Aminoalkoxybenzopyranones as antipsychotic and anxiolytic agents

Claim 1

A compound of the formula ##STR24## wherein n is an integer from 2-5; R is hydrogen, lower alkyl, trifluoromethyl, or lower alkoxy; R 1 is a radical of the formula ##STR25## in which represents a single or double bond, Ar is phenyl or phenyl substituted by lower alkyl, lower alkoxy, lower thioalkoxy, halogen, or trifluoromethyl, and Het is 2-, 3-, or 4-pyridinyl or 2-, 3-, or 4-pyridinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-, 4-, or 5-pyrimidinyl, or 2-, 4-, or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-pyrazinyl or 2-pyrazinyl substituted by lower alkyl, lower alkoxy, or halogen; 2- or 3-thienyl, or 2- or 3-thienyl substituted by lower alkyl or halogen; 2- or 3-furanyl, or 2- or 3-furanyl substituted by lower alkyl or halogen, or 2- or 5-thiazolyl or 2- or 5-thiazolyl substituted by lower alkyl or halogen, or a pharmaceutically acceptable acid addition salt thereof, with the exclusion of the compound wherein R is hydrogen or lower alkyl and R 1 is a radical of the formula ##STR26## in which Ar is phenyl or phenyl substituted by lower alkyl, lowe alkoxy, halogen, lower thioalkoxy, or trifluoromethyl.

Claim 11

A method of treating psychosis in a subject suffering therefrom comprising administering to said subject an effective amount of a compound of the formula ##STR30## wherein n is an integer from 2-5; R is hydrogen, lower alkyl, lower alkoxy, or trifluoromethyl; R 1 is a radical of the formula ##STR31## in which is a single or double-bond; Ar is phenyl or phenyl substituted by lower alkyl, lower alkoxy, lower thioalkoxy, halogen, or trifluoromethyl, and Het is 2-, 3-, or 4-pyridinyl or 2-, 3 or 4-pyridinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-, 4-, or 5-pyrimidinyl or 2-, 4-, or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-pyrazinyl or 2-pyrazinyl substituted by lower alkyl, lower alkoxy, or halogen; 2- or 3-thienyl or 2- or 3-thienyl substituted by lower alkyl or halogen; 2- or 3-furanyl or 2- or 3-furanyl substituted by lower alkyl or halogen, or 2- or 5-thiazolyl or 2- or 5-thiazolyl substituted by lower alkyl or halogen, or a pharmaceutically acceptable acid salt thereof in unit dosage form.

Claim 12

A method of treating psychosis in a subject suffering therefrom comprising administering to said subject an effective amount of a compound of the formula ##STR30## wherein n is an integer from 2-5; R is hydrogen, lower alkyl, lower alkoxy, or trifluoromethyl; R 1 is a radical of the formula ##STR31## in which is a single or double-bond; Ar is phenyl or phenyl substituted by lower alkyl, lower alkoxy, lower thioalkoxy, halogen, or trifluoromethyl, and Het is 2-, 3-, or 4-pyridinyl or 2-, 3 or 4-pyridinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-, 4-, or 5-pyrimidinyl or 2-, 4-, or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-pyrazinyl or 2-pyrazinyl substituted by lower alkyl, lower alkoxy, or halogen; 2- or 3-thienyl or 2- or 3-thienyl substituted by lower alkyl or halogen; 2- or 3-furanyl or 2- or 3-furanyl substituted by lower alkyl or halogen, or 2- or 5-thiazolyl or 2- or 5-thiazolyl substituted by lower alkyl or halogen, or a pharmaceutically acceptable acid salt thereof in unit dosage form.

Claim 14

A method of treating anxiety in a subject suffering therefrom comprising administering to said subject an effective amount of a comound of the formula ##STR32## wherein n is an integer from 2-5; R is hydrogen, lower alkyl, lower alkoxy, or trifluoromethyl; R 1 is a radical of the formula ##STR33## in which represents a single or double bond, Ar is phenyl or phenyl substituted by lower alkyl, lower alkoxy, lower thioalkoxy, halogen, or trifluoromethyl, and Het is 2-, 3-, or 4-pyridinyl or 2-, 3-, or 4-pyridinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-, 4-, or 5-pyrimidinyl, or 2-, 4-, or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-pyrazinyl or 2-pyrazinyl substituted by lower alkyl, lower alkoxy, or halogen; 2- or 3-thienyl, or 2- or 3thienyl substituted by lower alkyl or halogen, 2- or 3-furanyl or 2- or 3-furanyl substituted by lower alkyl or halogen, or 2- or 5-thiazolyl or 2- or 5-thiazolyl substituted by lower alkyl or halogen, or a pharmaceutically acceptable acid salt thereof in unit dosage form.

Claim 15

A method of treating anxiety in a subject suffering therefrom comprising administering to said subject an effective amount of a comound of the formula ##STR32## wherein n is an integer from 2-5; R is hydrogen, lower alkyl, lower alkoxy, or trifluoromethyl; R 1 is a radical of the formula ##STR33## in which represents a single or double bond, Ar is phenyl or phenyl substituted by lower alkyl, lower alkoxy, lower thioalkoxy, halogen, or trifluoromethyl, and Het is 2-, 3-, or 4-pyridinyl or 2-, 3-, or 4-pyridinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-, 4-, or 5-pyrimidinyl, or 2-, 4-, or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy, or halogen; 2-pyrazinyl or 2-pyrazinyl substituted by lower alkyl, lower alkoxy, or halogen; 2- or 3-thienyl, or 2- or 3thienyl substituted by lower alkyl or halogen, 2- or 3-furanyl or 2- or 3-furanyl substituted by lower alkyl or halogen, or 2- or 5-thiazolyl or 2- or 5-thiazolyl substituted by lower alkyl or halogen, or a pharmaceutically acceptable acid salt thereof in unit dosage form.