Cyclosporin analogs with modified "C-9 amino acids"

Claim 1

A compound of formula ##STR18## wherein R 1 is MeBMT; R 2 is ##STR19## where X, R, R a and R e are as defined below; R is (1) hydrogen; (2) loweralkyl; (3) loweralkenyl; (4) haloloweralkyl; (5) aryl; (6) oxyloweralkyl comprising lower alkyl and hydroxy lower alkyl; (7) thioloweralkyl comprising alkyl thio lower alkyl and mercapto lower alkyl; (8) heteroaryl; the aryl or heteroaryl group above can be substituted with one or more functional groups selected from a group consisting of (a) C 1-6 alkyl, (b) C 1-6 alkanoyl; (c) C 1-6 haloalkyl; (d) halo; (e) cyano; (f) hydroxy C 1-3 alkyl; (g) C 1-6 alkoxy; (h) ##STR20## where n is 0, 1 or 2; (i) --NR b COR c wherein R b and R c independently are H or C 1-6 alkyl; (j) --NO 2 ; (k) --NR b R c ; (l) --OR b ; (m) --CONR b R c (n) --COR b ; (o) --NR b CONR b R c ; (p) --NR b COR c ; (q) --OCOR b ; (r) --SCOR b ; or (s) --OCH 2 O--; and X is S, SO, SO 2 , O, or NR b R a is loweralkyl; R e is loweralkyl; loweralkylphenyl; or aryl; R 3 is sarcosyl; α-(methylmercapto)-sarcosyl; N-methyl-D-alanyl; N-methyl-L-alanyl; or D-prolyl; R 4 is N-methyl-L-leucyl; R 5 is L-valyl; or norvalyl; R 6 is N-methyl-L-leucyl; R 7 is L-ananyl; L-2-aminobutyryl; or L-phenylalanyl;; R 8 is D-alanyl or L-alanyl; R 9 is N-methyl-L-leucyl; or N-methyl-L-valyl; R 10 is N-methyl-L-leucyl; or L-leucyl; and R 11 is N-methyl-L-valyl; L-valyl; N-methylleucyl; or L-2-aminobutyryl.