公开(公告)号：KR1020120040980A

公开(公告)日：2012-04-30

申请号：KR1020100102522

申请日：2010-10-20

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  정명호 ,  엘가말모하메드 ,  유경호 ,  심태보 ,  최원경 ,  조정혁

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

Abstract: PURPOSE: A pyrrolo[3,2-c]pyridine derivative and a pharmaceutical composition containing the same are provided to ensure anti-proliferatioin activity of melanoma and to prevent or treat melanoma. CONSTITUTION: A pyrrolo[3,2-c]pyridine derivative is denoted by chemical formula I. A method for preparing the pyrrolo[3,2-c]pyridine derivative of chemical formula I' or pharmaceutically acceptable salt thereof comprises: a step of reacting 4-chloro-1-pyrrolo[2,3-b]pyridine of chemical formula II with nitroaniline to prepare a compound of chemical formula III; a step of reacting a compound of chemical formula III with benzoyl chloride to prepare a compound of chemical formula IV; a step of reducing the compound of chemical formula IV to prepare a compound of chemical formula V; and a step of reacting the compound of chemical formula V with a compound of chemical formula VI or formula VII.

Abstract translation: 目的：提供吡咯并[3,2-c]吡啶衍生物和含有它们的药物组合物，以确保黑色素瘤的抗增殖活性并预防或治疗黑素瘤。 构成：化学式I表示吡咯并[3,2-c]吡啶衍生物。制备化学式I'吡咯并[3,2-c]吡啶衍生物或其药学上可接受的盐的方法包括： 使化学式II的4-氯-1-吡咯并[2,3-b]吡啶与硝基苯胺反应制备化学式Ⅲ化合物; 使化学式III的化合物与苯甲酰氯反应以制备化学式IV的化合物的步骤; 降低化学式IV化合物以制备化学式V的化合物的步骤; 以及使化学式V的化合物与化学式VI或式VII的化合物反应的步骤。

公开(公告)号：KR101083421B1

公开(公告)日：2011-11-14

申请号：KR1020090055939

申请日：2009-06-23

Applicant: 한국과학기술연구원

Inventor： 하정미 ,  유경호 ,  심태보 ,  오창현 ,  유하나 ,  김환 ,  정윤경 ,  이정헌

IPC: C07D487/04 ,  C07D487/02 ,  A61K31/4188

Abstract: (상기화학식 1에서, R, R, R, R및 R는본 명세서에서정의된바와같다)

公开(公告)号：KR1020110019584A

公开(公告)日：2011-02-28

申请号：KR1020090077185

申请日：2009-08-20

Applicant: 한국과학기술연구원

Inventor： 심태보 ,  함영진 ,  유경호 ,  오창현 ,  하정미 ,  김환 ,  최환근 ,  이정헌

IPC: C07D209/04 ,  C07D403/04 ,  A61K31/40 ,  A61P29/00

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

Abstract: PURPOSE: A 1,3,6-substituted indole compound having an activity of suppressing protein kinase is provided to suppress various protein kinases and to prevent and treat abnormal cell growth diseases. CONSTITUTION: A 1,3,6-substituted indole compound is denoted by chemical formula 1. A pharmaceutical composition contains 1,3,6-substituted indole compound of chemical formula 1 as an active ingredient. The pharmaceutical composition prevents and treats abnormal cell growth diseases through protein kinase suppression mechanism selected from Raf, KDR, Fms, Tie2, SAPK2a, Ret, Abl, Abl(T315I), ALK, Aurora A, Bmx, CDK/cyclinE, Kit, Src, EGFR, EphA1, FGFR3, Flt3, Fms, IGF-1R, IKKb, IR, Itk, JAK2, KDR, Met, mTOR, PDGFRa, Plk1, Ret, Syk, Tie2, and TrtB. An agent for preventing and treating tumor contains 1,3,6-substituted indole compound of chemical formula 1.

