公开(公告)号：KR1020110121143A

公开(公告)日：2011-11-07

申请号：KR1020100040600

申请日：2010-04-30

Applicant: 원광대학교산학협력단 ,  한국화학연구원

Inventor： 박현 ,  김성연 ,  김석 ,  이규양 ,  김한영 ,  서지희 ,  김낙정

IPC: A61K31/423 ,  A61P31/00 ,  A61P43/00

CPC classification number: A61K31/423 ,  A23K20/137

Abstract: PURPOSE: A 1-[2-(4-nitro-phenyl)-benzooxazole-5-yl]-propane-1-one compound(1124JH0013) is provided to ensure excellent anti-coccidium effect. CONSTITUTION: A 1-[2-(4-nitro-phenyl)-benzooxazole-5-yl]-propane-1-one compound having anti-coccidium effect or pharmaceutically acceptable salt thereof is denoted by structural formula A. A veterinary composition for preventing or treating diseases caused by coccidium contains the compound of formula A or the salt as an active ingredient. A pharmaceutical composition for preventing and treating diseases caused by coccidium contains the compound as an active ingredient. An animal feed additive contains the compound of formula A as an active ingredient.

Abstract translation: 目的：提供1- [2-（4-硝基 - 苯基） - 苯并恶唑-5-基] - 丙烷-1-酮化合物（1124JH0013），以确保优异的抗球虫效果。 构成：具有抗球虫作用的1- [2-（4-硝基 - 苯基） - 苯并恶唑-5-基] - 丙烷-1-酮化合物或其药学上可接受的盐由结构式A表示。 预防或治疗由球虫引起的疾病，含有式A化合物或其盐作为活性成分。 用于预防和治疗由球虫引起的疾病的药物组合物含有该化合物作为活性成分。 动物饲料添加剂含有式A化合物作为活性成分。

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：KR101068152B1

公开(公告)日：2011-09-27

申请号：KR1020090013114

申请日：2009-02-17

Applicant: 순천대학교 산학협력단 ,  한국화학연구원

Inventor： 최상기 ,  이규양 ,  백형록 ,  오재현 ,  정상철 ,  김낙정 ,  채종학 ,  김선우

IPC: C07D261/20 ,  C07D263/54

Abstract: 본 발명은 병원성 진균류의 단백질 합성을 선택적으로 저해하여 우수한 항진균 활성을 갖는 플루오로페닐 벤조옥사졸 유도체, 이의 제조방법 및 항진균제로서의 용도에 관한 것이다.
단백질 합성, 병원성 진균류, 항진균제

Abstract translation: 本发明涉及使用作为苯基苯并恶唑衍生物，它们的制备和抗真菌剂氟烷具有优异的抗真菌活性，以选择性地抑制致病真菌的蛋白质的合成。

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：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：KR100871077B1

公开(公告)日：2008-11-28

申请号：KR1020070046077

申请日：2007-05-11

Applicant: 한국화학연구원

Inventor： 김낙정 ,  유성은 ,  이규양 ,  서지희 ,  안미자 ,  이병호 ,  오광석 ,  천혜경

IPC: C07D401/14 ,  C07D409/14 ,  C07D405/14 ,  A61K31/4439

Abstract: A pharmaceutical composition is provided to prevent and cure diseases relating to MCH using an aryl piperidine group-containing imidazole derivative as an active ingredient. A pharmaceutical composition includes an aryl piperidine group-containing imidazole derivative represented by a formula to an active ingredient. In the formula: R1 is group1, and group2 or group3; R4 is H, halogen, C1~C3 of a straight-chain or a side-chain alkyl, or C1~C3 of a straight-chain or a side-chain alkoxy; W is CH or N; Y is O, S or NR8; R8 is H or C1~C3 of a straight-chain or a side-chain alkyl; M is an integer of 1-2; R2 is H, halogen, C1~C3 of a straight-chain or a side-chain alkyl, or C1~C3 of a straight-chain or a side-chain alkoxy, NO2; R3 is C1~C3 of a straight-chain or a side-chain alkyl; A is CH; and N is an integer of 2-5.

