| 摘要 |
The present invention relates to novel semisynthetic cyclosporin analogs of Formula (I):X is absent, -C1-C6 alkyl-, or -C3-C6 cycloalkyl-Y is selected from the group consisting of:(i) C(O)-O-R1, where R1 is hydrogen, C1-C6 alkyl, optionally substituted with halogen, heterocyclic, aryl, C1-C6 alkoxy, C1-C6 alkylthio, halogen-substituted C1-C6 alkoxy, or halogen-substituted C1-C6 alkylthio;(ii) C(O)-S-R1, where R1 is as previously defined;(iii) C(O)-OCH2-OC(O)R2, where R2 is C1-C6 alkyl, optionally substituted with halogen, C1-C6 alkoxy; C1-C6 alkylthio, heterocyclic or aryl;(iv) C(S)-O-R1, where R1 is as previously defined, and(v) C(S)-S-R1, where R1 is as previously defined;B is -alphaAbu-, -Val-, -Thr- or -Nva-; andU is -(D)Ala-, -(D)Ser-, -[O-(2-hydroxyethyl)(D)Ser]-, -[O-acyl(D)Ser]- or -[O-(2-acyloxyethyl)(D)Ser]-.
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