公开(公告)号：KR1019990029501A

公开(公告)日：1999-04-26

申请号：KR1019980036299

申请日：1998-09-03

Applicant: 한국과학기술연구원 ,  주식회사 일화

Inventor： 박상우 ,  김동진 ,  신계정 ,  강용구 ,  김용주 ,  정용호 ,  이홍우 ,  허재두 ,  이상주 ,  서일홍 ,  고봉석

IPC: C07D477/04 ,  C07D487/04

Abstract: 본 발명은 일반식(I)로 표시되는 신규한 카바페넴 유도체 및 이들의 제조 방법에 관한 것이다. 이의 제조는 일반식(II)로 표시되는 카바페넴 모핵을 염기 존재하에 디페닐클로로포스페이트 또는 무수 트리플루오로메탄술폰산과 반응시켜 일반식(VII)로 표시되는 카바페넴 중간체를 제조하고, 이를 일반식(III)으로 표시되는 티올 유도체와 반응시켜 일반식(I)의 카바페넴 유도체를 제조하는 것으로, 이는 유용한 항생제로 사용할 수 있다.

公开(公告)号：KR1020120066699A

公开(公告)日：2012-06-25

申请号：KR1020100093304

申请日：2010-09-27

Applicant: 한국과학기술연구원

Inventor： 노은주 ,  박정은 ,  지완근 ,  신계정 ,  배애님 ,  최경일 ,  김동진 ,  금교창

IPC: C07D295/033 ,  A61K31/495 ,  A61P25/08 ,  A61P9/12

Abstract: PURPOSE: A pharmaceutical composition containing a novel 1-(4-halophenyl oxo or thio)-3-(4-substituted piperazine-1-yl)propane-2-ol derivative is provided to effectively suppress T type calcium channel activation and to prevent or treat hypertension, cancer, epilepsy, and neurogenic pain. CONSTITUTION: A novel 1-(4-halophenyl oxo or thio)-3-(4-substituted piperazine-1-yl)propan-2-ol derivative is denoted by chemical formula 1. A method for preparing the compound of chemical formula 1 comprises: a step of reacting a compound of chemical formula 2 with chiral epichlorohydrin under the presence of a base and solvent to prepare an epoxy compound of chemical formula 3; and a step of reacting the epoxy compound of chemical formula 3 with piperazine derivative of chemical formula 4. The base is potassium carbonate, sodium carbonate or pyridine. A pharmaceutical composition for preventing or treating diseases caused by overactivation of T type calcium channel contains the derivative or pharmaceutically acceptable salt thereof as an active ingredient.

Abstract translation: 目的：提供含有新型1-（4-卤代苯基氧代或硫代）-3-（4-取代哌嗪-1-基）丙-2-醇衍生物的药物组合物，以有效抑制T型钙通道激活和预防 或治疗高血压，癌症，癫痫和神经源性疼痛。 构成：化学式1表示新的1-（4-卤代苯基氧代或硫代）-3-（4-取代哌嗪-1-基）丙-2-醇衍生物。一种制备化学式1化合物的方法 包括：在碱和溶剂的存在下使化学式2的化合物与手性表氯醇反应以制备化学式3的环氧化合物的步骤; 和使化学式3的环氧化合物与化学式4的哌嗪衍生物反应的步骤。碱是碳酸钾，碳酸钠或吡啶。 用于预防或治疗由T型钙通道过度活化引起的疾病的药物组合物含有其衍生物或药学上可接受的盐作为活性成分。

公开(公告)号：KR101052065B1

公开(公告)日：2011-07-27

申请号：KR1020080101249

申请日：2008-10-15

Applicant: 한국과학기술연구원

Inventor： 남길수 ,  최경일 ,  김혜란 ,  서선희 ,  백이연 ,  김윤지 ,  신희섭 ,  김동진 ,  배애님 ,  정혜진 ,  추현아 ,  임혜원 ,  조용서 ,  노은주 ,  금교창 ,  최기현 ,  신계정 ,  한호규 ,  정찬성 ,  이재균 ,  남기달 ,  강용구 ,  김영수 ,  박웅서 ,  김은경 ,  김기선 ,  정혜선 ,  신동윤 ,  송치만

IPC: C07D403/12 ,  C07D403/10

CPC classification number: C07D231/12 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12

Abstract: 본 발명은 칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체 및 이의 약제학적으로 허용 가능한 염, 이들 화합물의 제조방법, 그리고 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다.
피라졸릴메틸아민-피페라진 유도체, 칼슘이온 채널 조절제, 뉴런, 탈분극화, 급성통증, 만성통증, 신경병증성 통증, 고혈압치료제

