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    NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF
    4.
    发明公开
    NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF 有权
    作为蛋白质酪氨酸激酶抑制剂的新型高比哌嗪衍生物及其药物用途

    公开(公告)号：EP2590981A1

    公开(公告)日：2013-05-15

    申请号：EP11738151.7

    申请日：2011-07-08

    申请人： Leo Pharma A/S

    发明人： NIELSEN, Simon, Feldbæk ,  GREVE, Daniel, Rodriguez ,  GRUE-SØRENSEN, Gunnar ,  RYTTERSGAARD, Carsten ,  SCHOU, Søren, Christian ,  SAMS, Anette, Graven

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P29/00 ,  A61P37/02

    CPC分类号： C07D487/04 ,  A61K31/5513 ,  A61K45/00

    摘要： The invention relates to compounds of general formula (I) wherein R
    1 ,R
    2 , R
    3 , R
    4 , m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

    摘要翻译： 本发明涉及其中R 1，R 2，R 3，R 4，m和n如本文定义所定义的通式（I）的化合物及其药学上可接受的盐，水合物或溶剂合物单独或在 在治疗中与一种或多种其它药物活性化合物联合用作预防，治疗或改善疾病及其并发症的JAK激酶和蛋白酪氨酸激酶抑制剂，所述疾病及其并发症包括例如牛皮癣，特应性皮炎，红斑痤疮，狼疮，多发性硬化，类风湿 关节炎，I型糖尿病，哮喘，癌症，自身免疫性甲状腺疾病，溃疡性结肠炎，克罗恩氏病，阿尔茨海默氏病，白血病，眼病如糖尿病性视网膜病和黄斑变性以及其他自身免疫性疾病和适应症，例如免疫抑制 器官移植。