Substituted succinimides, compositions and method of use

Claim 2

A succinimide derivative of the formula: ##STR20## wherein A is an oxygen atom, a methylene group, or an ethylene group and a full line accompanying a broken line is a single bond or a double bond, R is a phenyl group, optionally substituted with halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy or trifluoromethyl, a 2-pyridyl group or a 2-pyrimidinyl group and n is an integer of 3 or 4, or a pharmaceutically acceptable acid addition salt thereof.

Claim 3

The succinimide derivative as recited in claim 1, which is a compound of the formula: ##STR21## wherein A 1 is a methylene group or an ethylene group, and the full line accompanying a broken line is as defined in claim 1.

Claim 4

The succinimide derivative as recited in claim 1, which is N-[4-{4-(2-pyrimidinyl)-1-piperazinyl}butyl]bicyclo[2.2.1]-heptane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 5

The succinimide derivative as recited in claim 1, which is N-[3-{4-(2-pyrimidinyl-1-piperazinyl}propyl]bicyclo[2.2.1]heptane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 6

The succinimide derivative as recited in claim 1, which is N-[3-{4-(2-pyridyl)-1-piperazinyl}propyl]bicyclo-[2.2.1]heptane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 7

The succinimide derivative as recited in claim 1, which is N-[3-{4-(2-phenylpiperazinyl}propyl]bicyclo[2.2.1]heptane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 8

The succinimide derivative as recited in claim 1, which is N-[3-{4-(2-chlorophenyl)-1-piperazinyl}propyl]bicyclo[2.2.1]heptane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 9

The succinimide derivative as recited in claim 1, which is N-[4-{4-(2-pyrimidinyl)-1-piperazinyl}butyl]bicyclo[2.2.1]oct-4-ene-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 10

The succinimide derivative as recited in claim 1, which is N-[4-{4-(2-pyrimidinyl)-1-piperazinyl}butyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 11

The succinimide derivative as recited in claim 1, which is N-[4-{4-(2-chlorophenyl)-1-piperazinyl}butyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 12

The succinimide derivative as recited in claim 1, which is N-[3-{4-(2-pyrimidinyl)-1-piperazinyl}propyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 13

The succinimide derivative as recited in claim 1, which is N-[3-{4-(2-pyridyl)-1-piperazinyl}propyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 14

The succinimide derivative as recited in claim 1, which is N-[3-{4-(phenylpiperazinyl)}propyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide or a pharmaceutically acceptable acid addition salt thereof.

Claim 15

A pharmaceutical composition which comprises as an active ingredient a pharmaceutically effective amount of at least one of the compounds claimed in claim 1, and at least one pharmaceutically acceptable inert carrier or diluent.

Claim 16

The composition as recited in claim 14, wherein the active ingredient is at least one compound selected from the group consisting of: N-[4-{4-(2-pyrimidinyl)-1-piperazinyl}butyl]bicyclo[2.2.1]-heptane-2-exo-2-endo-methylenedicarboximide, N-[3-{4-(2-pyrimidinyl-1-piperazinyl}propyl]bicyclo[2.2.1]heptane-2-exo-2-endo-methylenedicarboximide, N-[3-{4-(2-pyridyl)-1-piperazinyl}propyl]bicyclo[2.2.1]heptane-2-exo-2-endo-methylenedicarboximide, N-[3-{4-(2-phenylpiperazinyl}propyl]bicyclo[2.2.1]heptane-2-exo-2-endo-methylenedicarboximide, N-[3-{4-(2-chlorophenyl)-1-piperazinyl}propyl]bicyclo[2.2.1]heptane-2-exo-2-endo-methylenedicarboximide, N-[4-{4-(2-pyrimidinyl)-1-piperazinyl}butyl]bicyclo[2.2.1]oct-5-ene-2-exo-2-endo-methylenedicarboximide, N-[4-{4-(2-pyrimidinyl)-1-piperazinyl}butyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide, N-[4-{4-(2-chlorophenyl)-1-piperazinyl}butyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide, N-[3-{4-(2-pyrimidinyl)-1-piperazinyl}-propyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide, N-[3-{4-(2-pyridyl)-1-piperazinyl}propyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide or N-[3-{4-(phenylpiperazinyl}propyl]bicyclo[2.2.2]octane-2-exo-2-endo-methylenedicarboximide or any pharmaceutically acceptable acid addition salt thereof.

Claim 17

A method or reducing anxiety, comprising: administering an effective anxiety reducing amount of the composition of claim 14 to a subject.

Claim 18

The composition as recited in claim 14, which is in the form of a tablet, capsule, syrup or suspension.

Claim 19

A method for reducing anxiety which comprises orally administering an effective anxiety reducing amount of the composition of claim 17 to a subject.

Claim 20

The composition as recited in claim 14, which is in the form of a solution, emulsion or suspension.

Claim 21

A method for reducing anxiety which comprises parenterally administering an effective anxiety reducing amount of the composition of claim 19 to a subject.

Claim 22

The composition as recited in claim 14, which is in the form of a suppository.

Claim 23

The method as recited in claim 16, wherein 1 to 300 mg of the active ingredient are administered daily in single doses or divided doses.

Claim 24

The method as recited in claim 22, wherein 5 to 100 mg of the active ingredient are administered daily in single doses or divided doses.