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1. 发明申请

WO2008008608A3 METHOD OF TREATING AND PREVENTING SECONDARY HYPERPARATHYROIDISM 审中-公开
公开(公告)号：WO2008008608A3
公开(公告)日：2008-01-17
申请号：PCT/US2007/071791
申请日：2007-06-21
申请人： PROVENTIV THERAPEUTICS, LLC , CYTOCHROMA INC. , BISHOP, Charles, W. , CRAWFORD, Keith, H. , MESSNER, Eric, J. , PETKOVICH, Martin, P. , HELVIG, Christian, F.
发明人： BISHOP, Charles, W. , CRAWFORD, Keith, H. , MESSNER, Eric, J. , PETKOVICH, Martin, P. , HELVIG, Christian, F.
IPC分类号： A61K31/59 , A61P5/20
摘要： A method of treating elevated blood levels of iPTH by increasing or maintaining blood concentrations of both 25 -hydroxy vitamin D and 1, 25-dihydroxyvitamin D in a patient by administering, as necessary, both Vitamin D repletion and Vitamin D hormone replacement therapies, is disclosed. The blood concentrations of 25 -hydroxy vitamin D are increased to and maintained at or above 30 ng/mL, and blood concentrations of 1, 25-dihydroxyvitamin D are increased to or maintained within a patient's normal historical physiological range for 1, 25-dihydroxyvitamin D without causing substantially increased risk of hypercalcemia, hyperphosphatemia or over suppression of plasma iPTH in the patient. The blood levels of 25- hydroxyvitamin D are maintained at or above 30 ng/mL between doses of Vitamin D repletion therapies, and the blood levels of 1, 25-dihydroxyvitamin D are maintained in the patient's normal historical physiological range between doses of Vitamin D hormone replacement therapies. In one aspect, the disclosure includes methods wherein the blood concentration of 25- hydroxyvitamin D during treatment comprises predominantly 25 -hydroxy vitamin D3, and/or wherein the method includes administering predominantly or solely 25-hydroxyvitamin D3 for 25 -hydroxy vitamin D repletion and/or maintenance

2. 发明申请

WO2007092755A2 TREATING VITAMIN D INSUFFICIENCY AND DEFICIENCY WITH 25-HYDROXYVITAMIN D2 AND 25-HYDROXYVITAMIN D3 审中-公开
标题翻译：用25羟维生素D2和25-羟维生素D3处理维生素D缺乏症和缺乏症
公开(公告)号：WO2007092755A2
公开(公告)日：2007-08-16
申请号：PCT/US2007/061521
申请日：2007-02-02
申请人： PROVENTIV THERAPEUTICS, LLC , BISHOP, Charles, W. , CRAWFORD, Keith, H. , MESSNER, Eric, J.
发明人： BISHOP, Charles, W. , CRAWFORD, Keith, H. , MESSNER, Eric, J.
IPC分类号： A61K31/592 , A61K31/593 , A61K9/20 , A61P3/02
CPC分类号： A61K31/593 , A61K9/00 , A61K9/0019 , A61K9/16 , A61K9/48 , A61K9/4808 , A61K9/4858 , A61K9/4866 , A61K9/4875 , A61K31/592 , A61K47/26
摘要： Methods and compositions for treating 25-hydiOxyvitamin D insufficiency and deficiency in a patient are described herein. The method includes orally administering to the patient a delayed, sustained release formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D 2 , 25-hydroxyvitamin D 3 , or a combination of 25-hydroxyvitamin D 2 and 25-hydroxyvitamin D 3 , or it inchides gradually administering to the patient an sterile intravenous formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D 2 , 25- hydroxyvitamin D 3 , or a combination of 25-hydroxyvitamin D 2 and 25-hydroxyvitamin D 3 .
摘要翻译：本文描述了用于治疗患者的25-羟基维生素D不足和缺乏症的方法和组合物。该方法包括口服给予患者延迟的持续释放制剂，其包括选自25-羟基维生素D 2，25-羟基维生素D 3 N，或25-羟基维生素D 2和25-羟基维生素D 3 3的组合，或其逐渐向患者施用无菌静脉内制剂，其包括选自下组的第一成分由25-羟基维生素D 2 H 2，25-羟基维生素D 3 3或25-羟基维生素D 2和25-羟基维生素D 2的组合组成， SUB> 3 。

