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Anti-infectious macrolide agents

机译:抗感染大环内酯类药物

摘要

Invention Patent "MACROLYDE ANTI-INFECTIOUS AGENTS". Compounds of formula (1), (2) or (3), in which R ~ a ~ is H; (1 - 10C) substituted or unsubstituted alkyl; (2 - 10C) substituted or unsubstituted alkenyl; (2 - 10C) substituted or unsubstituted alkynyl; (4 - 14C) substituted or unsubstituted aryl; (5 - 20C) substituted or unsubstituted arylalkyl; or OR ~ a ~ is replaced by H; R ~ b ~ is H or halogen; R ~ and ~ is H or a protecting group; R ~ d ~ is methyl, (3 - 10C) unsubstituted alkyl; (1 - 10C) substituted alkyl; (2 - 10C) substituted or unsubstituted alkynyl; (4 - 14C) substituted or unsubstituted aryl; (5 - 20C) substituted or unsubstituted arylalkyl; (5 - 20C) substituted or unsubstituted arylalkenyl; (5 - 20C) substituted or unsubstituted arylalkynyl; (5 - 20C) substituted or unsubstituted amidoarylalkyl; (5 - 20C) substituted or unsubstituted amidoarylalkenyl; or (5 - 20C) substituted or unsubstituted amidoarylalkynyl; R ~ and ~ is H or a protecting group; L is methylene or carbonyl; T is -O-, -N (R) -, -N (OR) -, -N (NHCOR) -, -N (N = CHR) -, or -N (NHR) - where R is H or R ~ a ~ as defined above, with the proviso that when L is methylene, T is -O-; one among Z and Y is H and the other is OH, OH protected, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle or Z and Y together are = O, = NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.
机译:发明专利“ MACROLYDE抗感染剂”。式(1),(2)或(3)的化合物,其中R〜a〜为H; (1-10C)取代或未取代的烷基; (2-10C)取代或未取代的烯基; (2-10C)取代或未取代的炔基; (4-14C)个取代或未取代的芳基; (5-20​​℃)取代或未取代的芳烷基;或OR〜a〜被H取代; R〜b〜是H或卤素; R〜和〜是H或保护基; R〜d〜是甲基,(3-10C)未取代的烷基; (1-10C)取代的烷基; (2-10C)取代或未取代的炔基; (4-14C)个取代或未取代的芳基; (5-20​​℃)取代或未取代的芳烷基; (5-20​​℃)取代或未取代的芳基烯基; (5-20​​℃)取代或未取代的芳基炔基; (5-20​​℃)取代或未取代的酰胺基芳基烷基; (5-20​​℃)取代或未取代的酰胺基芳基烯基;或(5-20​​℃)取代或未取代的酰胺基芳基炔基;或R〜和〜是H或保护基; L为亚甲基或羰基; T是-O-,-N(R)-,-N(OR)-,-N(NHCOR)-,-N(N = CHR)-或-N(NHR)-其中R是H或R〜 a〜如上定义,条件是当L为亚甲基时,T为-O-; Z和Y中的一个是H,另一个是OH,被OH保护的或氨基,单或二烷基氨基,被保护的氨基或氨基杂环,或者Z和Y一起是= O,= NOH或衍生的肟;包括其任何药学上可接受的盐和其任何立体异构形式以及其立体异构形式的混合物的抗微生物剂。

著录项

  • 公开/公告号BR0010680A

    专利类型

  • 公开/公告日2002-02-19

    原文格式PDF

  • 申请/专利权人 KOSAN BIOSCIENCES INC.;

    申请/专利号BR20000010680

  • 发明设计人 DANIEL T. W. CHU;GARY W. ASHLEY;

    申请日2000-04-14

  • 分类号C07H17/08;A61K31/70;

  • 国家 BR

  • 入库时间 2022-08-22 00:46:14

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