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1. 发明申请

US20050187201A1 Use of 2-methylene-19-nor-20(S)-1alpha,25-dihydroxyvitamin D3 for the prophylaxis of bone diseases 有权
标题翻译：使用2-亚甲基-19-nor-20（S）-1α，25-二羟基维生素D 3用于预防骨疾病
公开(公告)号：US20050187201A1
公开(公告)日：2005-08-25
申请号：US10782337
申请日：2004-02-19
申请人： Hector DeLuca , Lori Plum , Margaret Clagette-Dame
发明人： Hector DeLuca , Lori Plum , Margaret Clagette-Dame
IPC分类号： A61K31/59 , A61K31/593
CPC分类号： A61K31/593 , A61K31/59
摘要： This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3. This compound is characterized by high bone calcium mobilization activity demonstrating preferential activity on bone. This results in a novel therapeutic agent for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis. This compound also increases both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements, as well as use by normal subjects when high bone mass is desired.
摘要翻译：本发明提供2-亚甲基-19-去甲-20（S）-1α，25-二羟基维生素D 3 N的药用。该化合物的特征在于高骨钙动员活性，表现出骨优先活性。这导致用于治疗和预防需要骨形成的疾病，特别是骨质疏松症的新型治疗剂。这种化合物还增加骨骼的断裂强度和破碎强度，这些骨骼与骨替代手术如髋关节和膝关节置换术一起使用，以及在需要高骨质量时由正常受试者使用。

2. 发明申请

US20050065123A1 Use of 2-Methylene-19-nor-20(S)-1alpha,25-dihydroxyvitamin D3 to increase the life expectancy of human beings 有权
标题翻译：使用2-亚甲基-19-nor-20（S）-1α，25-二羟基维生素D 3以增加人的预期寿命
公开(公告)号：US20050065123A1
公开(公告)日：2005-03-24
申请号：US10669990
申请日：2003-09-24
申请人： Hector DeLuca , Lori Plum , Margaret Clagette-Dame
发明人： Hector DeLuca , Lori Plum , Margaret Clagette-Dame
IPC分类号： A61K31/593 , A61P35/00 , A61P35/02 , A61P43/00 , A61K31/59
CPC分类号： A61K31/593
摘要： This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3. Administration of this compound increases the life expectancy of human beings, especially elderly human beings. In particular, it increases the survival rate of females lacking estrogen, especially post-menopausal females, and reduces mortality resulting from spontaneous development of malignant tumors in both males and females.
摘要翻译：本发明提供2-亚甲基-19-去甲-20（S）-1α，25-二羟基维生素D3的药用。这种化合物的施用增加了人类，特别是老年人的预期寿命。特别是增加女性缺乏雌激素，特别是绝经后女性的生存率，并降低男性和女性恶性肿瘤自发发生的死亡率。

3. 发明申请

US20080096851A1 (20S)-1Alpha-Hydroxy-2-Methylene-19-Nor-Bishomopregnacalciferol and Its Uses 有权
标题翻译：（20S）-1α-羟基-2-亚甲基-19-不 - 双代孕代孕甾醇及其用途
公开(公告)号：US20080096851A1
公开(公告)日：2008-04-24
申请号：US11944150
申请日：2007-11-21
申请人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , A61P19/00
CPC分类号： A61K31/59 , C07C401/00
摘要： This invention discloses (20S)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat immune disorders in humans as well as renal osteodystrophy.
摘要翻译：本发明公开了（20S）-1α-羟基-2-亚甲基-19-去氧胆钙孕激素及其药物用途。该化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。该化合物也具有很少（如果有的话）钙活性，因此可用于治疗人类的免疫疾病以及肾性骨营养不良。

