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11. 发明申请

WO2012118154A1 パーシャルアゴニスト活性を持つ新規ビタミンD受容体モジュレーター审中-公开
标题翻译：新维生素D受体调节剂，具有局部激动剂活性
公开(公告)号：WO2012118154A1
公开(公告)日：2012-09-07
申请号：PCT/JP2012/055254
申请日：2012-03-01
申请人：学校法人日本大学 , 学校法人立教学院 , 槇島誠 , 山田幸子 , アントニオモウリーニョ , 常盤広明 , 工藤健 , 渡曾友祐 , 前川和樹
发明人：槇島　誠 , 山田幸子 , アントニオ　モウリーニョ , 常盤　広明 , 工藤　健 , 渡曾　友祐 , 前川　和樹
IPC分类号： C07C401/00 , A61K31/59 , A61P3/10 , A61P9/00 , A61P17/06 , A61P19/10 , A61P25/28 , A61P31/00 , A61P35/00 , A61P37/06 , A61P43/00
CPC分类号： C07C401/00 , C07C2601/14 , C07C2602/24 , C07C2603/74
摘要：　選択的ビタミンD受容体モジュレーターとして機能して、高カルシウム血症を誘導せずにその他の作用を引き起こす作用選択性または組織選択性を有する化合物を提供する。下記の式(I)で表される化合物、その溶媒和物又はそのプロドラッグ。（式中、ｍ及びｎはそれぞれ独立に１又は０であり、Ｒは水素原子又はアルキル基であり、Ｙはエタン-1,1-ジイル基又はエチン-1,2-ジイル基であり、Ｚ 1 は水素原子であり、Ｚ 2 はヒドロキシアルコキシ基であるか、あるいは、Ｚ 1 とＺ 2 が共同してメチレン基を形成する）
摘要翻译：提供作为选择性维生素D受体调节剂的化合物，并且具有诱导其他作用而不引起高钙血症的作用选择性或组织选择性。由式（I）表示的化合物，其溶剂合物或其前药。（式中，m和n各自独立地为1或0，R为氢原子或烷基，Y为乙烷-1,1-二基或乙炔-1,2-二基，Z1为氢原子，Z2是羟基烷氧基，或者Z1和Z2共同形成亚甲基。）

12. 发明申请

WO2012044689A1 (20R,25S)-2-METHYLENE-19,26-DINOR-1α, 25-DIHYDROXYVITAMIN D3 IN CRYSTALLINE FORM 审中-公开
标题翻译：（20R，25S）-2-甲基-19,26-DINOR-1a，25-二羟基维生素D3在结晶形式
公开(公告)号：WO2012044689A1
公开(公告)日：2012-04-05
申请号：PCT/US2011/053693
申请日：2011-09-28
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, F. , GRZYWACZ, Pawel , THODEN, James, B. , HOLDEN, Hazel
发明人： DELUCA, Hector, F. , GRZYWACZ, Pawel , THODEN, James, B. , HOLDEN, Hazel
IPC分类号： C07C401/00
CPC分类号： C07C401/00 , C07B2200/13 , C07C2601/14 , C07C2602/24
摘要： A method of purifying (20R,25S)-2-methylene-l9,26-dinor-lα,25-dihydroxyvitamin D 3 to obtain (20R,25S)-2-methylene-l9,26-dinor-lα,25-dihydroxyvitamin D 3 in crystalline form. The method includes the steps of preparing a solvent of methanol and water, dissolving a product containing (20R,25S)-2-methylene-19,26-dinor-lα,25-dihydroxyvitamin D 3 to be purified in the solvent, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of (20R,25S)-2-methylene-19,26-dinor-lα,25-dihydroxyvitamin D 3 crystals, and recovering the (20R,25S)-2-methylene-19,26-dinor-la,25-dihydroxyvitamin D 3 crystals.
摘要翻译：（20R，25S）-2-亚甲基-19,26-二氢-α，25-二羟基维生素D3的纯化方法，得到（20R，25S）-2-亚甲基-19,26-二氢-α，25-二羟基维生素D 3 呈结晶状。该方法包括以下步骤：制备甲醇和水的溶剂，将含有待纯化的（20R，25S）-2-亚甲基-19,26-二酮-d1，25-二羟基维生素D3的产物溶解在溶剂中，冷却溶剂并将产物溶解在环境温度以下足够的时间以形成（20R，25S）-2-亚甲基-19,26-二氢-1α-二氢 - 羟基维生素D3晶体的沉淀物，并回收（20R，25S） - 2-亚甲基-29,26-二氢-1α，25-二羟基维生素D 3晶体。

13. 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。

14. 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。

15. 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。

16. 发明申请

WO2010120698A1 VITAMIN D RECEPTOR AGONISTS AND USES THEREOF 审中-公开
标题翻译：维生素D受体激动剂及其用途
公开(公告)号：WO2010120698A1
公开(公告)日：2010-10-21
申请号：PCT/US2010/030777
申请日：2010-04-12
申请人： VIDASYM, LLC , KAWAI, Megumi
发明人： KAWAI, Megumi
IPC分类号： C07C401/00 , A61K31/59 , A61P7/00 , A61P9/00
CPC分类号： C07C401/00 , C07C2602/50
摘要： Disclosed is a compound of Formula (I), in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, and a are defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition comprising a compound or salt therof of Formula (I) and a method of treating a disease which benefits from the modulation of the vitamin D receptor, such as a bone disorder, cardiovascular disease, a cardiovascular complication associated with renal disease, endothelial dysfunction, hyperparathyroidism, hypocalcemia, an immune disorder, left ventricular hypertrophy, a proliferative disease, proteinuria, renal disease, and thrombosis.
摘要翻译：公开了式（I）的化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，X和a如本文所定义。还公开了包含式（I）的化合物或盐的药物组合物和治疗受益于维生素D受体调节的疾病的方法，例如骨骼疾病，心血管疾病，与肾脏相关的心血管并发症疾病，内皮功能障碍，甲状旁腺功能亢进，低钙血症，免疫疾病，左心室肥大，增殖性疾病，蛋白尿，肾脏疾病和血栓形成。

