1-phenyl-4-(1-[2-aryl]cyclopropyl)methylpiperazines: dopamine receptor ligands
AssigneeNeurogen Corporation
InventorsXiaoyan Zhang, Jennifer Tran, He Zhao, Andrew Thurkauf
Life of this patent
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Abstract
Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: R1, R2, R3 R4 and R5, R6, R7, and R8 represent organic and/or inorganic substituents as defined herein, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
Claims41
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and (a) a compound of the formula:
- or (b) a pharmaceutically acceptable addition salt thereof wherein:
- R1 and R2 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, perfluoro(C1-C6)alkyl or perfluoro(C1-C6)alkoxy;
- R3 and R4 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, perfluoro(C1-C6)alkyl or perfluoro(C1-C6)alkoxy;
- and
- R5, R6, R7, and R8 are the same or different and represent hydrogen or C1-C3 alkyl.
A compound of the formula:
- or pharmaceutically acceptable addition salts thereof wherein:
- R1 and R2 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, perfluoro(C1-C6)alkyl or perfluoro(C1-C6)alkoxy;
- R3 and R4 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, perfluoro(C1-C6)alkyl or perfluoro(C1-C6)alkoxy;
- and
- R5, R6, R7, and R8 are the same or different and represent hydrogen or C1-C3 alkyl;
- provided that neither of R1 and R2 is t-butyl and at least one of R3 and R4 is halogen.
A compound of the formula:
- or pharmaceutically acceptable addition salts thereof wherein:
- R1 is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, perfluoro(C1-C6)alkyl or perfluoro(C1-C6) alkoxy;
- R2 represents C1-C4 alkylthio, perfluoro (C1-C6) alkyl, or perfluoro(C1-C6)alkoxy;
- R3 and R4 are hydrogen, halogen, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, perfluoro(C1-C6)alkyl or perfluoro(C1-C6)alkoxy;
- and
- R5, R6, R7, and R8 are the same or different and represent hydrogen or C1-C3 alkyl.
Dependencies are inferred from the claim text.