| 摘要 |
The present invention provides compounds having H3 histamine receptor antagonist activity of the general formula: R2 is a hydrogen or a methyl or ethyl group; R3 is a hydrogen or a methyl or ethyl group; n is 1, 2, 2, 3, 4, 5, or 6; and R1 is selected from the group consisting of (a) C3 to C8 cycloalkyl; (b) phenyl or substituted phenyl; (c) alkyl; (d) heterocyclic; (e) decahydronapthalene; and (f) octahydroindene; with the provisos that when X is H, A can be -CH2CH2-,-COCH2-,-CONH-,-CON(CH3), CH=CH, -c=c-,-CH2-NH-, -CH2-N(CH3)-,-CH(OH)CH2-,-NH-CH2-, -N(CH3)-CH2-,-CH2O-,-CH2S-, and -NHCOO-; when X is NH2, NH(CH3), N(CH3)2, OH, OCH3, CH3, SH, and SCH3; A can be -NHCO-, -N(CH3)-CO-, -NHCH2-, -N(CH3)-CH2-, -CH=CH-; -COCH2, -CH2CH2-,-CH(OH)CH2, or -C=C-; and when R1 and X taken together denote a 5,6 or 6,6 saturated bicyclic ring structure X NH, O, or S and the pharmaceutically acceptable salts, and individual stereoisomers of compounds of structural formula (1.0) above. This invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of the above formula and a method of treating conditions in which antagonism of histamine H3 receptors may be of therapeutic importance.
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