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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
    9.
    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 有权
    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：US20100227839A1

    公开(公告)日：2010-09-09

    申请号：US12699864

    申请日：2010-02-03

    申请人： Katharina Reichenbächer ,  Robert J. Duguid ,  Jacqueline A. Simson ,  Douglas Phillipson

    发明人： Katharina Reichenbächer ,  Robert J. Duguid ,  Jacqueline A. Simson ,  Douglas Phillipson

    IPC分类号： A61K31/675 ,  C07D413/14 ,  A61P31/04

    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， 制备结晶形式的方法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相对于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菌，耐结核菌如结核分枝杆菌 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。

    CRYSTALLINE FORM OF R)-3-(4-(2-(2-METHYLTETRAZOL-5-YL)PYRIDIN- 5-YL)-3-FLUOROPHENYL)-5-HYDROXYMETHYL OXAZOLIDIN-2-ONE DIHYDROGEN PHOSPHATE
    10.
    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。