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1. 发明申请

US20070238704A1 2-Substituted-1Alpha,25-Dihydroxy-19,26,27-Trinor Vitamin D Analogs and Uses Thereof 有权
标题翻译： 2-取代的1Alpha，25-二羟基-19,26,27-维生素D类似物及其用途
公开(公告)号：US20070238704A1
公开(公告)日：2007-10-11
申请号：US11697434
申请日：2007-04-06
申请人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame , Pawel Grzywacz
发明人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame , Pawel Grzywacz
IPC分类号： A61K31/695 , 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，和 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，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; 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，并且可用于治疗各种生物学条件。

2. 发明申请

US20070219168A1 19,26,27-TRINOR-1alpha,25-DIHYDROXYVITAMIN D3 COMPOUNDS 有权
标题翻译： 19,26,27-三色素-1α，25-二羟基维生素D3化合物
公开(公告)号：US20070219168A1
公开(公告)日：2007-09-20
申请号：US11756333
申请日：2007-05-31
申请人： Hector DeLuca , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59
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， SUP＆gt; 1＆gt;和＆lt; 2＆gt;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。

3. 发明申请

US20070066566A1 19,23,24,25,26,27-Hexanor-1alpha-hydroxyvitamin D3 审中-公开
标题翻译： 19,23,24,25,26,27-六氢-1α-羟基维生素D3
公开(公告)号：US20070066566A1
公开(公告)日：2007-03-22
申请号：US11523750
申请日：2006-09-19
申请人： Hector DeLuca , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/695 , 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, X1 and X2 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。还提供了在给予受试者之后形成式1A化合物的化合物。

4. 发明申请

US20080081800A1 2-Methylene-(20R,25S)-19,27-Dinor-(22E)-Vitamin D Analogs 有权
标题翻译： 2-亚甲基 - （20R，25S）-19,27-二烯（22E） - 维生素D类似物
公开(公告)号：US20080081800A1
公开(公告)日：2008-04-03
申请号：US11860870
申请日：2007-09-25
申请人： Hector DeLuca , Margaret Clagett-Dame , Lori Plum , Grazia Chiellini , Pawel Grzywacz
发明人： Hector DeLuca , Margaret Clagett-Dame , Lori Plum , Grazia Chiellini , Pawel Grzywacz
IPC分类号： A61K31/593 , A61K31/59 , A61P17/00 , A61P17/06 , A61P19/00 , A61P29/00 , A61P3/04 , A61P35/00 , A61P37/00 , C07C401/00
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)-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 - （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（22E）-1α ，25-二羟基维生素D 3 N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。

5. 发明申请

US20070270391A1 2Alpha-Methyl and 2Beta-Methyl Analogs of 19,26,27-Trinor-(20S)-1Alpha-Hydroxyvitamin D3 and Their Uses 有权
标题翻译： 19,26,27-三硝基 - （20S）-1α-羟基维生素D 3及其用途的2α-甲基和2β-甲基类似物
公开(公告)号：US20070270391A1
公开(公告)日：2007-11-22
申请号：US11775042
申请日：2007-07-09
申请人： Hector DeLuca , Lori Plum , Pawel Grzywacz , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Pawel Grzywacz , Margaret Clagett-Dame
IPC分类号： A61K31/593 , A61P43/00 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804
摘要： This invention discloses 2α-methyl and 2β-methyl analogs of 19,26,27-trinor-(20S)-1α-hydroxyvitamin D3 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.
摘要翻译：本发明公开了19,26,27-三硝基 - （20S）-1α-羟基维生素D 3 3的2α-甲基和2b-甲基类似物及其药物用途。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。这些化合物也具有很少（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。这些化合物也可用于治疗或预防肥胖症。

