申请人:——
公开号:US20030176449A1
公开(公告)日:2003-09-18
A class of 3-phenylimidazo(1,2-&agr;) pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R
1
represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, —OR
a
, —SR
a
, —SOR
a
, —SO
2
R
a
, —SO
2
NR
a
R
b
, —NR
a
R
b
, —NR
a
COR
b
, —NR
a
CO
2
R
b
, —COR
a
, CO
2
R
a
, —CONR
a
R
b
or —CR
a
═NOR
b
; and R
a
and R
b
independently represent hydrogen, hydrocarbon or a heterocyclic group.), substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, are selective ligands for GABA
A
receptors, in particular having good affinity for the a2 and/or a3 and/or a5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
1
一类3-苯基咪唑[1,2-a]嘧啶衍生物(化学式I,或其盐或前药:I),其中Y代表化学键,氧原子,或—NH—连接;Z代表可选择取代的芳基或杂芳基团;R1代表氢,碳氢化合物,杂环基团,卤素,氰基,三氟甲基,硝基,—ORa,—SRa,—SORa,—SO2Ra,—SO2NRaRb,—NRaRb,—NRaCORb,—NRaCO2Rb,—CORa,CO2Ra,—CONRaRb或—CRa═NORb;而Ra和Rb独立地代表氢,碳氢化合物或杂环基团,取代苯环的间位由一个可选择取代的芳基或杂芳基团取代,该芳基或杂芳基团直接连接或通过氧原子或—NH—连接桥接,是GABAA受体的选择性配体,特别对a2和/或a3和/或a5亚基具有良好的亲和力,因此对于治疗和/或预防中枢神经系统的不良症状,包括焦虑、抽搐和认知障碍具有益处。