A compound having the structure of Formula I, wherein A is a substituted or unsubstituted aryl or heteroaryl group, D is a substituted or unsubstituted 5- or 6-membered heteroaryl or heterocyclyl group and E is a substituted or unsubstituted aryl, heteroaryl, cycloalkyl or heterocyclyl group. The compounds are used for the treatment of androgen modulated indications including cancer (prostate, breast, ovarian, endometrial or bladder cancer), hair loss, acne, hirsutism, ovarian cysts, polycystic ovary disease, precocious puberty and age related macular degeneration. The use of the compounds for the manufacture of a medicament for modulating AR activity, a method of treatment using such compounds and a pharmaceutical composition and a commercial package comprising said compounds are also described.

The University of British Columbia

Human androgen receptor DNA-binding domain (DBD) compounds as therapeutics and methods for their use

The present invention relates to compounds having at least one (substituted phenyl)-propenal moiety. The compounds are useful in treating a subject suffering from an androgen receptor-associated medical condition, e.g., inflammation, acne, alopecia, hirsutism, wound, Spinal and Bulbar Muscular Atrophy (SBMA, Kennedy's Disease), unwanted immune response, immune disorder, or cancer.

Allianz Pharmascience Ltd.

Compounds with (1E, 6E)-1,7-Bis-(3,4-dimethoxyphenyl)-4-4-distributed-hepta-1,6-diene-3,5-dio- ne structural scaffold, their biological activity, and uses thereof

This invention provides bisphenol derivatives having a structure of formula 1. Said compounds are modulators of the androgen receptor activity and are useful in the treatment of various diseases, including prostate cancer, breast cancer, ovarian cancer, endometrial cancer, acne, ovarian cysts, polycystic ovarian disease, age-related macular degeneration, precocious puberty, hirsutism and hair loss.

Sadar; Marianne D.

Mawji; Nasrin R.

Banuelos; Carmen Adriana

Andersen; Raymond J.

Fernandez; Javier Garcia

Brittish Columbia Cancer Agency Branch

Bisphenol derivatives and their use as androgen receptor activity modulators

Compounds having the structure or their salts: ##STR00001## are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia, male baldness, muscle atrophy and weakness, sarcopenia, male hypogonadism, erectile dysfunction, female sexual dysfunction and osteoporosis. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.

Labrie; Fernand

Singh; Shankar Mohan

Labrecque; Richard

Ciobanu; Liviu Constantin

ENDORECHERCHE, INC.

Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety

hirsutism

atrophy

hirsutism/atrophy

Human androgen receptor DNA-binding domain (DBD) compounds as therapeutics and methods for their use

Compounds with (1E, 6E)-1,7-Bis-(3,4-dimethoxyphenyl)-4-4-distributed-hepta-1,6-diene-3,5-dio- ne structural scaffold, their biological activity, and uses thereof

Bisphenol derivatives and their use as androgen receptor activity modulators

Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety

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