Substituted thiadiazolesulfonamides
    7.
    发明授权
    Substituted thiadiazolesulfonamides 有权
    取代的噻二唑磺酰胺

    公开(公告)号:US06503934B2

    公开(公告)日:2003-01-07

    申请号:US09779823

    申请日:2001-02-09

    IPC分类号: C07D28508

    CPC分类号: C07D285/08

    摘要: Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1&bgr; participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).

    摘要翻译: 式(I)化合物适用于制备用于预防和治疗所有这些疾病的药物,其中白细胞介素-1β参与其过程的浓度增加,例如脓毒性休克,白血病,肝炎,肌肉退化,HIV感染 或退行性关节疾病(例如骨关节炎,椎关节强硬,关节创伤后的软骨溶解或半月板或髌骨损伤后关节的延长固定或撕裂的韧带),结缔组织的疾病(如胶原病,牙周病或伤口愈合障碍) ,以及运动系统的慢性疾病(例如炎性或免疫学或代谢相关的急性和慢性关节炎,关节病,类风湿性关节炎,肌肉痛和骨骼代谢紊乱)。

    Enzyme activity screen with direct substrate reloading
    10.
    发明授权
    Enzyme activity screen with direct substrate reloading 失效
    具有直接底物重新加载的酶活性筛选

    公开(公告)号:US06867010B1

    公开(公告)日:2005-03-15

    申请号:US09390851

    申请日:1999-09-07

    CPC分类号: C12N9/00

    摘要: A method for in vitro selection, from a library of catalyst molecules, of a catalyst molecule of interest having a relatively more efficient specific catalytic activity of interest, as compared to the rest of the catalyst molecules within said library, and wherein said in vitro selection method is characterized by that it allows multiple catalytic activity turn-overs (i.e. substrate to product catalytic activity turn-overs), by the catalyst molecule of interest, before it is finally collected. The method is based on using one or more reagent(s) which are capable of converting a product generated by a catalyst molecule of interest back into the substrate for said catalyst of interest.

    摘要翻译: 与所述文库中的其余催化剂分子相比,从感兴趣的相对更有效的特定催化活性的目的催化剂分子的催化分子的文库中体外选择一种方法,其中所述体外选择 方法的特征在于,在最终收集之前,其通过感兴趣的催化剂分子允许多重催化活性翻转(即底物至产物催化活性翻转)。 该方法基于使用一种或多种试剂,其能够将由感兴趣的催化剂分子产生的产物转化为用于所述感兴趣的催化剂的底物。