公开(公告)号：KR1020050108567A

公开(公告)日：2005-11-17

申请号：KR1020040033474

申请日：2004-05-12

Applicant: 한국화학연구원

Inventor： 김봉진 ,  김재학 ,  김광호 ,  정희정 ,  전미애 ,  공재양 ,  조희영

IPC: C07D477/20

CPC classification number: Y02P20/55 ,  C07D477/18 ,  C07D477/20

Abstract: 본 발명은 그람양성균 및 그람음성균에 대해 광범위하게 항균효과를 나타내며, 메티실린 내성 스타필로코쿠스 아우레우스(methicillin resistant staphylococcus aureus, MRSA)를 비롯한 내성균에도 우수한 항균효과를 갖는 하기 화학식 1의 카바페넴 유도체, 이의 제조 방법 및 이를 함유하는 항생제 조성물에 관한 것이다.

상기 식에서, R
1 , R
2 및 R
3 는 각각 독립적으로, 수소, 탄소수 1-3개의 알킬기를 의미하며, M은 수소 또는 약리학적으로 허용가능한 염을 형성하는 짝이온을 나타낸다.

公开(公告)号：KR102141035B1

公开(公告)日：2020-08-06

申请号：KR1020190029309

申请日：2019-03-14

Applicant: 부산대학교 산학협력단 ,  한국화학연구원

Inventor： 정연진 ,  정성근 ,  조희영 ,  김현영

IPC: C07D213/72 ,  A61K31/44 ,  A61P1/00 ,  A61P29/00 ,  A23L29/00 ,  A23L33/10

公开(公告)号：KR101845931B1

公开(公告)日：2018-04-05

申请号：KR1020160067210

申请日：2016-05-31

Applicant: 한국화학연구원

Inventor： 이계형 ,  임희종 ,  조희영 ,  박우규 ,  김성환 ,  최정환

IPC: C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/506 ,  A23L1/30

CPC classification number: C07D487/04 ,  A61K9/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D471/04 ,  C07D519/00

Abstract: 본발명은헤테로아릴유도체또는이의약학적으로허용가능한염, 이의제조방법및 이를유효성분으로포함하는 PI3 키나아제관련질환의예방또는치료용약학적조성물에관한것이다. 본발명에따른헤테로아릴유도체는 PI3 키나아제에대하여선택적으로억제하는효과가우수하므로혈액암, 난소암, 자궁경부암, 유방암, 대장암, 간암, 위암, 췌장암, 결장암, 복막전이암, 피부암, 방광암, 전립선암, 폐암, 골육종, 섬유성종양, 뇌종양등과같은암, 류머티스성관절염, 전신홍반성루푸스, 다발성경화증, 제1형당뇨병, 갑상선기능항진증, 근무력증, 크론병, 강직성척추염, 건선, 자가면역성악성빈혈, 쇼그렌증후군등과같은자가면역질환, 만성폐쇄성폐질환(COPD), 비염, 천식, 만성기관지염, 만성폐 염증성질환, 규폐증, 폐형사르코이드증, 흉막염, 폐포염, 혈관염, 기종, 폐렴, 기관지확장증등과같은호흡기질환등의 PI3 키나아제관련질환을예방또는치료하는데유용하게사용할수 있다.

Abstract translation: 本发明涉及杂芳基衍生物或一个uiyakhak上可接受的盐，它们的制备和药物组合物包含其作为活性成分的PI3激酶相关的疾病的预防或治疗物质。 由于本发明的杂芳基衍生物是具有优异的效果，以选择性地抑制相对于PI3激酶血癌，卵巢癌，子宫颈癌，乳腺癌，结肠癌，肝癌，胃癌，胰腺癌，结肠直肠癌，腹膜转移，皮肤癌，膀胱癌， 癌症如前列腺癌，肺癌，骨肉瘤，纤维瘤，脑肿瘤，类风湿性关节炎，jeonsinhong红斑狼疮，多发性硬化症，1型糖尿病，甲状腺功能亢进症，重症肌无力，克罗恩病，强直性脊柱炎，牛皮癣，自身免疫性恶性贫血 自身免疫性疾病如斯耶格伦氏综合征，慢性阻塞性肺疾病（COPD），鼻炎，哮喘，慢性支气管炎，慢性肺部炎性疾病，矽肺，结节病pyehyeong，胸膜炎，肺泡炎，脉管炎，肺气肿，肺炎，支气管扩张，等等，和 一个PI3激酶相关的疾病，如呼吸道疾病可以是预防或治疗是有用的。

