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11. 发明申请

US20060264410A1 19,26,27-trinor-1alpha,25-dihydroxyvitamin D3 compounds 有权
标题翻译： 19,26,27-三硝基-1α，25-二羟基维生素D 3化合物
公开(公告)号：US20060264410A1
公开(公告)日：2006-11-23
申请号：US11416401
申请日：2006-05-02
申请人： Hector DeLuca , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula 1 are provided where X1, X2, and X3 are independently selected from H or hydroxy protecting groups, and R1 and R2 have the definitions provided herein. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
摘要翻译：提供式1化合物，其中X 1，X 2和X 3独立地选自H或羟基保护基， SUP＆gt; 1＆gt;和＆lt; 2＆gt;具有本文提供的定义。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。

12. 发明申请

US20060135800A1 2-Methylene-19,21-dinor-1alpha-hydroxy-bishomopregnacalciferol 有权
标题翻译： 2-亚甲基-1,2,3-dinor-1alpha-羟基 - 双代孕代孕甾醇
公开(公告)号：US20060135800A1
公开(公告)日：2006-06-22
申请号：US11283541
申请日：2005-11-18
申请人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula I are provided where X1 and X2 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：提供式I化合物，其中X 1和X 2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。

13. 发明申请

US20060135799A1 2-Methylene-19-NOR-(20R)-1alpha-hydroxy-bishomopregnacalciferol 有权
标题翻译： 2-亚甲基-19-NOR-（20R）-1α-羟基 - 双代孕代孕甾醇
公开(公告)号：US20060135799A1
公开(公告)日：2006-06-22
申请号：US11282972
申请日：2005-11-18
申请人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , C07F7/1804 , Y02P20/55
摘要： Compounds of formula I are provided where X1 and X2 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：提供式I化合物，其中X 1和X 2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。

14. 发明申请

US20060116352A1 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D3的2α-甲基和2beta-甲基类似物及其用途
公开(公告)号：US20060116352A1
公开(公告)日：2006-06-01
申请号：US11283124
申请日：2005-11-18
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： A61K31/695 , A61K31/59 , 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。

15. 发明申请

US20050143358A1 Methods for reducing body fat using vitamin D compounds 失效
标题翻译：使用维生素D化合物减少体脂的方法
公开(公告)号：US20050143358A1
公开(公告)日：2005-06-30
申请号：US10996642
申请日：2004-11-24
申请人： Hector DeLuca , Lori Plum , Hau Ke , Thomas Brown
发明人： Hector DeLuca , Lori Plum , Hau Ke , Thomas Brown
IPC分类号： A61K31/59 , A61K31/592 , A61K31/593
CPC分类号： A61K31/59 , A61K31/592 , A61K31/593
摘要： A treatment for obesity and overweight comprises administering a vitamin D analog. The analog effectively inhibits an increase in body fat to animals at risk and decreases the basal fat content of animals. The treatment has a positive effect on the lean body component such that while there is an overall decrease in body weight, there is also a decrease in percent body fat. This decrease can be proportionally greater than the overall decrease in body weight. In addition, the treatment has a positive effect on bone turnover and osteogenesis making the vitamin D analog a beneficial treatment for the symptoms of menopause. Various exemplary embodiments of the treatment use the 2-alkylidene derivatives of vitamin D3, such as the 2-alkylidene-19-nor derivatives in both the R and S configurations at carbon-20.
摘要翻译：肥胖和超重的治疗包括施用维生素D类似物。模拟物有效地抑制身体脂肪增加到有风险的动物，并降低动物的基础脂肪含量。治疗对瘦体成分具有积极作用，使体重总体上下降，体脂百分比也降低。这种减少可以成比例地大于体重的总体下降。此外，治疗对骨转换和成骨有积极的作用，使维生素D类似物成为更年期症状的有益治疗。处理的各种示例性实施方案使用维生素D 3的2-亚烷基衍生物，例如在碳-20的R和S构型中的2-亚烷基-19-还是衍生物。

16. 发明申请

US20120309719A1 (22E)-2-METHYLENE-26,27-CYCLO-22-DEHYDRO-1ALPHA-HYDROXY-19-NORVITAMIN D3 DERIVATIVES 有权
标题翻译：（22E）-2-甲基-26,27-环己基-22-脱水-1ALPHA-羟基-19-诺维生素D3衍生物
公开(公告)号：US20120309719A1
公开(公告)日：2012-12-06
申请号：US13485343
申请日：2012-05-31
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： A61K31/593 , A61P17/06 , A61P35/02 , A61P35/00 , A61P25/00 , A61P19/04 , A61P3/10 , A61P37/06 , A61P29/00 , A61P11/06 , A61P1/00 , A61P17/00 , A61P19/08 , A61P19/10 , A61P3/02 , A61P3/04 , A61P3/14 , C07C401/00
CPC分类号： C07C401/00 , C07C2601/02 , C07C2601/14 , C07C2602/24
摘要： Cyclopropane-containing vitamin D analogs of formulas I and IV are provided. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
摘要翻译：提供了具有式I和IV的含环丙烷的维生素D类似物。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。

