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公开(公告)号：WO2010050783A2
公开(公告)日：2010-05-06
申请号：PCT/KR2009/006357
申请日：2009-10-30
IPC: C07D493/10 , C07D493/04 , C07D493/02 , A61K31/35 , A61K31/36 , A61P19/10
CPC classification number: C07D493/10
Abstract: 본 발명은 스파이로키랄 탄소 골격을 갖는 신규한 화합물, 그의 입체이성질체, 그의 거울상이성질체, 생체 내에서 가수분해 가능한 그의 전구체 또는 약제학적으로 허용 가능한 그의 염을 제공한다. 상기 스파이로키랄 탄소 골격을 갖는 신규한 화합물은 조골세포 분화능이 우수하며, 비만세포 분화억제능 및 간에서의 지방산 합성 억제능을 가지므로, 골다공증, 지방간 및 비만치료에 획기적인 역할을 할 것으로 기대된다.
Abstract translation:
本发明提供了新颖的化合物，它们的立体异构体，其对映体，其在体内可水解前体，或具有间谍洛基LAL碳骨架的药物上可接受的盐。 具有间谍洛基LAL碳骨架和成骨细胞多能的新化合物是优异的，因为的肥大细胞分化的抑制能力的脂肪酸合成的抑制能力，和肝，预计是在骨质疏松症，脂肪肝和肥胖症的一个创新的作用。< / p>
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公开(公告)号：KR101427328B1
公开(公告)日：2014-08-06
申请号：KR1020130029279
申请日：2013-03-19
Applicant: 서울대학교산학협력단
CPC classification number: G01N33/582 , G01N27/447 , G01N33/68
Abstract: Provided of the present invention is a method for identifying a target protein of a physiologically active low molecular compound using a probe and a negative probe labeled with fluorescents having different wavelengths. The probe can be conjugated with a target protein binding to the physiologically active low molecular material and also be conjugated with proteins not binding to the physiologically active low molecular material. Therefore, a negative prove labeled with a fluorescent of a wavelength different from a fluorescent conjugated with the probe can be used, or a physiologically active low molecular substance and the probe can be also used.
Abstract translation: 本发明提供了使用探针和用不同波长的荧光标记的阴性探针鉴定生理活性低分子化合物的靶蛋白的方法。 探针可以与结合生理活性低分子材料的靶蛋白缀合，并且与不结合生理活性低分子材料的蛋白质缀合。 因此，可以使用用与探针结合的荧光波长不同的荧光标记的阴性证明，也可以使用生理活性低分子物质和探针。
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Patent Agency Ranking
公开(公告)号：KR1020140114958A
公开(公告)日：2014-09-30
申请号：KR1020130029283
申请日：2013-03-19
Applicant: 서울대학교산학협력단
IPC: C07D311/00 , A61K9/20 , A61P35/00
Abstract: Provided in the present invention are benzopyran derivatives inhibiting formation of microtubule, a pharmaceutically acceptable salt of the same, and a pharmaceutical composition containing the same as active component for treating cancer. A microtubule is in a state of single body and polymer to be controlled according to a need to control cell division, thus blocks movement between single body and polymer of the microtubule to inhibit cell division. The benzopyran derivatives of the present invention inhibit formation of microtubule to be used for treating cancer and other hyperproliferative diseases.
Abstract translation: 本发明提供了抑制微管形成的苯并吡喃衍生物及其药学上可接受的盐，以及含有与治疗癌症的活性成分相同的药物组合物。 微管处于单体和聚合物的状态，根据需要控制细胞分裂，从而阻止单体和微管聚合物之间的运动，以抑制细胞分裂。 本发明的苯并吡喃衍生物抑制用于治疗癌症和其它过度增生性疾病的微管的形成。
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公开(公告)号：KR1020120057716A
公开(公告)日：2012-06-07
申请号：KR1020100081896
申请日：2010-08-24
Applicant: 서울대학교산학협력단
IPC: C07D491/048 , A61K31/35 , A61P3/10 , A61P3/00
Abstract: PURPOSE: A pharmaceutical composition containing a compound which activates AMPK is provided to enhance glucose intake in cells and to prevent and treat type 2 diabetes, hypertension, cardiovascular diseases, and obesity. CONSTITUTION: A pharmaceutical composition for preventing and treating diseases needing AMPK(adenosine monophosphoate-activated protein kinase) activation contains 0.1-50 wt% of a compound of chemical formula I as an active ingredient, or pharmaceutically acceptable salt or solvate thereof. The diseases include type 2 diabetes, metabolic syndrome, hypertension, cardiovascular diseases, and obesity.
