This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
本发明涉及一类新型免疫抑制化合物,具有与FK-506结合蛋白(FKBP)亲和力。一旦与该蛋白结合,免疫抑制化合物抑制FKBP的脯
氨酰肽顺反异构酶(旋转酶)活性,并抑制T细胞活化。因此,本发明的化合物可用作
免疫抑制药物,以预防或显著减少骨髓和器官移植的移植排斥,并用于治疗人类和其他哺乳动物的广泛自身免疫性疾病。