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1. 发明申请

WO2011017165A8 METHOD OF PREVENTING RENAL DISEASE AND TREATING SYMPTOMS THEREOF 审中-公开
标题翻译：预防肾脏疾病及治疗其症状的方法
公开(公告)号：WO2011017165A8
公开(公告)日：2011-09-15
申请号：PCT/US2010043551
申请日：2010-07-28
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , KIM JAMES WONKEE , CLAGETT-DAME MARGARET , PLUM LORI
发明人： DELUCA HECTOR F , KIM JAMES WONKEE , CLAGETT-DAME MARGARET , PLUM LORI
IPC分类号： A61K31/593 , A61P13/12
CPC分类号： A61K31/593
摘要： The invention relates to novel methods of using 2-methylene-19-nor-20(S)-1,25- dihydroxyvitamin D3 to prevent renal disease, particularly Lupus nephritis, in a subject at risk of developing renal disease. Methods of preventing symptoms of renal disease, such as proteinuria, splenomegaly or glomerular damage are also provided. Methods of treating symptoms of renal disease, including proteinuria and splenomegaly, are also provided.
摘要翻译：本发明涉及使用2-亚甲基-19-去甲-20（S）-1,25-二羟基维生素D3预防处于发展成肾病风险的受试者的肾病，特别是狼疮肾炎的新方法。还提供了预防肾病症状的方法，例如蛋白尿，脾肿大或肾小球损伤。还提供了治疗肾病症状的方法，包括蛋白尿和脾肿大。

2. 发明申请

WO2011041579A3 (20S,22E)-2-METHYLENE-19-NOR-22-ENE-1a,25-DIHYDROXYVITAMIN D3 ANALOGS 审中-公开
标题翻译：（20S，22E）-2-甲基-19-NOR-22-ENE-1a，25-二羟基维生素D3类似物
公开(公告)号：WO2011041579A3
公开(公告)日：2011-06-03
申请号：PCT/US2010050956
申请日：2010-09-30
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , GRZYWACZ PAWEL , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , GRZYWACZ PAWEL , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07C401/00 , A61K31/59 , A61P35/00 , A61P35/02
CPC分类号： C07C401/00
摘要： This invention discloses (20S.22E)-2-mcthylenc-19-nor-22-enc-1a,25- dihydroxyvitamin D3 analogs, and specifically(20S,22E)-2 -methylene- 19-nor-22-ene- 1 a,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits significant vitamin D receptor binding activity and 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, 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（20S.22E）-2-谷氨酸-19-去甲-22-enc-1a，25-二羟基维生素D 3类似物，特别是（20S，22E）-2-亚甲基-19-去甲-22-烯-1 a，25-二羟基维生素D3及其药物用途。该化合物表现出显着的维生素D受体结合活性和转录活性，以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性，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。

3. 发明申请

WO2010006169A3 2-METHYLENE-19, 26-DINOR-(20S, 22E, 25R)-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-甲基-29,26-酮（20S，22E，25R） - 维他命D类似物
公开(公告)号：WO2010006169A3
公开(公告)日：2010-04-15
申请号：PCT/US2009050106
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , CHIELLINI GRAZIA , GRZYWACZ PAWELL , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , CHIELLINI GRAZIA , GRZYWACZ PAWELL , 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-19,26-dinor-(20S,22E,25R)- vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20S,22E,25R)-la,25- dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits 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 no activity in vivo on bone calcium mobilization and relatively low intestinal calcium transport activity compared to the native hormone la,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-29,26-二（20S，22E，25R） - 维生素D类似物，特别是2-亚甲基-19,26-二（20S，22E，25R）-la，25-二羟基维生素 D3及其制药用途。该化合物显示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，皮脂分泌不足。与天然激素la，25-二羟基维生素D 3相比，该化合物在体内对钙钙动员和钙运输活性没有显示活性，因此可用于治疗人的自身免疫性疾病或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。

