derivados de ciclohexanol espirocíclicos

derivados do ciclohexanol espirocíclicos. a invenção está relacionada com os derivados do ciclohexanol espirocíclicos, um método para a produção dos mesmos, medicamentos que incluem esses compostos e a utilização dos derivados do ciclohexanol espirocíclicos para a produção de medicamentos. Spiro-((4...

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Hauptverfasser: Klaus Linz, Michael Jonathan Lipkin, Stefan Oberbörsch, Helmut Sonnenschein, Bernd Sundermann, Birgitta Henkel, Elmar Friderichs, Valerie Sarah Rose, Otto Aulenbacher, Claudia Hinze, Hans Schick, Werner Englberger, Babette Yvonne Kögel
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Sprache:por
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Zusammenfassung:derivados do ciclohexanol espirocíclicos. a invenção está relacionada com os derivados do ciclohexanol espirocíclicos, um método para a produção dos mesmos, medicamentos que incluem esses compostos e a utilização dos derivados do ciclohexanol espirocíclicos para a produção de medicamentos. 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.