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71. 发明申请

WO2005051323A3 VITAMIN D ANALOGS FOR OBESITY PREVENTION AND TREATMENT 审中-公开
标题翻译：维生素D类似物的预防和治疗
公开(公告)号：WO2005051323A3
公开(公告)日：2005-07-07
申请号：PCT/US2004039625
申请日：2004-11-24
申请人： WISCONSIN ALUMNI RES FOUND , CLAGETT-DAME MARGARET , DELUCA HECTOR F , AHRENS JAMIE M , NTAMBI JAMES M , THOMSON BRIAN
发明人： CLAGETT-DAME MARGARET , DELUCA HECTOR F , AHRENS JAMIE M , NTAMBI JAMES M , THOMSON BRIAN
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 1a,25-dihydroxyvitamin D3 or 1a,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给予至少一种1a，25-二羟基维生素D3或1a，25-二羟基维生素D 2或药物组合物，其包括与有需要的受试者的类似物。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R1，R2和R3具有本文所述的值。

72. 发明申请

WO2005051323A2 VITAMIN D ANALOGS FOR OBESITY PREVENTION AND TREATMENT 审中-公开
标题翻译：维生素D类似物用于肥胖预防和治疗
公开(公告)号：WO2005051323A2
公开(公告)日：2005-06-09
申请号：PCT/US2004/039625
申请日：2004-11-24
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , CLAGETT-DAME, Margaret , DELUCA, Hector, F. , AHRENS, Jamie, M. , NTAMBI, James, M. , THOMSON, Brian
发明人： CLAGETT-DAME, Margaret , DELUCA, Hector, F. , AHRENS, Jamie, M. , NTAMBI, James, M. , THOMSON, Brian
IPC分类号： A61K
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 1a,25-dihydroxyvitamin D3 or 1a,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：用于治疗和预防受试者中肥胖，抑制脂肪细胞分化，抑制增加的SCD-1基因转录和/或减少体内脂肪的方法包括施用至少一种1a，25-二羟基维生素D3或 1a，25-二羟基维生素D 2或包含这种类似物的药物组合物给有需要的受试者。类似物可以是19-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R1，R2和R3具有本文所述的值。

73. 发明申请

WO2004065358A2 METHOD OF REDUCING TOXICITY OF RETINOIDS 审中-公开
标题翻译：降低视黄酸毒性的方法
公开(公告)号：WO2004065358A2
公开(公告)日：2004-08-05
申请号：PCT/US2004/001325
申请日：2004-01-16
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , CLAGETT-DAME, Margaret , HIGHLAND, Margaret, A.
发明人： DELUCA, Hector, F. , CLAGETT-DAME, Margaret , HIGHLAND, Margaret, A.
IPC分类号： C07C403/20
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。该方法包括用高度空间位阻的化合物（其优选为醇）酯化类维生素A的羧基的步骤。由此产生的类视黄醇酯比起始或母体类视色素的毒性小得多。该方法提供了毒性降低的类视黄醇酯类似物，因此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

WO03003987A3 SOLID PHASE SYNTHESIS OF ARYLRETINAMIDES 审中-公开
标题翻译：芳基酰胺的固相合成
公开(公告)号：WO03003987A3
公开(公告)日：2003-07-17
申请号：PCT/US0221452
申请日：2002-07-08
申请人： UNIV OHIO STATE RES FOUND , CURLEY ROBERT W JR , MERSHON SERENA M , BARNETT DEREK W , CLAGETT-DAME MARGARET , CHAPMAN JASON S
发明人： CURLEY ROBERT W JR , MERSHON SERENA M , BARNETT DEREK W , CLAGETT-DAME MARGARET , CHAPMAN JASON S
IPC分类号： A61K20060101 , A61K31/16 , A61K31/165 , A61K31/195 , C07C231/02 , C07C233/05 , C07C233/57 , C07C233/64 , C07C237/20
CPC分类号： C07C403/20 , C07C2601/16
摘要： A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent ; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride ; adding pyridine and a select arylamine to the resulting mixture ; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.
摘要翻译：提供了用于制备芳基乙酰胺的固相合成方法。该方法包括使六氯丙酮与溶剂悬浮的树脂结合的三苯基膦反应以提供包含活化的氯化剂的悬浮液; 使视黄酸与活化的氯化试剂反应以提供视黄酰氯; 向得到的混合物中加入吡啶和选择的芳基胺; 并将所得混合物搅拌一段时间并保持足以使所选择的芳基胺与视黄酰氯反应并提供芳基视黄酰胺的温度。还提供了可通过本发明方法制备的精选芳基乙酰胺，以及使用此类芳基乙酰胺在癌细胞中诱导凋亡的方法。

75. 发明申请

WO2012166938A2 (22E)-2-METHYLENE-26,27-CYCLO-22-DEHYDRO-1ALPHA-HYDROXY-19-NORVITAMIN D3 DERIVATIVES 审中-公开
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：WO2012166938A2
公开(公告)日：2012-12-06
申请号：PCT/US2012/040235
申请日：2012-05-31
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector , BARYCKI, Rafal , PLUM, Lori , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector , BARYCKI, Rafal , PLUM, Lori , CLAGETT-DAME, Margaret
IPC分类号： 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。

