Cerebroprojection method
AssigneeBoehringer Ingelheim GmbH
InventorsWalter Losel, Otto Roos, Dietrich Arndts, Franz Josef Kuhn, Ilse Strelle
Life of this patent
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Abstract
The invention relates to the use of carbocyclically and heterocyclically fused dihydropyridines as cerebroprotective agents, as agents for treating chronic inflammatory processes and as agents for inhibiting blood clotting, and also relates to new compounds of formula Ie ##STR1##
Claims9
A method of providing cerebroprotection in a warm-blooded animal which comprises administering to said animal a therapeutically effective amount of a carbocyclically and heterocyclically fused dihydropyridine of formula ##STR99## or the tautomeric form thereof of formula ##STR100## wherein X represents OR.sub.1 ;
- NHR.sub.2 ;
- NR.sub.3 R.sub.4 and R.sub.1 represents hydrogen, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxyalkyl
- R.sub.2 represents hydrogen;
- C.sub.3-6 -alkenyl, C.sub.3-6 -alkynyl;
- C.sub.3-6 -cycloalkyl;
- C.sub.3-6 -cycloalkenyl;
- straight-chained or branched C.sub.1-6 -alkyl which may if desired be mono- or polysubstituted with the substituents of groups a) to c) listed below, which may be identical or different:
- a) halogen;
- cyano;
- hydroxy;
- mercapto;
- C.sub.1-4 -alkoxy;
- C.sub.1-4 -alkylthio;
- amino;
- mono-C.sub.1-4 -alkylamino;
- di-C.sub.1-4 -alkylamino (wherein the alkyl radical may be identical or different) phenoxy (wherein the phenyl ring may be substituted as described in b) below.
- b) phenyl;
- optionally mono- or polysubstituted, by identical or different substituents, by the groups halogen, trifluoromethyl, C.sub.1-4 -alkoxy, hydroxy, mercapto, C.sub.1-4 -alkylthio, C.sub.1-4 -alkyl, amino, mono-C.sub.1-4 -alkylamino, di-C.sub.1-4 -alkylamino (wherein the alkyl groups may be identical or different), C.sub.2-3 -acylamino, C.sub.2-3 -acyloxy and the group --O--(CH.sub.2).sub.n --O vicinally by bound to the phenyl system (wherein n=1 or 2)
- c) a 5- or 6-membered saturated or wholly or partially unsaturated monocyclic heterocyclic group having up to 3 heteroatoms selected from the group N, O, S;
- and as a bicyclic heterocycle indole (whilst the above-mentioned heterocycles may be mono- or polysubstituted by C.sub.1-4 -alkyl), C.sub.3-6 -cycloalkyl;
- C.sub.5 or C.sub.6 -cycloalkenyl;
- C.sub.2-3 -acyl;
- C.sub.1-4 -alkylsulphonyl;
- or phenyl (which may in turn be substituted up to three times as described in b));
- or R.sub.2 represents phenyl, which may be substituted as described in b) above;
- R.sub.3 and R.sub.4 independently of each other represent C.sub.1-4 -alkyl, which may if desired be phenyl-substituted, whilst the phenyl substituent may in turn be substituted as under b) hereinbefore;
- or
- R.sub.3 and R.sub.4 together with the nitrogen atom to which they are bound represent a wholly or partially saturated heterocyclic 5- or 6-membered ring (which may also contain up to 2 further heteroatoms from the group N, O, S), whilst the heterocyclic group thus obtained may be substituted by C.sub.1-4 -alkyl, hydroxy or (CH.sub.2).sub.p -R.sub.5 (where p=0 or 1) and
- R.sub.5 represents a phenyl radical which is optionally substituted as under b) hereinbefore;
- A represents the fused ring systems ##STR101## wherein R.sub.8 represents hydrogen;
- C.sub.1-4 -alkyl or C.sub.1-4 -alkoxy
- R.sub.6 and R.sub.7 which may be identical or different represent hydrogen;
- hydroxy;
- C.sub.1-4 -alkyl;
- C.sub.1-4 -alkoxy;
- amino;
- methanesulphonylamino or
- R.sub.6 and R.sub.7 together represent -O--(CH.sub.2).sub.n --O-- (where n=1 or 2)
- R.sub.9 represents hydrogen;
- C.sub.1-4 -alkyl
- R.sub.10 represents hydrogen or 2-phenyl-2-ethoxycarbonylacetyl;
- and the salts thereof with physiologically acceptable acids, bases or complex-forming agents.
Dependencies are inferred from the claim text.