2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
申请人:Schering Corporation
公开号:US20040220194A1
公开(公告)日:2004-11-04
Compounds having the structural formula I
1
or a pharmaceutically acceptable salt thereof, wherein
R is
2
R
1
, R
2
, R
3
, R
4
and R
5
are H, alkyl or alkoxyalkyl;
R
6
is H, alkyl, hydroxyalkyl or —CH
2
F;
R
7
, R
8
and R
9
are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF
3
; and
Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed.
Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
具有结构式I或其药用可接受盐的化合物,其中R是R1,R2,R3,R4和R5为H,烷基或烷氧基烷基;R6为H,烷基,羟基烷基或—CH2F;R7,R8和R9为H,烷基,烷氧基,烷硫基,烷氧基烷基,卤素或—CF3;以及Z是可选择地取代的芳基,杂环芳基或杂环芳基烷基。还公开了化合物I的应用于治疗中枢神经系统疾病,特别是帕金森病,单独或与其他治疗帕金森病的药剂联合使用,以及包含它们的药物组合物。