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SYNTHESIS OF AMIDE DERIVATIVES OF SOME NONSTEROIDAL ANTIINFLAMMATORY DRUGS AS POTENTIAL PRO-DRUGS

机译：一些非甾体类抗炎药作为潜在的前药的酰胺衍生物的合成

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摘要

The present invention presents a method for masking acidic groups existing in NSAI drugs to prevent or to reduce the hazards of NSAI drugs to GI (gastrointestinal) system. The developed method comprises production of new amide derivatives by methyl esterification of carboxylic acid groups which belong to NSAI drugs and then amidification of the same. The invention is also related to the amide derivatives of new NSAI drugs which are suitable for use as pro-drugs.

机译：本发明提出了一种掩盖NSAI药物中存在的酸性基团的方法，以预防或减少NSAI药物对GI（胃肠道）系统的危害。所开发的方法包括通过将属于NSAI药物的羧酸基团进行甲基酯化来生产新的酰胺衍生物，然后使其酰胺化。本发明还涉及适合用作前药的新的NSAI药物的酰胺衍生物。

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公开/公告号EP2878592B1

专利类型
公开/公告日2019-02-20

原文格式PDF
申请/专利权人 KÜCÜKGÜZEL ILKAY;
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申请/专利号EP20140188019
发明设计人 KÜCÜKGÜZEL ILKAY;KULABAS NECLA;SET IREM;
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申请日2014-10-07
分类号C07C235/60;C07D263/57;C07C237/20;C07D491/052;C07D213/75;C07D213/80;C07D333/22;C07D333/24;C07C317/44;C07C233/22;C07C233/60;C07C235/34;C07D263/32;A61K31/165;A61P29;C07C235/78;C07C237/30;C07C237/44;C07D207/20;C07C245/08;C07D207/337;C07D209/28;C07D209/46;A61K31/40;A61K31/381;A61K31/421;A61K31/655;
国家 EP
入库时间 2022-08-21 12:29:43

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