公开(公告)号：KR1020100001288A

公开(公告)日：2010-01-06

申请号：KR1020080061148

申请日：2008-06-26

Applicant: 한국과학기술연구원

Inventor： 최경일 ,  남길수 ,  김혜란 ,  임혜원 ,  서선희 ,  백이연 ,  김윤지 ,  신희섭 ,  김동진 ,  배애님 ,  정혜진 ,  조용서 ,  추현아 ,  노은주 ,  강순방 ,  신계정 ,  한호규 ,  신동윤 ,  정찬성 ,  남기달 ,  강용구 ,  이재균 ,  박웅서 ,  김영수 ,  김은경 ,  김기선 ,  정혜선 ,  금교창 ,  이철주 ,  최기현

IPC: C07D233/61

CPC classification number: C07D233/60 ,  C07D209/48 ,  C07D233/54 ,  C07D233/61 ,  C07D403/06

Abstract: PURPOSE: A novel imidazolylalkylcarbonyl derivative which is effective as calcium ion channel regulator is provided to effectively block T-type calcium ion channel, prevent and treat brain diseases, heart diseases and pain. CONSTITUTION: An imidazolylalkylcarbonyl derivative is denoted by chemical formula 1. The imidazolylalkylcarbonyl derivative of chemical formula 1 is prepared by performing amide bond of piperazine derivative of chemical formula 3 with imidazolylalkylcarboxylic acid of chemical formula 2. The amide bond is performed using binder selected from phosphonium system, ammonium system, carbodiimide system, imidazolinium, and organic phosphine system. A method for preparing the imidazolylalkylcarboxylic acid of chemical formula 2 comprises: a step of performing hetero-michael addition reaction of ethy alkenoate with imidazole compound under the presence of KF/Al2O3 catalyst to produce ethoxycarbonylalkylimidazole compound of chemical formula 2a; and a step of hydrolyzing the ethoxycarbonylalkylimidazole compound of chemical formula 2a to prepare imidazolylalkylcarboxylic acid of chemical formula 2.

Abstract translation: 目的：提供一种有效阻断T型钙离子通道，预防和治疗脑疾病，心脏病和疼痛的新型咪唑烷基羰基衍生物，作为钙离子通道调节剂有效。 构成：化学式1表示咪唑烷基羰基衍生物。化学式1的咪唑烷基羰基衍生物通过化学式3的哌嗪衍生物与化学式2的咪唑基烷基羧酸的酰胺键进行制备。酰胺键使用选自鏻 系统，铵系统，碳二亚胺系统，咪唑啉鎓和有机膦系统。 制备化学式2的咪唑基烷基羧酸的方法包括：在KF / Al 2 O 3催化剂存在下，进行异丁烯酸乙酯与咪唑化合物的异迈克尔加成反应，生成化学式2a的乙氧基羰基烷基咪唑化合物的步骤; 以及水解化学式2a的乙氧基羰基烷基咪唑化合物以制备化学式2的咪唑基烷基羧酸的步骤。

公开(公告)号：KR100917037B1

公开(公告)日：2009-09-10

申请号：KR1020070111220

申请日：2007-11-01

Applicant: 한국과학기술연구원

Inventor： 최경일 ,  남길수 ,  황현숙 ,  임혜원 ,  서선희 ,  신희섭 ,  김동진 ,  한호규 ,  조용서 ,  배애님 ,  신계정 ,  강순방 ,  신동윤 ,  추현아 ,  노은주

IPC: C07D401/12 ,  C07D401/14

Abstract: 본 발명은 신규한 피라졸릴카르복스아미도알킬피페라진 유도체와 이의 제조방법 및 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다.
피라졸릴카르복스아미도알킬피페라진 유도체, 칼슘이온 채널 억제제, 뉴런, 틸분극화, 급성통증, 만성통증, 신경병증성 통증, 항암제, 고혈압치료제

公开(公告)号：KR1020090087732A

公开(公告)日：2009-08-18

申请号：KR1020080013153

申请日：2008-02-13

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  김유승 ,  이재균 ,  배애님 ,  추현아 ,  박지연

IPC: C07D311/26 ,  C07D311/22 ,  C07D311/28

Abstract: A method for producing a 1-(2-hydroxyphenyl)buta-2-en-1-one or cromene-4-one derivative is provided to simply synthesize and use as an intermediate of novel medicine. A 1-(2-hydroxyphenyl)buta-2-en-1-one derivative of the chemical formula 1 or cromene-4-one derivative of the chemical formula 2 is produced by reacting derivative of the chemical formula 3 and aldehyde derivative of the chemical formula 4 under the presence of lewis acid catalyst. In the chemical formulas, R1 is hydrogen atom, C1-C10 alkyl group, C5-C15 aryl group or C1-C10 alkyl silyl group, R2 is hydrogen atom, C1-C10 alkyl group or C5-C15 aryl group.

