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21. 发明授权

US6133274A Hydroxyl-containing bicyclic compounds 失效
标题翻译：含羟基的双环化合物
公开(公告)号：US6133274A
公开(公告)日：2000-10-17
申请号：US756703
申请日：1996-11-26
申请人： Gail E. Underiner , David Porubek , J. Peter Klein , Paul Woodson
发明人： Gail E. Underiner , David Porubek , J. Peter Klein , Paul Woodson
IPC分类号： A61K31/519 , A61K31/522 , C07D473/04 , A61K31/52
CPC分类号： A61K31/522 , A61K31/519
摘要： Disclosed are therapeutic compounds having the formula:(R)j-(core moiety),including resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one to three, the core moiety is either non-cyclic or comprises at least one five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, C.sub.1-6 alkyl or C.sub.1-6 alkenyl, and at least one R has the formula I: ##STR1## n is an integer from seven to twenty and at least one of X or Y is --OH. The other of X or Y, which is not --OH, is hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --, and each W.sub.1, W.sub.2, and W.sub.3 is independently hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --. The X, Y, W.sub.1, W.sub.2, or W.sub.3 alkyl groups may be unsubstituted or substituted by an hydroxyl, halo or dimethylamino group. The disclosed compounds and therapeutic compositions thereof are useful in treating individuals having a disease or treatment-induced toxicity, mediated by second messenger activity.
摘要翻译：公开了具有下式的治疗化合物：（R）j-（核心部分），包括拆分的对映异构体，非对映体，水合物，盐，溶剂合物及其混合物。 j是1至3的整数，核心部分是非环状的或包含至少一个五至七元环结构，R可以选自氢，卤素，羟基，氨基，取代或未取代的苄基，C 1-6烷基或C 1-6烯基，并且至少一个R具有式I：n是7至20的整数，X或Y中的至少一个是-OH。不是-OH的X或Y中的另一个是氢，CH 3 - ，CH 3 -CH 2 - ，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - ，并且每个W 1，W 2和W 3独立地氢，CH 3 - ，CH 3 -CH 2 - ，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - 。 X，Y，W1，W2或W3烷基可以是未取代的或被羟基，卤素或二甲基氨基取代。所公开的化合物及其治疗组合物可用于治疗由第二信使活性介导的患有疾病或治疗诱导的毒性的个体。

22. 发明授权

US5985926A Method for inhibiting intracellular viral replication 失效
标题翻译：抑制细胞内病毒复制的方法
公开(公告)号：US5985926A
公开(公告)日：1999-11-16
申请号：US797326
申请日：1997-02-10
申请人： David W. Leung , Gail E. Underiner , Jack W. Singer
发明人： David W. Leung , Gail E. Underiner , Jack W. Singer
IPC分类号： A61K31/4035 , A61K31/445 , A61K31/472 , A61K31/513 , A61K31/522 , C12N15/48 , A61K31/20
CPC分类号： A61K31/522 , A61K31/4035 , A61K31/445 , A61K31/472 , A61K31/513
摘要： There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an effective amount of a compound that inhibits cellular signaling through a specific phospholipid-based cellular signaling and signal amplification pathway. The invention further provides a method for preventing or delaying clinical symptoms of a group of viral diseases wherein the viral disease is mediated by host cell viral replication. The invention provides an advantage by attacking host cellular signaling mechanisms to prevent the development of drug resistance from rapidly mutating viruses.
摘要翻译：公开了通过施用有效量的抑制细胞信号传导的化合物通过特定的基于磷脂的细胞信号传导和信号扩增来预防或延迟人类免疫缺陷病毒（HIV）血清阳性人类中的获得性免疫缺陷综合征（AIDS）的发生的方法途径。本发明还提供了一种用于预防或延缓一组病毒性疾病的临床症状的方法，其中所述病毒性疾病由宿主细胞病毒复制介导。本发明通过攻击宿主细胞信号传导机制来提供一个优点，以防止快速突变病毒对耐药性的发展。

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