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Generated: November 23, 2017

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Title: Method of inhibiting the hyperproliferation of malignant cells
Abstract:1.alpha.-hydroxy vitamin D.sub.4 and analogues, preferably 1,24 dihydroxy vitamin D.sub.4, which are useful as active compounds of pharmaceutical compositions for the inhibition of hyperproliferative activity of malignant cells.
Inventor(s): Knutson; Joyce C. (Madison, WI), Bishop; Charles W. (Verona, WI)
Assignee: Bone Care International, Inc. (Madison, WI)
Filing Date:Jun 07, 1995
Application Number:08/486,387
Claims:1. A method of inhibiting the hyperproliferative activity of malignant cells, comprising treating the malignant cells with an antihyperproliferative-effective amount of compound of formula (I): ##STR2## wherein R.sub.1 is either H or OH and R.sub.2 is either H or OH and salts, hydrates and solvates thereof.

2. The method of claim 1 wherein the compound of formula (I) is 1.alpha.,24-dihydroxy vitamin D.sub.4.

3. The method of claim 2 wherein the compound of formula (I) is 1.alpha.,24(R)-dihydroxy vitamin D.sub.4, substantially free of its (S) form.

4. The method of claim 1 wherein said amount is about 1 .mu.g/dose to about 500 .mu.g/dose.

5. A method of treating a human to alleviate the hyperproliferative cellular activity of breast cancer and colon cancer, comprising administering to the human a therapeutically effective the word of of amount of compound of formula (I): ##STR3## wherein R.sub.1 is either H or OH and R.sub.2 is either H or OH and salts, hydrates and solvates thereof.

6. The method of claim 5 wherein the compound of formula (I) is 1.alpha.,24-dihydroxy vitamin D.sub.4.

7. The method of claim 6 wherein the compound of formula (I) is 1.alpha.,24(R)-dihydroxy vitamin D.sub.4, substantially free of its (S) form.

8. The method of claim 5 wherein said therapeutic amount is about 1 .mu.g/dose to about 500 .mu.g/dose.

9. A pharmaceutical composition, comprising a compound of the formula (I): ##STR4## wherein R.sub.1 is either H or OH and R.sub.2 is either H or OH in combination with a pharmaceutically acceptable vehicle.

10. The pharmaceutical composition of claim 9, wherein said composition is an oral composition and wherein the said compound of formula (I) is present at a concentration of about 1 .mu.g/g to about 100 .mu.g/g of composition.

11. The composition of claim 10, wherein the compound of formula (I) is 1.alpha.,24-dihydroxy vitamin D.sub.4.

12. The composition of claim 11, wherein the compound of formula (I) is 1.alpha.,24(R)-dihydroxy vitamin D.sub.4, substantially free of its (S) form.

13. The pharmaceutical composition of claim 9, wherein said composition is a topical composition and wherein the said compound of formula (I) is present at a concentration of about 1 .mu.g/g to about 100 .mu.g/g of composition.

14. The composition of claim 13, wherein the compound of formula (I) is 1.alpha.,24-dihydroxy vitamin D.sub.4.

15. The composition of claim 14, wherein the compound of formula (I) is 1.alpha.,24(R)-dihydroxy vitamin D.sub.4, substantially free of its (S) form.

16. The method of claim 1, wherein said treating step comprises exposing said cells to the compound of formula (I) in said amount sufficient to induce differentiation of said cells to nonmalignant monocytes.

17. The method of claim 16, wherein said cells are HL-60 human leukemia cells.

18. The method of claim 16, wherein said compound of formula (I) is 1.alpha.,24(R)-dihydroxyvitamin D.sub.4, substantially free of its (S) isomer.
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