Patent ID: 6057311
Filing Date: 2000-05-02
Classification: A61K,C07D,C07K

Abstract:
A compound of the formula ##STR10## wherein one of U and V is --CHR.sup.2 --, and the other of U and V is selected from the group consisting of --N(COR.sup.4)--, --CH(COR.sup.4)--, --N(SO.sub.2 R.sup.4)-- and --CH(SO.sub.2 R.sup.4)--, in which:R.sup.2 is H, --COOR.sup.5 wherein R.sup.5 is H or C.sub.1 to C.sub.4 hydrocarbyl, --CONR.sup.6 R.sup.7 wherein R.sup.6 is H or methyl and R.sup.7 is aryl, substituted aryl, or a group of the formula --(C.sub.1 to C.sub.4)alkylene-W, in which W is amidino, hydroxy, acyloxy, sulphamoyl, hydroxysulphonyl, carboxy, esterified carboxy, amidated carboxy, tetrazolyl, hydroxamyl, R.sup.14 --SO.sub.2 --NH--, R.sup.14 --SO.sub.2 --NH--CO--, R.sup.14 --SO.sub.2 --, R.sup.14 --SO--, R.sup.14 --CO--, R.sup.14 --CO--NH--, R.sup.14 --CO--NH--SO--, R.sup.14 --CO--NH--SO.sub.2 --, or R.sup.15 --NH--SO.sub.2 -- wherein R.sup.14 is selected from the group consisting of H, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 haloalkyl, aryl and substituted aryl, except that R.sup.14 may not be H when attached to a sulphur atom, and R.sup.15 is H, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 haloalkyl, aryl, substituted aryl, --OH or --CN; or R.sup.6 and R.sup.7 together form a carboxy-substituted propylene, butylene or pentylene group or --COR.sup.7 ; and R.sup.4 is H, C.sub.1 to C.sub.6 hydrocarbyl in which up to three of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom, provided that R.sup.4 does not contain a --O--O-- group, or R.sup.4 is a group of the formula --Q--R.sup.16 wherein Q is selected from the group consisting of a bond, --NR.sup.7 -- in which R.sup.17 is H or C.sub.1 to C.sub.3 alkyl and --O--, and R.sup.16 is aryl, substituted aryl, arylalkyl or (substituted aryl)alkyl;R is independently C.sub.1 to C.sub.3 alkyl,R.sup.1 is H or C.sub.1 to C.sub.15 hydrocarbyl wherein one or more hydrogen atoms may be replaced by halogen atoms, and one carbon atom may be replaced by a nitrogen, oxygen or sulphur atom;R.sup.3 is independently halo, alkyl, --NO.sub.2, --NH.sub.2 or --NHCOR.sup.5 ;X is H, and Y is H or C.sub.1 to C.sub.10 hydrocarbyl wherein one or more hydrogen atoms may be replaced by halogen atoms, and one carbon atom may be replaced by a nitrogen, oxygen or sulphur atom; or X and Y together are .dbd.O or .dbd.CH.sub.2 ;Z is: H; C.sub.1 to C.sub.15 hydrocarbyl, in which one or more hydrogen atoms may be replaced by a halogen atom, and up to three of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom, provided that Z does not contain a --O--O-- group; or --(CHR.sup.18).sub.m --R.sup.8, wherein R.sup.18 is H or C.sub.1 to C.sub.3 alkyl and R.sup.8 is phenyl, substituted phenyl or a group of the formula --COOR.sup.9 or --CONR.sup.9 R.sup.10, in which R.sup.9 and R.sup.10 are independently H or C.sub.1 to C.sub.6 alkyl, or R.sup.9 and R.sup.10 together form a propylene, butylene, pentylene or hexylene group; m is 1, 2 or 3; andn and p are independently from 0, 1, 2, or 3,or a pharmaceutically acceptable salt thereof.