4. 发明申请

US20070249569A1 2-Methylene-19-nor-1alpha-hydroxy-17-ene-homopregnacalciferol and its uses 有权
标题翻译： 2-亚甲基-19-去甲-α-羟基-17-烯 - 孕孕甾醇钙及其用途
公开(公告)号：US20070249569A1
公开(公告)日：2007-10-25
申请号：US11775117
申请日：2007-07-09
申请人： Hector DeLuca , Bulli Tadi , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Bulli Tadi , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C403/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 2-methylene-19-nor-17-ene vitamin D analogs, and specifically 2-methylene-19-nor-1α-hydroxy-17-ene-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
摘要翻译：本发明公开了2-亚甲基-19-去甲-17-烯维生素D类似物，特别是2-亚甲基-19-去甲-α-羟基-17-烯 - 孕孕甾醇钙及其药物用途。该化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。该化合物也具有很少（如果有的话）钙活性，因此可用于治疗人体中的自身免疫疾病和炎症性疾病以及肾性骨营养不良。该化合物也可用于治疗或预防肥胖症。

5. 发明申请

US20060241090A1 Use of 2-methylene-19-nor-20(S)-1alpha,25dihydroxyvitamin D3 to increase the life expectancy of human beings 有权
标题翻译：使用2-亚甲基-19-nor-20（S）-1α，25二羟基维生素D3来增加人的预期寿命
公开(公告)号：US20060241090A1
公开(公告)日：2006-10-26
申请号：US11472125
申请日：2006-06-21
申请人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59
CPC分类号： A61K31/593
摘要： This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3. Administration of this compound increases the life expectancy of human beings, especially elderly human beings. In particular, it increases the survival rate of females lacking estrogen, especially post-menopausal females, and reduces mortality resulting from spontaneous development of malignant tumors in both males and females.
摘要翻译：本发明提供2-亚甲基-19-去甲-20（S）-1α，25-二羟基维生素D 3 N的药用。这种化合物的施用增加了人类，特别是老年人的预期寿命。特别是增加女性缺乏雌激素，特别是绝经后女性的生存率，并降低男性和女性恶性肿瘤自发发生的死亡率。

6. 发明申请

US20060122157A1 2-Methylene-18,19-dinor-1alpha-hydroxy-homopregnacalciferol and its uses 有权
标题翻译： 2-亚甲基-18,19-二氢-1α-羟基 - 孕代孕甾醇及其用途
公开(公告)号：US20060122157A1
公开(公告)日：2006-06-08
申请号：US11283222
申请日：2005-11-18
申请人： Hector DeLuca , Rafal Barycki , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Rafal Barycki , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-18,19-dinor-vitamin D analogs, and specifically 2-methylene-18,19-dinor-1α-hydroxy-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
摘要翻译：本发明公开了2-亚甲基-18,19-二 - 维生素D类似物，特别是2-亚甲基-18,19-二牛-1α-羟基 - 同孕孕甾醇和其药物用途。该化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。该化合物也具有很少（如果有的话）钙活性，因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及肾性骨营养不良。该化合物也可用于治疗或预防肥胖症。

7. 发明申请

US20080081800A1 2-Methylene-(20R,25S)-19,27-Dinor-(22E)-Vitamin D Analogs 有权
标题翻译： 2-亚甲基 - （20R，25S）-19,27-二烯（22E） - 维生素D类似物
公开(公告)号：US20080081800A1
公开(公告)日：2008-04-03
申请号：US11860870
申请日：2007-09-25
申请人： Hector DeLuca , Margaret Clagett-Dame , Lori Plum , Grazia Chiellini , Pawel Grzywacz
发明人： Hector DeLuca , Margaret Clagett-Dame , Lori Plum , Grazia Chiellini , Pawel Grzywacz
IPC分类号： A61K31/593 , A61K31/59 , A61P17/00 , A61P17/06 , A61P19/00 , A61P29/00 , A61P3/04 , A61P35/00 , A61P37/00 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 2-methylene-(20R,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20R,25S)-19,27-dinor-(22E)-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
摘要翻译：本发明公开了2-亚甲基 - （20R，25S）-19,27-二（22E） - 维生素D类似物，特别是2-亚甲基 - （20R，25S）-19,27-二（22E）-1α ，25-二羟基维生素D 3 N及其药物用途。该化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。该化合物也具有很少（如果有的话）钙活性，因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及肾性骨营养不良。该化合物也可用于治疗或预防肥胖症。

