申请人:Merck & Co., Inc.
公开号:US05506228A1
公开(公告)日:1996-04-09
A class of 2,6-diarylpyridazinones of general structural formula I have been identified that exhibit exhibit immunosuppressant activity with human T-lymphocytes, and are useful as an immunosuppressants. ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form thereof, wherein: when M is S, R.sup.1 and R.sup.2 are selected from the following combinations: when R.sup.2 is 4-chloro, then R.sup.1 is 4-OCH.sub.3,2 -CH.sub.3, 4-Cl, 4-CH3, 3-Cl, 3-CH3, 2-Cl, 4-H, 4-Br, 3-NO.sub.2 ; and when R.sup.2 is H, then R.sup.1 is 4-OCH.sub.3, and when M is --SO.sub.2 --, then R.sup.2 is H and R.sup.1 is 4-OCH.sub.3. As an immunosuppressant, these compounds are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
已经发现了一类2,6-二芳基吡啶并咪唑酮,具有一般结构式I,表现出与人类T淋巴细胞相关的免疫抑制活性,可用作免疫抑制剂。其中:当M为S时,R1和R2从以下组合中选择:当R2为4-氯时,R1为4-OCH3,2-CH3,4-Cl,4-CH3,3-Cl,3-CH3,2-Cl,4-H,4-Br,3-NO2;当R2为H时,R1为4-OCH3;当M为--SO2--时,R2为H,R1为4-OCH3。作为免疫抑制剂,这些化合物在治疗自身免疫性疾病、预防外来器官移植的排斥以及相关疾病和疾病方面非常有用。