发明名称 1h-4(5)-substituted imidazole derivatives and their use in activating histamine H3 receptors
摘要 1h-4(5)-substituted imidazole derivatives of formula (I), with H3 histamine receptor agonist activity, wherein: A is (a); (b); or (c) and R1 is lower alkyl or lower alkoxy; R2, R3, R4, R5, R7 and R8 are each independently hydrogen or lower alkyl; R6 is lower alkyl or lower alkoxy and R5 and R6 can be joined to form a 4, 5, or 6 membered ring. The pharmaceutically acceptable salts, prodrugs, individual stereoisomers and tautomers of compounds of formula I above, as well as mixtures thereof, are also disclosed. Described is the use of compounds of formula (I) in the manufacture of a medicament for treating conditions in which activation of histamine H3 receptors may be of therapeutic importance such as allergy, inflammation, cardio or cerebrovascular disease (i.e. hyper or hypotension, ischemia, stroke, migraine), gastrointestinal disorders (acid secretion, motility) and CNS disorders involving psychiatric disorders (i.e., including anxiety, manic/depressive disorder, schizophrenia, obsessive-compulsive disorders, etc.) and sleep disorders (i.e., sleep apnea, insomnia, biological and circadian rhythms, hyper and hyposomnolence and related disorders) hypothalamic dysfunction (i.e., eating disorders such as anorexia/bulimia, thermoregulation, hormone release).
申请公布号 NZ311318(A) 申请公布日期 2000.08.25
申请号 NZ19960311318 申请日期 1996.06.06
申请人 GLIATECH, INC 发明人 PHILLIPS, JAMES G;KHAN, AMIN MOHAMMED;TEDFORD, CLARK E
分类号 C07D233/64;A61K31/415;A61K31/4164;A61K31/422;A61P3/04;A61P25/20;C07D233/54;C07D233/60;C07D413/04;(IPC1-7):A61K31/415 主分类号 C07D233/64
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