首页> 外国专利> PYRIMIDONVERBINDUNGEN, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE MITTEL.

PYRIMIDONVERBINDUNGEN, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE MITTEL.

机译:嘧啶酮化合物,其制备过程和包含这些化合物的药物产品。

摘要

Histamine H2-antagonists of the formula: IMAGE wherein m is an integer of from zero to 2, inclusive; n is an integer of from 2 to 5 inclusive; Z is sulfur, oxygen or methylene; R1 is NO2 or NR2R3; R2 and R3 each are independently hydrogen or (lower)alkyl, or, when R2 is hydrogen, R3 also may be formyl, carboalkoxy, alkanoyl or benzoyl; A is phenyl, furyl, thienyl, pyridyl, thiazolyl, imidazolyl, oxazolyl, oxadiazolyl, thiadiazolyl, triazolyl, isoxazolyl, isothiazolyl, pyrimidinyl, pyrazolyl, pyridazinyl or pyrazinyl; provided that A contains one or two substituents, the first substituent being selected from IMAGE and the second substituent being selected from (lower)alkyl, hydroxy, trifluoromethyl, halogen, amino, hydroxymethyl and (lower)alkoxy; q is an integer of from 0 to 6, inclusive; R4 is a hydrogen atom, a (lower)alkyl group optionally substituted by one or more halogen atoms, provided that there is no halogen atom on the carbon atom attached to the nitrogen atom, or a cyclo(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, (lower)alkanoyl or benzoyl group; R6 and R7 each are independently hydrogen, (lower)alkyl, (lower)alkenyl, (lower)alkynyl, phenyl(lower)alkyl or (lower)alkoxy(lower)alkyl in which the (lower)alkoxy moiety is at least two carbon atoms removed from the nitrogen atom, or R6 and R7, taken together with the nitrogen atom to which they are attached, may be pyrrolidino, methylpyrrolidino, dimethylpyrrolidino, morpholino, thiomorpholino, piperidino, methylpiperidino, dimethylpiperidino, hydroxypiperidino, N-methylpiperazino, homopiperidino, heptamethyleneimino, octamethyleneimino or 3-azabicyclo[3.2.2]non-3-yl; or a nontoxic pharmaceutically acceptable acid addition salt thereof.
机译:下式的组胺H 2拮抗剂:[IMAGE]其中m是0至2的整数,包括0和2。 n是2至5的整数,包括2和5。 Z为硫,氧或亚甲基; R1是NO2或NR2R3; R 2和R 3各自独立地是氢或(低级)烷基,或者,当R 2是氢时,R 3也可以是甲酰基,碳烷氧基,烷酰基或苯甲酰基; A为苯基,呋喃基,噻吩基,吡啶基,噻唑基,咪唑基,恶唑基,恶二唑基,噻二唑基,三唑基,异恶唑基,异噻唑基,嘧啶基,吡唑基,哒嗪基或吡嗪基;前提是A包含一个或两个取代基,第一取代基选自,第二取代基选自(低级)烷基,羟基,三氟甲基,卤素,氨基,羟甲基和(低级)烷氧基; q是0到6之间的整数(含0和6); R 4是氢原子,任选地被一个或多个卤素原子取代的(低级)烷基,只要在与氮原子连接的碳原子上不存在卤素原子,或环(低级)烷基,环(低级)烷基(低级)烷基,(低级)烷酰基或苯甲酰基; R 6和R 7各自独立地为氢,(低级)烷基,(低级)烯基,(低级)炔基,苯基(低级)烷基或(低级)烷氧基(低级)烷基,其中(低级)烷氧基部分为至少两个碳原子。从氮原子或R6和R7与其连接的氮原子一起除去的原子可以是吡咯烷基,甲基吡咯烷基,二甲基吡咯烷基,吗啉代基,硫代吗啉代基,哌啶子基,甲基哌啶子基,二甲基哌啶子基,羟基哌啶子基,N-甲基哌嗪子基,高哌啶子基,七亚甲基亚氨基,八亚甲基亚氨基或3-氮杂双环[3.2.2]非-3-基;或其无毒的药学上可接受的酸加成盐。

著录项

  • 公开/公告号CH665840A5

    专利类型

  • 公开/公告日1988-06-15

    原文格式PDF

  • 申请/专利权人 BRISTOL-MYERS COMPANY;

    申请/专利号CH19840004510

  • 发明设计人 ALGIERI ALDO A.;

    申请日1984-09-20

  • 分类号C07D239/46;C07D403/00;C07D405/00;A61K31/505;

  • 国家 CH

  • 入库时间 2022-08-22 06:53:05

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