Abstract translation: 提供1-（2-羟基苯基）丁-2-烯-1-酮或色烯-4-酮衍生物的制备方法，简单地合成并用作新药的中间体。 化学式1的1-（2-羟基苯基）丁-2-烯-1-酮衍生物或化学式2的色烯-4-酮衍生物通过使化学式3的衍生物与 化学式4在路易威酸催化剂存在下。 在化学式中，R 1是氢原子，C 1 -C 10烷基，C 5 -C 15芳基或C 1 -C 10烷基甲硅烷基，R 2是氢原子，C 1 -C 10烷基或C 5 -C 15芳基。

公开(公告)号：KR100843352B1

公开(公告)日：2008-07-03

申请号：KR1020070009627

申请日：2007-01-30

Applicant: 한국과학기술연구원 ,  주식회사 디비하이텍

Inventor： 배애님 ,  조용서 ,  추현아 ,  차주환 ,  김지혜 ,  고훈영 ,  박우규 ,  공재양 ,  채명윤 ,  조인선 ,  황봉운 ,  이동하

IPC: C07D401/12 ,  A61K31/502

CPC classification number: C07D237/32

Abstract: A 1,2-dihydro-1-oxophthalazinyl piperazine derivative is provided to show selective antagonistic activity on serotonin 5-HT2a or 5-HT2c receptor, thereby being used for a pharmaceutical composition for treating and preventing central nervous system diseases. A 1,2-dihydro-1-oxophthalazinyl piperazine derivative is represented by a formula(1) and is prepared by reacting an amine compound represented by a formula(2) with a carboxylic acid compound represented by a formula(3). In the formulae, R1 is H, halogen, C1-10 alkyl, C1-10 alkoxy, phenyl, pyridyl or pyrimidyl; R2 is aryl selected from the group consisting of phenyl, pyridyl and pyrimidyl which may be substituted or unsubstituted by a substituent selected from the group consisting of halogen, nitro, C1-10 alkyl, C1-10 haloalkyl, C1-10 alkoxy, C1-10 haloalkoxy, and C1-6 acyl; and n is an integer from 0 to 5. A pharmaceutical composition for treating and preventing diseases such as anxiety, depression, stroke, obsessive neurosis, psychosis, schizophrenia, suicidal tendency, sleep disorders, appetite disorders, withdrawal symptoms caused by drug abuse, and migraine comprises the 1,2-dihydro-1-oxophthalazinyl piperazine derivative represented by the formula(1) or a pharmaceutically acceptable salt thereof.

Abstract translation: 提供1,2-二氢-1-氧酞嗪哌嗪衍生物以显示对5-羟色胺5-HT2a或5-HT2c受体的选择性拮抗活性，从而用于治疗和预防中枢神经系统疾病的药物组合物。 1,2-二氢-1-氧代吖嗪基哌嗪衍生物由式（1）表示，通过使由式（2）表示的胺化合物与由式（3）表示的羧酸化合物反应制备。 式中，R 1为H，卤素，C 1-10烷基，C 1-10烷氧基，苯基，吡啶基或嘧啶基; R 2是选自苯基，吡啶基和嘧啶基的芳基，其可以被选自卤素，硝基，C 1-10烷基，C 1-10卤代烷基，C 1-10烷氧基，C 1-10烷氧基， 10个卤代烷氧基和C1-6酰基; n为0〜5的整数。用于治疗和预防焦虑，抑郁，中风，强迫神经症，精神病，精神分裂症，自杀倾向，睡眠障碍，食欲障碍，药物滥用引起的戒断症状的药物组合物，以及 偏头痛包含由式（1）表示的1,2-二氢-1-氧代嗪嗪哌嗪衍生物或其药学上可接受的盐。