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    Oxazolidinone containing dimer compounds, compositions and methods to make and use
    4.
    发明授权
    Oxazolidinone containing dimer compounds, compositions and methods to make and use 有权
    含恶唑烷酮的二聚体化合物，组合物和制备和使用的方法

    公开(公告)号：US08580767B2

    公开(公告)日：2013-11-12

    申请号：US12787293

    申请日：2010-05-25

    申请人： D. Keith Hester, II ,  Robert J. Duguid ,  John Finn

    发明人： D. Keith Hester, II ,  Robert J. Duguid ,  John Finn

    IPC分类号： A01N57/00 ,  A61K31/675 ,  C07F9/06 ,  C07F9/28

    CPC分类号： C07F9/65583 ,  A61K31/675

    摘要： Dosage forms or pharmaceutical compositions comprise a compound having the structure of Formula IV: wherein n is a non-negative integer; wherein each Z is an oxazolidinone-containing moiety having antibiotic activity in vivo upon cleaving, wherein M is independently OR1 or NR1R2; wherein R1 and R2 are independently selected from the group consisting of H, an optionally-substituted hydrocarbyl residue or a pharmaceutically acceptable cation; wherein the compound in the dosage form or a pharmaceutical composition is present in an amount effective for treating or preventing an antibacterial infection in a mammalian subject. Methods of preparing and using these dosage forms or pharmaceutical compositions are also disclosed.

    摘要翻译： 剂型或药物组合物包含具有式IV结构的化合物：其中n是非负整数; 其中每个Z是在裂解时在体内具有抗生素活性的含恶唑烷酮的部分，其中M独立地为OR 1或NR 1 R 2; 其中R1和R2独立地选自H，任选取代的烃基残基或药学上可接受的阳离子; 其中剂型中的化合物或药物组合物以有效治疗或预防哺乳动物受试者的抗菌感染的量存在。 还公开了制备和使用这些剂型或药物组合物的方法。

    CRYSTALLINE FORM OF R)-3-(4-(2-(2-METHYLTETRAZOL-5-YL)PYRIDIN- 5-YL)-3-FLUOROPHENYL)-5-HYDROXYMETHYL OXAZOLIDIN-2-ONE DIHYDROGEN PHOSPHATE
    8.
    发明申请
    CRYSTALLINE FORM OF R)-3-(4-(2-(2-METHYLTETRAZOL-5-YL)PYRIDIN- 5-YL)-3-FLUOROPHENYL)-5-HYDROXYMETHYL OXAZOLIDIN-2-ONE DIHYDROGEN PHOSPHATE 审中-公开
    R）-3-（4-（2-（2-甲基戊酰基-5-YL）吡啶-5-YL）-3-氟代戊烯）-5-羟基甲基氧化吡啶-2-酮二氢磷酸酯的晶体形式

    公开(公告)号：US20130310343A1

    公开(公告)日：2013-11-21

    申请号：US13867951

    申请日：2013-04-22

    申请人： Trius Therapeutics, Inc.

    发明人： Katharina Reichenbacher ,  Robert J. Duguid ,  Jacqueline A. Ware ,  Douglas Phillipson

    IPC分类号： C07F9/06

    CPC分类号： C07F9/65583 ,  A61K31/675 ,  C07D413/14 ,  C07F9/06

    摘要： A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.

    摘要翻译： 结晶形式的（R）-3-（4-（2-（2-甲基四唑-5-基）吡啶-5-基）-3-氟苯基）-5-羟基甲基恶唑烷-2-酮磷酸二氢盐，方法 使晶体形式和包含结晶形式的药物组合物是有用的抗生素。 此外，本发明的衍生物可以对各种人和动物病原体（包括葡萄球菌，肠球菌和链球菌）等革兰阳性菌，拟杆菌和梭菌等厌氧微生物和结核分枝杆菌等耐酸微生物产生有效的抗菌活性 和鸟分枝杆菌。 因此，包含结晶形式的组合物可以用于抗生素中。

    Method for Identifying Drug-Sensitizing Antisense DNA Fragments and Use Thereof
    10.
    发明申请
    Method for Identifying Drug-Sensitizing Antisense DNA Fragments and Use Thereof 审中-公开
    鉴定药物敏感反义DNA片段及其用途的方法

    公开(公告)号：US20110143359A1

    公开(公告)日：2011-06-16

    申请号：US13033128

    申请日：2011-02-23

    申请人： Robert Haselbeck ,  Mark Hilgers ,  Karen Shaw ,  Vickie Brown-Driver ,  Kedar GC ,  John M. Finn ,  Mark Stidham

    发明人： Robert Haselbeck ,  Mark Hilgers ,  Karen Shaw ,  Vickie Brown-Driver ,  Kedar GC ,  John M. Finn ,  Mark Stidham

    IPC分类号： C12Q1/68

    CPC分类号： C12N15/111 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2320/11 ,  C12N2330/30 ,  C12Y101/01158 ,  C12Y105/01003 ,  C12Y205/01031 ,  C12Y601/0101

    摘要： The invention provides a method for generating and selecting drug-sensitizing antisense DNA fragments. In one embodiment, the method includes identifying a gene of interest using knowledge of bacterial physiology, biochemistry, genetics, genomics, and other means. The method includes PCR amplification of a gene of interest using genomic DNA as a template; fragmentation of the DNA by sonication or other means; selecting DNA fragments no longer than 400 base pairs; ligating the DNA fragments into a suitable expression plasmid with a selectable marker; transforming the plasmids containing the DNA fragments into the organism from which the gene of interest originated; and selecting clones from transformed cells that show a phenotypic difference of the clone grown in the presence of the inducer relative to the phenotype in the absence of inducer.

    摘要翻译： 本发明提供了生产和选择药物敏化反义DNA片段的方法。 在一个实施方案中，该方法包括使用细菌生理学，生物化学，遗传学，基因组学和其他方法的知识来鉴定感兴趣的基因。 该方法包括使用基因组DNA作为模板对感兴趣的基因进行PCR扩增; 通过超声处理或其他方法破碎DNA; 选择不超过400个碱基对的DNA片段; 将DNA片段连接到具有选择性标记的合适的表达质粒中; 将含有DNA片段的质粒转化为目标基因来源的生物体; 并选择来自转化细胞的克隆，其在不存在诱导物的情况下显示在诱导物存在下生长的克隆相对于表型的表型差异。