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1. 发明申请

WO2013032846A1 2-METHYLENE-19,23,24-TRINOR-1α-HYDROXYVITAMIN D3 审中-公开
标题翻译： 2-甲基-1,2,3,24-三氢-1a-羟基维生素D3
公开(公告)号：WO2013032846A1
公开(公告)日：2013-03-07
申请号：PCT/US2012/052029
申请日：2012-08-23
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , GLEBOCKA, Agnieszka , SICINSKI, Rafal
发明人： DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , GLEBOCKA, Agnieszka , SICINSKI, Rafal
IPC分类号： C07C401/00 , A61K31/59 , A61P35/00 , A61P17/06
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24 , Y02P20/55
摘要： Compounds of Formula (I) are provided where R 1 and R 2 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R 1和R 2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。

2. 发明申请

WO2013003307A1 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-甲基 - （22E）-25-十六烷基-24-OXO-26,27-环C-22-脱氢-19-异维生素D类似物
公开(公告)号：WO2013003307A1
公开(公告)日：2013-01-03
申请号：PCT/US2012/044130
申请日：2012-06-26
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , BARYCKI, Rafal
发明人： DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , BARYCKI, Rafal
IPC分类号： C07C401/00 , A61K31/59 , A61P17/06 , A61P35/00
CPC分类号： C07C401/00 , 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-hexanoyI-24- oxo-26,27-cycIo-22-dehydro-19-nor-lα-hydroxyvitamin D 3 , 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-去甲基-L-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内的自身免疫性疾病或炎性疾病以及肾，骨营养不良。该化合物也可用于治疗或预防肥胖症。

3. 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。

4. 发明申请

WO2010006121A2 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：WO2010006121A2
公开(公告)日：2010-01-14
申请号：PCT/US2009/050043
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , 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 3β-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类似物以及药物用途。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。

5. 发明申请

WO2009026265A1 A METHOD OF EXTENDING THE DOSE RANGE OF VITAMIN D COMPOUNDS 审中-公开
标题翻译：一种延长维生素D化合物剂量范围的方法
公开(公告)号：WO2009026265A1
公开(公告)日：2009-02-26
申请号：PCT/US2008/073535
申请日：2008-08-19
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , PIKE, John, W. , SHEVDE, Nirupama , PLUM, Lori, A. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, F. , PIKE, John, W. , SHEVDE, Nirupama , PLUM, Lori, A. , CLAGETT-DAME, Margaret
IPC分类号： A61K31/00 , A61K31/59 , A61K31/593 , A61K31/663 , A61K45/06 , A61P19/08 , A61P19/10 , A61P5/18
CPC分类号： A61K45/06 , A61K31/565 , A61K31/593 , A61K2300/00
摘要： Inhibitors of bone calcium resorption are administered, and calcium intake in the subject's diet is restricted, to allow high doses of vitamin D compounds or mimetics to be given with the intent of treating diseases such as metabolic bone diseases, hyperparathyroidism, cancer, psoriasis, and autoimmune diseases without the dangers of calcification of kidney, heart, and aorta. Inhibitors of bone calcium resorption include the bis-phosphonates, OPG (osteoprotegerin) or the soluble RANKL (receptor activator of NF-κB ligand) receptor known as sRANK (soluble RANK which is the protein expressed by the NF-κB gene), and function to block the availability of calcium from bone thereby preventing hypercalcemia and the resulting calcification of soft tissues. Thus, high doses of lα,25-dihydroxyvitamin D3 (1,25-(OH)2D3), its analogs, prodrugs, or mimetics can be utilized to treat the target disease with minimal risk to a patient. Specifically, alendronate is shown to block the bone calcium mobilization activity of both 1,25-(OH)2D3 and its very potent analog, 2-methylene-19-nor-(20S)-lα,25-dihydroxyvitamin D3, as long as the subject being treated is on a low calcium diet.
摘要翻译：施用骨钙吸收的抑制剂，受限饮食中的钙摄入受到限制，以允许给予高剂量的维生素D化合物或模拟物，其目的是治疗诸如代谢性骨疾病，甲状旁腺功能亢进，癌症，牛皮癣和自身免疫性疾病，无肾脏，心脏和主动脉钙化的危险。骨钙吸收抑制剂包括称为sRANK的双膦酸盐，OPG（骨保护素）或可溶性RANKL（NF-βB配体受体活化剂）受体（可溶性RANK，其是由NF-κB基因表达的蛋白质），并且具有阻止骨从钙的可用性的作用，从而防止高钙血症和由此产生的软组织钙化。因此，可以利用高剂量的la，25-二羟基维生素D3（1,25-（OH）2D3），其类似物，前药或模拟物来以最小的风险对患者进行目标疾病的治疗。具体来说，阿仑膦酸被证明阻止1,25-（OH）2D3及其非常有效的类似物，2-亚甲基-19-去甲（20S）-la，25-二羟基维生素D 3的骨钙动员活性，只要被治疗的对象是低钙饮食。

6. 发明申请

WO2008125901A8 2-METHYLENE-1ALPHA,25-DIHYDROXY-18,19,21-TRINORVITAMIN D3 AND USES THEREOF 审中-公开
公开(公告)号：WO2008125901A8
公开(公告)日：2008-10-23
申请号：PCT/IB2007/003971
申请日：2007-04-06
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , PLUM, Lori, A. , CLAGETT-DAME, Margaret , BARYCKI, Rafal
发明人： DELUCA, Hector, F. , PLUM, Lori, A. , CLAGETT-DAME, Margaret , BARYCKI, Rafal
IPC分类号： C07C401/00 , A61K31/59 , A61P19/08 , A61P19/10 , A61P3/04 , A61P37/00
摘要： Compounds of formula I are provided where X 1 , X 2 and X3 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

