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：KR1020150080249A

公开(公告)日：2015-07-09

申请号：KR1020130168603

申请日：2013-12-31

Applicant: 한국화학연구원 ,  가톨릭대학교 산학협력단

Inventor： 조희영 ,  박우규 ,  임희종 ,  이계형 ,  정대영 ,  김현영 ,  김완욱 ,  조철수 ,  박수정 ,  한은진 ,  김중호

IPC: A61K31/4375 ,  A61P19/02 ,  A61P29/00

CPC classification number: A61K31/4375 ,  C07D455/03 ,  C07D491/147 ,  Y10S514/825

Abstract: 본발명은프로토베르베린유도체또는이의약학적으로허용가능한염을유효성분으로함유하는 NFAT5의활성관련질환의예방또는치료용약학적조성물에관한것으로써, 본발명에따른옥소프로토베르베린유도체또는이의약학적으로허용가능한염은 NFAT5 활성을억제하므로, NFAT5 활성관련질환, 특히류마티스관절염또는염증질환등의예방또는치료용약학적조성물로유용하게사용될수 있다.

Abstract translation: 本发明涉及一种药物组合物，其包含作为预防或治疗与NFAT5的活化有关的疾病的活性成分的原青蒿素衍生物或其药学上可接受的盐。 根据本发明，氧八环柏因衍生物或药学上可接受的盐抑制NFAT5的活化，因此可以有效地用作预防或治疗与NFAT5的活化有关的疾病，特别是类风湿性关节炎或炎症性疾病等的药物组合物。

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。

公开(公告)号：KR1020110012090A

公开(公告)日：2011-02-09

申请号：KR1020090069647

申请日：2009-07-29

Applicant: 한국화학연구원 ,  에스케이케미칼주식회사

Inventor： 공영대 ,  조희영 ,  이태호 ,  최길돈 ,  전문국 ,  박우규 ,  공재양 ,  황순희 ,  정대영 ,  이봉용 ,  엄기안 ,  김재선 ,  류근호 ,  류제호 ,  김신애 ,  한혜영 ,  손현주 ,  이현정 ,  김용혁 ,  박성훈

IPC: C07D311/24 ,  C07D311/16 ,  C07D311/12

Abstract: PURPOSE: A 2-methyl-2H-chromen-2-carboxamide compound is provided to ensure selective suppression to 11beta-HSD1 enzyme and prevent and treat glucocorticoid regulatory disease. CONSTITUTION: A 2-methyl-2H-chromen-2-carboxamide compound is denoted by chemical formula 1. A pharmaceutical composition contains the 2-methyl-2H-chromen-2-carboxamide compound. The pharmaceutical composition is used for treating and preventing type 1 and 2 diabetes, injured glucose resistance, hyperlipidemia or hypertension. The 2-methyl-2H-chromen-2-carboxamide compound in which an amide is induced is obtained by condensing R1-substituted 2-methyl-2H-chromen-2-carboxy acid compound of chemical formula 2 with amine compound(NHR^2R^3).

Abstract translation: 目的：提供2-甲基-2H-色烯-2-甲酰胺化合物，以确保对11beta-HSD1酶的选择性抑制，并预防和治疗糖皮质激素调节性疾病。 构成：2-甲基-2H-色烯-2-甲酰胺化合物由化学式1表示。药物组合物含有2-甲基-2H-色烯-2-甲酰胺化合物。 药物组合物用于治疗和预防1型和2型糖尿病，葡萄糖耐量受损，高脂血症或高血压。 通过将化学式2的R1取代的2-甲基-2H-色烯-2-羧酸化合物与胺化合物（NHR 2 R 2） ^ 3）。

