首页> 外国专利> MYOCARDIUM PROTECTING PYRROLE DERIVATIVES WITH ANTI-ARYTHMIC AND ANTI-PLATELET AGGREGATION ACTIVITY, PROCESS FOR THEIR PREPARATION AND MEDICINES CONTAINING THEM

MYOCARDIUM PROTECTING PYRROLE DERIVATIVES WITH ANTI-ARYTHMIC AND ANTI-PLATELET AGGREGATION ACTIVITY, PROCESS FOR THEIR PREPARATION AND MEDICINES CONTAINING THEM

机译:具有抗关节炎和抗血小板凝集活性的保护心肌吡咯衍生物,其制备方法和含有它们的药物

摘要

1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Derivatives of pyrrole of formula see diagramm : EP0054593,P16,F5 in which - R1 represents an atom of hydrogen, an alkyl group having from 1 to 6 atoms of carbon, a phenyl radical or a pyridyl-2 radical, - R2 represents an atom of hydrogen or an alkyl radical having from 1 to 6 atoms of carbon ; - R3 and R4 , which are identical or different, each represent an alkyl radical having from 1 to 6 atoms of carbon, or a cycloalkyl radical, or the group see diagramm : EP0054593,P17,F1 designates the pyrrolidinyl, piperidinyl, dimethyl-2,6 piperidinyl, morpholinyl, piperazinyl radical and the radical of formula see diagramm : EP0054593,P17,F2 - n is equal to 2 or 3, as well as the salts of these derivatives with the mineral or organic acids. 1. Claims for the Contracting State AT : Process for the preparation of derivatives of pyrrole of formula see diagramm : EP0054593,P17,F3 in which - R1 represents an atom of hydrogen, - R2 represents an atom of hydrogen or an alkyl radical having from 1 to 6 atoms of carbon, - R3 and R4 , which are identical or different, each represent an alkyl radical having from 1 to 6 atoms of carbon, or a cycloalkyl radical, or the group see diagramm : EP0054593,P17,F4 designates the pyrrolidinyl, piperidinyl, dimethyl-2,6 piperidinyl, morpholinyl, piperazinyl radical and the radical of formula see diagramm : EP0054593,P17,F5 and - n is equal to 2 or 3, as well as the salts of these derivatives with the mineral or organic acids, characterized in that the different following steps are carried out : - a compound of formula see diagramm : EP0054593,P17,F6 is used as starting product, - a saponification of the product in an alkaline medium, then a heating in an acid medium are carried out, to yield the butyric derivative of formula see diagramm : EP0054593,P18,F1 which is esterified by known processes into corresponding methyl ester, - the ester thus obtained is converted into amide by action of ammonia, - and said amide is heated with a product selected from a gamma-diketone of formula see diagramm : EP0054593,P18,F2 and dimethoxy-2,5 tetrahydrofuran, so as to form the pyrrolic cycle of the products of formula (I).
机译:1.对缔约国的索赔:BE,CH,DE,FR,GB,IT,LI,LU,NL,SE式的吡咯的衍生物参见示意图:EP0054593,P16,F5,其中-R1代表氢原子,具有1至6个碳原子的烷基,苯基或吡啶基-2基,-R 2表示氢原子或具有1至6个碳原子的烷基; -R 3和R 4相同或不同,各自代表具有1至6个碳原子的烷基或环烷基,或该基团见图:EP0054593,P17,F1表示吡咯烷基,哌啶基,二甲基-2 ,6哌啶基,吗啉基,哌嗪基基团和式的基团见图:EP0054593,P17,F2-n等于2或3,以及这些衍生物与无机或有机酸的盐。 1.缔约国的权利要求:制备式为吡咯的衍生物的方法,参见示意图:EP0054593,P17,F3其中-R1代表氢原子,-R2代表氢原子或具有1至6个相同或不同的碳原子,R 3和R 4,分别表示具有1至6个碳原子的烷基,或环烷基,或参见图的基团:EP0054593,P17,F4表示吡咯烷基,哌啶基,-2,6-二甲基哌啶基,吗啉基,哌嗪基基团和式的基团见图:EP0054593,P17,F5和-n等于2或3,以及这些衍生物与矿物或有机酸,其特征在于进行以下不同的步骤:-分子式参见示意图:EP0054593,P17,F6被用作起始产物,-产物在碱性介质中皂化,然后在酸中加热进行中,以yi产生下式的丁酸衍生物,参见图:EP0054593,P18,F1,其通过已知方法酯化为相应的甲酯,-如此获得的酯通过氨的作用转化为酰胺,-并将所述酰胺与选自以下的产物一起加热式的γ-二酮见图:EP0054593,P18,F2和二甲氧基-2,5-四氢呋喃,以形成式(I)产物的吡咯环。

著录项

  • 公开/公告号DE3070296D1

    专利类型

  • 公开/公告日1985-04-18

    原文格式PDF

  • 申请/专利权人 SANOFI SOCIETE ANONYME;

    申请/专利号DE19803070296T

  • 申请日1980-12-18

  • 分类号C07D207/325;C07D401/06;C07D403/06;A61K31/40;C07D487/04;

  • 国家 DE

  • 入库时间 2022-08-22 07:58:14

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