首页> 外国专利> Biphenyl Derivatives, a process for their preparation, their use for preparing a Drug, medicinal products based estoscompuestos,Pharmaceutical compositions containing them and Process for preparing such Pharmaceutical compositions.

Biphenyl Derivatives, a process for their preparation, their use for preparing a Drug, medicinal products based estoscompuestos,Pharmaceutical compositions containing them and Process for preparing such Pharmaceutical compositions.

机译:联苯衍生物,其制备方法,其在制备药物中的用途,基于雌二醇的药用产品,包含它们的药物组合物以及此类药物组合物的制备方法。

摘要

Biphenyl derivatives of formula (1) wherein R1, R4 independently represent -C (= NH) -NH2 which may also be monosubstituted with -COA, -CO- [C (R6) 2] n-Ar, -COOA, - OH or with a conventional amino protecting group, NH-C (= NH) -NH2, -CO-N = C (NH2) 2, formulas (2) (3),R2, R3, R5 independently represent H, A, OR6, N (R6) 2, NO2, CN, Hal, NHCOA, NHCOAr, NHSO2A, NHSO2Ar, COOR3, CON (R6) 2, CONHAr, COOR6, COAr, S (O) nA, S (O) nAr, -O- [C (R6) 2] m-COOR6, - [C (R6) 2] p-COOR6, -O- [C (R6) 2] m-CON (R6) 2, [C (R6) 2] p-CON (R6) 2, -O - [(R6) 2] m-CONHAr, or - [C (R6) 2] p-CONHAr, X represents - [C (R6 ) 2] n -, - CR6 = CR6 -, - [C (R6) 2] nO-,-O- C (R6) 2 n- -COO--OOC -, - CONR6- or -NR6CO-,R6 representa HA o bencilo A representa alquilo de 1 a 20 tomos de carbono en el cual uno o dos gruposde CH2 pueden estar reemplazadospor tomos de 0 o S o por grupos de -CR6 3DCR6 y 2Fo 1 a 7 tomos de H pueden estar reemplazados por And the salts of these compounds 1. Procedures for preparing these compounds and their salts, i.e. (a) separating them from a functional derivative by treatment with a Soviet or hydrogenolysis agent, (b) converting one or more R1, R2, R3, R4 and / or R5 residues to one or more R1, R2, R3, R4 and / or R5 residues, And / or (c) converting a formula group or acid to its salts. It also describes a formula for a drug, a drug ingredient containing at least one formula, and a procedure for preparing these drug ingredients,A formula compound is an inhibitor of XA coagulation factor, which can be used for disease prevention and / or treatment; a formula compound is an anticoagulation factor.
机译:式(1)的联苯衍生物,其中R 1,R 4独立地代表-C(= NH)-NH 2,它们也可以被-COA,-CO- [C(R 6)2] n-Ar,-COOA,-OH或具有常规氨基保护基的NH-C(= NH)-NH2,-CO-N = C(NH2)2,式(2)(3),R2,R3,R5独立地代表H,A,OR6,N (R6)2,NO2,CN,Hal,NHCOA,NHCOAr,NHSO2A,NHSO2Ar,COOR3,CON(R6)2,CONHAr,COOR6,COAr,S(O)nA,S(O)nAr,-O- [C (R6)2] m-COOR6,-[C(R6)2] p-COOR6,-O- [C(R6)2] m-CON(R6)2,[C(R6)2] p-CON( R6)2,-O-[(R6)2] m-CONHAr或-[C(R6)2] p-CONHAr,X代表-[C(R6)2] n-,-CR6 = CR6-,- [C(R6)2] nO-,-O- C(R6)2 n- -COO-OOC-,-CONR6-或-NR6CO-,R6代表HA o bencilo A代表alquilo de 1和20 tomos de carbono完整的CH2磷酸酯-CR6 3DCR6 y 2Fo 1 a 7磷酸酯7磷酸酯和这些化合物的盐1.这些化合物的制备方法化合物及其盐,即(a)通过用苏联解毒剂或氢解剂处理将其与功能衍生物分离,(b)将一个或多个R1,R2,R3,R4和/或R5残基转化为一个或多个R1,R2 ,R3,R4和/或R5残基,和/或(c)将式基团或酸转化为其盐。还描述了药物的配方,包含至少一种配方的药物成分以及制备这些药物成分的方法。配方化合物是XA凝血因子的抑制剂,可以用于疾病的预防和/或治疗;式化合物是抗凝因子。

著录项

  • 公开/公告号AR019264A1

    专利类型

  • 公开/公告日2002-02-13

    原文格式PDF

  • 申请/专利号AR1999P102014

  • 发明设计人

    申请日1999-04-30

  • 分类号C07C257/18;C07C257/20;C07C279/20;A61K31/155;

  • 国家 AR

  • 入库时间 2022-08-22 00:46:29

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