Patent ID: 6288105
Filing Date: 2001-09-11
Classification: A61P,C07D

Abstract:
A compound of formula I, or a pharmaceutically acceptable salt thereof, ##STR83##whereinD is CH, CR.sup.d or N in which R.sup.d is methyl or methoxy;E is CH, CR.sup.e or N in which R.sup.e is methyl, methoxy or halo;R.sup.2 is --{X.sup.2 --(CH.sub.2).sub.n }.sub.p --N(R.sup.a)--CO--A in which X.sup.2 is a direct bond, methylene or O; n is 1, 2, 3 or 4; p is 0 or 1, R.sup.a is hydrogen or methyl; and --CO--A is an .alpha.-amino acyl group derived from an .alpha.-amino acid selected from glycine, alanine, valine, leucine, isoleucine, phenylalanine, tyrosine, serine, threonine, methionine, cysteine, proline, azetidine-2-carboxylic acid, pipecolic acid, aspartic acid, asparginine, glutamic acid, glutamine, lysine, arginine or histidine in which an amino group may bear a t-butoxy carbonyl protecting group; a carboxy group may be protected as its (1-4C)alkyl ester; a hydroxy group may bear a benzyl protecting group; and a thiol group may bear a t-butyl protecting group; or --CO--A is represented as --CO--CH(R.sup.b)--NR.sup.f R.sup.g, each of R.sup.f and R.sup.g is hydrogen or methyl, or --NR.sup.f R.sup.g is a pyrrolidino, piperidino, morpholine or 1,1-dioxo thiomorpholin-4-yl group (and R.sup.b denotes the side chain or protected side chain of an .alpha.-amino acyl group as defined hereinabove), provided that p is 1 when --CO--A is a glycyl or N-substituted glycyl group; or --CO--A is 3-amino-4-hydroxy-1-oxobutyl;R.sup.3 is --X.sup.3 --(CH.sub.2).sub.s --NR.sup.s R.sup.t or --CH.sub.2 --R.sup.k, in which X.sup.3 is a direct bond, methylene or O; s is 1 or 2; provided that when s is 1, then X.sup.3 is a direct bond; and R.sup.s and R.sup.t are independently hydrogen or (1-3C)alkyl or the group NR.sup.s R.sup.t is pyrrolidino, piperidino, or morpholino; and R.sup.k is 2-oxopyrrolidin-1-yl or 3-(1-oxoethyl)imidazolidin-1-yl; andR.sup.6 is hydrogen, hydroxy or methoxy.