17. 发明申请

WO2009108388A8 ENZYMATIC PRODUCTION OR CHEMICAL SYNTHESIS AND USES FOR 5,7-DIENES AND UVB CONVERSION PRODUCTS THEREOF 审中-公开
标题翻译：合成生产或化学合成及其用于5,7-二烯和UVB转化产物的用途
公开(公告)号：WO2009108388A8
公开(公告)日：2010-07-01
申请号：PCT/US2009001324
申请日：2009-03-02
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： SLOMINSKI ANDRZEJ , LI WEI , ZBYTEK BLAZEJ , TUCKEY ROBERT C , ZJAWIONY JORDAN K , NGUYEN MINH NGOC , ZMIJEWSKL MICHAL A , JANJETOVIC ZORICA , SWEATMAN TREVOR W , MILLER DUANE D , CHEN JIANJUN
IPC分类号： A61K8/63 , A61P35/00 , C07J3/00 , C07J11/00
CPC分类号： C07C401/00 , A61K8/63 , A61K2800/81 , A61K2800/94 , A61Q19/00 , C07J3/00 , C07J11/00 , C12P7/02
摘要： Provided herein are steroidal compounds that are androsta-5,7-dienes or a pregna-5,7-dienes and ultraviolet B (UVB) conversion products thereof which includes pharmaceutical compositions of the steroidal compounds. Also provided is a method for producing hydroxylated metabolites of cholecalciferol via the P450scc (CYPl IA 1) or CYP27B 1 enzyme systems and the hydroxylated metabolites so produced. In addition, a method for inhibiting proliferation of either a normally or abnormally proliferating cell by contacting the cell with any of the compounds described herein. A related method is provided of treating a condition associated with the proliferating cell such as a cancer, a skin disorder, a defect in cell differentiation, cosmetic, prophylaxsis, or healthy cell maintenance.
摘要翻译：本文提供的甾族化合物是雄激素-5,7-二烯或其前体-5,7-二烯和紫外线B（UVB）转化产物，其包括甾体化合物的药物组合物。还提供了通过P450scc（CYP119A）或CYP27B1酶系统和如此制备的羟基化代谢产物来产生胆钙化甾醇的羟基化代谢物的方法。此外，通过使细胞与本文所述的任何化合物接触来抑制正常或异常增殖细胞增殖的方法。提供了一种相关方法来治疗与增殖细胞相关的病症，例如癌症，皮肤病症，细胞分化缺陷，化妆品，预防或健康细胞维持。

18. 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。

19. 发明申请

WO2010006169A2 2-METHYLENE-19, 26-DINOR-(20S, 22E, 25R)-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-METHYLENE-19,26-DINOR-（20S，22E，25R） - 维生素D类似物
公开(公告)号：WO2010006169A2
公开(公告)日：2010-01-14
申请号：PCT/US2009/050106
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , 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)-lα,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 lα,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-19,26-二酮（20S，22E，25R） - 维生素D类似物，特别是2-亚甲基-19,26-二酮（20S，22E， 25R）-1α，25-二羟基维生素D3及其药物用途。该化合物表现出转录活性以及在阻止未分化细胞增殖和诱导其向单核细胞分化中的明显活性，因此证明其用作抗癌剂并用于治疗皮肤疾病例如牛皮癣以及皮肤病症例如皱纹，皮肤松弛，皮肤干燥和皮脂分泌不足。与天然激素Iα，25-二羟基维生素D 3相比，该化合物在体内对骨钙动员没有活性和相对低的肠钙转运活性，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。这种化合物也可以用于治疗或预防肥胖症。

20. 发明申请

WO2010006162A2 2-METHYLENE-(20E)-20(22)-DEHYDRO-19-NOR-VITAMIN D ANALOGS 审中-公开
标题翻译： 2-亚甲基 - （20E）-20（22） - 脱氢-19-维生素D类似物
公开(公告)号：WO2010006162A2
公开(公告)日：2010-01-14
申请号：PCT/US2009/050094
申请日：2009-07-09
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION , DELUCA, Hector, E. , TADI, Padmaja, Bulli , PLUM, Lori, A. , CLAGETT-DAME, Margaret
发明人： DELUCA, Hector, E. , TADI, Padmaja, Bulli , PLUM, Lori, A. , CLAGETT-DAME, Margaret
IPC分类号： C07C401/00 , A61K31/593
CPC分类号： C07C401/00
摘要： This invention discloses 2-methylene-(20E)-20(22)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-(20E)-20(22)-dehydro-19-nor-lα,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 shows lower activity in vivo on bone calcium mobilization and similar in vivo intestinal calcium transport activity compared to the native hormone lα,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 - （20E）-20（22） - 脱氢-19-去甲 - 维生素D类似物，特别是2-亚甲基 - （20E）-20（22） - 脱氢 -19-去甲-1α，25-二羟基维生素D3及其药物用途。该化合物表现出相对高的转录活性以及明显的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并用于治疗皮肤疾病例如牛皮癣以及皮肤病如皱纹，皮肤松弛，皮肤干燥和皮脂分泌不足。与天然激素Iα，25-二羟基维生素D 3相比，该化合物在体内对骨钙动员和体内肠钙转运活性也表现出较低的活性，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性骨病。这种化合物也可以用于治疗或预防肥胖症。

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