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    CEFDINIR AND CEFIXIME FORMULATIONS AND USES THEREOF
    1.
    发明申请
    CEFDINIR AND CEFIXIME FORMULATIONS AND USES THEREOF 审中-公开
    CEFDINIR和CEFIXIME制剂及其用途

    公开(公告)号：US20140079647A1

    公开(公告)日：2014-03-20

    申请号：US14089355

    申请日：2013-11-25

    Applicant: Mahmut BILGIC

    Inventor： Mahmut BILGIC

    IPC: C07D501/00 ,  A61K9/16 ,  C07D501/04

    CPC classification number: C07D501/00 ,  A61K9/0007 ,  A61K9/0095 ,  A61K9/1617 ,  A61K9/1629 ,  A61K9/1694 ,  A61K9/2013 ,  A61K9/2022 ,  A61K31/546 ,  C07D501/04 ,  C07D501/16

    Abstract: The invention features pharmaceutically acceptable salts of cefdinir, including primary, secondary, and tertiary amine salts of cefdinir, and preparation methods, and pharmaceutical compositions including cefdinir. The invention also features water dispersible pharmaceutical dosage forms including cefdinir as active agent and methods for preparing the dosages. The invention also features tablet forms of cefixime characterized in that the tablets are in effervescent form. The invention also features the process for preparing effervescent tablet forms with cefdinir as active agents and pharmaceutical formulations obtained by the process.

    Abstract translation: 本发明的特征在于头孢地尼的药学上可接受的盐，包括头孢地尼的伯胺，仲胺和叔胺盐及其制备方法以及包括头孢地尼的药物组合物。 本发明还具有水分散性药物剂型，包括头孢地尼作为活性剂和制备剂量的方法。 本发明还具有头孢克肟片形式，其特征在于片剂为泡腾形式。 本发明还具有以头孢地尼作为活性剂和通过该方法获得的药物制剂来制备泡腾片形式的方法。

    Cefdinir and cefixime formulations and uses thereof
    2.
    发明授权
    Cefdinir and cefixime formulations and uses thereof 有权
    头孢地尼和头孢克肟制剂及其用途

    公开(公告)号：US08614315B2

    公开(公告)日：2013-12-24

    申请号：US13532120

    申请日：2012-06-25

    Applicant: Mahmut Bilgic

    Inventor： Mahmut Bilgic

    IPC: C07D501/00

    CPC classification number: C07D501/00 ,  A61K9/0007 ,  A61K9/0095 ,  A61K9/1617 ,  A61K9/1629 ,  A61K9/1694 ,  A61K9/2013 ,  A61K9/2022 ,  A61K31/546 ,  C07D501/04 ,  C07D501/16

    Abstract: The invention features pharmaceutically acceptable salts of cefdinir, including primary, secondary, and tertiary amine salts of cefdinir, and preparation methods, and pharmaceutical compositions including cefdinir. The invention also features water dispersible pharmaceutical dosage forms including cefdinir as active agent and methods for preparing the dosages. The invention also features tablet forms of cefixime characterized in that the tablets are in effervescent form. The invention also features the process for preparing effervescent tablet forms with cefdinir as active agents and pharmaceutical formulations obtained by the process.

    Abstract translation: 本发明的特征在于头孢地尼的药学上可接受的盐，包括头孢地尼的伯胺，仲胺和叔胺盐及其制备方法以及包括头孢地尼的药物组合物。 本发明还具有水分散性药物剂型，包括头孢地尼作为活性剂和制备剂量的方法。 本发明还具有头孢克肟片形式，其特征在于片剂为泡腾形式。 本发明还具有以头孢地尼作为活性剂和通过该方法获得的药物制剂来制备泡腾片形式的方法。

    Enzyme substrate comprising a functional dye and associated technology and methods
    3.
    发明授权
    Enzyme substrate comprising a functional dye and associated technology and methods 有权
    酶底物包含功能染料及相关技术和方法

    公开(公告)号：US08586325B2

    公开(公告)日：2013-11-19

    申请号：US13891406

    申请日：2013-05-10

    Applicant: Fei Mao ,  Hui Cen

    Inventor： Fei Mao ,  Hui Cen

    IPC: C12Q1/37 ,  A61K38/14 ,  C07D279/08

    CPC classification number: C12N9/96 ,  C07D263/60 ,  C07D417/06 ,  C07D501/00 ,  C07K7/06 ,  C12Q1/37 ,  C12Q1/48 ,  C12Q1/485 ,  G01N21/6486 ,  G01N33/582

    Abstract: Enzyme substrates and associated technology of the present invention are provided. An enzyme substrate of the invention may comprise a biologically functional fluorescent dye and an enzyme-specific substrate moiety attached in such a way that the functionality of the functional dye is diminished. An enzymatic reaction may cleave at least a portion of the substrate moiety from the enzyme substrate to provide a more functional product dye. This product dye may be nonfluorescent or weakly fluorescent, in general, and relatively fluorescent, in a particular condition, such as when bound to a partner biological molecule or an assembly of partner biological molecules. An enzyme substrate of the present invention may thus be useful in fluorescence detection, and/or in any of a variety of useful applications, such as the detection of enzymatic activity in a cell-free system or in a living cell, the screening of drugs, or the diagnosis of disease.

