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11. 发明授权

US07763598B2 1α-hydroxy-2-(3′-hydroxypropylidene)-19-nor-vitamin D compounds with a 1,1-dimethylpropyl side chain 有权
标题翻译： 1α-羟基-2-（3'-亚丙基亚基）-19-去甲维生素D化合物与1,1-二甲基丙基侧链
公开(公告)号：US07763598B2
公开(公告)日：2010-07-27
申请号：US11697430
申请日：2007-04-06
申请人： Hector F. DeLuca , Agnieszka Glebocka , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Agnieszka Glebocka , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804
摘要： This invention discloses 1α-hydroxy-2-(3′-hydroxypropylidene)-19-nor-vitamin D compounds with a 1,1-dimethylpropyl side chain, 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：本发明公开了具有1,1-二甲基丙基侧链的1α-羟基-2-（3'-羟基亚丙基）-19-去甲维生素D化合物及其药物用途。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。

12. 发明申请

US20090281340A1 1ALPHA-HYDROXY-2-(3'-HYDROXYPROPYLIDENE)-19-NOR-VITAMIN D COMPOUNDS AND METHODS OF MAKING AND TREATMENT THEREOF 审中-公开
标题翻译： 1ALPHA-羟基-2-（3'-羟基丙烯酰基）-19-异维生素D化合物及其制备和处理方法
公开(公告)号：US20090281340A1
公开(公告)日：2009-11-12
申请号：US12437892
申请日：2009-05-08
申请人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Agnieszka Glebocka
发明人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Agnieszka Glebocka
IPC分类号： C07C401/00 , C07C45/00
CPC分类号： C07C401/00 , C07C45/29 , C07C2602/24 , C07C49/443
摘要： Disclosed are 1α-hydroxy-2-(3′-hydroxypropylidene)-19-nor-vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3′-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.
摘要翻译：公开了1α-羟基-2-（3'-羟基亚丙基）-19-去甲维生素D化合物，药物组合物及其制备和处理方法。化合物通常指向生物活性的2-亚烷基-19-去甲维生素D化合物及其类似物，其特征在于在C-2存在3'-羟基亚丙基部分，并且存在没有任何的缩写的烷基侧链羟基部分。

13. 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。

14. 发明授权

US08058265B2 1a-hydroxy-2-(3'-hydroxypropylidene)-19-nor-vitamin D compounds and methods of making and treatment thereof 有权
标题翻译： 1a-羟基-2-（3'-亚丙基亚基）-19-去甲维生素D化合物及其制备和处理方法
公开(公告)号：US08058265B2
公开(公告)日：2011-11-15
申请号：US11732924
申请日：2007-04-05
申请人： Hector F. Deluca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Agnieszka Glebocka
发明人： Hector F. Deluca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Agnieszka Glebocka
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07C45/29 , C07C2602/24 , C07C49/443
摘要： Disclosed are 1α-hydroxy-2-(3′-hydroxypropylidene)-19-nor-vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3′-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.
摘要翻译：公开了1α-羟基-2-（3'-羟基亚丙基）-19-去甲维生素D化合物，药物组合物及其制备和处理方法。化合物通常指向生物活性的2-亚烷基-19-去甲维生素D化合物及其类似物，其特征在于在C-2存在3'-羟基亚丙基部分，并且存在没有任何的缩写的烷基侧链羟基部分。

15. 发明授权

US07538098B2 19-nor-vitamin D analogs with 1,2 or 3,2 heterocyclic ring 有权
标题翻译：具有1,2或3,2个杂环的19-维生素D类似物
公开(公告)号：US07538098B2
公开(公告)日：2009-05-26
申请号：US11697424
申请日：2007-04-06
申请人： Hector F. DeLuca , Rafal R. Sicinski , Agnieszka Glebocka , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Rafal R. Sicinski , Agnieszka Glebocka , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07D401/00
CPC分类号： C07D311/74
摘要： 19-nor-vitamin D analogs having an additional heterocyclic ring connecting the 3β-oxygen and carbon-2 or the 1α-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit significant activity in mobilization of bone, making them therapeutic agents for the treatment or prophylaxis of osteoporosis, osteomalacia, osteopenia, renal osteodystrophy and hypoparathyroidism.
摘要翻译：描述了具有连接3β-氧和碳-2的额外的杂环的19-维生素D类似物或类似物的A环的1α-氧和碳-2，以及药物用途。这些化合物在骨骼运动中表现出显着的活性，使其成为治疗或预防骨质疏松症，骨软化症，骨质减少症，肾性骨营养不良和甲状旁腺功能低下的治疗剂。

