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2-Alkylidene-18,19-Dinor-Vitamin D Compounds

  • US 20100179344A1
  • Filed: 02/19/2010
  • Published: 07/15/2010
  • Est. Priority Date: 04/09/2004
  • Status: Abandoned Application
First Claim
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1. A compound having the formula:

  • where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 and R8, which may be the same or different, are each selected from the group consisting of hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or, when taken together represent the group —

    (CH2)x

    where x is an integer from 2 to 5, and where the group R is represented by the structure;

    where the stereochemical center at carbon 20 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, —

    COR5 and a radical of the structure;

    where m and n, independently, represent the integers from 0 to 5, where R1 is selected from hydrogen, deuterium, hydroxy, protected hydroxy, fluoro, trifluoromethyl, and C1-5-alkyl, 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 deuterium, deuteroalkyl, hydrogen, fluoro, trifluoromethyl and C1-5 alkyl, 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, represent an oxo group, or the group —

    (CH2)q

    , where q is an integer from 2 to 5, and where R5 represents hydrogen, hydroxy, protected hydroxy, or C1-5 alkyl and wherein any of the CH-groups at positions 20, 22, or 23 in the side chain may be replaced by a nitrogen atom, or where any of the groups —

    CH(CH3)—

    , —

    (CH2)m-, —

    (CH2)n-, or —

    (CR1R2)—

    at positions 20, 22, and 23, respectively, may be replaced by an oxygen or sulfur atom.

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