A compound of formula: ##STR00001## wherein X is a C.sub.2-10 spacer, and R is a substituted or unsubstituted C.sub.6-30 aryl, a substituted or unsubstituted C.sub.5-30 heteroaryl, or ##STR00002## 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, a compound comprising same, and 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 aforementioned compound or composition, whereupon the patient is treated prophylactically or therapeutically for the disease.