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    항진균 활성을 갖는 트라이아졸 유도체, 이의 제조방법 및 이를 함유하는 약학 조성물
    51.
    发明公开
    항진균 활성을 갖는 트라이아졸 유도체, 이의 제조방법 및 이를 함유하는 약학 조성물 无效
    具有抗真菌活性的三唑衍生物，其制备方法和含有其的药物组合物

    公开(公告)号：KR1020090007675A

    公开(公告)日：2009-01-20

    申请号：KR1020080137288

    申请日：2008-12-30

    Applicant: 한국화학연구원 ,  주식회사 켐온

    Inventor： 김범태 ,  민용기 ,  허정녕 ,  이혁 ,  장성연 ,  박노균 ,  송시환 ,  오정자

    IPC: C07D401/14 ,  C07D417/14 ,  C07D413/14 ,  C07D513/04

    Abstract: A pharmaceutical composition comprising the triazole derivative having antifungal activity is provided to inhibit growth of various pathogenic bacteria, and reduce the toxicity compared to the conventional antifungal agent, thereby treating infection of fungus. The triazole derivative represented by the chemical formula(1) or pharmaceutically acceptable salts thereof have excellent antifungal activity, wherein n is 1 or 2; A indicates direct bonding or C=O; D is CH or N; Z is O or S; R2 is hydrogen, halogen, hydroxy, cyano, nitro, amino, hydroxy carbonyl, C1-6 alkyl, C2-6 alkenyl, C2-6 akynyl, C1-6 acyl, C1-6 acyloxy, heteroaryl-C1-6 alkyl amino or N-C1-6 alkyl N- heteroaryl-C1-6 alkyl amino; and R3 is phenyl and monocyclic heteroaryl, and is replaced by one radical selected from the group consisting of hydrogen, halogen, hydroxy, cyano, nitro, amino, hydroxy carbonyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, hydroxy C1-6 alkyl, C1-6 alkoxy C1-6 alkyl, perfluoro C1-6 alkyl and perfluoro C1-6 alkoxy.

    Abstract translation: 提供包含具有抗真菌活性的三唑衍生物的药物组合物，以抑制各种致病细菌的生长，并降低与常规抗真菌剂相比的毒性，从而治疗真菌的感染。 由化学式（1）表示的三唑衍生物或其药学上可接受的盐具有优异的抗真菌活性，其中n为1或2; A表示直接键合或C = O; D是CH或N; Z是O或S; R 2是氢，卤素，羟基，氰基，硝基，氨基，羟基羰基，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 1-6酰基，C 1-6酰氧基，杂芳基-C 1-6烷基氨基或 N-C 1-6烷基N-杂芳基-C 1-6烷基氨基; 并且R 3是苯基和单环杂芳基，并被一个选自氢，卤素，羟基，氰基，硝基，氨基，羟基羰基，C 1-6烷基，C 2-6烯基，C 2-6炔基， C 1-6烷氧基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，全氟C 1-6烷基和全氟C 1-6烷氧基。

    β-아미노알콜 유도체를 포함하는 ＴＮＦ-α 매개성 질환의예방 또는 치료용 약학 조성물
    53.
    发明公开
    β-아미노알콜 유도체를 포함하는 ＴＮＦ-α 매개성 질환의예방 또는 치료용 약학 조성물 失效
    包含用于预防或治疗TNF-α的β型 - 氨基醇衍生物的药物组合物; 媒介疾病

    公开(公告)号：KR1020080048193A

    公开(公告)日：2008-06-02

    申请号：KR1020060118230

    申请日：2006-11-28

    Applicant: 한국화학연구원 ,  주식회사 오스코텍

    Inventor： 김범태 ,  민용기 ,  이혁 ,  허정녕 ,  장성연 ,  박노균 ,  이우길 ,  김성환 ,  김정근 ,  김세원 ,  고선일 ,  장순화

    IPC: A61K31/045 ,  A61P35/00

    CPC classification number: Y02A50/411

    Abstract: A beta-amino alcohol derivative is provided to show excellent TNF-alpha(tumor necrosis factor-alpha) inhibitory activity, thereby being used for a pharmaceutical composition for preventing or treating TNF-alpha mediated diseases. A composition for inhibiting TNF-alpha comprises a beta-amino alcohol derivative represented by a formula(1) or a pharmaceutically acceptable salt thereof as an active ingredient. In the formula(1), R^1 is phenyl substituted or unsubstituted by halogen; R^2 is pyridinyl, pyrimidinyl, indolyl or quinolyl substituted or unsubstituted by cyano or halogen; and R^3 is H or C1-4 alkyl. A pharmaceutical composition for preventing or treating TNF-alpha mediated diseases comprises the beta-amino alcohol derivative of the formula(1) or the pharmaceutically acceptable salt thereof.

