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71. 发明申请

US20070105774A1 Use of calcitonin and calcitonin-like peptides to treat and prevent multiple sclerosis 有权
标题翻译：使用降钙素和降钙素样肽来治疗和预防多发性硬化症
公开(公告)号：US20070105774A1
公开(公告)日：2007-05-10
申请号：US11583267
申请日：2006-10-19
申请人： Hector DeLuca , Terrence Meehan , Bryan Becklund , Margaret Clagett-Dame
发明人： Hector DeLuca , Terrence Meehan , Bryan Becklund , Margaret Clagett-Dame
IPC分类号： A61K38/23 , A61K31/59
CPC分类号： A61K38/225 , A61K31/59 , A61K38/23 , A61K2300/00
摘要： Methods for treating and preventing multiple sclerosis by administering to a patient an effective amount of calcitonin, calcitonin-like peptides or calcitonin mimetics to a patient. Additionally, 1,25-dihydroxyvitamin D analogs can be used in combination with the calcitonin, calcitonin-like peptides or calcitonin mimetics.
摘要翻译：通过向患者施用有效量的降钙素，降钙素样肽或降钙素模拟物来治疗和预防多发性硬化的方法。此外，1,25-二羟基维生素D类似物可以与降钙素，降钙素样肽或降钙素模拟物组合使用。

72. 发明申请

US20050119242A1 Vitamin D analogs for obesity prevention and treatment 有权
标题翻译：用于肥胖预防和治疗的维生素D类似物
公开(公告)号：US20050119242A1
公开(公告)日：2005-06-02
申请号：US10997698
申请日：2004-11-24
申请人： Hector DeLuca , Margaret Clagett-Dame , Jamie Ahrens , James Ntambi , Brian Thomson
发明人： Hector DeLuca , Margaret Clagett-Dame , Jamie Ahrens , James Ntambi , Brian Thomson
IPC分类号： A61K31/59 , A61K31/592 , A61K31/593
CPC分类号： A61K31/59 , A61K31/592 , A61K31/593
摘要： Methods for treating and preventing obesity, inhibiting adipocyte differentiation, inhibiting increased SCD-1 gene transcription, and/or reducing body fat in a subject include administering at least one analog of 1α,25-dihydroxyvitamin D3 or 1α,25-dihydroxyvitamin D2 or a pharmaceutical composition that includes such an analog to a subject in need thereof. The analog may be a 19-nor vitamin D analog such as a compound of formula IA, a compound of formula IB, or a mixture thereof where the variables R1, R2, and R3 have the values described herein.
摘要翻译：用于治疗和预防肥胖症，抑制脂肪细胞分化，抑制增加的SCD-1基因转录和/或减少受试者体内脂肪的方法包括施用至少一种类似物的1α，25-二羟基维生素D 3或 1α，25-二羟基维生素D 2 N或包含与有需要的受试者类似的药物组合物。类似物可以是19-或维生素D类似物，例如式IA化合物，式IB化合物或其混合物，其中变量R 1，R 2， >，且R 3具有本文所述的值。

73. 发明申请

US20050085539A1 Method of reducing toxicity of retinoids 有权
标题翻译：类维生素A降低毒性的方法
公开(公告)号：US20050085539A1
公开(公告)日：2005-04-21
申请号：US10758794
申请日：2004-01-16
申请人： Hector DeLuca , Margaret Clagett-Dame , Margaret Highland
发明人： Hector DeLuca , Margaret Clagett-Dame , Margaret Highland
IPC分类号： A61K31/215 , C07C51/43 , C07C403/20 , C07J9/00
CPC分类号： C07C403/20 , A61K31/215 , C07C2601/16 , C07J9/00
摘要： A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group is described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably an alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window.
摘要翻译：描述了使具有游离羧基的类视黄醇的毒性最小化或降低的方法。该方法包括用高度位阻的化合物（其优选为醇）酯化类视黄醇的羧基的步骤。所得维生素A酯比起始或母体类视色素的毒性要低得多。该方法提供了毒性降低的类视黄醇酯类似物，使得其可以以最小的副作用和更大的治疗窗口口服给药。