8. 发明申请

US20070270391A1 2Alpha-Methyl and 2Beta-Methyl Analogs of 19,26,27-Trinor-(20S)-1Alpha-Hydroxyvitamin D3 and Their Uses 有权
标题翻译： 19,26,27-三硝基 - （20S）-1α-羟基维生素D 3及其用途的2α-甲基和2β-甲基类似物
公开(公告)号：US20070270391A1
公开(公告)日：2007-11-22
申请号：US11775042
申请日：2007-07-09
申请人： Hector DeLuca , Lori Plum , Pawel Grzywacz , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Pawel Grzywacz , Margaret Clagett-Dame
IPC分类号： A61K31/593 , A61P43/00 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804
摘要： This invention discloses 2α-methyl and 2β-methyl analogs of 19,26,27-trinor-(20S)-1α-hydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. These compounds may also be used for the treatment or prevention of obesity.
摘要翻译：本发明公开了19,26,27-三硝基 - （20S）-1α-羟基维生素D 3 3的2α-甲基和2b-甲基类似物及其药物用途。这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤，皮肤干燥，皮脂分泌不足。这些化合物也具有很少（如果有的话）钙活性，因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及肾性骨营养不良。这些化合物也可用于治疗或预防肥胖症。

9. 发明申请

US20070112077A1 Des-C,D analogs of 1alpha,25-dihydroxy-19-norvitamin D3 有权
标题翻译： 1α，25-二羟基-19-去甲维生素D3的Des-C，D类似物
公开(公告)号：US20070112077A1
公开(公告)日：2007-05-17
申请号：US11512705
申请日：2006-08-30
申请人： Hector DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/045
CPC分类号： C07C401/00 , C07B2200/07 , C07C35/17 , C07C45/292 , C07C45/30 , C07C47/19 , C07C403/08 , C07C2601/14 , C07F7/1804 , Y02P20/55
摘要： Des-C,D 2-methylene-19-norvitamin D3 analogs are provided including compounds of formula 1, in which R1 is a straight or branched chain alkyl or alkylene group having from 8 to 27 carbons and bearing an Oy3 group; and y1, y2 and y3 are independently selected from H or hydroxy-protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
摘要翻译：提供了包含式1化合物的Des-C，D 2 - 亚甲基-19-去甲维生素D 3 N 3类似物，其中R 1是直链或支链烷基或亚烷基具有8至27个碳并具有Oy 3+基团的基团; 且y 1，y 2和y 3独立地选自H或羟基保护基。这样的化合物可用于制备药物组合物，并且可用于治疗各种生物学条件。

10. 发明申请

US20060293291A1 2-Propylidene-19-nor-vitamin d compounds 审中-公开
标题翻译： 2-亚丙基-19-去甲维生素d化合物
公开(公告)号：US20060293291A1
公开(公告)日：2006-12-28
申请号：US10544163
申请日：2004-04-09
申请人： Hector DeLuca , Rafal Sicinski , Agnieszka Glebocka , Lori Plum
发明人： Hector DeLuca , Rafal Sicinski , Agnieszka Glebocka , Lori Plum
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804 , Y02P20/55
摘要： 2-propylidene-19-nor-vitamin D compounds are disclosed as well as pharmaceutical uses for these compounds and methods of synthesizing these compounds. These compounds are characterized by high bone calcium mobilization activity and high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment and prophylaxis of diseases where bone formation is desired, particularly osteoporosis, as well as autoimmune diseases such as multiple sclerosis, diabetes mellitus and lupus. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis. These compounds also increase both breaking strength and crushing strength of bones evidencing use in conjunction with bone replacement surgery such as hip and knee replacements.
摘要翻译：公开了2-亚丙基-19-去甲维生素D化合物以及这些化合物的药物用途和合成这些化合物的方法。这些化合物的特征在于高钙钙动员活性和高钙运输活性。这导致用于治疗和预防需要骨形成的疾病，特别是骨质疏松症以及自身免疫性疾病如多发性硬化，糖尿病和狼疮的新型治疗剂。这些化合物在阻止未分化细胞的增殖并诱导其分化成单核细胞方面也表现出显着的活性，因此证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣。这些化合物还增加骨骼的断裂强度和破碎强度，证明与骨替代手术（例如髋关节和膝盖置换）结合使用。

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