申请人:Hoffmann-La Roche Inc.
公开号:US08163740B2
公开(公告)日:2012-04-24
The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I)
wherein X, Y, R1 and R2 are as described herein, their manufacture, and pharmaceutical compositions containing them. The active compounds of the present invention are 5-HT5A receptor antagonists, useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders, Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
本发明涉及式(I)的6-取代苯并噁唑衍生物,其中X、Y、R1和R2如本文所述,它们的制备方法以及含有它们的制药组合物。本发明的活性化合物是5-HT5A受体拮抗剂,可用于预防和/或治疗抑郁症、焦虑症、精神分裂症、惊恐障碍、广场恐惧症、社交恐惧症、强迫症、创伤后应激障碍、疼痛、记忆障碍、痴呆症、饮食行为障碍、性功能障碍、睡眠障碍、药物滥用、运动障碍、帕金森病、精神障碍或胃肠障碍。