Patent ID: 6790834
Filing Date: 2004-09-14
Classification: A61K,A61P,C07C,C07D

Abstract:
A compound formula (I) whereinR is hydrogen or (C1-C6)alkyl; R1 is hydrogen; (C2-C6)alkyl; (C2-C6)alkenyl; phenyl or substituted phenyl; phenyl (C2-C6)alkyl or substituted phenyl (C2-C6)alkyl; phenyl (C2-C6)alkenyl or substituted phenyl(C2-C6)alkenyl; heterocyclyl or substituted heterocyclyl; heterocyclyl(C2-C6)alkyl or substituted heterocyclyl(C2-C6)alkyl; a group BSOnA- wherein n is 0, 1 or 2 and B is hydrogen or a (C2-C6)alkyl, phenyl, substituted phenyl, heterocyclyl substituted heterocyclyl, (C2-C6)acyl, phenacyl or substituted phenacyl group, and A represents (C2-C6)alkylene; hydroxy or (C2-C6)alkoxy; amino, protected amino, acylamino, (C2-C6)alkylamino or di-(C2-C6)alkylamino; mercapto or (C2-C6)alkylthio; amino(C2-C6)alkyl, (C2-C6)alkylamino(C2-C6)alkyl, di(C2-C6)alkylamino(C2-C6)alkyl, hydroxy(C2-C6)alkyl, mercapto(C2-C6)alkyl or carboxy(C2-C6)alkyl wherein the amino-, hydroxy-, mercapto- or carboxyl-group are optionally protected or the carboxyl- group amidated; lower alkyl substituted by carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, or carboxy-lower alkanoylamino; or a cycloalkyl, cycloalkenyl or non-aromatic heterocyclic ring containing up to 3 heteroatoms, any of which may be (i) substituted by one or more substituents selected from C1-C6 alkyl, C2-C6 alkenyl, halo, cyano (â€”CN), â€”CO2H, â€”CO2R, â€”CONH2, â€”CONHR, â€”CON(R)2, â€”OH, â€”OR, oxo-, â€”SH, â€”NHCOR, and â€”NHCO2R wherein R is C2-C6 alkyl or benzyl and/or (ii) fused to a cycloalkyl or heterocyclic ring; R2 is a C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, phenyl(C1-C6 alkyl)-, heteroaryl(C1-C6 alkyl)-, phenyl(C2-C6 alkenyl)-, heteroaryl(C2-C6 alkynyl)-, cycloalkyl(C1-C6 alkyl)-, cycloalkyl(C2-C6 alkenyl)-, cycloalkyl(C2-C6 alkynyl)-, cycloalkenyl(C1-C6 alkyl)-, cycloalkenyl(C2-C6 alkenyl)-, cycloalkenyl(C2-C6 alkynyl)-, phenyl(C1-C6 alkyl)O(C1-C6 alkyl)-, or heteroaryl(C1-C6 alkyl)O(C1-C6 alkyl)- group, any one of which may be substituted by C1-C6 alkyl, C1-C6 alkoxy, halo, cyano (â€”CN), phenyl, or phenyl substituted by (C1-C6) alkyl, (C2-C6) alkoxyl, halo, or cyano (â€”CN); R3 is the side chain of a natural or non-natural &agr; amino acid in which any functional groups may be protected; and R4 is an ester or thioester group of the formula R9 O(C&boxH;O)â€” â€”(C&boxH;O)SR9, â€”(C&boxH;S)SR9, or â€”(C&boxH;S)OR9 wherein R9 is (C1-C6)alkyl, (C2-C6)alkenyl, cycloalkyl, cycloalkyl(C1-C6)alkyl-, phenyl, heterocyclyl, phenyl(C1-C6)alkyl-, heterocyclyl(C1-C6)alkoxy(C1-C6)alkoxy(C1-C6)alkoxy(C1-C6)alkyl-, any of which may be substituted on a ring or non-ring carbon atom or on a ring heteroatom, or a pharmaceutically acceptable salt, hydrate or solvate thereof,PROVIDED THAT:(i) (i) when R and R1 are hydrogen, R2 is 4-chlorophenylpropyl, and R3 is tertbutyl, then R4 is not a methyl carboxylate ester group; and (ii) when R and R1 are hydrogen, R2 is phenylmethyl, and R3 is 1-methylprop-1-yl, then R4 is not a tert-butyl carboxylate ester group.