公开(公告)号：EP2292593A3

公开(公告)日：2011-05-25

申请号：EP10010651.7

申请日：2001-09-27

申请人： TopoTarget UK Limited

发明人： Watkins, Clare, J. ,  Romero-Martin, Maria-Rosario ,  Moore, Kathryn, G. ,  Richie, James ,  Finn, Paul, W. ,  Kalvinsh, Ivars ,  Loza, Einars ,  Dikovska, Klara ,  Gailite, Vija ,  Vorona, Maxim ,  Piskunova, Irina ,  Starchenkov, Igor ,  Andrianov, Victor ,  Harris, C., John ,  Duffy, James, E., S.

IPC分类号： C07C311/21 ,  C07D317/58 ,  C07D307/52 ,  C07D213/65 ,  C07D213/42 ,  C07D209/88 ,  A61K31/44 ,  A61K31/40 ,  A61K31/36 ,  A61K31/34 ,  A61P35/00 ,  A61P17/06

CPC分类号： C07D213/40 ,  C07C311/06 ,  C07C311/13 ,  C07C311/16 ,  C07C311/19 ,  C07C311/20 ,  C07C311/21 ,  C07C311/29 ,  C07C2602/08 ,  C07D209/88 ,  C07D213/42 ,  C07D213/65 ,  C07D213/71 ,  C07D307/52 ,  C07D317/58

摘要： The present invention relates to compounds of the following formula, and pharmaceutically acceptable salts and solvates thereof, wherein: A is C 5-20 heteroaryl or C 5-20 carboaryl, and is optionally substituted; Q 1 is: a covalent bond, a saturated aliphatic C 1-7 alkylene group and is optionally substituted, or a partially unsaturated aliphatic C 2-7 alkylene group and is optionally substituted; R 1 is hydrogen, C 1-7 alkyl, or C 5-20 aryl; and, Q 2 is -(CH 2 ) n - where n is 4, 5, 6, or 7. The present invention also relates to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

公开(公告)号：EP2292593A2

公开(公告)日：2011-03-09

申请号：EP10010651.7

申请日：2001-09-27

申请人： TopoTarget UK Limited

发明人： Watkins, Clare, J. ,  Romero-Martin, Maria-Rosario ,  Moore, Kathryn, G. ,  Richie, James ,  Finn, Paul, W. ,  Kalvinsh, Ivars ,  Loza, Einars ,  Dikovska, Klara ,  Gailite, Vija ,  Vorona, Maxim ,  Piskunova, Irina ,  Starchenkov, Igor ,  Andrianov, Victor ,  Harris, C., John ,  Duffy, James, E., S.

IPC分类号： C07C311/21 ,  C07D317/58 ,  C07D307/52 ,  C07D213/65 ,  C07D213/42 ,  C07D209/88 ,  A61K31/44 ,  A61K31/40 ,  A61K31/36 ,  A61K31/34 ,  A61P35/00 ,  A61P17/06

CPC分类号： C07D213/40 ,  C07C311/06 ,  C07C311/13 ,  C07C311/16 ,  C07C311/19 ,  C07C311/20 ,  C07C311/21 ,  C07C311/29 ,  C07C2602/08 ,  C07D209/88 ,  C07D213/42 ,  C07D213/65 ,  C07D213/71 ,  C07D307/52 ,  C07D317/58

摘要： The present invention relates to compounds of the following formula, and pharmaceutically acceptable salts and solvates thereof, wherein: A is C 5-20 heteroaryl or C 5-20 carboaryl, and is optionally substituted; Q 1 is: a covalent bond, a saturated aliphatic C 1-7 alkylene group and is optionally substituted, or a partially unsaturated aliphatic C 2-7 alkylene group and is optionally substituted; R 1 is hydrogen, C 1-7 alkyl, or C 5-20 aryl; and, Q 2 is -(CH 2 ) n - where n is 4, 5, 6, or 7. The present invention also relates to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐和溶剂合物，其中：A是C 5-20杂芳基或C 5-20碳芳基，并且任选被取代; Q1是：共价键，饱和脂肪族C 1-7亚烷基并且任选被取代，或者部分不饱和脂肪族C 2-7亚烷基并且被任选取代; R1是氢，C1-7烷基或C5-20芳基; 并且Q 2是 - （CH 2）n - ，其中n是4,5,6或7.本发明还涉及包含此类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应用， 抑制HDAC，并且例如抑制增殖性疾病如癌症和牛皮癣。