Isoxazolylalkylpiperazine 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, Kyung Ho Kang, Mi Young Cha, Jae Yang Kong, Dae Young Jeong, Hee-Yoon Lee
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Abstract
The present invention relates to isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or 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.
Claims8
A method of treating schizophrenia comprising administering to a patient in need thereof a composition comprising an effective amount of at least one isoxazolylalkylpiperazine derivative represented by the following formula (1), in racemic form or as individual optical isomers or a pharmaceutically acceptable salt thereof,
- wherein R1 represents at least one substituent selected from the group consisting of an aryl group, a phenylmethyl group, a diphenylmethyl group and a 2-keto-1-benzimidazolinylgroup, wherein the substituent may have at least one further substituent selected from the group consisting of C1-C6 alkyl group, C1-C6 alkoxy group and a fluorine atom, a chlorine atom and a trifluoromethyl group;
- R2 represents at least one substituent selected from the group consisting of an aryl group, a phenylvinyl group and a thiophene group, wherein the substituent may have at least one further substituent selected from the group consisting of a fluorine atom, a chlorine 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.