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71. 发明授权

US08114859B2 2-methylene-(20S,25S)-19,27-dinor-(22E)-vitamin D analogs 有权
标题翻译： 2-亚甲基 - （20S，25S）-19,27-二（22E） - 维生素D类似物
公开(公告)号：US08114859B2
公开(公告)日：2012-02-14
申请号：US11860863
申请日：2007-09-25
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini , Pawel Grzywacz
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini , Pawel Grzywacz
IPC分类号： A61K31/593 , C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-(20S,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20S,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 - （20S，25S）-19,27-二（22E） - 维生素D类似物，特别是2-亚甲基 - （20S，25S）-19,27-二（22E）-1α ，25-二羟基维生素D3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。

72. 发明申请

US20110294764A1 2-METHYLENE-19,26-NOR-(20S)-1alpha-HYDROXYVITAMIN D3 审中-公开
标题翻译： 2-甲基-29,26-NOR-（20S）-1α-羟基维生素D3
公开(公告)号：US20110294764A1
公开(公告)日：2011-12-01
申请号：US12955567
申请日：2010-11-29
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 , C07F7/18 , A61P17/06 , A61P35/02 , A61P35/00 , A61P25/00 , A61P19/04 , A61P3/10 , A61P37/06 , A61P29/00 , A61P11/06 , A61P1/00 , A61P17/00 , A61Q19/08 , A61P13/12 , A61P19/10 , A61P1/04 , C07C35/21
CPC分类号： C07C401/00 , A61K31/593 , C07C2601/14 , C07C2602/24 , 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。

73. 发明申请

US20110237557A1 DIASTEREOMERS OF 2-METHYLENE-19-NOR-22-METHYL-1ALPHA,25-DIHYDROXYVITAMIN D3 审中-公开
标题翻译： 2-甲基-19-异-20-甲基-1ALPHA，二羟甲基维生素D3的二异氰酸酯
公开(公告)号：US20110237557A1
公开(公告)日：2011-09-29
申请号：US13069074
申请日：2011-03-22
申请人： Hector F. DeLuca , Agnieszka Flores , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame , James B. Thoden , Hazel M. Holden
发明人： Hector F. DeLuca , Agnieszka Flores , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame , James B. Thoden , Hazel M. Holden
IPC分类号： A61K31/593 , C07C401/00 , A61P35/00 , A61P35/02 , A61P3/10 , A61P25/00 , A61P37/06 , A61P19/02 , A61P19/10 , A61P1/00 , A61P17/06
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24 , 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。

74. 发明授权

US07947666B2 2-methylene-(20S,25S)-19,26-dinor-vitamin D analogs 有权
标题翻译： 2-二甲基 - （20S，25S）-19,26-二 - 维生素D类似物
公开(公告)号：US07947666B2
公开(公告)日：2011-05-24
申请号：US12343592
申请日：2008-12-24
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini , Pawel Grzywacz
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini , Pawel Grzywacz
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-(20S,25S)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25S)-19,26-dinor-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 - （20S，25S）-19,26-二 - 维生素D类似物，特别是2-亚甲基 - （20S，25S）-19,26-二酮-1α，25-二羟基维生素D 3和药物用它。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。

75. 发明授权

US07713953B2 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs 有权
标题翻译： 2-亚甲基 - （22E）-25-（1-亚甲基 - 己基）-26,27-环-22-脱氢-19-维生素D类似物
公开(公告)号：US07713953B2
公开(公告)日：2010-05-11
申请号：US12171094
申请日：2008-07-10
申请人： Hector F. DeLuca , Rafal Barycki , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Rafal Barycki , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , A61K31/593 , A61K31/592 , C07C401/00
CPC分类号： C07C401/00 , C07C2601/02
摘要： This invention discloses 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-1α,24(R)-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 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 - （22E）-25-（1-亚甲基 - 己基）-26,27-环-22-脱氢-19-去甲维生素D类似物，特别是2-亚甲基 - （22E）-25 - （1-亚甲基 - 己基）-26,27-环-22-脱氢-19-去甲-1α，24（R） - 二羟基维生素D3及其药学用途。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肠钙转运活性方面的活性也较低，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。

76. 发明授权

US07713952B2 2-methylene-19,26,27-trinor-(20S)-1α-hydroxyvitamin D3 and its uses 有权
标题翻译：（20S）-1α-羟基维生素D3及其用途
公开(公告)号：US07713952B2
公开(公告)日：2010-05-11
申请号：US11775087
申请日：2007-07-09
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。

