DIPEPTIDE-BASED PRODRUG LINKERS FOR AROMATIC AMINE-CONTAINING DRUGS
    61.
    发明申请
    DIPEPTIDE-BASED PRODRUG LINKERS FOR AROMATIC AMINE-CONTAINING DRUGS 审中-公开
    用于含芳香胺的药物的基于代谢物的原料连接物

    公开(公告)号:US20130030359A1

    公开(公告)日:2013-01-31

    申请号:US13574157

    申请日:2011-01-21

    IPC分类号: A61K38/05 A61M5/31 C07C237/04

    摘要: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.

    摘要翻译: 本发明涉及其前体药物或其药学上可接受的盐,其包含药物接头缀合物D-L,其中D是含有芳族胺基团的生物活性部分通过含二肽的接头缀合至一种或多种聚合物载体。 这种载体连接的前药实现具有治疗有用的半衰期的药物释放。 本发明还涉及包含所述前体药物及其用作药物的药物组合物。

    Process and apparatus for continuously synthesizing alkoxypolysiloxanes
    64.
    发明授权
    Process and apparatus for continuously synthesizing alkoxypolysiloxanes 失效
    用于连续合成烷氧基聚硅氧烷的方法和设备

    公开(公告)号:US4609752A

    公开(公告)日:1986-09-02

    申请号:US752937

    申请日:1985-07-08

    摘要: A continuous process for the preparation of alkoxypolysiloxane in which silane or a silane mixture and a mixture of hydrogen chloride-containing alcohol and water is fed continuously into the lower region of preferably cylindrical stirred reactor, the reaction product formed together with excess hydrogen chloride-containing alcohol is drawn off continuously after residence time of 30 to 180 minutes at the upper end of the reactor and the undissolved, gaseous portion of hydrogen chloride is carried off at the head of the reactor, the temperature of the reaction mixture or the reaction product, as it flows through the reactor, being raised from a range of -17.degree. to +30.degree. C. to range of +30.degree. to +80.degree. C., the temperature gradient having to be at least 10.degree. C., and the excess alcohol and dissolved hydrogen chloride being removed outside of the reactor in a known manner from the reaction product formed, and the hydrogen chloride-containing alcohol obtained while working up to reaction product being recycled to the reactor. The invention furthermore relates to an apparatus which is particularly suitable for implementing the process.

    摘要翻译: 制备其中将硅烷或硅烷混合物和含氯化氢的醇和水的混合物的烷氧基聚硅氧烷的连续方法连续进料到优选圆柱形搅拌反应器的下部区域中,将反应产物与过量的含氯化氢 在反应器上端的停留时间为30至180分钟后连续抽出醇,并且在反应器的头部,反应混合物或反应产物的温度下将氯化氢的未溶解气态部分, 当其流过反应器时,从-17°至+ 30℃的范围升高至+ 30℃至+ 80℃的范围,温度梯度必须至少为10℃,并且 过量的醇和溶解的氯化氢以已知的方式从所形成的反应产物中除去反应器外部,并且在加工反应时获得的含氯化氢的醇 离子产物被再循环到反应器中。 本发明还涉及一种特别适用于实施该方法的装置。

    Process for the preparation of heat-curable silicone resins usable
especially as electrical insulating resins
    65.
    发明授权
    Process for the preparation of heat-curable silicone resins usable especially as electrical insulating resins 失效
    制备可用作电绝缘树脂的可热固化的有机硅树脂的方法

    公开(公告)号:US4408031A

    公开(公告)日:1983-10-04

    申请号:US343185

    申请日:1982-01-27

    摘要: The invention relates to a process for the preparation of heat-curable resins, usable especially as electrically insulating resins, by the reaction of alkoxy siloxanes of the formula ##STR1## in which OR.sup.1 represents an alkoxy group of primary or secondary aliphatic alcohols with 1 to 4 carbon atoms,R.sup.2 represents an alkyl or a phenyl group,a has a value of 1.0 to 1.5,b has a value of 0.1 to 1.0; witha mixture of low molecular weight, multihydric alcohols consisting of(a) 25 to 95 mole percent of neopentylglycol hydroxypivalate, and(b) 75 to 5 mole percent of a low molecular weight, at least trihydric alcoholat temperatures of 80.degree. to 200.degree. C. The resins thus prepared can be utilized advantageously for the insulation of generators, transformers and the like. They possess high elasticity and excellent adhesion.

    摘要翻译: 本发明涉及一种制备可热固化树脂的方法,特别是电绝缘树脂,通过式“IMAGE”的烷氧基硅氧烷的反应,其中OR 1表示伯或仲脂族醇的烷氧基,其中1至 4个碳原子,R 2表示烷基或苯基,a的值为1.0〜1.5,b为0.1〜1.0的值。 与(a)25至95摩尔%的新戊二醇羟基新戊酸酯和(b)75至5摩尔%的低分子量,至少三元醇在80至200℃的温度下混合的低分子量多元醇 因此制备的树脂可有利地用于发电机,变压器等的绝缘。 它们具有高弹性和优异的附着力。