This invention provides androgen receptor targeting agents (ARTA). The
agents define a new subclass of compounds, which are selective androgen
receptor modulators (SARM). Several of the SARM compounds have been found
to have an unexpected androgenic and anabolic activity of a nonsteroidal
ligand for the androgen receptor. Other SARM compounds have been found to
have an unexpected antiandrogenic activity of a nonsteroidal ligand for
the androgen receptor. The SARM compounds, either alone or as a
composition, are useful for a) male contraception; b) treatment of a
variety of hormone-related conditions, for example conditions associated
with Androgen Decline in Aging Male (ADAM), such as fatigue, depression,
decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism,
osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,
osteoporosis, benign prostate hyperplasia, alterations in mood and
cognition and prostate cancer; c) treatment of conditions associated with
Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased
sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis,
alterations in cognition and mood, depression, anemia, hair loss,
obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer;
d) treatment and/or prevention of acute and/or chronic muscular wasting
conditions; e) preventing and/or treating dry eye conditions; f) oral
androgen replacement therapy; and/or g) decreasing the incidence of,
halting or causing a regression of prostate cancer.