| 摘要 |
The present invention provides a cyclosporin of the following Formula (I), or a pharmaceutically acceptable salt, ester or prodrug thereof. In Formula (I), A is wherein: X is selected from the group consisting of: -(CH2)n- and -CH2-CH=CH-(CH2)m-, where n is an integer of from 1 to 8 and m is an integer of from 2 to 5; Y is selected form the group consisting of: OH, OAc, halogen, N3, CN and OS(O)2R10, wherein R10 is selected from the group consisting of F, CH3, CF3, Ph, MePh; or, alternatively, X and Y taken together are selected from the group consisting of: -CH=CH2, -CHO, and -CH2CH3; R is selected from the group consisting of: hydrogen and a hydroxyl protecting group; B is selected from the group consisting of: -alphaAbu-, -Val-, -Thr- and -Nva-; and U is selected from the group consisting of: -(D)Ala-, -(D)Ser-, -[O-(2 hydroxyethyl)(D)Ser]-, -[O-acyl(D)Ser]- and -[O-(2-acyloxyethyl)(D)Ser]-.
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