| 摘要 |
The present invention provides compounds having H3 histamine receptor antagonist activity of the general formula: <IMAGE> (1.0) where X is H, A is -CH2CH2-, -COCH2-, -CONH-, -CON(CH3)-, -CH=CH-, -C 3BOND C-, -CH2-NH-, -CH2-NCH3-, -CH(OH)CH2-, -NH-CH2-, -N(CH3) -CH2-, -NHSO2-, -CH2O-, -CH2S-, CH2SO2-, or -CH2S(O)-; R2 is a hydrogen or a methyl or ethyl group; R3 is a hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; and R1 is selected from the group consisting of (a) C3 to C8 cycloalkyl; (b) H; (c) phenyl or substituted phenyl; (d) alkyl; (e) heterocyclic; and (f) bicyclic alkyl; and when X is NH2, NHCH3, N(CH3)2, OH, OCH3, NHR4, OR4, SH, SR4, or SO2R4; A is -NHCO-, -N(CH3)-CO-, -NHCH2-, -N(CH3)-CH2-, -NHSO2-, -CH=CH-, -CH=CHF-, -COCH2-, -CH2CH2-, -CH(OH)CH2-, or -C 3BOND C-; R2 is a hydrogen or a methyl or ethyl group; R3 is a hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; R1 is selected from the group consisting of (a) C3 to C8 cycloalkyl; (b) H; (c) phenyl or substituted phenyl; (d) alkyl; (e) heterocyclic; and (f) bicyclic alkyl and R4 is designated to mean that X is contained within a ring such as octahydroindole. |
