Bone Care International, Inc.

Other

The United States of America As Represented by the Secretary of

Genzyme Corporation

Stephen Strugnell

Charles W Bishop

Joyce C Knutson

Glenville Jones

Robert M Moriarty

Raju A Penmasta

Liang Guo

Lei Zhao

Ronald L Horst

Timothy A Reinhardt

Nicholas J Koszewski

Sanjay K Singhal

Richard B Mazess

Don Wigington

The invention provides 24-hydroxyvitamin D compounds and methods for their use in the treatment and prophylaxis of hyperparathyroidism and hyperproliferative diseases, and in the modulation of the immune and inflammatory responses as well as the treatment of bone depletive disorders.

24-hydroxyvitamin D, analogs and uses thereof

The invention provides therapeutic methods for inhibiting, ameliorating or alleviating the hyperproliferative cellular activity of diseases of the breast, e.g., breast cancer, which includes administering to a patient in need thereof an active vitamin D analogue and another anticancer agent. Cell differentiation is promoted, induced or enhanced without causing to the patient dose-limiting hypercalcemia and hypercalciuria.

Method of treating breast cancer using a combination of vitamin D analogues and other agents

A method of inhibiting the hyperproliferation of malignant or neoplastic cells, comprising treating the cells with an antiproliferative amount of 1&agr;,24(S)-dihydroxyvitamin D . The method also includes the co-administration of cyotoxic angents with the 1&agr;,24(S)-dihydroxyvitamin D .

Methods for preparation and use of 1&agr;,24(S)-dihydroxyvitamin D2

1&agr;,24(S)-Dihydroxy vitamin D,which is useful as an active compound of pharmaceutical compositions for the treatment of disorders of calcium metabolism and for various skin disorders. The invention also includes preparation of synthetic 1&agr;,24(S)-dihydroxy vitamin D,starting from ergosterol which is converted in six steps to 24-hydroxyergosterol. 24-Hydroxyergosterol is irradiated and thermally converted to 24-hydroxy vitamin D,which is converted in six steps to 1&agr;,24(S)-dihydroxy vitamin D,. The syntheses also produced novel intermediates.

Methods for preparation and use of 1&agr;,24(S)-dihydroxy vitamin D2

Methods for preparation and use of 1&agr;,24 (S)-dihydroxy vitamin D2

1.alpha.,24(S)-Dihydroxy vitamin D.sub.2 which is useful as an active compound of pharmaceutical compositions for the treatment of disorders of calcium metabolism and for various skin disorders. The invention also includes preparation of synthetic 1.alpha.,24(S)-dihydroxy vitamin D.sub.2 starting from ergosterol which is converted in six steps to 24-hydroxyergosterol. 24-Hydroxyergosterol is irradiated and thermally converted to 24-hydroxy vitamin D.sub.2 which is converted in six steps to 1.alpha.,24(S)-dihydroxy vitamin D.sub.2. The syntheses also produced novel intermediates.

Methods for preparation and use of 1.alpha.,24(S)-Dihydroxy vitamin      .

Methods for preparation and use of 1.alpha., 24(S) -dihydroxy vitamin D2

The invention provides 1.alpha.-hydroxyvitamin D compounds in which the C-25 or equivalent position of the C-17 side chain has a double bond and method for their use in the treatment and prophylaxis of hyperparathyroidism and hyperproliferative diseases, and in the modulation of the immune and inflammatory responses as well as the treatment of bone depletive disorders.

1 .alpha.-hydroxy-25-ene-vitamin D, analogs and uses thereof

Methods for preparation and use of 1A,24(S)-dihydroxy vitamin D2

Methods for preparation and use of 1.alpha.,24(S)-dihydroxy vitamin D.sub.2

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Madison, WI, United States of America

Stephen Strugnell