3. 发明申请

WO2007047327A3 METHODS AND ARTICLES FOR TREATING 25-HYDROXYVITAMIN D INSUFFICIENCY AND DEFICIENCY 审中-公开
公开(公告)号：WO2007047327A3
公开(公告)日：2007-04-26
申请号：PCT/US2006/039787
申请日：2006-10-12
申请人： PROVENTIV THERAPEUTICS, LLC , BISHOP, Charles, W. , CRAWFORD, Keith, H. , MESSNER, Eric, J.
发明人： BISHOP, Charles, W. , CRAWFORD, Keith, H. , MESSNER, Eric, J.
IPC分类号： A61K9/16 , A61K9/48 , A61K31/593 , A61K31/59 , A61K45/06
摘要： A controlled-release phaπnaceutical formulation including cholecalciferol and/or ergocalciferol, a method of making the formulation, and a method of administering the formulation to treat 25-hydroxyvitamin D insufficiency or deficiency, are disclosed. The composition and method of administration preferably result in delayed release of the • vitamin(s) in the ileum of the small intestine and sustained, substantially constant, release of the vitamin(s) over an extended period, e.g., at least 4 hours or more. Individual and combined dosages of 500 IU to 50,000 IU per dosage form, preferably daily, are disclosed. The compositions and methods are contemplated to exhibit one or more advantages including, but not limited to efficiency of vitamin D repletion and maintenance; mitigation or avoidance of first pass effects of the Vitamin D compounds on the duodenum; mitigation or avoidance of adverse supraphysiological surges in intralumenal, intracellular and blood levels of cholecalciferol, ergocalciferol and 25- hydroxyvitamin D and their consequences; and mitigation or avoidance of serious side effects associated with Vitamin D supplementation, namely Vitamin D toxicity.

4. 发明申请

WO2004082631A3 METHODS FOR PREPARATION AND USE OF 1α,24(S)-DIHYDROXYVITAMIN D2 审中-公开
公开(公告)号：WO2004082631A3
公开(公告)日：2004-09-30
申请号：PCT/US2004/008136
申请日：2004-03-16
申请人： BONECARE INTERNATIONAL, INC. , BISHOP, Charles, W. , KNUTSON, Joyce, C. , STRUGNELL, Stephen , MAZESS, Richard, B.
发明人： BISHOP, Charles, W. , KNUTSON, Joyce, C. , STRUGNELL, Stephen , MAZESS, Richard, B.
IPC分类号： A61K31/045
摘要： A method of inhibiting the hyperproliferation of malignant or neoplastic cells, comprising treating the cells with an antiproliferative amount of lα,24(S)-dihydroxyvitamin D 2 . The method also includes the co-administration of cyotoxic agents with the 1α,24(S)-dihydroxyvitamin D 2 .

5. 发明申请

WO0206218A3 STABILIZED 1 alpha -HYDROXY VITAMIN D 审中-公开
标题翻译：稳定的1α-羟基维生素D
公开(公告)号：WO0206218A3
公开(公告)日：2002-07-18
申请号：PCT/US0122729
申请日：2001-07-18
申请人： BONE CARE INT INC , KNUTSON JOYCE C , MAZESS RICHARD B , BISHOP CHARLES W
发明人： KNUTSON JOYCE C , MAZESS RICHARD B , BISHOP CHARLES W
IPC分类号： A61K31/59 , A61K31/592 , A61K31/593 , A61P3/02 , C07C401/00
CPC分类号： C07C401/00 , A61K31/59
摘要： The invention provides a stabilized 1 alpha -hydroxy vitamin D ("SHVD") which is particularly well suited for pharmaceutical formulations.
摘要翻译：本发明提供了稳定的1α-羟基维生素D（“SHVD”），其特别适用于药物制剂。

6. 发明申请

WO1992012165A1 METHODS FOR PREPARATION AND USE OF 1'alpha',24-DIHYDROXY VITAMIN D2 审中-公开
标题翻译： 1α，24-二羟基维生素D 2的制备和使用方法
公开(公告)号：WO1992012165A1
公开(公告)日：1992-07-23
申请号：PCT/US1992000313
申请日：1992-01-07
申请人： LUNAR CORPORATION , BISHOP, Charles, W. , JONES, Glenville , KNUTSON, Joyce, C. , MORIARTY, Robert, M. , PENMASTA, Raju , STRUGNELL, Stephen
发明人： LUNAR CORPORATION
IPC分类号： C07J75/00
CPC分类号： A61K31/59 , A61K31/592 , A61K45/06 , C07C401/00 , C07J9/00 , C07J71/0042 , A61K2300/00
摘要： 1 alpha ,24-dihydroxy vitamin D2 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-dihydroxy vitamin D2 starting from ergosterol which is converted in six steps to 24-hydroxyergosterol. 24-hydroxyergosterol is irradiated and thermally converted to 24-hydroxy vitamin D2 which is converted in five steps to 1 alpha ,24-dihydroxy vitamin D2. The syntheses also produce novel intermediates.
摘要翻译： 1α，24-二羟基维生素D 2，其可用作用于治疗钙代谢紊乱和各种皮肤病症的药物组合物的活性化合物。本发明还包括从麦角甾醇开始合成的1α，24-二羟基维生素D2的制备，其将六步转化为24-羟基麦角固醇。将24-羟基麦角固醇照射并热转化成24-羟基维生素D2，其以5步转化为1α，24-二羟基维生素D2。这些合成物也产生新的中间体。

