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1. 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 .

2. 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。

3. 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。

4. 发明申请

WO2004080467A3 METHOD OF TREATING AND PREVENTING HYPERPARATHYROIDISM WITH VITAMIN D2 OR D4 COMPOUNDS 审中-公开
标题翻译：维生素D2或D4化合物治疗和预防高血糖的方法
公开(公告)号：WO2004080467A3
公开(公告)日：2005-01-20
申请号：PCT/US2004003059
申请日：2004-02-04
申请人： BONE CARE INT INC , MAZESS RICHARD B , STRUGNELL STEPHEN A , KNUTSON JOYCE C
发明人： MAZESS RICHARD B , STRUGNELL STEPHEN A , KNUTSON JOYCE C
IPC分类号： A61K31/565 , A61K31/59 , A61K31/592 , A61K31/593 , A61K31/66 , A61K31/663 , A61K31/714 , A61K33/00 , A61K33/06 , A61K33/16 , A61K33/22 , A61K38/23 , A61K45/06 , A61P5/20 , C07C401/00
CPC分类号： A61K45/06 , A61K31/565 , A61K31/59 , A61K31/592 , A61K31/593 , A61K31/66 , A61K31/663 , A61K31/714 , A61K33/00 , A61K33/06 , A61K33/16 , A61K33/22 , A61K38/23 , C07C401/00 , A61K2300/00
摘要： This invention relates to a method for treating or preventing hyperthyroidism associated with chronic kidney disease by administering a sufficient amount of a vitamin D2 or vitamin D4 compound, the chronic kidney disease being stages 1-4.
摘要翻译：本发明涉及通过施用足量的维生素D 2或维生素D 4化合物来治疗或预防与慢性肾脏疾病相关的甲状腺功能亢进的方法，慢性肾脏病是1-4期。

5. 发明申请

WO2004082631A2 METHODS FOR PREPARATION AND USE OF 1alpha,24(S)-DIHYDROXYVITAMIN D2 审中-公开
标题翻译： 1α，24（S） - 二羟基维生素D2的制备和使用方法
公开(公告)号：WO2004082631A2
公开(公告)日：2004-09-30
申请号：PCT/US2004008136
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： A61K20060101 , A61K31/045 , A61K31/047 , A61K31/59 , A61K31/592 , A61K45/06 , A61P35/00 , A61P35/02 , C07C401/00 , C07J9/00 , C07J71/00 , A61K
CPC分类号： A61K31/047 , A61K31/59 , A61K31/592 , A61K45/06 , C07C401/00 , C07J9/00 , C07J71/0042 , A61K2300/00
摘要： A method of inhibiting the hyperproliferation of malignant or neoplastic cells, comprising treating the cells with an antiproliferative amount of lalpha,24(S)-dihydroxyvitamin D2. The method also includes the co-administration of cyotoxic agents with the 1alpha,24(S)-dihydroxyvitamin D2.
摘要翻译：一种抑制恶性或肿瘤细胞过度增殖的方法，包括用抗增殖量的α，24（S） - 二羟基维生素D2处理细胞。该方法还包括联合给予1α，24（S） - 二羟基维生素D2的细胞毒性试剂。

6. 发明申请

WO2004080467A2 METHOD OF TREATING AND PREVENTING HYPERPARATHYROIDISM WITH VITAMIN D COMPOUNDS 审中-公开
标题翻译：维生素D化合物治疗和预防高血糖病的方法
公开(公告)号：WO2004080467A2
公开(公告)日：2004-09-23
申请号：PCT/US2004/003059
申请日：2004-02-04
申请人： BONE CARE INTERNATIONAL, INC. , MAZESS, Richard, B. , STRUGNELL, Stephen, A. , KNUTSON, Joyce, C.
发明人： MAZESS, Richard, B. , STRUGNELL, Stephen, A. , KNUTSON, Joyce, C.
IPC分类号： A61K31/592
CPC分类号： A61K45/06 , A61K31/565 , A61K31/59 , A61K31/592 , A61K31/593 , A61K31/66 , A61K31/663 , A61K31/714 , A61K33/00 , A61K33/06 , A61K33/16 , A61K33/22 , A61K38/23 , C07C401/00 , A61K2300/00
摘要： This invention relates to a method for treating or preventing hyperthyroidism associated with chronic kidney disease by administering a sufficient amount of a vitamin D compound utilizing a variety of effective treatment protocols, the kidney disease being stages 1-4.
摘要翻译：本发明涉及通过使用多种有效治疗方案施用足够量的维生素D化合物来治疗或预防与慢性肾脏疾病相关的甲状腺功能亢进的方法，肾脏疾病是1-4期。

