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    신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물
    2.
    发明申请
    신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물 审中-公开
    新型吡咯烷衍生物和药物组合物，包括作为活性成分的组合物

    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

    Applicant: 한국보건산업진흥원 ,  한미약품 주식회사 ,  박철현 ,  김원정 ,  정영희 ,  김남두 ,  장영길 ,  김맹섭

    Inventor： 박철현 ,  김원정 ,  정영희 ,  김남두 ,  장영길 ,  김맹섭

    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。

    신규 페닐 옥사디아졸 유도체 및 이를 포함하는 약학 조성물
    5.
    发明公开
    신규 페닐 옥사디아졸 유도체 및 이를 포함하는 약학 조성물 无效
    新型苯亚胺衍生物和包含其的药物组合物

    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

    Inventor： 박철현 ,  김원정 ,  정영희 ,  김남두 ,  장영길

    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。

    신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물
    8.
    发明公开
    신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물 无效
    新型吡嗪衍生物和包含其的药物组合物

    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

    Inventor： 박철현 ,  김원정 ,  정영희 ,  김남두 ,  장영길 ,  김맹섭

    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。

    Ｇ 단백질-커플링된 수용체의 조절을 위한 신규한 비사이클릭 화합물
    9.
    发明公开
    Ｇ 단백질-커플링된 수용체의 조절을 위한 신규한 비사이클릭 화합물 无效
    用于调节G蛋白偶联受体的新型双相化合物

    公开(公告)号：KR1020120079015A

    公开(公告)日：2012-07-11

    申请号：KR1020110146537

    申请日：2011-12-29

    Applicant: 한미약품 주식회사

    Inventor： 손정범 ,  김남두 ,  장영길 ,  김희철 ,  김지숙 ,  정영희

    IPC: C07D413/14 ,  C07D495/04 ,  A61K31/519 ,  A61P3/00

    CPC classification number: C07D495/04 ,  C07D487/04

    Abstract: PURPOSE: A novel bicyclic compound for controlling G protein-coupled receptors is provided to treat or prevent diseases associated with the receptor control. CONSTITUTION: A bicyclic compound is denoted by chemical formula 1. A pharmaceutical composition for preventing or treating diseases caused by G protein-coupled receptor control contains the compound of chemical formula 1 as an active ingredient. The G protein-coupled receptor is a GPR119G protein-coupled receptor. The diseases include diabetes, hyperglycemia, injured glucose resistance, insulin resistance, hyperinsulinemia, retinopathy, neuropathy, nephropathy, delayed wound healing, and atherosclerosis.

    Abstract translation: 目的：提供一种用于控制G蛋白偶联受体的新型双环化合物，用于治疗或预防与受体控制相关的疾病。 构成：化学式1表示双环化合物。用于预防或治疗由G蛋白偶联受体控制引起的疾病的药物组合物含有化学式1的化合物作为活性成分。 G蛋白偶联受体是GPR119G蛋白偶联受体。 疾病包括糖尿病，高血糖症，葡萄糖耐量损失，胰岛素抵抗，高胰岛素血症，视网膜病变，神经病变，肾病，延迟伤口愈合和动脉粥样硬化。

    비시클릭 헤테로아릴 유도체 및 이를 포함하는 약학 조성물
    10.
    发明公开
    비시클릭 헤테로아릴 유도체 및 이를 포함하는 약학 조성물 审中-实审
    双相异构体衍生物和药物组合物

    公开(公告)号：KR1020130117678A

    公开(公告)日：2013-10-28

    申请号：KR1020130040860

    申请日：2013-04-15

    Applicant: 한미약품 주식회사

    Inventor： 정승현 ,  김지숙 ,  홍동진 ,  정영희 ,  장욱

    IPC: C07D495/04 ,  A61K31/519 ,  A61P3/00 ,  A61P9/00

    CPC classification number: C07D495/04 ,  C07D519/00

    Abstract: PURPOSE: A pharmaceutical composition containing bicyclic heteroaryl derivatives is provided to selectively and effectively suppress the activation of diacylglycerol O-acyltransferase type 1 (DGAT1), thereby being used as an effective therapeutic agent without side effects. CONSTITUTION: A compound is selected from a bicyclic heteroaryl derivative of chemical formula 1 and a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof. A pharmaceutical composition for suppressing the activation of DGAT1 contains the compound as an active ingredient. The pharmaceutical composition is used for preventing or treating diseases mediated by the activation of DGAT1.

    Abstract translation: 目的：提供含有双环杂芳基衍生物的药物组合物，以有选择地和有效地抑制二酰基甘油O-酰基转移酶1型（DGAT1）的活化，从而用作有效治疗剂，无副作用。 构成：化合物选自化学式1的双环杂芳基衍生物及其药学上可接受的盐，异构体，水合物和溶剂化物。 用于抑制DGAT1活化的药物组合物含有作为活性成分的化合物。 药物组合物用于预防或治疗由激活DGAT1介导的疾病。

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