Patent ID: 6172100
Filing Date: 2001-01-09
Classification: A61P,C07D

Abstract:
A method of inhibiting thrombin comprising using an effective amount of a thrombin inhibiting compound of formula I (or a pharmaceutically acceptable salt thereof) ##STR25##whereinE is CH or CR.sup.e in which R.sup.e is methyl, methoxy or halo;R.sup.1 is carboxy, [(1-4C)alkoxy]carbonyl, hydroxymethyl or --X.sup.1 --(CH.sub.2).sub.s --NR.sup.s R.sup.t in which X.sup.1 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;R.sup.2 is benzyloxy, --X.sup.2 --(CH.sub.2).sub.m --NR.sup.a R.sup.b in which X.sup.2 is a direct bond, methylene, O or S; m is 1, 2, 3, 4 or 5;provided that when m is 1, then X.sup.2 is a direct bond; and R.sup.a and R.sup.b are independently hydrogen or (1-3C)alkyl or the group NR.sup.a R.sup.b is pyrrolidino, piperidino, or morpholino; orR.sup.2 is --X.sup.2 --(CH.sub.2).sub.n --R.sup.f in which X.sup.2 is a direct bond, methylene or O; n is 1, 2 or 3; and R.sup.f is 5-tetrazolyl, carboxy, [(1-4C)alkoxy]carbonyl or hydroxymethyl;R.sup.3 is hydrogen, chloro or a benzyl group which may bear a methyl or methoxy substituent at the 3-position and a [(1-4C)alkoxy]carbonyl substituent at the 4-position; andR.sup.5 is hydrogen, hydroxy or methoxy; andprovided that at least one of R.sup.1 and R.sup.2 includes an amino moiety --NR.sup.s R.sup.t or --NR.sup.a R.sup.b.