Patent ID: 6770656
Filing Date: 2004-08-03
Classification: A61P,C07B,C07C,C07D

Abstract:
An amine according to formula I: whereinA1 and A2 are selected independently from each other from the group consisting of â€”C(O)â€” and â€”SO2â€”; Ra is C1-C10 alkyl Rb is CH3, or Ra and Rb taken together with the atoms to which they are attached form a five-membered saturated ring optionally containing a sulfur atom or a six-membered saturated ring optionally fused with an aryl or heteroaryl group; R1 is either H or C1-C6 alkyl; R2 is â€”(Rdâ€”X1)mâ€”Re wherein m is an integer from 0 to 8; wherein Rd is aryl, heteroaryl, C1-C18 alkyl, 3-8-membered cycloalkyl, C2-C18 alkenyl, 3-8-membered cycloalkenyl, C2-C18 alkynyl; X1 is a bond, O, NH, NRg, NRgNgâ€², S, Si(RgRgâ€²), SO, SO2, wherein Rg and Rgâ€² are independently substituted or unsubstituted C1-C6 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, aryl or heteroaryl; Re is aryl-C1-C18 alkyl, aryl-C2-C18 alkenyl, aryl-C2-C18 alkynyl, heteroaryl-C1-C18 alkyl, heteroaryl-C2-C18 alkenyl, heteroaryl-C2-C18 alkynyl, C1-C18 alkyl, C2-C18 alkenyl, C2-C18 alkynyl, wherein said C1-C18 alkyl, C2-C18 alkenyl and C2-C18 alkynyl have a terminal substituent of the formula â€”NRRâ€² or â€”N+RRâ€²Râ€³ wherein R, Râ€², Râ€³ are H, C1-C6-alkyl; or R1 and R2 together with the N atom to which they are attached form an unsubstituted or substituted 4-12 membered unsaturated or saturated ring containing one further heteroatom selected from the group consisting of O, and N optionally substituted by Re, or R1 and R2 together with the N atom to which they are attached form an unsubsituted or substituted 4-12 membered unsaturated or saturated ring substituted by Re, or by a substituent of the formula â€”NRRâ€² or â€”N+RRâ€²Râ€³ wherein R, Râ€², Râ€³ are H, C1-C6-alkyl; R0 is Rfâ€”X2â€”Rfâ€² wherein Rf and Rfâ€² are independently from each other aryl, heteroaryl, 3-8-membered cycloalkenyl, 3-8-membered cycloalkyl, C2-C18 alkyl, C2-C18alkenyl, C2-C18 alkynyl, aryl-C1-C18 alkyl, aryl-C2-C18 alkenyl, aryl-C2-C18 alkynyl, heteroaryl-C1-C18 alkyl, heteroaryl-C2-C18 alkenyl, or heteroaryl-C2-C18 alkynyl; X2 is a bond, O, S, Si(RgRgâ€²), SO, or SO2; and geometrical isomers, optically active enantiomers, diastereomers, racemates and pharmaceutically acceptable salts thereof.