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1. 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。

2. 发明申请

US20090227545A1 METHODS OF INCREASING EPIDERMAL SKIN THICKNESS BY TOPICAL ADMINISTRATION OF A 19-NOR CONTAINING VITAMIN D COMPOUND 有权
标题翻译：通过19-NOR含维生素D化合物的局部给药增加皮肤厚度的方法
公开(公告)号：US20090227545A1
公开(公告)日：2009-09-10
申请号：US12399070
申请日：2009-03-06
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Nirca J. Nieves , Jamie Ahrens
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Nirca J. Nieves , Jamie Ahrens
IPC分类号： A61K31/59 , A61P17/00
CPC分类号： A61K31/59
摘要： Methods of increasing the thickness of the epidermal layer in the skin of a human comprising topically administering a therapeutically effective dose of an active pharmaceutical ingredient comprising a vitamin D analog including 2-methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-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-(20S)-19-nor-1α-hydroxy-trishomopregnacalciferol, 2-methylene-(20R)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-(3′hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, or 13,13-dimethyl-des-C,D analog of (20S)-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3, and pharmaceutical topical formulations and topical dosage forms thereof using a pharmaceutically suitable carrier vehicle.
摘要翻译：增加人皮肤中表皮层厚度的方法，包括局部施用治疗有效剂量的包含维生素D类似物的活性药物成分，所述维生素D类似物包括2-亚甲基-19-去甲-20（S）-1α-羟基 - （2H） - 二亚甲基-1α，25-二羟基维生素D3，2-亚甲基-19-去甲 - （24R）-1α，25-二羟基维生素D 2，2-亚甲基 -1α，25-二羟基 - （17E）-17（20） - 脱氢-19-去甲维生素D3，2-亚甲基 - （20R，25S）-19,26-二牛醇-1α，25-二羟基维生素D3，亚甲基-18,19-二烯 - （20S）-1α，25-二羟基维生素D3，2-亚甲基-19-去甲-alpha-羟基 - 孕代孕甾醇，1α-羟基-2-亚甲基-19-去高孕孕甾烷醇（20R） 1-羟基-2-亚甲基-19-去氧胆钙孕激醇，2-亚甲基 - （20S）-19-去甲-α-羟基 - 三孕代孕甾醇，2-亚甲基 - （20R）-23,23-二氟-1α-羟基（20S）-23,23-二氟-alpha-hydroxy-19-nor-bish-19-nor-bishomopregnacalciferol，2- 孕激素钙，2-（3'-羟基丙基-1'，2'-亚苯基）-19,23,24-三硝基 - （20S）-1α-羟基维生素D3或13,13-二甲基-de-C，D类似物（ 20S）-2-亚甲基-1α，25-二羟基-19-去甲维生素D3，以及使用药学上合适的载体载体的药物局部制剂及其局部剂型。

3. 发明申请

US20080096851A1 (20S)-1Alpha-Hydroxy-2-Methylene-19-Nor-Bishomopregnacalciferol and Its Uses 有权
标题翻译：（20S）-1α-羟基-2-亚甲基-19-不 - 双代孕代孕甾醇及其用途
公开(公告)号：US20080096851A1
公开(公告)日：2008-04-24
申请号：US11944150
申请日：2007-11-21
申请人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , A61P19/00
CPC分类号： A61K31/59 , C07C401/00
摘要： This invention discloses (20S)-1α-hydroxy-2-methylene-19-nor-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 immune disorders in humans as well as renal osteodystrophy.
摘要翻译：本发明公开了（20S）-1α-羟基-2-亚甲基-19-去氧胆钙孕激素及其药物用途。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，因此可用于治疗人类的免疫疾病以及肾性骨营养不良。

4. 发明申请

US20070249569A1 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：US20070249569A1
公开(公告)日：2007-10-25
申请号：US11775117
申请日：2007-07-09
申请人： Hector DeLuca , Bulli Tadi , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Bulli Tadi , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C403/00
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。

5. 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。

6. 发明申请

US20060241090A1 Use of 2-methylene-19-nor-20(S)-1alpha,25dihydroxyvitamin D3 to increase the life expectancy of human beings 有权
标题翻译：使用2-亚甲基-19-nor-20（S）-1α，25二羟基维生素D3来增加人的预期寿命
公开(公告)号：US20060241090A1
公开(公告)日：2006-10-26
申请号：US11472125
申请日：2006-06-21
申请人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59
CPC分类号： A61K31/593
摘要： This invention provides pharmaceutical uses for 2-methylene-19-nor-20(S)-1α,25-dihydroxyvitamin D3. Administration of this compound increases the life expectancy of human beings, especially elderly human beings. In particular, it increases the survival rate of females lacking estrogen, especially post-menopausal females, and reduces mortality resulting from spontaneous development of malignant tumors in both males and females.
摘要翻译：本发明提供2-亚甲基-19-去甲-20（S）-1α，25-二羟基维生素D 3 N的药用。这种化合物的施用增加了人类，特别是老年人的预期寿命。特别是增加女性缺乏雌激素，特别是绝经后女性的生存率，并降低男性和女性恶性肿瘤自发发生的死亡率。

