公开(公告)号：KR100743255B1

公开(公告)日：2007-07-27

申请号：KR1020060040614

申请日：2006-05-04

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  추현아 ,  배애님 ,  차주환 ,  고훈영 ,  김화실 ,  임혜원 ,  서선희

IPC: C07D209/48

Abstract: Novel 1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel are provided to treat brain diseases including epilepsy, hypertension and angina pectoris, heart disease and nerve system pain by inhibiting the T-type calcium channel as a representative low-voltage activated calcium channel. The 1,3-dioxoisoindole derivatives represented by the formula(1) or their pharmaceutically acceptable salts are provided, wherein R1 is phenyl group or benzyl group which is substituted or unsubstituted by halogen atom, C1-C6 alkoxy group, C1-C6 alkyl group, or cyano group; R2 is a hetero ring group selected from piperidinyl group, pyrolidinyl group, morpholinyl group and piperazinyl group which is substituted or unsubstituted by C1-C6 alkyl substituent; and n is 1 or 2, provided that a compound in which R2 is morpholinyl group when R1 is C1-C6 alkyl-substituted phenyl group is excluded.

Abstract translation: 通过抑制T型钙通道作为代表性的低电压来提供具有T型钙通道选择性拮抗作用的新型1,3-二氧代异吲哚衍生物来治疗包括癫痫，高血压和心绞痛，心脏病和神经系统疼痛的脑疾病 激活钙通道。 由式（1）表示的1,3-二氧代异吲哚衍生物或它们的药学上可接受的盐，其中R1是被卤素原子，C1-C6烷氧基，C1-C6烷基取代或未被取代的苯基或苄基 或氰基; R2是选自哌啶基，吡咯烷基，吗啉基和由C1-C6烷基取代基取代或未取代的哌嗪基的杂环基; 并且n是1或2，条件是当R 1是C 1 -C 6烷基取代的苯基时，其中R 2是吗啉基的化合物被排除在外。