    Abstract translation: 提供了本发明的酶底物和相关技术。 本发明的酶底物可以包含生物功能性荧光染料和酶特异性底物部分，其功能性染料的官能度减弱。 酶反应可以从酶底物切割底物部分的至少一部分以提供更多功能的产物染料。 通常，在特定条件下，例如当结合到伴侣生物分子或伴侣生物分子的组合时，该产物染料通常可以是非荧光的或弱荧光的，并且是相对荧光的。 因此，本发明的酶底物可用于荧光检测和/或各种有用应用中的任何一种，例如在无细胞系统或活细胞中检测酶活性，筛选药物 ，或疾病的诊断。

    Enzyme substrate comprising a functional dye and associated technology and methods
    6.
    发明授权
    Enzyme substrate comprising a functional dye and associated technology and methods 有权
    酶底物包含功能染料及相关技术和方法

    公开(公告)号：US08092784B2

    公开(公告)日：2012-01-10

    申请号：US12095322

    申请日：2006-11-21

    Applicant: Fei Mao ,  Hui Cen ,  Wai-yee Leung

    Inventor： Fei Mao ,  Hui Cen ,  Wai-yee Leung

    IPC: A61B10/00 ,  C12Q1/68

    CPC classification number: C12N9/96 ,  C07D263/60 ,  C07D417/06 ,  C07D501/00 ,  C07K7/06 ,  C12Q1/37 ,  C12Q1/48 ,  C12Q1/485 ,  G01N21/6486 ,  G01N33/582

    Abstract: Enzyme substrates and associated technology of the present invention are provided. An enzyme substrate of the invention may comprise a biologically functional fluorescent dye and an enzyme-specific substrate moiety attached in such a way that the functionality of the functional dye is diminished. An enzymatic reaction may cleave at least a portion of the substrate moiety from the enzyme substrate to provide a more functional product dye. This product dye may be nonfluorescent or weakly fluorescent, in general, and relatively fluorescent, in a particular condition, such as when bound to a partner biological molecule or an assembly of partner biological molecules. An enzyme substrate of the present invention may thus be useful in fluorescence detection, and/or in any of a variety of useful applications, such as the detection of enzymatic activity in a cell-free system or in a living cell, the screening of drugs, or the diagnosis of disease.

    Abstract translation: 提供了本发明的酶底物和相关技术。 本发明的酶底物可以包含生物功能性荧光染料和酶特异性底物部分，其功能性染料的官能度减弱。 酶反应可以从酶底物切割底物部分的至少一部分以提供更多功能的产物染料。 通常，在特定条件下，例如当结合到伴侣生物分子或伴侣生物分子的组合时，该产物染料通常可以是非荧光的或弱荧光的，并且是相对荧光的。 因此，本发明的酶底物可用于荧光检测和/或各种有用应用中的任何一种，例如在无细胞系统或活细胞中检测酶活性，筛选药物 ，或疾病的诊断。

    Substrates for beta-lactamase and uses thereof
    7.
    发明授权
    Substrates for beta-lactamase and uses thereof 有权
    β-内酰胺酶底物及其用途

    公开(公告)号：US08071761B2

    公开(公告)日：2011-12-06

    申请号：US11606642

    申请日：2006-11-29

    Applicant: Roger Y. Tsien ,  Gregor Zlokarnik

    Inventor： Roger Y. Tsien ,  Gregor Zlokarnik

    IPC: C07D501/14

    CPC classification number: C07D501/36 ,  C07D501/00 ,  C07D505/00 ,  C07D519/00 ,  C12N9/86 ,  C12N15/85 ,  C12N2800/90 ,  C12N2830/002 ,  C12P17/184 ,  C12P17/188 ,  C12P35/00 ,  C12Q1/18 ,  C12Q1/34 ,  C12Q1/6897 ,  C12Q2334/00 ,  G01N2333/986 ,  G01N2415/00 ,  Y10S435/805

    Abstract: Substrates for β-lactamase of the general formula I in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R′ is selected from the group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH2)nOH, in which n is 0 or an integer from 1 to 5; R″ is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, —CHR2OCO(CH2)nCH3, —CHR2OCOC (CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z′ and Z″ are linkers for the fluorescent donor and quencher moieties. Methods of assaying β-lactamase activity and monitoring expression in systems using β-lactamase as a reporter gene also are disclosed.

    Abstract translation: X和Y中的一个是荧光供体部分，另一个是猝灭剂（其可以或不再发射）的通式I的β-内酰胺酶底物; R'选自H，低级（即1至约5个碳原子的烷基）和（CH 2）nOH，其中n为0或1至5的整数; -CH 2 COO（CH 2）n CH 3，-CHR 2 OCOC（CH 3）3，酰基硫代甲基，酰氧基-α-苄基，δ-丁基内酰胺，甲氧基羰氧基甲基，苯基，甲基亚磺酰基甲基， β-吗啉基乙基，二烷基氨基乙基，酰氧基烷基，二烷基氨基羰氧基甲基和脂族基，其中R2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; 和Z'和Z“是荧光供体和猝灭剂部分的接头。 公开了使用β-内酰胺酶作为报道基因的系统中测定β-内酰胺酶活性和监​​测表达的方法。

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