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    Ｔ-형 칼슘 채널에 활성을 가지는 5각형의 헤테로방향족 화합물
    81.
    发明公开
    Ｔ-형 칼슘 채널에 활성을 가지는 5각형의 헤테로방향족 화합물 无效
    具有T型钙通道活性的新型五元杂环化合物

    公开(公告)号：KR1020120088398A

    公开(公告)日：2012-08-08

    申请号：KR1020110009730

    申请日：2011-01-31

    Applicant: 한국과학기술연구원

    Inventor： 배애님 ,  조용서 ,  추현아 ,  최경일 ,  김동진 ,  서선희 ,  임혜원 ,  최기현 ,  송치만 ,  김윤정 ,  임건승

    IPC: C07D413/06 ,  C07D413/12 ,  A61K31/496 ,  A61P9/00

    Abstract: PURPOSE: A pharmaceutical composition containing pentagonal heteroaromatic compound, a pharmaceutically acceptable salt thereof having a pharmaceutical activity to T-type calcium channel is provided to treat heart disease, brain diseases, stroma, chronic pain, neuropathic pain, and cancer. CONSTITUTION: A pentagonal heteroaromtaic compound with T-type calcium channel is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating stroma, hypertension, angina, chronic pain, neuropathic pain, and cancer contains the compound as an active ingredient. A method for preparing the compound comprises a step of binding carbochloride compound of chemical formula 3a and heterocyclic amine compounds of chemical formula 2a under the presence of an alkyl amine base.

    Abstract translation: 目的：提供含有对T型钙通道具有药学活性的五价杂芳族化合物及其药学上可接受的盐的药物组合物，用于治疗心脏病，脑疾病，基质，慢性疼痛，神经性疼痛和癌症。 构成：用化学式1表示具有T型钙通道的五价杂合化合物。用于预防和治疗基质，高血压，心绞痛，慢性疼痛，神经性疼痛和癌症的药物组合物含有该化合物作为活性成分。 制备该化合物的方法包括在烷基胺基的存在下结合化学式3a的氯化碳化合物和化学式2a的杂环胺化合物的步骤。

    Ｔ-형 칼슘 채널에 활성을 지닌 신규 옥사졸-피페라진 유도체 및 이의 제조방법
    84.
    发明公开
    Ｔ-형 칼슘 채널에 활성을 지닌 신규 옥사졸-피페라진 유도체 및 이의 제조방법 有权
    具有T型钙通道活性的新型奥氮唑 - 哌嗪化合物

    公开(公告)号：KR1020110020023A

    公开(公告)日：2011-03-02

    申请号：KR1020090077687

    申请日：2009-08-21

    Applicant: 한국과학기술연구원

    Inventor： 배애님 ,  추현아 ,  조용서 ,  이지은 ,  금교창 ,  최경일 ,  김동진 ,  신희섭 ,  임혜원 ,  정혜진 ,  서선희 ,  송치만

    IPC: C07D413/12 ,  C07D413/10

    Abstract: PURPOSE: An oxazole-piperazine compound having a pharmaceutical activity with respect to T-type calcium channel is provided to ensure excellent activity as an antagonist of the channel and to prevent and treat cancer, epilepsy, heart diseases, and pain. CONSTITUTION: An oxazole-piperazine compounds is denoted by chemical formula 1. A pharmaceutical composition for treating epilepsy, cancer, hypertension, myocardial infarction, neuropathic pain, and acute and chronic pain contains the oxazole-piperazine compound of chemical formula 1. The compound of chemical formula 1 is prepared by reacting piperazine-amine compound of chemical formula 2 and oxazole aldehyde compound of chemical formula 3 by reductive amination. The reductive amination is performed under the presence of molecules of 4-8 meshes and NaBH(OAc)_3, NaBH_3CN, or NaBH_4.

    Abstract translation: 目的：提供相对于T型钙通道具有药学活性的恶唑 - 哌嗪化合物，以确保作为通道拮抗剂的优异活性，并预防和治疗癌症，癫痫，心脏病和疼痛。 构成：化学式1表示恶唑 - 哌嗪化合物。用于治疗癫痫，癌症，高血压，心肌梗死，神经性疼痛和急性和慢性疼痛的药物组合物含有化学式1的恶唑 - 哌嗪化合物。 化学式1通过化学式2的哌嗪 - 胺化合物和化学式3的恶唑醛化合物通过还原胺化反应来制备。 还原胺化在4-8目和NaBH（OAc）3，NaBH 3 CN或NaBH 4的分子存在下进行。

    Ｔ-형 칼슘 채널에 활성을 지닌 신규 아이소인돌리논유도체 및 이의 제조방법
    85.
    发明公开
    Ｔ-형 칼슘 채널에 활성을 지닌 신규 아이소인돌리논유도체 및 이의 제조방법 无效
    具有T型钙通道活性的新型茚二酮衍生物

    公开(公告)号：KR1020100005476A

    公开(公告)日：2010-01-15

    申请号：KR1020080065522

    申请日：2008-07-07

    Applicant: 한국과학기술연구원

    Inventor： 조용서 ,  이재균 ,  오유나 ,  추현아 ,  배애님 ,  임혜원 ,  서선희

    IPC: C07D403/12

    CPC classification number: C07D401/12 ,  A61K31/454

    Abstract: PURPOSE: An isoindolinone derivative having pharmaceutical activation to T-type calcium channel is provided to have antagonistic activity to T-type calcium channel and use as a therapeutic agent for hypertension, cancer, and neurogenic pain. CONSTITUTION: An isoindolinone derivative is denoted by chemical formula 1. In chemical formula 1, R1 is hydrogen atom, halogen atom, alkoxy group of C1-C6, haloalkyl group of C1-C6, nitro group, cyano group, or hydroxyl group. R2 is hydrogen atom, alkyl group of C1-C6, or aryl group. The isoindolinone derivative is obtained by reacting piperidinyl propylamine derivative of chemical formula 9 with isoindolinone carboxylic acid derivative of chemical formula 8 through amide reaction. A pharmaceutical composition for treating hypertension, cancer, epilepsy, and neurogenic pain contains the isoindolinone derivative and its pharmaceutically acceptable salt.

