公开(公告)号：EP1471063A1

公开(公告)日：2004-10-27

申请号：EP03290490.6

申请日：2003-02-28

申请人： Exonhit Therapeutics S.A.

发明人： Leblond, Bertrand ,  Petit, Silvère ,  Picard, Virginie ,  Taverne, Thierry ,  Schweighoffer, Fabien

IPC分类号： C07D309/38 ,  C07D407/14 ,  A61K31/351 ,  A61K31/381 ,  A61K31/4709 ,  A61P35/00

CPC分类号： C07D405/12 ,  C07D411/12

摘要： The present invention relates to compounds having a general formula (1) and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having antiproliferative and antiangiogenic activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, or associated with unregulated angiogenesis including growth and metastasis of solid tumors, ocular diseases and especially retinopathies, or arthritis, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers, ocular diseases and arthritis.

摘要翻译： 喹啉衍生物（I）及其互变异构体，光学和几何异构体，外消旋体，盐，水合物或混合物是新的。 式（I）的喹啉衍生物及其互变异构体，光学和几何异构体，外消旋体，盐，水合物或混合物是新的。 式（a1）的R 1吡喃衍生物，式（a2）的哌啶衍生物，式（a3）的二氢吡咯衍生物，式（a4）的烷烃衍生物或式（a5）的胺衍生物; R 2H，3-6C烷基或3-6C烯基; B：卤素，优选氯，羟基，O-CH 2 -O-CH 3（MOM），O-CH 2 -O-CH 2 -CH 2 -O-CH 3（MEM），OSO 2-烷基或OSi（ CH 3）2tBu; D：O，NR 3，CR'R“或S; X，Y：O，S或基团NR 4; R 3 H，烷基，羧酸酯，酰基，羧酰胺或SO 2 - 烷基; R'，R“：H或烷基; R 4H，1-10C烷基，芳基或芳烷基; 接头：（CH 2）n; n：1-10; （可选地被杂原子（优选N，O，S和P）或羰基或芳基二烷基（优选二甲苯基）中断;和式（a6-a7）的A：喹啉衍生物，式（a8）的苯并嘧啶衍生物或式 式（a9）的苯并噻吩衍生物（均为任选取代的）。[图像]活性：细胞抑制;抗血管生成;血管性;抗关节炎;抗糖尿病;眼科学。作用机制：无给予。

公开(公告)号：EP1541549A1

公开(公告)日：2005-06-15

申请号：EP03293143.8

申请日：2003-12-12

申请人： Exonhit Therapeutics S.A.

发明人： Leblond, Bertrand ,  Beausoleil, Eric

IPC分类号： C07C259/10 ,  C07C233/80 ,  C07C259/06 ,  A61K31/167 ,  A61P35/00

CPC分类号： C07C259/10 ,  C07C233/80 ,  C07C259/06 ,  C07C2602/10

摘要： The present invention relates to compounds and methods for inhibiting histone deacetylase enzymatic activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit histone deacetylases (HDACs), and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, and also central nervous system diseases. It further deals with processes for preparing said compounds.

摘要翻译： 本发明涉及抑制组蛋白脱乙酰酶酶活性的化合物和方法。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制组蛋白脱乙酰酶（HDAC），以及在治疗HDAC介导的病症，癌症，增殖性病症 ，牛皮癣以及中枢神经系统疾病。 它还涉及制备所述化合物的方法。