17. 发明申请

US20070259953A1 2-METHYLENE-19-NOR-(23S)-25-DEHYDRO-1ALPHA-HYDROXYVITAMIN D3-26,23-LACTONE AND 2-METHYLENE-19-NOR-(23R)-25-DEHYDRO-1ALPHA-HYDROXYVITAMIN D3-26,23-LACTONE 有权
标题翻译： 2-甲基-19-异 - （23S）-25-脱氢-1ALPHA-羟基维生素D3-26,23-赖酮和2-甲基-19-异 - （23R）-25-脱氢-1ALPHA-羟基维生素D3-26， 23-LACTONE
公开(公告)号：US20070259953A1
公开(公告)日：2007-11-08
申请号：US11767085
申请日：2007-06-22
申请人： Hector DeLuca , Lori PLUM , Margaret CLAGETT-DAME , Grazia CHIELLINI , Pawel GRZYWACZ
发明人： Hector DeLuca , Lori PLUM , Margaret CLAGETT-DAME , Grazia CHIELLINI , Pawel GRZYWACZ
IPC分类号： A61K31/365 , A61P11/06 , A61P17/00
CPC分类号： C07C401/00 , C07F7/1804 , Y02P20/55
摘要： Compounds of formula 1A and 1B are provided where X1 and X2 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 disorders.
摘要翻译：提供式1A和1B的化合物，其中X 1和X 2独立地选自H或羟基保护基。这些化合物可用于制备药物组合物，并且可用于治疗多种生物学疾病。

18. 发明申请

US20070254857A1 2Alpha-Methyl-19-Nor-(20S)-1Alpha-Hydroxy-Bishomopregnacalciferol and Its Uses 有权
标题翻译： 2Aα-甲基-19-诺 - （20S）-1α-羟基 - 二高钙孕激素及其用途
公开(公告)号：US20070254857A1
公开(公告)日：2007-11-01
申请号：US11775074
申请日：2007-07-09
申请人： Hector DeLuca , Rafal Sicinski , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Rafal Sicinski , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , A61P11/06 , A61P17/06 , A61P19/02 , A61P3/00 , A61P3/10 , A61P35/00 , A61P35/02 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804
摘要： This invention discloses 2α-methyl-19-nor-(20S)-vitamin D analogs, and specifically 2α-methyl-19-nor-(20S)-1α-hydroxy-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 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2α-甲基-19-去甲 - （20S） - 维生素D类似物，特别是2α-甲基-19-去 - （20S）-1α-羟基 - 双代孕代孕甾醇及其药物用途。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。

19. 发明申请

US20070249568A1 17,20(E)-dehydro vitamin D analogs and their uses 有权
标题翻译： 17,20（E） - 脱氢维生素D类似物及其用途
公开(公告)号：US20070249568A1
公开(公告)日：2007-10-25
申请号：US11775108
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： A61K31/593 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 17,20(E)-dehydro vitamin D analogs, and specifically 17(E)-1α,25 -dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin 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 and inflammatory diseases in humans as well as renal osteodystrophy and obesity.
摘要翻译：本发明公开了17,20（E） - 脱氢维生素D类似物，特别是17（E）-1α，25-二羟基-17（20） - 脱氢-2-亚甲基-19-去甲维生素D 3 / SUB>及其制药用途。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自身免疫疾病和炎症性疾病以及肾性骨营养不良和肥胖。

20. 发明申请

US20070238704A1 2-Substituted-1Alpha,25-Dihydroxy-19,26,27-Trinor Vitamin D Analogs and Uses Thereof 有权
标题翻译： 2-取代的1Alpha，25-二羟基-19,26,27-维生素D类似物及其用途
公开(公告)号：US20070238704A1
公开(公告)日：2007-10-11
申请号：US11697434
申请日：2007-04-06
申请人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame , Pawel Grzywacz
发明人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame , Pawel Grzywacz
IPC分类号： A61K31/695 , A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula I, II or III are provided where X1, X2 and X3 are independently selected from H and hydroxy protecting groups and R1 and R2 are independently selected from H or straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms; and R3 is independently selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
摘要翻译：提供式I，II或III的化合物，其中X 1，X 2和X 3独立地选自H和羟基保护基，和 R 1和R 2独立地选自H或具有1至8个碳原子的直链或支链烷基，具有2至8个碳原子的直链或支链烯基具有1至8个碳原子的直链或支链羟基取代的烷基，或具有2至8个碳原子的直链和支链羟基取代的烯基; R 3独立地选自具有1至8个碳原子的直链或支链烷基，具有2至8个碳原子的直链或支链烯基，直链或支链羟基取代的烷基具有1至8个碳原子的基团，或具有2至8个碳原子的直链和支链羟基取代的烯基。这些化合物用于制备药物组合物，并且可用于治疗各种生物学条件。

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