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2-substituted ergoline derivatives, process for their preparation and to their application as a medicinal product

机译:2-取代的麦角灵衍生物,其制备方法及其作为药物的用途

摘要

Novel ergoline derivatives, substituted in the 2-position, of the formula IMAGE (I) wherein C8---C9 and C9---C10 each independently is a CC-single or a C=C-double bond, but not together a cumulated double bond, and the substituent in the 8-position is in the alpha - or beta -configuration where C8---C9 is a CC-single bond, R2 is a CN, SR, SOR, IMAGE wherein n is 2 or 3, IMAGE and -CH(OR)R wherein R has the meaning of H or C1-4-alkyl, the grouping COR' and CSR' wherein R'=OH, OC1-4-alkyl, benzyl, NH2 or NHR'', the grouping CH=CH-CO2R'' and CH2-CH2-CO2R' wherein R''=C1-4-alkyl, the grouping C 3BOND C-R''' and HC=CH-R''' wherein R'''=hydrogen, C1-4-alkyl, phenyl, CH2OH, CR''2OH, IMAGE CO2R'', CH2NR''2 or SiMe2R''; C1-3-alkyl, or C1-3-alkyl substituted by OH or phenyl; or IMAGE wherein R'' is C1-4 alkyl, R6 is C1-4-alkyl and R8 is methyl, NH-CO-NEt2 or NH-CS-NEt2, and the physiologically acceptable acid addition salt thereof, possess biological efficacy in the region of the central nervous system,, e.g., as neuroleptics and antidepressants.
机译:(I)的2位取代的新型麦角灵衍生物,其中C8--C9和C9--C10各自独立地为CC单键或C = C-双键,但不是一起是一个累积的双键,并且在8位上的取代基处于α-或β-构型,其中C8-C9是CC单键,R2是CN,SR,SOR,,其中n是2或3,和-CH(OR)R,其中R具有H或C1-4-烷基的含义,基团COR'和CSR'其中R'= OH,OC1-4-烷基,苄基, NH2或NHR'',基团CH = CH-CO2R''和CH2-CH2-CO2R',其中R''= C1-4烷基,基团C 3BOND C-R'''和HC = CH-R' '',其中R'''=氢,C1-4-烷基,苯基,CH2OH,CR''2OH, CO2R'',CH2NR''2或SiMe2R''; C1-3-烷基,或被OH或苯基取代的C1-3-烷基;或,其中R”是C1-4烷基,R6是C1-4烷基并且R8是甲基,NH-CO-NEt2或NH-CS-NEt2,及其生理学上可接受的酸加成盐,具有生物学功效在中枢神经系统区域中,例如作为抗精神病药和抗抑郁药。

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