Irreversible inhibition of human 5.alpha.-reductase
AssigneeMerck & Co., Inc.
InventorsHerb G. Bull, Georgianna S. Harris
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Abstract
The invention concerns the treatment of hyderandrogenic conditions in humans by the formation of a novel mechanism-based irreversible inhibitor of human 5.alpha.-reductase enzymes from 3-oxo-4-azasteroids having a 1,2-double bond and the pyridine-nucleotide cofactor of the 5.alpha.-reductase enzyme, NADPH. Until the present invention, it was not know or predicted that 3-oxo-4-azasteroids having 1,2-double bond would form a complex with NADPH by the mechanism of 5.alpha.-reductase in vivo. The invention further relates to the novel inhibitor-cofactor complex and pharmaceutical compositions containing the complex.
Claims2
A method for irreversibly inhibiting human 5.alpha.-reductase in a human without covalently modifying the 5.alpha.-reductase enzyme, which comprises the administration to the human of a 3-oxo-4-azasteroid having a 1,2 double bond and a hydrogen substituent on the 4-nitrogen, provided that the 3-oxo-4-azasteroid having a 1,2 double bond and a hydrogen substituent on the 4-nitrogen is not:
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Dependencies are inferred from the claim text.