Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...
Patent
1992-12-02
1994-08-30
Shah, Mukund J.
Organic compounds -- part of the class 532-570 series
Organic compounds
Unsubstituted hydrocarbyl chain between the ring and the -c-...
C07D26700
Patent
active
053429354
ABSTRACT:
Hydroxymacrolides and derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation at C-20. These macrolides are useful as antagonists of FK-506-type immunosuppressants. The compounds of the present invention are useful for modifying dosages of FK-506-type immunosuppressants in the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, the compounds of the present invention have utility as antidotes for overdoses of FK-506-type immunosuppressants.
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Tanaka, et al., J. Am. Chem. Soc., 109, 5031-5033 (1987).
March, Adv. Org. Chem., 3d ed., John Wiley & Sons, N.Y., 1985, pp. 627 & 1057.
Petros, et al., FEBS Lett., 308(3), 309-314 (Aug. 1992).
Beattie Thomas R.
Dumont Francis J.
Wyvratt Matthew J.
DiPrima Joseph F.
Gupta Y. N.
Merck & Co. , Inc.
Rose David L.
Shah Mukund J.
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