16. 发明申请

US20130178449A1 2-Methylene-20(21)-Dehydro-19,24,25,26,27-Pentanor-Vitamin D Analogs 审中-公开
标题翻译： 2-亚甲基-20（21） - 脱氢-19,24,25,26,27-戊醇维生素D类似物
公开(公告)号：US20130178449A1
公开(公告)日：2013-07-11
申请号：US13547111
申请日：2012-07-12
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Agnieska Glebocka , Rafal R. Sicinski
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Agnieska Glebocka , Rafal R. Sicinski
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-1α-hydroxyvitamin 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 lower in vivo intestinal calcium transport activity as 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 secondary hyperparathyroidism and 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-19,24,25,26,27-戊醇维生素D类似物，特别是2-亚甲基-20（21） - 脱氢-19,24,25,26 ，27-戊酰-1α-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D 3相比，该化合物在骨钙动员和体内肠内钙转运活性方面的体内活性也较低，因此可用于治疗人的自身免疫性疾病或炎症性疾病继发性甲状旁腺功能亢进和肾性骨营养不良。该化合物也可用于治疗或预防肥胖症。

17. 发明申请

US20120071562A1 2alpha-Methyl-19-Nor-(20S)-1alpha-Hydroxy-Bishomopregnacalciferol and Its Uses 审中-公开
标题翻译： 2α-甲基-19-诺 - （20S）-1α-羟基 - 二高钙孕激素及其用途
公开(公告)号：US20120071562A1
公开(公告)日：2012-03-22
申请号：US13302709
申请日：2011-11-22
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： A61K31/047 , A61P17/10
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。

18. 发明申请

US20110082121A1 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：US20110082121A1
公开(公告)日：2011-04-07
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： A61K31/593 , C07C35/21 , C07F9/28 , A61P13/12 , A61P19/10 , A61P17/06 , A61P35/00
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。

19. 发明申请

US20120322775A1 3-Desoxy-2-Methylene-19-Nor-Vitamin D Analogs and Their Uses 有权
标题翻译： 3-脱氧-2-亚甲基-19-不维生素D类似物及其用途
公开(公告)号：US20120322775A1
公开(公告)日：2012-12-20
申请号：US13495548
申请日：2012-06-13
申请人： Hector F. DeLuca , Lori A. Plum , Rafal R. Sicinski , Izabela Sibilska , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Lori A. Plum , Rafal R. Sicinski , Izabela Sibilska , Margaret Clagett-Dame
IPC分类号： A61K31/593 , A61P35/00 , C07F9/53 , A61P19/10 , A61P19/08 , C07C401/00 , A61P35/02
CPC分类号： C07F9/5325 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24 , C07F9/53
摘要： This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1α,25-dihydroxy-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 monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.
摘要翻译：本发明公开了3-脱氧-2-亚甲基-19-去甲维生素D类似物，特别是（20S）-3-脱氧-2-亚甲基-1α，25-二羟基-19-去甲维生素D3和（20R） - 3-脱氧-2-亚甲基-1α，25-二羟基-19-去甲维生素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。这些化合物还表现出相对较高的钙摄取活性，其用于治疗骨疾病。

20. 发明申请

US20120157418A1 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：US20120157418A1
公开(公告)日：2012-06-21
申请号：US13278846
申请日：2011-10-21
申请人： Hector F. DeLuca , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
发明人： Hector F. DeLuca , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal R. Sicinski , Katarzyna M. Barycka , Katarzyna Plonska-Ocypa , Rafal Barycki
IPC分类号： A61K31/593 , C07F7/18 , C07F9/53 , A61P35/02 , A61P19/08 , A61P19/10 , C07C401/00 , A61P35/00
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。

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