7. 发明申请

WO2008134518A2 METHODS AND COMPOUNDS FOR VITAMIN D THERAPY 审中-公开
标题翻译：维生素D治疗方法与化合物
公开(公告)号：WO2008134518A2
公开(公告)日：2008-11-06
申请号：PCT/US2008/061586
申请日：2008-04-25
申请人： CYTOCHROMA INC. , PROVENTIV THERAPEUTICS, LLC , PETKOVICH, P., Martin , BISHOP, Charles, W. , MESSNER, Eric, J. , CRAWFORD, Keith, H.
发明人： PETKOVICH, P., Martin , BISHOP, Charles, W. , MESSNER, Eric, J. , CRAWFORD, Keith, H.
IPC分类号： A61K31/593
CPC分类号： A61K31/592 , A61K9/0019 , A61K9/0053 , A61K47/14 , A61K47/44
摘要： Methods and compositions comprising 1,25-dihydroxyvitamin D 2 are disclosed. A method for lowering or maintaining lowered serum parathyroid hormone in human patients including administering to said patients an effective amount of 1,25-dihydroxyvitamin D 2 to lower or maintain lowered serum parathyroid hormone levels is disclosed. Dosage forms and dosing regimens are also disclosed.
摘要翻译：公开了包含1,25-二羟基维生素D 2 N 2的方法和组合物。一种降低或维持人类患者血清甲状旁腺激素降低或降低的方法，包括向所述患者施用有效量的1,25-二羟基维生素D 2以降低或维持降低的血清甲状旁腺激素水平。还公开了剂量形式和给药方案。

8. 发明申请

WO2008134512A1 ORAL CONTROLLED RELEASE COMPOSITIONS COMPRISING VITAMIN D COMPOUND AND WAXY CARRIER 审中-公开
标题翻译：包含维生素D化合物和卵泡载体的口服对照释放组合物
公开(公告)号：WO2008134512A1
公开(公告)日：2008-11-06
申请号：PCT/US2008/061579
申请日：2008-04-25
申请人： CYTOCHROMA INC. , PROVENTIV THERAPEUTICS, LLC , TABASH, Samir, P. , WHITE, Jay, A. , BISHOP, Charles, W.
发明人： TABASH, Samir, P. , WHITE, Jay, A. , BISHOP, Charles, W.
IPC分类号： A61K9/48 , A61K31/593 , A61K47/06 , A61K47/14 , A61K47/44
CPC分类号： A61K9/48 , A61K9/0019 , A61K9/0053 , A61K9/4825 , A61K9/4858 , A61K9/4866 , A61K31/59 , A61K31/593 , A61K47/06 , A61K47/10 , A61K47/14 , A61K47/44
摘要： A stable, controlled release formulation for oral dosing of vitamin D compounds is disclosed. The formulation is prepared by incorporating one or more vitamin D compounds into a solid or semi-solid mixture of waxy materials. Oral dosage forms can be prepared by melt-blending the components described herein and filling gelatin capsules with the formulation.
摘要翻译：公开了用于口服给药维生素D化合物的稳定的控释制剂。通过将一种或多种维生素D化合物掺入蜡状材料的固体或半固体混合物中来制备制剂。口服剂型可以通过将本文所述的组分熔融共混并用制剂填充明胶胶囊来制备。

