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Details for Patent: 7,122,530

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Details for Patent: 7,122,530

Title:24-hydroxyvitamin D, analogs and uses thereof
Abstract: The invention provides 24-hydroxyvitamin D compounds and methods for their use in the treatment and prophylaxis of hyperparathyroidism and hyperproliferative diseases, and in the modulation of the immune and inflammatory responses as well as the treatment of bone depletive disorders.
Inventor(s): Bishop; Charles W. (Madison, WI), Knutson; Joyce C. (Madison, WI), Strugnell; Stephen (Madison, WI)
Assignee: Genzyme Corporation (Cambridge, MA)
Filing Date:Jan 03, 2001
Application Number:09/753,697
Claims:1. A method of achieving an effect in a patient in need thereof comprising administering an effective amount of a vitamin D compound which is a 24-hydroxyvitamin D compound wherein the effect is treating hyperparathyroidism, and wherein said 24-hydroxyvitamin D is a compound of formula (I): ##STR00009## wherein Z is a side chain of formula (IIB): ##STR00010## wherein R.sup.5 and R.sup.6 are each hydrogen or taken together form a double bond between C-22 and C-23, R.sup.3 is hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; R.sup.4 is lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; and R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl, lower fluoroalkenyl, lower cycloalkyl or taken together with the carbon to which they are bonded form a C.sub.3 C.sub.8 cyclocarbon ring; Y is a methylene group if Y is double bonded to the A-ring or a methyl group or hydrogen if Y is single bonded; and X is hydrogen, lower alkyl or lower fluoroalkyl.

2. A method of achieving an effect in a patient in need thereof comprising administering an effective amount of a vitamin D compound which is a 24-hydroxyprevitamin D, wherein the effect is treating hyperparathyroidism, wherein said 24-hydroxyprevitamin D is a compound of formula (III): ##STR00011## wherein Z is a side chain of formula IIB, IID or IIF: ##STR00012## wherein R.sup.5 and R.sup.6 are each hydrogen or taken together form a double bond between C-22 and C-23, R.sup.3, R.sup.9 and R.sup.10 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; R.sup.4 and R.sup.7 are independently lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; and R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl, lower fluoroalkenyl, lower cycloalkyl or taken together with the carbon to which they are bonded form a C.sub.3 C.sub.8 cyclocarbon ring; Y is a methyl group or hydrogen; and X is hydrogen, lower alkyl or lower fluoroalkyl.

3. A method of achieving an effect in a patient in need thereof comprising administering an effective amount of a vitamin D compound which is a 24-hydroxyvitamin D, wherein the effect is lowering or maintaining lowered parathyroid hormone levels, and wherein the 24-hydroxyvitamin D is a compound of formula (I): ##STR00013## wherein Z is a side chain of formula IIB, IID or IIF: ##STR00014## wherein R.sup.5 and R.sup.6 are each hydrogen or taken together form a double bond between C-22 and C-23, R.sup.3, R.sup.9 and R.sup.10 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; R.sup.4 and R.sup.7 are independently lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; and R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl, lower fluoroalkenyl, lower cycloalkyl or taken together with the carbon to which they are bonded form a C.sub.3 C.sub.8 cyclocarbon ring; Y is a methylene group if Y is double bonded to the A-ring or a methyl group or hydrogen if Y is single bonded; and X is hydrogen, lower alkyl or lower fluoroalkyl.

4. A method of achieving an effect in a patient in need thereof comprising administering an effective amount of a vitamin D compound which is a 24-hydroxyprevitamin D wherein the effect is lowering or maintaining lowered parathyroid hormone levels, wherein said 24-hydroxyprevitamin D is a compound of formula (III): ##STR00015## wherein Z is a side chain of formula IIB, IID or IIF: ##STR00016## wherein R.sup.5 and R.sup.6 are each hydrogen or taken together form a double bond between C-22 and C-23, R.sup.3, R.sup.9 and R.sup.10 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; R.sup.4 and R.sup.7 are independently lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; and R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl, lower fluoroalkenyl, lower cycloalkyl or taken together with the carbon to which they are bonded form a C.sub.3 C.sub.8 cyclocarbon ring; Y is a methyl group or hydrogen; and X is hydrogen, lower alkyl or lower fluoroalkyl.

5. A method of treating a human in need thereof to alleviate the pathological effects of hyperparathyroidism, wherein the method comprises administering to the human in need thereof a vitamin D compound which is a 24-hydroxyvitamin D of formula (I), wherein said compound is administered to the human in need thereof in an amount sufficient to lower or maintain lowered parathyroid hormone level in the human in need thereof; wherein formula (I) is: ##STR00017## wherein Z is a side chain of formula IIB, IID or IIF: ##STR00018## wherein R.sup.5 and R.sup.6 are each hydrogen or taken together form a double bond between C-22 and C-23, R.sup.3, R.sup.9 and R.sup.10 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; R.sup.4 and R.sup.7 are independently lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; and R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl, lower fluoroalkenyl, lower cycloalkyl or taken together with the carbon to which they are bonded form a C.sub.3 C.sub.8 cyclocarbon ring; Y is a methylene group if Y is double bonded to the A-ring or a methyl group or hydrogen if Y is single bonded; and X is hydrogen, lower alkyl or lower fluoroalkyl.