4. 发明申请

WO2010006125A3 2-METHYLENE-19,26-DINOR-(20R,22E,25R)-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-甲基-19,26-DINOR-（20R，22E，25R） - 维他命D类似物
公开(公告)号：WO2010006125A3
公开(公告)日：2010-04-01
申请号：PCT/US2009050048
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , CHIELLINI GRAZIA , GRZYWACZ PAWELL , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , CHIELLINI GRAZIA , GRZYWACZ PAWELL , 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-19,26-dinor-(20R,22E,25R)-vitamin D analogs, and specifically 2-methylene-19,26-dinor-(20R,22E,25R)-1a,25- dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits 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 very low activity in vivo on bone calcium mobilization and relatively high intestinal calcium transport activity compared to 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-19,26-二烯 - （20R，22E，25R） - 维生素D类似物，特别是2-亚甲基-19,26-二烯 - （20R，22E，25R）-1a，25-二羟基维生素 D3及其制药用途。该化合物显示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，因此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，皮脂分泌不足。与天然激素1a，25-二羟基维生素D3相比，该化合物在骨钙动员和体内相对较高的肠内钙转运活性中也显示出非常低的活性，因此可用于治疗人类以及肾脏中的自身免疫性疾病或炎性疾病性骨病。该化合物也可用于治疗或预防肥胖症。

5. 发明申请

WO2010006121A3 19-NOR-VITAMIN D ANALOGS WITH 3,2-DIHYDROFURAN RING 审中-公开
标题翻译： 19-NOR-VITAMIN D模拟与3,2二氢呋喃环
公开(公告)号：WO2010006121A3
公开(公告)日：2010-03-25
申请号：PCT/US2009050043
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , GLEBOCKA AGNIESZKA , SOKOLOWSKA KATARZYNA , SICINSKI RAFAL R , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , GLEBOCKA AGNIESZKA , SOKOLOWSKA KATARZYNA , SICINSKI RAFAL R , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： C07D307/79 , A61K31/593 , A61P3/04 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/02
CPC分类号： C07D307/79
摘要： 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 3ß-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类似物和药物用途。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。

6. 发明申请

WO2006119309A2 19,26,27-TRINOR-1a,25-DIHYDROXYVITAMIN D3 COMPOUNDS 审中-公开
标题翻译： 19,26,27-三硝基-1a，25-二羟基维生素D3化合物
公开(公告)号：WO2006119309A2
公开(公告)日：2006-11-09
申请号：PCT/US2006016875
申请日：2006-05-02
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , GRZYWACZ PAWEL , PLUM LORI A , CLAGETT-DAME MARGARET
发明人： DELUCA HECTOR F , GRZYWACZ PAWEL , PLUM LORI A , CLAGETT-DAME MARGARET
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： Compounds of formula (1) are provided where X 1 , X 2 , and X 3 are independently selected from H or hydroxy protecting groups, and R 1 and R 2 have the definitions provided herein. 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（1）化合物，其中X 1，X 2和X 3独立地选自H或羟基保护基，和 R 1和R 2具有本文提供的定义。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。

7. 发明申请

WO2006057932A2 2-METHYLENE-18,19-DINOR-1a-HYDROXY-HOMOPREGNACALCIFEROL AND ITS USES 审中-公开
标题翻译： 2-METHYLENE-18,19-DINOR-1a-HYDROXY-HOMOPREGNACALCIFEROL及其用途
公开(公告)号：WO2006057932A2
公开(公告)日：2006-06-01
申请号：PCT/US2005042030
申请日：2005-11-18
申请人： WISCONSIN ALUMNI RES FOUND , 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 , A61P29/00 , A61P35/00 , A61P37/00
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-1a-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-18,19-二醇-1α-羟基 - 高级别氢化次黄甾醇及其制药用途。该化合物在阻止未分化细胞的增殖和诱导其向单核细胞的分化方面表现出明显的活性，因此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如皱纹，皮肤松弛，皮肤干燥，皮脂分泌不足。该化合物如果有钙化活性也很少，因此可用于治疗人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