7. 发明申请

WO2008023278A2 1 ALPHA-HYDROXY-2-(3'-HYDROXYPROPYLIDENE) 19-NOR-VITAMIN D COMPOUNDS WITH A 1,1-DIMETHYLPROPYL SIDE CHAIN 审中-公开
标题翻译： 1个ALPHA-羟基-2-（3'-羟基丙烯酰）具有1,1-二甲基丙烯酰胺链的19-非 - 维生素D化合物
公开(公告)号：WO2008023278A2
公开(公告)日：2008-02-28
申请号：PCT/IB2007/003643
申请日：2007-04-06
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , GLEBOCKA, Angieszka , SICINSKI, Rafal, R. , PLUM, Lori, A. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, F. , GLEBOCKA, Angieszka , SICINSKI, Rafal, R. , PLUM, Lori, A. , CLAGETT-DAME, Margaret
CPC分类号： C07C401/00 , C07F7/1856
摘要： This invention discloses lα-hydroxy-2-(3'-hydroxypropylidene)-19-nor- vitamin D compounds with a 1,1-dimethylpropyl side chain, 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：本发明公开了具有1,1-二甲基丙基侧链的α-羟基-2-（3'-羟基亚丙基）-19-去甲维生素D化合物及其制药用途。这些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，因此可用于治疗人类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。

8. 发明申请

WO2007118198A2 2-METHYLENE-1α,25-DIHYDROXY-19,21-DINORVITAMIN D3 ANALOGS AND USES THEREOF 审中-公开
标题翻译： 2-甲基-1a，25-二羟基-19,21-维生素D3模拟物及其用途
公开(公告)号：WO2007118198A2
公开(公告)日：2007-10-18
申请号：PCT/US2007/066154
申请日：2007-04-23
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F , PLUM, Lori, A. , CLAGETT-DAME, Margaret , BARYCKI, Rafal
发明人： DELUCA, Hector, F , PLUM, Lori, A. , CLAGETT-DAME, Margaret , BARYCKI, Rafal
IPC分类号： C07C401/00 , A61K8/67 , A61K31/59 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P11/06 , A61P35/00 , A61P5/20
CPC分类号： A61Q19/08 , A61K8/342 , A61K8/585 , A61K8/63 , A61Q19/06 , C07C401/00 , 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 are 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。

9. 发明申请

WO2006057885A3 17,20(E)-DEHYDRO VITAMIN D ANALOGS AND THEIR USES 审中-公开
公开(公告)号：WO2006057885A3
公开(公告)日：2006-06-01
申请号：PCT/US2005/041670
申请日：2005-11-18
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , 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 , A61P35/00 , A61P29/00 , A61P37/00
摘要： This invention discloses 17,20(E)-dehydro vitamin D analogs, and specifically 17(E)-1α,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.

10. 发明申请

WO2012151058A1 (20S)-24-(P-TOLUENESULFONYLOXY)-25,26,27-TRINORVITAMIN D3 ANALOGS AND THEIR USES 审中-公开
标题翻译：（20S）-24-（对 - 戊二烯氧基）-25,26,27-三硝基维生素D3类似物及其用途
公开(公告)号：WO2012151058A1
公开(公告)日：2012-11-08
申请号：PCT/US2012/034266
申请日：2012-04-19
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , BARYCKI, Rafal
发明人： DELUCA, Hector, F. , CLAGETT-DAME, Margaret , PLUM, Lori, A. , BARYCKI, Rafal
IPC分类号： A61K31/593 , C07C309/73 , A61P35/00
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This invention discloses (20S)-24-( p -toluenesulfonyloxy)-25,26,27-trinorvitarnin D 3 analogs, and especially (20S)-25,26,27-trinor-24-|( p -methyiphenylsulfonate)-vitamin D 3 , its biological activities, and pharmaceutical uses therefor. This compound exhibits relatively little calcemic activity and does not promote cellular differentiation of HL-60 leukemia cells, but rather kills the cells. This cell death activity is found in small cell lung carcinoma also, but not in prostate, bone or ovarian cancer cells. This compound thus causes specific cell death in the absence of changes in calcium levels and without general toxicity in an animal. Therefore it might serve as a useful therapy for treatment of some forms of cancer, such as leukemia and lung cancer.
摘要翻译：本发明公开了（20S）-24-（对甲苯磺酰氧基）-25,26,27-三硝维生素D3类似物，特别是（20S）-25,26,27-三硝基-24-（对甲基亚苯基磺酸酯） - 维生素D3 ，其生物活性及其制药用途。该化合物显示相对较少的钙血活性，并且不促进HL-60白血病细胞的细胞分化，而是杀死细胞。这种细胞死亡活动也在小细胞肺癌中发现，但在前列腺，骨或卵巢癌细胞中也没有。因此，该化合物在没有钙水平的变化并且在动物中没有一般毒性的情况下引起特异性细胞死亡。因此，它可能是治疗某些形式的癌症（如白血病和肺癌）的有用治疗方法。

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