Abstract translation: 本发明是有效的吡唑基甲胺作为钙离子通道调节剂 - 哌嗪衍生物和化学，以允许它的药学上可接受的盐，在疾病治疗由钙用于生产这些化合物和药物用于化合物工艺通道具有抑制作用 等等。

公开(公告)号：KR1020100042111A

公开(公告)日：2010-04-23

申请号：KR1020080101249

申请日：2008-10-15

Applicant: 한국과학기술연구원

Inventor： 남길수 ,  최경일 ,  김혜란 ,  서선희 ,  백이연 ,  김윤지 ,  신희섭 ,  김동진 ,  배애님 ,  정혜진 ,  추현아 ,  임혜원 ,  조용서 ,  노은주 ,  금교창 ,  최기현 ,  신계정 ,  한호규 ,  정찬성 ,  이재균 ,  남기달 ,  강용구 ,  김영수 ,  박웅서 ,  김은경 ,  김기선 ,  정혜선 ,  신동윤 ,  송치만

IPC: C07D403/12 ,  C07D403/10

CPC classification number: C07D231/12 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12

Abstract: PURPOSE: A pyrazolylmethylamine-piperazine derivative which is effective as a calcium ion channel modulator is provided to ensure effective activation as an T-type calcium ion channel antagonist and to use as an agent for preventing and treating brain diseases, heart diseases and pain diseases. CONSTITUTION: A pyrazolylmethylamine-peperazine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating brain diseases, heart diseases or pain diseases by T-type calcium ion channel antagonism contains the pyrazolylmethylamine-peperazine derivative of chemical formula 1 or its pharmaceutically acceptable salt an active ingredient. The brain disease is epilepsy, depression, Parkison's disease, dementia or somnipathy. The heart disease is hypertension, cardiac arrhythmia, myocardial infarction, or congestive failure. The pain disease is chronic pain, acute pain, or neurogenic pain. The pyrazolylmethylamine-peperazine derivative is prepared by binding pyrazolylmethylamine compound of chemical formula 3 with piperazine acetyl halide compound of chemical formula 2.

Abstract translation: 目的：提供作为钙离子通道调节剂有效的吡唑基甲胺 - 哌嗪衍生物，以确保作为T型钙离子通道拮抗剂的有效活化，并用作预防和治疗脑疾病，心脏病和疼痛疾病的药剂。 构成：吡唑基甲胺 - 哌嗪衍生物由化学式1表示。用于通过T型钙离子通道拮抗作用预防和治疗脑疾病，心脏病或疼痛疾病的药物组合物含有化学式1的吡唑基甲基 - 哌嗪衍生物或其药学上可接受的盐 可接受的盐为活性成分。 脑疾病是癫痫，抑郁症，帕金森病，痴呆或嗜睡。 心脏病是高血压，心律失常，心肌梗死或充血性衰竭。 疼痛疾病是慢性疼痛，急性疼痛或神经源性疼痛。 通过将化学式3的吡唑基甲基胺化合物与化学式2的哌嗪乙酰卤化合物结合，制备吡唑基甲胺 - 哌嗪衍生物。

公开(公告)号：KR1020090063869A

公开(公告)日：2009-06-18

申请号：KR1020070131388

申请日：2007-12-14

Applicant: 한국과학기술연구원 ,  재단법인서울대학교산학협력재단

Inventor： 신계정 ,  문지연 ,  배애님 ,  김은경 ,  서선희

IPC: C07D215/38 ,  C07D215/48 ,  C07D401/12 ,  A61K31/47

Abstract: An antibacterial composition containing a quinoline-carboxylic acid amide derivative or its pharmaceutically allowable salt is provided to suppress bacteria proliferation by inhibiting Fab I activation which is related to the last step of fatty acid biosynthesis. An antibacterial composition comprises a quinoline-carboxylic acid-amide derivative of the chemical formula 1 or its pharmaceutically allowable salt. A method for manufacturing the quinoline-carboxylic acid-amide derivative comprises: a step of reacting an aldehyde group of the chemical formula 2 with a phosphate, whose cyano group is substituted, to obtain a compound of the chemical formula 3; a step of performing intramolecular cyclization of the compound of the chemical formula 3 to obtain a quinoline compound of the chemical formula 4; a step of reacting the compound of the chemical formula 4 with a secondary amine to obtain a compound of the chemical formula 1(1a); and a step of reacting the compound of the chemical formula 1(1a) with an isocyanate to obtain the compound of the chemical formula 1.