74. 发明申请

US20070043092A1 Use of aryl hydrocarbon receptor ligand as a therapeutic intervention in angiogenesis-implicated disorders 有权
标题翻译：使用芳烃受体配体作为治疗干预血管生成相关疾病
公开(公告)号：US20070043092A1
公开(公告)日：2007-02-22
申请号：US11402581
申请日：2006-04-10
申请人： Hector DeLuca , Margaret Clagett-Dame , Jiasheng Song , Stuart Helfand , Nasim Akhtar
发明人： Hector DeLuca , Margaret Clagett-Dame , Jiasheng Song , Stuart Helfand , Nasim Akhtar
IPC分类号： A61K31/427 , C07D417/02
CPC分类号： C07D417/06 , A61K31/427
摘要： A method of treating angiogenesis-implicated disorders by selecting a subject predisposed to an angiogenesis-implicated disorder and then administering an effective amount of an endogenous aryl hydrocarbon receptor ligand or its analogs according to a formula as disclosed herein is disclosed.
摘要翻译：公开了一种通过选择倾向于血管生成相关病症的受试者，然后根据本文公开的式施用有效量的内源性芳基烃受体配体或其类似物来治疗血管生成相关病症的方法。

75. 发明申请

US20060189532A1 Use of calcitonin and calcitonin-like peptides to treat and prevent multiple sclerosis 审中-公开
公开(公告)号：US20060189532A1
公开(公告)日：2006-08-24
申请号：US11352717
申请日：2006-02-13
申请人： Hector DeLuca , Terrence Meehan , Bryan Becklund , Margaret Clagett-Dame
发明人： Hector DeLuca , Terrence Meehan , Bryan Becklund , Margaret Clagett-Dame
IPC分类号： A61K38/23
CPC分类号： A61K31/593 , A61K38/23 , A61K2300/00
摘要： Methods for treating and preventing multiple sclerosis by administering to a patient an effective amount of calcitonin, calcitonin-like peptides or calcitonin mimetics to a patient. Additionally, 1,25-dihydroxyvitamin D analogs can be used in combination with the calcitonin, calcitonin-like peptides or calcitonin mimetics.

76. 发明申请

US20130178449A1 2-Methylene-20(21)-Dehydro-19,24,25,26,27-Pentanor-Vitamin D Analogs 审中-公开
标题翻译： 2-亚甲基-20（21） - 脱氢-19,24,25,26,27-戊醇维生素D类似物
公开(公告)号：US20130178449A1
公开(公告)日：2013-07-11
申请号：US13547111
申请日：2012-07-12
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Agnieska Glebocka , Rafal R. Sicinski
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Agnieska Glebocka , Rafal R. Sicinski
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19,24,25,26,27-pentanor-1α-hydroxyvitamin 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 lower in vivo intestinal calcium transport activity as compared to the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as secondary hyperparathyroidism and 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-19,24,25,26,27-戊醇维生素D类似物，特别是2-亚甲基-20（21） - 脱氢-19,24,25,26 ，27-戊酰-1α-羟基维生素D3及其药学用途。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。与天然激素1α，25-二羟基维生素D 3相比，该化合物在骨钙动员和体内肠内钙转运活性方面的体内活性也较低，因此可用于治疗人的自身免疫性疾病或炎症性疾病继发性甲状旁腺功能亢进和肾性骨营养不良。该化合物也可用于治疗或预防肥胖症。

77. 发明授权

US08222235B2 2-methylene-19-nor-(20R)-1α-hydroxy-bishomopregnacalciferol 有权
标题翻译： 2-亚甲基-19-去 - （20R）-1α-羟基 - 双代孕代孕甾醇
公开(公告)号：US08222235B2
公开(公告)日：2012-07-17
申请号：US11282972
申请日：2005-11-18
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： A61K31/59 , C07D401/00
CPC分类号： C07C401/00 , C07F7/1804 , Y02P20/55
摘要： Compounds of formula I are provided where X1 and X2 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和X 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。

