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1. 发明授权

US5696084A Amino-lipopetide antifungal agents 失效
标题翻译：氨基脂肽抗真菌剂
公开(公告)号：US5696084A
公开(公告)日：1997-12-09
申请号：US698610
申请日：1996-08-16
申请人： Paul A. Lartey , Leping Li , Larry Lewis Klein , Christina Louise Leone , Sheela Albert Thomas , Ming Clinton Yeung , David Allen Degoey , David J. Grampovnik
发明人： Paul A. Lartey , Leping Li , Larry Lewis Klein , Christina Louise Leone , Sheela Albert Thomas , Ming Clinton Yeung , David Allen Degoey , David J. Grampovnik
IPC分类号： A61K38/00 , C07K7/56 , A61K38/12 , C07K5/00
CPC分类号： C07K7/56 , A61K38/00
摘要： Disclosed are novel antifungal agents having the formula: ##STR1## or a pharmaceutically acceptable acid, ester or prodrug thereof, wherein preferred compounds include those compounds wherein R.sub.1 is selected from the group consisting of --NH.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, fluoro, and hydroxyl; R.sub.3 is selected from the group consisting of --CH.sub.2 (p-C.sub.6 H.sub.4).sub.3 O(CH.sub.2).sub.3 CH.sub.3, --CH.sub.2 (p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --COO(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(Piperazinyl)(p-C.sub.6 H.sub.4).sub.2 OCH.sub.3, --CO(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.4 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)OCH.sub.3, and --CO(p-C.sub.6 H.sub.4)(Piperazinyl)O(CH.sub.2).sub.6 CH.sub.3 ; and R.sub.4 is selected from the group consisting of --CH(OH)CH.sub.3, --CH.sub.2 OH, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, --CH.sub.2 (CH.sub.2)NH.sub.2, --CH.sub.2 NH.sub.2, --CH.sub.2 (CH.sub.2).sub.2 (NH)C.dbd.(NH)--NH.sub.2, --CH.sub.3, --CH.sub.2 (Ph)OH, hydrogen, --CH.sub.2 CH.sub.2 COOH, and --CH.sub.2 COOH. Also disclosed are pharmaceutical compositions containing such compounds and the use of the same in the treatment of fungal infections.
摘要翻译：公开了具有下式的新型抗真菌剂：其中优选的化合物包括那些其中R 1选自-NH 2;或其药学上可接受的酸，酯或前药。 R2选自氢，氟和羟基; R 3选自-CH 2（对-C 6 H 4）3 O（CH 2）3 CH 3，-CH 2（对-C 6 H 4）O（CH 2）6 CH 3，-COO（对-C 6 H 4）O（CH 2）6 CH 3，-CO（哌嗪基）（对-C 6 H 4）2 OCH 3，-CO（p-C 6 H 4）O（CH 2）6 CH 3，-CO（p-C 6 H 4）（哌嗪基）（对-C 6 H 4）O（CH 2）4 CH 3，-CO（p-C 6 H 4）（哌嗪基）（p-C6H4）O（CH2）6CH3，-CO（对-C6H4）（哌嗪基）（对-C 6 H 4）OCH 3和-CO（对-C 6 H 4）（哌嗪基）O（CH 2）并且R 4选自-CH（OH）CH 3，-CH 2 OH，-CH 2 CH 3，-CH 2 CH 2 CH 2 NH 2，-CH 2（CH 2）NH 2，-CH 2 NH 2，-CH 2（CH 2）2（NH）C =（NH） NH 2，-CH 3，-CH 2（Ph）OH，氢，-CH 2 CH 2 COOH和-CH 2 COOH。还公开了含有这些化合物的药物组合物及其在治疗真菌感染中的用途。

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