| 摘要 |
A calcitriol analog of 19-nor-vitamin D shown as Formula (I), particularly 19-nor-1,25-(OH)2D2 possess low calcemic and phosphatemic activity while also having the ability to suppress parathyroid hormone (PTH) production. The suppressive effect on PTH secretion of these 19-nor analogs without significant changes in serum calcium or serum phosphorus is useful for the treatment of secondary hyperparathyroidism in patients having kidney disorders. Wherein; X1 and X2 each represent, independently, hydrogen or a hydroxy-protecting group; R is represented by Formula (II), wherein the stereochemical center may have the R or S configuration, and where Z is selected from Y, -OY, -CH2OY, -C=CY and -CH=CHY, where the double bond may have the cis or trans geometry, and where Y is selected from hydrogen, methyl, -CR5O and a radical of the structure represented by Formula (III); wherein m and n represent 0 to 5, R1 is selected from hydrogen, hydroxy, protected hydroxy, fluoro, trifluoromethyl, and C1-5alkyl, which may be straight chain or branched and, optionally, bear a hydroxy or protected-hydroxy substituent; and where each of R2, R3, and R4, independently, is selected from hydrogen, fluoro, trifluoromethyl and C1-5alkyl, which may be straight-chain or branched, and optionally, bear a hydroxy or protected-hydroxy substituent; and where R1 and R2, taken together represent an oxo group, or an alkylidene group, =CR2R3, or the group -(CH2)p-, where p is an integer from 2 to 5; and where R3 and R4, taken together, represents an oxo group, or a group -(CH2)q-, where q is an integer from 2 to 5; and where R5 represents hydrogen, hydroxy, protected hydroxy, or C1-5alkyl.
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