| abstract |
Spiro-((4-amino-cyclohexane)-1,1'-1',3',4',9'-tetrahydropyrano-(3,4-b)-indole) derivatives (I) are new. Spiro-cyclic cyclohexylamine derivatives of formula (I), optionally in the form of racemates, pure stereoisomers (especially enantiomers or diastereomers) or their mixtures in all proportions, including free bases, free acids, salts (specifically acid or base addition salt) or solvates (specifically hydrates), are new. [Image] R 1, R 2 : H, optionally unsaturated, optionally mono- or polysubstituted 1-4C alkyl or CHO; R 3 : -(CH 2) n-Aryl; n : 0-2; R 4 : H, optionally unsaturated, optionally mono- or polysubstituted 1-3C alkyl or -CO-(CH 2) m-H; m : 0-2; R 5 - R 8 : H; 1-5C alkyl or 1-3C alkoxy (both optionally unsaturated and optionally mono- or polysubstituted); or halo, OH, SH, SMe, OMe, NH 2, COOH, COOMe, NHMe, NMe 2 or NO 2. ACTIVITY : Analgesic; Tranquilizer; Antidepressant; Anticonvulsant; Neuroprotective; Nootropic; Antiaddictive; Antialcoholic; Vasotropic; Cardiant; Hypotensive; Hypertensive; Auditory; Antipruritic; Antimigraine; Laxative; Anorectic; Antidiarrheic; Immunomodulator; Uropathic; Relaxant; Anesthetic; Diuretic. The hydrochloride of the non-polar diastereomer of 1,1-(3-dimethylamino-3-phenyl-pentamethylene)-1,3,4,9-tetrahydropyrano-(3,4-b)-indole) (Ia) had analgesic ED 5 0 3.5 MicroM i.v. in the mouse tail-flick test. MECHANISM OF ACTION : Nociceptin/ORL1 receptor (opioid receptor like-receptor 1) system modulator; ORL1 receptor ligand. |