发明名称 Nitrogenous-ring acylguanidine derivative
摘要 [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided.;[Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.;
申请公布号 US8853242(B2) 申请公布日期 2014.10.07
申请号 US201013388872 申请日期 2010.08.05
申请人 Astellas Pharma Inc. 发明人 Kinoyama Isao;Miyazaki Takehiro;Koganemaru Yohei;Washio Takuya;Hamaguchi Wataru
分类号 A61K31/472;A61K31/47;A61K31/4709;A61P25/00;A61P25/18;A61P25/28;C07D215/48;C07D215/60;C07D217/14;C07D215/54;C07D217/02;C07D217/22;C07D217/16;C07D401/04 主分类号 A61K31/472
代理机构 Finnegan, Henderson, Farabow, Garrett & Dunner LLP 代理人 Finnegan, Henderson, Farabow, Garrett & Dunner LLP
主权项 1. A compound of formula (I) or a pharmaceutically acceptable salt thereof: (wherein the symbols have the following meanings:  : aryl, cycloalkyl, cycloalkenyl or monocyclic nitrogen-containing heterocyclic group, Z1, Z2, Z3, Z4 and Z5: one of any of them is a nitrogen atom, and the others are carbon atoms, in which the nitrogen atom is optionally oxidized to form an N-oxide, R1, R2 and R3: each independently represents H, lower alkyl, halogen, halogeno-lower alkyl, —CN, —NO2, —ORa, —S-lower alkyl, —O-halogeno-lower alkyl, —CO2Ra, —C(O)NRbRc, —SO2-lower alkyl, or -lower alkylene-ORa, R4, R5 and R6: each independently represents H, lower alkyl, cycloalkyl, halogen, halogeno-lower alkyl, —CN, —NO2, —ORa, —SO2-lower alkyl, —O-halogeno-lower alkyl, —CO2Ra, —C(O)NRbRc, —SO2-lower alkyl, or lower alkylene-ORa, Ra, Rb and Rc: each independently represents H or lower alkyl, and R7 and R8: each independently represents H or lower alkyl).
地址 Chuo-Ku, Tokyo JP