7. 发明申请

WO1992005130A1 NOVEL 1'alpha'-HYDROXY VITAMIN D4 AND NOVEL INTERMEDIATES AND ANALOGUES 审中-公开
标题翻译：新型1α-羟基维生素D4和新型中间体和类似物
公开(公告)号：WO1992005130A1
公开(公告)日：1992-04-02
申请号：PCT/US1991006865
申请日：1991-09-20
申请人： LUNAR CORPORATION , KNUTSON, Joyce, C. , BISHOP, Charles, W. , MORIARTY, Robert, M.
发明人： LUNAR CORPORATION
IPC分类号： C07C09/00
CPC分类号： A61K31/592 , C07C35/21 , C07C401/00
摘要： Novel 1 alpha -hydroxy vitamin D4 and novel analogues, 1,25 dihydroxy vitamin D4 and 1,24 dihydroxy vitamin D4 which are useful as active compounds of pharmaceutical compositions for the treatment of disorders of calcium metabolism. Preparation of the novel 1 alpha -hydroxy vitamin D4 starts from ergosterol which is converted in six steps to 22,23-dihydroergosterol. 22,23-dihydroergosterol was irradiated to yield vitamin D4 which is converted in four steps to 1 alpha -hydroxy vitamin D4 using a cyclovitamin procedure which produces the novel intermediates, vitamin D4 tosylate, 3,5 cyclovitamin D4 and 1 alpha -hydroxy cyclovitamin D4. 1,25 dihydroxy vitamin D4 and 1,24 dihydroxy vitamin D4 are isolated as biological products of the metabolism of novel 1 alpha -hydroxy vitamin D4 using cultured human liver cells.
摘要翻译：新型1α-羟基维生素D4和新型类似物，1,25二羟基维生素D4和1,24二羟基维生素D4，其可用作治疗钙代谢紊乱的药物组合物的活性化合物。新型1α-羟基维生素D4的制备从麦角甾醇开始，其被六步转化为22,23-二氢麦角甾醇。 22,23-二氢麦角甾醇被照射以产生维生素D4，其使用环维生素方法四步转化为1α-羟基维生素D4，其产生新的中间体维生素D4甲苯磺酸酯，3,5环维生素D4和1α-羟基环维生素D4 。使用培养的人肝细胞分离1,25二羟基维生素D4和1,24二羟基维生素D4作为新型1α-羟基维生素D4的代谢的生物产物。

8. 发明申请

WO2003088976A1 METHOD FOR TREATING AND PREVENTING HYPERPARATHYROIDISM 审中-公开
标题翻译：治疗和预防高尿酸血症的方法
公开(公告)号：WO2003088976A1
公开(公告)日：2003-10-30
申请号：PCT/US2003/012013
申请日：2003-04-17
申请人： BONE CARE INTERNATIONAL, INC. , MAZESS, Richard, B. , STRUGNELL, Stephen, A. , KNUTSON, Joyce, C.
发明人： MAZESS, Richard, B. , STRUGNELL, Stephen, A. , KNUTSON, Joyce, C.
IPC分类号： A61K31/59
CPC分类号： C07C401/00 , A61K31/565 , A61K31/59 , A61K31/592 , A61K31/593 , A61K31/663 , A61K31/714 , A61K33/16 , A61K33/22 , A61K45/06 , A61K2300/00
摘要： This invention relates to a method for treating or preventing hyperthyroidism associated with aging and/or with Aging-Related Vitamin D Deficiency (ARVDD) syndrome by administering a sufficient amount of an active vitamin D compound utilizing a variety of effective treatment protocols. The invention further relates to treating or preventing one or more of the following conditions, e.g., (1) primary vitamin D deficiency, (2) 1,25-(OH)2D3 deficiency, and (3) 1,25-(OH)2D3 resistance included within the syndrome of ARVDD.
摘要翻译：本发明涉及一种通过使用各种有效治疗方案施用足够量的活性维生素D化合物来治疗或预防与衰老相关的甲状腺功能减退和/或老化相关维生素D缺乏症（ARVDD）综合征的方法。本发明还涉及治疗或预防一种或多种以下病症，例如（1）初级维生素D缺乏症，（2）1,25-（OH）2D3缺乏症和（3）1,25-（OH）包括在ARVDD综合征内的2D3电阻。

9. 发明申请

WO1994000128A1 ORAL 1'alpha'-HYDROXYPREVITAMIN D 审中-公开
标题翻译：口服1α-羟基丙氨酸D
公开(公告)号：WO1994000128A1
公开(公告)日：1994-01-06
申请号：PCT/US1993005961
申请日：1993-06-22
申请人： LUNAR CORPORATION , KNUTSON, Joyce, C. , VALLIERE, Charles, R. , BISHOP, Charles, W.
发明人： LUNAR CORPORATION
IPC分类号： A61K31/59
CPC分类号： A61K31/593 , A61K9/5078 , A61K31/59 , A61K31/592 , A61K31/66 , A61K31/70 , A61K33/24 , A61K38/23 , A61K2300/00 , A61K31/565
摘要： Method of increasing activated vitamin D blood level by administering orally a 1 alpha -hydroxyprevitamin D or a delayed and sustained release formulation of activated vitamin D or a combination thereof. Both the previtamin D form and the delayed and sustained release activated vitamin D formulation increase vitamin D blood level without significant risk of hypercalcemia associated with other oral dosing of vitamin D forms.
摘要翻译：通过口服1α-羟基维生素D或活化维生素D的延迟和持续释放制剂或其组合来增加活化的维生素D血液水平的方法。维生素D组合物和延迟释放激活的维生素D制剂都能增加维生素D血浆水平，而与其他口服维生素D形式相关的高钙血症并不具有显着的风险。

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