Patent ID: 6333338
Filing Date: 2001-12-25
Classification: A61P,C07D,Y02P

Abstract:
Compounds of formula: ##STR16##in which:i) either R.sub.1 is chosen from:C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.12 mono- or bicyclic cycloalkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl groups, these groups optionally being substituted with groups chosen from halogens and the hydroxyl group;mono-, bi- or tricyclic C.sub.6 -C.sub.14 aryl groups,heteroaryl groups chosen from pyridyl, thienyl, furyl, quinolyl, benzodioxanyl, benzodioxolyl, benzothienyl, benzofuryl and pyrazinyl groups;phenyl (C.sub.1 -C.sub.4)alkyl and naphthyl(C.sub.1 -C.sub.4)alkyl groups optionally substituted on the aryl nucleus,the aryl and heteroaryl groups possibly being substituted with one or more groups chosen independently from halogens, C.sub.1 -C.sub.4 alkyl, trifluoromethyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkyloxy, nitro and groups --COOR, --CH.sub.2 COOR or --O--CH.sub.2 --COOR, R being a C.sub.1 -C.sub.4 alkyl group,the groups of formula: ##STR17##in which R.sub.4 and R'.sub.4 are chosen from C.sub.1 -C.sub.8 alkyl and mono- or polycyclic C.sub.3 -C.sub.12 cycloalkyl groups, these groups optionally being substituted with groups chosen from halogens and the hydroxyl group, R'.sub.4 also possibly being hydrogen, or alternatively R.sub.4 and R'.sub.4 together form a tetramethylene or pentamethylene group, these last two groups themselves possibly being substituted, in particular with a C.sub.6 -C.sub.14 aryl or (C.sub.6 -C.sub.14)aryl(C.sub.1 -C.sub.4)alkyl residue;the groups of formula: ##STR18##in which m=1 to 4 and R.sub.5 is chosen from phenyl, methoxyphenyl, indolyl, benzodioxolyl, benzodioxanyl, benzothienyl and benzofuryl groups,and R.sub.2 is hydrogen,ii) or R.sub.1 is hydrogen and R.sub.2 is chosen from the groups of formula:--NH--CO--R.sub.6,R.sub.6 being chosen from C.sub.1 -C.sub.4 alkoxy, C.sub.3 -C.sub.7 cycloalkoxy, benzyloxy, methoxyphenyl, dimethoxyphenyl, benzodioxolyl and benzodioxanyl groups,and the groups of formula:--NH--SO.sub.2 --R.sub.7,R.sub.7 being chosen from:C.sub.1 -C.sub.5 alkyl groups optionally substituted with one or more groups chosen from halogens, hydroxyl groups and the trifluoromethyl group;C.sub.2 -C.sub.5 alkenyl groups;mono- or bicyclic C.sub.3 -C.sub.12 cycloalkyl groups;mono-, bi- or tricyclic C.sub.6 -C.sub.14 aryl groups;heteroaryl groups chosen from pyridyl, furyl, thienyl, quinolyl, benzodioxanyl, benzodioxolyl, isoxazolyl, benzodioxinyl, benzothienyl, thiazolyl, pyrazolyl, benzofuryl and benzothiazolyl groups;phenyl(C.sub.1 -C.sub.4)alkyl and naphthyl(C.sub.1 -C.sub.4)alkyl groups;and the groups of formula: ##STR19##in which n=1, 2 or 3 and B is chosen from --CH.sub.2 --, O or S and --NH--,the aryl or heteroaryl groups optionally being substituted with one or more groups chosen independently from halogens, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, trifluoromethyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkyloxy, C.sub.1 -C.sub.4 alkylsulfonyl, nitro, di((C.sub.1 -C.sub.4)alkyl)amino and groups --COOR, --CH.sub.2 --COOR or --O--CH.sub.2 COOR, R being a C.sub.1 -C.sub.4 alkyl group, phenyl and naphthyl groups and heteroaryl groups chosen from thienyl, furyl and pyridyl groups,iii) R.sub.3 is chosen from a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group and a phenyl (C.sub.1 -C.sub.4) alkyl group;iv) A is chosen from groups --NH--CHR.sub.10 --, --NH--CHR.sub.10 --CH.sub.2 -- and ##STR20##with p=1 or 2,R.sub.10 being chosen from hydrogen, a C.sub.1 -C.sub.4 alkyl group and a C.sub.6 -C.sub.14 aryl group,v) and Z.sub.1 and Z.sub.2 are hydrogen or an amine-protecting group, and the addition salts thereof with pharmaceutically acceptable acids.