Claims
- 1. A 4-(2-pyrimidinyl)-1-piperazinyl heterocyclic carbonyl derivative having the formula: ##STR12## wherein n is an integer of from 2 to 5; X is the radical ##STR13## R.sub.1 and R.sub.2 are each methyl or when taken together form a tetramethylene or pentamethylene ring; and the pharmaceutically acceptable acid addition salts thereof.
- 2. A compound according to claim 1 wherein X is the radical ##STR14##
- 3. A compound according to claim 1, which is 1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-tetrahydro-6,6-dimethylpyrimidine-2,4-dione and the pharmaceutically acceptable salts thereof.
- 4. A compound according to claim 1 wherein X is the radical ##STR15##
- 5. A compound according to claim 1, which is 2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butylimino]-tetrahydro-4,4-dimethyl-6H-1,3-oxazine-6-one and the pharmaceutically acceptable salts thereof.
- 6. A process for the preparation of a 4-(2-pyrimidinyl)-1-piperazinyl heterocyclic carbonyl derivative according to claim 1 which comprises reacting an alkyl ester of 3-[(N-alkyl)ureido]propionic acid having the formula ##STR16## wherein n, R.sub.1 and R.sub.2 are as described in claim 1, R is lower alkyl group and Y is an appropriate leaving group, reacting said propionic acid with 1-(2-pyrimidinyl)piperazine to form an alkyl ester of 3-[N-[.omega.-[4-(2-pyrimidinyl)]-1-piperazinyl]alkyl]ureido]propionic acid; cyclizing said alkyl ester of (2-pyrimidinyl)-1-piperazinyl]alkyl]ureido]propionic acid, and isolating the desired 4-(2-pyrimidinyl)-1-piperazinyl heterocyclic carbonyl derivative therefrom.
- 7. A method for relieving the symptoms of anxiety in a patient in need thereof, which comprises the administration to said patient of an anxiolytic effective amount of a compound of claim 1.
- 8. An anxiolytic composition comprising an anxiolytic effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier or diluent.
CROSS REFERENCE TO RELATED APPLICATION
This is a continuation of application Ser. No. 836,277, filed Mar. 5, 1986, now abandoned.
Foreign Referenced Citations (1)
Number |
Date |
Country |
170213 |
Feb 1986 |
EPX |
Non-Patent Literature Citations (1)
Entry |
Peroutka, Biol. Psychiatry, [1985]; 20: 971-979. |
Continuations (1)
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Number |
Date |
Country |
Parent |
836277 |
Mar 1986 |
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