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    • 92. 发明授权
    • Steroid extraction process from urine sources
    • 来自尿源的类固醇提取过程
    • US08349819B2
    • 2013-01-08
    • US11055257
    • 2005-02-10
    • John LomansCarmen Leiva-paredes
    • John LomansCarmen Leiva-paredes
    • A01N45/00A61K31/56A61K35/22C07J3/00
    • A61K31/56C07J1/00
    • A process in which urine is optionally filtered to remove solid extraneous matter and optionally treated so as to reduce the phenolic content of the urine to give and the resulting fluid is then subjected to a solid extraction of the major concentration steroids content therefrom by a first suitable resin (to yield a first resin laden with major concentration steroids and a minor concentration steroid laden first liquid remainder). The minor concentration steroid liquid remainder is subjected to a solid extraction of the minor concentration steroid content therefrom by a second suitable resin (to yield a second resin laden with minor concentration steroids and a second liquid remainder). The first and second resins laden with their respective steroids are then eluted and the eluates are collected separately and optionally subjected to further purification and chromatographic separations, with each resulting separate collection being analyzed for the steroid content thereof. The separate analyzed materials are dried and stored for recombination in an appropriate manner to meet a desired profile. The ultimate product has very nearly the same steroid components and concentrations from batch to batch.
    • 其中任选地过滤尿液以去除固体外来物质并任选地处理尿液以减少尿液的酚含量并使所得流体通过第一适合的方式从其中固体提取主要浓度类固醇含量 树脂(以产生具有主要浓度类固醇的第一树脂和载有少量固体的第一液体剩余物)。 通过第二合适的树脂(稍微浓缩类固醇和第二液体余量)产生次要浓度的类固醇液体残余物从其中提取少量的类固醇含量。 然后洗脱含有它们各自类固醇的第一种和第二种树脂,分离收集洗脱液,任选进行进一步纯化和色谱分离,分析每种所得的单独收集物的类固醇含量。 将分离的分析的材料干燥并以适当的方式储存以进行重组以满足期望的分布。 最终产品具有几乎相同的类固醇成分和浓度从批次到批次。
    • 93. 发明授权
    • 17β-cyano-19-nor-androst-4-ene derivative, its use and medicaments comprising the derivative
    • 17-氰基-19-去甲 - 雄甾-4-烯衍生物,其用途和药物包含衍生物
    • US08207150B2
    • 2012-06-26
    • US12137111
    • 2008-06-11
    • Joachim KuhnkeJan HuebnerRolf BohlmannThomas FrenzelUlrich KlarFrederik MengesSven RingSteffen BordenHans-Peter MuhnKatja Prelle
    • Joachim KuhnkeJan HuebnerRolf BohlmannThomas FrenzelUlrich KlarFrederik MengesSven RingSteffen BordenHans-Peter MuhnKatja Prelle
    • A61K31/56C07J3/00
    • C07J53/008C07J41/0094C07J53/007
    • The 17β-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, in which R is hydrogen or C1-C4-alkyl, R4 is hydrogen or halogen, furthermore either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4-alkyl, C2-C3-alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together form methylene or are omitted with formation of a double bond between C6 and C7, R9, R10 are hydrogen or are omitted with formation of a double bond between C9 and C10, R15, R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4-alkyl and allyl, where at least one of the substituents R4, R6a, R6b, R7, R15, R16 and R17 is unequal to hydrogen or R6b and R7 are omitted with formation of a double bond between C6 and C7, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts.
    • 本发明的17α-氰基-19-去雄甾-4-烯衍生物具有孕激活作用。 它们具有一般化学式1,其中Z选自O,两个氢原子,NOR和NNHSO 2 R,其中R是氢或C 1 -C 4 - 烷基,R 4是氢或卤素,此外:R 6a, R6b一起形成亚甲基或1,2-乙二基或R6a为氢,R6b选自氢,甲基和羟基亚甲基,R7选自氢,C1-C4-烷基,C2-C3-烯基和 环丙基,或者:R6a是氢,R6b和R7一起形成亚甲基,或者在C6和C7之间形成双键被省略,R9,R10是氢或在C9与C10之间形成R15,R16 是氢或一起形成亚甲基,R 17选自氢,C 1 -C 4 - 烷基和烯丙基,其中至少一个取代基R4,R6a,R6b,R7,R15,R16和R17不等于氢或R6b 并且在C6和C7之间形成双键而省略R7,此外, 上升它们的溶剂合物,水合物,立体异构体,非对映异构体,对映体和盐。