Bone Care International, Inc.

Lunar Corporation

Other

The United States of America As Represented by the Secretary of

Genzyme Corporation

Horst, Ronald L.

Koszewski, Nicholas J.

Reinhardt, Timothy A.

Joyce C Knutson

Charles W Bishop

Stephen Strugnell

Robert M Moriarty

Richard B Mazess

Charles R Valliere

Raju A Penmasta

Glenville Jones

Liang Guo

Lei Zhao

Ronald L Horst

Timothy A Reinhardt

Nicholas J Koszewski

Sanjay K Singhal

Sanjay K Singh-Al

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 a stabilized 1&#x3b1;-hydroxyvitamin D ('SHVD') which is particularly well suited for pharmaceutical formulations.

Stabilized hydroxyvitamin D

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

Method of treating prostatic diseases using active vitamin D analogues

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

A method for reducing or preventing elevated blood parathyroid hormone level in a human being suffering from primary hyperparathyroidism, secondary hyperparathyroidism, or hyperparathyroidism secondary to end stage renal disease by administering a sufficient amount of 1&agr;,24(S)-(OH) vitamin D .

Method for treating and preventing hyperparathyroidism

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      .

Method of treating or preventing osteoporosis by administering orally a 1.alpha.-hydroxyprevitamin D. This previtamin D form increases vitamin D blood level without significant risk of hypercalcemia associated with other oral dosing of vitamin D forms. The 1.alpha.-hydroxyprevitamin is compounded into a pharmaceutical composition in combination with a pharmaceutically acceptable excipient.

Method and composition for treating or preventing osteoporosis

Method of treating psoriasis by administering orally a 1.alpha.-hydroxyprevitamin D. This previtamin D form treats psoriasis without significant risk of hypercalcemia associated with other oral dosing of vitamin D forms. The 1.alpha.-hydroxyprevitamin is compounded into a pharmaceutical composition in combination with a pharmaceutically acceptable excipient.

Oral 1.alpha.-hydroxyprevitamin D in composition and method for treating

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

Method of increasing activated vitamin D blood level by administering orally a 1.alpha.-hydroxyprevitamin D. This previtamin D form increases vitamin D blood level without significant risk of hypercalcemia associated with other oral dosing of vitamin D forms. The 1.alpha.-hydroxyprevitamin is compounded into a pharmaceutical composition in combination with a pharmaceutically acceptable excipient.

Oral 1.alpha.-hydroxyprevitamin D in methods for increasing blood level

Disclosed is 1.alpha.,24-dihydroxy vitamin D.sub.4 having the following structure: ##STR1## and pharmaceutical compositions containing said compound. The compound and composition are useful in the treatment of abnormal calcium metabolism. Also Disclosed is a method for the preparation of 1.alpha.,24-dihydroxy vitamin D.sub.4.

1.alpha.-hydroxy vitamin D.sub.4 and novel intermediates and analogues

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.

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Madison, WI, United States of America

Joyce C Knutson