1-substituted-1-aminomethyl-cycloalkane derivatives (= gabapentin analogues), their preparation and their use in the treatment of neurological disorders
申请人:Warner-Lambert Company LLC
公开号:EP1475371A1
公开(公告)日:2004-11-10
Novel amines of formulas 1, 1C, 1F, 1G and 1H
or a pharmaceutical acceptable salt thereof wherein
n is an integer of from 0 to 2;
m is an integer of from 0 to 3;
R is sulfonamide,
amide,
heterocycle,
sulfonic acid, or
hydroxamic acid;
A' is a bridged ring selected from
wherein
is the point of attachment;
Z1 to Z4 are each independently selected from hydrogen and methyl;
o is an integer of from 1 to 4; and
p is an integer of from 0 to 2.
In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.
式 1、1C、1F、1G 和 1H 的新型胺
或其可接受的药用盐 其中
n 是 0 至 2 的整数
m 是 0 至 3 的整数;
R 是磺酰胺、
酰胺
杂环
磺酸或
羟肟酸;
A' 是桥接环,选自
其中
是连接点;
Z1 至 Z4 各自独立地选自氢和甲基;
o 是 1 至 4 的整数;以及
p 是 0 至 2 的整数。
在上述式(1)中,当 m 为 2 和 n 为 1 时,R 不能是磺酸,这些物质已被公开,可作为治疗癫痫、晕厥发作、运动功能减退、颅脑疾病、神经退行性疾病、抑郁症、焦虑症、恐慌症、疼痛、神经病理学疾病、炎症性疾病和胃肠道疾病,特别是肠易激综合征的药物。