Iontophoretic delivery of an antimigraine drug
    3.
    发明授权
    Iontophoretic delivery of an antimigraine drug 失效
    离子电渗递送抗偏头痛药物

    公开(公告)号:US5674871A

    公开(公告)日:1997-10-07

    申请号:US586700

    申请日:1996-01-26

    摘要: The present invention relates to the iontophoretic delivery to a patient, more in particular to a migraine patient, of a compound of formula (I) as shown hereinunder. The invention also relates to a device for the iontophoretic delivery of a compound of formula (I), as well as to a composition containing a compound of formula (I), which can be applied in a device for iontophoretic delivery. Said compounds are benzopyranalkylaminoalkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 taken together form a bivalent radical of formula --(CH.sub.2).sub.m - wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n -, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd.; R.sup.4 and R.sup.5 each independently are hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; Alk.sup.2 is a bivalent C.sub.2-15 alkanediyl radical; and R.sup.6 and R.sup.7 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, hydroxy, C.sub.1-6 alkyloxy or cyano.

    摘要翻译: PCT No.PCT / EP94 / 02764 Sec。 371日期1996年1月26日 102(e)日期1996年1月26日PCT 1994年8月19日PCT PCT。 公开号WO95 / 05815 日期1995年3月2日本发明涉及如下所示的式(I)化合物对患者,特别是偏头痛患者的离子电渗疗法输送。 本发明还涉及用于离子电渗疗法递送式(I)化合物的装置,以及含有式(I)化合物的组合物,其可以应用于用于离子电渗疗法递送的装置中。 所述化合物是具有下式的苯并吡喃烷基氨基烷基取代的胍(I)其药学上可接受的酸加成盐及其立体化学异构形式,其中R 1是氢或C 1-6烷基; R2是氢,C1-6烷基,C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或R 2和R 3一起形成式 - (CH 2)m-的二价基团,其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - (CH 2)n - 的二价基团,其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =的二价基团时,R 3可以表示键; R 4和R 5各自独立地为氢或C 1-6烷基; Alk1是二价C 1-3烷二基; Alk2是二价C2-15烷二基; R 6和R 7各自独立地为氢,卤素,C 1-6烷基,C 3-6烯基,C 3-6炔基,羟基,C 1-6烷氧基或氰基。

    Itraconazole and saperconazole stereoisomers
    4.
    发明授权
    Itraconazole and saperconazole stereoisomers 失效
    伊曲康唑和舒康唑立体异构体

    公开(公告)号:US06346518B1

    公开(公告)日:2002-02-12

    申请号:US08295885

    申请日:1995-01-26

    IPC分类号: A61K31495

    摘要: The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula and the pharmaceutically acceptable acid addition salt forms thereof, processes for preparing said stereoisomeric forms, the complexes thereof with cyclodextrin derivatives, pharmaceutical compositions comprising said complexes and methods of preparing said complexes and pharmaceutical compositions.

    摘要翻译: 本发明涉及伊曲康唑(X = Cl)和沙美康唑(X = F)的立体异构形式,其可以由下式表示:其药学上可接受的酸加成盐形式,制备所述立体异构形式的方法及其复合物 与环糊精衍生物,包含所述复合物的药物组合物和制备所述复合物和药物组合物的方法。