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公开(公告)号：KR1020100123459A
公开(公告)日：2010-11-24
申请号：KR1020090042691
申请日：2009-05-15
Applicant: 한국화학연구원
IPC: C07D209/46 , C07D209/44 , A61K31/4035 , A61P19/10
Abstract: PURPOSE: An isoindolinone derivative and pharmaceutical composition containing the same are provided to enhance expression of alkaline phosphatase. CONSTITUTION: An insoindolinone derivative is denoted by chemical formula 1. A method for preparing the isoindolinone derivative comprises a step of amide-coupling phenylene diamine with a compound of chemical formula 8 to obtain an isoindolinone of chemical formula 2. In case of that one or more substituent R1-R4 in chemical formula 8 are halogen, the method further comprises a step of Suzuki-coupling boronic acid compound of chemical formula 17(RB(OH)_2) under the presence of palladium catalyst. A pharmaceutical composition for preventing or treating bone diseases contains the isoindolinone derivative of chemical formula 1 or pharmaceutically acceptable salt as an active ingredient.
Abstract translation: 目的：提供异吲哚啉酮衍生物和含有它们的药物组合物，以增强碱性磷酸酶的表达。 构成：异吲哚啉酮衍生物由化学式1表示。制备异吲哚啉酮衍生物的方法包括将苯二胺与化学式8的化合物酰胺偶联以获得化学式2的异吲哚满酮的步骤。如果是那种或 化学式8中更多的取代基R 1 -R 4是卤素，该方法还包括在钯催化剂存在下的化学式17（RB（OH）2）的Suzuki-偶联硼酸化合物的步骤。 用于预防或治疗骨疾病的药物组合物含有化学式1的异吲哚啉酮衍生物或其药学上可接受的盐作为活性成分。
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公开(公告)号：KR101142053B1
公开(公告)日：2012-05-03
申请号：KR1020090042691
申请日：2009-05-15
Applicant: 한국화학연구원
IPC: C07D209/46 , C07D209/44 , A61K31/4035 , A61P19/10
Abstract: 본 발명은 하기 화학식 1의 이소인돌리논 유도체, 이의 제조 방법 및 이를 유효성분으로 포함하는 약학 조성물에 관한 것으로, 본 발명에 따른 이소인돌리논 유도체는 런스 영역 전사 인자의 전사 활성 및 알칼라인 포스파타아제의 발현을 증가시켜 골 생성을 촉진시키는 동시에 골 소실을 억제하는 효과를 나타내어 골다공증, 골 성장 장애, 골절, 치주 질환, 파제트병, 골전이암, 또는 류마티스 관절염 등의 골 질환의 예방 및 치료제로서 유용하게 사용될 수 있다:
상기 식에서, A, R
1 내지 R
4 , 및 Z는 명세서 중에 정의한 바와 같다.
이소인돌리논, 제조방법, 약학 조성물, 골 질환, Runx2, 골생성-
公开(公告)号：KR1020100123379A
公开(公告)日：2010-11-24
申请号：KR1020090042585
申请日：2009-05-15
Applicant: 한국화학연구원
IPC: C07C237/40 , C07C231/10 , A61K31/167 , A61P19/08
Abstract: PURPOSE: A benzamide derivative, a manufacturing method thereof, and a prevention and curing pharmaceutical composition containing thereof are provided to prevent the loss of bones, and to prevent the bone diseases including osteoporosis and periodontal disease. CONSTITUTION: A manufacturing method of a benzamide derivative comprises the following steps: reacting a compound marked with chemical formula 2, with a compound marked with chemical formula 3, to obtain a compound marked with chemical formula 4; hydrolyzing the compound marked with the chemical formula 4, to obtain a compound marked with chemical formula 5; and couple-reacting the compound marked with the chemical formula 5, to obtain the benzamide derivative marked with chemical formula 1.
Abstract translation: 目的：提供苯甲酰胺衍生物及其制造方法以及含有它们的预防和治疗药物组合物，以防止骨骼的损失，并防止包括骨质疏松症和牙周病在内的骨疾病。 构成：苯甲酰胺衍生物的制造方法包括以下步骤：使化学式2标记的化合物与化学式3所示的化合物反应，得到化学式4的化合物; 水解化学式4标记的化合物，得到化学式5标记的化合物; 并与化学式5标记的化合物进行偶联反应，得到化学式1所示的苯甲酰胺衍生物。
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