公开(公告)号：US20080275058A1

公开(公告)日：2008-11-06

申请号：US12065565

申请日：2005-11-23

申请人： Churlmin Seong ,  Nosang Park ,  Jinil Choi ,  Wookyu Park ,  Jaeyang Kong ,  Chulmin Park

发明人： Churlmin Seong ,  Nosang Park ,  Jinil Choi ,  Wookyu Park ,  Jaeyang Kong ,  Chulmin Park

IPC分类号： A61K31/496 ,  C07D401/04 ,  A61P25/28 ,  A61P25/24

CPC分类号： C07D215/38

摘要： The present invention relates to compounds of N-substituted -1H-quinoline-2,4-diones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of N-substituted-1H-quinoline-2,4-diones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by methamphetamine and don't show rotatod deficit in mice. Thereof the compounds according to the present invention may be valuably used for treatment if a 5HT6 receptor relating disorder

摘要翻译： 本发明涉及作为5HT6受体拮抗剂的N-取代的-1H-喹啉-2,4-二酮的化合物及其制备方法，以及含有该化合物的治疗中枢神经系统病症的药物组合物。 根据本发明的N-取代-1H-喹啉-2,4-二酮的化合物对5HT6受体具有优异的结合亲和力，对5HT6受体的选择性优于其他受体。 此外，化合物反转甲基苯丙胺对PPI的破坏，并且在小鼠中不显示旋转异物。 根据本发明的化合物可以有价值地用于治疗，如果5HT6受体相关疾病

公开(公告)号：US20090203708A1

公开(公告)日：2009-08-13

申请号：US12304670

申请日：2006-07-05

申请人： Churlmin Seong ,  Nosang Park ,  Jinil Choi ,  Chul Min Park ,  Wookyu Park ,  Jaeyang Kong

发明人： Churlmin Seong ,  Nosang Park ,  Jinil Choi ,  Chul Min Park ,  Wookyu Park ,  Jaeyang Kong

IPC分类号： A61K31/496 ,  C07D403/10 ,  A61P25/28

CPC分类号： C07D239/96 ,  C07D401/06 ,  C07D405/06

摘要： Disclosed herein are novel substituted-1H-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted-1H-quinazoline-2,4-dione derivatives are excellent in binding affinity and selectivity for 5-HT6 receptors over other receptors, inhibit serotonin(5-HT)-stimulated cAMP accumulation, and disrupt apomorphine(2 mg/kg, i.p.)-induced hyperactivity in rats. Thanks to these effects, the derivatives are useful in the treatment of 5-HT6 receptor-related central nervous system diseases.

摘要翻译： 本文公开了新的取代的1H-喹唑啉-2,4-二酮衍生物，其制备方法和含有该化合物的药物组合物。 新型取代的1H-喹唑啉-2,4-二酮衍生物对5-HT6受体与其他受体的结合亲和力和选择性优异，抑制5-羟色胺（5-HT）刺激的cAMP积聚，并破坏阿扑吗啡（2mg / kg ，ip）诱导大鼠活动过度。 由于这些效果，衍生物可用于治疗5-HT6受体相关的中枢神经系统疾病。

公开(公告)号：US20060084676A1

公开(公告)日：2006-04-20

申请号：US11242665

申请日：2005-10-04

申请人： Churlmin Seong ,  Nosang Park ,  Yungsik Jung ,  Jinil Choi ,  Wookyu Park ,  Heeyung Cho ,  Jaeyang Kong ,  Daeyoung Jung ,  Sunhee Kang ,  Sukjin Song ,  Kyungran Kwark

发明人： Churlmin Seong ,  Nosang Park ,  Yungsik Jung ,  Jinil Choi ,  Wookyu Park ,  Heeyung Cho ,  Jaeyang Kong ,  Daeyoung Jung ,  Sunhee Kang ,  Sukjin Song ,  Kyungran Kwark

IPC分类号： A61K31/4704 ,  C07D215/36

CPC分类号： C07C233/55 ,  C07C235/38 ,  C07C237/20 ,  C07C271/44 ,  C07C275/42 ,  C07D215/22

摘要： The present invention relates to compounds of 3-aryl-3-methyl-quinoline-2,4-diones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of 3-aryl-3-methyl-quinoline-2,4-diones according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders because of its excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors.

