06-11-2014 дата публикации
Номер: US20140329831A1
Принадлежит:
The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction. 3. The compound of formula I according to or , or tautomers , racemates , optical isomers , pharmaceutically acceptable salts or solvates thereof , wherein L is —CHCHCHCH— , or cis- or trans —CHCH═CHCH—.4. The compound of formula I according to or , or tautomers , racemates , optical isomers , pharmaceutically acceptable salts or solvates thereof , wherein R , R , and Reach are independently H , F , Cl , Br , I , C-Calkyl , or C-Calkyloxy; preferably , wherein R , R , and Reach are independently H , F , Cl , methyl , ethyl , methyloxy , or ethyloxy.5. The compound of formula I according to or , or tautomers , racemates , optical isomers , pharmaceutically acceptable salts or solvates thereof , wherein X is O.6. The compound of formula I according to or , or tautomers , racemates , optical isomers , pharmaceutically acceptable salts or solvates thereof , wherein both Y and Z are C.76. The compound of formula I according to any one of - claims 1 , which is selected from:N-{4-[4-(5-chloro-2-methylphenyl)piperazinyl]butyl}-benzoxazolin-2-one-5-carboxamide;N-{4-[4-(5-chloro-2-methylphenyl)piperazinyl]butyl}-benzoxazolin-2-one-6-carboxamide;N-{4-[4-(2-methyloxyphenyl)piperazinyl]butyl}-benzoxazolin-2-one-5-carboxamide;N-{4-[4-(2-methyloxyphenyl)piperazinyl]butyl}-benzoxazolin-2-one-6-carboxamide;N-{4-[4-(5-chloro-2-methylphenyl)piperazinyl]-trans-2-buten-1 ...
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