6. The method of claim 1, wherein said 24-hydroxyvitamin D compound is administered in a dosage of about 3.5 .mu.g to about 1000 .mu.g/week.

7. The method of claim 2 wherein Z is a side chain of formula (IIB).

8. The method of claim 7, wherein said 24-hydroxyprevitamin D is 24-hydroxyprevitamin D.sub.2; 24(S)-hydroxyprevitamin D.sub.2; 24-hydroxyprevitamin D.sub.4; or 24(R)-hydroxyprevitamin D.sub.4.

9. The method of claim 2 wherein Z is a side chain of formula (IID).

10. The method of claim 9 wherein said 24-hydroxyprevitamin D compound is 24-OH-25-ene-preD.sub.2.

11. The method of claim 1, wherein the effect is treating hyperparathyroidism.

12. The method of claim 1, wherein the vitamin D compound is 24-hydroxy-19-nor-vitamin D.

13. The method of claim 1, wherein the vitamin D compound is 24-hydroxyvitamin D.sub.2.

14. The method of claim 2, wherein the effect is treating hyperparathyroidism.

15. The method of claim 2, wherein the vitamin D compound is 24-hydroxyprevitamin D.sub.2.

16. The method of claim 3, wherein the effect is lowering or maintaining lowered parathyroid hormone level.

17. The method of claim 3, wherein the vitamin D compound is 24-hydroxy-19-nor-vitamin D.

18. The method of claim 3, wherein the vitamin D compound is 24-hydroxyvitamin D.sub.2.

19. The method of claim 4 wherein the effect is lowering or maintaining lowered parathyroid hormone level.

20. The method of claim 4, wherein the vitamin D compound is 24-hydroxyprevitamin D.sub.2.

21. The method of claim 5 wherein the method of treatment alleviates the pathological effects of hyperparathyroidism.

22. The method of claim 5 wherein the vitamin D compound is administered to the human in an amount sufficient to lower or maintain lowered parathyroid hormone level.

23. The method of claim 5, wherein the vitamin D compound is 24-hydroxy-19-nor-vitamin D.

24. The method of claim 5, wherein the vitamin D compound is 24-hydroxyvitamin D.sub.2.

25. The method of claim 5 wherein the Z side chain is formula IIB.

26. The method of claim 25, wherein said 24-hydroxyvitamin D is 24-hydroxyvitamin D.sub.2; 24(S)-hydroxyvitamin D.sub.2; 24-hydroxyvitamin D.sub.4; 24(R)-hydroxyvitamin D.sub.4.

27. The method of claim 5 wherein the Z side chain is formula IID.

28. The method of claim 5 wherein the Z side chain is formula IIF.

29. A method of treating a human in need thereof to alleviate the pathological effects of hyperparathyroidism, wherein the method comprises administering to the human in need thereof a vitamin D compound which is a 24-hydroxyprevitamin D of formula (III), wherein said compound is administered to the human in need thereof in an amount sufficient to lower elevated or maintain lowered parathyroid hormone level in the human in need thereof; wherein formula (III) is: ##STR00019## wherein Z is a side chain of formula IIB, IID or IIF: ##STR00020## wherein R.sup.5 and R.sup.6 are each hydrogen or taken together form a double bond between C-22 and C-23, R.sup.3, R.sup.9 and R.sup.10 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; R.sup.4 and R.sup.7 are independently lower alkyl, lower fluoroalkyl, lower alkenyl or lower fluoroalkenyl; and R.sup.1 and R.sup.2 are independently hydrogen, lower alkyl, lower fluoroalkyl, lower alkenyl, lower fluoroalkenyl, lower cycloalkyl or taken together with the carbon to which they are bonded form a C.sub.3 C.sub.8 cyclocarbon ring; Y is a methyl group or hydrogen; and X is hydrogen, lower alkyl or lower fluoroalkyl.

30. The method of claim 29 wherein the method of treatment alleviates the pathological effects of hyperparathyroidism.

31. The method of claim 29 wherein the Z side chain is formula IIB.

32. The method of claim 29, wherein said 24-hydroxyprevitamin D is 24-hydroxyprevitamin D.sub.2; 24(S)-hydroxyprevitamin D.sub.2; 24-hydroxyprevitamin D.sub.4; 24(R)-hydroxyprevitamin D.sub.4.

33. The method of claim 32, wherein the vitamin D compound is 24-hydroxyprevitamin D.sub.2.

34. The method of claim 29 wherein the Z side chain is formula IID.

35. The method of claim 29 wherein the Z side chain is formula IIF.
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