公开(公告)号：KR101810209B1

公开(公告)日：2017-12-19

申请号：KR1020160042938

申请日：2016-04-07

Applicant: 한국화학연구원 ,  김진홍

Inventor： 조희영 ,  박우규 ,  임희종 ,  이계형 ,  김현영 ,  정대영 ,  이나라 ,  이현준 ,  김진홍

IPC: A61K31/20 ,  A61K31/201 ,  A61K31/19 ,  A61K36/185 ,  A61K8/36 ,  A61K8/97 ,  A23L1/30 ,  A61Q19/00

Abstract: 본발명은아토피피부질환개선및 치료용조성물에관한것으로, 보다상세하게는히드노카핀산(hydnocarpic acid) 및고를산(gorlic acid)을포함하는아토피피부질환개선및 치료용조성물에관한것으로, 본발명을통해얻은아토피피부질환개선및 치료용조성물은종래의대풍자유추출물을이용한결과와비교하였을때 세포및 동물개체실험에서소량처리를통해서도현저한항아토피및 면역억제효과가있음을발견하였고, 이를통해향우아토피피부질환의완치를위해유용하게활용될수 있을것으로기대된다.

Abstract translation: 本发明涉及一种特应性皮肤病改善，而且用于治疗组合物，更具体地，羟丙基诺卡特应性皮炎改善和含有治疗性组合物中的酸（hydnocarpic酸）和挑酸（gorlic酸），本发明 特应性皮肤疾病，改善和通过获得治疗性组合物，发现当使用常规大丰游离提取物的细胞和动物个体实验少量通过显着的抗过敏性和免疫抑制处理相比，结果在效果，hyangwoo通过该 预计它可用于治疗特应性皮肤病。

公开(公告)号：KR1020160139074A

公开(公告)日：2016-12-07

申请号：KR1020150072687

申请日：2015-05-26

Applicant: 순천향대학교 산학협력단 ,  한국화학연구원

Inventor： 송호연 ,  남궁우 ,  장웅식 ,  이기인 ,  조희영 ,  이병의

IPC: C07D307/92 ,  C07C50/12 ,  A61K31/343

Abstract: 본발명의결핵치료용약학조성물은, 나프토퀴논유도체또는이의약학적으로허용되는염을유효성분으로포함하여, 다재내성결핵균과수퍼결핵을포함하는내성결핵균에대해서도항결핵활성을갖는약학조성물을제공한다.

公开(公告)号：KR101448015B1

公开(公告)日：2014-10-08

申请号：KR1020130041609

申请日：2013-04-16

Applicant: 한국화학연구원

Inventor： 이선경 ,  송종환 ,  조희영 ,  김현영

IPC: C07D413/06 ,  C07D403/06 ,  A61K31/4245 ,  A61P3/06

Abstract: The present invention relates to a novel indole derivative or a pharmaceutically allowable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating dyslipidemia containing the same as an active ingredient. The novel indole derivative according to the present invention combines a niacin GPR109A receptor, activates the receptor, and induces less activation of beta-arrestin signal transduction pathway, thereby minimizing a facial blushing side effect and being used as a composition for preventing, alleviating, or treating dyslipidemia such as hyperlipemia, hypercholesterinemia, hypertriglyceridemia, etc.

