首页> 外国专利> IMIDAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, NOVEL INTERMEDIATE PRODUCTS, THEIR APPLICATIONS AS PHARMACEUTICALS AND PHARMACEUTICAL COMPOSITIONS HOLDING SAME

IMIDAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, NOVEL INTERMEDIATE PRODUCTS, THEIR APPLICATIONS AS PHARMACEUTICALS AND PHARMACEUTICAL COMPOSITIONS HOLDING SAME

机译:咪唑衍生物,其制备过程,新型中间体产品,其在制药和制药组合物中的应用

摘要

ABSTRACT OF THE DISCLOSURE: The invention relates to the products of formula (I): (I) wherein: A is residue of a radical as boxyclique-or heterocyclic saturated or unsaturated, R represents alkyl, alkenyl or alkynyl; R1, R2, R3 and R4 are hydrogen; halogen; hydroxyl; cyano; nitro; sulfo; formyl; benzoyl; acyl; acyloxy; carboxy free, salified or esterified; mercapto; alkyl; alkenyl; alkynyl; alkoxy; alkylthio; aryl; arylalkyl; arylalkenyl; - (CH2) m-SO2-X-R14; or in which: either R6 and R7 or R8 and R9, identical or different, represent hydrogen, alkyl, alkenyl, aryl, arylalkyl, and - (CH2) m-SO2-X-R14 where m is 0 to 4, or X R4 is NH2, or X is NH, NH-CO-NH or NH-CO- or single bond and R14 is alkyl, alkenyl or aryl, or R6 and R7 or R8 and R9 together with nitrogen to which they are attached form a carbocyclic or heterocyclic radical, or R8 and R9, identical or different, represent acyl, alkyl or arylsulfonyl; R5 represents alkylene; -Y1 Y-B-Y2 wherein Y1 represents carbocyclic or heterocyclic aryl optionally substituted by R1, R2, R3 and R4, B is either single bond between Y1 and Y2, or -CO-, -NH-CO-, -CO-NH- or -O- (CH2) n- with n represent 0 to 3, Y2 is Y1, if B represents a single bond, hydrogen, cyano, carboxy free, salified or esterified, provided that: when A represents phenyl optionally substituted by halogen, alkyl, alkoxy, acyl, free carboxy or substituted phenyl by 5 fluorine atoms, R5 is -CH2-, and Y is -Y1-B-Y2 wherein Y1 represents unsubstituted phenyl and Y 2 is phenyl substituted ortho free carboxy optionally salified, tetrazolyl, trifluoromethyl-sulphonamide and optionally halogen, alkyl, nitro or methoxy, then B represents -CO-NH- or -O- (CH2) n- where n is 2 or 3, said products of formula (I) being in all the possible racemic, enantiomeric and diastereoisomers, and the addition salts with mineral and organic acids or with mineral and organic bases of said products of formula (I). The invention also relates to a method for manufacturing said products, their use for the preparation of medicaments, pharmaceutical compositions containing said products and intermediates for the preparation of said products.
机译:发明内容本发明涉及式(I)的产物:(I):其中:A是作为叔丁基或杂环饱和或不饱和基团的基团的残基,R代表烷基,烯基或炔基; R1,R2,R3和R4为氢;卤素;羟;氰基;硝基磺基甲酰基苯甲酰基;酰基酰氧基;不含羧基,成盐或酯化的;巯基烷基;烯基炔基烷氧基烷硫基芳基芳烷基;芳基烯基; -(CH2)m-SO2-X-R14;或其中:R6和R7或R8和R9相同或不同,表示氢,烷基,烯基,芳基,芳基烷基和-(CH2)m-SO2-X-R14其中m为0至4,或X R4是NH2,或X是NH,NH-CO-NH或NH-CO-或单键,R14是烷基,烯基或芳基,或R6和R7或R8和R9与它们连接的氮一起形成碳环或杂环基,或R 8和R 9相同或不同,表示酰基,烷基或芳基磺酰基; R5代表亚烷基; -Y1 YB-Y2,其中Y1表示可被R1,R2,R3和R4任选取代的碳环或杂环芳基,B是Y1和Y2之间的单键,或-CO-,-NH-CO-,-CO-NH-或-O-(CH2)n-,n表示0至3,如果B表示单键,则氢,氰基,无羧基,成盐或酯化,则Y2为Y1,条件是:当A表示可被卤素取代的苯基时,烷基,烷氧基,酰基,游离羧基或被5个氟原子取代的苯基,R5为-CH2-,Y为-Y1-B-Y2,其中Y1代表未取代的苯基,Y 2为苯基取代的邻位羧基,任选盐化,四唑基,三氟甲基-磺酰胺和任选的卤素,烷基,硝基或甲氧基,则B代表-CO-NH-或-O-(CH2)n-,其中n为2或3,式(I)的产物在所有可能的外消旋体中,对映异构体和非对映异构体,以及所述式(I)产物与矿物和有机酸或与矿物和有机碱的加成盐。本发明还涉及一种用于制造所述产品的方法,其在制备药物中的用途,包含所述产品的药物组合物以及用于制备所述产品的中间体。

著录项

  • 公开/公告号CA2044087A1

    专利类型

  • 公开/公告日1991-12-09

    原文格式PDF

  • 申请/专利权人 ROUSSEL-UCLAF;

    申请/专利号CA19912044087

  • 申请日1991-06-07

  • 分类号C07D235/02;C07D471/04;C07D487/04;C07D491/04;C07D495/04;C07D403/12;C07D333/36;A61K31/415;A61K31/44;A61K31/52;C07D233/66;

  • 国家 CA

  • 入库时间 2022-08-22 05:32:18

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