Abstract translation: 提供了一种药物组合物，用于使用含芳基哌啶基的咪唑衍生物作为活性成分来预防和治疗与MCH有关的疾病。 药物组合物包含由式表示的含有芳基哌啶基的咪唑衍生物作为活性成分。 在公式中：R1是group1，group2或group3; R4是直链或侧链烷基的H，卤素，C1〜C3，或直链或侧链烷氧基的C1〜C3; W是CH或N; Y为O，S或NR8; R8是直链或侧链烷基的H或C1〜C3; M为1-2的整数; R2是直链或侧链烷基的H，卤素，C1〜C3，或直链或侧链烷氧基的C1〜C3; R3是直链或侧链烷基的C1〜C3; A是CH; N为2-5的整数。

公开(公告)号：KR100832750B1

公开(公告)日：2008-05-27

申请号：KR1020060124581

申请日：2006-12-08

Applicant: 한국화학연구원

Inventor： 서지희 ,  유성은 ,  김낙정 ,  김은희 ,  정용삼 ,  이윤숙 ,  서해영

IPC: A61K31/166 ,  A61P9/10

Abstract: A composition is provided to decrease ischemic apoptosis significantly, thereby being usefully utilized as a prophylactic or therapeutic agent of ischemic diseases mediated by the ischemic apoptosis, or an organ protecting agent. A composition for preventing or treating an ischemic disease selected from the group consisting of cerebral ischemia, cardiac ischemia, diabetic cardiovascular diseases, cardiac failure, hypertrophy, retinal ischemia, ischemic colitis, ischemic acute cardiac failure, stroke, traumatic brain injury, Alzheimer's disease, Parkinson's disease, newborn hypoxia, glaucoma and diabetic neurosis mediated by ischemic apoptosis comprises an N-phenyl amide derivative represented by a formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient, wherein the ischemic apoptosis is induced under low oxygen condition. In the formula(1), R^1 is H, -CO2R^5, -CH2OR^5, -CONR^5R^5, or a structural formula(1)(wherein each R^5 and R^6 is independently H or methyl); each R^2, R^3 and R^4 is independently H, C1-3 alkyl or alkoxy, or halogen; B is H or phenyl; n is 0 or 1; Y is S; Z is H, halogen or C1-3 alkoxy; and A is CH or N.

Abstract translation: 提供了显着降低缺血性凋亡的组合物，从而有效地用作由缺血性细胞凋亡介导的缺血性疾病或器官保护剂的预防或治疗剂。 用于预防或治疗缺血性疾病的组合物，其选自脑缺血，心脏缺血，糖尿病心血管疾病，心力衰竭，肥大，视网膜缺血，缺血性结肠炎，缺血性急性心力衰竭，中风，创伤性脑损伤，阿尔茨海默氏病， 由缺血性细胞凋亡介导的帕金森病，新生儿缺氧，青光眼和糖尿病性神经症包括由式（1）表示的N-苯基酰胺衍生物或其药学上可接受的盐作为有效成分，其中在低氧条件下诱导缺血性凋亡。 在式（1）中，R 1是H，-CO 2 R 5，-CH 2 OR 5，-CONR 5 R 5或结构式（1）（其中每个R 5和R 6独立地是H 或甲基）; 每个R 2，R 3和R 4独立地是H，C 1-3烷基或烷氧基或卤素; B是H或苯基; n为0或1; Y是S; Z是H，卤素或C 1-3烷氧基; A是CH或N.

