首页> 外国专利> Piperazine derivatives and piperazinona substituted Heterocycles useful as Tachykinin Receptor Antagonists, Pharmaceutical composition that includes one of these Derivatives.Use of these compounds in the preparation of compositions and Process for the preparation of derivatives

Piperazine derivatives and piperazinona substituted Heterocycles useful as Tachykinin Receptor Antagonists, Pharmaceutical composition that includes one of these Derivatives.Use of these compounds in the preparation of compositions and Process for the preparation of derivatives

机译:用作速激肽受体拮抗剂的哌嗪衍生物和哌嗪酮取代的杂环化合物,包括这些衍生物之一的药物组合物。这些化合物在组合物的制备中的用途以及制备衍生物的方法

摘要

The derivative of the present invention conforms to formula (I),Where G is - ch2-o-c (o) -;AR1 is a kind of radical substance selected from phenyl, substituted phenyl, nafilo, substituted naftio, R1 is hydrogen, a kind of hot acrylonitrile, - (CH2) qar2 or CH 2C (o) ar2; q is an integer from 1 to 4, ar2 is nontoxic phenyl, substituted phenyl or isobutylene; R2 is hydrogen, C1-C4 tar or Cho; R3 refers to hydrogen or radical substance selected from phenyl, phenyl substitute, northwest non-n-butyl or its stereoisomer or pharmaceutically acceptable salt. An intermediate is also introduced for plasma repair of these derivatives, which conforms to the formula of (2), wherein R1, R3 and R2 are intermediates defined above, and R5 is selected from nitrogen,Preparation procedure for c1-c (or) or7 hydrogen (or) C1-C4 hydrocarbon groups and these derivatives between C1-C4 and R6. The derivatives of piperazina and piperazina are useful as symbionts of taquikininas receptors for the treatment of diseases and conditions controlled by taquikininas, including asthma, cough and bronchitis. These derivatives are included in pharmaceutical ingredients and have acceptable pharmaceutical ingredients.
机译:本发明的衍生物符合式(I),其中G为-ch 2 -oc(o)-; AR 1为选自苯基,取代苯基,萘酚,取代萘基的一种自由基物质,R 1为氢。热丙烯腈,-(CH2)qar2或CH 2C(o)ar2; q是1-4的整数,ar2是无毒的苯基,取代的苯基或异丁烯; R2是氢,C1-C4焦油或Cho; R 3表示氢或选自苯基,苯基取代基,西北非正丁基或其立体异构体或药学上可接受的盐的自由基物质。还引入了中间体,用于这些衍生物的血浆修复,该中间体符合式(2),其中R1,R3和R2是以上定义的中间体,R5选自氮,c1-c(或)或7的制备方法氢(或)C1-C4烃基以及C1-C4和R6之间的这些衍生物。 Piperazina和Piperazina的衍生物可用作Taquikininas受体的共生体,用于治疗由Taquikininas控制的疾病和病症,包括哮喘,咳嗽和支气管炎。这些衍生物包括在药物成分中并且具有可接受的药物成分。

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