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。