利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

6 条记录 (耗时 0.01 秒)

    COMPLEXES OF SIROLIMUS AND ITS DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    1.
    发明公开
    COMPLEXES OF SIROLIMUS AND ITS DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
    复从及其制备方法和药物组合物，以雷帕霉素及其衍生物，PROCESS

    公开(公告)号：EP3104844A1

    公开(公告)日：2016-12-21

    申请号：EP15710913.3

    申请日：2015-02-13

    申请人： Druggability Technologies IP Holdco Limited

    发明人： ANGI, Erzsébet Réka ,  SOLYMOSI, Tamás ,  KÁRPÁTI, Richard Balázs ,  FENYVESI, Zsófia ,  ÖTVÖS, Zsolt ,  MOLNÁR, László ,  GLAVINAS, Hristos ,  FILIPCSEI, Genovéva ,  FERENCZI, Katalin ,  HELTOVICS, Gábor

    IPC分类号： A61K9/16 ,  A61K47/10 ,  A61K47/20

    CPC分类号： A61K31/436 ,  A61K47/10 ,  A61K47/20 ,  A61K47/58 ,  A61K47/6933

    摘要： The invention is directed to a stable complex with controlled particle size, increased apparent solubility and increased dissolution rate comprising as active compound Sirolimus or derivatives thereof, which is useful in the prophylaxis of organ rejection in patients receiving renal transplants, in the treatment of psoriasis, facial angiofibromas associated with tuberous sclerosis, fibrofolliculomas found in Birt-Hogg-Dubé Syndrome, chronic erosive oral lichen planus, Early Stage Cutaneous T-cell Lymphoma, Treatment of Autoimmune Active Anterior Uveitis, dry eye syndrome, age-related macular degeneration, diabetic macular edema, noninfectious uveitis, telangiectasia, inflammatory skin diseases (dermatitis, including psoriasis and lichen ruber planus), Pachyonychia Congenita and in the suppression of angiogenesis pathways. More specifically, the complex of the present invention possesses increased apparent solubility, permeability and enhanced biological performance including significantly improved exposure, earlier tmax, higher Cmax and higher trough concentrations at 24 hours which will allow the reduction of the dose.

    摘要翻译： 本发明涉及具有受控的颗粒尺寸的稳定的复合物，增加的表观溶解度和增加的溶解速率，其包括作为活性化合物西罗莫司或它们的衍生物，所有这些是在器官排斥在牛皮癣的治疗接收肾移植的患者的预防是有用的， 结节性硬化症相关联的面部血管纤维瘤，fibrofolliculomas在伯特-霍格-杜贝综合征，慢性糜烂口腔扁平苔藓发现，早期皮肤T细胞淋巴瘤，自身免疫性主动前葡萄膜炎，干眼综合征，年龄相关性黄斑变性，糖尿病性黄斑治疗 水肿，葡萄膜炎非传染性，毛细血管扩张，炎性皮肤疾病（皮炎，牛皮癣和扁平苔癣包含）先天性厚甲和在血管生成途径的抑制。 更具体地，本发明的复合物具有增加的表观溶解度，渗透性和增强的生物学性能，包括显着提高的曝光，t最大早些时候，在24小时时更高的C max和较高谷浓度whichwill允许剂量的减少。