Patent ID: 6022873
Filing Date: 2000-02-08
Classification: A61P,C07D,Y02P

Abstract:
A compound of formula (I) ##STR73## wherein V is HO-- or HONH--n is 1, 2, 3 or 4;R.sub.1 is a C.sub.1 -C.sub.12 alkyl,C.sub.2 -C.sub.12 alkenyl,C.sub.2 -C.sub.12 alkynyl,perfluoroalkyl,phenyl(C.sub.1 -C.sub.6 alkyl)-,heteroaryl(C.sub.1 -C.sub.6 alkyl)-,non-aryl heterocyclyl(C.sub.1 -C.sub.6 alkyl)-,cycloalkyl(C.sub.1 -C.sub.6 alkyl)-,cycloalkenyl(C.sub.1 -C.sub.6 alkyl)-,phenoxy(C.sub.1 -C.sub.6 alkyl)-,heteroaryloxy(C.sub.1 -C.sub.6 alkyl)-,phenyl(C.sub.1 -C.sub.6 alkyl)O(C.sub.1 -C.sub.6 alkyl)-,heteroaryl(C.sub.1 -C.sub.6 alkyl)O(C.sub.1 -C.sub.6 alkyl)-,phenyl(C.sub.1 -C.sub.6 alkyl)S(C.sub.1 -C.sub.6 alkyl)- orheteroaryl(C.sub.1 -C.sub.6 alkyl)S(C.sub.1 -C.sub.6 alkyl)- group,any one of which may be optionally substituted by C.sub.1 -C.sub.6 alkyl, trifluoromethyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, halo, cyano (--CN), phenyl, substituted phenyl or heteroaryl;R.sub.2 is a saturated 5- to 8-membered monocyclic N-heterocyclic ring which is attached via the N atom and which, (i) optionally contains as a ring member O, S, SO, SO.sub.2, or NR.sub.5 wherein R.sub.5 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.6 alkoxy)C.sub.1 -C.sub.6 alkyl, benzyl, acyl, an amino protecting group, or a group --SO.sub.2 R.sub.6 wherein R.sub.6 is C.sub.1 -C.sub.6 alkyl or a substituted or unsubstituted phenyl or heteroaryl group, and/or (ii) is optionally substituted on one or more C atoms by hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, cyano, oxo, ketalised oxo, amino, mono(C.sub.1 -C.sub.6 alkyl)amino, di(C.sub.1 -C.sub.6 alkyl)amino, carboxy, C.sub.1 -C.sub.6 alkoxycarbonyl, hydroxymethyl, C.sub.1 -C.sub.6 alkoxymethyl, carbamoyl, mono(C.sub.1 -C.sub.6 alkyl)carbamoyl, di(C.sub.1 -C.sub.6 alkyl)carbamoyl, or hydroxyimino;R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or acetyl; andR.sub.4 is optionally substitutedC.sub.1 -C.sub.6 alkyl,C.sub.2 -C.sub.6 alkenyl,C.sub.2 -C.sub.6 alkynyl,C.sub.1 -C.sub.3 perfluoroalkyl,cycloalkyl,cycloalkyl(C.sub.1 -C.sub.6 alkyl)-,cycloalkenyl,cycloalkenyl(C.sub.1 -C.sub.6 alkyl)-,di-(C.sub.1 -C.sub.6 alkyl)amino,phenyl,phenyl(C.sub.1 -C.sub.6 alkyl)-,biphenyl,phenyl-heteroaryl,naphthyl,non-aryl heterocyclyl,non-aryl heterocyclyl(C.sub.1 -C.sub.6 alkyl)-,heteroaryl orheteroaryl(C.sub.1 -C.sub.6 alkyl)-;heteroaryl-phenyl;heteroaryl-heteroaryl;aryloxyaryl;or a pharmaceutically acceptable salt hydrate or solvate thereof.