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21. 发明授权

US08399438B2 2α-methyl-19-nor-1α-hydroxy-homopregnacalciferol and its uses 有权
标题翻译： 2α-甲基-19-去甲-αα-羟基 - 同孕孕甾醇钙及其用途
公开(公告)号：US08399438B2
公开(公告)日：2013-03-19
申请号：US11283261
申请日：2005-11-18
申请人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Sumithra Gowlugari
发明人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Sumithra Gowlugari
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2α-methyl-19-nor-vitamin D analogs, and specifically 2α-methyl-19-nor-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2α-甲基-19-去甲维生素D类似物，特别是2α-甲基-19-nor-1α-羟基 - 高孕蛋白胨和其药物用途。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。

22. 发明授权

US08193171B2 13,13-dimethyl-des-C,D analogs of 1α,25-dihydroxy-19-nor-vitamin D3 compounds and topical composition dosage forms and methods of treating skin conditions thereof 有权
标题翻译： 1α，25-二羟基-19-去甲维生素D3化合物的13,13-二甲基-de-C，D类似物和局部组合物剂型及治疗其皮肤病症的方法
公开(公告)号：US08193171B2
公开(公告)日：2012-06-05
申请号：US12357702
申请日：2009-01-22
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal R. Sicinski , Katarzyna Plonska-Ocypa , Nirca J. Nieves , Pawel Grzywacz
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal R. Sicinski , Katarzyna Plonska-Ocypa , Nirca J. Nieves , Pawel Grzywacz
IPC分类号： A61K31/047 , C07C35/17 , C07C401/00 , A61P17/00
CPC分类号： C07C401/00 , C07C2601/14
摘要： 13,13-Dimethyl-des-C,D analogs of 1α,25-dihydroxy-19-nor-vitamin D3 compounds and topical composition dosage forms thereof, and methods of treating skin conditions thereof. Exemplary active pharmaceutical ingredients include (1R,3R)-5-[(E)-(S)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-methylene-cyclohexane-1,3-diol, (1R,3R)-5-[(Z)-(S)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-methylene-cyclohexane-1,3-diol, (1R,3R)-5-[(E)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-methylene-cyclohexane-1,3-diol, and (1R,3R)-5-[(Z)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-methylene-cyclohexane-1,3-diol.
摘要翻译： 1α，25-二羟基-19-去甲维生素D3化合物的13,13-二甲基-D-脱氧-D类似物及其局部组合物剂型，以及其皮肤病症的治疗方法。示例性的活性药物成分包括（1R，3R）-5 - [（E） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - 十二烷-2'-亚基] -2 亚甲基环己烷-1,3-二醇，（1R，3R）-5 - [（Z） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - （1R，3R）-5 - [（E） - （R）-11'-羟基-5'，5'，7'，11' 和（1R，3R）-5 - [（Z） - （R）-11'-羟基-5'，5'，5'-二甲基环己烷-1,3-二醇 '，7'，11'-四甲基 - 十二烷-2'-亚炔基] -2-亚甲基 - 环己烷-1,3-二醇。

23. 发明授权

US08178517B2 6-methylvitamin D3 analogs and their uses 有权
标题翻译： 6-甲基维生素D3类似物及其用途
公开(公告)号：US08178517B2
公开(公告)日：2012-05-15
申请号：US12895577
申请日：2010-09-30
申请人： Hector F. DeLuca , Katarzyna Sokolowska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Antonio Mouriño
发明人： Hector F. DeLuca , Katarzyna Sokolowska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Antonio Mouriño
IPC分类号： A61K31/59 , C07D401/00
CPC分类号： C07C401/00
摘要： This invention discloses 6-methylvitamin D3 analogs, and specifically 1α,25-dihydroxy-6-methylvitamin D3, and pharmaceutical uses therefor. This compound exhibits vitamin D receptor binding activity and transcription activity as well as 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. This compound also exhibits low in vivo calcemic activity, but because it binds the receptor with the same affinity as the native hormone calcitriol, it may act as an antagonist to inhibit development of hypercalcemia.
摘要翻译：本发明公开了6-甲基维生素D3类似物，特别是1α，25-二羟基-6-甲基维生素D3及其药物用途。该化合物显示维生素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活性，从而证明其用作抗癌剂，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。该化合物还具有体内低钙活性，但由于其以与天然激素骨化三醇相同的亲和力结合受体，所以它可以作为抑制高钙血症发展的拮抗剂。