    Abstract translation: 提供β-氨基醇衍生物以显示优异的TNF-α（肿瘤坏死因子-α）抑制活性，从而用于预防或治疗TNF-α介导的疾病的药物组合物。 用于抑制TNF-α的组合物包含由式（1）表示的β-氨基醇衍生物或其药学上可接受的盐作为活性成分。 在式（1）中，R 1是被卤素取代或未取代的苯基; R 2是被氰基或卤素取代或未取代的吡啶基，嘧啶基，吲哚基或喹啉基; R 3为H或C 1-4烷基。 用于预防或治疗TNF-α介导的疾病的药物组合物包含式（1）的β-氨基醇衍生物或其药学上可接受的盐。

    광학활성 α-플루오로메틸 프로파길 알콜 유도체의제조방법
    54.
    发明公开
    광학활성 α-플루오로메틸 프로파길 알콜 유도체의제조방법 失效
    制备丙烯酸甲酯衍生物丙酸衍生物的方法

    公开(公告)号：KR1020080019345A

    公开(公告)日：2008-03-04

    申请号：KR1020060081510

    申请日：2006-08-28

    Applicant: 한국화학연구원

    Inventor： 이혁 ,  김범태 ,  민용기 ,  허정녕 ,  박노균 ,  이우길 ,  김성환 ,  전난영 ,  고성진

    IPC: C12P41/00

    Abstract: A method for preparing a chiral alpha-fluoromethyl propargyl alcohol derivative is provided to obtain the desired product with maximum 99% optical purity easily from a racemic raw material compound. A method for preparing a compound represented by the formula(1) comprises the steps of: (a) reacting the compound of the formula(1) with vinyl alkanoate represented by the formula(1) for a stereoselective esterification at room temperature to 60 deg.C in an organic solvent such as diethyl ether, CH2Cl2, hexane, toluene, and a mixture thereof in the presence of a lipase catalyst derived from Candida antarctica or Mucor miehei to obtain a (-)-compound of the formula(1) and an ester derivative represented by the formula(3); and (b) after isolating the (-)-compound of the formula(1) and the ester derivative of the formula(3), hydrolyzing the ester derivative of the formula(1) to obtain a (+)-compound of the formula(1). In the formulae, R^1 is CF3, CF2BR or CF2Cl; R^2 is phenyl, cyclohexyl, n-hexyl, n-butyl or n-propyl; and R^3 is methyl, ethyl or n-propyl.

    Abstract translation: 提供了制备手性α-氟甲基炔丙醇衍生物的方法，以从外消旋原料化合物中容易地获得具有最大99％光学纯度的所需产物。 制备由式（1）表示的化合物的方法包括以下步骤：（a）使式（1）的化合物与由式（1）表示的链烷酸乙烯酯在室温至60℃下进行立体选择性酯化反应 在有机溶剂如乙醚，CH 2 Cl 2，己烷，甲苯及其混合物中，在衍生自南极假丝酵母（Candida Antarctica）或米色木霉（Mucor miehei）的脂肪酶催化剂的存在下，得到式（1）的（ - ） - 化合物和 由式（3）表示的酯衍生物; 和（b）在分离式（1）的（ - ） - 化合物和式（3）的酯衍生物之后，水解式（1）的酯衍生物，得到式（I）化合物 （1）。 在式中，R 1是CF 3，CF 2 BR或CF 2 Cl; R 2是苯基，环己基，正己基，正丁基或正丙基; 乙基或正丙基。

    리파제를 이용한 라세믹 2-히드록시-1-아릴프로파논유도체로부터 알-2-아실옥시-1-아릴프로파논 및에스-2-히드록시-1-아릴프로파논 유도체의 제조방법
    55.
    发明授权
    리파제를 이용한 라세믹 2-히드록시-1-아릴프로파논유도체로부터 알-2-아실옥시-1-아릴프로파논 및에스-2-히드록시-1-아릴프로파논 유도체의 제조방법 失效
    리파제를이용한라세믹2-록드록시-1-아릴프로파논유도체알-2-아실옥시-1아릴프로파논및에스-2-록드록시-1아릴프로파논유도체의제조방

