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51. 发明申请

US20110086824A1 (20S,22E)-2-Methylene-19-Nor-22-Ene-1Alpha,25-Dihydroxyvitamin D3 有权
标题翻译：（20S，22E）-2-亚甲基-19-壬-22-Ene-1Alpha，25-二羟基维生素D 3
公开(公告)号：US20110086824A1
公开(公告)日：2011-04-14
申请号：US12895390
申请日：2010-09-30
申请人： Hector F. DeLuca , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/593 , C07C35/21 , A61P35/00
CPC分类号： C07C401/00
摘要： This invention discloses (20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 analogs, and specifically(20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits significant vitamin D receptor binding activity and transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：本发明公开了（20S，22E）-2-亚甲基-19-去甲-22-烯-1α，25-二羟基维生素D3类似物，特别是（20S，22E）-2-亚甲基-19-去甲-22-烯-1α ，25-二羟基维生素D3及其药物用途。该化合物表现出显着的维生素D受体结合活性和转录活性，以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性，因此证明其用作抗癌剂，特别是用于治疗或预防白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。

52. 发明授权

US07888339B2 2-methylene-20(21)-dehydro-19-nor-vitamin D analogs 有权
标题翻译： 2-亚甲基-20（21） - 脱氢-19-去甲维生素D类似物
公开(公告)号：US07888339B2
公开(公告)日：2011-02-15
申请号：US12171056
申请日：2008-07-10
申请人： Hector F. DeLuca , Bulli Padmaja Tadi , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Bulli Padmaja Tadi , Lori A. 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-20(21)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19-nor-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as 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 shows lower activity in vivo on bone calcium mobilization and similar in vivo intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, 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-20（21） - 脱氢-19-去甲维生素D类似物，特别是2-亚甲基-20（21） - 脱氢-19-去甲-17α-二羟基维生素D 3及其药物用途。该化合物显示相对较高的转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的明显活性，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，皮肤松弛，皮肤干燥和皮脂分泌不足。与天然激素1α，25-二羟基维生素D3相比，该化合物在骨钙动员和体内肠钙运输活性方面的体内活性也较低，因此可用于治疗人体以及肾脏中的自身免疫疾病或炎性疾病骨营养不良。该化合物也可用于治疗或预防肥胖症。

53. 发明授权

US07704981B2 2-methylene-1alpha,25-dihydroxy-18,19,21-trinorvitamin D3 and uses thereof 有权
标题翻译： 2-亚甲基-1α，25-二羟基-18,19,21-三维维生素D3及其用途
公开(公告)号：US07704981B2
公开(公告)日：2010-04-27
申请号：US11697436
申请日：2007-04-06
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula I are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups. 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化合物，其中X 1，X 2和X 3独立地选自H或羟基保护基。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。

54. 发明申请

US20100009947A1 2-Methylene-19,26-Dinor-(20S,22E,25R)-Vitamin D Analogs 有权
标题翻译：（20S，22E，25R） - 维生素D类似物
公开(公告)号：US20100009947A1
公开(公告)日：2010-01-14
申请号：US12171120
申请日：2008-07-10
申请人： Hector F. DeLuca , Grazia Chiellini , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Grazia Chiellini , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00 , A61P3/00 , A61P17/00 , A61P1/00 , A61P19/02 , A61P11/06
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This invention discloses 2-methylene-19,26-dinor-(20S,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20S,22E,25R)-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as 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 shows no activity in vivo on bone calcium mobilization and relatively low intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, 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-19,26-二（20S，22E，25R） - 维生素D类似物，特别是2-亚甲基-19,26-二（20S，22E，25R）-1α，25-二羟基维生素 D3及其制药用途。该化合物显示转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性，因此证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，皮肤松弛，皮肤干燥，皮脂分泌不足。与天然激素1α，25-二羟基维生素D 3相比，该化合物在体内钙离子活动和体内钙转运活性相对较低，因此可用于治疗人类自身免疫性疾病或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。

