摘要:
For use an an anticonvulsive: dihydrouracil compounds of the formula where one of A and B is (where Y, Y 2 and Y 3 are each H, C 1 -C 4 straight- or branched-chain alkyl, halogen, nitro, amino. carboxyl, alkoxycarbonyl of 2-7 carbon atoms or -CF 3 ), naphthyl or diphenylmethyl and the other is H, C 1 -C 6 straight- or branched-chain alkyl, C 1 -C 6 alkenyl, cyclopentyl, cyclohexyl or (where Z 1 , Z 2 and Z 3 are each H, C 1 -C 4 straight- or branched-chain alkyl, halogen or -CF 3 ); X is 0 or S; and R 1 , R 2 and R 3 are each H or C 1 -C 3 straight- or branched-chain alkyl.
摘要:
A phosphorus-containing peptide derivative represented by the general formula [I]: {wherein R, is hydrogen, lower alkyl, lower alkoxycarbonyl, aralkyloxycarbonyl or [wherein R e is hydrogen, alkyl having 1 to 17 carbon atoms, unsubstituted or substituted aryl (wherein the substituent is selected from lower alkyl, lower alkoxy and halogen), unsubstituted or substituted aralkyl (wherein the substituent is selected from lower alkyl, lower alkoxy and halogen), or cycloalkyl having 5 or 6 carbon atoms]; R 2 is hydrogen, unsubstituted or substituted lower alkyl (wherein the substituent is selected from amino, mercapto, lower alkylthio, carboxyl, hydroxyl, guanidino and imidazolyl), unsubstituted or substituted aryl (wherein the substituent is selected from amino, hydroxyl, lower alkoxy, aralkyloxy, lower alkyl, halogen and nitro), unsubstituted or substituted aralkyl (wherein the substituent is seiected from amino, lower alkyl halogen and nitro) or
(wherein R 7 has the same meaning as R 3 ); R 3 is hydrogen, lower alkyl, unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R e ), R 8 -CO-(wherein R 8 has the same meaning as R e ), R 9 -O-CO-[wherein R 9 is lower alkyl, unsubstituted or substituted aryl (wherein the substituent has the same meaning as in R e ), unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R 8 )], or R 9 NHCO- (wherein R 9 has the same meaning as defined above); and R 4 and R 5 are the same or different, and are hydrogens, alkyls having 1 to 18 carbon atoms, unsubstituted or substituted aryl (wherein the substituent has the same meaning as in R e ), unsubstituted or substituted aralkyl (wherein the substituent has the same meaning as in R 6 ), -(CH 2 CH 2 O) m CH 3 (wherein m is an integer of 1 - 4), or -CH[CH 2 OCO(CH 2 ) n CH 3 ] 2 (wherein n is 0 or an integer of 1 - 10) }, and pharmacologically acceptable salts thereof is prepared. Said compounds have an angiotensin converting enzyme-inhibiting action and as the result an anti-hypertensive action.
摘要:
New piperidine derivatives are disclosed having the following general formula: wherein Y is a group represented by R 10 or R 10 is hydrogen, alkyl having 1 - 3 carbon atoms, or substituted or unsubstituted benzyl, and when Y is Q is H; m is 0 or an integer of 1 - 5; A is hydroxyl, halogen, C 1 -C 5 alkyl, C 1 -C 5 alkoxy, C 2 -C 5 alkenyloxy, C 2 -C 5 alkinyloxy, C 1 -C 5 alkylthio, carboxyl, C 1 -C 5 alkoxycarbonyl, nitro, amino, C 1 -C 5 alkylamino, C 1 -C 5 alkanoylamino, sulfamoyl, mono or di-(C I -C 5 alkyl) aminosulfonyl, C 1 -C 5 alkylsulfonyl, carbamoyl, cyano or trifluoromethyl; when m is 2 or more, the A groups may be the same or different, or two A groups may be combined to form a C 1 -C 5 alkylenedioxy group; X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene; R is straight-chain alkylene having 1 - 4 carbon atoms, or straight-chain alkylene having 1 - 4 carbon atoms and having a C 1 -C 5 alkyl substituent; Q is hydrogen, C 1 -C 5 alkyl, halogen, hydroxyl or C 1 -C 5 alkanoyloxy; n is 0 or an integer of 1 - 4; R 2 is hydroxyl, C 1 -C 5 alkoxy, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, nitro or amino; when n is 2 or more, the R 2 groups may be the same or different, or two R 2 groups may by combined to form a C 1 -C 5 alkylenedioxy; B is -NH-, -N(R)- (wherein R is C 1 -C 5 alkyl, or substituted or unsubstituted phenyl) or -0-; and acid addition salts thereof. The new piperidine derivatives wherein Y is have a hypotensive activity.