公开(公告)号：KR101862765B1

公开(公告)日：2018-05-30

申请号：KR1020170051775

申请日：2017-04-21

Applicant: 한국화학연구원

Inventor： 임채조 ,  이규양 ,  이병호 ,  오광석 ,  이정현 ,  서호원 ,  김대근

IPC: C07D401/12 ,  A61K31/496 ,  A23L33/10

CPC classification number: C07D401/12 ,  A23L33/10 ,  A23V2002/00 ,  A23V2200/30 ,  A61K31/496

Abstract: 본발명은 N-아릴사이클릭아민유도체, 이의제조방법및 이를유효성분으로포함하는유로텐신-Ⅱ수용체활성관련질환의예방또는치료용약학적조성물에관한것이다. 본발명에따른 N-아릴사이클릭아민유도체는유로텐신-Ⅱ수용체에대한길항제로작용함으로써울혈성심부전, 심장허혈, 심근경색, 심장비대증, 심장섬유증, 관상동맥질환, 동맥경화증, 고혈압, 천식, 신부전, 당뇨병, 혈관염증, 신경퇴행성질환, 뇌졸중, 통증, 우울증, 정신병, 암등과같은유로텐신-Ⅱ수용체활성관련질환을예방또는치료하는데유용하게사용할수 있다.

公开(公告)号：KR101571529B1

公开(公告)日：2015-11-24

申请号：KR1020130145437

申请日：2013-11-27

Applicant: 한국화학연구원

Inventor： 이병호 ,  이규양 ,  오광석 ,  임채조 ,  이정현 ,  김낙정 ,  서지희 ,  서호원

IPC: C07D413/14 ,  A61K31/538 ,  A61P9/00

Abstract: 본발명은 5각형헤테로아릴기를포함하는벤조옥사지논유도체또는이의약학적으로허용가능한염, 이의제조방법및 이를유효성분으로함유하는유로텐신-Ⅱ수용체과활성에의한질환의예방또는치료용약학적조성물에관한것으로, 본발명에따른 5각형헤테로아릴기를포함하는벤조옥사지논유도체는유로텐신-Ⅱ수용체에대한길항제로작용함으로써, 울혈성심부전, 심장허혈, 심근경색, 심장비대증, 심장섬유증, 관상동맥질환, 동맥경화증, 고혈압, 천식, 신부전, 당뇨병, 혈관염증, 신경퇴행성질환, 뇌졸중, 통증, 우울증, 정신병및 암과같은 U-Ⅱ수용체과활성에의한질환을예방, 개선또는치료하는데유용하게사용할수 있다.

公开(公告)号：KR1020130100587A

公开(公告)日：2013-09-11

申请号：KR1020120021943

申请日：2012-03-02

Applicant: 한국화학연구원

Inventor： 이병호 ,  이규양 ,  오광석 ,  임채조 ,  서호원 ,  이진수 ,  박휘정

IPC: C07D401/12 ,  C07D403/10 ,  A61K31/454 ,  A61P9/00

Abstract: PURPOSE: A 1H-indazole-5-ylamino-substituted heterocyclic compound is provided to prevent or treat various cardiovascular diseases caused by vasoconstriction. CONSTITUTION: A 1H-indazole-5-ylamino-substituted heterocyclic compound of chemical formula 1 or a pharmaceutically acceptable salt, a solvate, or a hydrate thereof is provided. The compound is selected among compounds of chemical formulas 2-4. A pharmaceutical composition for preventing or treating cardiovascular diseases contains pharmaceutically effective amount of the compound and a pharmaceutically acceptable carrier.