24. 发明申请

US20090186950A1 13,13-Dimethyl-des-C,D Analogs of 1Alpha,25-Dihydroxy-19-Nor-Vitamin D3 Compounds and Topical Composition Dosage Forms and Methods of Treating Skin Conditions Thereof 有权
标题翻译： 1Alpha，25-二羟基-19-不维生素D3化合物的13,13-二甲基-D-C，D类似物和局部组合物剂型及其治疗皮肤病症的方法
公开(公告)号：US20090186950A1
公开(公告)日：2009-07-23
申请号：US12357702
申请日：2009-01-22
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal R. Sicinski , Katarzyna Plonska-Ocypa , Nirca J. Nieves , Pawel Grzywacz
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal R. Sicinski , Katarzyna Plonska-Ocypa , Nirca J. Nieves , Pawel Grzywacz
IPC分类号： A61K31/047 , C07C35/17 , A61P35/00
CPC分类号： C07C401/00 , C07C2601/14
摘要： 13,13-Dimethyl-des-C,D analogs of 1α,25-dihydroxy-19-nor-vitamin D3 compounds and topical composition dosage forms thereof, and methods of treating skin conditions thereof. Exemplary active pharmaceutical ingredients include (1R,3R)-5-[(E)-(S)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol, (1R,3R)-5-[(Z)-(S)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol, (1R,3R)-5-[(E)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol, and (1R,3R)-5-[(Z)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol.
摘要翻译： 1α，25-二羟基-19-去甲维生素D 3化合物的13,13-二甲基-D-C，D类似物及其局部组合物剂型，以及其皮肤病症的治疗方法。示例性的活性药物成分包括（1R，3R）-5 - [（E） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - 十二烷-2'-亚基] -2 （1R，3R）-5 - [（Z） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - 十二烷基-2- （1R，3R）-5 - [（E） - （R）-11'-羟基-5'，5'，7'，11' （1R，3R）-5 - [（Z） - （R）-11'-羟基-5'，5'，5'-二甲基环己烷-1,3-二醇 '，7'，11'-四甲基 - 十二烷-2'-亚炔基] -2-亚甲基 - 环己烷-1,3-二醇。

25. 发明授权

US06579861B2 1&agr;-hydroxy-2-methylene-19-nor-homopregnacalciferol and its uses 有权
公开(公告)号：US06579861B2
公开(公告)日：2003-06-17
申请号：US10165123
申请日：2002-06-07
申请人： Hector F. DeLuca , Rafal R. Sicinski , Sumithra Gowlugari , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Rafal R. Sicinski , Sumithra Gowlugari , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K3159
CPC分类号： A61K8/345 , A61K8/67 , A61K31/59 , A61Q19/007 , A61Q19/08 , C07C401/00
摘要： This invention discloses 1&agr;-hydroxy-2-methylene-19-nor-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 immune disorders in humans as well as renal osteodystrophy.

26. 发明授权

US08642579B2 1-desoxy-2-methylene-19-nor-vitamin D analogs and their uses 有权
标题翻译： 1-脱氧-2-亚甲基-19-维生素D类似物及其用途
公开(公告)号：US08642579B2
公开(公告)日：2014-02-04
申请号：US12895478
申请日：2010-09-30
申请人： Hector F. DeLuca , Katarzyna M. Barycka , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki , Rafal R. Sicinski , Katarzyna Plonska-Ocypa
发明人： Hector F. DeLuca , Katarzyna M. Barycka , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki , Rafal R. Sicinski , Katarzyna Plonska-Ocypa
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07F9/5325
摘要： This invention discloses 1-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-1-desoxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and 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1-脱氧-2-亚甲基-19-去甲维生素D类似物，特别是（20S）-25-羟基-1-脱氧-2-亚甲基-19-去甲维生素D3及其药物用途。该化合物在阻止未分化细胞的增殖和诱导其分化为单核细胞方面表现出相对较高的结合活性和明显的活性，从而证明其用作抗癌剂，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。

