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24 条记录 (耗时 0.037 秒)

    Method for treating and preventing mycobacterium infections
    11.
    发明授权
    Method for treating and preventing mycobacterium infections 失效
    治疗和预防分枝杆菌感染的方法

    公开(公告)号：US06268393B1

    公开(公告)日：2001-07-31

    申请号：US09417672

    申请日：1999-10-14

    申请人： Ze-Qi Xu ,  Yuh Meei Lin ,  Michael T. Flavin

    发明人： Ze-Qi Xu ,  Yuh Meei Lin ,  Michael T. Flavin

    IPC分类号： A61K31353

    CPC分类号： A61K45/06 ,  A61K31/366 ,  A61K31/37

    摘要： Calanolides and analogues thereof that demonstrate potent mycobacterium activity are provided. Also provided is a method of using calanolides and analogues thereof for treating or preventing mycobacterium infections. The calanolides and analogues thereof provided are obtained via syntheses employing chromene 4 and chromanone 7 as key intermediates.

    摘要翻译： 提供了表现出有效的分枝杆菌活性的卡立仑内酯及其类似物。 还提供了用于治疗或预防分枝杆菌感染的calanolide及其类似物的方法。 所提供的癸内酰胺及其类似物通过使用色烯4和苯并二氢吡喃酮7作为关键中间体的合成获得。

    Method for the preparation of aldol product 7B
    14.
    发明授权
    Method for the preparation of aldol product 7B 失效
    醛醇产品7B的制备方法

    公开(公告)号：US5840921A

    公开(公告)日：1998-11-24

    申请号：US925992

    申请日：1997-09-09

    申请人： Michael T. Flavin ,  Ze-Qi Xu ,  John D. Rizzo ,  Albert Khilevich

    发明人： Michael T. Flavin ,  Ze-Qi Xu ,  John D. Rizzo ,  Albert Khilevich

    IPC分类号： C07D311/58 ,  A61K31/365 ,  A61K45/06 ,  A61P31/12 ,  A61P37/04 ,  C07D311/16 ,  C07D493/04 ,  C07D493/14 ,  C07D493/00

    CPC分类号： C07D493/04 ,  A61K45/06 ,  C07D311/16 ,  C07D493/14

    摘要： A method of preparing (.+-.)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. Useful intermediates for preparing (+)-calanolide A and its derivatives are also provided. According to the disclosed method, chromene 4 intermediate was reacted with acetaldehyde diethyl acetal or paraldehyde in the presence of an acid catalyst with heating, or a two-step reaction including an aldol reaction with acetaldehyde and cyclization either under acidic conditions or neutral Mitsunobu conditions, to produce chromanone 7. Reduction of chromanone 7 with sodium borohydride, in the presence of cerium trichloride, produced (.+-.)-calanolide A. A method for resolving (.+-.)-calanolide A into its optically active forms by a chiral HPLC system or by enzymatic acylation and hydrolysis is also disclosed. Finally, a method for treating or preventing viral infections using (.+-.)-calanolide A or (-)-calanolide A is provided.

    摘要翻译： 提供了从色烯4制备（+/-） - 丙内酰脲A，1，一种有效的HIV逆转录酶抑制剂的方法。 还提供了制备（+） - 蒎烯内酯A及其衍生物的有用的中间体。 根据所公开的方法，在酸催化剂的存在下，将色烯4中间体与乙醛二乙基缩醛或对甲醛反应，或者在酸性条件或中性Mitsunobu条件下，包括醛醇与乙醛反应和醛化反应的两步反应， 产生苯并二氢吡喃酮7.在三氯化铈的存在下，用硼氢化钠还原色酮7.产生（+/-） - 甘露糖苷A。一种通过手性拆分（+/-） - 卡立拉内酯A至其光学活性形式的方法 还公开了HPLC系统或通过酶酰化和水解。 最后，提供了一种使用（+/-） - 蒎烯内酰胺A或（ - ） - cal醇酯A治疗或预防病毒感染的方法。

    Scalable method for the isolation of anti-HIV agents from the tropical plant calophyllum
    15.
    发明授权
    Scalable method for the isolation of anti-HIV agents from the tropical plant calophyllum 失效
    用于从热带植物calophyllum分离抗HIV药物的可扩展方法

    公开(公告)号：US6160131A

    公开(公告)日：2000-12-12

    申请号：US213192

    申请日：1998-12-17

    申请人： Yuh-Meei Lin ,  Herbert M. Anderson ,  Tuah R. Jenta ,  Michael J. Williams ,  Michael T. Flavin ,  Ze-Qi Xu

    发明人： Yuh-Meei Lin ,  Herbert M. Anderson ,  Tuah R. Jenta ,  Michael J. Williams ,  Michael T. Flavin ,  Ze-Qi Xu

    IPC分类号： C07D493/14 ,  C07D311/78 ,  C07D407/14

    CPC分类号： C07D493/14

    摘要： An efficient and scalable method is reported for the isolation of costatolide (2), an HIV-1-specific nonnucleoside reverse transcriptase inhibitor (NNRTI), from the latex of Calophyllum plants such as C. teysmannii var. inophylloide. An overall yield of 10.6% of costatolide, with a purity of 96%, was obtained by repetitive recrystallization of the latex from a single organic solvent after the oily material was removed by treatment with hexane. A second major component of the latex, soulattrolide (3), another HIV-1 NNRTI, was also isolated. Both compounds were characterized by spectroscopic and chromatographic analyses and their in vitro anti-HIV activities were also confirmed. The results suggest that sufficient supplies of costatolide can be obtained in a relatively low-cost manner from natural sources.

    摘要翻译： 报道了从Calphyllum植物如C.teysmannii变种的胶乳中分离Costatolide（2）（一种HIV-1特异性非核苷逆转录酶抑制剂（NNRTI））的有效和可扩展的方法。 叶黄素 通过用己烷处理除去油状物后，通过从单一有机溶剂中的胶乳的重复重结晶，可以获得纯度为96％的花色滑石的总产率10.6％。 还分离了乳胶的另一个主要组分，即另外的HIV-1 NNRTI的soulattrolide（3）。 通过光谱和色谱分析表征了两种化合物，并证实了其体外抗HIV活性。 结果表明，可以以相对低成本的方式从天然来源获得足够的costatolide供应。