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Abstract

The present invention relates to novel semisynthetic cyclosporin analogs of Formula (I): ##STR1## 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)--OCH.sub.2 --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-; and U is -(D)Ala-, -(D)Ser-, --[O-(2-hydroxyethyl)(D)Ser]-, --[O-acyl(D)Ser]-or --[O-(2-acyloxyethyl)(D)Ser]-.

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First Claim