ANTIANDROGENS WITH MARGINAL AGONIST ACTIVITY AND METHODS OF USE

WIPO Patent Application WO2004089304

A3

The instant invention provides potent antiandrogen compounds, such as 3beta -acetoxyandrost-1,5-diene-17-ethylene ketal and 3beta-hydroxyandrost-1, 5-diene-17ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

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LARDY HENRY A (US)
MARWAH ASHOK K (US)
MARWAH PADMA (US)

PCT/US2004/009739

May 06, 2005

March 30, 2004

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HOLLIS EDEN PHARMACEUTICALS (US)
LARDY HENRY A (US)
MARWAH ASHOK K (US)
MARWAH PADMA (US)

A61K31/4745; A61K31/58; C07D471/02; C07J1/00; C07J21/00; A61K; (IPC1-7): C07J1/00; C07J21/00; A61K31/58

SCHUBERT ET AL: "Stereospecific Hydrogenation of delta4-,delta1,delta4,6- and delta1,4,6-3-Ketosteroids by Clostridium Paraputrificum", STEROIDS, vol. 58, no. 1, 1965, pages 175 - 184, XP002985045

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