公开(公告)号：KR100758317B1

公开(公告)日：2007-09-13

申请号：KR1020060039225

申请日：2006-05-01

Applicant: 한국과학기술연구원

Inventor： 금교창 ,  김유승 ,  강순방 ,  임혜원 ,  장민석 ,  구일회

IPC: A61K31/5375 ,  A61P9/04

CPC classification number: A61K31/5375

Abstract: A composition for blocking T-type calcium channel comprising morpholin-2-one derivatives is provided to block the T-type calcium channel in the same level as the conventional T-type calcium channel blocker, mibefradil, without side effects. A composition for blocking T-type calcium channel comprises morpholin-2-one derivatives represented by the formula(1), or pharmaceutically acceptable salts thereof, wherein R^1 and R^2 are each independently hydrogen, C1-C6 alkyl, C1-C6 cycloalkyl, or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy; and R^3 and R^4 are each independently hydrogen, C1-C6 alkyl, C1-C6 thioalkyl, amino or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy. The composition prevents or treats diseases caused by overexpression of T-type calcium channel including angina pectoris, hypertension, myocardiac infarction, pain and epilepsy.

Abstract translation: 提供一种用于阻断包含吗啉-2-酮衍生物的T型钙通道的组合物，以阻断与常规T型钙通道阻滞剂米非司酮相同水平的T型钙通道，无副作用。 用于阻断T型钙通道的组合物包括由式（1）表示的吗啉-2-酮衍生物或其药学上可接受的盐，其中R 1和R 2各自独立地为氢，C 1 -C 6烷基， C 6环烷基或任选被卤素，硝基，羟基或C 1 -C 6烷氧基取代的苯基; R 3和R 4各自独立地为氢，C 1 -C 6烷基，C 1 -C 6硫代烷基，任选被卤素，硝基，羟基或C 1 -C 6烷氧基取代的氨基或苯基。 该组合物预防或治疗由过度表达T型钙通道引起的疾病，包括心绞痛，高血压，心肌梗塞，疼痛和癫痫。