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Summary for Patent: 4,933,361
|Title:||Derivatives of bicyclic aminoacids agents containing these compounds and their use|
|Abstract:||Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0, 1 or 2, R.sub.1 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl which can optionally be substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 -C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 -C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.6 -C.sub.9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, hydroxyl, halogen, nitro, amino, (C.sub.1 -C.sub.4)-alkylamino, di-(C.sub.1 -C.sub.4 -alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process of the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.|
|Inventor(s):||Urbach; Hansjorg (Kronberg/Tannus, DE), Henning; Rainer (Frankfurt am Main, DE), Teetz; Volker (Hofheim am Taunus, DE), Geiger; Rolf (Frankfurt am Main, DE), Becker; Reinhard (Wiesbaden, DE), Gaul; Holger (Niederneisen, DE)|
|Assignee:||Hoechst Aktiengesellschaft (Framkfurt am Main, DE)|
|Patent Litigation and PTAB cases:||See patent lawsuits and PTAB cases for patent 4,933,361|
1. A compound of the formula ##STR33## or a physiologically acceptable salt thereof, wherein the hydrogen atoms on the bridgehead C atoms in the 3a-position and 7a-position have the
trans-configuration relative to one another and those carbon atoms labelled with an asterisk all have the (S) configuration;
R.sub.1 is (C.sub.1 -C.sub.3)-alkyl; and
R.sub.2 is hydrogen or (C.sub.1 -C.sub.4)-alkyl.
2. A compound or salt as in claim 1 wherein the C atom in the 2-position of the bicyclic ring system and those C atoms in the side chain labeled with an asterisk all have the S configuration.
3. A compound or salt as in claim 1 wherein the hydrogen atoms on the bridgehead C atom in the 3a-position and on the C atom in the 2-position of the bicyclic ring system are on the same side of the reference plane of the ring atoms.
4. A compound or salt as in claim 1 wherein the hydrogen atoms on the bridgehead C atom in the 3a-position and on the C atom in the 2-position of the bicyclic ring system are on opposite sides of the reference plane of the ring atoms.
5. A compound or salt as in claim 1 wherein R.sub.1 is methyl and X is phenyl.
6. A compound or salt as in claim 1 wherein R.sub.2 is hydrogen or ethyl.
7. A compound as in claim 1 which is N-(1S-carbethoxy-3-phenylpropyl)-S-alanyl-2S,3aS,7aR-octahydroindole-2-car boxylic acid or a physiologically acceptable salt thereof.
8. A compound as in claim 1 which is N-(1S-carbethoxy-3-phenylpropyl)-S-alanyl-2S,3aR,7aS-octahydroindole-2-car boxylic acid or a physiologically acceptable salt thereof.
9. A method for treating high blood pressure in a patient suffering therefrom which comprises administering to said patient a hypotensively effective amount of a compound or salt as in claim 1.
10. A composition for the treatment of high blood pressure comprising a hypotensively effective amount of a compound or salt as in claim 1 and a pharmaceutically acceptable excipient therefor.
11. A method as in claim 9 wherein said compound or salt is administered together with a diuretic.
12. A composition as in claim 10 which additionally comprises a diuretic.
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