derivados do ciclohexanol espirocíclicos, medicamento incluindo pelo menos um derivado do ciclohexano espirocíclico e uso de um derivado do ciclohexano espirocíclico

"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 medicamento...

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Hauptverfasser: Klaus Linz, Michael Jonathan Lipkin, Helmut Sonnenschein, Stefan Oberdörsch, Bernd Sundermann, Birgitta Henkel, Elmar Friderichs, Werner Gunter Englberger, Valerie Sarah Rose, Otto Aulenbacher, Claudia Hinze, Hans Schick, Babette Yvonne Kögel
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creator Klaus Linz
Michael Jonathan Lipkin
Helmut Sonnenschein
Stefan Oberdörsch
Bernd Sundermann
Birgitta Henkel
Elmar Friderichs
Werner Gunter Englberger
Valerie Sarah Rose
Otto Aulenbacher
Claudia Hinze
Hans Schick
Babette Yvonne Kögel
description "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.
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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. 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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. 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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.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title derivados do ciclohexanol espirocíclicos, medicamento incluindo pelo menos um derivado do ciclohexano espirocíclico e uso de um derivado do ciclohexano espirocíclico
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