Abstract translation: 目的：提供一种含有激活AMPK的化合物的药物组合物，以增强细胞中的葡萄糖摄入量，并预防和治疗2型糖尿病，高血压，心血管疾病和肥胖。 构成：用于预防和治疗需要AMPK（单磷酸腺苷活化蛋白激酶）活化的疾病的药物组合物含有0.1-50重量％的化学式I化合物作为活性成分或其药学上可接受的盐或溶剂化物。 这些疾病包括2型糖尿病，代谢综合征，高血压，心血管疾病和肥胖。
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公开(公告)号：KR101149878B1
公开(公告)日：2012-05-24
申请号：KR1020090104124
申请日：2009-10-30
Applicant: 서울대학교산학협력단
IPC: C07D493/10 , C07D493/02 , A61K31/435 , A61P3/04
CPC classification number: C07D493/10
Abstract: Provided are a novel compound with a spiro chiral carbon backbone, a stereoisomer thereof, an enantiomer thereof, an in vivo hydrolysable precursor thereof, or a pharmaceutically acceptable salt thereof. The novel compound with the spiro chiral carbon backbone has excellent osteoblast differentiation activity, mast cell inhibitoryactivity, and fatty acid synthesis inhibitory activity in the liver. Therefore, the novel compound can be expected to play an innovative role in treatment of osteoporosis, fatty liver, and obesity.
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公开(公告)号：KR101190141B1
公开(公告)日：2012-10-12
申请号：KR1020100081896
申请日：2010-08-24
Applicant: 서울대학교산학협력단
IPC: C07D491/048 , A61K31/35 , A61P3/10 , A61P3/00
Abstract: 본 발명은 AMPK(Adenosine monophosphate-activated protein kinase; AMP-activated protein kinase)를 활성화시키는 화합물을 유효성분으로 함유하는, AMPK의 활성화가 필요한 질환의 예방 및 치료용 약학조성물에 관한 것이다. AMPK는 비만 및 제2형 당뇨병을 포함하는 대사 장애의 치료를 위한 매력적인 표적 분자로서 부각되고 있다. 본 발명자들은 간접적인 AMPK 활성제(activator)로서 특별한 벤조피란 부분구조(privileged benzopyran substructure)를 갖는 신규한 저분자, 특히 앰프키논(ampkinone, AKN)을 발견하였으며, 이는 다양성-지향적 합성(diversity-oriented synthesis)에 의해 구축된 저분자 라이브러리로부터 유래된다. AKN은 다양한 세포주 내에서 AMPK의 간접적 활성화를 통해 AMPK의 인산화(phosphorylation)를 자극(stimulate)하였다. AKN-매개된 AMPK의 활성화는 LKB1의 활성을 필요로 하였으며, 근육세포에서 증가된 글루코스 섭취(uptake)를 야기하였다. 또한, AKN-처리된 DIO(Diet-induced obesity) 마우스는 총 체중 및 전체 지방 질량이 현저하게 감소되었다. 지질 파라미터의 조직학적 검사 및 측정은, DIO 마우스 모델에서의 대사 이상(metabolic abnormality)을 AKN이 효과적으로 개선시켰음을 나타내었다. 따라서, 본 발명의 특별한 벤조피란 부분구조(privileged benzopyran substructure)를 갖는 저분자인 AKN은 AMPK의 간접 자극을 통해 항당뇨 및 항비만 치료용 치료제의 신규 클래스로서의 잠재성을 갖는다.
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公开(公告)号：KR1020100048934A
公开(公告)日：2010-05-11
申请号：KR1020090104124
申请日：2009-10-30
Applicant: 서울대학교산학협력단
IPC: C07D493/10 , C07D493/02 , A61K31/435 , A61P3/04
CPC classification number: C07D493/10
Abstract: PURPOSE: A novel compound having spiro chiral carbon skeleton is provided to suppress mastocyte differentiation and fatty acid synthesis and use in treating osteoporosis, fatty liver, and obesity. CONSTITUTION: A novel compound having spiro chiral carbon skeleton is denoted by chemical formula 1. A method for preparing the compound of chemical formula 1 comprises: a step of cutting and drying Phorbas sp. and extracting with C1-C4; a step of dividing the extracting with water and methylene chloride to remove solvent of organic layer; a step of distributing with mixture solution of normal hexane, methanol, and water; a step of removing solvent of methanol layer; and a step of performing chromatography to obtain fraction.
Abstract translation: 目的：提供一种具有螺状手性碳骨架的新型化合物，用于抑制肥大细胞分化和脂肪酸合成，并用于治疗骨质疏松症，脂肪肝和肥胖症。 构成：具有螺状手性碳骨架的新化合物由化学式1表示。化学式1化合物的制备方法包括：切割并干燥佛波斯 并用C1-C4提取; 用水和二氯甲烷分离提取物以除去有机层的溶剂的步骤; 用正己烷，甲醇和水的混合溶液分配的步骤; 去除甲醇层溶剂的步骤; 以及进行色谱以获得级分的步骤。
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