Abstract translation: 目的：提供1H-吲唑-5-基氨基取代的杂环化合物，以预防或治疗由血管收缩引起的各种心血管疾病。 构成：提供化学式1的1H-吲唑-5-基氨基取代的杂环化合物或其药学上可接受的盐，溶剂化物或其水合物。 化合物选自化学式2-4的化合物。 用于预防或治疗心血管疾病的药物组合物含有药学上有效量的化合物和药学上可接受的载体。

公开(公告)号：KR1020120103220A

公开(公告)日：2012-09-19

申请号：KR1020110021367

申请日：2011-03-10

Applicant: 한국화학연구원

Inventor： 이규양 ,  임채조 ,  이은경 ,  김수희 ,  송석진

IPC: C07D405/12 ,  C07D405/14 ,  A61K31/4525 ,  A61P3/00

Abstract: PURPOSE: A method for preparing novel benzofuran-2-carboxamide derivative is provided to prevent or treat MCH receptor-1 related diseases such as obesity, diabetes, metabolic disorder, anxiety, and depression. CONSTITUTION: A benzofuran-2-carboxamide derivative is denoted by chemical formula 1. A pharmaceuticalcomposition for preventing and treating MCH receptor-1 related diseases contains the derivative or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. A food composition for preventing or treating MCH receptor-1 related diseases contains the derivative or salt of hydrate thereof as an active ingredient. A method for preparing the derivative comprises a step of reacting a compound of chemical formula 2 with a compound of chemical formula 3 in a solvent. [Reference numerals] (AA) Condensation

Abstract translation: 目的：提供一种制备新型苯并呋喃-2-甲酰胺衍生物的方法，以预防或治疗MCH受体1相关疾病，如肥胖，糖尿病，代谢紊乱，焦虑和抑郁。 构成：苯并呋喃-2-甲酰胺衍生物由化学式1表示。用于预防和治疗MCH受体-1相关疾病的药物组合物含有作为活性成分的衍生物或其药学上可接受的盐或水合物。 用于预防或治疗MCH受体-1相关疾病的食物组合物含有其水合物的衍生物或盐作为活性成分。 制备衍生物的方法包括使化学式2的化合物与化学式3的化合物在溶剂中反应的步骤。 （附图标记）（AA）冷凝

公开(公告)号：KR1020120034829A

公开(公告)日：2012-04-13

申请号：KR1020100084156

申请日：2010-08-30

Applicant: 한국화학연구원

Inventor： 이규양 ,  임채조 ,  김낙정 ,  이병호 ,  이상달 ,  서무영 ,  왕수미

IPC: C07D401/06 ,  A61K31/501 ,  A61P3/00

Abstract: PURPOSE: A phthalazinone derivative containing an aryl piperidine group and a pharmaceutical composition containing the same are provided to prevent or treat MCH-associated diseases. CONSTITUTION: A phthalazinone derivative containing an aryl piperidine group is denoted by chemical formula 1. A method for preparing the derivative comprises a step of alkylating a compound of chemical formula 2 with a piperidine compound of chemical formula 3 under the presence of organic solvent and base. The organic solvent ether solvent, low alcohol of C1-C4, DMF(dimethyl formamide), DMSO(dimethyl sulfoxide, acetonitrile or water. The base is an organic base including pyridine, triethyl amine, N,N-diisopropyl ethyl amine(DIPEA), 1,8-diazabicylco[5.4.0]-undecene(DBU); or an inorganic base including sodium hydroxide, sodium carbonate, potassium carbonate, cesium carbonate, and sodium hydride.

Abstract translation: 目的：提供含有芳基哌啶基的酞嗪酮衍生物和含有该芳基哌啶基团的药物组合物以预防或治疗MCH相关疾病。 构成：含有芳基哌啶基的酞嗪酮衍生物由化学式1表示。制备该衍生物的方法包括在有机溶剂和碱的存在下用化学式3的哌啶化合物烷基化化学式2的化合物的步骤 。 有机溶剂醚溶剂，C1-C4的低级醇，DMF（二甲基甲酰胺），DMSO（二甲基亚砜，乙腈或水），碱是包括吡啶，三乙胺，N，N-二异丙基乙胺（DIPEA） ，1,8-二氮杂双环[5.4.0] - 十一碳烯（DBU）;或包含氢氧化钠，碳酸钠，碳酸钾，碳酸铯和氢化钠的无机碱。

