Compounds are provided which are useful in the treatment of androgen
receptor-associated conditions, such as age-related diseases, which
compounds have the structure 1
wherein
R.sub.1 is hydrogen (H), alkyl or substituted alkyl, alkenyl or
substituted alkenyl, arylalkyl or substituted arylalkyl,
CO.sub.2R.sub.4a, CONR.sub.4aR.sub.4b, and CH.sub.2OR.sub.4a;
R.sub.2 is hydrogen (H), OR.sub.3, SR.sub.3, halo, NHR.sub.3,
NHCOR.sub.4c.sub..sub.1, NHCO.sub.2R.sub.4c.sub..sub.1,
NHCONR.sub.4cR.sub.4d and NHSO.sub.2R.sub.4c;
R.sub.3 in each functional group is hydrogen (H), alkyl or substituted
alkyl, CHF.sub.2, CF.sub.3 and CON.sub.4e;
R.sub.4, R.sub.4a, R.sub.4b, R.sub.4c, R.sub.4c.sub..sub.1, R.sub.4d,
R.sub.4e, R.sub.4f, R.sub.4g, or R.sub.4h in each functional group are
the same or different and are hydrogen(H), alkyl or substituted alkyl,
alkenyl or substituted alkenyl, alkynyl or substituted alkynyl,
cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl,
aryl or substituted aryl, or heteroaryl or substituted heteroaryl;
R.sub.5 and R.sub.5' are the same or different and are hydrogen(H), alkyl
or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or
substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or
substituted arylalkyl, aryl or substituted aryl, or heteroaryl or
substituted heteroaryl, wherein at least one of R.sub.5 and R.sub.5' is
hydrogen, or R.sub.5 and R.sub.5' taken together form a double bond with
oxygen (O), sulfur (S), NR.sub.7 or CR.sub.7R.sub.7';
where R.sub.7 and R.sub.7' are as defined herein;
G is an aryl, heterocyclo or heteroaryl group, wherein said group is mono-
or polycyclic, and which is optionally substituted; and
n is an integer of 1 or 2,
m is an integer of 1 or 2,
Z is oxygen (--O--) or NR.sub.4h,
a prodrug ester, all stereoisomers thereof and a pharmaceutically
acceptable salt.
A method for treating androgen receptor-associated conditions such as
age-related diseases is also provided.