-11-30
Classification: A61P,C07B,C07C

Abstract:
A substituted norbornylamino compound having exo-configured nitrogen and an endo-fused five-, six- or seven-membered ring of the formula I or a pharmaceutically acceptable salt or trifluoroacetate salt thereof, or having exo-configured nitrogen and an exo-fused five-, six- or seven-membered ring of the formula I a or a pharmaceutically acceptable salt or trifluroacetate salt thereof in which:A is (C1-C4)-alkylene; S1 is a free electron pair or (C1-C4)-alkyl; S2 is (C1-C4)-alkyl or H; where, if S1 and S2 are alkyl, a group â€”N+ (S1S2)-Xâˆ’ is obtained, wherein Xâˆ’ corresponds to a pharmacologically acceptable anion or trifluoroacetate; B is a saturated or unsaturated five-, six- or seven-membered carbon ring which may be mono- or, independently of one another, polysubstituted by oxo, hydroxyl, (C1-C4)-alkoxy and (C1-C4)-alkyl; and R1, R2, R3, R4 and R5 are, independently of one another, H, OH, F, Cl, Br, I, CN, NO2, amidino, â€”CO2R(11), â€”CONR(11)R(12), â€”SOrR(11), â€”SOsNR(11)-R(12), (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyloxy, hydroxy-(C1-C4)-alkyl, (C3-C7)-cycloalkoxy or phenyloxy, where phenyl is unsubstituted or substituted by up to three substituents, which are independent of one another and are F, Cl, Br, or methoxy; amino, (C1-C4)-alkylamino, di-(C1-C4)-alkylamino, amino-(C1-C4)-alkyl, di-(C1-C4)-alkylamino-(C1-C4)-alkyl, (C1-C4)-alkylamino-(C1-C4)-alkyl, where some or all of the hydrogen atoms in the alkyl radicals may be substituted by fluorine; R11 and R12 are, independently of one another, H or (C1-C4)-alkyl, where some or all of the hydrogen atoms in the alkyl radicals may be substituted by fluorine; r is 0, 1 or 2; s is 1 or 2; or at least one of R1 and R2, R2 and R3, R3 and R4 or R4 and R5 together form one or more groups â€”Oâ€”(CH2)nâ€”Oâ€”; n is 1 or 2; and the radical or radicals R1, R2, R3, R4 or R5 which do not form said group or groups â€”Oâ€”(CH2)nâ€”Oâ€” is or are, independently of one another, H, OH, F, Cl, Br, I, CN, NO2, amidino, â€”CO2R(11), â€”CONR(11)R(12), â€”SOrR(11), â€”SOsNR(11)â€”R(12), (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C3-C7)-cycloalkoxy, hydroxy-(C1-C4)-alkyl, amino, (C1-C4)-alkyl-amino, di-(C1-C4)-alkylamino, amino-(C1-C4)-alkyl, di-(C1-C4)-alkylamino-(C1-C4)-alkyl, (C1-C4)-alkylamino-(C1-C4)-alkyl, where some or all of the hydrogen atoms in the alkyl radicals may be substituted by fluorine; R11 and R12 are, independently of one another, H or (C1-C4)-alkyl, where some or all of the hydrogen atoms in the alkyl radicals may be substituted by fluorine; r is 0, 1 or 2; s is 1 or 2; except for benzyl(octahydro-4,7-methanoinden-5-yl)amine.