PROCESS FOR THE SYNTHESIS OF BUPRENORPHINE
    3.
    发明公开

    公开(公告)号:EP4335853A2

    公开(公告)日:2024-03-13

    申请号:EP24152430.5

    申请日:2021-01-27

    申请人: AZAD Pharma AG

    IPC分类号: C07D498/12

    摘要: The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.

    Ophtalmic oil-in-water emulsions containing prostaglandins
    9.
    发明公开
    Ophtalmic oil-in-water emulsions containing prostaglandins 审中-公开
    ProstaglandinhaltigeÖl-in-Wasser-Emulsionenfürdas Auge

    公开(公告)号:EP1985298A1

    公开(公告)日:2008-10-29

    申请号:EP07008357.1

    申请日:2007-04-24

    申请人: Azad Pharma AG

    摘要: The present invention refers to an oil-in-water emulsion for ophthalmic application comprising at least one prostaglandin as active agent and a surfactant component comprising a combination of at least two non-ionic surfactants. The emulsion is suitable for medical applications, particularly for the treatment of glaucoma, and has an increased chemical stability of the prostaglandin active agent so to allow long-term storage also at room temperature.

    摘要翻译: 本发明涉及用于眼科应用的水包油乳液,其包含至少一种作为活性剂的前列腺素和包含至少两种非离子表面活性剂的组合的表面活性剂组分。 该乳剂适用于医疗应用,特别是用于治疗青光眼,并且具有增加的前列腺素活性剂的化学稳定性,从而允许在室温下长期储存。