77. 发明授权

US07648973B2 2-methylene-1α,25-dihydroxy-19,21-dinorvitamin D3 analogs and uses thereof 有权
标题翻译： 2-亚甲基-1α，25-二羟基-19,21-二维生素D3类似物及其用途
公开(公告)号：US07648973B2
公开(公告)日：2010-01-19
申请号：US11697439
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： A61Q19/08 , A61K8/342 , A61K8/585 , A61K8/63 , A61Q19/06 , 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。

78. 发明授权

US07541349B2 2-methylene-19-nor-(23S)-25-dehydro-1α-hydroxyvitamin D3-26,23-lactone and 2-methylene-19-nor-(23R)-25-dehydro-1α-hydroxyvitamin D3-26,23-lactone 有权
标题翻译：（23S）-25-脱氢-1α-羟基维生素D3-26,23-内酯和2-亚甲基-19-去 - （23R）-25-脱氢-1α-羟基维生素D3-26， 23-内酯
公开(公告)号：US07541349B2
公开(公告)日：2009-06-02
申请号：US11767085
申请日：2007-06-22
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Grazia Chiellini , Pawel Grzywacz
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Grazia Chiellini , Pawel Grzywacz
IPC分类号： A61K31/59 , C07C401/00
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X1和X2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。

79. 发明申请

US20080249068A1 Method of Extending the Dose Range of Vitamin D Compounds 审中-公开
标题翻译：延长维生素D剂量范围的方法
公开(公告)号：US20080249068A1
公开(公告)日：2008-10-09
申请号：US11842752
申请日：2007-08-21
申请人： Hector F. DeLuca , John W. Pike , Nirupama Shevde , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , John W. Pike , Nirupama Shevde , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/66 , A61K31/59 , A61P19/08
CPC分类号： A61K45/06 , A61K31/565 , A61K31/593 , A61K2300/00
摘要： Inhibitors of bone calcium resorption are administered, and calcium intake in the subject's diet is restricted, to allow high doses of vitamin D compounds or mimetics to be given with the intent of treating diseases such as metabolic bone diseases, hyperparathyroidism, cancer, psoriasis, and autoimmune diseases without the dangers of calcification of kidney, heart, and aorta. Inhibitors of bone calcium resorption include the bis-phosphonates, OPG (osteoprotegerin) or the soluble RANKL (receptor activator of NF-κB ligand) receptor known as sRANK (soluble RANK which is the protein expressed by the NF-κB gene), and function to block the availability of calcium from bone thereby preventing hypercalcemia and the resulting calcification of soft tissues. Thus, high doses of 1α,25-dihydroxyvitamin D3 (1,25-(OH)2D3), its analogs, prodrugs, or mimetics can be utilized to treat the target disease with minimal risk to a patient. Specifically, alendronate is shown to block the bone calcium mobilization activity of both 1,25-(OH)2D3 and its very potent analog, 2-methylene-19-nor-(20S)-1α,25-dihydroxyvitamin D3, as long as the subject being treated is on a low calcium diet.
摘要翻译：施用骨钙吸收的抑制剂，受限饮食中的钙摄入受到限制，以允许给予高剂量的维生素D化合物或模拟物，其目的是治疗诸如代谢性骨疾病，甲状旁腺功能亢进，癌症，牛皮癣和自身免疫性疾病，无肾脏，心脏和主动脉钙化的危险。骨钙吸收抑制剂包括称为sRANK（可溶性RANK，由NF-κB基因表达的蛋白质）的双膦酸盐，OPG（骨保护素）或可溶性RANKL（NF-κB配体的受体活化剂）受体）和功能以阻止骨骼中钙的供应，从而防止高钙血症和软组织的钙化。因此，高剂量的1α，25-二羟基维生素D 3 N（1,25-（OH）2 N 3），其类似物，前药，或模拟物可用于以最小的患者风险来治疗目标疾病。具体地说，阿仑膦酸被显示阻断1,25-（OH）2 N 3 N 3和其非常有效的类似物2-亚甲基-19- （20S）-1α，25-二羟基维生素D 3 N，只要被治疗的受试者处于低钙饮食即可。

80. 发明申请

US20070238706A1 2-Methylene-1Alpha,25-Dihydroxy-19,21-Dinorvitamin D3 Analogs and Uses Thereof 有权
标题翻译： 2-亚甲基-1α，25-二羟基-19,21-二维生素D3类似物及其用途
公开(公告)号：US20070238706A1
公开(公告)日：2007-10-11
申请号：US11697439
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： A61K31/695 , A61K31/59 , C07C401/00
CPC分类号： A61Q19/08 , A61K8/342 , A61K8/585 , A61K8/63 , A61Q19/06 , 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。

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