    公开(公告)号：KR100688905B1

    公开(公告)日：2007-03-02

    申请号：KR1020050080097

    申请日：2005-08-30

    Applicant: 한국화학연구원

    Inventor： 김범태 ,  이연수 ,  민용기 ,  허정녕 ,  이혁 ,  박노균

    IPC: C07C45/61 ,  C12P41/00

    Abstract: Provided is a process for preparing R-2-acyloxy-1-arylpropane derivative and S-2-hydroxy-1-arylpropanone derivative having a high optical purity from a racemic 2-hydroxy-1-arylpropanone derivative with a high yield in an industrial scale. The process for preparing an S-2-hydroxy-1-arylpropanone derivative represented by a formula 2 and an R-2-acyloxy-1-arylpropane derivative represented by a formula 3 comprises a step of acylating a racemic 2-hydroxy-1-arylpropanone represented by a formula 1 in the presence of a lipase catalyst derived from candida antartica by using an acyl donating agent. In formulae 1-3, X is H or Cln, Brn, Fn, acyl, alkyl, nitro or a combination thereof (n is 1 or 2); and R is a C1-C10 saturated or unsaturated alkyl group.

    Abstract translation: 本发明提供一种在工业上高收率地由外消旋​​体2-羟基-1-芳基丙酮衍生物制造R-2-酰氧基-1-芳基丙烷衍生物和具有高光学纯度的S-2-羟基-1-芳基丙酮衍生物的方法 规模。 制备由式2表示的S-2-羟基-1-芳基丙酮衍生物和由式3表示的R-2-酰氧基-1-芳基丙烷衍生物的方法包括将外消旋2-羟基-1-芳基丙酮衍生物 在衍生自南极假丝酵母的脂肪酶催化剂存在下，通过使用酰基供体试剂，由式1表示的1-芳基丙酮。 在式1-3中，X是H或Cln，Brn，Fn，酰基，烷基，硝基或它们的组合（n是1或2）。 R是C1-C10饱和或不饱和烷基。

    신규한 헤테로고리 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
    58.
    发明公开
    신규한 헤테로고리 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 审中-实审
    一种新的杂环化合物，其制备方法，以及含有该化合物作为活性成分的用于预防或治疗癌症的药物组合物

    公开(公告)号：KR1020170120521A

    公开(公告)日：2017-10-31

    申请号：KR1020170051186

    申请日：2017-04-20

    Applicant: 한국화학연구원

    Inventor： 박성준 ,  허정녕 ,  김광록 ,  김성수 ,  임환정 ,  이혁 ,  장성연 ,  김범태 ,  윤은영 ,  임병호

    IPC: C07D403/06 ,  A61K31/506 ,  A61K31/404 ,  A23L33/10

    CPC classification number: A23L33/10 ,  A61K31/404 ,  A61K31/506 ,  C07D403/06

    Abstract: 본발명은신규한헤테로고리화합물, 이의제조방법및 이를유효성분으로함유하는 NAE(NEDD8-Activating Enzyme) 또는 SAE(Sumo Activating Enzyme) 관련질환의예방또는치료용약학적조성물에관한것으로, 본발명에따른헤테로고리화합물은 NAE(NEDD8-Activating Enzyme) 또는 SAE(Sumo Activating Enzyme)를나노몰단위의농도로우수하게저해할수 있어, 이를유효성분으로함유하는 NAE(NEDD8-Activating Enzyme) 또는 SAE(Sumo Activating Enzyme) 관련질환예를들어, 암의예방또는치료용약학적조성물로유용하게사용될수 있다.

    Abstract translation: 本发明涉及新的杂环化合物，其制备方法，和相关病症的预防和治疗药物的药物组合物的方法本NAE（NEDD8激活酶）或SAE（sumo活化酶）含有作为活性成分的，根据本发明 杂环化合物NAE（NEDD8激活酶）或SAE（sumo活化酶），用于它可以在纳摩尔单元的浓度极好的抑制作用，此NAE（NEDD8激活酶）含有作为活性成分或SAE（相扑活化酶 ）相关疾病，例如，作为用于预防或治疗癌症的药物组合物。

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