Abstract translation: 目的：提供具有抑制蛋白激酶活性的1,3,6-取代的吲哚化合物以抑制各种蛋白激酶并预防和治疗异常的细胞生长疾病。 构成：1,3,6-取代的吲哚化合物由化学式1表示。药物组合物含有化学式1的1,3,6-取代的吲哚化合物作为活性成分。 药物组合物通过选自Raf，KDR，Fms，Tie2，SAPK2a，Ret，Abl，Abl（T315I），ALK，Aurora A，Bmx，CDK / cyclinE，Kit，Src的蛋白激酶抑制机制预防和治疗异常细胞生长疾病 ，EGFR，EphA1，FGFR3，Flt3，Fms，IGF-1R，IKKb，IR，Itk，JAK2，KDR，Met，mTOR，PDGFRa，Plk1，Ret，Syk，Tie2和TrtB。 用于预防和治疗肿瘤的药物含有化学式1的1,3,6-取代的吲哚化合物。

公开(公告)号：KR1020100047998A

公开(公告)日：2010-05-11

申请号：KR1020080106962

申请日：2008-10-30

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  유경호 ,  심태보 ,  이소하 ,  하정미 ,  김희진 ,  정명호

IPC: C07D487/04

Abstract: PURPOSE: A novel pyrollo[3,2-b]pyridine derivative and a pharmaceutical composition for preventing or treating melanoma containing the same are provided to ensure high anti-proliferative activity to melanoma cells. CONSTITUTION: A pyrollo(3,2-b)pyridine derivative is denoted by chemical formula 1. A method for preparing the pirrolo(3,2,-b)pyridine derivative comprises: a step of coupling 1-iodine-4-nitrobenze to a compound of chemical formula 2 to obtain a compound of chemical formula 3; a step of reducing the compound of chemical formula 3 to obtain a compound of chemical formula 4; and a step of coupling the compound of chemical formula 4 with a phenylcarboxylic acid or amine derivative which trifluoromethyl, halogen, morpholine, piperazine. A pharmaceutical composition for preventing or treating melanoma contains the pyrollo(3,2-b)pyridine derivative or pharmaceutically acceptable salt as an active ingredient.

Abstract translation: 目的：提供一种新型的吡咯并[3,2-b]吡啶衍生物和用于预防或治疗含有此类黑色素瘤的药物组合物，以确保对黑素瘤细胞的高抗增殖活性。 构成：吡咯（3,2-b）吡啶衍生物由化学式1表示。制备吡罗咯（3,2，-b）吡啶衍生物的方法包括：将1-碘-4-硝基苯偶联到 化学式2的化合物，得到化学式3的化合物; 还原化学式3的化合物以获得化学式4的化合物的步骤; 以及将化学式4的化合物与三氟甲基，卤素，吗啉，哌嗪的苯基羧酸或胺衍生物偶合的步骤。 用于预防或治疗黑素瘤的药物组合物含有吡罗洛（3,2-b）吡啶衍生物或其药学上可接受的盐作为活性成分。

公开(公告)号：KR1020090129377A

公开(公告)日：2009-12-16

申请号：KR1020090052245

申请日：2009-06-12

Applicant: 한국과학기술연구원 ,  한미사이언스 주식회사

Inventor： 김동진 ,  유경호 ,  변지훈 ,  김영수 ,  김혜연 ,  이관순 ,  김맹섭 ,  안영길 ,  이지훈 ,  이명환 ,  황하나 ,  류지연

IPC: C07D307/78 ,  C07D307/81 ,  C07D307/77

CPC classification number: C07D307/81 ,  C07D307/80

Abstract: PURPOSE: A pharmaceutical composition containing styrylbenzofuran compound is provided to ensure suppression efficiency of beta amyloid fibril formation. CONSTITUTION: A styrylbenzofuran compound is denoted by chemical formula 1. A compound of chemical formula 1 is obtained through Honer-Emmons reaction of a compound of chemical formula 2 with a compound of chemical formula 3 and alkali under the presence of organic solvent. The alkali is hydride of alkali metal, alkyl alkali metal compound, alkoxide compound of alkali metal or alkali metal amide compound. The organic solvent is ether organic solvent. A product thorugh Honer-Emmons reaction is demethylated using boron trichloride, boron trifluoride, boron tribromide or iodotrimethylsilane.

Abstract translation: 目的：提供含有苯乙烯基苯并呋喃化合物的药物组合物，以确保β-淀粉样蛋白原纤维形成的抑制效率。 组成：苯乙烯基苯并呋喃化合物由化学式1表示。化学式1的化合物通过化学式2的化合物与化学式3的化合物和碱在有机溶剂的存在下的Hon-Emmons反应获得。 碱是碱金属的氢化物，烷基碱金属化合物，碱金属或碱金属酰胺化合物的醇盐化合物。 有机溶剂为醚有机溶剂。 使用三氯化硼，三氟化硼，三溴化硼或碘代三甲基硅烷将Honer-Emmons反应产物脱甲基化。

