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1. 发明申请

WO2006057885A2 17,20(E)-DEHYDRO VITAMIN D ANALOGS AND THEIR USES 审中-公开
标题翻译： 17,20（E）-DEHYDRO维生素D类似物及其用途
公开(公告)号：WO2006057885A2
公开(公告)日：2006-06-01
申请号：PCT/US2005041670
申请日：2005-11-18
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07C401/00 , A61K31/59 , A61P11/06 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 17,20(E)-dehydro vitamin D analogs, and specifically 17(E)-1a,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin 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 and inflammatory diseases in humans as well as renal osteodystrophy and obesity.
摘要翻译：本发明公开了17,20（E） - 脱氢维生素D类似物，特别是17（E）-1a，25-二羟基-17（20） - 脱氢-2-亚甲基-19-去甲维生素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，因此可用于治疗人类的自身免疫疾病和炎症性疾病以及肾性骨营养不良和肥胖。

2. 发明申请

WO2010006172A2 2-METHYLENE-20(21)-DEHYDRO-19-NOR-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-亚甲基-20（21） - 脱氢-19-维生素D类似物
公开(公告)号：WO2010006172A2
公开(公告)日：2010-01-14
申请号：PCT/US2009050110
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07C401/00 , A61K31/593 , A61P3/04 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/02
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-20(21)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19-nor-1a,25-dihydroxyvitamin 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 lower activity in vivo on bone calcium mobilization and similar in vivo intestinal calcium transport activity compared to the native hormone 1a,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-20（21） - 脱氢-19-去甲 - 维生素D类似物，特别是2-亚甲基-20（21） - 脱氢-19-去甲-1a，25-二羟基维生素D3及其药物用途。该化合物表现出相对高的转录活性以及明显的抑制未分化细胞增殖和诱导其向单核细胞分化的活性，因此证明其用作抗癌剂并用于治疗皮肤疾病例如牛皮癣以及皮肤病如皱纹，皮肤松弛，皮肤干燥和皮脂分泌不足。与天然激素1a，25-二羟基维生素D 3相比，该化合物在体内对骨钙动员和体内肠钙转运活性也表现出较低的活性，因此可用于治疗人类以及肾中的自身免疫病症或炎性疾病性骨病。该化合物也可用于治疗或预防肥胖症。

3. 发明申请

WO2010006135A3 2-METHYLENE-(17Z)-17(20)-DEHYDRO-19,21-DINOR-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-甲基 - （17Z）-17（20）-DEHYDRO-19,21-维生素D类似物
公开(公告)号：WO2010006135A3
公开(公告)日：2010-04-15
申请号：PCT/US2009050060
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07C401/00 , A61K31/593 , A61P3/04 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/02
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This invention discloses 2-methylene-(17Z)-17(20)-dehydro-19,21 -dinor-vitamin D analogs, and specifically 2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-1a,25-dihydroxyvitamin 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 has significant calcemic activity in vivo having about the same bone calcium mobilization activity and intestinal calcium transport activity as the native hormone 1a,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 - （17Z）-17（20） - 脱氢-19,21-维生素D类似物，特别是2-亚甲基 - （17Z）-17（20） - 脱氢-19,21-二 -1a，25-二羟基维生素D 3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。该化合物在体内也具有显着的钙活性，其具有与天然激素1a，25-二羟基维生素D 3大致相同的骨钙动员活性和肠钙转运活性，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

WO2006057901A3 2-METHYLENE-19-NOR-1a-HYDROXY-17-ENE-HOMOPREGNACALCIFEROL AND ITS USES 审中-公开
标题翻译： 2-甲基-19-nor-1a-羟基-17-烯丙基胆甾醇及其用途
公开(公告)号：WO2006057901A3
公开(公告)日：2006-07-13
申请号：PCT/US2005041820
申请日：2005-11-18
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07C401/00 , A61K31/59 , A61P11/06 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 2-methylene-19-nor-17-ene vitamin D analogs, and specifically 2-methylene-19-nor-1a-hydroxy-17-ene-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 aut6oimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment of obesity.
摘要翻译：本发明公开了2-亚甲基-19-去甲-17-烯维生素D类似物，特别是2-亚甲基-19-去甲-a-羟基-17-烯 - 孕孕甾醇和其药物用途。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，因此可用于治疗人类中的自身免疫性疾病和炎性疾病以及肾性骨营养不良。该化合物也可用于治疗肥胖症。

5. 发明申请

WO2006057900A2 17,20(Z)-DEHYDRO VITAMIN D ANALOGS AND THEIR USES 审中-公开
标题翻译： 17,20（Z）-DEHYDRO维生素D类似物及其用途
公开(公告)号：WO2006057900A2
公开(公告)日：2006-06-01
申请号：PCT/US2005041819
申请日：2005-11-18
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , TADI BULLI PADMAJA , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07C401/00 , A61K31/59 , A61P11/06 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 17,20(Z)-dehydro vitamin D analogs, and specifically 17(Z)-1a,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin 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 may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy and obesity. This compound also has significant calcemic activity making it a therapeutic agent for the treatment or prophylaxis of osteoporosis, osteomalacia, renal osteodystrophy and hypoparathyroidism.
摘要翻译：本发明公开了17,20（Z） - 脱氢维生素D类似物，特别是17（Z）-1a，25-二羟基-17（20） - 脱氢-2-亚甲基-19-去甲维生素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。该化合物也可用于治疗人类的自身免疫疾病和炎性疾病以及肾性骨营养不良和肥胖。该化合物还具有显着的钙血活性，使其成为用于治疗或预防骨质疏松症，骨软化症，肾性骨营养不良和甲状旁腺功能低下的治疗剂。

