Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1985-08-12
1987-09-08
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514221, 514248, 540460, 540500, 540501, 544238, A61K 3150, C07D24500, C07D48706, C07D23702
Patent
active
046924388
ABSTRACT:
Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,
as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, 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.
REFERENCES:
patent: 4512924 (1985-04-01), Attwood et al.
Natoff et al, Chem. Abst., 103-81466b.
Derwent 17676D (abstract).
Derwent 25836D (abstract).
Derwent 209E (abstract).
Derwent 83-821929 (abstract).
Hassall Cedric H.
Lawton Geoffrey
Redshaw Sally
Daus Donald G.
Hoffmann-La Roche Inc.
Isgro William G.
Leon Bernard S.
Saxe Jon S.
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