公开(公告)号：KR100820246B1

公开(公告)日：2008-04-07

申请号：KR1020060098670

申请日：2006-10-10

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  정준원 ,  박창민 ,  소원영 ,  강남숙 ,  서지희 ,  김낙정 ,  박순찬 ,  천혜경 ,  조영식 ,  배명애 ,  김기영 ,  송진숙 ,  현영란 ,  김용은 ,  노성구 ,  이태규 ,  조중명 ,  유성은

IPC: C07D231/12 ,  C07D401/04

Abstract: A novel pyrazole compound is provided to show excellent inhibitory activity on PDE-4 enzyme, thereby being used in order to prevent and treat asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases. A 1-(3,4-dialkoxybenzyl)-1H-pyrazole compound is represented by the formula(1), wherein each R1 and R2 is independently H, linear or branched C1-7 alkyl, linear or branched C1-7 C1-7 alkyl including halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, 3- to 7-membered heterocycloalkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkyl including O, N or S in a hetero-cycle, phenyl, benzyl or allyl, or R1 and R2 may be linked to each other with C1-3 alkylene or C1-3 alkylene including halogen; R3 is H, formyl, halogen, linear or branched C1-10 alkyl, C1-10 alkoxy, C3-7 cycloalkyl, (C1-7)alkoxy(C1-7)alkyl, C1-7 alkyl ketone, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, (C1-10)alkylcarboxylic acid, carboxyl(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl; (C3-7)cycloalkylamino, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide, cyano, nitro, carboxylic acid guanidine, urea, phenoxy, benzyloxy, or an Aryl represented by the group(I); each R4 and R5 is independently H, halogen, formyl, linear or branched C1-10 alkyl, C1-10 alkoxy, (C1-10)alkoxy(C1-10)alkyl, C1-7 alkylketone, hydroxy(C1-10)alkyl, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, carboxylic acid, carboxyl(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, phenyl, phenoxy, benzyl, benzyloxy, 3- to 7-membered heterocycloalkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkoxy including O, N or S in a hetero-cycle, cyano, nitro, (C3-7)cycloalkylamino, guanidine, or urea. A method for preparing the compound of the formula(1) comprises a step of reacting a halobenzyl compound represented by the formula(3) with a pyrazole compound represented by the formula(4), each R1, R2, R3, R4, and R5 are same as defined above, and X is halogen. A pharmaceutical composition for preventing and treating inflammation related diseases such as asthma and chronic obstructive pulmonary diseases comprises the compound of the formula(1) as an effective ingredient.

Abstract translation: 提供了一种新的吡唑化合物，以显示对PDE-4酶的优异抑制活性，从而用于预防和治疗哮喘，慢性阻塞性肺病，关节炎，特应性皮炎，肿瘤和退行性脑疾病。 1-（3,4-二烷氧基苄基）-1H-吡唑化合物由式（1）表示，其中每个R 1和R 2独立地为H，直链或支链C 1-7烷基，直链或支链C 1-7 C1-7 烷基，包括卤素，C 3-7环烷基，（C 3-7）环烷基（C 1-7）烷基，在杂环中包括O，N或S的3-至7-元杂环烷基，3-至7-元杂环烷基 -7）烷基，包括异环周期中的O，N或S，苯基，苄基或烯丙基，或者R 1和R 2可以与C 1-3亚烷基或包括卤素的C 1-3亚烷基彼此连接; R 3为H，甲酰基，卤素，直链或支链C 1-10烷基，C 1-10烷氧基，C 3-7环烷基，（C 1-7）烷氧基（C 1-7）烷基，C 1-7烷基酮，（C 3-7） 环烷基（C1-7）烷基，（C3-7）环烷基（C1-7）烷氧基，（C1-10）烷基羧酸，羧基（C1-10）烷基酯，羧基（C1-10）烷基酰胺，氨基，单或二 （C 1-7）烷基氨基，单或二（C 1-7）烷基氨基羰基; （C3-7）环烷基氨基，吗啉，吗啉氧化物，哌啶，哌嗪，哌嗪氧化物，氰基，硝基，羧酸胍，脲，苯氧基，苄氧基或由基团（I）表示的芳基。 每个R 4和R 5独立地为H，卤素，甲酰基，直链或支链C 1-10烷基，C 1-10烷氧基，（C 1-10）烷氧基（C 1-10）烷基，C 1-7烷基酮，羟基（C 1-10）烷基 ，C3-7环烷基，（C3-7）环烷基（C1-7）烷基，（C3-7）环烷基（C1-7）烷氧基，羧酸，羧基（C1-10）烷基酯，羧基（C1-10）烷基酰胺 ，氨基，单或二（C1-7）烷基氨基，单或二（C1-7）烷基氨基羰基，苯基，苯氧基，苄基，苄氧基，包含异质周期中的O，N或S的3-至7-元杂环烷基， 包含杂环中的O，N或S的3-至7-元杂环烷基（C 1-7）烷基，异异环中包括O，N或S的3-至7-元杂环烷基（C 1-7）烷氧基， 氰基，硝基，（C 3-7）环烷基氨基，胍或脲。 制备式（1）化合物的方法包括使由式（3）表示的卤苄基化合物与式（4）表示的吡唑化合物反应，每个R 1，R 2，R 3，R 4和R 5 与上述相同，X为卤素。 用于预防和治疗炎症相关疾病如哮喘和慢性阻塞性肺疾病的药物组合物包含式（1）化合物作为有效成分。