6. 发明申请

WO2011041579A3 (20S,22E)-2-METHYLENE-19-NOR-22-ENE-1a,25-DIHYDROXYVITAMIN D3 ANALOGS 审中-公开
标题翻译：（20S，22E）-2-甲基-19-NOR-22-ENE-1a，25-二羟基维生素D3类似物
公开(公告)号：WO2011041579A3
公开(公告)日：2011-06-03
申请号：PCT/US2010050956
申请日：2010-09-30
申请人： WISCONSIN ALUMNI RES FOUND , 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： C07C401/00 , A61K31/59 , A61P35/00 , A61P35/02
CPC分类号： C07C401/00
摘要： This invention discloses (20S.22E)-2-mcthylenc-19-nor-22-enc-1a,25- dihydroxyvitamin D3 analogs, and specifically(20S,22E)-2 -methylene- 19-nor-22-ene- 1 a,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits significant vitamin D receptor binding activity and 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, 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（20S.22E）-2-谷氨酸-19-去甲-22-enc-1a，25-二羟基维生素D 3类似物，特别是（20S，22E）-2-亚甲基-19-去甲-22-烯-1 a，25-二羟基维生素D3及其药物用途。该化合物表现出显着的维生素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显着活性，因此证明其用作抗癌剂，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。

7. 发明申请

WO2010006169A3 2-METHYLENE-19, 26-DINOR-(20S, 22E, 25R)-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-甲基-29,26-酮（20S，22E，25R） - 维他命D类似物
公开(公告)号：WO2010006169A3
公开(公告)日：2010-04-15
申请号：PCT/US2009050106
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , CHIELLINI GRAZIA , GRZYWACZ PAWELL , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , CHIELLINI GRAZIA , GRZYWACZ PAWELL , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07C401/00 , A61K31/593 , A61P3/04 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/02
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)-la,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 la,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）-la，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，皮脂分泌不足。与天然激素la，25-二羟基维生素D 3相比，该化合物在体内对钙钙动员和钙运输活性没有显示活性，因此可用于治疗人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。

8. 发明申请

WO2010006125A3 2-METHYLENE-19,26-DINOR-(20R,22E,25R)-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-甲基-19,26-DINOR-（20R，22E，25R） - 维他命D类似物
公开(公告)号：WO2010006125A3
公开(公告)日：2010-04-01
申请号：PCT/US2009050048
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , CHIELLINI GRAZIA , GRZYWACZ PAWELL , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , CHIELLINI GRAZIA , GRZYWACZ PAWELL , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07C401/00 , A61K31/593 , A61P3/04 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/02
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This invention discloses 2-methylene-19,26-dinor-(20R,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20R,22E,25R)-1a,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 relatively high intestinal calcium transport activity compared to the native hormone 1a,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-19,26-二烯 - （20R，22E，25R） - 维生素D类似物，特别是2-亚甲基-19,26-二烯 - （20R，22E，25R）-1a，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明显活性，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1a，25-二羟基维生素D3相比，该化合物在骨钙动员和体内相对较高的肠内钙转运活性中也显示出非常低的活性，因此可用于治疗人类以及肾脏中的自身免疫性疾病或炎性疾病性骨病。该化合物也可用于治疗或预防肥胖症。

9. 发明申请

WO2010006121A3 19-NOR-VITAMIN D ANALOGS WITH 3,2-DIHYDROFURAN RING 审中-公开
标题翻译： 19-NOR-VITAMIN D模拟与3,2二氢呋喃环
公开(公告)号：WO2010006121A3
公开(公告)日：2010-03-25
申请号：PCT/US2009050043
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , GLEBOCKA AGNIESZKA , SOKOLOWSKA KATARZYNA , SICINSKI RAFAL R , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , GLEBOCKA AGNIESZKA , SOKOLOWSKA KATARZYNA , SICINSKI RAFAL R , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07D307/79 , A61K31/593 , A61P3/04 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/02
CPC分类号： C07D307/79
摘要： 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 3ß-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, metabolic bone diseases, osteomalacia, osteopenia, secondary hyperparathyroidism, psoriasis, or other skin diseases.
摘要翻译：描述了具有连接类似物的A环的3β-氧和碳-2的另外的二氢呋喃环的19-维生素D类似物和药物用途。这些化合物表现出选择性的体外和体内活性，使其成为治疗或预防自身免疫性疾病，某些类型的癌症，代谢性骨病，骨软化症，骨质减少症，继发性甲状旁腺功能亢进，牛皮癣或其它皮肤疾病的治疗剂。

10. 发明申请

WO2006119309A2 19,26,27-TRINOR-1a,25-DIHYDROXYVITAMIN D3 COMPOUNDS 审中-公开
标题翻译： 19,26,27-三硝基-1a，25-二羟基维生素D3化合物
公开(公告)号：WO2006119309A2
公开(公告)日：2006-11-09
申请号：PCT/US2006016875
申请日：2006-05-02
申请人： WISCONSIN ALUMNI RES FOUND , 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： Compounds of formula (1) are provided where X 1 , X 2 , and X 3 are independently selected from H or hydroxy protecting groups, and R 1 and R 2 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，和 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。

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