US RE39,056 E1 · 4-Azasteroids for treatment of hyperandrogenic conditions

Abstract

Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.

Claims15

Dependent claims

A compound of structural formula I:

or a pharmaceutically acceptable salt or ester thereof, wherein:
R1 is selected from methyl and ethyl;
R2 is selected from:
(a) H, and
(b) C1-6 alkyl;
R3 is heteroaryl, either unsubstituted or substituted with one to three substituents independently selected from:
(1) halo (F, Cl, Br, I),
(2) C1-2 alkyl;
(3) trifluoromethyl,
(4) nitro,
(5) hydroxy,
(6) cyano,
(7) amino,
(8) C1-2 alkyloxy,
(9) phenyl, and
(10) heteroaryl;
and
R4 selected from:
(a) C1-4 alkyl,
(b) phenyl, and
(c) heteroaryl.

18 more elements

Dependencies are inferred from the claim text.

4-Azasteroids for treatment of hyperandrogenic conditions

Life of this patent

4-Azasteroids for treatment of hyperandrogenic conditions

Life of this patent

Abstract

Claims15