公开(公告)号：US06251929B1

公开(公告)日：2001-06-26

申请号：US09434494

申请日：1999-11-05

申请人： Mitsuru Naiki ,  Takumi Numazawa ,  Tomoyuki Okada ,  Kazuharu Ienaga ,  Kazuyoshi Sawada

发明人： Mitsuru Naiki ,  Takumi Numazawa ,  Tomoyuki Okada ,  Kazuharu Ienaga ,  Kazuyoshi Sawada

IPC分类号： A64K31415

CPC分类号： A61K31/4166

摘要： A highly safe therapeutic agent for intractable vasculitis such as malignant rheumatoid arthritis contains a hydantoin derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof as an effective ingredient: wherein each of R1, and R2, which may be the same or different, represents hydrogen, an alkyl group or a cycloalkyl group; and each of X and Y, which may be the same or different, represents hydrogen, a hydroxyl group, an alkyl group or an alkoxy group, or X and Y together represent an oxo group. The hydantoin derivatives significantly suppress the generation of arthritis and arteritis (cutaneous ulcer and auricular infarcted necrosis) which are naturally developed in model animals (MRL/lpr), and further significantly elongate the survival rate of MRL/lpr mice. Consequently, the hydantoin derivatives, having low toxicity and little side effects are very useful as highly safe therapeutic agents for intractable vasculitis such as malignant rheumatoid arthritis.

摘要翻译： 用于顽固性血管炎的恶性类风湿性关节炎的高度安全的治疗剂含有式（I）表示的乙内酰脲衍生物或其药学上可接受的盐作为有效成分：其中R1和R2可以相同或不同 表示氢，烷基或环烷基; X和Y各自可以相同或不同，表示氢，羟基，烷基或烷氧基，或X和Y一起表示氧代基。 乙内酰脲衍生物显着抑制模型动物（MRL / lpr）中天然发育的关节炎和动脉炎（皮肤溃疡和耳廓梗塞坏死）的产生，并进一步显着延长MRL / lpr小鼠的存活率。 因此，具有低毒性和少量副作用的乙内酰脲衍生物作为难治性血管炎如恶性类风湿性关节炎的高度安全的治疗剂是非常有用的。