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11. 发明授权

US5075289A 9-R-azacyclic erythromycin antibiotics 失效
标题翻译： 9-R-抗坏血酸抗菌药物
公开(公告)号：US5075289A
公开(公告)日：1991-12-24
申请号：US203400
申请日：1988-06-07
申请人： Richard J. Pariza , Paul A. Lartey , Clarence J. Maring , Larry L. Klein
发明人： Richard J. Pariza , Paul A. Lartey , Clarence J. Maring , Larry L. Klein
IPC分类号： A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61P31/00 , A61P31/04 , C07H17/08 , C07H19/04
CPC分类号： C07H17/08
摘要： Semisynthetic antibiotics with improved therapeutic properties are disclosed. In particular, 9-R-azacyclic derivatives of erythromycin, its derivatives, and their salts and esters show superior antimicrobial activity compared to other macrolide compounds.

12. 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。

13. 发明授权

US5578579A 4"-deoxyerythromycin derivatives 失效
标题翻译： 4“ - 脱氧红霉素衍生物
公开(公告)号：US5578579A
公开(公告)日：1996-11-26
申请号：US284730
申请日：1994-08-02
申请人： Paul A. Lartey , Larry L. Klein , Ramin Faghih , Hugh N. Nellans
发明人： Paul A. Lartey , Larry L. Klein , Ramin Faghih , Hugh N. Nellans
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/00 , A61P1/08 , A61P1/10 , A61P31/04 , C07D233/22 , C07H17/08
CPC分类号： C07H17/08
摘要： 4"-Deoxy derivatives of erythromycin having the Formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are enhancers of gastric motility but have minimal antibacterial activity, as well as pharmaceutical compositions containing the same and methods for their use and preparation.
摘要翻译： 4'' - 具有式（I）的红霉素的脱氧衍生物及其药学上可接受的盐，其是胃动力的增强剂，但是具有最小的抗菌活性，以及含有它们的药物组合物以及它们的方法使用和准备。

14. 发明授权

US5140014A Rosaramicin derivatives and method of treating bacterial infections 失效
标题翻译：罗斯玛林衍生物和治疗细菌感染的方法
公开(公告)号：US5140014A
公开(公告)日：1992-08-18
申请号：US431582
申请日：1989-11-13
申请人： Clarence J. Maring , Paul A. Lartey , Leslie A. Freiberg
发明人： Clarence J. Maring , Paul A. Lartey , Leslie A. Freiberg
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention is directed to the production and utilization of novel antibiotic compounds. These compounds are derivatives of the antibacterial agents tylosin and rosaramicin and exert a broad spectrum antibiotic activity toward several bacterial strains. Pharmaceutical compositions and methods of treating bacterial infections are described.
摘要翻译：本发明涉及新型抗生素化合物的生产和利用。这些化合物是抗菌剂泰乐菌素和rosaramicin的衍生物，并向几种细菌菌株发挥广谱抗生素活性。描述了治疗细菌感染的药物组合物和方法。

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