| 摘要 |
This invention relates to novel compounds which bind to central cholinergic muscarinic M1 receptors and may be useful for treatment of diseases attributed to cholinergic insufficiency such as presenile dementia, senile dementia of the Alzheimer's type, Parkinson's disease, Down's syndrome, and dementia pugilistica. The compounds useful in this invention have the formula <IMAGE> or a 6, 7, 8, 9 tetrahydro analog thereof, where R1 is selected from H, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, cyano, halo, nitro, and -NR4R5, where R4 and R5 are independently selected from H, C1-C6 alkyl and phenyl, optionally substituted with halo, cyano, hydroxy, nitro, amino, mono or di C1-C6 alkylamino, phenylamino, C1-C6 alkyl or C1-C6 alkoxy; R2 is CF3-, CF3CH2-, or -CH2-X-R6 where X is oxygen or NH and R6 is C1-C6 alkyl, phenyl-(CH2)n- or -(CH2)n-NR7R8 where R7 and R8 are selected from H or C1-C6 alkyl, or R2 is equal to R3, and when the compound is hydrogenated at positions 6, 7, 8, and 9, R2 can also be C1-C6 alkyl, and R3 is -(CH2)m-NR9R10 where R9 and R10 are independently H, C1-C6 alkyl, phenyl, phenyl-(CH2)n-, or NR9R10 forms a mono or bicyclic azacycloalkane group having from 5 to 10 members, one of which may be a heteroatom selected from O, S, or NR11 where R11 is C1-C6 alkyl, phenyl, pyrimidinyl, pyridinyl, or pyrazinyl or R9 is H and R10 is a mono or bicyclic azacycloalkyl group having from 5 to 10 members where the nitrogen is either a bridgehead nitrogen or the nitrogen may be optionally substituted with C1-C6 alkyl, phenyl-(CH2)n- or C3-C6 cycloalkyl; n is 1-6 and m is 2-5; or a pharmaceutically acceptable salt thereof.
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