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    • 61. 发明授权
    • Substrates for beta-lactamase and uses thereof
    • β-内酰胺酶底物及其用途
    • US08071761B2
    • 2011-12-06
    • US11606642
    • 2006-11-29
    • Roger Y. TsienGregor Zlokarnik
    • Roger Y. TsienGregor Zlokarnik
    • C07D501/14
    • C07D501/36C07D501/00C07D505/00C07D519/00C12N9/86C12N15/85C12N2800/90C12N2830/002C12P17/184C12P17/188C12P35/00C12Q1/18C12Q1/34C12Q1/6897C12Q2334/00G01N2333/986G01N2415/00Y10S435/805
    • 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.
    • 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。
    • 69. 发明申请
    • Process for the manufacture of cefpodoxime proxetil
    • 头孢泊肟酯的制备方法
    • US20060149055A1
    • 2006-07-06
    • US10541473
    • 2003-01-06
    • Milind GharpureSanjay DeshmukhRajendra Mahale
    • Milind GharpureSanjay DeshmukhRajendra Mahale
    • C07D501/14
    • C07D501/60C07D501/04C07D501/12
    • A process for obtaining cefpodoxime proxetil of formula (I), of high purity conforming to pharmacopoeial specifications is disclosed. The process comprises addition of a solution of methanesulfonic acid in water to a solution of impure cefpodoxime proxetil of formula (I) in an organic solvent to form the corresponding cefpodoxime proxetil methanesulfonate of formula (II1), followed by addition of a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II1) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II1) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6, or, addition of impure cefpodoxime proxetil of formula (I) to a solution of methanesulfonic acid in water to form the corresponding solution of cefpodoxime proxetil methanesulfonate of formula (II1) in water, followed by sequential addition of a first organic solvent and a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II1) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II1) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6.
    • 公开了一种获得符合药典规格的高纯度的式(I)头孢泊肟酯的方法。 该方法包括将甲磺酸水溶液加入到有机溶剂中的式(I)不纯的头孢泊肟酯的溶液中以形成相应的式(II)的头孢泊肟甲磺酸盐,随后 通过加入共溶剂和含有非对映异构体比率为(R / R + S)为0.5至0.6的式(II-1)的头孢泊肟甲基磺酸酯的水相的分离,随后中和 具有碱的甲磺酸盐(II-1),得到不含杂质并且(R / R + S)的非对映异构体比率在0.5至0.6之间的头孢泊肟酯(I),或加入不纯 式(I)的头孢泊肟酯与甲磺酸在水中的溶液形成相应的式(II 1)的头孢泊肟甲磺酸盐溶液在水中的溶液,然后依次加入第一有机溶剂和 共溶剂和水相c的分离 使用具有(R / R + S)的非对映异构体比率为0.5至0.6的随后的甲磺酸盐中和的式(II-1)的头孢泊肟甲磺酸酯(II 1) ),得到不含杂质的头孢泊肟酯(I)和(R / R + S)的非对映异构体比例在0.5至0.6之间。