Patent ID: 6326359
Filing Date: 2001-12-04
Classification: A61P,C07H

Abstract:
A compound of formula (I): ##STR143##whereinR.sup.1 is alkyl or cyclopropylmethyl;R.sup.2 is phenyl-alkylene or naphthyl-alkylene, said alkylene chain being optionally further substituted by phenyl or naphthyl, each phenyl or naphthyl being optionally substituted by one or more substituents each independently selected from alkyl, alkoxy, halo and cyano;n is 1 or 2;A is NR.sup.a, NR.sup.a C(O), NR.sup.a C(O)NR.sup.a, NR.sup.a C(O)O, OC(O)NR.sup.a, C(O)NR.sup.a, NR.sup.a SO.sub.2, SO.sub.2 NR.sup.a, O, S or SO.sub.2 ;R.sup.a is H, alkyl or benzyl optionally ring-substituted by one or more substituents each independently selected from alkyl, alkoxy, halo and cyano;R.sup.3 is a group of the formula --(CH.sub.2).sub.p --R.sup.p --B;p is 0, 1 or 2;R.sup.p is a bond, alkylene, cycloalkylene, phenylene or naphthylene, said cycloalkylene, phenylene and naphthylene each being optionally substituted by one or more substituents each independently selected from alkyl, alkoxy, halo and alkoxyalkylene;B is(i) H, --NR.sup.b R.sup.b, R.sup.b R.sup.b N-alkylene, --OR.sup.b, --COOR.sup.b, --OCOR.sup.b, --SO.sub.2 R.sup.b, --CN, --SO.sub.2 NR.sup.b R.sup.b, --NR.sup.b COR.sup.b, --NR.sup.b SO.sub.2 R.sup.b or --CONR.sup.b R.sup.b, in which each R.sup.b is the same or different and is selected from H, alkyl, phenyl and benzyl, provided that,(a) when B is --OCOR.sup.b, --SO.sub.2 R.sup.b, --NR.sup.b COR.sup.b or --NR.sup.b SO.sub.2 R.sup.b, then the terminal R.sup.b is not H, and,(b) R.sup.p is a bond, p is 0 and B is H only when A is NR.sup.a, NR.sup.a C(O)NR.sup.a, OC(O)NR.sup.a, C(O)NR.sup.a, SO.sub.2 NR.sup.a, O or S,(ii) an optionally-substituted, fully- or partially-saturated or -unsaturated, mono- or bicyclic, heterocyclic group, which is linked to R.sup.p by a ring carbon atom, or(iii) N-linked azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl, each optionally substituted by one or more alkyl substituents, with the proviso that --(CH.sub.2).sub.p --R.sup.p -- is not --CH.sub.2 --; andwhere A is NR.sup.a, C(O)NR.sup.a, OC(O)NR.sup.a or SO.sub.2 NR.sup.a, R.sup.a and R.sup.3 taken together with the nitrogen atom to which they are attached can form an azetidine, pyrrolidine, piperidine or piperazine ring, optionally substituted by one or more alkyl substituents:or a pharmaceutically acceptable salt or solvate thereof.