Abstract Compounds of the formula <IMAGE> I wherein R1 is hydrogen, alkanoyl or aroyl; R2 is hydrogen or alkyl; R3 is hydrogen or aryl; R4 and R5 each are hydrogen or R4 and R5 taken together are oxo; and Y is -CH2-, -CH2CH2- or -N(R6)- in which R6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is -N(R6)-, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described. The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
A compound of the formula ##STR25## wherein R 3 is hydrogen or phenyl which may be substituted with one or more substituents selected from halogen, alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 8 carbon atoms or trifluromethyl; R 4 and R 5 each are hydrogen or R 4 and R 5 taken together are oxo; R 20 is alkyl having 1 to 8 carbon atoms; Y is --CH 2 --, --CH 2 CH 2 or --N(R 60 )-- in which R 60 is alkyl having 1 to 8 carbon atoms or benzyl, 2-phenylethyl, 3-phenylpropyl, 4-chlorobenzyl or 4-methoxybenzyl; and Z is a halogen atom, an alkylsulfonate group group having 1 to 8 carbon atoms or the p-toluenesulfonate group.
Claim 2
Dependent Claim
121 words
A compound of the formula ##STR25## wherein R 3 is hydrogen or phenyl which may be substituted with one or more substituents selected from halogen, alkyl having 1 to 8 carbon atoms, alkoxy having 1 to 8 carbon atoms or trifluromethyl; R 4 and R 5 each are hydrogen or R 4 and R 5 taken together are oxo; R 20 is alkyl having 1 to 8 carbon atoms; Y is --CH 2 --, --CH 2 CH 2 or --N(R 60 )-- in which R 60 is alkyl having 1 to 8 carbon atoms or benzyl, 2-phenylethyl, 3-phenylpropyl, 4-chlorobenzyl or 4-methoxybenzyl; and Z is a halogen atom, an alkylsulfonate group group having 1 to 8 carbon atoms or the p-toluenesulfonate group.
Claim 3
Dependent Claim
9 words
A compound, in accordance with claim 1, tert.butyl 8-benzyl-octahydro-9-methanesulfonyloxymethyl-6,10-dioxo-6H-pyridazo[1,2-a][1,2,5]triazepine-1(S)-carboxylate.
Claim 4
Dependent Claim
9 words
A compound, in accordance with claim 1, tert.butyl 8-methyl-octahydro-9-methanesulfonyloxymethyl-6,10-dioxo-6H-pyridazo[1,2-a][1,2,5]triazepine-1(S)-carboxylate.