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    CAPREOMYCIN DERIVATIVES AND THEIR USE AS ANTIBACTERIALS
    3.
    发明申请
    CAPREOMYCIN DERIVATIVES AND THEIR USE AS ANTIBACTERIALS 审中-公开
    CAPIROMYCIN衍生物及其作为抗生素的使用

    公开(公告)号：US20090203585A1

    公开(公告)日：2009-08-13

    申请号：US12299258

    申请日：2007-03-13

    申请人： Joseph P. Lyssikatos ,  Steven Mark Wenglowsky ,  D. David Hennings ,  Daniel John Watson

    发明人： Joseph P. Lyssikatos ,  Steven Mark Wenglowsky ,  D. David Hennings ,  Daniel John Watson

    IPC分类号： A61K38/12 ,  C07K7/06 ,  C07K1/06 ,  C12P21/04 ,  A61P31/04

    CPC分类号： C07K7/56 ,  A61K38/00 ,  Y02A50/401

    摘要： The present invention relates to phenylurea derivatives of capreomycin I, IIB, IIA, or IB, and metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present invention are useful as antibacterial agents for treating bacterial infections and for treating disorders caused by bacterial infections. The present invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial infections by administering such compounds. The present invention also relates to methods of preparing such compounds.

    摘要翻译： 本发明涉及卷曲霉素I，IIB，IIA或IB的苯基脲衍生物及其代谢产物及其药学上可接受的盐和溶剂化物。 本发明的化合物可用作治疗细菌感染和治疗由细菌感染引起的疾病的抗菌剂。 本发明还涉及含有这些化合物的药物组合物和通过施用这些化合物治疗细菌感染的方法。 本发明还涉及制备这些化合物的方法。

    Dynamic resolution of isomers and resolved isomers
    6.
    发明授权
    Dynamic resolution of isomers and resolved isomers 有权
    动态拆分异构体和拆分的异构体

    公开(公告)号：US07388098B2

    公开(公告)日：2008-06-17

    申请号：US09961932

    申请日：2001-09-24

    申请人： John J. Venit ,  Gary D. Madding ,  Victor W. Rosso ,  Francis J. Okuniewicz ,  Robert P. Discordia ,  Susanne Kiau ,  Atul S. Kotnis ,  Michael E. Randazzo ,  D. David Hennings ,  Jingyang Zhu ,  Jason G. Chen

    发明人： John J. Venit ,  Gary D. Madding ,  Victor W. Rosso ,  Francis J. Okuniewicz ,  Robert P. Discordia ,  Susanne Kiau ,  Atul S. Kotnis ,  Michael E. Randazzo ,  D. David Hennings ,  Jingyang Zhu ,  Jason G. Chen

    IPC分类号： C07C53/134 ,  C07D233/00 ,  C07D277/00 ,  C07B55/00

    CPC分类号： C07D233/78 ,  C07C51/412 ,  C07C51/43 ,  C07C213/08 ,  C07C213/10 ,  C07D233/74 ,  C07C57/58

    摘要： Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and the leaving group or (ii) to produce the increase in the less soluble amine salt in the absence of a strong base; and (c) maintaining the reaction for a period of time effective to increase the amount of the desired alpha-substituted carboxylic acid isomer.

    摘要翻译： 提供了相对于不期望的异构体富集α-取代的羧酸的所需异构体的动态拆分方法，该方法包括：（a）在溶剂中使α-取代的羧酸接触，其中α取代为 离去基团，其中所述α碳是手性的，与同基因胺形成在所选择的反应条件下部分不溶的盐，其中选择所述同基因胺，使得不需要的α-取代羧酸的胺盐的溶解度为 在选择的反应条件下大于所需α-取代羧酸的胺盐的浓度; （b）在所选择的反应条件下使所述盐与亲核试剂反应，其中所述反应有效地产生所述α-取代羧酸的较不溶性胺盐的净增加，并且其中所选择的条件选择为：（i） 促进亲核试剂和离去基团的亲核取代，或（ii）在没有强碱的情况下产生较不溶性胺盐的增加; 和（c）保持反应一段时间有效以增加所需的α-取代的羧酸异构体的量。