Abstract translation: 本发明涉及一种新的吲哚衍生物或其药学上允许的盐，其制备方法和用于预防或治疗含有其的活性成分的血脂异常的药物组合物。 根据本发明的新型吲哚衍生物结合了烟酸GPR109A受体，激活受体，并诱导较少的β-抑制蛋白信号转导途径的活化，从而使脸部脸红的副作用最小化，并用作预防，缓解或 治疗血脂异常，如高脂血症，高胆固醇血症，高甘油三酯血症等

公开(公告)号：KR1020140008645A

公开(公告)日：2014-01-22

申请号：KR1020120075365

申请日：2012-07-11

Applicant: 한국화학연구원 ,  사회복지법인 삼성생명공익재단

Inventor： 조희영 ,  최길돈 ,  박우규 ,  정대영 ,  김현영 ,  이선경 ,  남도현 ,  설호준

IPC: A61K31/52 ,  A61K31/519 ,  A61K31/4164 ,  A61P35/00

CPC classification number: A61K31/52 ,  A61K31/495

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating cancers or Temodal-resistant glioblastoma, containing azathioprine as an active ingredient. The azathioprine according to the present invention effectively suppresses the proliferation of glioblastoma, which is a kind of brain tumor, and exhibits an excellent therapeutic effect even on glioblastoma cancer cells having resistance to Temodal (temozolomide), which is an existing agent for treating glioblastoma. Therefore, the azathioprine according to the present invention can be useful as an active ingredient of a pharmaceutical composition for preventing or treating cancers such as brain tumors (especially, glioblastoma) and Temodal-resistant glioblastoma. [Reference numerals] (AA) Inhibition ratio (%)

Abstract translation: 本发明涉及含有硫唑嘌呤作为有效成分的用于预防或治疗癌症或耐炎性胶质母细胞瘤的药物组合物。 根据本发明的硫唑嘌呤有效地抑制了作为一种脑肿瘤的胶质母细胞瘤的增殖，并且甚至对具有抗肿瘤成分（替莫唑胺）的成胶质细胞瘤癌细胞也是显示出优异的治疗效果，其是用于治疗胶质母细胞瘤的现有药剂。 因此，根据本发明的硫唑嘌呤可以用作用于预防或治疗诸如脑肿瘤（特别是成胶质细胞瘤）和耐甲状腺成胶质细胞瘤的癌症的药物组合物的活性成分。 （附图标记）（AA）抑制率（％）

公开(公告)号：KR1020130122361A

公开(公告)日：2013-11-07

申请号：KR1020120045621

申请日：2012-04-30

Applicant: 한국화학연구원

Inventor： 임희종 ,  이계형 ,  박우규 ,  조희영

IPC: C07D403/12 ,  C07D235/14 ,  A61K31/4178 ,  A61P25/00

Abstract: The present invention relates to 4-(benzimidazole-2-ylamino)pyrrolidine derivatives of chemical formula 1 or pharmaceutically acceptable salts thereof; a pharmaceutical composition containing the same as an active ingredient for preventing and treating neurodegenerative diseases; and an inhibitor composition of the activation of beta-secretase (BACE), containing the same as an active ingredient. The 4-(benzimidazole-2-ylamino)pyrrolidine derivatives according to the present invention suppresses the activation of BACE and generation of beta-amyloid proteins which cause damage to nerve cells, thereby effectively preventing or treating neurodegenerative diseases such as Alzheimer’s disease and Down syndrome.

Abstract translation: 本发明涉及化学式1的4-（苯并咪唑-2-基氨基）吡咯烷衍生物或其药学上可接受的盐; 含有与用于预防和治疗神经变性疾病的活性成分相同的药物组合物; 以及含有与活性成分相同的β-分泌酶（BACE）活化的抑制剂组合物。 根据本发明的4-（苯并咪唑-2-基氨基）吡咯烷衍生物抑制BACE的活化和产生引起神经细胞损伤的β-淀粉样蛋白，从而有效地预防或治疗神经变性疾病如阿尔茨海默氏病和 唐氏综合症。