公开(公告)号：KR1020090042579A

公开(公告)日：2009-04-30

申请号：KR1020070108420

申请日：2007-10-26

Applicant: 한국과학기술연구원

Inventor： 이지훈 ,  김동진 ,  박웅서 ,  강용구 ,  유경호 ,  이혀지 ,  문대혁 ,  오승준 ,  류진숙 ,  김재승 ,  김의녕

IPC: C07D209/48 ,  A61K31/4035 ,  A61P25/28

CPC classification number: C07D209/46 ,  C07D209/48

Abstract: An Isoindolone compound showing excellent binding affinity to beta-Amyloid fibril is provided to treat and prevent degenerative brain diseases by inhibiting generation of beta-Amyloid fibril. A pharmaceutical composition comprises an Isoindolone compound represented by the formula 1 or pharmaceutically allowable salts. In the formula 1, A is C=O or CH2; R1 is a halogen atom selected among H, OH, F, Br and I, a substituted C1-C8 alkoxy group or a C1-C8 alkylamino group, of which the substituted group is selected among a C1-C8 alkyl group, a C1-C8 alkoxy group, a tosyloxy-C1-C8 alkoxy group, a mesyloxy-C1-C8 alkoxy group, a nosyloxy-C1-C8 alkoxy group, H, OH, F, Br and I; R2 is a C1-C8 alkyl group or a halogen atom selected among H, OH, F, Br and I; and R3 and R4 are independently H, a C1-C8 alkoxy group or a C1-C8 alkylamino group.

Abstract translation: 提供了对β-淀粉样蛋白原纤维显示出优异结合亲和力的异吲哚酮化合物，通过抑制β-淀粉样蛋白原纤维的产生来治疗和预防退行性脑疾病。 药物组合物包含由式1表示的异吲哚酮化合物或其药学上可允许的盐。 在式1中，A为C = O或CH 2; R1是选自H，OH，F，Br和I中的卤素原子，取代的C1-C8烷氧基或C1-C8烷基氨基，其取代基选自C1-C8烷基，C1- C8烷氧基，甲苯磺酰氧基-C1-C8烷氧基，甲磺酰氧基-C1-C8烷氧基，Nosyloxy-C1-C8烷氧基，H，OH，F，Br和I; R2是C1-C8烷基或选自H，OH，F，Br和I中的卤素原子; 且R 3和R 4独立地为H，C 1 -C 8烷氧基或C 1 -C 8烷基氨基。

公开(公告)号：KR1020080022988A

公开(公告)日：2008-03-12

申请号：KR1020060086900

申请日：2006-09-08

Applicant: 한국과학기술연구원 ,  한미사이언스 주식회사

Inventor： 김동찬 ,  김동진 ,  유경호 ,  신계정 ,  변성림 ,  이관순 ,  김맹섭 ,  안영길 ,  묵인희

IPC: C07D213/34 ,  C07D213/26 ,  C07D213/30

CPC classification number: C07D213/38 ,  C07D213/30

Abstract: An inhibitory compound for formation of beta-amyloid fibril is provided to inhibit formation of senile plaque caused by beta-amyloid by specifically recognizing beta-amyloid without cytotoxicity and improve brain blood barrier(BBB) permeability, so that the compound is useful for treatment of degenerative brain disease containing dementia. A compound for inhibiting formation of beta-amyloid fibril represented by the formula(1) is prepared by performing Honer-Emmons reaction of compounds represented by the formula(2) with aldehyde compounds represented by the formula(3) and base such as metal hydrogen compound, metal alkoxide, alkyl alkali metal compound or amide type alkali metal compound in an organic solvent, wherein X is N or C; R^1 is H, halogen, C1-C3 alkyl, C1-C3 alkoxy or C1-C3 alkylamino group; and R^2 and R^3 are each independently OH, p-methoxybenzyloxy(OPMB), C1-C3 alkoxy, NO2, NH2, C1-C3 alkyl amino or di C1-C3 alkyl amino. Further, the organic solvent is an ether typed organic solvent.

