Arylpiperidinol and arylpiperidine derivatives and pharmaceuticals containing the same
申请人:——
公开号:US20030130312A1
公开(公告)日:2003-07-10
A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca
2+
overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I):
1
wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH
2
)
n
— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.
一种药物组合物,特别是一种用于缓解或治疗缺血性疾病引起的症状以及癫痫发作、癫痫和偏头痛引起的症状的药物组合物,以及一种 Ca
2+
过载抑制剂,含有具有式(I)的芳基哌啶醇或芳基哌啶衍生物:
1
其中,R 是 H、任选取代的苯基、任选取代的苯氧基或任选取代的苯甲酰基;A 是连接键、环烷基或任选被低级烷基取代的烯基;B 是任选被 OH 或烷氧取代的烷基或 -NHCO(CH
2
)
n
- 其中 n 是 1 至 5 的整数,E 是连接键、O 或亚甲基,X 是 OH 或 H,但当 E 是 O 或亚甲基时,X 不是 H,Y 和 Z 独立地是 H、卤素、烷氧基或任选被卤素取代的烷基。