首页> 外国专利> STEROID COMPOUNDS (VARIANTS), PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT OF PATIENTS WITH NERVOUS DISORDERS (VARIANTS) AND METHOD OF ANESTHESIA INDUCTION IN ANIMAL

STEROID COMPOUNDS (VARIANTS), PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT OF PATIENTS WITH NERVOUS DISORDERS (VARIANTS) AND METHOD OF ANESTHESIA INDUCTION IN ANIMAL

机译:类固醇化合物(变体),药物成分,神经紊乱患者的治疗方法(变体)和动物麻醉诱导方法

摘要

FIELD: organic chemistry, steroids, pharmacy. SUBSTANCE: invention describes steroid compounds of the general formula (I) where: a) R4 means 3'-methyl-but-3'-ene-1'-inyl or cyclopro-pylethynyl; R5 means methyl; R6 means acetyl; dotted line means a single bond; b) R4 means trifluoromethyl-group; R5 means methyl; R6 means acetyl; dotted line means a single or a double bond and in the case when this bond is a single one, R6 is hydroxyacetyl and R5 is hydrogen atom then R4 can mean fluoromethyl-group; c) R4- means ethynyl; R5 means methyl; R6 means hydroxymethyl or hydroxyacetyl; dotted line means a single bond, or their physiologically acceptable 21-esters, 3,20-diesters or 3,21-diesters or where: a) R6 means hydroxyacetyl; R5 means hydrogen atom in the case when R4 is trifluoromethyl-group and compound is presented as sodium 21-hemisuccinate; b) R6 means hydroxyacetyl; R5 means methyl and R4 can mean the following values: hydrogen atom in the case when compound is presented as bis-hemisuccinate; ethynyl in the case of 21-hemisuccinate; trifluoromethyl-group in the case of sodium 21-hemifumarate, methyl-21-succinate, 21-propionate; and c) R4 means methyl; R5 means methyl; R6 means isopropylideneaminoethanol being dotted line means a single bond. Compounds of the formula (I) show ability to modulate excitability of GRC complex and therefore they can be used for treatment of patients with stresses, anxiety state, epileptic attack, mood disorders, premenstrual syndrome and post-delivery depression and for induction of anesthesia also. EFFECT: improved method of treatment and induction, valuable medicinal properties. 15 cl, 8 tbl, 31 ex
机译:领域:有机化学,类固醇,药学。物质:本发明描述了通式(I)的类固醇化合物。<图像文件=“ 00000002.GIF” he =“ 41” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 43” />其中:a)R < Sub> 4 是指3'-甲基-but-3'-ene-1'-inyl或环脯氨酸。 R 5 表示甲基; R 6 表示乙酰基;虚线表示单键; b)R 4 是指三氟甲基; R 5 表示甲基; R 6 表示乙酰基;虚线表示单键或双键,当该键为单键时,R 6 为羟乙酰基,R 5 为氢原子,则R 4 表示氟甲基; c)R 4 -是乙炔基; R 5 表示甲基; R 6 是指羟甲基或羟乙酰基;虚线是指单键或其生理学上可接受的21个酯,3,20个二酯或3,21个二酯,或其中:a)R 6 是指羟基乙酰基;当R 4 为三氟甲基且化合物以21-半琥珀酸钠存在时,R 5 是指氢原子。 b)R 6 表示羟乙酰基; R 5 表示甲基,R 4 表示以下值:当化合物以双半琥珀酸酯形式存在时的氢原子;乙炔基(21-半琥珀酸酯);在21-半富马酸钠的情况下为三氟甲基,而21-琥珀酸甲酯,21-丙酸为三氟甲基; c)R 4 表示甲基; R 5 表示甲基; R 6 是指异丙叉亚氨基乙醇,虚线是单键。式(I)的化合物显示出调节GRC复合物的兴奋性的能力,因此它们可以用于治疗患有压力,焦虑状态,癫痫发作,情绪障碍,经前综合症和分娩后抑郁的患者,还可以用于诱导麻醉。 。效果:改进的治疗和诱导方法,有价值的药物特性。 15 cl,8 tbl,31前

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