9. 发明申请

WO2007092755A3 TREATING VITAMIN D INSUFFICIENCY AND DEFICIENCY WITH 25-HYDROXYVITAMIN D2 AND 25-HYDROXYVITAMIN D3 审中-公开
标题翻译： 25-羟维生素D2和25-羟维生素D3处理维生素D不足和缺乏
公开(公告)号：WO2007092755A3
公开(公告)日：2007-09-27
申请号：PCT/US2007061521
申请日：2007-02-02
申请人： PROVENTIV THERAPEUTICS LLC , BISHOP CHARLES W , CRAWFORD KEITH H , MESSNER ERIC J
发明人： BISHOP CHARLES W , CRAWFORD KEITH H , MESSNER ERIC J
IPC分类号： A61K31/592 , A61K9/20 , A61K31/593 , A61P3/02 , A61P19/08
CPC分类号： A61K31/593 , A61K9/00 , A61K9/0019 , A61K9/16 , A61K9/48 , A61K9/4808 , A61K9/4858 , A61K9/4866 , A61K9/4875 , A61K31/592 , A61K47/26
摘要： Methods and compositions for treating 25-hydiOxyvitamin D insufficiency and deficiency in a patient are described herein. The method includes orally administering to the patient a delayed, sustained release formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D 2 , 25-hydroxyvitamin D 3 , or a combination of 25-hydroxyvitamin D 2 and 25-hydroxyvitamin D 3 , or it inchides gradually administering to the patient an sterile intravenous formulation including a first ingredient selected from the group consisting of 25-hydroxyvitamin D 2 , 25- hydroxyvitamin D 3 , or a combination of 25-hydroxyvitamin D 2 and 25-hydroxyvitamin D 3 .
摘要翻译：本文描述了用于治疗患者中的25-羟基维生素D不足和缺乏的方法和组合物。该方法包括对患者口服给药延迟的缓释制剂，该制剂包含选自25-羟基维生素D 2，25-羟基维生素D 3，25-羟基维生素D 3，或者25-羟基维生素D 2和25-羟基维生素D 3的组合，或者其逐渐向患者施用包含选自组的第一成分的无菌静脉制剂其由25-羟基维生素D 2，25-羟基维生素D 3或25-羟基维生素D 2和25-羟基维生素D 3的组合组成， SUB> 3 。

10. 发明申请

WO2007047327A2 METHODS AND ARTICLES FOR TREATING 25-HYDROXYVITAMIN D INSUFFICIENCY AND DEFICIENCY 审中-公开
标题翻译：治疗25-羟维生素D缺乏症和缺乏症的方法和文章
公开(公告)号：WO2007047327A2
公开(公告)日：2007-04-26
申请号：PCT/US2006039787
申请日：2006-10-12
申请人： PROVENTIV THERAPEUTICS LLC , BISHOP CHARLES W , CRAWFORD KEITH H , MESSNER ERIC J
发明人： BISHOP CHARLES W , CRAWFORD KEITH H , MESSNER ERIC J
IPC分类号： A61K31/59 , A61K31/593 , A61K45/06 , A61P43/00
CPC分类号： A61K31/59 , A61K9/4841 , A61K9/4858 , A61K9/4875 , A61K9/4891 , A61K31/593 , A61K45/06 , A61K2300/00
摘要： A controlled-release phapnaceutical formulation including cholecalciferol and/or ergocalciferol, a method of making the formulation, and a method of administering the formulation to treat 25-hydroxyvitamin D insufficiency or deficiency, are disclosed. The composition and method of administration preferably result in delayed release of the vitamin(s) in the ileum of the small intestine and sustained, substantially constant, release of the vitamin(s) over an extended period, e.g., at least 4 hours or more. Individual and combined dosages of 500 IU to 50,000 IU per dosage form, preferably daily, are disclosed. The compositions and methods are contemplated to exhibit one or more advantages including, but not limited to efficiency of vitamin D repletion and maintenance; mitigation or avoidance of first pass effects of the Vitamin D compounds on the duodenum; mitigation or avoidance of adverse supraphysiological surges in intralumenal, intracellular and blood levels of cholecalciferol, ergocalciferol and 25- hydroxyvitamin D and their consequences; and mitigation or avoidance of serious side effects associated with Vitamin D supplementation, namely Vitamin D toxicity.
摘要翻译：公开了包括胆钙化甾醇和/或麦角钙化醇的控释药物制剂，制备方法和施用该制剂以治疗25-羟基维生素D不足或不足的方法。组合物和给药方法优选地导致维生素在小肠回肠中的延迟释放和持续的，基本上恒定的维生素释放在延长的时间内，例如至少4小时或更长时间。公开了每剂量形式的500IU至50,000IU的个体和组合剂量，优选每天。预期组合物和方法表现出一个或多个优点，包括但不限于维生素D补充和维持的效率; 缓解或避免维生素D化合物对十二指肠的首过效应; 缓解或避免胆钙化醇，麦角钙化醇和25-羟基维生素D的肠内，细胞内和血液中的不良超生理波动及其后果; 并减轻或避免与维生素D补充相关的严重副作用，即维生素D毒性。

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