| 摘要 |
The in vivo release of vitamin D compounds may be regulated by derivatizing the hydroxy group at carbon 25 with an acyl group or a hydrocarbyloxycarbonyl group to obtain a vitamin D derivative of formula (I). These compounds may be used in medicaments for the treatment of disease states resulting form calcium metabolism disorders. In formula (I); R5 and R6 represent hydrogen, or taken together R5 and R6 are methylene; R is represented by the structure 1, where the stereochemical centre at carbon 20 in the side chain may have the R or S configuration; Z is selected from Y, -OY, -CH2OY, C CY and CH = CHY, where the double bond may have the cis or trans stereochemical configuration; Y is selected from a radical of the structure 2; m and n, independently, represent the integers from 0 to 5; R1 is selected from the group consisting of hydrogen, OX4, fluoro, trifluoromethyl and C1-5- alkyl, which may be straight chain or branched and, optionally, bear a hydroxy substituent; R2 is selected from the group consisting of hydrogen, fluoro, trifluoromethyl and C15 alkyl, which may be straight-chain or branched, and optionally, bear a hydroxy substituent; and R3 and R4 are selected from trifluoromethyl and C15 alkyl, which may be straight chain or branched and optionally bear a hydroxy substituent; or R1 and R2 taken together, represent an oxo group, or an alkylidene group, =CR2R2, =CR2R3, or the group -(CH2)p-, where p is an integer from 2 to 5; or R3 and R4, taken together, represent the group (CH2)q-, where q is an integer from 2 to 5; X1, X2, and X4 are each hydrogen, an acyl group, or a hydrocarbyloxycarbonyl group; and X3 represents an acyl group or a hydrocarbyloxycarbonyl group.
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