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1. 发明授权

US5789591A Process for preparing 1-substituted 8-chloro-7-fluoro-9-methyl-4-oxo-4H-quinolizine-3-carboxylic acid ethyl ester compounds 失效
标题翻译：制备1-取代的8-氯-7-氟-9-甲基-4-氧代-4H-喹嗪-3-羧酸乙酯化合物的方法
公开(公告)号：US5789591A
公开(公告)日：1998-08-04
申请号：US735625
申请日：1996-10-23
申请人： Daniel T. Chu , David Allen Degoey , David J. Grampovnik , Larry Lewis Klein , Paul A. Lartey , Christina Louise Leone , Sheela Albert Thomas , Ming Clinton Yeung
发明人： Daniel T. Chu , David Allen Degoey , David J. Grampovnik , Larry Lewis Klein , Paul A. Lartey , Christina Louise Leone , Sheela Albert Thomas , Ming Clinton Yeung
IPC分类号： C07D455/02
CPC分类号： C07D455/02
摘要： A process for preparing a compound having the formula: ##STR1## wherein R is selected from the group consisting of C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkylmethyl, C.sub.1 -C.sub.6 -alkyl, allyl and 2-methoxyethyl, by reacting: ##STR2## under defined conditions with subsequent stepwise reactions of the respective intermediate compounds with a malonic acid diester, POCl.sub.3, and by heating the final intermediate in a high boiling solvent.
摘要翻译：制备具有下式的化合物的方法：其中R选自C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基甲基，C 1 -C 6 - 烷基，烯丙基和2-甲氧基乙基，通过以下反应：在定义的条件下，将各种中间体化合物与丙二酸二酯POCl 3的后续逐步反应，并通过在高沸点溶剂中加热最终的中间体，在图像> 下进行。

2. 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。

3. 发明授权

US08129417B2 Substituted octahydrocyclopenta[C]pyrrol-4-amines as calcium channel blockers 有权
标题翻译：取代的八氢环戊二烯并[C]吡咯-4-胺作为钙通道阻断剂
公开(公告)号：US08129417B2
公开(公告)日：2012-03-06
申请号：US12625754
申请日：2009-11-25
申请人： Andrew O. Stewart , Xenia B. Searle , Daria Darczak , Ming Clinton Yeung , Stanley DiDomenico
发明人： Andrew O. Stewart , Xenia B. Searle , Daria Darczak , Ming Clinton Yeung , Stanley DiDomenico
IPC分类号： A61K31/4439 , A61K31/403 , C07D401/04 , C07D209/52
CPC分类号： C07D209/02
摘要： The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
摘要翻译：本申请涉及含有式（I）化合物的钙通道抑制剂，其中L1，L2，R1，R2和R3如说明书中所定义。本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗病症和病症的方法。

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