| 摘要 |
The present invention relates to novel semisynthetic cyclosporin analogs of formula (I), wherein A is (II), 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 -.alpha.Abu-, -Val-, - Thr- or -Nva- ;U and is -(D)Ala-, -(D)Ser-, -[O-(2 -hydroxyethyl)(D)Ser]-, -[O- acyl(D)Ser]- or -[O-(2-acyloxyethyl) (D )Ser]-.
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