7. 发明申请

US20060122157A1 2-Methylene-18,19-dinor-1alpha-hydroxy-homopregnacalciferol and its uses 有权
标题翻译： 2-亚甲基-18,19-二氢-1α-羟基 - 孕代孕甾醇及其用途
公开(公告)号：US20060122157A1
公开(公告)日：2006-06-08
申请号：US11283222
申请日：2005-11-18
申请人： Hector DeLuca , Rafal Barycki , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Rafal Barycki , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-18,19-dinor-vitamin D analogs, and specifically 2-methylene-18,19-dinor-1α-hydroxy-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 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-18,19-二 - 维生素D类似物，特别是2-亚甲基-18,19-二牛-1α-羟基 - 同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。

8. 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。

9. 发明授权

US08143238B2 Methods of increasing epidermal skin thickness by topical administration of a 19-nor containing vitamin D compound 有权
标题翻译：通过局部施用19-不含维生素D化合物来增加表皮皮肤厚度的方法
公开(公告)号：US08143238B2
公开(公告)日：2012-03-27
申请号：US12399070
申请日：2009-03-06
申请人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Nirca J. Nieves , Jamie Ahrens
发明人： Hector F. DeLuca , Margaret Clagett-Dame , Lori A. Plum , Nirca J. Nieves , Jamie Ahrens
IPC分类号： A61K31/59 , C07D401/00
CPC分类号： A61K31/59
摘要： Methods of increasing the thickness of the epidermal layer in the skin of a human comprising topically administering a therapeutically effective dose of an active pharmaceutical ingredient comprising a vitamin D analog including 2-methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-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-(20S)-19-nor-1α-hydroxy-trishomopregnacalciferol, 2-methylene-(20R)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-(3′hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, or 13,13-dimethyl-des-C,D analog of (20S)-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3, and pharmaceutical topical formulations and topical dosage forms thereof using a pharmaceutically suitable carrier vehicle.
摘要翻译：包括局部施用治疗有效剂量的包含维生素D类似物的活性药物成分的方法，所述维生素D类似物包括2-亚甲基-19-去甲基-20（S）-1α-羟基 - （2H） - 二亚甲基-1α，25-二羟基维生素D3，2-亚甲基-19-去甲 - （24R）-1α，25-二羟基维生素D 2，2-亚甲基 -1α，25-二羟基 - （17E）-17（20） - 脱氢-19-去甲维生素D3，2-亚甲基 - （20R，25S）-19,26-二酮-1α，25-二羟基维生素D3，亚甲基-18,19-二（20S）-1α，25-二羟基维生素D 3，2-亚甲基-19-去甲-1α-羟基 - 孕代孕甾醇，1α-羟基-2-亚甲基-19-去高孕孕甾烷醇（20R） -1α-羟基-2-亚甲基-19-去氧胆钙孕激醇，2-亚甲基 - （20S）-19-去甲-α-羟基 - 三孕代孕甾醇，2-亚甲基 - （20R）-23,23-二氟-1α-羟基（20S）-23,23-二氟-1α-羟基-19-去氧胆钙孕激醇，2-（3'-羟基脯氨酸（20S）-2-亚甲基 - （20S）-1α-羟基维生素D3或13,13-二甲基-de-C，D类似物， 1α，25-二羟基-19-去甲维生素D3，以及使用药学上合适的载体载体的药物局部制剂及其局部剂型。

10. 发明申请

US20120309719A1 (22E)-2-METHYLENE-26,27-CYCLO-22-DEHYDRO-1ALPHA-HYDROXY-19-NORVITAMIN D3 DERIVATIVES 有权
标题翻译：（22E）-2-甲基-26,27-环己基-22-脱水-1ALPHA-羟基-19-诺维生素D3衍生物
公开(公告)号：US20120309719A1
公开(公告)日：2012-12-06
申请号：US13485343
申请日：2012-05-31
申请人： Hector DeLuca , Rafal Barycki , Lori Plum , Margaret Clagett-Dame
发明人： Hector DeLuca , Rafal Barycki , Lori Plum , Margaret Clagett-Dame
IPC分类号： A61K31/593 , A61P17/06 , A61P35/02 , A61P35/00 , A61P25/00 , A61P19/04 , A61P3/10 , A61P37/06 , A61P29/00 , A61P11/06 , A61P1/00 , A61P17/00 , A61P19/08 , A61P19/10 , A61P3/02 , A61P3/04 , A61P3/14 , C07C401/00
CPC分类号： C07C401/00 , C07C2601/02 , C07C2601/14 , C07C2602/24
摘要： Cyclopropane-containing vitamin D analogs of formulas I and IV are provided. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
摘要翻译：提供了具有式I和IV的含环丙烷的维生素D类似物。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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