| abstract |
Compounds of benzolactam and cyclic thioamide, substituted, including their pharmaceutically acceptable salts, which have a special value in view of their ability to antagonize the action of substance P (pharmaceutically active neuropeptide that is synthesized in mammals and that has a characteristic amino acid sequence ). Compounds of the general formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is methylene, ethylene, propylene, vinylene, CH2-O, O-CH2, CH2-S or S-CH2; R1, R2 and R3 are independently hydrogen, alkyl, alkoxy-alkyl or halo-alkyl, provided that when W is methylene, neither R2 nor R3 are hydrogen; or one of R2 or R3 can be hydroxy; X is halo, alkoxy, alkyl, halo-alkoxy, or alkenyl; Y is NH or O; Q is oxygen or sulfur and has a double bond with the carbon to which it is attached, or Q is CH3 and has a single bond with the carbon to which it is attached; T is (2S, 3S) -2-diphenylmethylquinuclidin-3-yl, (2S, 3S) -2-diphenylmethyl-1-azanorbornan-3-yl; or (2S, 3S) -2-phenylpiperidin-3-yl, the phenyl group of the latter being optionally substituted with one or more substituents. For example: (2S, 3S) -2-diphenylmethyl-3- (6-methoxy-1,3,3-trimethyloxyindole-5-yl) -methylamino-1-azabicyclo (2.2.2) octane monomesylate. Methods of treating various CNS disorders and other disorders using said compounds and pharmaceutical compositions thereof. |