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2-Azasfiro[4.(3+N)]-3-carboxylic acid derivatives, a process for their preparation, agents containing these derivatives and their use
| Details |
Inventors: Teetz, Volker; Urbach, Hansjorg; Becker, Reinhard;
Assignee: Hoechst Aktiengesellschaft (DE)
Primary Examiner:
Assistant Examiner:
Attorney, Agent or Firm:
The invention relates to compounds of the formula I ##STR1## in which n denotes 1, 2, 3 or 4, R is alkyl, alkenyl cycloalkyl, aryl, optionally mono-, di- oder trisubstituted by alkyl, alkoxy, hydroxy, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or indol-3-yl, R.sup.1 denotes an optionally protected radical of a naturally occurring amino acid HOOC--CH(NH.sub.2)--R.sup.1, R.sup.2 denotes hydrogen, alkyl or optionally nitro-substituted aralkyl, R.sup.3 denotes hydrogen, alkyl or cycloalkyl or optionally nitro-substituted aralkyl and X denotes 2 hydrogen atoms or 1 oxygen atom, their physiologically tolerated salts with acids and, if R.sup.2 and/or R.sup.3 denote hydrogen, with bases, a process for their preparation, agents containing these derivatives and their use as medicaments. |
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DETAILED DESCRIPTION We claim: 1.
A compound of the formula I ##STR11## in which n denotes 1, 2, 3 or 4, R denotes (C.
sub.
1 -C.
sub.
6)-alkyl, (C.
sub.
2 -C.
sub.
6)-alkenyl, (C.
sub.
5 -C.
sub.
9)-cycloalkyl, (C.
sub.
6 -C.
sub.
12)-aryl, optionally mono-, di- or trisubstituted by (C.
sub.
1 -C.
sub.
4)-alkyl, (C.
sub.
1 -C.
sub.
4)-alkoxy, hydroxy, halogen, nitro, amino, (C.
sub.
1 -C.
sub.
4)-alkylamino, di-(C.
sub.
1 -C.
sub.
4)-alkylamino or methylenedioxy or indol-3-yl, R.
sub.
1 denotes a side-chain of an amino acid selected from the group consisting of Ala, Ser, Thr, Val, Leu, Ile, Asp, Asp-NH2, Glu, Glu-NH2, Cys, Met, Arg, Lys, Hyl, Orn, Cit, Tyr, Phe, Trp and His, a side chain of Lys, Hyl or Orn, the amino group of which is protected by (C.
sub.
1 -C.
sub.
6)-alkanoyl, or Ser, Thr, Hyl or Tyr, the hydroxyl group of which is protected by alkyl, R.
sup.
2 denotes hydrogen, alkyl having 1 to 6 C atoms or optionally nitro-substituted aralkyl having 7 to 9 C atoms, R.
sup.
3 denotes hydrogen, alkyl having 1 to 10 C atoms, cycloalkyl having 3 to 10 C atoms or optionally nitro-substituted aralkyl having 7 to 9 C atoms and X denotes 2 hydrogen atoms or 1 oxygen atom, and its physiologically tolerated salts with acids and, if R.
sup.
2 and/or R.
sup.
3 denote hydrogen, with bases.
2.
A compound of the formula I as claimed in claim 1, wherein the C atom in the 3-position of the spirocycle and the C atoms marked with an asterisk in the chain each have the S configuration.
3.
A compound of the formula I as claimed in claim 1, wherein R.
sup.
1 denotes methyl, 4-methoxybenzyl or 4-ethoxybenzyl, R.
sup.
2 denotes hydrogen, an alkyl having 1 to 4 C atoms, benzyl or nitrobenzyl and R.
sup.
3 denotes hydrogen.
4.
A compound of the formula I as claimed in claim 1, wherein n denotes 2, R.
sup.
1 denotes 4-methoxybenzyl or 4-ethoxybenzyl.
5.
A pharmaceutical composition comprising (1) a hypotensively effective amount of a compound as claimed in claim 1 or a pharmaceutically acceptable salt thereof; and (2) a pharmaceutically acceptable carrier.
6.
A method of treating hypertension by administering to a patient a compound as claimed in claim 1 or a pharmaceutically acceptable salt thereof in an amount effective to achieve a hypotensive effect in said patient
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Vasodialators 
