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1. 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。

2. 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。

3. 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。

4. 发明授权

US08030295B2 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：US08030295B2
公开(公告)日：2011-10-04
申请号：US11756333
申请日：2007-05-31
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 , C07D401/00
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，并且R 1和R 2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。

5. 发明申请

US20110237556A1 (20S)-2-METHYLENE-19-NOR-22-DIMETHYL-1alpha,25-DIHYDROXYVITAMIN D3 AND (20R)-2-METHYLENE-19-NOR-22-DIMETHYL-1alpha,25-HYDROXYVITAMIN D3 有权
标题翻译：（20S）-2-甲基-19-异-D-二甲基-1α，25-二羟基维生素D3和（20R）-2-甲基-19-异-D-二甲基-1α，25-羟基维生素D3
公开(公告)号：US20110237556A1
公开(公告)日：2011-09-29
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 , A61P3/10 , A61P35/02 , A61P17/06 , A61P35/00 , A61P25/00 , A61P29/00 , A61P11/06 , A61P19/02 , A61P19/10 , A61P17/00 , A61Q19/00
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。

6. 发明申请

US20090186950A1 13,13-Dimethyl-des-C,D Analogs of 1Alpha,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： 1Alpha，25-二羟基-19-不维生素D3化合物的13,13-二甲基-D-C，D类似物和局部组合物剂型及其治疗皮肤病症的方法
公开(公告)号：US20090186950A1
公开(公告)日：2009-07-23
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 , A61P35/00
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-metylene-cyclohexane-1,3-diol, (1R,3R)-5-[(Z)-(S)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol, (1R,3R)-5-[(E)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol, and (1R,3R)-5-[(Z)-(R)-11′-hydroxy-5′,5′,7′,11′-tetramethyl-dodec-2′-enylidene]-2-metylene-cyclohexane-1,3-diol.
摘要翻译： 1α，25-二羟基-19-去甲维生素D 3化合物的13,13-二甲基-D-C，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 （1R，3R）-5 - [（Z） - （S）-11'-羟基-5'，5'，7'，11'-四甲基 - 十二烷基-2- （1R，3R）-5 - [（E） - （R）-11'-羟基-5'，5'，7'，11' （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。

7. 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。

8. 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。

9. 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。

10. 发明授权

US07803789B2 Vitamin D analog—RAK, methods and uses thereof 有权
标题翻译：维生素D类似物-RAK，其方法和用途
公开(公告)号：US07803789B2
公开(公告)日：2010-09-28
申请号：US11669053
申请日：2007-01-30
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
CPC分类号： C07C401/00 , A61K8/67 , A61Q19/08 , C07F7/1804 , Y02P20/55
摘要： Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is 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; 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IA或IB的化合物，其中X 1，X 2和X 3独立地选自H或羟基保护基，R 1选自具有1至8个碳原子的直链或支链烷基; 具有2-8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; 具有2-8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。

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