申请人:Nielsen Simon Feldbæk
公开号:US20120178740A1
公开(公告)日:2012-07-12
The invention relates to compounds of general formula (I) wherein A, R
1
, R
2
, R
3
, R
4
, R
5
, R
9
, 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 disease, 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.
本发明涉及通式(I)化合物,其中A,R1,R2,R3,R4,R5,R9,m和n如本说明书所定义,并且其药学上可接受的盐,水合物或溶剂化物,在治疗中使用 - 单独或与一个或多个其他药学活性化合物结合使用 - 作为JAK激酶和蛋白酪氨酸激酶抑制剂,用于预防,治疗或改善疾病及其并发症,包括例如银屑病,特应性皮炎,酒渣鼻,狼疮,多发性硬化症,类风湿性关节炎,1型糖尿病,哮喘,癌症,自身免疫性甲状腺疾病,溃疡性结肠炎,克罗恩病,阿尔茨海默病,白血病,眼部疾病例如糖尿病视网膜病变和黄斑变性以及其他自身免疫性疾病和需要免疫抑制的适应症,例如器官移植。