78. 发明申请

US20120071562A1 2alpha-Methyl-19-Nor-(20S)-1alpha-Hydroxy-Bishomopregnacalciferol and Its Uses 审中-公开
标题翻译： 2α-甲基-19-诺 - （20S）-1α-羟基 - 二高钙孕激素及其用途
公开(公告)号：US20120071562A1
公开(公告)日：2012-03-22
申请号：US13302709
申请日：2011-11-22
申请人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Rafal R. Sicinski , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/047 , A61P17/10
CPC分类号： C07C401/00 , C07F7/1804
摘要： This invention discloses 2α-methyl-19-nor-(20S)-vitamin D analogs, and specifically 2α-methyl-19-nor-(20S)-1α-hydroxy-bishomopregnacalciferol 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2α-甲基-19-去甲（20S） - 维生素D类似物，特别是2α-甲基-19-去甲（20S）-1α-羟基 - 双代孕代孕甾醇及其药物用途。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。

79. 发明授权

US08026220B2 C-linked glucuronide of N-(4-hydroxybenzyl) retinone, analogs thereof, and method of using the same to inhibit neoplastic cell growth 有权
标题翻译： N-（4-羟基苄基）视黄醛的C-连接葡糖苷酸及其类似物，及其用于抑制肿瘤细胞生长的方法
公开(公告)号：US08026220B2
公开(公告)日：2011-09-27
申请号：US12357737
申请日：2009-01-22
申请人： Margaret Clagett-Dame , Robert W. Curley, Jr. , Joel R. Walker , Hussein Abou-Issa , Galal A. Alshafie
发明人： Margaret Clagett-Dame , Robert W. Curley, Jr. , Joel R. Walker , Hussein Abou-Issa , Galal A. Alshafie
IPC分类号： A01N43/04 , A61K31/70 , C07H1/00 , C07C49/00
CPC分类号： C07D309/10 , C07H15/04 , C07H15/203
摘要： Compounds of the formula: are described, along with pharmaceutical compositions containing these compounds, and methods of using the compounds to prevent and to treat cancer in mammals, including humans.
摘要翻译：描述式的化合物以及含有这些化合物的药物组合物，以及使用该化合物预防和治疗包括人在内的哺乳动物的癌症的方法。

80. 发明申请

US20110195941A1 Methods of Use To Orally and Topically Treat Acne and Other Skin Conditions By Administering a 19-NOR Containing Vitamin D Analog With or Without a Retinoid 审中-公开
公开(公告)号：US20110195941A1
公开(公告)日：2011-08-11
申请号：US13087764
申请日：2011-04-15
申请人： Margaret Clagett-Dame , Hector F. DeLuca , Nirca J. Nieves , Lori A. Plum , Mary E. Kaiser
发明人： Margaret Clagett-Dame , Hector F. DeLuca , Nirca J. Nieves , Lori A. Plum , Mary E. Kaiser
IPC分类号： A61K31/59 , A61P17/00
CPC分类号： A61K31/59 , A61K8/67 , A61K9/0014 , A61K9/0053 , A61K9/0095 , A61K31/203 , A61K47/10 , A61K47/44 , A61K2800/92 , A61Q19/00 , A61Q19/004 , A61Q19/08
摘要： Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer. Exemplary vitamin D analogs as active pharmaceutical ingredients include 2-methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-1α-hydroxy-pregnacalciferol, 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-19-nor-(20S)-1α-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnancalciferol, (2-(3′ hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1α,25-dihydroxyvitamin D3, a stereoisomer thereof, a prodrug thereof in oral compositions, a salt thereof, and/or a solute thereof. Compounds that activate retinoic acid receptors, such as retinoyls and retinoyl esters, include 13-cis-retinoic acid, all-trans-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexeneyl)nona-2,4,6,8-tetraenoic acid, 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid, 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-napthoic acid, 4-[1-(3,5,5,8,8-pentamethyl-tetralin-2-yl)ethenyl]benzoic acid, retinobenzoic acid, ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl]pyridine-3-carboxylate, retinoyl t-butyrate, retinoyl pinacol, retinoyl cholesterol, an isomer thereof, a prodrug thereof for oral compositions, an ester thereof, a salt thereof, and/or, a solute thereof. Combinations of such active ingredients demonstrate synergistic efficacy.

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