公开(公告)号：KR100633095B1

公开(公告)日：2006-10-12

申请号：KR1020040019097

申请日：2004-03-20

Applicant: 한국화학연구원

Inventor： 이규양 ,  이선경 ,  김낙정 ,  서지희 ,  이병호 ,  김태미 ,  유성은

IPC: C07D307/68

Abstract: 본 발명은 3,5-위치가 치환된 퓨란-2-카르보닐구아니딘 유도체, 그의 제조방법 및 이를 포함하는 약학적 조성물에 관한 것이다.
본 발명의 3,5-위치가 치환된 퓨란-2-카르보닐구아니딘 유도체는 나트륨/수소 교환통로인 NHE-1에 대하여 강력한 억제작용을 나타내고, 적출 허혈심장모델에서 허혈/재관류에 의한 심장기능 손상의 회복을 증진시키며,
in vivo 허혈동물모델에서 심근경색의 크기를 유의성있게 감소시켜 우수한 심장보호효과를 나타낸다.
따라서, 본 발명의 조성물은 심근경색, 부정맥, 협심증 등의 허혈성 심장질환의 예방 및 치료에 유용하게 사용될 수 있으며, 관동맥우회술, 관동맥경피성형술 등 심장시술 시 또는 혈전용해제 등 재관류요법에 대한 심장보호제 등으로 사용될 수 있다.

公开(公告)号：KR100518184B1

公开(公告)日：2005-10-04

申请号：KR1020030098027

申请日：2003-12-27

Applicant: 한국화학연구원

Inventor： 이규양 ,  이선경 ,  김낙정 ,  서지희 ,  황순희 ,  이병호 ,  서호원 ,  황선경 ,  유성은

IPC: C07D307/68

CPC classification number: C07D307/68

Abstract: 본 발명은 퓨란카보닐구아니딘 유도체, 그의 제조방법 및 그를 포함하는 약학적 조성물에 관한 것이다.
본 발명의 퓨란카보닐구아니딘 유도체는 나트륨/수소 교환통로인 NHE-1 (sodium-hydrogen exchanger isoform 1)을 억제하여 허혈/재관류 손상에 대하여 심장기능 회복을 증진시키고 심근경색율을 감소시켜 심근세포 손상을 보호함으로써, 심근경색, 부정맥, 협심증 등의 허혈성 심장질환의 예방 및 치료제로 사용할 수 있으며, 또한 관동맥우회술, 관동맥경피성형술 등 심장시술시 또는 혈전용해제 등 재관류요법에 대한 심장보호제 등으로 사용할 수 있다.