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    신규 1-베타메틸카바페넴 유도체 및 그의 제조방법
    31.
    发明公开
    신규 1-베타메틸카바페넴 유도체 및 그의 제조방법 失效
    新一代甲基胆碱衍生物及其制备方法

    公开(公告)号：KR1020020003789A

    公开(公告)日：2002-01-15

    申请号：KR1020000038284

    申请日：2000-07-05

    Applicant: 한국과학기술연구원

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

    IPC: C07D477/10

    CPC classification number: C07D477/20 ,  C07D413/06 ,  C07D417/06

    Abstract: PURPOSE: Provided are novel 1 β-Methylcarbapenem derivatives and their preparation process, which derivatives show stability to dihydropeptidase-I, and have antibacterial effects on both gram positive and gram negative bacteria. Thus, they are used as antibacterial agents. CONSTITUTION: Novel 1 β-Methylcarbapenem derivatives have substituted 5-(2-isoxazolyl ethenyl)pyrrolidine-3-thio or 5-(2-isothiazolyl ethenyl)pyrrolidine-3-thio group as a main functional group at 1-beta methylcarbapenem represented by the formula(1). A pharmaceutical composition for an antibacterial agent contains the 1 β-Methylcarbapenem derivatives, as active ingredients. In the formula(1), R is described as in the description and has cis- or trans stereomer, X is hydrogen, methoxycarbonyl, hydroxymethyl, methylaminomethyl, C1-C4 alkoxy or halogen atom, and Y is hydrogen or halogen atom.

    Abstract translation: 目的：提供新型1型β-甲基碳青霉烯衍生物及其制备方法，该衍生物显示对二氢肽酶-I的稳定性，对革兰氏阳性菌和革兰氏阴性菌均具有抗菌作用。 因此，它们被用作抗菌剂。 构成：新型1β-甲基碳青霉烯衍生物具有取代的5-（2-异恶唑基乙烯基）吡咯烷-3-硫基或5-（2-异噻唑基乙烯基）吡咯烷-3-硫基作为主要官能团，以1-β甲基碳青霉烯为代表 公式（1）。 作为抗菌剂的药物组合物含有作为活性成分的1β-甲基碳青霉烯衍生物。 在式（1）中，R如说明书所述，具有顺式或反式立体异构体，X为氢，甲氧基羰基，羟甲基，甲基氨基甲基，C1-C4烷氧基或卤原子，Y为氢或卤素原子。

    Ｔ형 칼슘 채널 저해작용을 가지는 신규 1-(4-할로페닐 옥소 또는 싸이오)-3-(4-치환피페라진-1-일)프로판-2올 유도체 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 하는 약학적 조성물
    33.
    发明公开
    Ｔ형 칼슘 채널 저해작용을 가지는 신규 1-(4-할로페닐 옥소 또는 싸이오)-3-(4-치환피페라진-1-일)프로판-2올 유도체 또는 이의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 하는 약학적 조성물 无效
    新型1-（4-戊烯基氧基或硫代）-3-（4-取代的哌嗪-1-基）丙烷-2-醇衍生物，其具有T型钙通道抑制活性或药物可接受的盐，其制备方法和药物组合物包含 同样作为活跃成分

    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。

    칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체와 이의 제조방법
    36.
    发明公开
    칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체와 이의 제조방법 失效
    新型吡咯烷基胺化合物作为钙通道调节剂及其制备方法

    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。

    1,2-디[2-메톡시-4-(2-카르복실비닐)]페녹시에탄 화합물을유효성분으로 함유하는 파킨슨병 예방 및 치료용 약학적조성물
    38.
    发明公开
    1,2-디[2-메톡시-4-(2-카르복실비닐)]페녹시에탄 화합물을유효성분으로 함유하는 파킨슨병 예방 및 치료용 약학적조성물 无效
    用于预防和治疗含有1,2-二[2-甲氧基-4-（2-羧基乙基）]苯氧基乙烷作为活性成分的帕金森病的药物组合物

    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。

    용액상 평행 조합화학을 이용한 크로몬-3-카복실산유도체의 제조방법
    39.
    发明公开
    용액상 평행 조합화학을 이용한 크로몬-3-카복실산유도체의 제조방법 无效
    在溶液相中使用平行组合化学制备氯酚-3-羧酸衍生物的制备方法

    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。

    카바페넴유도체및이의제조방법
    40.
    发明授权
    카바페넴유도체및이의제조방법 失效
    碳青霉烯衍生物及其制备方法

    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.

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