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Alpha-adrenergic receptor, dopamine, histamine, imidazoline and serotonin receptor ligands and uses thereof

机译:α-肾上腺素能受体,多巴胺,组胺,咪唑啉和5-羟色胺受体配体及其用途

摘要

The invention relates to novel ligands the broad spectrum of biological activity of which includes simultaneously ±-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, among them serotonin 5-HT 7 receptors, which are compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers, pharmaceutically acceptable salts and/or hydrates, wherein: R1 is a substituent of amino group, selected from hydrogen, optionally substituted C 1 -C 4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C 1 -C 4 alkyl, CF 3 , CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulfonyl; Ar is optionally substituted aryl not necessarily annalated with heterocyclyl, or optionally substituted aromatic heterocyclyl; W is optionally substituted (CH 2 ) m group, optionally substituted CH=CH group, optionally substituted CH 2 -CH=CH group, C‰¡C group, SO 2 group; n = 1, 2; m = 1, 2, 3; solid line accompanied by dotted line, i.e. ( --- ) may represent single or double bond. The invention also relates to active ingredients, pharmaceutical compositions comprising the said ligands as active ingredients; to novel medicaments useful for treatment of diseases and conditions of central nervous system (CNS) of humans and warm-blooded animals.
机译:本发明涉及具有广泛生物学活性的新型配体,其同时包括±肾上腺素受体,多巴胺受体,组胺受体,咪唑啉受体和5-羟色胺受体,其中包括5-羟色胺5-HT 7受体,它们是通式1中的通式1的化合物。游离碱,几何异构体,外消旋混合物或单个旋光异构体,可药用盐和/或水合物的形式,其中:R1为氨基的取代基,选自氢,任选取代的C 1 -C 4烷基,酰基,杂环基,烷氧羰基,取代的磺酰基; R2是环状系统的取代基,其选自氢,卤素,任选取代的C 1 -C 4烷基,CF 3,CN,烷氧基,烷氧基羰基,羧基,杂环基或取代的磺酰基; Ar为任选取代的芳基,其不必与杂环基或任何任选取代的芳族杂环基环化; W为任选取代的(CH 2)m基,任选取代的CH = CH基,任选取代的CH 2 -CH = CH基,C‰C基,SO 2基; n = 1,2; m = 1,2,3;带有虚线的实线,即(-)可能代表单键或双键。本发明还涉及活性成分,包含所述配体作为活性成分的药物组合物;用于治疗人类和温血动物的中枢神经系统(CNS)疾病和状况的新型药物。

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