Abstract translation: 提供含有喹啉羧酸酰胺衍生物或其药学上可允许的盐的抗菌组合物，通过抑制与脂肪酸生物合成的最后步骤相关的Fab I激活来抑制细菌增殖。 抗菌组合物包含化学式1的喹啉羧酸 - 酰胺衍生物或其药学上可允许的盐。 喹啉羧酸 - 酰胺衍生物的制造方法包括：使化学式2的醛基与氰基取代的磷酸酯反应，得到化学式3的化合物的工序; 化学式3的化合物进行分子内环化的步骤，得到化学式4的喹啉化合物; 使化学式4的化合物与仲胺反应以获得化学式1（1a）的化合物的步骤; 以及使化学式1（1a）的化合物与异氰酸酯反应以获得化学式1的化合物的步骤。

公开(公告)号：KR1020090044924A

公开(公告)日：2009-05-07

申请号：KR1020070111220

申请日：2007-11-01

Applicant: 한국과학기술연구원

Inventor： 최경일 ,  남길수 ,  황현숙 ,  임혜원 ,  서선희 ,  신희섭 ,  김동진 ,  한호규 ,  조용서 ,  배애님 ,  신계정 ,  강순방 ,  신동윤 ,  추현아 ,  노은주

IPC: C07D401/12 ,  C07D401/14

Abstract: 본 발명은 신규한 피라졸릴카르복스아미도알킬피페라진 유도체와 이의 제조방법 및 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다.
피라졸릴카르복스아미도알킬피페라진 유도체, 칼슘이온 채널 억제제, 뉴런, 틸분극화, 급성통증, 만성통증, 신경병증성 통증, 항암제, 고혈압치료제

Abstract translation: 本发明涉及一种药用根据新颖吡唑基 - 甲酰氨基烷基哌嗪衍生物及其制备方法和用这种化合物钙离子通道抑制作用在治疗疾病，其使用。

公开(公告)号：KR1020080035294A

公开(公告)日：2008-04-23

申请号：KR1020060101803

申请日：2006-10-19

Applicant: 한국과학기술연구원

Inventor： 신계정 ,  김동진 ,  황온유

IPC: A61K31/194 ,  A61P25/28

CPC classification number: A61K31/194

Abstract: A pharmaceutical composition comprising 1,2-di[2-methoxy-4-(2-carboxylvinyl)]phenoxyethane is provided to protect dopaminergic nerve cells from toxic materials including 1-methyl4-phenylpyridinum(MMP^+), tetrahydrobiopterin(BH4), hydrogen peroxide(H2O2), 1-methyl-4-phenyl-1,2,4,6-tetrahydropyridine, so that the composition is useful for prevention and treatment of Parkinson's disease. A pharmaceutical composition for prevention and treatment of Parkinson' s disease comprises 1,2-di[2-methoxy-4-(2-carboxylvinyl)]phenoxyethane represented by the formula(1) which is prepared by reacting hydroxybenzaldehyde represented by the formula(2) with ethyleneglycol detosylate represented by the formula(3) in the presence of base to prepare benzaldehyde dimmer represented by the formula(4); and reacting the benzaldehyde dimmer represented by the formula(4) with malonic acid at 80-100 deg. C for 2-6 hours, or its pharmaceutically acceptable salts.

Abstract translation: 提供了包含1,2-二[2-甲氧基-4-（2-羧基乙烯基）]苯氧基乙烷的药物组合物，以保护多巴胺能神经细胞免受毒性物质的影响，包括1-甲基-4-苯基吡啶（MMP ^ +），四氢生物喋呤（BH4） 过氧化氢（H 2 O 2），1-甲基-4-苯基-1,2,4,6-四氢吡啶，使得该组合物可用于预防和治疗帕金森病。 用于预防和治疗帕金森病的药物组合物包含由式（1）表示的1,2-二[2-甲氧基-4-（2-羧基乙烯基）]苯氧基乙烷，其通过使由式（1）表示的羟基苯甲醛 2）与由式（3）表示的乙二醇脱甲苯磺酸在碱存在下反应制备式（4）所示的苯甲醛二聚体; 并使由式（4）表示的苯甲醛二聚体与丙烯酸在80-100℃反应。 2-6小时，或其药学上可接受的盐。

