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Abstract

This invention relates to compounds which possess immunosuppressive and/or anti tumor and/or antinflammatory activity in vivo and/or inhibit thymocyte proliferation in vitro. These compounds are therefore useful in the treaiment of transplantation rejection, autoimmune diseases such as lupus, rheumatoid ardiritis, diabetes mellitus, multiple sclerosis and in the treatment of Candida albicans infections and also in treatment of diseases of inflammation. These compounds are represented by the formula below ##STR1## wherein W and Y are OR.sup.1 and X and Z together form a bond or W and X are OR.sup.2 and Y and Z together form a bond, wherein: R.sup.1 is selected from --(CH.sub.2).sub.n --Ar with a proviso that Ar is not phenyl, --(CH.sub.2 CH.sub.2 O).sub.n CH.sub.3 with a proviso that n is greater than one, --CH.sub.2 CH.sub.2 CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3, --(CH.sub.2).sub.n --CH.sub.2 CH(OR.sup.3)CH.sub.2 OR.sup.4 where R.sup.3 and R.sup.4 are H, C.sub.1 -C.sub.10 alkyl, or R.sup.3 and R.sup.4 together are ethylene, methylene or dimethylmethylene; --CH.sub.2 (CH.sub.2).sub.n --OR.sup.3 with a proviso that R.sup.3 is not H, C.sub.1 -C.sub.10 alkyl, or C(O)C.sub.1 -C.sub.10 alkyl; and --CH.sub.2 (CH.sub.2).sub.n --X where X is F, Cl, Br or I; R.sup.2 is selected from H, C.sub.1 -C.sub.10 alkyl, Ar(CH.sub.2).sub.n --, C.sub.3 -C.sub.10 alkenyl, --(CH.sub.2 (CH.sub.2 O).sub.n CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3, --CH.sub.2 (CH.sub.2).sub.n --OR.sup.3, --CH.sub.2 (CH.sub.2).sub.n --X where X is F, Cl, Br or I; and --(CH.sub.2).sub.n --CH.sub.2 CH(OR.sup.5)CH.sub.2 OR.sup.6 where R.sup.5 and R.sup.6 are selected independently from H, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.n --Ar, --CONH(CH.sub.2).sub.n --Ar or COC(CH.sub.3).sub.2 --(CH.sub.2).sub.n --Ar, --COR.sup.7 and --CO.sub.2 R.sup.7, where R.sup.7 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or Ar; or R.sup.5 and R.sup.6 together are methylene, ethylene, or dimethylmethylene; R.sup.3 and R.sup.4 indepently are H, methyl, --(CH.sub.2).sub.n CH.sub.3, --(CH.sub.2).sub.n Ar, --(CH.sub.2).sub.n CH.dbd.CH.sub.2, --C(O)R.sup.7, --CO.sub.2 R.sup.7, --CONH(CH.sub.2).sub.n Ar or --C(O)C(CH.sub.3).sub.2 --(CH.sub.2).sub.n Ar; Ar is selected independently from phenyl, pyridinyl, quinolinyl, indolyl, furanyl, 1, 2, 3-triazolyl and tetrazolyl; n=1-10 independently; and m=1-5 independently, or a pharmaceutically acceptable acid addition salt where one can be formed.

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First Claim