Use of aryl-cyclohexylamine derivatives in the manufacture of NMDA receptor blockers
申请人:F. HOFFMANN-LA ROCHE AG
公开号:EP0982026A2
公开(公告)日:2000-03-01
The present invention relates to the use of compounds of the general formula
wherein
Ar1is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by hydroxy, lower alkoxy, nitro, amino or methanesulfonamide;
Ar2is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by lower alkyl or halogen;
Xis C, CH, C(OH) or N;
Yis -CH2-, CH or O
Z-CH2-, -CH(CH3)- or -C(CH3)2-;
R1is hydrogen, lower alkyl or acetyl;
Ais C=O or -(CHR2)n-, wherein R2 is hydrogen, lower alkyl or hydroxy-lower alkyl;
Bis -(CH2)n-, O, -CH(OH)(CH2)n-, -CH(CH2OH)(CH2)n-, -(CH2)n CH(OH)- or -CH(CH2OH)-;
---may be a bond and
nis 0-4
and to pharmaceutically acceptable acid addition salts thereof for the manufacture of medicaments which represent therapeutic indications for NMDA receptor subtype specific blockers.
本发明涉及通式化合物的用途
式中
Ar1 是苯基、萘基或四氢萘基,可选择被羟基、低级烷氧基、硝基、氨基或甲磺酰胺取代;
Ar2 是苯基、萘基或四氢萘基,可选择被低级烷基或卤素取代;
X 是 C、CH、C(OH) 或 N;
Y 是-CH2-、CH 或 O
Z-CH2-、-CH(CH3)- 或 -C(CH3)2-;
R1 是氢、低级烷基或乙酰基;
A 是 C=O 或 -(CHR2)n-,其中 R2 是氢、低级烷基或羟基低级烷基;
双-(CH2)n-、O、-CH(OH)(CH2)n-、-CH(CH2OH)(CH2)n-、-(CH2)n CH(OH)-或-CH(CH2OH)-;
---可为键且
n 为 0-4
及其药学上可接受的酸加成盐,用于制造代表 NMDA 受体亚型特异性阻断剂治疗适应症的药物。