申请人:NIPPON SHINYAKU COMPANY, LIMITED
公开号:EP0852233A1
公开(公告)日:1998-07-08
The invention provides a novel cyclosporin compound which is water-soluble, improved in the amount of absorption and absorption rate after oral administration, with low nephrotoxicity, and a pharmaceutical composition comprising the same compound.
The compound of the invention includes such cyclosporin phosphate derivatives as [phosphonothreonine2]cyclosporin A, [phosphono-4-hydroxynorvaline2]cyclosporin A, [phosphono-D-serine8]cyclosporin A, [phosphonothreonine2, phosphono-D-serine8]cyclosporin A, etc. or salts thereof, and solvates thereof.
本发明提供了一种新型环孢素化合物,该化合物具有水溶性,口服后吸收量和吸收率均有所改善,肾毒性低,还提供了包含该化合物的药物组合物。
本发明的化合物包括[phosphonothreonine2]cyclosporin A、[phosphono-4-hydroxynorvaline2]cyclosporin A、[phosphono-D-serine8]cyclosporin A、[phosphonothreonine2,phosphono-D-serine8]cyclosporin A 等环孢素磷酸衍生物或其盐类,以及其溶液。