Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1982-08-06
1987-03-24
Roberts, Elbert L.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
2603972, 514167, C07J 900
Patent
active
046524053
ABSTRACT:
1.alpha.,25-Dihydroxy-24R-fluorocholecalciferol and 1.alpha.,25-dihydroxy-24S-fluorocholecalciferol, analogs of 1.alpha.,25-dihydroxy-cholecalciferol which is physiologically the most active metabolite of vitamin D.sub.3, are synthesized in a multistep process from the known substance 1.alpha.,3.beta.-dihydroxyandrost-5-en-17-one. The new analogs are characterized by the ability to increase intestinal calcium transport, increase serum calcium and phosphate concentrations and to increase the deposition of these minerals in bones. These compounds will find a ready application as substitutes for natural 1.alpha.,25-dihydroxycholecalciferol in the treatment of disease states characterized by metabolic calcium and phosphate deficiencies. Exemplary of such disease states are the following: osteosclerosis, anticonvulsant treatment, osteopenia, fibrogenesis-imperfecta ossium, secondary hyperparathyrodism, hypoparathyroidism, hyperparathyroidism, cirrhosis, obstructive jaundice, drug induced metabolism, medullary carcinoma, chronic renal disease, hypophosphatemic VDRR, vitamin D-dependent rickets, sarcoidosis, glucocorticoid antagonism, malabsorption syndrome, steatorrhea, tropical sprue, idiopathic hypercalcemia and milk fever.
REFERENCES:
patent: 3847955 (1974-11-01), DeLuca
patent: 4229357 (1980-10-01), DeLuca et al.
patent: 4428946 (1984-01-01), DeLuca et al.
Partridge John J.
Shiuey Shian-Jan
Uskokovic Milan R.
Boxer Mathew
Hoffman-La Roche Inc.
Leon Bernard S.
Roberts Elbert L.
Saxe Jon S.
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