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301 条记录 (耗时 0.015 秒)

    Method for determining pharmacodynamic parameters and designing a dosing regimen for a drug
    103.
    发明公开
    Method for determining pharmacodynamic parameters and designing a dosing regimen for a drug 失效
    一种用于确定药效学参数和设计给药方案的药物方法

    公开(公告)号：EP0737926A1

    公开(公告)日：1996-10-16

    申请号：EP96105625.6

    申请日：1996-04-10

    申请人： HOECHST MARION ROUSSEL, INC.

    发明人： Natarajan, Chandra

    IPC分类号： G06F17/00 ,  A61K9/00

    CPC分类号： A61K9/00

    摘要： Method for determining a particular characteristic value of an effect compartment, such as the exit rate constant, after administration of a drug to a central compartment coupled to the effect compartment. Drug concentrations in the effect compartment are ascertained as a function of the exit rate constant, and a measured effect of the drug is obtained. A hysteresis loop between the drug concentrations in the effect compartment and the measured effect is graphically formed, and the hysteresis loop is collapsed by varying the exit rate constant of the effect compartment. A pharmacodynamic model which fits the curve of the collapsed hysteresis loop is selected, and a predicted effect is obtained in accordance with the selected pharmacodynamic model and the drug concentrations in the effect compartment. An error between the predicted effect and the measured effect is calculated, and the exit rate constant of the effect compartment is then adjusted until the calculated error between the predicted effect and the measured effect is minimized, thus obtaining the exit rate constant of the effect compartment. A dosing regimen for the drug is then designed in accordance with the exit rate constant at which the calculated error is minimized.

    摘要翻译： 确定性采矿方法的效果隔室，：如出口速率常数的特定特征值，药物的给药后耦合到所述效应室的中心隔室中。 在效应室药物浓度被确定为出射速率常数的函数，和药物的测定效果被获得。 在效应室和测量的效果的药物浓度之间的磁滞回线图形形成，且磁滞回线是通过改变作用隔室的出口速率常数折叠。 符合该倒塌的磁滞回线的曲线A药效学模型选择和预测效果即可在雅舞蹈与所选择的药物动力学模型，并在效应室的药物浓度。 预测的效果和所测量的效应之间的误差进行计算，然后被调节的效果隔室的出射率恒定，直到预测的效果和所测量的效应之间的计算误差最小化，由此获得的效果隔间的出口速率常数 ， 对于药物给药方案，然后在与其中最小化计算的误差，出口速率常数雅舞蹈设计。

    Heterogeneous synthesis of azepinones from esters
    106.
    发明公开
    Heterogeneous synthesis of azepinones from esters 失效
    异源合成on on

    公开(公告)号：EP0415384A2

    公开(公告)日：1991-03-06

    申请号：EP90116565.4

    申请日：1990-08-29

    申请人： HOECHST MARION ROUSSEL, INC.

    发明人： Martin, Daniel E.

    IPC分类号： C07D281/10 ,  C07B43/06

    CPC分类号： C07D281/10

    摘要： An amino-acid ester compound can be cyclized into a cyclic amido-carbonyl compound by contacting the amino-acid ester compound in a liquid medium with a heterogeneous acidic ion-exchange substance. For example, 2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)propionic acid, methyl ester, threo form, can be cyclized in an aqueous mixture into cis-2-(4-methoxyphenyl)-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one by employing a sulfonated polystyrene-divinylbenzene ion-exchange resin in its acid form, e.g., Dowex 50X4-400, at yields exceeding 85 percent of theory, and the product can be used to make diltiazem hydrochloride.

    摘要翻译： 氨基酸酯化合物可通过使液体介质中的氨基酸酯化合物与异质酸性离子交换物质接触而环化成环状酰胺基 - 羰基化合物。 例如，可以将2-羟基-3-（2-氨基苯硫基）-3-（4-甲氧基苯基）丙酸甲酯，苏式形式在含水混合物中环化为顺式-2-（4-甲氧基苯基）-3 - 羟基-2,3-二氢-1,5-苯并硫氮杂-4（5H） - 酮，其采用其酸形式的磺化聚苯乙烯 - 二乙烯基苯离子交换树脂，例如Dowex 50X4-400，产率超过85％ 理论上，该产品可用于制备盐酸地尔硫卓。