- Humanetics Corporation

Hollis-eden Pharmaceuticals, Inc.

Other

Harbor Biosciences, Inc.

Humanetic Corp.

Henry A Lardy

Padma Marwah

Ashok Marwah

Charles E Weeks

Yong Wei

Ieva L Reich

Jennifer Y Shi

Bruce E Partridge

Ashok Kumar Marwah

C David Pauza

The instant invention provides potent antiandrogen compounds, such as 3&#x3b2;-acetoxyandrost-1,5-diene-17-ethylene ketal and 3&#x3b2;-hydroxyandrost-1,5-diene-17-ethylene 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.

Diene and triene compounds and formulations

Diene compounds and formulations

Prostate cancer treatment

Steroids having 1,8-unsaturation and formulations comprising same

Lupus erythematosus can be treated by administering therapeutic amounts of &#x394;5-androstene-3&#x3b2;-ol-7,17-dione and metabolizable precursors thereof, such as &#x394;5-androstene-3b-acetoxy-7,17-dione, which are readily metabolized in vivo to &#x394;5-androstene-3&#x3b2;-ol-7,17-dione but are not appreciably metabolizable in vivo to androgens, estrogens or dehydroepiandrosterone. Such treatment can be prophylactic, ameliorative or curative in nature.

Use of &#x394;5-androstene-3&#x3b2;-ol-7,17-dione in the treatment of lupus erythematosus

A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of a periodic acid or metal periodate and an alkyl hydroperoxide under conditions of normal as well as elevated pressure of a suitable gas like air. The reaction can conveniently be conducted at temperatures between about 0-65&deg; C. in a cosolvent system of water and organic solvent(s).

Process for effecting allylic oxidation

Lupus erythematosus can be treated by administering therapeutic amounts of &Dgr;5-androstene-3&bgr;-ol-7,17-dione and metabolizable precursors thereof, such as &Dgr;5-androstene-3&bgr;-acetoxy-7,17-dione, which are readily metabolized in vivo to &Dgr;5-androstene-3&bgr;-ol-7,17-dione but are not appreciably metabolizable in vivo to androgens, estrogens or dehydroepiandrosterone. Such treatment can be prophylactic, ameliorative or curative in nature.

Use of &Dgr;5-androstene-3&bgr;ol-7,17-dione in the treatment of lupus erythematosus

The memory of a healthy mammal and the memory of a mammal with age impaired memory can be improved by administering an effective amount of &Dgr;5-Androstene-3&bgr;-ol-7,17-dione and 3&bgr; esters thereof.

Memory by the administration of &Dgr;5-androstene-3&bgr;-ol-7,17-dione and 3&bgr; esters

A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of an N-hydroxy dicarboxylic acid imide and a chromium-containing oxidant. The reaction can conveniently be conducted under ambient temperature and pressure conditions, and is conveniently conducted in a co-solvent system of water and organic solvent(s).

Process for effecting allylic oxidation using dicarboxylic acid imides and chromium reagents

Lupus erythematosus can be treated by administering therapeutic amounts of delta-5-androstene-3-beta-ol-7,17-dione and its metabolizable precursors, which are not appreciably metabolized in vivo to androgens, estrogens or dehydroepiandrosterone. Such treatment can be prophylactic, ameliorative or curative in nature.

Use of delta5-androstene-3beta-ol-7, 17-dione in the treatment of lupus erythematosus

The present invention is directed to a process for effecting the allylic oxidation of an allylic compound having at least two allylic hydrogen atoms on the same carbon atom into corresponding &agr;,&bgr;-unsaturated carbonyl compound, using a combination of a metal hypochlorite and an alkyl hydroperoxide in a mixture of suitable conventional organic solvent(s) and/or water at a temperature of between about &minus;5&deg; C. to &plus;25&deg; C.

Process for allylic oxidation using metal hypochlorite and alkyl hydroperoxide

The memory of a healthy mammal and the memory of a mammal with age impaired memory can be improved by administering an effective amount of .DELTA.5-Androstene-3.beta.-ol-7,17-dione and 3.beta. esters thereof.

Memory enhancement by the administration of

A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of a periodic acid or metal periodate and an alkyl hydroperoxide under conditions of normal as well as elevated pressure of a suitable gas like air. The reaction can conveniently be conducted at temperatures between about 0-65.degree. C. in a cosolvent system of water and organic solvent(s).

HIV-related weight loss, HIV-related cachexia and HIV-related wasting syndrome can be treated by administering therapeutic amounts of the steroid .DELTA.5-androstene-3.beta.-ol-7,17 dione and metabolizable precursors thereof, such as .DELTA.5-androstene-3.beta.-acetoxy-7,17 dione, which are readily metabolized in vivo to .DELTA.5 androstene-3.beta.-ol-7,17 dione. Such treatment can be prophylactic, modulatory, ameliorative or curative in nature.

Growing community of inventors

Madison, WI, United States of America

Henry A Lardy