首页> 外国专利> Beta tiopropionilaminoacidos Derivatives, Pharmaceutical compositions containing such Derivatives, Process for preparing them,Use of dichosderivados for Treatment of bacterial infections and intermediaries in the Composite Application procedure

Beta tiopropionilaminoacidos Derivatives, Pharmaceutical compositions containing such Derivatives, Process for preparing them,Use of dichosderivados for Treatment of bacterial infections and intermediaries in the Composite Application procedure

机译:βtiopropionilaminoacidos衍生物,包含此类衍生物的药物组合物,其制备方法,双歧杆菌在复合应用程序中用于治疗细菌感染和中间体的用途

摘要

Derivatives of beta-mercapto amino acids and solvates or pharmaceutically acceptable in vivo hydrolysable esters of formula (I) in which R is hydrogen, a salt-forming cation, or an in vivo hydrolytable ester forming group; R1 is deformul a (II) where A is a monocyclic aryl or a heteroaryl ring, and B is a monocyclic aryl, an alicyclic or heterocyclic ring, C and D are independently -Zp (CR8R9) q -O - (CR8R9) q-Zp , where p is O or 1,Q is 0 or 3, if P + Q in C is not o, R8 and R9 are independent hydrogen or asphalt (C18),Or add together to represent oxo, YZ is O, nr10 or s (o),Where R10 is hydrogen tar (C1-6),X is 0-2, where C and D are combined at each or the orthogonal position between ring a and brominated diphenyl ether (b);R2 is hydrogen, pitch (C1-6) or aril acquilo (C1-6) R3 is hydrogen, pitch (C1-6) can be selectively replaced by up to three dehalogeno, cycloquilo (c3-7) atoms,1. Aril cycloquilo (c3-7) capacitor, asphalt cycle (c3-7) asphalt (c2-6) alquenilo (c2-6),Penicillin (c2-6),aryl, aryl- (CH2) mX- (CH2) N, heterocyclyl or heterocyclyl- (CH2) mX- (CH2) n, where m is O to 3, n is 1 to 3, and X is O, S (O) x, where x is 0-2 or a link; R4 is hydrogen, or an in vivo hydrolyzable group and R5 and R6 are independently hydrogen and (C1-6) alkyl or together represent (CH2),where r is 2 to 5 salts, solvates, esters.Useful in the treatment of bacterial infections in human animals, by administration together with a beta-lactam antibiotic.Also the synthesis of such derivatives and other advanced objects in the Title.
机译:β-巯基氨基酸的衍生物和式(I)的溶剂化物或药学上可接受的体内可水解酯,其中R为氢,成盐阳离子或体内可水解成酯基团; R1为甲(II),其中A为单环芳基或杂芳基环,并且B为单环芳基,脂环或杂环,C和D独立地为-Zp(CR8R9)q -O-(CR8R9)q- Zp,其中p为O或1,Q为0或3,如果C中的P + Q不为o,R8和R9为独立的氢或沥青(C18),或加在一起表示oxo,YZ为O,nr10或s(o),其中R10为氢焦油(C1-6),X为0-2,其中C和D在环a和溴化二苯醚之间的每个或正交位置(b)结合; R2为氢,螺距(C1-6)或Aril acquilo(C1-6)R3是氢,沥青(C1-6)可以被最多三个脱卤代,环喹(c3-7)原子选择性地取代,1。阿里尔环奎洛(c3-7)电容器,沥青循环(c3-7)沥青(c2-6)阿奎洛(c2-6),青霉素(c2-6),芳基,芳基-(CH2)mX-(CH2)N,杂环基或杂环基-(CH 2)mX-(CH 2)n,其中m为O至3,n为1至3,并且X为O,S(O)x,其中x为0-2或链接; R 4是氢或体内可水解基团,R 5和R 6独立地是氢和(C 1-6)烷基或一起代表(CH 2),其中r是2至5个盐,溶剂化物,酯。用于治疗细菌感染通过与β-内酰胺类抗生素一起给药在人类动物体内。此类衍生物和标题中其他高级物体的合成。

著录项

  • 公开/公告号AR009987A1

    专利类型

  • 公开/公告日2000-05-17

    原文格式PDF

  • 申请/专利权人 SMITHKLINE BEECHAM P.L.C;

    申请/专利号AR1997P104739

  • 发明设计人

    申请日1997-10-15

  • 分类号C07C321/10;C07D209/86;C07D333/24;C07D307/54;C07D409/00;C07D417/00;A61K31/095;A61K31/335;A61K31/38;A61K31/425;

  • 国家 AR

  • 入库时间 2022-08-22 01:57:32

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