Pyrroloisoquinolinyl-dimethyloxoalkyl alkonoates and their use a

Details Pyrroloisoquinolinyl-dimethyloxoalkyl alkonoates and their use a Pyrroloisoquinolinyl-dimethyloxoalkyl alkonoates and their use a

1986-05-23

1988-03-22

Jiles, Henry R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514284, 546 84, 546 70, 560262, 560185, A61K 3140, A61K 31435, C07D47104, C07C 6702

Patent

active

047329025

ABSTRACT:
The invention relates to long-acting depot producing antipsychotic pyrroloisoquinolinyl-dimethyloxoalkyl alkanoates of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently, are hydrogen, alkyl of 1 to 4 carbon atoms, cycloalkyl or alkenyl, or taken together are alkylene of 3 to 6 carbon atoms; and R.sub.3 is hydrogen, alkyl, hydroxyalkyl, phenylhydroxyalkyl, halophenylhydroxyalkyl, alkylphenylhydroxyalkyl, alkoxyphenylhydroxyalkyl, alkoxyalkyl, aryloxyhydroxyalkyl, alkoxyhydroxyalkyl, acyloxyalkyl, arylcarbonylalkyl, alkoxycarbonylalkyl, aralkyl, alkenyl, alkylcycloalkyl, alkynyl, thienylalkyl, furylalkyl, arylcarboxamidoalkyl, acylalkyl, cyclic-alkyloxoalkyl, cyclic-alkylhydroxyalkyl, alkenyloxyalkyl, aralkenyl, aryloxyalkyl, or aryl-N-imidazolonylalkyl; R.sub.4 is alkyl; and n is the integer 2 or 3,
their corresponding optical isomers, geometric isomers, and mixtures thereof, and the pharmaceutically acceptable acid additional salts.
The compounds of formula I are useful as antipsychotic agents.

REFERENCES:
patent: 4260762 (1981-04-01), Berger et al.
patent: 4334070 (1982-06-01), Berger et al.
C.A. 28-Heterocycles, vol. 84 1976 84: 121690T.
CA 35 Synthetic High Polymers, vol. 79, 1973 67040n.
C.A. 23-Aliphatics, vol. 78, 1973 71478h.
C.A. vol. 77, 1972 74835n.
C.A. 23-Aliphatics, vol. 76, 1972-3405r.
C.A. vol. 69, 1968 51496y.
C.A. vol. 75, 1971-5191w.
C.A. 28-Heterocycles, vol. 96, 1982 96:199688j.
C.A. vol. 100, 1984-100:34529c.
C.A. vol. 93, 1980 93: 185705V.

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