Increasing blood-brain barrier permeability with permeabilizer peptide derivatives of bradykinin
    47.
    发明公开
    Increasing blood-brain barrier permeability with permeabilizer peptide derivatives of bradykinin 失效
    通过使用透气性促进的增加血脑屏障的渗透性,从肽缓激肽衍生

    公开(公告)号:EP0885900A2

    公开(公告)日:1998-12-23

    申请号:EP98113628.6

    申请日:1992-04-23

    申请人: ALKERMES, INC.

    摘要: Peptides called receptor mediated permeabilizers (RMP) increase the permeability of the blood/brain barrier to molecules such as therapeutic agents or diagnostic agents. The permeabilizer A-7 or conformational analogues can be intravenously coadministered to a host together with molecules whose desired destination is the interstitial fluid compartment of the brain. Alternatively, the permeabilizer A-7 or conformational analogues can be administered sequentially with the molecule(s) of interest and these molecules can also be administered by routes other than intravascular. The permeabilizer A-7 or conformational analogues allow these molecules to penetrate the blood-brain barrier and arrive in the interstitial fluid.

    摘要翻译: 肽称为受体介导的permeabilizers(RMP)增加血/脑屏障的分子的渗透性:如治疗剂或诊断剂。 所述渗透剂A-7或构象的类似物可经静脉内连同分子,其希望的目的地是脑的间质液隔室共同施用至宿主。 可替代地,渗透剂A-7或构象类似物可与兴趣和合成分子的分子(多个)被依次施用因此,可以通过血管内比其它途径给药。 所述渗透剂A-7或构象类似物允许合成分子穿透血 - 脑屏障,并在间质液到达。

    SELECTIVE OPIOID COMPOUNDS
    50.
    发明授权
    SELECTIVE OPIOID COMPOUNDS 有权
    选择性阿片类化合物

    公开(公告)号:EP2252150B1

    公开(公告)日:2018-04-11

    申请号:EP09710456.6

    申请日:2009-02-13

    申请人: Alkermes, Inc.

    IPC分类号: A01N43/42 A61K31/44

    摘要: The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which relates to morphinan compounds useful as μ, δ, and/or &kgr; receptor opioid compounds and pharmaceuticals containing same that may be useful for mediating analgesia, combating drug addiction, alcohol addiction, drug overdose, mental illness, bladder dysfunctions, neurogenic bladder, interstitial cystitis, urinary incontinence, premature ejaculation, inflammatory pain, peripherally mediated and neuropathic pain, cough, lung edema, diarrhea, cardiac disorders, cardioprotection, depression, and cognitive, respiratory, diarrhea, irritable bowel syndrome and gastro-intestinal disorders, immunomodulation, and anti-tumor agents.