    Abstract translation: 目的：提供具有T型钙通道药学活性的异吲哚啉酮衍生物，对T型钙通道具有拮抗作用，用作高血压，癌症和神经源性疼痛的治疗剂。 构成：异吲哚啉酮衍生物由化学式1表示。在化学式1中，R 1为氢原子，卤素原子，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，硝基，氰基或羟基。 R2是氢原子，C1-C6烷基或芳基。 异吲哚啉酮衍生物通过化学式9的哌啶基丙胺衍生物与化学式8的异吲哚酮羧酸衍生物反应而得到。 用于治疗高血压，癌症，癫痫和神经原性疼痛的药物组合物含有异吲哚啉酮衍生物及其药学上可接受的盐。

    세로토닌 ５―ＨＴ₃Ａ 길항적 효과를 갖는 퀴나졸린유도체 함유 약제 조성물
    88.
    发明授权
    세로토닌 ５―ＨＴ₃Ａ 길항적 효과를 갖는 퀴나졸린유도체 함유 약제 조성물 失效
    含有喹唑啉衍生物的药物组合物，用于治疗作为血清素受体拮抗剂

    公开(公告)号：KR100879636B1

    公开(公告)日：2009-01-21

    申请号：KR1020070084322

    申请日：2007-08-22

    Applicant: 한국과학기술연구원

    Inventor： 남길수 ,  임혜원 ,  배애님 ,  추현아 ,  최경일 ,  나승렬

    IPC: A61K31/517 ,  A61P25/00

    CPC classification number: A61K31/517 ,  A61K31/5377

    Abstract: A pharmaceutical composition for preventing and treating the disease related to the central nervous system, and a food composition are provided to obtain the effect on emesis, nausea, alcoholism, drugs abuse, depression, compulsion neurosis, anxiety, etc. A pharmaceutical composition for preventing and treating the disease related to the central nervous system comprises a quinoline derivative compound represented by the formula 1 or its pharmaceutically acceptable salt as an active ingredient, wherein R1 is H, a C1-C6 alkyl group, a phenyl group or a benzyl group; R2 is a heterocyclic group selected from morpholine, pyrrolidine and piperidine; the phenyl group or the benzyl group can be substituted with a substituent selected from a halogen atom, a C1-C6 alkyl group and a C1-C6 alkoxy group; and n is an integer of 1-6.

    Abstract translation: 提供了用于预防和治疗与中枢神经系统有关的疾病的药物组合物和食物组合物，以获得对呕吐，恶心，酒精中毒，药物滥用，抑郁，强迫性神经症，焦虑等的作用。 并且治疗与中枢神经系统相关的疾病包括由式1表示的喹啉衍生物化合物或其药学上可接受的盐作为活性成分，其中R1是H，C1-C6烷基，苯基或苄基; R2是选自吗啉，吡咯烷和哌啶的杂环基; 苯基或苄基可以被选自卤素原子，C1-C6烷基和C1-C6烷氧基的取代基取代; n为1-6的整数。

    두 고리형 테트라하이드로퓨란 화합물과 이의 제조방법
    89.
    发明授权
    두 고리형 테트라하이드로퓨란 화합물과 이의 제조방법 失效
    두고리형테트라하이드로퓨란화합물과이의제조방두

    公开(公告)号：KR100645371B1

    公开(公告)日：2006-11-14

    申请号：KR1020050061697

    申请日：2005-07-08

    Applicant: 한국과학기술연구원

    Inventor： 조용서 ,  배애님 ,  차주환 ,  고훈영 ,  신철

    IPC: C07D493/04

    Abstract: Novel bicyclic tetrahydrofuran derivatives, and a process for preparing the same compounds are provided to improve efficiency of preparation, so that they are useful as intermediates for synthesis of natural products. The bicyclic tetrahydrofuran derivatives represented by the formula(1) are provided, wherein n is 1 or 2; R is phenyl group or substituted phenyl group by C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group; and R1 is C1-C6 alkyl group. The bicyclic tetrahydrofuran derivatives represented by the formula(1) are prepared by intramolecular cyclizing tetrahydrofuran-allenol derivatives in the presence of alcohol compounds, transition metal catalyst and carbon monoxide(CO), wherein the transition metal catalyst is palladium chloride or copper chloride; and the reaction temperature is 0 to 25 deg.C.

    Abstract translation: 新型双环四氢呋喃衍生物及其制备方法可提高制备效率，因此它们可用作合成天然产物的中间体。 提供由式（1）表示的双环四氢呋喃衍生物，其中n是1或2; R 1为C 1 -C 6烷基，C 1 -C 6烷氧基，羟基或C 1 -C 6羟烷基的苯基或取代的苯基; 并且R 1是C 1 -C 6烷基。 由式（1）表示的双环四氢呋喃衍生物是在醇化合物，过渡金属催化剂和一氧化碳（CO）存在下通过分子内环化四氢呋喃 - 烯醇衍生物制备的，其中过渡金属催化剂为氯化钯或氯化铜; 反应温度为0〜25℃。

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