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公开(公告)号：WO2013015535A2
公开(公告)日：2013-01-31
申请号：PCT/KR2012/005193
申请日：2012-06-29
IPC: C07D495/04 , C07D487/04 , A61K31/519 , A61P3/10
CPC classification number: C07D495/04 , C07D487/04
Abstract: 본 발명은 디아실글리세롤 0-아실전이효소 1형의 활성을 억제하는 하기 화학식 1의 화합물, 및 이의 약학적으로 허용 가능한 염으로 이루어진 군으로부터 선택된 화합물 및 이를 유효성분으로 함유하는 약학 조성물에 관한 것으로, 본 발명의 화합물은 DGAT1의 활성에 의해 유발되는 비만, 제2형 당뇨병, 이상지질혈증, 대사증후군 등의 질환에 대한 부작용 없이 효과적인 치료제로서 활용될 수 있다. 상기 [화학식 1]에서, A, B, X 및 R 5~7 은 본원 명세서에서 정의한 바와 같다.
Abstract translation: 本发明涉及一种选自由化学式1表示的化合物的化合物，其用于抑制1型二酰基甘油O-酰基转移酶的活性及其药学上可接受的盐，以及含有作为活性成分的药物组合物。 本发明的化合物可用作治疗由DGAT1的活性引起的肥胖，II型糖尿病，血脂异常，代谢综合征等疾病，无副作用的有效治疗剂。 在化学式1中，A，B，X和R5-7与本说明书中定义的相同。
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公开(公告)号：KR1020130074524A
公开(公告)日：2013-07-04
申请号：KR1020110142617
申请日：2011-12-26
Applicant: 한미약품 주식회사
IPC: C07D271/10 , C07D271/12 , A61K31/5395 , A61P3/00
Abstract: PURPOSE: A novel phenyl oxadiazole derivative is provided to be used as an effective therapeutic agent for treating diseases, such as obesity and type 2 diabetes, caused by DGAT1 (diacylglycerol O-acyltransferase type 1) activation. CONSTITUTION: A pharmaceutical composition for suppressing DGAT1 activation contains a compound of chemical formula 1, or a pharmaceutically acceptable salt, an isomer, a hydrate, or a solvate thereof. The pharmaceutical composition is used for preventing or treating diseases or state mediated by DGAT1 activation. The disease or state is selected from obesity, hyperlipidemia, hypertriglyceridemia, lipid metabolism disorder, insulin resistance syndrome, impaired glucose tolerance, diabetes, diabetes complication, cataract, gestational diabetes, non-alcoholic fatty liver, polycystic ovary syndrome, arteriosclerosis, diabetic atherosclerosis, ischemic heart disease, hyperphagia, hypertension, cerebrovascular diseases, coronary artery disease, fatty liver, abnormal breathing, back pain, gonarthrosis, gout, and cholelithiasis.
Abstract translation: 目的：提供一种新的苯基恶二唑衍生物，用作治疗由DGAT1（二酰基甘油O-酰基转移酶1型）激活引起的疾病如肥胖和2型糖尿病的有效治疗剂。 构成：用于抑制DGAT1活化的药物组合物含有化学式1的化合物或其药学上可接受的盐，异构体，水合物或溶剂合物。 该药物组合物用于预防或治疗由DGAT1激活介导的疾病或状态。 该疾病或状态选自肥胖症，高脂血症，高甘油三酯血症，脂质代谢障碍，胰岛素抵抗综合征，葡萄糖耐量降低，糖尿病，糖尿病并发症，白内障，妊娠糖尿病，非酒精性脂肪肝，多囊卵巢综合征，动脉硬化，糖尿病动脉粥样硬化， 缺血性心脏病，食欲过高，高血压，脑血管疾病，冠状动脉疾病，脂肪肝，呼吸异常，背痛，关节病，痛风和胆石病。
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公开(公告)号：KR1020130013199A
公开(公告)日：2013-02-06
申请号：KR1020110074706
申请日：2011-07-27
Applicant: 한미약품 주식회사
IPC: C07D495/04 , C07D487/04 , A61K31/519 , A61P3/00
CPC classification number: C07D495/04 , C07D487/04
Abstract: PURPOSE: A compound which suppresses the activity of diacylglycerol O-acyltransferase type 1(DGAT1) is provided to be used as a therapeutic agent for treating obesity and type 2 diabetes without side effects. CONSTITUTION: A compound which suppresses the activity of diacylglycerol O-acyltransferase type 1(DGAT1) is denoted by chemical formula 1. In chemical formula 1, X is independently S or NR, wherein R is H or C1-4 alkyl. A pharmaceutical composition for suppressing DGAT1 activity contains the compound of chemical formula 1 as an active ingredient. The pharmaceutical composition is used for preventing and treating diseases mediated by DGAT1 activity. A method for preparing the compound of chemical formula 1 comprises: a step of performing Suzuki coupling reaction of 7-bromo-4-chlorothieno[3,2-d]pyrimidine or N-substituted 7-bromo-4-chloro-pyrrolo[3,2-d]pyrimidine with tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenylcarbamate for substitution reaction; a step of performing Suzuki coupling reaction again and preparing a compound of chemical formula 2; and a step of reacting the compound of chemical formula 2 with isocyanate or thioisocyanate compound.
Abstract translation: 目的：抑制二酰基甘油O-酰基转移酶1型（DGAT1）活性的化合物用作治疗肥胖症和2型糖尿病而无副作用的治疗剂。 构成：抑制二酰基甘油O-酰基转移酶1（DGAT1）的活性的化合物由化学式1表示。在化学式1中，X独立地为S或NR，其中R为H或C 1-4烷基。 用于抑制DGAT1活性的药物组合物含有化学式1化合物作为活性成分。 该药物组合物用于预防和治疗由DGAT1活性介导的疾病。 制备化学式1化合物的方法包括：进行7-溴-4-氯噻吩并[3,2-d]嘧啶或N-取代的7-溴-4-氯 - 吡咯并[3,3-d]嘧啶的Suzuki偶联反应的步骤 ，2-d]嘧啶与4-（4,4,5,5-四甲基-1,3,2-二氧杂环戊硼烷-2-基）苯基氨基甲酸叔丁酯进行取代反应; 再次进行Suzuki偶联反应并制备化学式2的化合物的步骤; 和使化学式2的化合物与异氰酸酯或硫代异氰酸酯化合物反应的步骤。
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