4,5,-dihydroisoxazolylakylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptor, and preparation thereof
AssigneesKorea Institute of Science and Technology, Korea Research Institute of Chemical Technology, Korea Advanced Institute of Science and Technology
InventorsHun Yeong Koh, Kyung Il Choi, Yong Seo Cho, Ae Nim Pae, Jae Yang Kong, Dae Young Jeong, Sun Ho Jung, Ji Young Jung, Hee-Yoon Lee
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Abstract
The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, wherein R1, R2, X and n are the same as defined in the specification.
Claims5
A method of treating schizophrenia which comprises administering to a patient an effective amount of at least one 4,5-dihydroisoxazolylalkylpiperazine derivative represented by the following formula (1), or a pharmaceutically acceptable addition salt thereof, in racemic form or as individual optical isomers:
- wherein R1 represents at least one substituent of the group consisting of an aryl group, a phenylmethyl group, a diphenylmethyl group, and pyrimidinyl group, and wherein the substituent may have one or more further substituents selected from the group consisting of C1-C6 alkyl group, C1-C6 alkoxy group, a fluorine atom and a chlorine atom;
- R2 represents at least one substituent selected from the group consisting of an aryl group, a styryl group, and a thiophene group, and wherein the substituent may have at least one further substituent, selected from the group consisting of a fluorine atom, a nitro group, a C1-C6 alkyl group, a C1-C6 alkoxy group and a phenoxy group;
- X represents CH or a nitrogen atom;
- and
- n represents 3 or 4.
Dependencies are inferred from the claim text.