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1. 发明授权

US08987235B2 N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs and their uses 有权
标题翻译： N-环丙基 - （20R）-2-亚甲基-19,26,27-三硝基-25-氮杂 - 维生素D类似物及其用途
公开(公告)号：US08987235B2
公开(公告)日：2015-03-24
申请号：US13473259
申请日：2012-05-16
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Grazia Chiellini
IPC分类号： A61K31/59 , C07C401/00 , C07C211/03 , C07C271/24 , C07C215/42 , C07C225/10 , C07F7/18
CPC分类号： C07C401/00 , C07C215/42 , C07C225/10 , C07C271/24 , C07C2601/02 , C07C2601/14 , C07C2602/24 , C07F7/1804
摘要： This invention discloses N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs, and specifically N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-1α-hydroxyvitamin 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N-环丙基 - （20R）-2-亚甲基-19,26,27-三硝基-25-氮杂 - 维生素D类似物，特别是N-环丙基 - （20R）-2-亚甲基-19,26,27 - 紫霉素-25-氮杂-1α-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。

2. 发明授权

US08609643B2 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs 有权
标题翻译： 2-二甲基 - （20S，25R）-19,26-二 - 维生素D类似物
公开(公告)号：US08609643B2
公开(公告)日：2013-12-17
申请号：US12343586
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： A61K31/593 , C07C401/00 , A61P17/06 , A61P1/00 , A61P17/00 , A61P37/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25R)-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，25R）-19,26-二 - 维生素D类似物，特别是2-亚甲基 - （20S，25R）-19,26-二牛-1al，25-二羟基维生素D3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。

3. 发明申请

US20090170820A1 2-Methylene-(20S,25R)-19,26-Dinor-Vitamin D Analogs 有权
标题翻译： 2-亚甲基 - （20S，25R）-19,26-维生素D类似物
公开(公告)号：US20090170820A1
公开(公告)日：2009-07-02
申请号：US12343586
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： A61K31/593 , C07C401/00 , A61P1/00 , A61P17/00 , A61P19/08 , A61P3/04 , A61P5/18 , A61P17/06 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/00 , A61P19/02 , A61P11/06
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-(20S,25R)-19,26-dinor-vitamin D analogs, and specifically 2-methylene-(20S,25R)-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，25R）-19,26-二 - 维生素D类似物，特别是2-亚甲基 - （20S，25R）-19,26-二牛-1al，25-二羟基维生素D3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。

4. 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。

5. 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。

6. 发明申请

US20090170821A1 2-Methylene-(20S,25S)-19,26-Dinor-Vitamin D Analogs 有权
标题翻译： 2-亚甲基 - （20S，25S）-19,26-维生素D类似物
公开(公告)号：US20090170821A1
公开(公告)日：2009-07-02
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： A61K31/593 , A61K31/59 , C07C401/00 , A61P37/00 , A61P17/00 , A61P3/04 , A61P29/00 , A61P35/00 , A61P17/06
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）-19,26-二牛醇-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。

7. 发明申请

US20120283228A1 2alpha-Methyl and 2beta-Methyl Analogs of 19,26-Dinor-1alpha,25-Dihydroxyvitamin D3 and Their Uses 审中-公开
标题翻译： 19,26-Dinor-1al，25-二羟基维生素D3及其用途的2α-甲基和2beta-甲基类似物
公开(公告)号：US20120283228A1
公开(公告)日：2012-11-08
申请号：US13463557
申请日：2012-05-03
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Pawel Grzywacz , Grazia Chiellini , Lori A. Plum
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Pawel Grzywacz , Grazia Chiellini , Lori A. Plum
IPC分类号： C07C401/00 , A61P17/06 , A61P35/00 , A61P35/02 , A61P17/00 , A61P3/10 , A61P29/00 , A61P11/06 , A61P1/00 , A61K31/593 , A61P37/06
CPC分类号： C07C401/00 , A61K8/67 , A61Q19/007 , A61Q19/08 , C07C2601/14 , C07C2602/24 , C07F7/1804
摘要： This invention discloses 2α-methyl and 2β-methyl analogs of 19,26-dinor-1α,25-dihydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit in vitro biological activities 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 have little, if any, in vivo calcemic activity and therefore may be used to treat autoimmune disorders in humans as well as secondary hyperparathyroidism and renal osteodystrophy.
摘要翻译：本发明公开了19,26-二氢-1α，25-二羟基维生素D 3的2α-甲基和2'-二甲基类似物及其药物用途。这些化合物表现出体外生物活性，其证明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，干性皮肤和皮脂分泌不足。这些化合物在体内的钙活性很少（如果有的话），因此可以用于治疗人类的自身免疫性疾病以及继发性甲状旁腺功能亢进和肾性骨营养不良。

8. 发明授权

US08193170B2 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs 有权
标题翻译： 2-亚甲基-19,26-二烯 - （20R，22E，25R） - 维生素D类似物
公开(公告)号：US08193170B2
公开(公告)日：2012-06-05
申请号：US12171113
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 , C07C35/17 , A61P17/00
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This invention discloses 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20R,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 very low activity in vivo on bone calcium mobilization and relatively high 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-29,26-二烯 - （20R，22E，25R） - 维生素D类似物，特别是2-亚甲基-19,26-二（20R，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，该化合物在骨钙动员和体内相对较高的肠钙迁移活性中也显示出非常低的活性，因此可用于治疗人类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。

9. 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。

10. 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。

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