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    Rifamycin derivatives
    2.
    发明授权
    Rifamycin derivatives 有权
    利福霉素衍生物

    公开(公告)号：US07229996B2

    公开(公告)日：2007-06-12

    申请号：US11186187

    申请日：2005-07-21

    申请人： Zhenkun Ma ,  Jing Li ,  Susan Harran ,  Yong He ,  Keith P. Minor ,  In Ho Kim ,  Charles Z. Ding ,  Jamie C. Longgood ,  Yafei Jin ,  Keith D. Combrink

    发明人： Zhenkun Ma ,  Jing Li ,  Susan Harran ,  Yong He ,  Keith P. Minor ,  In Ho Kim ,  Charles Z. Ding ,  Jamie C. Longgood ,  Yafei Jin ,  Keith D. Combrink

    IPC分类号： C07D498/08 ,  A61K31/4709 ,  A61P31/04

    CPC分类号： C07D401/12 ,  C07D455/02

    摘要： Novel rifamycin derivatives of formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or their salts, hydrates or prodrugs thereof, wherein: a preferred R comprises hydrogen, acetyl; L is a linker, a preferred linker group elements selected from any combination of 1 to 5 groups shown FIG. 1, provided L is not wherein R1 is H, methyl or alkyl. The inventive compounds exhibit valuable antibiotic properties. Formulations having these compounds can be used in the control or prevention of infectious diseases in mammals, both humans and non-humans. In particular, the compounds exhibit a pronounced antibacterial activity, even against multiresistant strains of microbes.

    摘要翻译： 式I的新型利福霉素衍生物（氢醌和相应的醌（C 1 -C 4））形成）：或其盐，水合物或前药，其中：优选的R 包括氢，乙酰基; L是接头，优选的连接基团元素选自1至5个组的任何组合，如图1所示。 1，其中L不是其中R 1是H，甲基或烷基。 本发明化合物显示出有价值的抗生素性质。 具有这些化合物的制剂可以用于控制或预防哺乳动物，包括人和非人的感染性疾病。 特别地，这些化合物甚至显示出显着的抗菌活性，即使是针对多抗菌菌株的微生物。

    Rifamycin imino derivatives effective against drug-resistant microbes
    3.
    发明授权
    Rifamycin imino derivatives effective against drug-resistant microbes 有权
    对抗耐药性微生物有效的利福霉素亚氨基衍生物

    公开(公告)号：US07238694B2

    公开(公告)日：2007-07-03

    申请号：US11034279

    申请日：2005-01-12

    申请人： Charles Z. Ding ,  Yafei Jin ,  Jamie C. Longgood ,  Zhenkun Ma ,  Jing Li ,  In Ho Kim ,  Keith P. Minor ,  Susan Harran

    发明人： Charles Z. Ding ,  Yafei Jin ,  Jamie C. Longgood ,  Zhenkun Ma ,  Jing Li ,  In Ho Kim ,  Keith P. Minor ,  Susan Harran

    IPC分类号： C07D498/08 ,  C07D519/00 ,  A61K31/4709 ,  A61K31/496 ,  A61P31/04

    CPC分类号： C07D498/08 ,  C07D519/00

    摘要： The present invention relates to rifamycin 3-iminomethylenyl (—CH═N—) derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. The claimed rifamycin derivative has a rifamycin moiety covalently linked to a linker through an iminomethylenyl (—CH═N—) group at the C-3 carbon of the rifamycin moiety and the linker is, in turn, covalently linked to a quinolone structure or its pharmacophore within the DNA gyrase and topoisomerase IV inhibitor family. The inventive rifamycins are novel and exhibit activity against both rifampin and ciprofloxacin-resistant microorganisms.

    摘要翻译： 本发明涉及具有抗菌活性的利福霉素3-亚氨基亚甲基（-CH-N-）衍生物，其包括抗药性微生物的活性。 所要求的利福霉素衍生物具有通过利莫霉素部分的C-3碳上的亚氨基亚甲基（-CH-N-）基团与连接体共价连接的利福霉素部分，并且连接体又与喹诺酮结构共价连接或其 DNA促旋酶和拓扑异构酶IV抑制剂家族内的药效团。 本发明的利福霉素是新颖的，并且表现出抵抗利福平和环丙沙星抗性微生物的活性。

    Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases
    6.
    发明授权
    Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases 失效
    用于抑制G蛋白功能的三环酰胺的代谢物和治疗增殖性疾病的方法

    公开(公告)号：US07271174B2

    公开(公告)日：2007-09-18

    申请号：US10874556

    申请日：2004-06-23

    申请人： Swapan K. Chowdhury ,  Anima Ghosal ,  Robert M. Iannucci ,  Wenqing Feng ,  Tze-Ming Chan ,  Shmuel Zbaida ,  Kevin B. Alton ,  Ronald J. Doll ,  Keith P. Minor

    发明人： Swapan K. Chowdhury ,  Anima Ghosal ,  Robert M. Iannucci ,  Wenqing Feng ,  Tze-Ming Chan ,  Shmuel Zbaida ,  Kevin B. Alton ,  Ronald J. Doll ,  Keith P. Minor

    IPC分类号： C07D221/06 ,  A61K31/435

    CPC分类号： C07D401/14

    摘要： The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): and pharmaceutically acceptable isomers, salts, solvates or esters of the compound of formula (I), wherein: R1 is selected from the group consisting of H and ═O; R2-R5 can be the same or different, each being independently selected from the group consisting of H, —OH, halide, —NH2 and ═O; and, the combination solid-dashed lines independently represent either single bonds or double bonds, wherein the number of combination solid-dashed lines that are double bonds is not greater than 2, and when, the double bonds are not adjacent, and when 0, one of R1-R5 is not H. Also disclosed are methods of treatment of proliferative diseases and methods for inhibiting the abnormal growth of cells, and for inhibiting farnesyl protein transferase using the novel compounds.

    摘要翻译： 本发明涉及由结构式（I）表示的三环酰胺的代谢物和结构相关的化合物：和式（I）化合物的药学上可接受的异构体，盐，溶剂化物或酯，其中：R 1 选自H和-O; R 2 -R 5可以相同或不同，各自独立地选自H，-OH，卤化物，-NH 2， SUB>和-O; 并且，组合虚线独立地表示单键或双键，其中双键的组合实线的数目不大于2，当双键不相邻时，当为0时， R 1〜R 5之一不是H.还公开了治疗增殖性疾病的方法和抑制细胞异常生长的方法，以及用于抑制法呢基蛋白转移酶 使用新型化合物。