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1. 发明申请

WO2012151420A1 2α-METHYL AND 2β-METHYL ANALOGS OF 19,26-DINOR-1α, 25-DIHYDROXYVITAMIN D3 AND THEIR USES 审中-公开
标题翻译： 19,26-DINOR-1a，25-二羟基维生素D3及其用途的2-甲基和2-甲基类似物
公开(公告)号：WO2012151420A1
公开(公告)日：2012-11-08
申请号：PCT/US2012/036356
申请日：2012-05-03
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , CLAGETT-DAME, Margaret , GRZYWACZ, Pawel , CHIELLINI, Grazia , PLUM, Lori, A.
发明人： DELUCA, Hector, F. , CLAGETT-DAME, Margaret , GRZYWACZ, Pawel , CHIELLINI, Grazia , PLUM, Lori, A.
IPC分类号： C07C401/00 , A61K8/67 , A61K31/56 , A61P7/00 , A61P19/00 , A61P35/00 , A61P5/20
CPC分类号： C07F7/1844 , A61K8/67 , A61Q19/007 , A61Q19/08 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This invention discloses 2α-methyl and 2β-methyl analogs of 19,26-dinor-1α,25-dihydroxyvitamin D 3 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-1a，25-二羟基维生素D3的2a-甲基和2β-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状况如皱纹，松弛皮肤，干性皮肤和不足的皮脂分泌。这些化合物几乎没有体内的血钙活性，因此可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。

2. 发明申请

WO2006057884A3 2α-METHYL AND 2ß-METHYL ANALOGS OF 19,26,27-TRINOR-(20S)-1α-HYDROXYVITAMIN D3 AND THEIR USES 审中-公开
公开(公告)号：WO2006057884A3
公开(公告)日：2006-06-01
申请号：PCT/US2005/041669
申请日：2005-11-18
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , PLUM, Lori, A. , GRZYWACZ, Pawel, K. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, F. , PLUM, Lori, A. , GRZYWACZ, Pawel, K. , CLAGETT-DAME, Margaret
IPC分类号： C07C401/00 , A61K31/59 , A61P11/06 , A61P17/06 , A61P35/00 , A61P29/00 , A61P37/00
摘要： This invention discloses 2α-methyl and 2ß-methyl analogs of 19,26,27-trinor (20S)-lα-hydroxyvitamin D 3 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.

3. 发明申请

WO2008039754A1 2-METHYLENE-(20R,25S)-19,27-DINOR-(22E)-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-甲基 - （20R，25S）-19,27-DINOR-（22E） - 维他命D类似物
公开(公告)号：WO2008039754A1
公开(公告)日：2008-04-03
申请号：PCT/US2007/079384
申请日：2007-09-25
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , CHIELLINI, Grazia , GRZYWACZ, Pawel
发明人： DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , CHIELLINI, Grazia , GRZYWACZ, Pawel
IPC分类号： C07C401/00 , A61K31/59 , A61P35/00 , A61P3/04 , A61P17/06
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 2-methylene-(20R,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20R,25S)-19,27-dinor-(22E)-lα,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 - （20R，25S）-19,27-二（22E） - 维生素D类似物，特别是2-亚甲基 - （20R，25S）-19,27-二酮（22E）-la ，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。

4. 发明申请

WO2007038094A1 19,23,24,25,26,27-HEXANOR-1ALPHA-HYDROXYVITAMIN D3 审中-公开
标题翻译： 19,23,24,25,26,27-HEXANOR-1ALPHA-羟基维生素D3
公开(公告)号：WO2007038094A1
公开(公告)日：2007-04-05
申请号：PCT/US2006/036509
申请日：2006-09-19
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , GRZYWACZ, Pawel , PLUM, Lori, A. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, F. , GRZYWACZ, Pawel , PLUM, Lori, A. , CLAGETT-DAME, Margaret
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： A compound or composition is provided that comprises a compound of formula (1A), where, X 1 and X 2 are independently selected from H or hydroxy-protecting groups. Also provided are compounds that form the compound of formula (1A) after they are administered to a subject.
摘要翻译：提供了包含式（1A）化合物的化合物或组合物，其中X 1和X 2独立地选自H或羟基保护基团。还提供了在给予受试者之后形成式（1A）化合物的化合物。

5. 发明申请

WO2007028000A2 DES-C,D ANALOGS OF 1ALPHA,25-DIHYDROXY-19-NORVITAMIN D3 审中-公开
标题翻译： 1ALPHA的DES-C，D类似物，25-二羟基-19-诺维素D3
公开(公告)号：WO2007028000A2
公开(公告)日：2007-03-08
申请号：PCT/US2006/034196
申请日：2006-08-30
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , PLONSKA-OCYPA, Katarzyna , SICINSKI, Rafal , GRZYWACZ, Pawel , PLUM, Lori, A. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, F. , PLONSKA-OCYPA, Katarzyna , SICINSKI, Rafal , GRZYWACZ, Pawel , PLUM, Lori, A. , CLAGETT-DAME, Margaret
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , C07B2200/07 , C07C35/17 , C07C45/292 , C07C45/30 , C07C47/19 , C07C403/08 , C07C2601/14 , C07F7/1852 , Y02P20/55
摘要： Des -C,D 2-methylene-19-norvitamin D 3 analogs are provided including compounds of formula 1, in which R 1 is a straight or branched chain alkyl or alkylene group having from 8 to 27 carbons and bearing an OY 3 group; and Y 1 , Y 2 and Y 3 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. Formula(I)
摘要翻译： DES-C，

