申请人:Sepracor Inc.
公开号:US07884124B2
公开(公告)日:2011-02-08
This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure:
wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O−X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.
本发明提供了D-氨基酸氧化酶的新型抑制剂,以及包括本发明化合物的制药组合物。本发明还提供了用于治疗和预防神经系统疾病,如神经精神疾病和神经退行性疾病,以及疼痛、共济失调和抽搐的方法。本发明化合物具有以下一般结构:
其中A为NH或S。Q为选择自CR1和N的成员。X和Y是独立选择自O、S、CR2、N和NH的成员。R1、R2和R4是独立选择自H和F的成员,但至少选择自R1、R2和R4中的一个成员为F。R6为选择自O−X+和OH的成员,其中X+为正离子,其为选择自无机正离子和有机正离子的成员。