发明授权
US06642229B2 3-Phenyl-imidazo-pyrimidine derivatives as ligands for GABA receptors
失效
3-苯基 - 咪唑并 - 嘧啶衍生物作为GABA受体的配体
- 专利标题: 3-Phenyl-imidazo-pyrimidine derivatives as ligands for GABA receptors
- 专利标题(中): 3-苯基 - 咪唑并 - 嘧啶衍生物作为GABA受体的配体
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申请号: US10296116申请日: 2002-11-22
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公开(公告)号: US06642229B2公开(公告)日: 2003-11-04
- 发明人: Wesley Peter Blackaby , Simon Charles Goodacre , David James Hallett , Andrew Jennings , Richard Thomas Lewis , Kevin William Moore , Leslie Joseph Street
- 申请人: Wesley Peter Blackaby , Simon Charles Goodacre , David James Hallett , Andrew Jennings , Richard Thomas Lewis , Kevin William Moore , Leslie Joseph Street
- 主分类号: A61K315337
- IPC分类号: A61K315337
摘要:
A class of 3-phenylimidazo(1,2-a)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; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, CO2Ra, —CONRaRb or —CRa═NORb; and Ra and Rb 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 GABAA 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.
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