| 摘要 |
Compounds of formula (1.0) have H3 histamine receptor antagonist activity and may be used to treat conditions such as allergy, inflammation, cardiovascular disease (i.e. hyper or hypotension), gastrointestinal disorders (acid secretion, motility) and CNS disorders involving attention or cognitive disorders, (i.e., Alzheimer's, Attention Deficit Disorder, age-related memory dysfunction, stroke, etc), psychiatric disorders (i.e., depression, schizophrenia, obsessive-compulsive disorders, tourette's syndrome, etc.), sleep disorders (i.e., narcolepsy, sleep apnea, insomnia, disturbed biological and circadian rhythms, hyper and hyposomnolence, and related sleep disorders), epilepsy or hypothalamic dysfunction (i.e., eating disorders such as obesity, anorexia/bulimia, thermoregulation, hormone release). In formula (1.0): 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) phenyl or substituted phenyl; (c) alkyl; (d) heterocyclic; (e) decahydronapthalene; and (f) octahydroindene; when X is H, A can be -CH2CH2-, -COCH2-, -CONH-, -CON(CH3)-, -CH=CH-, -CºC-, -CH2-NH-, -CH2-N(CH3)-, -CH(OH)CH2-, -NH-CH2-, -N(CH3)-CH2-, -NHSO2-, -CH2O-, -CH2S- or -NHCOO-; and when X is NH2, NH(CH3), N(CH3)2, OH, OCH3, CH3, SH or SCH3, A can be -NHCO-, -N(CH3)-CO-, -NHCH2-, -N(CH3)-CH2-, -CH=CH-, -COCH2-, -CH2CH2-, -CH(OH)CH2-, or -CºC-; and when R1 and X taken together denote a 5,6 or 6,6 saturated bicyclic ring structure, X can be NH, O or S.
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