Abstract translation: 提供用于形成β-淀粉样蛋白原纤维的抑制化合物，以通过特异性识别β-淀粉样蛋白而不具有细胞毒性并改善脑血管屏障（BBB）通透性，从而抑制由β-淀粉样蛋白引起的老年斑的形成，使得该化合物可用于治疗 退行性脑病包含痴呆症。 由式（1）表示的抑制β-淀粉样蛋白原纤维形成的化合物通过由式（2）表示的化合物与由式（3）表示的醛化合物和碱例如金属氢进行Hon-Emmons反应来制备 化合物，金属醇盐，烷基碱金属化合物或酰胺型碱金属化合物在有机溶剂中，其中X是N或C; R 1是H，卤素，C 1 -C 3烷基，C 1 -C 3烷氧基或C 1 -C 3烷基氨基; R 2和R 3各自独立地为OH，对甲氧基苄氧基（OPMB），C1-C3烷氧基，NO2，NH2，C1-C3烷基氨基或二C1-C3烷基氨基。 此外，有机溶剂是醚类有机溶剂。

公开(公告)号：KR1020060048259A

公开(公告)日：2006-05-18

申请号：KR1020050048832

申请日：2005-06-08

Applicant: 한국과학기술연구원

Inventor： 유경호 ,  김동진 ,  강용구 ,  이경석 ,  이관순 ,  김맹섭 ,  강재훈

IPC: C07D477/20

CPC classification number: C07D477/20

Abstract: 본 발명은 하기 화학식 1의 신규한 1-베타메틸카바페넴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조 방법 및 이를 포함하는 항균제용 조성물에 관한 것으로, 본 발명의 1-베타메틸카바페넴 유도체는 데하이드로펩티다제-I에 대해 안정하고 그람 양성균 및 그람 음성균 모두에 대해 우수한 항균활성을 나타내므로 항균제로서 매우 유용하다.

상기 식에서,
R은 수소 또는 나트륨이다.

公开(公告)号：KR100345465B1

公开(公告)日：2002-07-26

申请号：KR1020000038284

申请日：2000-07-05

Applicant: 한국과학기술연구원

Inventor： 김동진 ,  박상우 ,  신계정 ,  유경호 ,  강용구 ,  서경재

IPC: C07D477/10

Abstract: 본 발명은 항균제로 유용한 신규의 1-베타메틸카바페넴 유도체, 그를 포함하는 약학적 조성물 및 그의 제조방법에 관한 것으로서, 구체적으로 화학식 1로 표시되는 카바페넴 모핵의 2번 위치에 주요 관능기로서 5-(2'-이소옥사졸릴에텐닐)피롤리딘-3-티오기 또는 5-(2'-이소티아졸릴에텐닐)피롤리딘-3-티오기가 치환된 1-베타메틸카바페넴 유도체, 그를 포함하는 약학적 조성물 및 그의 제조방법에 관한 것이며, 본 발명에 의한 1-베타메틸카바페넴 유도체는 디하이드로펩티다제-I에 대해 안정하고 그람양성균 및 그람음성균 모두에 대해 우수한 항균 활성을 보이는 유용한 항균제이다.

상기 화학식 1에서, R은 명세서에 기재된 바와 같다.

公开(公告)号：KR1020020005334A

公开(公告)日：2002-01-17

申请号：KR1020000039375

申请日：2000-07-10

Applicant: 한국과학기술연구원

Inventor： 김동진 ,  박상우 ,  신계정 ,  유경호 ,  강용구

IPC: C07D477/10

Abstract: PURPOSE: Provided is a novel 1-β- methylcarbapenem derivative which has an antibacterial effect on both gram negative and positive bacteria and stability to dihydropeptidase-I, and is thus useful as antibacterial agent. And a pharmaceutical composition containing it and its manufacturing method are also provided. CONSTITUTION: The novel 1-β- methylcarbapenem derivative is represented by the formula(I), wherein R is described as in the description, X is ethoxycarbonyl group or hydroxymethyl group; Y is hydroxymethyl group or ethoxycarbonyl group; and Z is methyl group or carbamoylmethyl group. Its manufacturing method comprises the steps of: reacting enolphosphate with thiol derivative in the presence of base, in appropriate solvent to prepare protected carbapenem derivative; and deprotecting the protected carbapenem derivative to obtain 1-β- methylcarbapenem derivative.

Abstract translation: 目的：提供一种新型的1-β-甲基碳青霉烯衍生物，对革兰阴性和阳性细菌具有抗菌作用，对二氢肽酶-I具有稳定性，因此可用作抗菌剂。 还提供含有它的药物组合物及其制备方法。 构成：新颖的1-β-甲基碳青霉烯衍生物由式（I）表示，其中R如描述中所述，X是乙氧基羰基或羟甲基; Y是羟甲基或乙氧基羰基; Z为甲基或氨基甲酰基甲基。 其制造方法包括以下步骤：在碱的存在下，在合适的溶剂中使烯醇化磷酸酯与硫醇衍生物反应，制备保护的碳青霉烯衍生物; 并将保护的碳青霉烯衍生物脱保护得到1-β-甲基碳青霉烯衍生物。