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21. 发明申请

US20080300223A1 (20R)-2a-Methyl-19,26,27-Trinor-Vitamin D Analogs 有权
标题翻译：（20R）-2a-甲基-19,26,27-三维 - 维生素D类似物
公开(公告)号：US20080300223A1
公开(公告)日：2008-12-04
申请号：US12171085
申请日：2008-07-10
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： A61K31/59 , C07C403/06 , A61K31/593 , A61P35/00 , A61P37/00 , A61P3/10
CPC分类号： C07C401/00
摘要： This invention discloses (20R)-2α-methyl-19,26,27-trinor-vitamin D analogs, and specifically (20R)-2α-methyl-19,26,27-trinor-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 very low 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（20R）-2α-甲基-19,26,27-三硝基维生素D类似物，特别是（20R）-2α-甲基-19,26,27-三硝基-1α，25-二羟基维生素D 3和药物用它。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，该化合物在体内对钙钙动员和肠钙运输活性的活性也显示出非常低的活性，因此可用于治疗人类的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。

22. 发明授权

US07241909B2 19,26,27-trinor-1α,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：US07241909B2
公开(公告)日：2007-07-10
申请号：US11416401
申请日：2006-05-02
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： C07D401/00 , A61K31/59
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

23. 发明授权

US08445468B2 (20S,22E)-2-methylene-19-nor-22-ene-1α,25-dihydroxyvitamin D3 有权
标题翻译：（20S，22E）-2-亚甲基-19-去甲-22-烯-1α，25-二羟基维生素D 3
公开(公告)号：US08445468B2
公开(公告)日：2013-05-21
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 , C07C401/00
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D 3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。

24. 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。

25. 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。

26. 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。

27. 发明授权

US08664206B2 Diastereomers of 2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin D3 有权
标题翻译： 2-亚甲基-19-去甲基-22-甲基-1α，25-二羟基维生素D3的非对映异构体
公开(公告)号：US08664206B2
公开(公告)日：2014-03-04
申请号：US13344987
申请日：2012-01-06
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 , C07C35/23
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。

28. 发明授权

US08604009B2 (20S)-2-methylene-19-nor-22-dimethyl-1α,25-dihydroxyvitamin D3 and (20R)-2-methylene-19-nor-22-dimethyl-1α,25-hydroxyvitamin D3 有权
标题翻译：（20S）-2-亚甲基-19-去甲基-22-二甲基-1α，25-二羟基维生素D3和（20R）-2-亚甲基-19-去甲基-22-二甲基-1α，25-羟基维生素D3
公开(公告)号：US08604009B2
公开(公告)日：2013-12-10
申请号：US13053844
申请日：2011-03-22
申请人： Hector F. DeLuca , Agnieszka Flores , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Agnieszka Flores , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/593 , C07C401/00
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。

29. 发明授权

US08193169B2 (20R)-2α-methyl-19,26,2-trinor-vitamin D analogs 有权
标题翻译：（20R）-2α-甲基-19,26,2-三 - 维生素D类似物
公开(公告)号：US08193169B2
公开(公告)日：2012-06-05
申请号：US12171085
申请日：2008-07-10
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： A61K31/59 , C07C401/00 , C07C35/17 , A61P17/00
CPC分类号： C07C401/00
摘要： This invention discloses (20R)-2α-methyl-19,26,27-trinor-vitamin D analogs, and specifically (20R)-2α-methyl-19,26,27-trinor-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 very low 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（20R）-2α-甲基-19,26,27-三硝基维生素D类似物，特别是（20R）-2α-甲基-19,26,27-三硝基-1α，25-二羟基维生素D3和药物用它。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，该化合物在体内对钙钙动员和肠钙迁移活性的活性也显示出非常低的活性，因此可用于治疗人类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。

30. 发明授权

US07534777B2 Des-C,D analogs of 1α,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：US07534777B2
公开(公告)日：2009-05-19
申请号：US11512705
申请日：2006-08-30
申请人： Hector F. DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/45 , C07D401/00
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-诺维生素D3类似物，其中R 1是具有8至27个碳并具有OY 3基团的直链或支链烷基或亚烷基; 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。

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