BLOMS-FUNKE, PETRA, DR.,ENGLBERGER, WERNER, DR.,HENNIES, HAGEN-HEINRICH, DR.
申请号：
EP08008351.2
公开号：
EP1970060B1
申请日:
2004.11.26
申请国别(地区):
EP
年份:
2012
代理人:
摘要：
The use of eleven specific C-(2-phenyl-cyclohexyl)-methylamine compounds (I) (all preferably in 1R,2R-enantiomer form), e.g. 3-(2-dimethylaminomethyl-cyclohexyl)-phenol (Ia) or (2-(3-methoxyphenyl)-cyclohexylmethyl)-dimethylamine, as medicaments for treating anxiety disorders or as adjuvant for standard antidepressants is new. The use of C-(2-phenyl-cyclohexyl)-methylamine compounds (I) is claimed in the production of medicaments for treating anxiety disorders and in the production of adjuvants for standard antidepressants. (I) is selected from 3-(2-dimethylaminomethyl-cyclohexyl)-phenol (Ia), (2-(3-methoxyphenyl)-cyclohexylmethyl)-dimethylamine, sulfuric acid mono-(3-(2-dimethylaminomethyl-cyclohexyl)-phenyl) ester, 3-(2-methylaminomethyl-cyclohexyl)-phenol, 3-(2-dimethylaminomethyl-cyclohexyl)-phenol N-oxide, 6-(3-(2-dimethylaminomethyl-cyclohexyl)-phenoxy)-3,4,5-trihydroxy-tetrahydropyran-2-carboxylic acid, 4-(2-dimethylaminomethyl-cyclohexyl)-catechol, 3-(2-aminomethyl-cyclohexyl)-phenol, C-(2-(3-methoxyphenyl)-cyclohexyl)-methylamine, (2-(3-methoxyphenyl)-cyclohexylmethyl)-methylamine and (2-(3-methoxyphenyl)-cyclohexylmethyl)-dimethylamine N-oxide. All compounds are optionally in the form of racemates or pure stereoisomers (specifically enantiomers or diastereomers) or their mixtures in all proportions； and/or in the form of salts or solvates (specifically hydrates). (I) are preferably in 1R,2R-enantiomer form. ACTIVITY : Tranquilizer； antidepressant； analgesic. In 'elevated plus maze' tests for anxiolytic activity in rats (see Psychopharmagcology, 2002, 163, 121-141), 3-(2-dimethylaminomethyl-cyclohexyl)-phenol (Ia) gave residence time of 118.2 seconds at a dose of 16 mg/kg, compared with 16.8 seconds in vehicle-only controls. MECHANISM OF ACTION : psi -Opiate agonist； serotonin reuptake inhibitor； noradrenaline reuptake inhibitor. (Ia) had K i values of 0.14 mu M, 0.05 mu M and 0.16 mu M in mu -opioid affinity, serotonin reuptake inhibiting and noradrenaline
