公开(公告)号：US20140200201A1

公开(公告)日：2014-07-17

申请号：US13780587

申请日：2013-02-28

申请人： Andrzej T. Slominski ,  Robert C. Tuckey ,  Blazej Zbytek ,  Michal A. Zmijewski ,  Minh Ngoc Nguyen ,  Zorica Janjetovic ,  Jianjun Chen ,  Wei Li ,  Duane D. Miller ,  Jordan K. Zjawiony ,  Arnold E. Postlethwaite ,  Trevor W. Sweatman

发明人： Andrzej T. Slominski ,  Robert C. Tuckey ,  Blazej Zbytek ,  Michal A. Zmijewski ,  Minh Ngoc Nguyen ,  Zorica Janjetovic ,  Jianjun Chen ,  Wei Li ,  Duane D. Miller ,  Jordan K. Zjawiony ,  Arnold E. Postlethwaite ,  Trevor W. Sweatman

IPC分类号： C07C401/00 ,  C12P7/02

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 as shown in Tables 1 and 2. Also provided is a method for producing hydroxylated metabolites of cholecalciferol or ergocalciferol via the P450scc (CYP11A1) or CYP27B1 enzyme systems where the hydroxylase has an activity to hydroxylate position C20 of a secosteroid or its 5,7-dieneal precursor 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： 本文提供的是类固醇化合物，其是雄甾-5,7-二烯或其前体-5,7-二烯和紫外线B（UVB）转化产物，其包括如表1和2所示的甾体化合物的药物组合物。还提供 是通过P450scc（CYP11A1）或CYP27B1酶系统产生胆钙化醇或麦角钙化醇的羟化代谢物的方法，其中羟化酶具有使羟基化为羟基化的第二类固醇或其5,7-二醛前体的位置C20和如此生成的羟基化代谢物的活性。 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。

公开(公告)号：US20110118228A1

公开(公告)日：2011-05-19

申请号：US12807178

申请日：2010-08-30

申请人： Andrzej Slominski ,  Wei Li ,  Blazej Zbytek ,  Robert C. Tuckey ,  Jordan K. Zjawiony ,  Minh Ngoc Nguyen ,  Zorica Janjetovic ,  Michal A. Zmijewski ,  Trevor W. Sweatman ,  Duane D. Miller ,  Jianjun Chen ,  Arnold E. Postlethwaite

发明人： Andrzej Slominski ,  Wei Li ,  Blazej Zbytek ,  Robert C. Tuckey ,  Jordan K. Zjawiony ,  Minh Ngoc Nguyen ,  Zorica Janjetovic ,  Michal A. Zmijewski ,  Trevor W. Sweatman ,  Duane D. Miller ,  Jianjun Chen ,  Arnold E. Postlethwaite

IPC分类号： A61K31/57 ,  C07J5/00 ,  C12N5/00 ,  A61P35/00 ,  A61P35/02 ,  A61P17/00 ,  A61P19/02 ,  A61P3/10 ,  A61P3/04 ,  A61P9/10 ,  C12P33/06

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 as shown in Tables 1 and 2. Also provided is a method for producing hydroxylated metabolites of cholecalciferol or ergocalciferol via the P450scc (CYP11A1) or CYP27B1 enzyme systems where the hydroxylase has an activity to hydroxylate position C20 of a secosteroid or its 5,7-dieneal precursor 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： 本文提供的是类固醇化合物，其是雄甾-5,7-二烯或其前体-5,7-二烯和紫外线B（UVB）转化产物，其包括如表1和2所示的甾体化合物的药物组合物。还提供 是通过P450scc（CYP11A1）或CYP27B1酶系统产生胆钙化醇或麦角钙化醇的羟化代谢物的方法，其中羟化酶具有使羟基化为羟基化的第二类固醇或其5,7-二醛前体的位置C20和如此生成的羟基化代谢物的活性。 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。

公开(公告)号：US20120258938A1

公开(公告)日：2012-10-11

申请号：US13460375

申请日：2012-04-30

申请人： Andrej Slominski ,  Robert C. Tuckey ,  Edith Tang ,  Elaine Tieu ,  Minh Nguyen ,  Zorica Janjetovic ,  Jianjun Chen ,  Wei Li ,  Yan Lu ,  Duane D. Miller ,  Jordan K. Zjawiony ,  Arnold E. Postlethwaite

发明人： Andrej Slominski ,  Robert C. Tuckey ,  Edith Tang ,  Elaine Tieu ,  Minh Nguyen ,  Zorica Janjetovic ,  Jianjun Chen ,  Wei Li ,  Yan Lu ,  Duane D. Miller ,  Jordan K. Zjawiony ,  Arnold E. Postlethwaite

IPC分类号： C12P15/00 ,  A61K31/593 ,  A61K8/67 ,  A61P17/00 ,  A61P17/06 ,  A61P35/00 ,  A61P37/06 ,  A61P29/00 ,  A61P25/00 ,  A61P1/00 ,  A61P3/10 ,  A61P3/04 ,  A61P9/10 ,  A61Q19/00 ,  C12N5/07 ,  A61P19/06 ,  C07C401/00

CPC分类号： C07J3/00 ,  A61K8/345 ,  A61Q19/08 ,  C07J11/00

摘要： Provided herein are steroidal compounds that are androsta-5,7-dienes or pregna-5,7-dienes and ultraviolet B (UVB) conversion products thereof and cholecalciferol derivatives hydroxylated at one or more of C1, C17, C20, C23, C24, C25, and C26 which includes pharmaceutical, cosmeceutical or nutraceutical compositions of the steroidal compounds as shown in Tables 1A, 2A and 3. Also provided is a method for producing hydroxylated metabolites of cholecalciferol via CYP11A1, CYP24, CYP27A1, or CYP27B1 enzyme systems where the hydroxylase has an activity to hydroxylate position C1 or C20 or other position of the sidechain of a secosteroid or its 5,7-dieneal precursor and the hydroxylated metabolites so produced. Methods are provided for inhibiting proliferation of either a normally or abnormally proliferating cell, for modifying immune activity, or for treating a condition associated with the proliferating or quiescent cell or immune cells by contacting the cell with or administering any of the compounds described herein.

摘要翻译： 本文提供的是甾族-5,7-二烯或前 - 5,7-二烯的甾族化合物和其紫外线B（UVB）转化产物和在C1，C17，C20，C23，C24， C25和C26，其包括如表1A，2A和3所示的甾体化合物的药物，药妆或营养组合物。还提供了通过CYP11A1，CYP24，CYP27A1或CYP27B1酶系统生产胆钙化甾醇的羟化代谢物的方法，其中 羟化酶具有羟基化位置C1或C20或类固醇或其5,7-二醛前体的侧链的其它位置和如此生成的羟基化代谢物的活性。 提供了通过使细胞与本文所述的任何化合物接触或施用任何本文所述的化合物来抑制正常或异常增殖细胞增殖，改善免疫活性或用于治疗与增殖或静止细胞或免疫细胞相关的病症的方法。