WO2006057885A2 17,20(E)-DEHYDRO VITAMIN D ANALOGS AND THEIR USES 审中-公开
标题翻译： 17,20（E）-DEHYDRO维生素D类似物及其用途
公开(公告)号：WO2006057885A2
公开(公告)日：2006-06-01
申请号：PCT/US2005041670
申请日：2005-11-18
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 , A61K31/59 , A61P11/06 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07C401/00 , Y02P20/55
摘要： This invention discloses 17,20(E)-dehydro vitamin D analogs, and specifically 17(E)-1a,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D 3 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 and obesity.
摘要翻译：本发明公开了17,20（E） - 脱氢维生素D类似物，特别是17（E）-1a，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。该化合物也具有很少（如果有的话）钙活性，因此可用于治疗人类的自身免疫疾病和炎症性疾病以及肾性骨营养不良和肥胖。

9. 发明申请

WO2011041596A2 19-NOR-VITAMIN D ANALOGS WITH 1,2-OR 3,2-CYCLOPENTENE RING 审中-公开
标题翻译：具有1,2-或3,2-环戊烯环的19-NOR-维生素D类似物
公开(公告)号：WO2011041596A2
公开(公告)日：2011-04-07
申请号：PCT/US2010050984
申请日：2010-09-30
申请人： WISCONSIN ALUMNI RES FOUND , DELUCA HECTOR F , GLEBOCKA AGNIESZKA , PLUM LORI A , CLAGETT-DAME MARGARET , SICINSKI RAFAL R
发明人： DELUCA HECTOR F , GLEBOCKA AGNIESZKA , PLUM LORI A , CLAGETT-DAME MARGARET , SICINSKI RAFAL R
IPC分类号： A61K31/59 , A61P35/00 , A61P35/02 , C07C35/23 , C07C49/633 , C07F7/08
CPC分类号： C07C401/00
摘要： 19-nor-vitamin D analogs having an additional cyclopentene ring connecting carbon 1 and carbon 2, or connecting carbon 3 and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro activities, making them therapeutic agents for the treatment or prophylaxis of some types of cancers, particularly leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.
摘要翻译：描述了具有连接碳1和碳2的另外的环戊烯环或连接类似物的A环的碳3和碳-2的19-去甲 - 维生素D类似物及其药物用途。这些化合物表现出选择性的体外活性，使其成为治疗或预防某些类型的癌症，特别是白血病，结肠癌，乳腺癌，皮肤癌或前列腺癌的治疗剂。

10. 发明申请

WO2008083370A3 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：WO2008083370A3
公开(公告)日：2009-06-18
申请号：PCT/US2007089193
申请日：2007-12-31
申请人： WISCONSIN ALUMNI RES FOUND , 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 , A61K31/203 , A61K31/59 , A61K47/10 , A61K47/44
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)-la-hydroxy-bishomopregnacalciferol, 19-nor- 26,27-dimethylene-20(S)-2-methylene-la,25-dihydroxyvitamin D3, 2-methylene-la,25- dihydroxy-( 17E)- 17(20)-dehydro- 19-nor-vitamin D3, 2-methylene- 19-nor-(24R)- 1 a,25- dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-la,25-dihydroxyvitamin D3, 2- methylene- 19-nor- 1 a-hydroxy-pregnacalciferol, 1 a-hydroxy-2-methylene- 19-nor- homopregnacalciferol, (20R)- 1 a-hydroxy-2-methylene- 19-nor-bishomopregnacalciferol, 2- methylene- 19-nor-(20S)- 1 a-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro- 1 a-hydroxy- 19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23 -difluoro- 1 a-hydroxy- 19-nor-bishomopregnancalciferol, (2 -(3 'hydroxypropyl- 1 ',2 ' -idene)- 19,23,24-trinor-(20S)- la-hydroxyvitamin D3, 2-methylene- 18, 19-dinor-(20S)-la,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-去甲基（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）-19,26-二氢-17,25-二羟基维生素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，前体药物的口服组合物，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。

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