公开(公告)号：EP3027612B1

公开(公告)日：2018-10-10

申请号：EP14750663.8

申请日：2014-07-29

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： MARUGAN, Juan Jose ,  XIAO, Jingbo ,  FERRER, Marc ,  SOUTHALL, Noel Terrence ,  FREE, R. Benjamin ,  SIBLEY, David Robert

IPC分类号： C07D417/12 ,  C07D281/16 ,  A61K31/554 ,  A61P25/14 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D281/16 ,  C07D417/12

摘要： The disclosure includes compounds and pharmaceutically acceptable salts of Formula (I). Certain compounds and salts of Formula (I) are selective inhibitors of the Dopamine D2 receptor. The variables R1-R4, n, and L are defined herein. The disclosure also provides methods of synthesizing compounds of Formula (I) and pharmaceutical compositions containing compounds of Formula (I). Additionally the disclosure provides methods or treating patients suffering from central nervous system disorders, including Tourette's syndrome, bipolar disorder, hyperprolactinemia, tardive dyskinesia, Huntington's chorea, psychosis, depression, or schizophrenia.

公开(公告)号：EP3027612A1

公开(公告)日：2016-06-08

申请号：EP14750663.8

申请日：2014-07-29

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： MARUGAN, Juan Jose ,  XIAO, Jingbo ,  FERRER, Marc ,  SOUTHALL, Noel Terrence ,  FREE, R. Benjamin ,  SIBLEY, David Robert

IPC分类号： C07D417/12 ,  C07D281/16 ,  A61K31/554 ,  A61P25/14 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D281/16 ,  C07D417/12

摘要： The disclosure includes compounds and pharmaceutically acceptable salts of Formula (I). Certain compounds and salts of Formula (I) are selective inhibitors of the Dopamine D2 receptor. The variables R1-R4, n, and L are defined herein. The disclosure also provides methods of synthesizing compounds of Formula (I) and pharmaceutical compositions containing compounds of Formula (I). Additionally the disclosure provides methods or treating patients suffering from central nervous system disorders, including Tourette's syndrome, bipolar disorder, hyperprolactinemia, tardive dyskinesia, Huntington's chorea, psychosis, depression, or schizophrenia.

摘要翻译： 本公开内容包括式（I）的化合物和药学上可接受的盐。 某些化合物和式（I）的盐是多巴胺D2受体的选择性抑制剂。 变量R1-R4，n和L在本文中定义。 本公开还提供了合成式（I）化合物和含有式（I）化合物的药物组合物的方法。 此外，本公开提供了方法或治疗患有中枢神经系统疾病的患者，包括图雷特综合征，双相情感障碍，高催乳素血症，迟发性运动障碍，亨廷顿舞蹈病，精神病，抑郁症或精神分裂症。