专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

81. 发明申请

US20100009945A1 19-NOR-VITAMIN D ANALOGS WITH 3,2-DIHYDROFURAN RING 有权
标题翻译： 19-NOR-VITAMIN D模拟与3,2二氢呋喃环
公开(公告)号：US20100009945A1
公开(公告)日：2010-01-14
申请号：US12171108
申请日：2008-07-10
申请人： Hector F. DeLuca , Agnieszka Glebocka , Katarzyna Sokolowska , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Agnieszka Glebocka , Katarzyna Sokolowska , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07D307/77 , A61P17/06 , A61P35/00 , A61P37/02 , A61P29/00 , A61P17/00 , A61P13/12 , A61P3/04 , A61P19/08
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。

82. 发明申请

US20090281340A1 1ALPHA-HYDROXY-2-(3'-HYDROXYPROPYLIDENE)-19-NOR-VITAMIN D COMPOUNDS AND METHODS OF MAKING AND TREATMENT THEREOF 审中-公开
标题翻译： 1ALPHA-羟基-2-（3'-羟基丙烯酰基）-19-异维生素D化合物及其制备和处理方法
公开(公告)号：US20090281340A1
公开(公告)日：2009-11-12
申请号：US12437892
申请日：2009-05-08
申请人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Agnieszka Glebocka
发明人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame , Agnieszka Glebocka
IPC分类号： C07C401/00 , C07C45/00
CPC分类号： C07C401/00 , C07C45/29 , C07C2602/24 , C07C49/443
摘要： Disclosed are 1α-hydroxy-2-(3′-hydroxypropylidene)-19-nor-vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3′-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.
摘要翻译：公开了1α-羟基-2-（3'-羟基亚丙基）-19-去甲维生素D化合物，药物组合物及其制备和处理方法。化合物通常指向生物活性的2-亚烷基-19-去甲维生素D化合物及其类似物，其特征在于在C-2存在3'-羟基亚丙基部分，并且存在没有任何的缩写的烷基侧链羟基部分。

83. 发明申请

US20080249068A1 Method of Extending the Dose Range of Vitamin D Compounds 审中-公开
标题翻译：延长维生素D剂量范围的方法
公开(公告)号：US20080249068A1
公开(公告)日：2008-10-09
申请号：US11842752
申请日：2007-08-21
申请人： Hector F. DeLuca , John W. Pike , Nirupama Shevde , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , John W. Pike , Nirupama Shevde , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/66 , A61K31/59 , A61P19/08
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 1α,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)-1α,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（可溶性RANK，由NF-κB基因表达的蛋白质）的双膦酸盐，OPG（骨保护素）或可溶性RANKL（NF-κB配体的受体活化剂）受体）和功能以阻止骨骼中钙的供应，从而防止高钙血症和软组织的钙化。因此，高剂量的1α，25-二羟基维生素D 3 N（1,25-（OH）2 N 3），其类似物，前药，或模拟物可用于以最小的患者风险来治疗目标疾病。具体地说，阿仑膦酸被显示阻断1,25-（OH）2 N 3 N 3和其非常有效的类似物2-亚甲基-19- （20S）-1α，25-二羟基维生素D 3 N，只要被治疗的受试者处于低钙饮食即可。

84. 发明申请

US20070238706A1 2-Methylene-1Alpha,25-Dihydroxy-19,21-Dinorvitamin D3 Analogs and Uses Thereof 有权
标题翻译： 2-亚甲基-1α，25-二羟基-19,21-二维生素D3类似物及其用途
公开(公告)号：US20070238706A1
公开(公告)日：2007-10-11
申请号：US11697439
申请日：2007-04-06
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki
IPC分类号： A61K31/695 , A61K31/59 , C07C401/00
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 X1, X2 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.
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。

85. 发明申请

US20070238705A1 2-Methylene-1Alpha,25-Dihydroxy-18,19,21-Trinorvitamin D3 and Uses Thereof 有权
标题翻译： 2-亚甲基-1α，25-二羟基-18,19,21-维生素D3及其用途
公开(公告)号：US20070238705A1
公开(公告)日：2007-10-11
申请号：US11697436
申请日：2007-04-06
申请人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki
发明人： Hector F. DeLuca , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki
IPC分类号： A61K31/695 , A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , 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 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。

86. 发明授权

US07241750B2 2-methylene-19-nor-1alpha-hydroxy-17-ene-homopregnacalciferol and its uses 有权
标题翻译： 2-亚甲基-19-去甲-α-羟基-17-烯 - 孕孕甾醇钙及其用途
公开(公告)号：US07241750B2
公开(公告)日：2007-07-10
申请号：US11283125
申请日：2005-11-18
申请人： Hector F. DeLuca , Bulli Padmaja Tadi , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Bulli Padmaja Tadi , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
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-1α-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 autoimmune disorders and 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-去甲-17-烯维生素D类似物，特别是2-亚甲基-19-去甲-α-羟基-17-烯 - 孕孕甾醇钙及其药物用途。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疾病和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。

