| 摘要 |
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. |
| 主权项 |
1. A compound of formula 1,or a tautomer, racemate, optical isomer, or pharmaceutically acceptable salt thereof, wherein:
L is —CH2CH2CH2CH2— or cis- or trans-CH2CH═CHCH2—; R1, R2, and R3 each are independently H, halogen, C1-C6 alkyl, substituted C1-C6 alkyl, C1-C6 alkenyl, substituted C1-C6 alkenyl, C1-C6 alkyloxy, C1-C6 alkylamino, di-(C1-C6 alkyl)amino, C1-10 hydrocarbonylcarbonyloxy, C1-10 hydrocarbonylamido, C1-10 hydrocarbonyloxycarbonyl, carbamoyl, or C1-10 hydrocarbonylcarbamoyl; wherein the substituent of each group having a substituent is independently selected from halogen, hydroxyl, cyano, nitro, C1-6 alkyl, C1-6 alkyloxy, C1-6 alkylthio, mono-, di- or tri-halogenated C1-6 alkyl, amino, C1-6 alkylamino, C1-10 hydroxycarbonylcarbonyloxy, or C1-10 hydrocarbonylamido; X is O or S; Y and Z are each independently CH or N; and the carbonyl may be at the 4-, 5-, 6-, or 7-position of the benzoxazolin-2-one or benzthiazolin-2-one ring. |
