公开(公告)号：KR1020120034829A

公开(公告)日：2012-04-13

申请号：KR1020100084156

申请日：2010-08-30

Applicant: 한국화학연구원

Inventor： 이규양 ,  임채조 ,  김낙정 ,  이병호 ,  이상달 ,  서무영 ,  왕수미

IPC: C07D401/06 ,  A61K31/501 ,  A61P3/00

Abstract: PURPOSE: A phthalazinone derivative containing an aryl piperidine group and a pharmaceutical composition containing the same are provided to prevent or treat MCH-associated diseases. CONSTITUTION: A phthalazinone derivative containing an aryl piperidine group is denoted by chemical formula 1. A method for preparing the derivative comprises a step of alkylating a compound of chemical formula 2 with a piperidine compound of chemical formula 3 under the presence of organic solvent and base. The organic solvent ether solvent, low alcohol of C1-C4, DMF(dimethyl formamide), DMSO(dimethyl sulfoxide, acetonitrile or water. The base is an organic base including pyridine, triethyl amine, N,N-diisopropyl ethyl amine(DIPEA), 1,8-diazabicylco[5.4.0]-undecene(DBU); or an inorganic base including sodium hydroxide, sodium carbonate, potassium carbonate, cesium carbonate, and sodium hydride.

Abstract translation: 目的：提供含有芳基哌啶基的酞嗪酮衍生物和含有该芳基哌啶基团的药物组合物以预防或治疗MCH相关疾病。 构成：含有芳基哌啶基的酞嗪酮衍生物由化学式1表示。制备该衍生物的方法包括在有机溶剂和碱的存在下用化学式3的哌啶化合物烷基化化学式2的化合物的步骤 。 有机溶剂醚溶剂，C1-C4的低级醇，DMF（二甲基甲酰胺），DMSO（二甲基亚砜，乙腈或水），碱是包括吡啶，三乙胺，N，N-二异丙基乙胺（DIPEA） ，1,8-二氮杂双环[5.4.0] - 十一碳烯（DBU）;或包含氢氧化钠，碳酸钠，碳酸钾，碳酸铯和氢化钠的无机碱。

公开(公告)号：KR101207420B1

公开(公告)日：2012-12-05

申请号：KR1020100084156

申请日：2010-08-30

Applicant: 한국화학연구원

Inventor： 이규양 ,  임채조 ,  김낙정 ,  이병호 ,  이상달 ,  서무영 ,  왕수미

IPC: C07D401/06 ,  A61K31/501 ,  A61P3/00

Abstract: 아릴피페리딘기를함유하는프탈라지논유도체, 이의제조방법및 이를유효성분으로포함하는약학적조성물을제공한다. 본발명에따른아릴피페리딘기를함유하는프탈라지논유도체는 MCH(멜라닌농축호르몬) 수용체에대한길항제로작용함으로써 MCH가 MCH 수용체에결합함으로써유발되는비만, 당뇨병, 대사장애, 불안증및 우울증과같은 MCH 관련질환을예방또는치료하는데유용하게사용할수 있다.