专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 发明申请

US20070238702A1 2-Methylene-1Alpha-Hydroxy-19,21-Dinorvitamin D3 Analogs and Uses Thereof 有权
标题翻译： 2-亚甲基-1α-羟基-19,21-二维维生素D3类似物及其用途
公开(公告)号：US20070238702A1
公开(公告)日：2007-10-11
申请号：US11697418
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： C07C401/00 , 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 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和X 2个独立地选自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。

3. 发明授权

US10479764B2 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs 有权
公开(公告)号：US10479764B2
公开(公告)日：2019-11-19
申请号：US13533018
申请日：2012-06-26
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal Barycki
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal Barycki
IPC分类号： C07C401/00 , A61K31/593
摘要： This invention discloses 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-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 low activity in vivo on bone calcium mobilization, 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.

4. 发明申请

US20130005686A1 2-Methylene-(22E)-25-Hexanoyl-24-OXO-26,27-Cyclo-22-Dehydro-19-Nor-Vitamin D Analogs 审中-公开
标题翻译： 2-亚甲基 - （22E）-25-己酰基-24-OXO-26,27-环-22-脱氢-19-维生素D类似物
公开(公告)号：US20130005686A1
公开(公告)日：2013-01-03
申请号：US13533018
申请日：2012-06-26
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal Barycki
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Rafal Barycki
IPC分类号： A61K31/593 , A61P17/06 , A61P35/02 , A61P35/00 , A61P25/00 , A61P19/04 , A61P3/10 , A61P37/06 , A61P29/00 , A61P11/06 , A61P1/00 , A61P17/00 , A61P13/12 , A61P3/04 , A61P5/20 , A61K31/695 , C07C401/00
CPC分类号： C07C401/00 , A61K31/593 , C07C2601/02 , C07C2601/14 , C07C2602/24
摘要： This invention discloses 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(22E)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-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 low activity in vivo on bone calcium mobilization, 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-己酰基-24-氧代-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-己酰基 -24-氧代-26,27-环-22-脱氢-19-去甲-α-羟基维生素D3及其药物用途。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。该化合物在骨钙动员中的体内活性也低，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。

5. 发明授权

US07915242B2 Vitamin D receptor antagonists and their use in treating asthma 有权
标题翻译：维生素D受体拮抗剂及其在治疗哮喘中的应用
公开(公告)号：US07915242B2
公开(公告)日：2011-03-29
申请号：US11059313
申请日：2005-02-16
申请人： Hector F. DeLuca , Rafal Barycki , Moisés A. Rivera-Bermúdez , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Rafal Barycki , Moisés A. Rivera-Bermúdez , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07C2601/02
摘要： Various compounds such as those having the formula I and XIV where the variables have the values described herein antagonize the vitamin D receptor and are useful in treating conditions such as asthma and in preparing medicaments for use in antagonizing the vitamin D receptor or treating conditions such as asthma
摘要翻译：各种化合物，例如具有式I和XIV的化合物，其中变量具有本文所述的值，其拮抗维生素D受体并且可用于治疗诸如哮喘的病症和用于制备用于拮抗维生素D受体的药物或用于拮抗维生素D受体的治疗条件哮喘

6. 发明授权

US07648972B2 2-methylene-1α-hydroxy-19,21-dinorvitamin D3 analogs and uses thereof 有权
标题翻译： 2-亚甲基-1α-羟基-19,21-二维生素D3类似物及其用途
公开(公告)号：US07648972B2
公开(公告)日：2010-01-19
申请号：US11697418
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： C07C401/00 , 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 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和X 2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。

7. 发明授权

US07238681B2 2-Methylene-18,19-dinor-1α-hydroxy-homopregnacalciferol and its uses 有权
标题翻译： 2-亚甲基-18,19-二氢-1α-羟基 - 孕代孕甾醇及其用途
公开(公告)号：US07238681B2
公开(公告)日：2007-07-03
申请号：US11283222
申请日：2005-11-18
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 , C07D401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-18,19-dinor-vitamin D analogs, and specifically 2-methylene-18,19-dinor-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2-亚甲基-18,19-二 - 维生素D类似物，特别是2-亚甲基-18,19-二牛-1α-羟基 - 同孕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。

8. 发明授权

US08575136B2 2-methylene-1α-hydroxy-18,19,21-trinorvitamin D3 analogs and uses thereof 有权
标题翻译： 2-亚甲基-1α-羟基-18,19,21-三维生素D3类似物及其用途
公开(公告)号：US08575136B2
公开(公告)日：2013-11-05
申请号：US11697414
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： C07C401/00 , 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 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和X 2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。

9. 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。

10. 发明授权

US07704981B2 2-methylene-1alpha,25-dihydroxy-18,19,21-trinorvitamin D3 and uses thereof 有权
标题翻译： 2-亚甲基-1α，25-二羟基-18,19,21-三维维生素D3及其用途
公开(公告)号：US07704981B2
公开(公告)日：2010-04-27
申请号：US11697436
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： 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式