6. 发明申请

US20070112077A1 Des-C,D analogs of 1alpha,25-dihydroxy-19-norvitamin D3 有权
标题翻译： 1α，25-二羟基-19-去甲维生素D3的Des-C，D类似物
公开(公告)号：US20070112077A1
公开(公告)日：2007-05-17
申请号：US11512705
申请日：2006-08-30
申请人： Hector DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Katarzyna Plonska-Ocypa , Rafal Sicinski , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/045
CPC分类号： C07C401/00 , C07B2200/07 , C07C35/17 , C07C45/292 , C07C45/30 , C07C47/19 , C07C403/08 , C07C2601/14 , C07F7/1804 , Y02P20/55
摘要： Des-C,D 2-methylene-19-norvitamin D3 analogs are provided including compounds of formula 1, in which R1 is a straight or branched chain alkyl or alkylene group having from 8 to 27 carbons and bearing an Oy3 group; and y1, y2 and y3 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：提供了包含式1化合物的Des-C，D 2 - 亚甲基-19-去甲维生素D 3 N 3类似物，其中R 1是直链或支链烷基或亚烷基具有8至27个碳并具有Oy 3+基团的基团; 且y 1，y 2和y 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。

7. 发明申请

US20060264410A1 19,26,27-trinor-1alpha,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：US20060264410A1
公开(公告)日：2006-11-23
申请号：US11416401
申请日：2006-05-02
申请人： Hector DeLuca , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Pawel Grzywacz , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
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， SUP＆gt; 1＆gt;和＆lt; 2＆gt;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。

8. 发明申请

US20060116352A1 2alpha-Methyl and 2beta-methyl analogs of 19,26,27-trinor-(20S)-1alpha-hydroxyvitamin D3 and their uses 有权
标题翻译： 19,26,27-三硝基 - （20S）-1α-羟基维生素D3的2α-甲基和2beta-甲基类似物及其用途
公开(公告)号：US20060116352A1
公开(公告)日：2006-06-01
申请号：US11283124
申请日：2005-11-18
申请人： Hector DeLuca , Lori Plum , Pawel Grzywacz , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Pawel Grzywacz , Margaret Clagett-Dame
IPC分类号： A61K31/695 , A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07F7/1804
摘要： This invention discloses 2α-methyl and 2β-methyl analogs of 19,26,27-trinor-(20S) -1α-hydroxyvitamin D3 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.
摘要翻译：本发明公开了19,26,27-三硝基 - （20S）-1α-羟基维生素D 3 3的2α-甲基和2b-甲基类似物及其药物用途。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。这些化合物也具有很少（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。这些化合物也可用于治疗或预防肥胖症。

9. 发明申请

US20080081799A1 2-Methylene-(20S,25S)-19,27-Dinor-(22E)-Vitamin D Analogs 有权
标题翻译： 2-亚甲基 - （20S，25S）-19,27-二烯（22E） - 维生素D类似物
公开(公告)号：US20080081799A1
公开(公告)日：2008-04-03
申请号：US11860863
申请日：2007-09-25
申请人： Hector DeLuca , Margaret Clagett-Dame , Lori Plum , Grazia Chiellini , Pawel Grzywacz
发明人： Hector DeLuca , Margaret Clagett-Dame , Lori Plum , Grazia Chiellini , Pawel Grzywacz
IPC分类号： A61K31/593 , A61K31/59 , A61P17/00 , A61P17/06 , A61P19/00 , A61P29/00 , A61P3/04 , A61P35/00 , A61P37/00 , 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D 3 N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. 发明申请

US20070249567A1 2-Methylene-19,26,27-Trinor-(20S)-1Alpha-Hydroxyvitamin D3 and Its Uses 有权
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：US20070249567A1
公开(公告)日：2007-10-25
申请号：US11775087
申请日：2007-07-09
申请人： Hector DeLuca , Lori Plum , Pawel Grzywacz , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Pawel Grzywacz , Margaret Clagett-Dame
IPC分类号： A61K31/593 , C07C401/00 , C07C49/303
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24 , C07F7/1804 , 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)-1α-hydroxyvitamin 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-19,26,27-三硝基 - （20S） - 维生素D类似物，特别是2-亚甲基-19,26,27-三硝基 - （20S）-1α-羟基维生素D 3， / SUB>及其制药用途。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。

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