公开(公告)号：KR101069166B1

公开(公告)日：2011-09-30

申请号：KR1020090048675

申请日：2009-06-02

Applicant: 한국화학연구원

Inventor： 김낙정 ,  배명애 ,  유성은 ,  강남숙 ,  허정녕 ,  이규양 ,  서지희 ,  임채조 ,  황은숙 ,  홍정호

IPC: C07D257/04 ,  C07D403/08 ,  A61P19/10

Abstract: 본 발명은 이미다조 페닐테트라졸 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 골다공증, 비만, 당뇨 또는 고지혈증의 예방 또는 치료용 약학적 조성물에 관한 것으로서, 상기 유도체는 TAZ 단백질을 조절하므로, 골다공증, 비만, 당뇨 또는 고지혈증의 예방 또는 치료에 유용하게 사용될 수 있다.
이미다조 페닐테트라졸 유도체, TAZ, 골다공증, 비만, 당뇨, 고지혈증

公开(公告)号：KR1020100093944A

公开(公告)日：2010-08-26

申请号：KR1020090013112

申请日：2009-02-17

Applicant: 순천대학교 산학협력단 ,  한국화학연구원

Inventor： 최상기 ,  이규양 ,  백형록 ,  오재현 ,  박정로 ,  김낙정 ,  임채조 ,  채종학 ,  김선호

IPC: C07D263/58 ,  C07D263/54

Abstract: PURPOSE: A fluorphenyl benzoxazole derivative with antifungal activity is provided to selectively suppress protein synthesis of pathogenic fungus. CONSTITUTION: A fluorophenyl benzyoxazole derivative is denoted by chemical formula 1. The fluorophenyl benzyoxazole derivative is 2,2-dibromo-1-(2-(4-fluorophenyl)benzo[d]oxazole-5-yl)ethanone, 3,3-dibromo-1-(2-(4-fluorophenyl)benzo[d]oxazole-5-yl)propane-1-one; or 2-bromo-1-(2-(4-fluorophenyl)benzo[d]oxazole-5-yl)propane-1-one. A compound of chemical formula 1 is prepared by halogenationg of a compound of chemical formula 2 with halogenating agent. An antifungal composition contains the fluorophenyl benzyoxazole derivative or pharmaceutically acceptable salt thereof as an active ingredient.

Abstract translation: 目的：提供具有抗真菌活性的氟苯基苯并恶唑衍生物，以选择性抑制病原真菌的蛋白质合成。 氟苯基苯并恶唑衍生物是2,2-二溴-1-（2-（4-氟苯基）苯并[d]恶唑-5-基）乙酮，3,3-二氟-1-苯并恶唑衍生物， 二溴-1-（2-（4-氟苯基）苯并[d]恶唑-5-基）丙烷-1-酮; 或2-溴-1-（2-（4-氟苯基）苯并[d]恶唑-5-基）丙-1-酮。 通过用卤化剂卤化化学式2的化合物制备化学式1的化合物。 抗真菌组合物含有氟苯基苯并恶唑衍生物或其药学上可接受的盐作为活性成分。

公开(公告)号：KR1020100093943A

公开(公告)日：2010-08-26

申请号：KR1020090013111

申请日：2009-02-17

Applicant: 순천대학교 산학협력단 ,  한국화학연구원

Inventor： 최상기 ,  이규양 ,  백형록 ,  오재현 ,  성치남 ,  임채조 ,  서지희 ,  채종학

IPC: C07D263/58 ,  C07D263/54

Abstract: PURPOSE: A fluorophenyl oxazole derivative with antifungal activity is provided to selectively suppress protein synthesis of pathogenic fungus and to use as various antifungal agents. CONSTITUTION: A fluorophenyl oxazole derivative is denoted by chemical formula 1. A method for preparing fluorophenyl oxazole derivative or pharmaceutically acceptable salt thereof comprises: a step of performing nitration of a compound of chemical formula 6 to obtain a compound of chemical formula 7; a step of reducing the nitro compound of chemical formula 7 to obtain hydroxyl amine compound of chemical formula 8; a step of performing acylation of the hydroxy amine compound of chemical formula 8 with a compound of chemical formula 9 to obtain an amide compound of chemical formula 10; and a step of cyclizing the amide compound of chemical formula 10 to obtain the compound of chemical formula 1.