55. 发明授权

US07563783B2 2-methylene-19-nor-(20S-24S)-1α,25-dihydroxyvitamin-D2 有权
标题翻译： 2-二甲基-19-去 - （20S-24S）-1α，25-二羟基维生素-D2
公开(公告)号：US07563783B2
公开(公告)日：2009-07-21
申请号：US11352454
申请日：2006-02-10
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804 , Y02P20/55
摘要： Compounds of formula I are provided where X1, X2, and X3 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，X 2和X 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。

56. 发明申请

US20090170818A1 (20S)-23,23-Difluoro-Methylene-19-Nor-Bishomopregnacalciferol-Vitamin D Analogs 有权
标题翻译：（20S）-23,23-二氟 - 亚甲基-19-不 - 双代孕代孕甾醇 - 维生素D类似物
公开(公告)号：US20090170818A1
公开(公告)日：2009-07-02
申请号：US12343576
申请日：2008-12-24
申请人： Hector F. DeLuca , Lori A. Plum , Rafal Barycki , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Lori A. Plum , Rafal Barycki , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00 , C07C49/403 , A61P13/00 , A61P3/00 , A61P17/00 , A61P29/00 , A61P35/04
CPC分类号： C07C401/00 , C07B2200/07 , C07C35/52 , C07C49/477 , C07C2602/24
摘要： This invention discloses (20S)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs, and specifically (20S)-23,23-difluoro-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 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（20S）-23,23-二氟-2-亚甲基-19-去氧胆固醇酯维生素D类似物，特别是（20S）-23,23-二氟-1α-羟基-2-亚甲基-19-不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。

57. 发明授权

US07534778B2 (20S)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol and its uses 有权
标题翻译：（20S）-1α-羟基-2-亚甲基-19-去氧胆钙孕激素及其用途
公开(公告)号：US07534778B2
公开(公告)日：2009-05-19
申请号：US11944150
申请日：2007-11-21
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59
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。

58. 发明授权

US07244719B2 2-methylene-19,26,27-trinor-(20S)-1α-hydroxyvitamin D3 and its uses 有权
标题翻译： 2-亚甲基-19,26,27-三硝基 - （20S）-1α-羟基维生素D3及其用途
公开(公告)号：US07244719B2
公开(公告)日：2007-07-17
申请号：US11283306
申请日：2005-11-18
申请人： Hector F. DeLuca , Lori A. Plum , Pawel K. Grzywacz , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Lori A. Plum , Pawel K. Grzywacz , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24 , C07F7/1804 , Y02P20/55
摘要： This invention discloses 2-methylene-19,26,27-trinor-(20S)-vitamin D analogs, and specifically 2-methylene-19,26,27-trinor-(20S)-1α-hydroxyvitamin 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-19,26,27-三硝基 - （20S） - 维生素D类似物，特别是2-亚甲基-19,26,27-三硝基 - （20S）-1α-羟基维生素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。

59. 发明授权

US08399439B2 2-methylene-19,26-dinor-(20S,22E,25R)-vitamin D analogs 有权
标题翻译：（20S，22E，25R） - 维生素D类似物
公开(公告)号：US08399439B2
公开(公告)日：2013-03-19
申请号：US12171120
申请日：2008-07-10
申请人： Hector F. DeLuca , Grazia Chiellini , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Grazia Chiellini , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This invention discloses 2-methylene-19,26-dinor-(20S,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20S,22E,25R)-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as 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 shows no activity in vivo on bone calcium mobilization and relatively low intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, 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-29,26-二（20S，22E，25R） - 维生素D类似物，特别是2-亚甲基-19,26-二（20S，22E，25R）-1α，25-二羟基维生素 D3及其制药用途。该化合物显示转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性，因此证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，皮肤松弛，皮肤干燥，皮脂分泌不足。与天然激素1α，25-二羟基维生素D3相比，该化合物在骨钙动员和体内相对低的肠运输活性中也没有表现出活性，因此可用于治疗人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。

60. 发明授权

US08222235B2 2-methylene-19-nor-(20R)-1α-hydroxy-bishomopregnacalciferol 有权
标题翻译： 2-亚甲基-19-去 - （20R）-1α-羟基 - 双代孕代孕甾醇
公开(公告)号：US08222235B2
公开(公告)日：2012-07-17
申请号：US11282972
申请日：2005-11-18
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07D401/00
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。

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