Patent ID: 6423725
Filing Date: 2002-07-23
Classification: A61P,C07D

Abstract:
A compound of the following formula: or the pharmaceutically acceptable salts thereof, whereinR1 and R2 are independently C1-C4 alkyl; or R1 and R2, taken together with the carbon atom to which they are attached, form a mono-, bi-, tri- or spiro-cyclig group having 6 to 13 carbon atoms, wherein the cyclic group is optionally substituted by one to five substituents independently selected from C1-C4 alkyl, C2-C4 alkylene, C1-C4 alkoxy, hydroxy, oxo, &boxH;CH2 and &boxH;CHâ€”C1-C4 alkyl; R3 is C1-C7 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, phenyl-C1-C5 alkyl, phenyl optionally substituted by one to three substituents independently selected from fluorine, C1-C3 alkyl and C1-C3 alkoxy, or a heteroaryl group selected from furyl, thienyl, pyrrolyl and pyridyl, wherein said heteroaryl group is optionally substituted by one to three substituents independently selected from halo, C1-C3 alkyl and C1-C3 alkoxy, with the proviso that when both R1 and R2 are C1-C4 alkyl, then R3 is other than C1-C7 alkyl, C2-C5 alkenyl and C2-C5 alkynyl; R4 is selected from: 1) hydrogen, 2) optionally mono- or di-substituted, C1-C8 alkyl C3-C7 cycloalkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C6 alkyl-Zâ€”, C1-C6 alkyl-Zâ€”(C1-C6)alkyl, C3-C7 cycloalkyl-Zâ€”(C1-C6)alkyl, C2-C6 alkenyl-Zâ€”(C1-C6)alkyl or C2-C6 alkynyl-Zâ€”(C1-C6)alkyl, wherein Z is selected from O, S, SO, SO2, CO, CO2, OCO, NR, CONR and NRCO wherein R is hydrogen or C1-C6 alkyl, and the substituents to be attached to the alkyl, alkenyl, alkynyl or cycloalkyl moiety are independently selected from halo, hydroxy, carboxy, amino, mono- or di-(C1-C4 alkyl)amino, hydrazino, azido, ureido, amidino and guanidino; or 3) optionally mono- or di- substituted, aryl, heterocyclic, aryl(C1-C5)alkyl, heterocyclic(C1-C5)alkyl, heterocyclic-heterocyclic(C1-C5)alkyl, aryl-heterocyclic(C1-C5)alkyl, heterocyclic-Zâ€”(C1-C5)alkyl, aryl-Zâ€”(C1-C5)alkyl, aryl(C1-C5)alkyl-Zâ€”(C1-C5)alkyl, or heterocyclic(C1-C5)alkyl-Zâ€”(C1-C5)alkyl, wherein Z is selected from O, S, SO, SO2, CO, CO2, OCO, NR, CONR and NRCO, wherein R is hydrogen or C1-C6 alkyl, and the substituents to be attached to the aryl or heterocyclic moiety are independently selected from halo, hydroxy, carboxy, C1-C4 alkyl, halo C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-COâ€”, amino(C1-C4)alkyl-COâ€”, phenyl, benzyl, amino, mono- or di-(C1-C4 alkyl)amino, hydrazino, azido, ureido, amidino and guanidino; R5 is independently selected from halo, C1-C3 alkyl, C1-C3 alkoxy, C1-C3 alkylsulfonyl, CF3, carboxy, hydroxy, amino, alkylamino, acylamino, arylcarbonyl, alkylcarbonyl and hydroxyalkyl; and n is 0, 1, 2, 3 or 4.