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1. 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。

2. 发明申请

WO2008035207A2 2-METHYLENE-1ALPHA-HYDROXY-19,21-DINORVITAMIN D3 ANALOGS AND USES THEREOF 审中-公开
标题翻译： 2-亚甲基-1α-羟基-19,21-酮基维生素D3类似物及其用途
公开(公告)号：WO2008035207A2
公开(公告)日：2008-03-27
申请号：PCT/IB2007/003167
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
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula I are provided where X 1 and X 2 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和X 2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，并可用于治疗各种生物病症。

3. 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。

4. 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.

5. 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。

6. 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.

7. 发明申请

WO2008125901A2 2-METHYLENE-1ALPHA,25-DIHYDROXY-18,19,21-TRINORVITAMIN D3 AND USES THEREOF 审中-公开
标题翻译： 2-甲基-1ALPHA，25-二羟基-18,19,23-三氢维纳明D3及其用途
公开(公告)号：WO2008125901A2
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
CPC分类号： C07C401/00 , Y02P20/55
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.
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。

8. 发明申请

WO2008083370A2 COMPOUNDS, COMPOSTIONS, KITS AND METHODS OF USE TO ORALLY AND TOPICALLY TREAT ACNE AND OTHER SKIN CONDITIONS BY ADMINSTERING A 19-NOR CONTAINING VITAMIN D ANALOG WITH OR WITHOUT A REYINOID 审中-公开
标题翻译：化合物，组合物，使用方法和使用方法通过给予含有或不含有REYINOID的19-NOR含维生素D类似物进行口服治疗和其他皮肤病症
公开(公告)号：WO2008083370A2
公开(公告)日：2008-07-10
申请号：PCT/US2007/089193
申请日：2007-12-31
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , CLAGETT-DAME, Margaret , DELUCA, Hector, F. , NIEVES, Nirca, J. , PLUM, Lori, A. , KAISER, Mary, E. , BARYCKI, Rafal
发明人： CLAGETT-DAME, Margaret , DELUCA, Hector, F. , NIEVES, Nirca, J. , PLUM, Lori, A. , KAISER, Mary, E. , BARYCKI, Rafal
IPC分类号： A61K9/00 , A61K9/48 , A61K47/10 , A61K47/44 , A61K31/203 , A61K31/59
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)-lα-hydroxy-bishomopregnacalciferol, 19-nor- 26,27-dimethylene-20(S)-2-methylene-lα,25-dihydroxyvitamin D3, 2-methylene-lα,25- dihydroxy-( 17E)- 17(20)-dehydro- 19-nor-vitamin D3, 2-methylene- 19-nor-(24R)- 1 α,25- dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-lα,25-dihydroxyvitamin D3, 2- methylene- 19-nor- 1 α-hydroxy-pregnacalciferol, 1 α-hydroxy-2-methylene- 19-nor- homopregnacalciferol, (20R)- 1 α-hydroxy-2-methylene- 19-nor-bishomopregnacalciferol, 2- methylene- 19-nor-(20S)- 1 α-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro- 1 α-hydroxy- 19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23 -difluoro- 1 α-hydroxy- 19-nor-bishomopregnancalciferol, (2 -(3 'hydroxypropyl- 1 ',2 ' -idene)- 19,23,24-trinor-(20S)- lα-hydroxyvitamin D3, 2-methylene- 18, 19-dinor-(20S)-lα,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-cw-retmoic acid, all-trafls-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9- (2,6,6-trimethyl-l-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-methox yphenyl] -2- napthoic acid, 4-[l-(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.
摘要翻译：用于治疗各种皮肤病，包括痤疮，牛皮癣，鱼鳞病，光老化，光损伤皮肤和皮肤癌的口服和局部药物组合物，试剂盒和治疗方法。作为活性药物成分的示例性维生素D类似物包括2-亚甲基-19-去甲-20（S）-la-羟基 - 双代孕代孕甾醇，19-降-26,27-二亚甲基-20（S）-2-亚甲基-1a，25 - 二羟基维生素D3，2-亚甲基-1a，25-二羟基 - （17E）-17（20） - 脱氢-19-去甲维生素D3，2-亚甲基-19-去甲 - （24R）-1a，25-二羟基维生素 D2，2-亚甲基 - （20R，25S）-19,26-二（二）-1α，25-二羟基维生素D3，2-亚甲基-19-去甲-α-羟基 - 孕代孕甾醇，1α-羟基-2-亚甲基-19 （20R）-1α-羟基-2-亚甲基-19-去氧胆钙孕激醇，2-亚甲基-19-去甲 - （20S）-1α-羟基 - 三孕代孕代胆甾醇，2-亚甲基-23,23 （20S）-23,23-二氟-11α-羟基-19-去氧胆钙孕激醇，（2-（3'羟丙基-1'，2-羟基丙基）（20S）-L-羟基维生素D3，2-亚甲基-18,19-二烯 - （20S）-la，25-二羟基维生素D 3，其立体异构体，前体药物在口服组合物中为盐和/或其溶质。激活视黄酸受体的化合物，如视黄酰基和视黄酰酯，包括13-cw-retmo酸，全转录维甲酸（2E，4E，6Z，8E）-3,7-二甲基-9-（2， 6,6-三甲基-1-环己烯基）壬-2,4,6,8-四烯酸，9-（4-甲氧基-2,3,6-三甲基 - 苯基）-3,7-二甲基 - 壬-2 ，4,6,8-四烯酸，6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸，4- [1-（3,5,5,8,8-五甲基 - 四氢化萘-2-基）乙烯基]苯甲酸，视黄基苯甲酸，6- [2-（4,4-二甲基二氢苯并噻喃-6-基）乙炔基]吡啶-3-甲酸乙酯，视黄酸叔丁酸酯，视黄酰基频哪醇，视黄酰胆固醇，其异构体，其口服组合物的前药，其酯，其盐和/或其溶质。这些活性成分的组合表现出协同效力。

9. 发明申请

WO2006057932A3 2-METHYLENE-18,19-DINOR-1α-HYDROXY-HOMOPREGNACALCIFEROL AND ITS USES 审中-公开
公开(公告)号：WO2006057932A3
公开(公告)日：2006-06-01
申请号：PCT/US2005/042030
申请日：2005-11-18
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , BARYCKI, Rafal , PLUM, Lori, A. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, F. , BARYCKI, Rafal , 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 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.

10. 发明申请

WO2009086437A1 (20R)-23,23-DIFLUORO-2-METHYLENE-19-NOR-BISHOMOPREGNACALCIFEROL-VITAMIN D ANALOGS 审中-公开
标题翻译：（20R）-23,23-二氟-2-甲基-19-异 - 双异噻唑烷基 - 维生素D类似物
公开(公告)号：WO2009086437A1
公开(公告)日：2009-07-09
申请号：PCT/US2008/088272
申请日：2008-12-24
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： A61P17/00 , A61K31/593 , C07C401/00
CPC分类号： C07D401/00
摘要： This invention discloses (20R)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs, and specifically (20R)-23,23-difluoro-lα-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 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（20R）-23,23-二氟-2-亚甲基-19-去氧胆固醇酯 - 维生素D类似物，特别是（20R）-23,23-二氟-1a-羟基-2-亚甲基-19-不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。

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