PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    4.
    发明授权
    PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 失效
    哌嗪衍生物和工艺及其

    公开(公告)号:EP0850222B1

    公开(公告)日:2003-05-28

    申请号:EP97930868.1

    申请日:1997-06-28

    摘要: The present invention relates to novel compound having strong antitumor activities of general formula (I), wherein R1 and R2 are independently hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted C3-C6 cycloalkyl, substituted or unsubstituted C2-C8 unsaturated alkyl, ketone, substituted or unsubstituted aryl, substituted or unsubstituted C1-C4 alkoxy, substituted or unsubstituted arylhydroxy, substituted or unsubstituted amino, C1-C4 lower ester, C1-C4 lower thioester, thiol, substituted or unsubstituted carboxyl, epoxy, substituted or unsubstituted C1-C4 lower thioalkoxy; or R1 and R2 are fused to form C3-C4 saturated or unsaturated chain; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, C1-C4 lower ester, C1-C4 lower alkyl, C1-C4 lower thioalkyl, substituted or unsubstituted C3-C6 cycloalkyl, C1-C4 lower alkoxy, C1-C4 lower thioalkoxy, substituted or unsubstituted aryl, substituted or unsubstituted lower arylalkoxy, substituted or unsubstituted lower alkylamino, or lower alkyl substituted or unsubstituted carbamate; or among R3, R4, R5, R6 and R7, two adjacent groups are bonded with each other to form 1,2-phenylene or 2,3-naphthylene; X is oxygen, sulfur, or substituted or unsubstituted imino; Y is bonded at the 3-position or 4-position of the aromatic ring part wherein Y is oxygen or -NR8- (wherein, R8 is the same with the above-mentioned R3); Z is hydroxy, C1-C4 lower alkoxy, C1-C4 lower thioalkoxy, substituted or unsubstituted aryloxy, C1-C4 lower alkylamino, substituted or unsubstituted cycloamino containing 1-5 nitrogen atoms; A is nitrogen or -CH=; its pharmaceutically acceptable acid addition salts and process for the preparation thereof.

    IMPROVED COMPOSITIONS AND METHODS FOR CHEMODENERVATION USING NEUROTOXINS
    5.
    发明授权
    IMPROVED COMPOSITIONS AND METHODS FOR CHEMODENERVATION USING NEUROTOXINS 失效
    FOR化学去神经改良的组合物和方法与NEURO毒素

    公开(公告)号:EP0773788B1

    公开(公告)日:2003-05-07

    申请号:EP96917968.8

    申请日:1996-06-04

    申请人: Pearce, L. Bruce

    IPC分类号: A61K38/16 A61P21/02 A61P25/00

    摘要: The compositions and methods disclosed herein utilize admixtures of neurotoxins to cause denervation which is unexpectedly more localized and of longer duration than otherwise occurs with single neurotoxins. The compositions and methods of the invention utilize neurotoxin admixtures calibrated in median paralysis units rather than LD50s. Admixtures of neurotoxins include, but are not limited to, the botulinum serotypes A-G and tetanus toxin. The clinical benefits of the disclosed invention include: lengthening intervals between neurotoxin treatments; reducing adverse immunogenic responses to neurotoxins; and, reducing adverse diffusion-dependent side-effects of neurotoxin treatments.