Vitamin d3-analogs

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 5/02 (2006.01) A61K 31/59 (2006.01) C07C 401/00 (2006.01)

Patent

CA 2133144

The invention relates to the compounds 1,25-dihydroxy-16-ene-24-oxo- cholecalciferol and 1,24,25-trihydroxy-16-ene-cholecalciferol which stimulate differentiation of HL-60 cells, rendering them useful as an agent for the treatment of neoplastic diseases such as leukemia, and also decrease proliferation of human keratinocytes, rendering them useful as an agent for the treatment of hyperproliferative disorders of the skin such as psoriasis. They are prepared by perfusing 1,25-dihydroxy-16-ene-cholecalciferol in rate kidneys, extracting the perfusate and isolating 1,25-dihydroxy-16-ene- 24-oxo-cholecalciferol and 1,24,25-trihydroxy-16-ene-cholecalciferol.

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