公开(公告)号：KR1020110012089A

公开(公告)日：2011-02-09

申请号：KR1020090069646

申请日：2009-07-29

Applicant: 한국화학연구원 ,  에스케이케미칼주식회사

Inventor： 공영대 ,  조희영 ,  이태호 ,  최길돈 ,  전문국 ,  박우규 ,  공재양 ,  황순희 ,  정대영 ,  이봉용 ,  엄기안 ,  김재선 ,  류근호 ,  류제호 ,  김신애 ,  한혜영 ,  손현주 ,  이현정 ,  김용혁 ,  박성훈

IPC: C07D311/58 ,  C07D311/04 ,  C07D311/02

Abstract: PURPOSE: A 2-(2-amido methyl)-2-methyl-2H-benzypyrane compound is provided to ensure selective suppression to 11 beta-HSD 1 enzyme and to prevent and treat clucocorticoid regulatory diseases. CONSTITUTION: A 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound is denoted by chemical formula 1. The 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound is 3-methoxy-N-methyl-N-[(2-methyl-8-nitro-2H-chromen-2-yl)methyl]benzamide or 3-chloro-N-[(2,6-dimethyl-2H-chromen-2-yl)methyl]-N-methylbenzamide. A pharmaceutical composition contains the 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound and prevents and treats impaired glucose tolerance(IGT), type 1 and 2 diabetes, insulin resistance, dyslipidemia or hypertension.

Abstract translation: 目的：提供2-（2-氨基甲基）-2-甲基-2H-苯并吡喃化合物，以确保对11β-HSD 1酶的选择性抑制，并预防和治疗类皮质激素调节性疾病。 构成：2-（2-氨基甲基）-2-甲基-2H-苯并吡喃化合物由化学式1表示。2-（2-酰氨基甲基）-2-甲基-2H-苯并吡喃化合物是3-甲氧基 - N-甲基-N - [（2-甲基-8-硝基-2H-色烯-2-基）甲基]苯甲酰胺或3-氯-N - [（2,6-二甲基-2H-色烯-2-基） 甲基] -N-甲基苯甲酰胺。 药物组合物含有2-（2-酰氨基甲基）-2-甲基-2H-苯并吡喃化合物，并预防和治疗葡萄糖耐量异常（IGT），1型和2型糖尿病，胰岛素抵抗，血脂异常或高血压。

公开(公告)号：KR100916716B1

公开(公告)日：2009-09-10

申请号：KR1020070097554

申请日：2007-09-27

Applicant: 한국화학연구원 ,  (주)아모레퍼시픽

Inventor： 공영대 ,  조희영 ,  전문국 ,  이태호 ,  최길돈 ,  공재양 ,  박우규 ,  황순희 ,  김정주 ,  이창훈 ,  고재영 ,  노민수 ,  한은실 ,  김혁 ,  윤준원 ,  모주현 ,  김도훈

IPC: C07D401/12 ,  A61K31/498 ,  A61P29/00

CPC classification number: C07D401/12

Abstract: 본 발명은 하기 화학식 1로 표시되는 3-클로로-5-치환-퀴녹살린-2-아민 유도체 및 약제학적으로 허용 가능한 그의 염, 그의 제조방법 및 그를 유효성분으로 함유하는 SPC 수용체 활성으로 유발되는 염증관련 질환에 유용한 그의 용도에 관한 것이다.
본 발명의 3-클로로-5-치환-퀴녹살린-2-아민 유도체는 사람으로부터 유래된 진피세포 및 마우스를 이용한 동물실험을 통하여 항염증 효과를 검색한 결과, SPC 수용체에 대한 우수한 억제활성을 규명함으로써, 상기 3-클로로-5-치환-퀴녹살린-2-아민 유도체 및 약제학적으로 허용 가능한 그의 염을 유효성분으로 함유하여 SPC 수용체 활성으로 유발되는 아토피성 피부염, 기타 질환에서 나타나는 염증, 소양증 또는 피부 감염증에 유효한 염증관련 질환 치료제로서 유용하게 활용될 수 있다.


(상기 식에서, R
1 및 R
2 는 명세서에서 정의한 바와 같다.)