公开(公告)号：KR1020120050841A

公开(公告)日：2012-05-21

申请号：KR1020100112296

申请日：2010-11-11

Applicant: 한국화학연구원

Inventor： 박우규 ,  공재양 ,  조희영 ,  정대영 ,  최길돈 ,  고훈영 ,  이희윤 ,  정선호 ,  이해황 ,  이정국 ,  서용완

IPC: C07D403/06 ,  A61K31/496 ,  A61P25/00

Abstract: PURPOSE: A pyrazole butyl compound and a pharmaceutical composition containing the same are provided to ensure dopamine D4 receptor affinity and to prevent and treat central nervous system diseases. CONSTITUTION: A pyrazole butyl compound and pharmaceutically acceptable salt thereof are denoted by chemical formula 1. The salt includes inorganic acid salt, organic acid salt, amino acid salt, alkali metal salt, or ammonium salt. A method for preparing the pyrazole butyl compounds comprises: a step of performing reductive amination of pyrazole aldehyde compound of chemical formula 2 with heterocycle compounds of chemical formula 3 under the presence of reducing agent and base. A pharmaceutical composition for treating central nervous system diseases contains 1-(4-chlorophenyl)-4-(4-(1-phenyl-3-propyl-1H-pyrazole-5-yl)butyl)piperazine(compound No. 33) or 1-(4-(1-phenyl-3-propyl-1H-pyrazole-5-yl)butyl)-4-(3-(trifluoromethyl)phenyl)piperazine(compound No. 36).

Abstract translation: 目的：提供吡唑丁基化合物和含有它们的药物组合物以确保多巴胺D4受体亲和力并预防和治疗中枢神经系统疾病。 构成：吡唑基丁基化合物及其药学上可接受的盐由化学式1表示。盐包括无机酸盐，有机酸盐，氨基酸盐，碱金属盐或铵盐。 制备吡唑丁基化合物的方法包括：在还原剂和碱的存在下，用化学式3的杂环化合物进行化学式2的吡唑醛化合物的还原胺化的步骤。 用于治疗中枢神经系统疾病的药物组合物含有1-（4-氯苯基）-4-（4-（1-苯基-3-丙基-1H-吡唑-5-基）丁基）哌嗪（化合物33）或 1-（4-（1-苯基-3-丙基-1H-吡唑-5-基）丁基）-4-（3-（三氟甲基）苯基）哌嗪（化合物36）。

公开(公告)号：KR1020110024940A

公开(公告)日：2011-03-09

申请号：KR1020090083133

申请日：2009-09-03

Applicant: 한국화학연구원 ,  인하대학교 산학협력단

Inventor： 고훈영 ,  김지희 ,  카말키숄포파트로랜지 ,  공재양 ,  박우규 ,  조희영 ,  정대영 ,  최길돈 ,  이희윤

IPC: C07D403/08 ,  C07D403/06 ,  A61K31/415 ,  A61P25/18

Abstract: PURPOSE: A pharmaceutical composition containing a novel 3-(methoxymethyl)pyrazole derivative is provided to ensure dopamine D3 and D4 receptor affinity and to suppress psychotic behavior(cage climbing) in a mouse. CONSTITUTION: A novel 3-(methoxymethyl)pyrazole derivative is denoted by chemical formula 1. The compound of chemical formula 1 is prepared by reductive amination of pyrazole aldehyde derivative of chemical formula 2 with piperazine derivative of chemical formula 3 under the presence of reductant and base. A pharmaceutical composition for treating central nervous system diseases contains the compound of chemical formula 1.

Abstract translation: 目的：提供含有新的3-（甲氧基甲基）吡唑衍生物的药物组合物，以确保多巴胺D3和D4受体的亲和力，并抑制小鼠的精神病性行为（笼养）。 组成：化学式1表示新的3-（甲氧基甲基）吡唑衍生物。化学式1的化合物通过化学式2的吡唑醛衍生物与化学式3的哌嗪衍生物在还原剂的存在下还原胺化而制备， 基础。 用于治疗中枢神经系统疾病的药物组合物含有化学式1的化合物。