公开(公告)号：US08680126B2

公开(公告)日：2014-03-25

申请号：US13820480

申请日：2011-08-29

申请人： Joan Gil Santano ,  Rodolfo Lavilla Grifols ,  Fernando Albericio Palomera ,  Alba Pérez Perarnau ,  Sara Preciado Gallego ,  Diana Ma González Gironès ,  Daniel Iglesias Serret ,  Rosario Ramón Albalate

发明人： Joan Gil Santano ,  Rodolfo Lavilla Grifols ,  Fernando Albericio Palomera ,  Alba Pérez Perarnau ,  Sara Preciado Gallego ,  Diana Ma González Gironès ,  Daniel Iglesias Serret ,  Rosario Ramón Albalate

IPC分类号： A61K31/425 ,  C07D417/00

CPC分类号： C07D277/30 ,  C07D277/12 ,  C07D277/22 ,  C07D277/24 ,  C07D277/32 ,  C07D277/56 ,  C07D417/04

摘要： Compounds of formula (I) or their pharmaceutically acceptable salts, or their stereoisomers or mixtures of stereoisomers, where: R1 is selected from the group consisting of: phenyl, and phenyl mono-, di-, or tri-substituted by a radical independently selected from the group consisting of F, Cl, Br, I, (C1-C6)-alkyl, COO—(C1-C6)-alkyl, and (C1-C6)-alkoxy; and R2 is a radical selected from the same group as R1, further including a phenyl substituted in 4-position by a radical independently selected from the group consisting of —O(CH2)CONH(CH2)3CH3 and OCH2COOC(CH3)3, a biphenyl-4-yl, thiazol-2-yl, and a thiazol-2-yl mono- or di-substituted by a radical selected from F and phenyl; inhibit cell proliferation of tumor cells independently of p53 protein and may also induce apoptosis in several tumor cells independently of p53 protein, being useful for the treatment of several types of cancer.

摘要翻译： 式（I）化合物或其药学上可接受的盐或其立体异构体或立体异构体的混合物，其中：R 1选自：苯基和被独立选择的基团单，二或三取代的苯基 （C 1 -C 6） - 烷基，COO-（C 1 -C 6） - 烷基和（C 1 -C 6） - 烷氧基; 并且R 2是选自与R 1相同的基团，还包括被独立地选自-O（CH 2）CONH（CH 2）3 CH 3和OCH 2 COOC（CH 3）3的基团在4-位取代的苯基， 联苯-4-基，噻唑-2-基和被选自F和苯基的基团单取代或二取代的噻唑-2-基; 与p53蛋白无关地抑制肿瘤细胞的细胞增殖，并且可以独立于p53蛋白诱导几种肿瘤细胞的凋亡，可用于治疗几种类型的癌症。

公开(公告)号：US20130190367A1

公开(公告)日：2013-07-25

申请号：US13820480

申请日：2011-08-29

申请人： Joan Gil Santano ,  Rodolfo Lavilla Grífols ,  Fernando Albericio Palomera ,  Alba Pérez Perarnau ,  Sara Preciado Gallego ,  Diana Mª González Gironès ,  Daniel Iglesias Serret ,  Rosario Ramón Albalate

发明人： Joan Gil Santano ,  Rodolfo Lavilla Grífols ,  Fernando Albericio Palomera ,  Alba Pérez Perarnau ,  Sara Preciado Gallego ,  Diana Mª González Gironès ,  Daniel Iglesias Serret ,  Rosario Ramón Albalate

IPC分类号： C07D277/30 ,  C07D277/24 ,  C07D277/22

CPC分类号： C07D277/30 ,  C07D277/12 ,  C07D277/22 ,  C07D277/24 ,  C07D277/32 ,  C07D277/56 ,  C07D417/04

摘要： Compounds of formula (I) or their pharmaceutically acceptable salts, or their stereoisomers or mixtures of stereoisomers, where: R1 is selected from the group consisting of: phenyl, and phenyl mono-, di-, or tri-substituted by a radical independently selected from the group consisting of F, Cl, Br, I, (C1-C6)-alkyl, COO-(C1-C6)-alkyl, and (C1-C6)-alkoxy; and R2 is a radical selected from the same group as R1, further including a phenyl substituted in 4-position by a radical independently selected from the group consisting of —O(CH2)CONH(CH2)3CH3 and OCH2COOC(CH3)3, a biphenyl-4-yl, thiazol-2-yl, and a thiazol-2-yl mono- or di-substituted by a radical selected from F and phenyl; inhibit cell proliferation of tumor cells independently of p53 protein and may also induce apoptosis in several tumor cells independently of p53 protein, being useful for the treatment of several types of cancer.

摘要翻译： 式（I）化合物或其药学上可接受的盐或其立体异构体或立体异构体的混合物，其中：R 1选自：苯基和被独立选择的基团单，二或三取代的苯基 （C 1 -C 6） - 烷基，COO-（C 1 -C 6） - 烷基和（C 1 -C 6） - 烷氧基; 并且R 2是选自与R 1相同的基团，还包括被独立地选自-O（CH 2）CONH（CH 2）3 CH 3和OCH 2 COOC（CH 3）3的基团在4-位取代的苯基， 联苯-4-基，噻唑-2-基和被选自F和苯基的基团单取代或二取代的噻唑-2-基; 与p53蛋白无关地抑制肿瘤细胞的细胞增殖，并且可以独立于p53蛋白诱导几种肿瘤细胞的凋亡，可用于治疗几种类型的癌症。