87. 发明授权

US07241748B2 17,20(Z)-dehydro vitamin D analogs and their uses 有权
标题翻译： 17,20（Z） - 脱氢维生素D类似物及其用途
公开(公告)号：US07241748B2
公开(公告)日：2007-07-10
申请号：US11283090
申请日：2005-11-18
申请人： Hector F. DeLuca , Bulli Padmaja Tadi , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Bulli Padmaja Tadi , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 17,20(Z)-dehydro vitamin D analogs, and specifically 17(Z)-1α,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin 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 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）-1α，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。

88. 发明授权

US06579861B2 1&agr;-hydroxy-2-methylene-19-nor-homopregnacalciferol and its uses 有权
公开(公告)号：US06579861B2
公开(公告)日：2003-06-17
申请号：US10165123
申请日：2002-06-07
申请人： Hector F. DeLuca , Rafal R. Sicinski , Sumithra Gowlugari , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Rafal R. Sicinski , Sumithra Gowlugari , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K3159
CPC分类号： A61K8/345 , A61K8/67 , A61K31/59 , A61Q19/007 , A61Q19/08 , C07C401/00
摘要： This invention discloses 1&agr;-hydroxy-2-methylene-19-nor-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 immune disorders in humans as well as renal osteodystrophy.

89. 发明授权

US08759328B2 Once-a-week administration of 25-hydroxy vitamin D3 to sustain elevated steady-state pharmacokinetic blood concentration 有权
标题翻译：每周施用25-羟基维生素D3以维持升高的稳态药代动力学血药浓度
公开(公告)号：US08759328B2
公开(公告)日：2014-06-24
申请号：US12672190
申请日：2009-07-24
申请人： Hector F. Deluca , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. Deluca , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/593 , A61K31/592 , A61P3/02
CPC分类号： A61K31/593
摘要： An oral dosage form comprising a single dose of 25-hydroxy-vitamin D3 sufficient to elevate the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml for at least 7 days and a pharmaceutically suitable oral carrier system, wherein subsequent single doses at least every 7 days are sufficient to sustain the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml at steady-state pharmacokinetics is disclosed. A method of elevating and sustaining the blood level concentration of 25-hydroxy-vitamin D3 in a human in need thereof comprising orally administering or parenterally administering by injection or infusion, at least once every 7 days, a single dose of 25-hydroxy-vitamin D3 sufficient to elevate the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml for at least 7 days, wherein the single doses orally administered at least every 7 days are sufficient to sustain the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml at steady-state pharmacokinetics is disclosed. The human in need thereof may be a human deficient in vitamin D having a serum level concentration of 25-hydroxy-vitamin D3 less than 30 ng/ml.
摘要翻译：口服剂型，其包含单剂量的25-羟基 - 维生素D3，其足以将人体血清水平升高至30ng / ml至200ng / ml范围内的浓度至少7天，以及药学上合适的口服载体系统，其中至少每7天的后续单次剂量足以在稳定的药代动力学下将人的血清水平维持在30ng / ml至200ng / ml范围内的浓度。一种在有需要的人中提高和维持25-羟基 - 维生素D3的血液浓度的方法，包括通过注射或输注至少每7天至少一次口服给药或肠胃外给药单次剂量的25-羟基维生素 D3足以将人体血清水平升高至30ng / ml至200ng / ml范围内的浓度至少7天，其中至少每7天口服施用的单次剂量足以维持血清水平在稳定的药代动力学中，人的浓度范围为30ng / ml至200ng / ml。有需要的人可能是缺乏维生素D的人，其维生素D浓度低于30ng / ml的25-羟基维生素D3。

90. 发明授权

US08642579B2 1-desoxy-2-methylene-19-nor-vitamin D analogs and their uses 有权
标题翻译： 1-脱氧-2-亚甲基-19-维生素D类似物及其用途
公开(公告)号：US08642579B2
公开(公告)日：2014-02-04
申请号：US12895478
申请日：2010-09-30
申请人： Hector F. DeLuca , Katarzyna M. Barycka , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki , Rafal R. Sicinski , Katarzyna Plonska-Ocypa
发明人： Hector F. DeLuca , Katarzyna M. Barycka , Izabela Sibilska , Lori A. Plum , Margaret Clagett-Dame , Rafal Barycki , Rafal R. Sicinski , Katarzyna Plonska-Ocypa
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07F9/5325
摘要： This invention discloses 1-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25-hydroxy-1-desoxy-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and 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1-脱氧-2-亚甲基-19-去甲维生素D类似物，特别是（20S）-25-羟基-1-脱氧-2-亚甲基-19-去甲维生素D3及其药物用途。该化合物在阻止未分化细胞的增殖和诱导其分化为单核细胞方面表现出相对较高的结合活性和明显的活性，从而证明其用作抗癌剂，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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式