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    Cephalosporin derviatives
    4.
    发明授权
    Cephalosporin derviatives 失效
    头孢菌素衍生物

    公开(公告)号：US5620969A

    公开(公告)日：1997-04-15

    申请号：US427778

    申请日：1995-04-25

    申请人： Joanne J. Bronson ,  Stanley V. D'Andrea ,  Shelley E. Hoeft ,  John D. Matiskella ,  Peter F. Misco, Jr. ,  Bing Y. Luh ,  Dane M. Springer ,  Yasutsugu Ueda ,  John A. Wichtowski

    发明人： Joanne J. Bronson ,  Stanley V. D'Andrea ,  Shelley E. Hoeft ,  John D. Matiskella ,  Peter F. Misco, Jr. ,  Bing Y. Luh ,  Dane M. Springer ,  Yasutsugu Ueda ,  John A. Wichtowski

    IPC分类号： C07D501/00 ,  C07D501/36 ,  A61K31/545

    CPC分类号： C07D501/00

    摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).

    摘要翻译： 由通式表示的新型头孢烯衍生物，其中酰基取代基是下式的基团：其中Ar是亲脂性任选取代的苯基，萘基或吡啶基; R1表示杂环氨基酸的残基或被羧基和式-NR9R10或基团取代的C2-C10烷基，其中R9和R10各自独立地为氢或C1-C6烷基， 所述C 2 -C 10烷基任选被一个或多个氮原子或羰基中断，并且R 2和R 3各自独立地为氢，烷基或氨基烷基为革兰氏阳性抗菌剂，特别可用于治疗由甲氧西林抗性引起的疾病 金黄色葡萄球菌（以下也称为MRSA或耐甲氧西林金黄色葡萄球菌）。

    Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
    7.
    发明授权
    Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives 有权
    取代的氮杂脱氧乙酸哌嗪衍生物的组成和抗病毒活性

    公开(公告)号：US07354924B2

    公开(公告)日：2008-04-08

    申请号：US10969675

    申请日：2004-10-20

    申请人： Tao Wang ,  Zhongxing Zhang ,  Nicholas A. Meanwell ,  John F. Kadow ,  Zhiwei Yin ,  Qiufen May Xue ,  Alicia Regueiro-Ren ,  John D. Matiskella ,  Yasutsugu Ueda

    发明人： Tao Wang ,  Zhongxing Zhang ,  Nicholas A. Meanwell ,  John F. Kadow ,  Zhiwei Yin ,  Qiufen May Xue ,  Alicia Regueiro-Ren ,  John D. Matiskella ,  Yasutsugu Ueda

    IPC分类号： A61K31/496 ,  C07D487/02 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506

    CPC分类号： C07D471/04 ,  A61K31/496 ,  A61K45/06 ,  C07D491/048

    摘要： This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. Compound I is wherein: Q is selected from the group consisting of: m is 1 or 2; —W— is A is selected from the group consisting of C1-6alkoxy, aryl and heteroaryl; in which said aryl is phenyl or napthyl; said heteroaryl is selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, triazinyl, furanyl, thienyl, pyrrolyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, quinolinyl, isoquinolinyl, benzofuranyl, benzothienyl, benzoimidazolyl and benzothiazolyl; and said aryl or heteroaryl is optionally substituted with one or two of the same or different members selected from the group consisting of amino, nitro, cyano, hydroxy, C1-6alkoxy, —C(O)NH2; and C1-6alkyl, —NHC(O)CH3, halogen and trifluoromethyl.

    摘要翻译： 本发明提供具有药物和生物影响性质的化合物I，其药物组合物和使用方法。 特别地，本发明涉及氮杂吲哚乙酰基哌嗪衍生物。 这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药，抗感染剂，免疫调节剂或HIV进入抑制剂组合使用。 更具体地说，本发明涉及艾滋病毒和艾滋病的治疗。 化合物I是其中：Q选自：m是1或2; -W-是A选自C 1-6烷氧基，芳基和杂芳基; 其中所述芳基是苯基或萘基; 吡啶基，吡嗪基，咪唑基，噻唑基，异噻唑基，恶唑基，异恶唑基，喹啉基，异喹啉基，苯并呋喃基，苯并噻吩基，苯并咪唑基和苯并噻唑基; 并且所述芳基或杂芳基任选被一个或两个相同或不同的选自氨基，硝基，氰基，羟基，C 1-6烷氧基，-C（O） NH 2; 和C 1-6烷基，-NHC（O）CH 3，卤素和三氟甲基。