Patent ID: 6458801
Filing Date: 2002-10-01
Classification: A61P,C07D

Abstract:
A compound of formula (I) in whicheither R1 and R2, independently from one another represent a hydrogen atom or an alkyl group containing from 1 to 6 carbon atoms non-substituted or substituted by R3, or R1 and R2 together form a divalent alkylene radical containing 2 to 9 carbon atoms, saturated or unsaturated, such as â€”(CH2)pâ€” in which p is 2, 3, 4, 5, 6, 7, 8 or 9, non-substituted or substituted by one or more radicals chosen from halogen, (C1-C6)-alkyl, (C1-C6)-alkoxy, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C6)-alkyl, (C5-C14)-heteroaryl, (C5-C14)-heteroaryl-(C1-C6)-alkyl, (C3-C12)-cycloalkyl (C3-C12)-cycloalkyl-(C1-C6)-alkyl and oxo, said divalent alkylene radical being able to be attached at the level of the carbon-carbon bond to a carbocycle or a heterocycle with 5 to 7 members, containing 1 or 2 nitrogen atoms, saturated or unsaturated, non-substituted or substituted by 1 or 2 R3 radicals; R3 represents a (C1-C8)-alkyl, (C1-C8)-alkoxy, (C5-C14)-aryl, (C5-C14)-aryl-(C1-C4)-alkyl, halogen, trifluoromethyl, hydroxyl, nitro, amino, NHâ€”((C1-C4)-alkyl), N((C1-C4)alkyl)2, NHCOâ€”(C1-C4)-alkyl or COâ€”(C1-C4)alkyl group; R4 represents either a hydrogen atom, or a (C1-C6)-alkyl-COâ€”Oâ€”(C1-C4)-alkyl or (C1-C6)-alkyl group, non-substituted or substituted by a radical chosen from hydroxyl, (C1-C4)-alkoxy, (C1-C4)-alkyl-SO2, NR9R9â€² and N+R9R9â€²R9â€³Qâˆ’, in which R9, R9â€² and R9â€³ independently from one another, represent a hydrogen, a (C1-C6)-alkyl, (C5-C14)-aryl or (C5-C14)-aryl-(C1-C6)-alkyl group and Qâˆ’ is a physiologically acceptable anion, or one of the following radicals: â€ƒthe dotted lines representing the position of the bond; R5 represents a hydrogen atom or a group chosen from COR6, CO2R6, SO2R6, SO2NHR6, SO2NHCOR6, SO2NHCO2R6, CONH2 and CONHR6 in which R6 represents (C1-C8)-alkyl, (C6-C14)-aryl, (C6-C14)-aryl-(C1-C6)-alkyl, (C5-C14)-heteroaryl or (C5-C14)-heteroaryl-(C1-C6)-alkyl, (C3-C20) (mono-, bi- or tri-)-cycloalkyl, (C3-C20) (mono-, bi- or tri-)-cycloalkyl-(C1-C6)alkyl, the aryl or heteroaryl radical being non-substituted or substituted by 1, 2 or 3 R3 radicals; R7 represents a hydrogen atom, (C1-C6)-alkyl-Oâ€”COâ€”, hydroxyl, (C1-C6)-alkyl-Oâ€”COâ€”O or nitro; m is equal to 0, 1, 2 or 3; n is an integer equal to 1, 2 or 3; said compounds of formula (I) being in all their possible isomer forms, alone or in a mixture in any ratio, the acylguanidine group adjacent to the phenyl being in para or meta position of the oxygen, as well as their physiologically acceptable salts and their promedicaments (prodrugs).