6. 发明申请

WO2006057886A2 2-METHYLENE-19,26,27-TRINOR-(20S)-1α-ALPHA-HYDROXYVITAMIN D3 AND ITS USES 审中-公开
标题翻译： 2-亚甲基-19,26,27-三 - （20S）-1α-羟基维生素D3及其用途
公开(公告)号：WO2006057886A2
公开(公告)日：2006-06-01
申请号：PCT/US2005/041671
申请日：2005-11-18
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , PLUM, Lori, A. , GRZYWACZ, Pawel, K. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, F. , PLUM, Lori, A. , GRZYWACZ, Pawel, K. , CLAGETT-DAME, Margaret
IPC分类号： C07C401/00 , A61K31/59 , A61P11/06 , A61P17/06 , A61P35/00 , A61P29/00 , A61P37/00
CPC分类号： C07F7/1856 , C07C401/00 , C07C2601/14 , C07C2602/24 , Y02P20/55
摘要： This invention discloses 2-methylene-19,26,27-trinor-(20S)-vitamin D analogs, and specifically 2-methylene-19,26,27-trinor-(20S)-lα-hydroxyvitamirt D 3 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-19,26,27-三环 - （20S） - 维生素D类似物，特别是2-亚甲基-19,26,27-三环 - （20S）-1α β-羟基维生素D 3及其制药用途。该化合物在阻止未分化细胞的增殖和诱导其向单核细胞的分化方面表现出明显的活性，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如皱纹，皮肤松弛，皮肤干燥，皮脂分泌不足。该化合物如果有钙化活性也很少，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。这种化合物也可以用于治疗或预防肥胖症。

7. 发明申请

WO2011119622A1 DIASTEREOMERS OF 2-METHYLENE-19-NOR-22-METHYL-1α,25- DIHYDROXYVITAMIN D3 审中-公开
标题翻译： 2-甲基-19-异-22-甲基-1a，25-二羟基维生素D3的二异氰酸酯
公开(公告)号：WO2011119622A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/029452
申请日：2011-03-22
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , FLORES, Agnieszka , GRZYWACZ, Pawel , PLUM, Lori, A. , CLAGETT-DAME, Margaret , THODEN, James, B. , HOLDEN, Hazel, M.
发明人： DELUCA, Hector, F. , FLORES, Agnieszka , GRZYWACZ, Pawel , PLUM, Lori, A. , CLAGETT-DAME, Margaret , THODEN, James, B. , HOLDEN, Hazel, M.
IPC分类号： C07C401/00 , C07F7/18 , A61K31/59 , A61P19/08 , A61P17/06 , A61P37/00
CPC分类号： C07F7/1856 , C07C401/00 , C07C2601/14 , C07C2602/24 , Y02P20/55
摘要： Compounds of formula I are provided where X 1 , X 2 , and X 3 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。

8. 发明申请

WO2009086439A2 2-METHYLENE-(20S,25S)-19,26-DINOR-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-甲基 - （20S，25S）-19,26-维生素D类似物
公开(公告)号：WO2009086439A2
公开(公告)日：2009-07-09
申请号：PCT/US2008/088275
申请日：2008-12-24
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , CHIELLINI, Grazia , GRZYWACZ, Pawel
发明人： DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , CHIELLINI, Grazia , GRZYWACZ, Pawel
IPC分类号： C07C401/00 , A61K31/593 , A61P3/14 , A61P17/06 , A61P35/02 , A61P37/06 , A61P19/02
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-lα,25- dihydroxyvitamin D 3 , 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）-19,26-二氢-α，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。

9. 发明申请

WO2008039751A2 2-METHYLENE-(20S,25S)-19,27-DINOR-(22E)-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-甲基 - （20S，25S）-19,27-酮 - （22E） - 维生素D类似物
公开(公告)号：WO2008039751A2
公开(公告)日：2008-04-03
申请号：PCT/US2007/079381
申请日：2007-09-25
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , CHIELLINI, Grazia , GRZYWACZ, Pawel
发明人： DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , CHIELLINI, Grazia , GRZYWACZ, Pawel
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 D 3 , 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）-19,27-二酮（22E） - 维生素D类似物，特别是2-亚甲基 - （20S，25S）-19,27 （22E）-1α，25-二羟基维生素D 3及其制药用途。该化合物在阻止未分化细胞的增殖和诱导其向单核细胞的分化方面表现出明显的活性，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如皱纹，皮肤松弛，皮肤干燥，皮脂分泌不足。该化合物如果有钙化活性也很少，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。这种化合物也可以用于治疗或预防肥胖症。

10. 发明申请

WO2008035228A2 2- SUBSTITUTED-1ALPHA, 25-DIHYDROXY-19,26,27-TRINOR VITAMIN D ANALOGS AND USES THEREOF 审中-公开
标题翻译： 2-取代-1α，25-二羟基-19,26,27-三羟基维生素D类似物及其用途
公开(公告)号：WO2008035228A2
公开(公告)日：2008-03-27
申请号：PCT/IB2007/003919
申请日：2007-04-06
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , PLUM, Lori, A. , CLAGETT-DAME, Margaret , GRZYWACZ, Pawel, K.
发明人： DELUCA, Hector, F. , PLUM, Lori, A. , CLAGETT-DAME, Margaret , GRZYWACZ, Pawel, K.
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of Formula (I), (II) or (III) are provided where X 1 , X 2 and X 3 are independently selected from H and hydroxy protecting groups and R 1 and R 2 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 R 3 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，并且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碳原子，具有2至8个碳原子的直链或支链链烯基，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个碳的直链和支链羟基取代的链烯基原子; 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，直链或支链羟基取代的烷基具有1至8个碳原子的基团或具有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，并可用于治疗各种生物病症。

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