公开(公告)号：US20120196915A1

公开(公告)日：2012-08-02

申请号：US13387634

申请日：2010-07-28

申请人： Ramon Mangues Bafalluy ,  Isolda Casanova Rigalt ,  Fernando Albericio Palomera ,  Mercedes Álvarez ,  Svetlana Savina

发明人： Ramon Mangues Bafalluy ,  Isolda Casanova Rigalt ,  Fernando Albericio Palomera ,  Mercedes Álvarez ,  Svetlana Savina

IPC分类号： A61K31/402 ,  A61P35/00 ,  C07D207/325

CPC分类号： C07D207/333 ,  C07D207/335

摘要： The present invention relates to a new series of 1,2-diphenylpyrroles of formula (I) or their pharmaceutically acceptable salts, or their pharmaceutically acceptable solvates, having antitumor activity, wherein R1 and R2 are individually selected from the group consisting of halogen, optionally substituted O(C1-C4)alkyl and optionally substituted (C1-C4)alkyl; and R3 is selected from the group consisting of H, (C1-C4)alkyl, CONH2 and (C═NH)NH2. It also relates to a process for preparing them, to pharmaceutical compositions containing them, and to their use for the treatment of cancer, in particular lung carcinoma, colorectal carcinoma, breast carcinoma and/or prostate carcinoma.

摘要翻译： 本发明涉及新的一系列式（I）的1,2-二苯基吡咯或其药学上可接受的盐或其药学上可接受的溶剂化物，其具有抗肿瘤活性，其中R1和R2分别选自卤素，任选地 取代的O（C 1 -C 4）烷基和任选取代的（C 1 -C 4）烷基; 并且R 3选自H，（C 1 -C 4）烷基，CONH 2和（C = NH）NH 2。 它还涉及其制备方法，含有它们的药物组合物及其用于治疗癌症，特别是肺癌，结肠直肠癌，乳腺癌和/或前列腺癌的用途。