Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes
AssigneeBiophysica, Inc.
InventorsMilos Sovak, Allen L. Seligson, James Gordon Douglass, III, Brian Campion, Jason W. Brown
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Abstract
Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in the therapy of indications associated with the androgen receptor, such as, hirsutism, acne and androgenetic alopecia, and in the therapy and diagnosis of cell hyperplasia dependent on androgens.
Claims7
A compound of the formula:
- wherein:
- X3 is nitro or cyano;
- V3 is CF3;
- n3 is 1 or 2;
- Q3 is chalcogen;
- when n is 1, Y3 is a bond or linking group of a total of from 1 to 6 atoms, which are C, N, O and S;
- and
- Z3 is polyfluoroacylamido of from 2 to 6 carbon atoms and at least 2m−2 fluorine atoms, wherein m is the number of carbon atoms, or haloanilino, where halo is of atomic number from 9 to 80;
- when n is 2, Y3 and Z3 are taken together to form a linking group of a total of 1 to 0 C., N, O, and S atoms.
A pharmaceutical formulation for treatment of an indication dependent upon activation of the androgen receptor comprising a compound of the formula:
- wherein:
- X3 is nitro or cyano;
- V3 is CF3;
- n3 is 1 or 2;
- Q3 is chalcogen;
- when n is 1, Y3 is a bond or linking group of a total of from 1 to 6 atoms, which are C, N, O, and S;
- and
- Z3 is alkyl of from 1 to 6 carbon atoms, polyfluoroacylamido of from 2 to 6 carbon atoms and at least 2m−2 fluorine atoms, wherein m is the number of carbon atoms, or haloanilino, where halo is of atomic number from 9 to 80;
- when n is 2, Y3 and Z3 are taken together to form a linking group of a total of 1 to 10 C., N, O, and S atoms, and a pharmacologically acceptable carrier.
Dependencies are inferred from the claim text.