76. 发明申请

WO2011119622A1 DIASTEREOMERS OF 2-METHYLENE-19-NOR-22-METHYL-1α,25- DIHYDROXYVITAMIN D3 审中-公开
标题翻译： 2-甲基-19-异-22-甲基-1a，25-二羟基维生素D3的二异氰酸酯
公开(公告)号：WO2011119622A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/029452
申请日：2011-03-22
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , FLORES, Agnieszka , GRZYWACZ, Pawel , PLUM, Lori, A. , CLAGETT-DAME, Margaret , THODEN, James, B. , HOLDEN, Hazel, M.
发明人： DELUCA, Hector, F. , FLORES, Agnieszka , GRZYWACZ, Pawel , PLUM, Lori, A. , CLAGETT-DAME, Margaret , THODEN, James, B. , HOLDEN, Hazel, M.
IPC分类号： C07C401/00 , C07F7/18 , A61K31/59 , A61P19/08 , A61P17/06 , A61P37/00
CPC分类号： C07F7/1856 , C07C401/00 , C07C2601/14 , C07C2602/24 , 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 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，X 2和X 3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。

77. 发明申请

WO2011041599A2 6-METHYLVITAMIN D3 ANALOGS AND THEIR USES 审中-公开
标题翻译： 6-甲基维生素D3类似物及其用途
公开(公告)号：WO2011041599A2
公开(公告)日：2011-04-07
申请号：PCT/US2010/050989
申请日：2010-09-30
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Haector, F. , PLUM, Lori, A. , CLAGETT-DAME, Margaret , SOKOLOWSKA, Katarzyna , MOURINO, Antonio , SICINSKI, Rafal, R.
发明人： DELUCA, Haector, F. , PLUM, Lori, A. , CLAGETT-DAME, Margaret , SOKOLOWSKA, Katarzyna , MOURINO, Antonio , SICINSKI, Rafal, R.
IPC分类号： A61K31/593 , C07C35/21 , A61P13/12 , A61P17/06 , A61P19/10 , A61P35/00
CPC分类号： C07C401/00
摘要： This invention discloses 6-methylvitamin D3 analogs, and specifically lα,25- dihydroxy-6-methylvitamin D3, and pharmaceutical uses therefor. This compound exhibits vitamin D receptor binding activity and transcription activity as well as 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. This compound also exhibits low in vivo calcemic activity, but because it binds the receptor with the same affinity as the native hormone calcitriol, it may act as an antagonist to inhibit development of hypercalcemia.
摘要翻译：本发明公开了6-甲基维生素D 3类似物，特别是1α，25-二羟基-6-甲基维生素D 3及其药物用途。该化合物表现出维生素D受体结合活性和转录活性以及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，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。该化合物还具有低的体内钙血活性，但是因为它以与天然激素钙三醇相同的亲和力结合受体，所以它可以作为抑制高钙血症发展的拮抗剂。

78. 发明申请

WO2011041590A3 1-DESOXY-2-METHYLENE-19-NOR-VITAMIN D ANALOGS AND THEIR USES 审中-公开
公开(公告)号：WO2011041590A3
公开(公告)日：2011-04-07
申请号：PCT/US2010/050977
申请日：2010-09-30
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , SIBILSKA, Izabela , BARYCKA, Katarzyna, M. , SICINSKI, Rafal, R. , PLONSKA-OCYPA, Katarzyna , BARYCKI, Rafal , PLUM, Lori, A. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, F. , SIBILSKA, Izabela , BARYCKA, Katarzyna, M. , SICINSKI, Rafal, R. , PLONSKA-OCYPA, Katarzyna , BARYCKI, Rafal , PLUM, Lori, A. , CLAGETT-DAME, Margaret
IPC分类号： C07C401/00 , A61K31/59 , A61P35/00 , A61P35/02
摘要： This invention discloses l-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25 -hydroxy- l-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.

79. 发明申请

WO2011041590A2 1-DESOXY-2-METHYLENE-19-NOR-VITAMIN D ANALOGS AND THEIR USES 审中-公开
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：WO2011041590A2
公开(公告)日：2011-04-07
申请号：PCT/US2010050977
申请日：2010-09-30
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , SIBILSKA IZABELA , BARYCKA KATARZYNA M , SICINSKI RAFAL R , PLONSKA-OCYPA KATARZYNA , BARYCKI RAFAL , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , SIBILSKA IZABELA , BARYCKA KATARZYNA M , SICINSKI RAFAL R , PLONSKA-OCYPA KATARZYNA , BARYCKI RAFAL , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： A61K31/593 , A61P13/12 , A61P17/06 , A61P19/10 , A61P35/00 , C07C35/21 , C07F9/28
CPC分类号： C07C401/00 , C07F9/5325
摘要： This invention discloses l-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-25 -hydroxy- l-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。该化合物显示出相对高的结合活性和明显的阻止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，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。

80. 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。

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