Abstract translation: 目的：提供具有抗真菌活性的氟苯基恶唑衍生物，以选择性抑制病原真菌的蛋白质合成并用作各种抗真菌剂。 构成：氟苯基恶唑衍生物由化学式1表示。制备氟苯基恶唑衍生物或其药学上可接受的盐的方法包括：对化学式6的化合物进行硝化以获得化学式7化合物的步骤; 降低化学式7的硝基化合物以获得化学式8的羟胺化合物的步骤; 用化学式9的化合物进行化学式8的羟基胺化合物的酰化以获得化学式10的酰胺化合物的步骤; 使化学式10的酰胺化合物环化，得到化学式1的化合物的工序。

公开(公告)号：KR1020100022618A

公开(公告)日：2010-03-03

申请号：KR1020080081209

申请日：2008-08-20

Applicant: 한국화학연구원

Inventor： 이규양 ,  이선경 ,  김낙정 ,  서지희 ,  임채조 ,  이병호 ,  오광석 ,  서호원 ,  유성은 ,  이경희 ,  김유선

IPC: C07D235/28 ,  A61K31/137 ,  A61K9/20

Abstract: PURPOSE: A 2-sulfanyl-benzimidazole-4-carboximidazole derivative is provided to repair damaged DNA and suppress poly(ADP-ribose)polymerase-1(PARP-1) which is an enzyme causing cell damage and apoptosis. CONSTITUTION: A 2-sulfanyl-benzimidazole-4-carboximidazole derivative is denoted by chemical formula 1. A 2-sulfanyl-benzimidazole-4-carboximidazole derivative is prepared by performing alkylation of a compound of chemical formula 2 and a compound of chemical formula 3. A basic catalyst is used in the preparation. The basic catalyst is carbonate including sodium carbonate, potassium carbonate, or cesium carbonate; hydroxide including potassium hydroxide or sodium hydroxide; hydride including sodium hydride; alkoxide including sodium methoxide and sodium t-butoxide; triethylamine; or pyridine. A pharmaceutical composition for preventing or treating diseases caused by over-activation contains the 2-sulfanyl-benzimidazole-4-carboximidazole derivative or its pharmaceutically acceptable salt as an active ingredient.

Abstract translation: 目的：提供2-硫基 - 苯并咪唑-4-甲胺唑衍生物修复损伤的DNA，并抑制作为引起细胞损伤和细胞凋亡的酶的聚（ADP-核糖）聚合酶-1（PARP-1）。 构成：2-硫基 - 苯并咪唑-4-甲胺唑衍生物由化学式1表示。2-硫基 - 苯并咪唑-4-甲胺咪唑衍生物是通过化学式2的化合物和化学式3的化合物的烷基化制备的 在制备中使用碱性催化剂。 碱性催化剂是碳酸钠，碳酸钾或碳酸铯; 氢氧化物包括氢氧化钾或氢氧化钠; 氢化物包括氢化钠; 包括甲醇钠和叔丁醇钠的醇盐; 三乙胺; 或吡啶。 用于预防或治疗由过度活化引起的疾病的药物组合物含有2-硫基 - 苯并咪唑-4-甲胺唑衍生物或其药学上可接受的盐作为活性成分。

公开(公告)号：KR101667563B1

公开(公告)日：2016-10-28

申请号：KR1020150047057

申请日：2015-04-02

Applicant: 한국화학연구원

Inventor： 이병호 ,  이규양 ,  임채조 ,  서지희 ,  오광석 ,  이정현 ,  장주영

IPC: C07D417/12 ,  C07D417/10 ,  A61K31/433 ,  A23L1/30

Abstract: 본발명은 1,3,4-싸이아다이아졸-2-아민유도체, 이의제조방법, 및이를유효성분으로포함하는유로텐신-Ⅱ수용체활성관련질환의예방또는치료용약학적조성물에관한것이다. 본발명에따른 1,3,4-싸이아다이아졸-2-아민유도체는유로텐신-Ⅱ수용체에대한길항제로작용함으로써울혈성심부전, 심장허혈, 심근경색, 심장비대증, 심장섬유증, 관상동맥질환, 동맥경화증, 고혈압, 천식, 신부전, 당뇨병, 혈관염증, 신경퇴행성질환, 뇌졸중, 통증, 우울증, 정신병, 암등과같은유로텐신-Ⅱ수용체활성관련질환을예방또는치료하는데유용하게사용할수 있다.