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US 4,735,960 AGranted
Aromatase inhibitors
AssigneeEli Lilly and Company
InventorsKenneth S. Hirsch, Charles D. Jones, Harold M. Taylor
Life of this patent
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Abstract
This invention provides a method of inhibiting aromatase and treating estrogen-dependent diseases in mammals by administering certain azole derivatives. Certain azole derivatives and their pharmaceutical formulations are also provided.
Claims12
A method of inhibiting aromatase in a mammal which comprises administering to said mammal an aromatase inhibiting amount of a compound of ##STR3## wherein:
- A is a 5-membered heterocyclic group containing at least one nitrogen atom beta to the point of attachment selected from the group consisting of 5-thiazolyl, 4-isothiazolyl, 5-isothiazolyl, 2-1,3,4-thiadiazolyl, 5-1,2,3-thiadiazolyl, 5-1,2,4-thiadiazolyl, 4-1,2,3-thiadiazolyl, and 3-1,2,5-thiadiazolyl;
- E and G are independently N or CH;
- and
- R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently hydrogen, halo, nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, or trifluoromethyl;
- and pharmaceutically acceptable salts thereof.
2 more elements
A method of treating estrogen-dependent diseases by inhibiting aromatase in a mammal which comprises administering to said mammal an effective amount of a compound of ##STR4## wherein:
- A is a 5-membered heterocyclic group containing at least one nitrogen atom beta to the point of attachment selected from the group consisting of 5-thiazolyl, 4-isothiazolyl, 5-isothiazolyl, 2-1,3,4-thiadiazolyl, 5-1,2,3-thiadiazolyl, 5-1,2,4-thiadiazolyl, 4-1,2,3-thiadiazolyl, and 3-1,2,5-thiadiazolyl;
- E and G are independently N or CH;
- and
- R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently hydrogen, halo, nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, or trifluoromethyl;
- and pharmaceutically acceptable salts thereof.
2 more elements
Dependencies are inferred from the claim text.