公开(公告)号：US06967195B2

公开(公告)日：2005-11-22

申请号：US10275257

申请日：2001-05-11

申请人： Robert Henry Hesse ,  Sundara Katugam Srinivasasetty Setty ,  Maurice Murdoch Pechet ,  Michael Gile

发明人： Robert Henry Hesse ,  Sundara Katugam Srinivasasetty Setty ,  Maurice Murdoch Pechet ,  Michael Gile

IPC分类号： A61K31/56 ,  C07J5/00 ,  C07J7/00 ,  C07J9/00

CPC分类号： C07J5/00 ,  A61K31/56 ,  C07J7/00 ,  C07J9/00 ,  Y02P20/55

摘要： Compounds of formula (I) in which: R1 represents a hydrogen atom or an O-protecting group; R2 represents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; R3 represents a methyl group having α- or β-configuration; X represents a C1-3 alkylene group or a valence bond; Y represents a carboxaldehyde group or a group of formula —C(R4)(R5)OR1 where R1 is as defined above and R4 and R5, which may be the same or different, are each selected from hydrogen atoms, alkyl, alkenyl and alkynyl groups such that the total carbon content of R4 and R5 does not exceed three atoms, with the proviso that X is a valence bond when both R4 and R5 are other than hydrogen; and the dotted line signifies that a double bond may optionally be present at the 16(17)-position exhibit potent cell modulating activity, including antiproliferative and antiangiogenic effects.

摘要翻译： 式（I）的化合物，其中：R 1表示氢原子或O-保护基; R 2表示羟基，低级烷氧基，甲醛，低级烷-1-烯基或羟基或低级烷氧基取代的低级烷基; R 3表示具有α-或β-构型的甲基; X表示C 1-3亚烷基或价键; Y表示甲醛基或式-C（R 4）（R 5）或其中R 1的基团， / SUP>如上所定义，R 4和R 5和R 5可以相同或不同，各自选自氢原子，烷基，烯基和炔基，例如 R 4和R 5的总碳含量不超过三个原子，条件是当R 4和R 4均为两价时，X为价键 >和R 5不同于氢; 并且虚线表示在16（17）位上任选存在双键表现出有力的细胞调节活性，包括抗增殖和抗血管生成作用。