申请人:Merck & Co., Inc.
公开号:US05252732A1
公开(公告)日:1993-10-12
O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
通用结构式I的O-杂环芳基、O-烷基杂环芳基、O-烯基杂环芳基和O-炔基杂环芳基大环内酯已经通过在环己基环的C-3"和/或C-4"处进行烷基化和/或芳基化制备自适应的前体。这些大环内酯免疫抑制剂在哺乳动物宿主中用于治疗自身免疫性疾病、传染病、预防外源器官移植的排斥和/或相关疾患、疾病和疾病。