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1. (WO2003000634) VITAMIN D RECEPTOR ANTAGONISTS AND RELATED COMPOSITIONS AND METHODS OF USE
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WHAT IS CLAIMED IS:

1. A compound of formula:



wherein X is a C2-ιo spacer, and R is a substituted or unsubstituted C6-30 aryl, a substituted or unsubstituted C5-3o heteroaryl, or

O

II
C-N-R"
R'

where R' and R" are independently a substituted or unsubstituted aryl or a substituted or unsubstituted alkyl, wherein said compound is a vitamin D receptor (VDR) antagonist, with the proviso that, when X is CH2CH2; R is not 4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene.

The compound of claim 1, wherein X is CH2CH2 and R is:


The compound of claim 1, wherein X is CH2CH and R is:

The compound and R is:


The compound of claim 1, wherein X is CH2CH2 and R is:


The compound of claim 1, wherein X is CH2CH2 and R is:



1. A composition comprising the compound of any of claims 1 -5 and a carrier therefor.

8. The composition of claim 7, wherein the composition is a pharmaceutical composition and the carrier is pharmaceutically acceptable.

9. A pharmaceutical composition comprising a VDR-antagonizing effective amount of a compound of formula:

wherein X is a CH2CH2, and R is 4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene, and a pharmaceutically acceptable carrier.

10. A method of treating a patient for a disease that can be treated
prophylactically or therapeutically by administration of a VDR antagonist, which method comprises administering an effective amount of a compound of formula:



wherein X is a C2-10 spacer, and R is a substituted or unsubstituted C6-30 aryl, a substituted or unsubstituted C5-30 heteroaryl, or
O

II
— C-N-R"
I
R*

where R' and R" are independently a substituted or unsubstituted aryl or a substituted or unsubstituted alkyl, wherein said compound is a VDR antagonist, whereupon the patient is treated prophylactically or therapeutically for the disease.

11. The method of claim 10, wherein the disease is characterized by abnormal cellular proliferation.

12. The method of claim 11 , wherein the disease is cancer.

13. The method of claim 12, wherein the cancer is cancer of the breast, prostate, colon, rectum, or brain.

14. The method of claim 12, wherein the cancer is leukemia.

15. The method of claim 12, wherein the cancer is primary or metastatic melanoma.

16. The method of claim 12, wherein the cancer is glyoma.

17. The method of claim 10, wherein the disease is primary or secondary hyperparathyroidism.

18. The method of claim 10, wherein the disease is disease of the bone.

19. The method of claim 10, wherein the disease is vascular calcification.

20. The method of claim 10, wherein the disease is renal failure or kidney stones.

21. The method of claim 10, wherein the disease is psoriasis.