摘要翻译： 本发明涉及作为5HT6受体拮抗剂的3-芳基-3-甲基 - 喹啉-2,4-二酮的化合物，其制备方法和含有该化合物的药物组合物，用于治疗中枢神经系统疾病。 根据本发明的3-芳基-3-甲基 - 喹啉-2,4-二酮的化合物可以有价值地用于治疗5HT6受体相关疾病，因为其对5HT6受体具有优异的结合亲和力，并且对于 5HT6受体超过其他受体。

公开(公告)号：US07592457B2

公开(公告)日：2009-09-22

申请号：US11242665

申请日：2005-10-04

申请人： Churlmin Seong ,  Nosang Park ,  Yungsik Jung ,  Jinil Choi ,  Wookyu Park ,  Heeyung Cho ,  Jaeyang Kong ,  Daeyoung Jung ,  Sunhee Kang ,  Sukjin Song ,  Kyungran Kwark

发明人： Churlmin Seong ,  Nosang Park ,  Yungsik Jung ,  Jinil Choi ,  Wookyu Park ,  Heeyung Cho ,  Jaeyang Kong ,  Daeyoung Jung ,  Sunhee Kang ,  Sukjin Song ,  Kyungran Kwark

IPC分类号： C07D215/38

CPC分类号： C07C233/55 ,  C07C235/38 ,  C07C237/20 ,  C07C271/44 ,  C07C275/42 ,  C07D215/22

摘要： The present invention relates to compounds of 3-aryl-3-methyl-quinoline-2,4-diones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of 3-aryl-3-methyl-quinoline-2,4-diones according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders because of its excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors.

摘要翻译： 本发明涉及作为5HT6受体拮抗剂的3-芳基-3-甲基 - 喹啉-2,4-二酮的化合物，其制备方法和含有该化合物的药物组合物，用于治疗中枢神经系统疾病。 根据本发明的3-芳基-3-甲基 - 喹啉-2,4-二酮的化合物可以有价值地用于治疗5HT6受体相关疾病，因为其对5HT6受体具有优异的结合亲和力，并且对于 5HT6受体超过其他受体。

公开(公告)号：US20100035866A1

公开(公告)日：2010-02-11

申请号：US12293965

申请日：2006-03-28

申请人： Churlmin Seong ,  Jinil Choi ,  Chul Min Park ,  Wookyu Park ,  Jaeyang Kong ,  Sunhee Kang ,  Chimin Park

发明人： Churlmin Seong ,  Jinil Choi ,  Chul Min Park ,  Wookyu Park ,  Jaeyang Kong ,  Sunhee Kang ,  Chimin Park

IPC分类号： A61K31/5415 ,  C07D285/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/24 ,  A61P25/22 ,  A61P25/32

CPC分类号： C07D285/24

摘要： The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.

摘要翻译： 本发明涉及作为5HT6受体拮抗剂的取代-1,1-二氧代 - 苯并[1,2,4]噻二嗪-3-酮的化合物，其制备方法和含有该化合物的药物组合物，其用于治疗 中枢神经系统疾病。 根据本发明的取代的-1,1-二氧代 - 苯并[1,2,4]噻二嗪-3-酮的化合物对5HT6受体具有优异的结合亲和力，对其它受体的5HT6受体的选择性优异。 此外，化合物反转了阿朴吗啡对PPI的破坏，并且在小鼠中不显示旋转异位缺陷。 因此，根据本发明的化合物可以有价值地用于治疗5HT6受体相关疾病。