公开(公告)号：KR1020080013162A

公开(公告)日：2008-02-13

申请号：KR1020060074298

申请日：2006-08-07

Applicant: 한국과학기술연구원

Inventor： 신계정 ,  오희숙

IPC: C07D311/24

Abstract: A preparing method of chromone-3-carboxyl acid derivatives is provided to improve preparation yield and reduce the preparation time by preparing various derivatives in each step through a series of reactions without purification by using parallel combinatorial chemistry in solution phase. A preparing method of chromone-3-carboxyl acid derivatives represented by the formula(1) comprises the steps of: o-acetylsalicylic acid chloride represented by the formula(2) with tertiary butoxycarbonylmethylene triphenylphosphorane represented by the formula(7) in the presence of catalyst to prepare phosphorane compound represented by the formula(3); deacetylating the phosphorane compound represented by the formula(3) in the presence of base to prepare compounds represented by the formula(4); reacting the compounds represented by the formula(4) with an excessive amount of acid chloride in the presence of base and catalyst to prepare compounds represented by the formula(5); preparing compounds represented by the formula(6) from the compounds represented by the formula(5) through Wittig reaction; and deesterifying the compounds represented by the formula(6) under acid condition to remove tertiary butyl group, wherein R1 is hydrogen, chlorine, bromine, methoxy group or methyl group, and R2 is aromatic group or hetero aromatic group substituted by chloride, fluorine, methoxy group, methyl group or hydroxy group.

Abstract translation: 提供了色酮-3-羧酸衍生物的制备方法，通过在溶液相中使用平行的组合化学反应，通过一系列反应制备各种衍生物，从而提高制备产率，缩短制备时间。 由式（1）表示的色酮-3-羧酸衍生物的制备方法包括以下步骤：由式（2）表示的邻乙酰基水杨酰氯与式（7）表示的叔丁氧羰基亚甲基三苯基正膦在存在下 催化剂制备由式（3）表示的正膦化合物; 在碱的存在下，使式（3）表示的正膦烷化合物脱乙酰化，制备式（4）表示的化合物。 在碱和催化剂的存在下使式（4）表示的化合物与过量的酰氯反应以制备由式（5）表示的化合物; 通过Wittig反应从式（5）表示的化合物制备由式（6）表示的化合物; 在酸性条件下使式（6）表示的化合物脱酯化以除去叔丁基，其中R 1是氢，氯，溴，甲氧基或甲基，R 2是被氯，氟， 甲氧基，甲基或羟基。

公开(公告)号：KR100327758B1

公开(公告)日：2002-09-09

申请号：KR1019980036299

申请日：1998-09-03

Applicant: 한국과학기술연구원 ,  주식회사 일화

Inventor： 박상우 ,  김동진 ,  신계정 ,  강용구 ,  김용주 ,  정용호 ,  이홍우 ,  허재두 ,  이상주 ,  서일홍 ,  고봉석

IPC: C07D477/04 ,  C07D487/04

Abstract: PURPOSE: Carbapenem derivatives and a preparation process thereof are provided, thereby preparing carbapenem derivatives having improved antimicrobial activity and renal dehydropeptidase I(DHP-I) stability. CONSTITUTION: Carbapenem derivatives represented by formula(I) are provided, wherein R1 and R2 are independently hydrogen, hydroxy substituted or unsubstituted C1 to C5 lower alkyl, or allyl, and form C3 to C6 heterocycle containing nitrogen and optionally hetero atoms of S or O together; and X is carbonyl or sulfonyl. A process for preparing the carbapenem derivatives of formula(I) comprises the steps of: reacting carbapenem scaffold of formula(II) with diphenylchloro phosphate or anhydrous trifluoromethane sulfonic acid in the presence of base and a solvent to prepare a carbapenem intermediate of formula(VII); reacting the carbapenem intermediate of formula(VII) with thiol derivative of formula(III) in the presence of base and a solvent to prepare a protected carbapenem derivative of formula(VIII); and hydrogenating the protected carbapenem derivative of formula(VIII) in the presence of a catalyst to remove a protecting group, wherein R3 is para-nitrobenzyl or allyl; R4 is para-nitrobenzyloxycarbonyl or allyoxycarbonyl; X is carbonyl or sulfonyl; and Y is -OPO(OPh)2 or -OSO2CF3.

公开(公告)号：KR100345468B1

公开(公告)日：2002-07-26

申请号：KR1020000039375

申请日：2000-07-10

Applicant: 한국과학기술연구원

Inventor： 김동진 ,  박상우 ,  신계정 ,  유경호 ,  강용구

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'-이소옥사졸로피롤리딘-3'-일티오기가 치환된 1-베타메틸카바페넴 유도체, 그를 포함하는 약학적 조성물 및 그의 제조방법에 관한 것이며, 본 발명에 의한 1-베타메틸카바페넴 유도체는 디히드로펩티다제-I에 대해 안정하고 그람양성균 및 그람음성균 모두에 대해 우수한 항균 활성을 보이는 유용한 항균제이다.

상기 화학식 1에서, R은 명세서에 기재된 바와 같다.