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1. 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.

2. 发明授权

US08993547B2 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-维生素D类似物及其用途
公开(公告)号：US08993547B2
公开(公告)日：2015-03-31
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： A61K31/59 , C07C401/00 , C07F9/02 , C07F9/53 , A61K31/593
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。

3. 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。

4. 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。

5. 发明授权

US08404666B2 2-substituted-1α,25-dihydroxy-19,26,27-trinor vitamin D analogs and uses thereof 有权
标题翻译： 2-取代-1α，25-二羟基-19,26,27-三核维生素D类似物及其用途
公开(公告)号：US08404666B2
公开(公告)日：2013-03-26
申请号：US11697434
申请日：2007-04-06
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Pawel Grzywacz
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Pawel Grzywacz
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula I, II or III are provided where X1, X2 and X3 are independently selected from H and hydroxy protecting groups and R1 and R2 are independently selected from H or straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms; and R3 is independently selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. 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，II或III的化合物，其中X 1，X 2和X 3独立地选自H和羟基保护基，R 1和R 2独立地选自H或具有1至8个碳原子的直链或支链烷基，直链或具有2至8个碳原子的支链烯基，具有1至8个碳原子的直链或支链羟基取代的烷基，或具有2至8个碳原子的直链和支链羟基取代的烯基; 并且R 3独立地选自具有1至8个碳原子的直链或支链烷基，具有2至8个碳原子的直链或支链烯基，具有1至8个碳原子的直链或支链羟基取代的烷基或具有2至8个碳原子的直链和支链羟基取代的烯基。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。

6. 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。

7. 发明授权

US08349818B2 Method of preventing Type 1 diabetes 有权
标题翻译：预防1型糖尿病的方法
公开(公告)号：US08349818B2
公开(公告)日：2013-01-08
申请号：US12909253
申请日：2010-10-21
申请人： Hector F. DeLuca , Jamie Nehring , Ehren N. Rudolph , Lori Plum
发明人： Hector F. DeLuca , Jamie Nehring , Ehren N. Rudolph , Lori Plum
IPC分类号： A61K31/59
CPC分类号： A61K31/593
摘要： The invention relates to novel methods of using 2α-methyl-19-nor-20(S)-1α,25-dihydroxyvitamin D3 or 2-methylene-19-nor-20(S)-1,25-dihydroxyvitamin D3 to prevent Type 1 diabetes in a subject at risk of developing Type 1 diabetes without causing hypercalcemia in the subject.
摘要翻译：本发明涉及使用2α-甲基-19-nor-20（S）-1α，25-二羟基维生素D 3或2-亚甲基-19-去甲基-2（S）-1,2-二羟基维生素D 3来防止类型 1型糖尿病患有发生1型糖尿病的风险，而不会导致该受试者的高钙血症。

8. 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。

9. 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。

10. 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。

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