公开(公告)号：EP2848617A1

公开(公告)日：2015-03-18

申请号：EP13787305.5

申请日：2013-05-09

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： LIU, Hong ,  ZHEN, Xuechu ,  SUN, Haifeng ,  ZHU, Liyuan ,  QIAN, Wangke ,  YU, Leiping ,  LI, Zeng ,  ZHOU, Shengbin ,  CAI, Wenxian ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D455/03 ,  A61K31/4375 ,  A61P25/00 ,  A61P25/18

CPC分类号： C07D471/14 ,  C07D455/03 ,  C07D491/147 ,  C07D491/22 ,  C07D495/14 ,  C07D495/22

摘要： The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.

摘要翻译： 本发明涉及式（I）的二芳基[a，g]喹唑啉化合物，其对映体，非对映异构体，外消旋体，混合物，药学上可接受的盐，结晶水合物或溶剂化物; 其制备方法及其在制备与多巴胺受体和5-HT受体有关的实验模型药物或用于治疗或预防与多巴胺受体和5-HT受体有关的疾病的药物中的用途。

公开(公告)号：EP2716640A1

公开(公告)日：2014-04-09

申请号：EP12793899.1

申请日：2012-04-09

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： LIU, Hong ,  ZHEN, Xuechu ,  SUN, Haifeng ,  ZHU, Liyuan ,  LI, Zeng ,  JIANG, Hualiang ,  CHEN, Kaixian ,  XIE, Xin ,  LI, Jing ,  CHEN, Ying

IPC分类号： C07D455/03 ,  A61K31/4375 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/30

CPC分类号： C07D491/153 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D455/03 ,  C07D491/056 ,  C07D491/147 ,  C07D491/22

摘要： The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.

摘要翻译： 本发明涉及由通式（I）表示的新六氢二苯并[a，g]喹啉化合物及其衍生物，对映体，非对映异构体，外消旋体及其混合物，以及其药学上可接受的盐。 本发明还涉及该化合物的制备方法，该化合物对神经系统疾病，特别是与多巴胺受体和5-羟色胺受体相关疾病具有良好的预防和治疗效果。 生物活性实验表明，该化合物有望发展成为治疗多巴胺受体和5-羟色胺受体相关疾病的新型有效化学实体，特别是精神分裂症，帕金森病，药物成瘾，偏头痛等。