27. 发明授权

US08518917B2 2-methylene-19-nor-vitamin D analogs and their uses 有权
标题翻译： 2-亚甲基-19-维生素D类似物及其用途
公开(公告)号：US08518917B2
公开(公告)日：2013-08-27
申请号：US13278846
申请日：2011-10-21
申请人： Hector F. DeLuca , Izabela Sibliska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
发明人： Hector F. DeLuca , Izabela Sibliska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00 , C07F7/1804 , C07F9/5325
摘要： This invention discloses 2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-19-nor-vitamin D3 and (20R)-25-hydroxy-2-methylene-19-nor-vitamin D3, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and 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 osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. Although these compounds have relatively low calcemic activities they may also be useful in the treatment of bone diseases due to their ability to act as prodrugs in vivo.
摘要翻译：本发明公开了2-亚甲基-19-去甲维生素D类似物，特别是（20S）-25-羟基-2-亚甲基-19-去甲维生素D3和（20R）-25-羟基-2-亚甲基-19- 维生素D3，以及其用途。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相对较高的结合活性和显着的活性，从而证明其用作抗癌剂，特别是用于治疗或预防骨肉瘤，白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌。虽然这些化合物具有相对较低的血钙活性，但是由于它们在体内作为前药的能力，它们也可用于治疗骨骼疾病。

28. 发明授权

US08093232B2 2α-methyl-19-nor-(20S)-1α-hydroxy-bishomopregnacalciferol and its uses 有权
标题翻译： 2α-甲基-19-去甲 - （20S）-1α-羟基 - 双代孕代孕甾醇及其用途
公开(公告)号：US08093232B2
公开(公告)日：2012-01-10
申请号：US11775074
申请日：2007-07-09
申请人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07D401/00
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-去甲（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。

29. 发明申请

US20110082123A1 6-Methylvitamin D3 Analogs and Their Uses 有权
标题翻译： 6-甲基维生素D3类似物及其用途
公开(公告)号：US20110082123A1
公开(公告)日：2011-04-07
申请号：US12895577
申请日：2010-09-30
申请人： Hector F. DeLuca , Katarzyna Sokolowska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Antonio Mouriño
发明人： Hector F. DeLuca , Katarzyna Sokolowska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Antonio Mouriño
IPC分类号： A61K31/593 , C07C35/21 , A61P13/12 , A61P17/06 , A61P19/10 , A61P35/00
CPC分类号： C07C401/00
摘要： This invention discloses 6-methylvitamin D3 analogs, and specifically 1α,25-dihydroxy-6-methylvitamin D3, and pharmaceutical uses therefor. This compound exhibits vitamin D receptor binding activity and transcription activity as well as 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. This compound also exhibits low in vivo calcemic activity, but because it binds the receptor with the same affinity as the native hormone calcitriol, it may act as an antagonist to inhibit development of hypercalcemia.
摘要翻译：本发明公开了6-甲基维生素D3类似物，特别是1α，25-二羟基-6-甲基维生素D3及其药物用途。该化合物显示维生素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活性，从而证明其用作抗癌剂，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。该化合物还具有体内低钙活性，但由于其以与天然激素骨化三醇相同的亲和力结合受体，所以它可以作为抑制高钙血症发展的拮抗剂。

30. 发明授权

US06440953B1 1&agr;-hydroxy-2-methylene-19-nor-homopregnacalciferol and its uses 失效
标题翻译： 1α-羟基-2-亚甲基-19-去高孕孕甾醇和其用途
公开(公告)号：US06440953B1
公开(公告)日：2002-08-27
申请号：US09878438
申请日：2001-06-11
申请人： Hector F. DeLuca , Rafal R. Sicinski , Sumithra Gowlugari , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Rafal R. Sicinski , Sumithra Gowlugari , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K3159
CPC分类号： A61K8/345 , A61K8/67 , A61K31/59 , A61Q19/007 , A61Q19/08 , C07C401/00
摘要： This invention discloses 1&agr;-hydroxy-2-methylene-19-nor-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 anticancer 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1α-羟基-2-亚甲基-19-去稳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和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，干性皮肤皮脂分泌不足。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。

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