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    Broad spectrum beta-lactamase inhibitors
    1.
    发明授权
    Broad spectrum beta-lactamase inhibitors 有权

    公开(公告)号：US10239890B2

    公开(公告)日：2019-03-26

    申请号：US15991315

    申请日：2018-05-29

    申请人： Gladius Pharmaceuticals Corporation

    发明人： Larry Sutton ,  Sophia Yu

    IPC分类号： C07D501/22 ,  C07D501/24 ,  C07D501/60 ,  A01N43/90

    摘要： Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

    Broad Spectrum Beta-Lactamase Inhibitors
    2.
    发明申请
    Broad Spectrum Beta-Lactamase Inhibitors 审中-公开

    公开(公告)号：US20180273549A1

    公开(公告)日：2018-09-27

    申请号：US15991315

    申请日：2018-05-29

    申请人： Gladius Pharmaceuticals Corporation

    发明人： Larry SUTTON ,  Sophia YU

    IPC分类号： C07D501/24 ,  C07D501/60 ,  C07D501/22 ,  A01N43/90

    CPC分类号： C07D501/24 ,  A01N43/90 ,  C07D501/22 ,  C07D501/60

    摘要： Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

    Broad spectrum beta-lactamase inhibitors
    4.
    发明授权
    Broad spectrum beta-lactamase inhibitors 有权
    广谱β-内酰胺酶抑制剂

    公开(公告)号：US09453032B2

    公开(公告)日：2016-09-27

    申请号：US14491806

    申请日：2014-09-19

    申请人： GLADIUS PHARMACEUTICALS CORPORATION

    发明人： Larry Sutton ,  Sophia Yu

    IPC分类号： C07D501/22 ,  C07D501/24 ,  C07D501/60 ,  A01N43/90 ,  A61K31/00

    CPC分类号： C07D501/24 ,  A01N43/90 ,  C07D501/22 ,  C07D501/60

    摘要： Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

    摘要翻译： 广谱β-内酰胺酶抑制剂。 除了β-内酰胺酶抑制之外，某些抑制剂还表现出有效的抗生素活性。 本发明的化合物被设计成使得在β-内酰胺环切割时产生可以使β-内酰胺酶失活的活性部分。 还提供了制备β-内酰胺酶抑制剂和表现出这种抑制作用的β-内酰胺抗生素的方法。 另外提供了用于治疗或预防细菌感染的药物组合物和治疗这种感染的方法。

    Process for the crystallisation of cefadroxil monohydrate
    5.
    发明授权
    Process for the crystallisation of cefadroxil monohydrate 有权
    头孢羟氨苄一水合物结晶方法

    公开(公告)号：US08420806B2

    公开(公告)日：2013-04-16

    申请号：US12300046

    申请日：2007-05-11

    申请人： Carlos Enrique Lenhard ,  Harold Monro Moody ,  Theodorus Johannes Godfried Maria Van Dooren

    发明人： Carlos Enrique Lenhard ,  Harold Monro Moody ,  Theodorus Johannes Godfried Maria Van Dooren

    IPC分类号： C07D501/22 ,  A61K31/546

    CPC分类号： C07D501/20 ,  C07D501/12 ,  C07D501/22

    摘要： The present invention relates to a process for the preparation of cefadroxil in crystal form, comprising a) adding an aqueous solution of cefadroxil to a crystallization vessel and a titrant to keep a pH in the crystallization vessel of between 7 to 9; and b) lowering the pH in the crystallization vessel to a value of between 5 and 6.5 to obtain a suspension of the β-lactam compound in crystal form. The invention further relates to cefadroxil in crystal form obtainable by the process according to the present invention. The invention also relates to cefadroxil in crystal form with a CIE b value of below 12 when stored at a temperature of 25° C. for at least 1 month.

    摘要翻译： 本发明涉及一种晶体形式的头孢羟氨苄的制备方法，其包括：a）向结晶容器中加入头孢羟氨苄水溶液，滴定剂将结晶容器中的pH值保持在7-9之间; 和b）将结晶容器中的pH降低至5至6.5的值，以获得晶体形式的β-内酰胺化合物的悬浮液。 本发明还涉及通过本发明的方法获得的晶体形式的头孢羟氨苄。 本发明还涉及当在25℃的温度下储存至少1个月时，CIE b值低于12的晶体形式的头孢羟氨苄。

    Cefdinir intermediate
    8.
    发明授权
    Cefdinir intermediate 失效
    头孢地尼中间体

    公开(公告)号：US07250508B2

    公开(公告)日：2007-07-31

    申请号：US10524397

    申请日：2003-08-12

    申请人： Peter Kremminger ,  Siegfried Wolf ,  Johannes Ludescher

    发明人： Peter Kremminger ,  Siegfried Wolf ,  Johannes Ludescher

    IPC分类号： C07D501/22 ,  C07D417/12

    CPC分类号： C07D501/00

    摘要： 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula I in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula I in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.

    摘要翻译： 具有结晶盐形式的式I的7- [2-（2-氨基噻唑-4-基）-2-（甲基羰氧基亚氨基）乙酰氨基] -3-乙烯基头孢烯-4-羧酸及其用途， 在制备纯头孢地尼。 在另一方面，本发明涉及任选呈结晶形式的盐形式的式I化合物，其中盐选自磷酸盐，磷酸氢盐，甲磺酸盐，甲苯磺酸盐，硫酸盐，硫酸氢盐和氨基磺酸盐。

    Compounds and method for preparing 3-methylcephams
    9.
    发明授权
    Compounds and method for preparing 3-methylcephams 失效
    化合物和制备3-甲基脑炎的方法

    公开(公告)号：US06908996B2

    公开(公告)日：2005-06-21

    申请号：US10706683

    申请日：2003-11-12

    申请人： Robin D. G. Cooper ,  Anthony G. M. Barrett

    发明人： Robin D. G. Cooper ,  Anthony G. M. Barrett

    IPC分类号： C07D205/095 ,  C07D403/04 ,  C07D501/00 ,  C07D501/08 ,  C07D501/14 ,  C07D501/22 ,  C07D501/24 ,  C07D401/04 ,  C07D407/12 ,  C07D409/12

    CPC分类号： C07D403/04 ,  C07D205/095 ,  C07D501/00 ,  Y02P20/55

    摘要： The present invention relates to novel intermediates for the preparation of 3-methylenecephams of the formula IIA. wherein: R is a carboxylic acid protecting group; R1 is a group of the formula; R10 is C1-C6 alkyl, C1-C6 polyfluoroalkyl, C3-C6 cycloalkyl, adamantyl, phenyl, substituted phenyl, phenyl(C1-C3 alkyl), diphenylmethyl, or substituted phenyl(C1-C3 alkyl), or a group of the formula Z is solid polymer support; and Z1 is one or two groups independently selected from the group consisting of hydrogen, halo, hydroxy, protected hydroxy, nitro, cyano, trifluoromethyl, C1-C4 alkyl, and C1-C4 alkoxy.

    摘要翻译： 本发明涉及用于制备式IIA的3-亚甲基头孢的新型中间体。 其中：R是羧酸保护基; R 1是下式的基团： R 10是C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 多氟烷基，C 3 -C 6环烷基，金刚烷基，苯基，取代的苯基，苯基（C 1 -C 3 - 烷基），二苯基甲基或取代的苯基（C 1 -C 3烷基）或式Z的基团是固体聚合物载体; 和Z 1是独立地选自氢，卤素，羟基，保护的羟基，硝基，氰基，三氟甲基，C 1 -C 3的一个或两个基团 C 1-4烷基和C 1 -C 4烷氧基。