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    Rifamycin imino derivatives effective against drug-resistant microbes
    1.
    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。

    QUINOLONE CARBOXYLIC ACID-SUBSTITUTED RIFAMYCIN DERIVATIVES
    2.
    发明申请
    QUINOLONE CARBOXYLIC ACID-SUBSTITUTED RIFAMYCIN DERIVATIVES 有权
    喹诺酮羧酸取代的赖氨明衍生物

    公开(公告)号：US20090143373A1

    公开(公告)日：2009-06-04

    申请号：US12269652

    申请日：2008-11-12

    申请人： Charles Z. Ding ,  Yafei Jin ,  Keith Combrink ,  In Ho Kim

    发明人： Charles Z. Ding ,  Yafei Jin ,  Keith Combrink ,  In Ho Kim

    IPC分类号： A61K31/4709 ,  C07D498/04 ,  C07D471/20 ,  A61K31/5383 ,  A61P31/04

    CPC分类号： C07D491/20 ,  C07D498/16

    摘要： The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.

    摘要翻译： 化合物包括取代的利福霉素衍生物，其中喹诺酮羧酸药效团与苯并恶嗪利福霉素或螺哌啶利多霉素共价键合。 利福霉素衍生物可用作抗微生物剂，并且对许多人和兽医革兰氏阳性和革兰氏阴性病原体有效。 本发明化合物的优点在于利福霉素和喹诺酮类抗菌药代动力剂与匹配的药代动力学共同输送到感兴趣的靶向病原体。 同时向目标病原体递送多个抗菌药代动力，最大限度地实现协同作用，并最大限度地减少给予抗生素的耐药性。

    Spiro-rifamycin derivatives targeting RNA polymerase
    4.
    发明授权
    Spiro-rifamycin derivatives targeting RNA polymerase 有权
    螺 - 利福霉素衍生物靶向RNA聚合酶

    公开(公告)号：US07202246B2

    公开(公告)日：2007-04-10

    申请号：US11147520

    申请日：2005-06-08

    申请人： Zhenkun Ma ,  In Ho Kim ,  Jing Li

    发明人： Zhenkun Ma ,  In Ho Kim ,  Jing Li

    IPC分类号： C07D225/04 ,  A61K31/495 ,  A61P31/04

    CPC分类号： C07D491/22

    摘要： Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the current invention relate to a series of novel spiro rifamycin derivatives which have demonstrated potent antimicrobial activity.

    摘要翻译： 本发明的化合物涉及具有抗微生物活性的利福霉素衍生物，包括抗耐药微生物的活性。 更具体地，本发明的化合物涉及一系列已经证明有效的抗微生物活性的新型螺利福霉素衍生物。

    Rifamycin C-11 oxime cyclo derivatives effective against drug-resistant microbes
    7.
    发明授权
    Rifamycin C-11 oxime cyclo derivatives effective against drug-resistant microbes 有权
    对抗耐药微生物有效的利福霉素C-11肟环衍生物

    公开(公告)号：US07265107B2

    公开(公告)日：2007-09-04

    申请号：US11076173

    申请日：2005-03-09

    申请人： Jing Li ,  Zhenkun Ma

    发明人： Jing Li ,  Zhenkun Ma

    IPC分类号： C07D498/18 ,  A61K31/395 ,  A61K31/535 ,  A61P31/04

    CPC分类号： C07D498/18

    摘要： The current invention relates to a series of rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the 3,4-cyclo-rifamycin derivatives having an oxime group at the C-11 position.

    摘要翻译： 本发明涉及一系列具有抗菌活性的利福霉素衍生物，包括抗药性微生物的活性，具体地说，具有C-11位上肟基的3,4-环 - 利福霉素衍生物。

    C-25 carbamate rifamycin derivatives with activity against drug-resistant microbes
    8.
    发明授权
    C-25 carbamate rifamycin derivatives with activity against drug-resistant microbes 有权
    C-25氨基甲酸酯利福霉素衍生物，具有抗药性的微生物活性

    公开(公告)号：US07250413B2

    公开(公告)日：2007-07-31

    申请号：US11114384

    申请日：2005-04-26

    申请人： Keith Combrink ,  Susan Harran ,  Daniel Denton ,  Zhenkun Ma

    发明人： Keith Combrink ,  Susan Harran ,  Daniel Denton ,  Zhenkun Ma

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

    CPC分类号： C07D498/08 ,  C07D498/18 ,  C07D519/00

    摘要： Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the current invention relate to C-25 carbamate derivatives of rifamycin having another functional group or pharmacophore covalently attached to this position through a carbamate linkage. The resulting compounds exert their antimicrobial activity through a dual-function mechanism and therefore exhibit reduced frequency of resistance.

    摘要翻译： 本发明的化合物涉及具有抗微生物活性的利福霉素衍生物，包括抗耐药微生物的活性。 更具体地，本发明的化合物涉及具有另一官能团的利福霉素的C-25氨基甲酸酯衍生物或通过氨基甲酸酯键共价连接到该位置的药效团。 所得化合物通过双功能机制发挥其抗微生物活性，因此表现出降低的抗性频率。

    Rifamycin derivatives
    10.
    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。