Endorecherche, Inc.

Shankar Mohan Singh

Fernand Labrie

Yves M Merand

Rock Breton

Sylvain Gauthier

Van Luu-The

René Maltais

Donald Poirier

Alain Belanger

Richard Labrecque

Liviu Constantin Ciobanu

Yvon Frechette

Sylvain Chenard

Rene Maltais

Louis Provencher

Compounds having the structure or their salts: 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.

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

Compounds having the structure or their salts: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Some of these compounds having tissue-specific antiandrogenic activity and tissue-specific androgenic activity can be used to treat or reduce the risk of developing diseases related to loss of androgenic stimulation. Combinations with other active pharmaceutical agents are also disclosed.

Helix 12 directed pharmaceutical products

Compounds having the structure (or their salts): 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 and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.

Helix 12 directed non-steroidal antiandrogens

Biphenyl derivatives are disclosed for use in the treatment of androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, precocious puberty, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and premature male baldness. For example, some preferred compounds having the structure:are formulated together with pharmaceutically acceptable diluent or carrier for topical use in the treatment of acne, hirutism, seborrhea or androgenic alopecia, or for systemic use in the treatment of androgen-dependent prostate cancer.

Antiandrogenic biphenyls

Novel methods of medical treatment and/or inhibition of development of diseases are disclosed for diseases that are sensitive to androgenic or estrogenic activity. The treatments utilize inhibitors of type 5 and/or type 3 17&bgr;-hydroxysteroid dehydrogenase. Novel inhibitors of type 5 17&bgr;-hydroxysteroid dehydrogenase are also disclosed, as are novel inhibitors of type 3 17&bgr;-hydroxysteroid dehydrogenase.

Inhibitors of type 5 and type 3 17&bgr;-hydroxysteroid dehydrogenase and methods for their use

Androgen nucleus derivatives having specified substituents at the 17.alpha. position are disclosed for use as antiandrogens for the treatment of androgen-dependent diseases. In some preferred embodiments, the compound ##STR1## is formulated together with pharmaceutically acceptable diluent or carrier for topical use in the treatment of androgen-dependent diseases associated with the skin.

Antiandrogens

Inhibitors of testosterone 5.alpha.-reductase activity, for example those of formula: ##STR1## wherein novel substituents are provided at the R.sup.4, R.sup.6, R.sup.7, R.sup.17.alpha. and/or R.sup.17.beta. positions are useful for the treatment of diseases whose progress is aided by activation of androgen receptors, e.g., prostate cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, androgenic alopecia and the like.

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Shankar Mohan Singh