[DE] GESÄTTIGTE UND UNGESÄTTIGTE HETEROARYLCYCLOALKYMETHYL-AMINE ALS ANTIDEPRESSIVA [EN] SATURATED AND UNSATURATED HETEROARYLCYCLOALKYLMETHYL AMINES AS ANTI-DEPRESSANTS [FR] HETEROARYLCYCLOALKYMETHYL AMINES SATUREES ET INSATUREES EN TANT QU'ANTIDEPRESSEURS
Synthesis and stereochemistry of tetrahydro-4-aryl-3-[(dimethylamino)methyl]-2<i>H</i>-pyranols as potential analgesics
作者:Erno Mohacsi、Jay P. O'Brien、John F. Blount、Jerry Sepinwall
DOI:10.1002/jhet.5570270618
日期:1990.9
Diastereomeric cis- and trans-tetrahydro-4-aryl-3-[(dimethylamino)methyl]-2H-pyranols derived from 3-[(dimethylamino)methyl]tetrahydro-4H-pyran-4-one (5), have been prepared and their configurations were established on the basis of ir data. The biologically more potent trans isomer 3 was resolved into its optical antipodes and the absolute stereochemistry of one of the enantiomers 14, was determined by
ZNS-wirksame Phenylpyrane: 3-Dimethylaminomethyl-4-(3-methoxyphenyl)-tetrahydro-4-pyranol und -4-thiopyranol
作者:Fritz Eiden、Michael Schmidt
DOI:10.1002/ardp.198700016
日期:1987.11
Die aus dem Tetrahydropyranon 2 bzw. ‐thiopyranon 3 durch Reaktion mit dem Iminiumchlorid 4 und m‐Methoxyphenylmagnesiumbromid darstellbaren O‐ und S‐Analogen des Tramadols waren im Tierversuch deutlich analgetisch wirksam, und zwar das Oxanaloge 7 doppelt so stark wie das Thiaanaloge 8.
曲马多的 O 和 S 类似物可以由四氢吡喃酮 2 或 -噻喃酮 3 通过与亚胺氯化物 4 和间甲氧基苯基溴化镁反应制备,在动物实验中具有明显的镇痛作用,即 ox 类似物 7 的强度是硫杂类似物 8 的两倍。
Saturated and unsaturated heteroarylcycloalkylmethyl amines as anti-depressants
申请人:Bloms-Funke Petra
公开号:US20060025456A1
公开(公告)日:2006-02-02
Saturated and unsaturated heteroarylcycloalkylmethyl-amine compounds corresponding to formula I,
processes for their preparation, pharmaceutical formulations comprising these compounds and the use of saturated and unsaturated heteroarylcycloalkylmethyl-amines for the preparation of pharmaceutical formulations. pharmaceutical formulations and related methods of treatment or prophylaxis of certain condition, especially depression and/or pain, are also disclosed.
The present invention directs to provide a novel compound for treating and/or preventing pain, having excellent skin permeation and reduced skin irritation. The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof (R1: a methyl group or other like group, R2: a fluorine atom or other like group, R3: a methyl group or other like group, R4: a methyl group or other like group, R5: a methyl group or other like group)