4 - (piperidin-4-yl ylmethyl) benzamides, or their salts, esters or solvates and Pharmaceutical compositions containing Same, and Uses Thereof for preparing Drugs, and a Kit for use in the treatment of Cognitive or neurodegenerative disease

摘要

A 4 - (piperidin-4-yl methyl) benzamide has the Structural formula (1) or a Salt, Ester or pharmaceutically acceptable solvate, where Structural formula: R1 - R5 cycloalkyl - 8 C3, R5 cycloalkyl alkyl C1 - C3 - 8 - 6, R5 - aryl - aryl alkyl, R5 R5 C1 - 6 or - heteroaryl alkyl; R2 is H, C1 - 6 Cycloalkyl, R6 - C3 - 8 - 8 - cicloalquil R6 C1 C3 alkyl - 6, - heterocicloalquilo R6,R6 - bridged or cycloalkyl c6-10, R6 - heterocicloalquilo bridged; R3 is C1 - 6 - CH2OH alkyl or alkyl; R4 is H, or C1 - 6; R5 is 1 to 4 substituents selected from the group consisting of independently C1 - 6 h, alkyl, halogen, alkoxy - C1 - 6 CF3, - CN, - - - so2nhr4 conhr4 co2r4,,,- nhso2r4 and (OR) - NHC R4 and R6 is 1 to 4 substituents selected from the group consisting of independently C1 - 6 h, alkyl, halogen, alkoxy - C1 - 6, CF3, - NH2, - 6, phenyl alquilamino C1, C1 and C1 alcoxicarbonilo alquilendioxi - 2 - 6.The Compounds, salts, esters, or pharmaceutically acceptable solvates are Muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions comprising a therapeutically effective amount of the compounds, salts, esters, or pharmaceutically acceptable solvates in a pharmaceutically acceptable Carrier.The Compounds, salts, esters, or pharmaceutically acceptable solvates or compositions, optionally in combination with an inhibitor of acetylcholinesterase, are used for preparing drugs for the treatment of Cognitive diseases and Neurodegenerative Diseases.The drugs are administered in an effective amount of the compounds, esters, salts, solvates and pharmaceutically acceptable compositions or to a Mammal in need of such treatment.A Kit for treating a disease includes Cognitive or neurodegenerative disease in separate containers in a single package, Pharmaceutical compositions for use in combination, a compound in a container, Salt, Ester or pharmaceutically acceptable solvate, a pharmaceutically Carrier Acceptable and in a Second container,An inhibitor of acetylcholinesterase in a pharmaceutically acceptable Carrier, being the combined quantities in an effective amount.