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    헬리코박터 파이로리의 성장 억제 효과를 지닌 신규 마크로라이드 화합물
    21.
    发明公开
    헬리코박터 파이로리의 성장 억제 효과를 지닌 신규 마크로라이드 화합물 失效
    具有抑制活性的新型马来酸化合物用于生长HELICOBACTER PYLORI

    公开(公告)号：KR1020010077376A

    公开(公告)日：2001-08-17

    申请号：KR1020000005140

    申请日：2000-02-02

    Applicant: 한국과학기술연구원

    Inventor： 김중협 ,  김성훈 ,  남길수 ,  서재홍

    IPC: C07D309/04

    Abstract: PURPOSE: A novel macrolide compound having an inhibiting activity for the growth of Helicobacter pylori is provided, which is not easily decomposed by gastric acid. CONSTITUTION: The macrolide compound is represented by formula (1), in which R1 is hydrogen, 4-methoxy phenoxy methyl, 2-methoxy phenoxy methyl or methoxy ethoxy methyl; R2 is hydrogen, acyl or lower alkoxy; R3 is the same or different and hydrogen or acyl; and Q and W form oxo together or independently -OR4 and hydrogen, wherein R4 is hydrogen. It has an inhibiting activity for the growth of Helicobacter pylori which causes several stomach diseases.

    Abstract translation: 目的：提供一种具有幽门螺杆菌生长抑制活性的新型大环内酯类化合物，不易被胃酸分解。 构成：大环内酯类化合物由式（1）表示，其中R1是氢，4-甲氧基苯氧基甲基，2-甲氧基苯氧基甲基或甲氧基乙氧基甲基; R2是氢，酰基或低级烷氧基; R3相同或不同，为氢或酰基; 并且Q和W一起或独立地代表-OR4和氢，其中R4是氢。 它对幽门螺杆菌的生长具有抑制作用，导致多种胃部疾病。

    세로토닌 5-ＨＴ6 저해 활성을 갖는 5,6,7,8-테트라하이드로퀴나졸린-2-아민 화합물
    24.
    发明授权
    세로토닌 5-ＨＴ6 저해 활성을 갖는 5,6,7,8-테트라하이드로퀴나졸린-2-아민 화합물 有权

    公开(公告)号：KR101730790B1

    公开(公告)日：2017-04-28

    申请号：KR1020150186413

    申请日：2015-12-24

    Applicant: 한국과학기술연구원

    Inventor： 남길수 ,  추현아 ,  최경일

    IPC: C07D239/84 ,  C07D239/72 ,  C07D239/78

    Abstract: 본발명은세로토닌서브타입중하나인 5-HT수용체에대하여저해활성을가지는신규 5,6,7,8-테트라하이드로퀴나졸린-2-아민화합물과상기화합물이포함된중추신경계 (CNC) 질환의예방또는치료용약제조성물또는중추신경계 (CNC) 질환의진단시약에관한것이다. 본발명의신규화합물은 5-HT수용체에대한결합력및 저해활성을가지므로알쯔하이머(AD), 주의력결핍증(ADHD), 간질, 우울증(depression), 비만, 정신분열증, 수면장애, 통증불안증과같은중추신경계(CNS, central nervous system) 질환의진단, 예방및 치료를목적으로유용하게사용될수 있다.

    메틸리덴-헤테로싸이클릭 화합물
    25.
    发明公开
    메틸리덴-헤테로싸이클릭 화합물 有权
    甲基 - 杂环化合物

    公开(公告)号：KR1020130010784A

    公开(公告)日：2013-01-29

    申请号：KR1020110071653

    申请日：2011-07-19

    Applicant: 한국과학기술연구원

    Inventor： 노은주 ,  신계정 ,  송혜승 ,  양정은 ,  김남윤 ,  배애님 ,  남길수 ,  추현아 ,  지완근

    IPC: C07D417/10 ,  C07D417/12 ,  C07D277/36 ,  A61K31/427

    Abstract: PURPOSE: A methylidene-heterocyclic compound and a pharmaceutical composition containing the same are provided to strongly suppress IkappaB kinase-b(IKK-b) and to treat various inflammatory diseases. CONSTITUTION: A methylidene-heterocyclic compound is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating inflammatory diseases contains the compound of chemical formula 1 as an active ingredient. The inflammatory diseases include rheumatoid arthritis, juvenile arthritis, asthma, spondyloarthopathies, gout, osteoarthritis, allergic rhinitis, atopic dermatitis, systemic lupuserythematosus, psoriasis, ulcerative colitis, SIRS, sepsis, or polymyositis. A method for preparing the compound of chemical formula 1 comprises: a step of cyclizing an aniline compound of chemical formula 2 and preparing a 3-phenyl rhodanine compound of chemical formula 3; and a step of condensing the compound of chemical formula 3 with aldehyde compound of R2-C(O)H under an acidic condition. [Reference numerals] (AA) Step 1; (BB) Step 2

    Abstract translation: 目的：提供亚甲基杂环化合物和含有它们的药物组合物以强烈抑制IkappaB激酶b（IKK-b）并治疗各种炎性疾病。 构成：亚甲基杂环化合物由化学式1表示。用于预防和治疗炎性疾病的药物组合物含有化学式1的化合物作为活性成分。 炎性疾病包括类风湿性关节炎，青少年关节炎，哮喘，脊椎动物病痛，痛风，骨关节炎，过敏性鼻炎，特应性皮炎，系统性红斑狼疮，牛皮癣，溃疡性结肠炎，SIRS，败血症或多发性肌炎。 制备化学式1的化合物的方法包括：使化学式2的苯胺化合物环化并制备化学式3的3-苯基绕丹宁化合物的步骤; 和在酸性条件下将化学式3的化合物与R2-C（O）H的醛化合物缩合的步骤。 （附图标记）（AA）步骤1; （BB）步骤2

    1,6-이치환-3-아미노-4,5,6,7-테트라하이드로-1Ｈ-피라졸로［3,4-ｃ］피리딘-7-온 화합물 및 이 화합물의 제조방법
    26.
    发明公开
    1,6-이치환-3-아미노-4,5,6,7-테트라하이드로-1Ｈ-피라졸로［3,4-ｃ］피리딘-7-온 화합물 및 이 화합물의 제조방법 有权
    新的1,6-二异丙基氨基-4,5,6,7-四氢-1H-吡唑并[3,4-C]吡啶-7-酮化合物及其制备方法

    公开(公告)号：KR1020110139988A

    公开(公告)日：2011-12-30

    申请号：KR1020100060138

    申请日：2010-06-24

    Applicant: 한국과학기술연구원

    Inventor： 남길수 ,  배애님 ,  최경일 ,  추현아 ,  와니 ,  서선희

    IPC: C07D471/04 ,  C07D403/02 ,  A61K31/437 ,  A61P35/00

    CPC classification number: C07D471/04

    Abstract: PURPOSE: A novel 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-7-one is provided to suppress cancer cells. CONSTITUTION: A 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-7-one compound is denoted by chemical formula 1. A pharmaceutical composition for anticancer contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A method for preparing the compound of chemical formula 1 comprises a step of alkylating 3-amino compounds of chemical formula 2 with haloalkylcarbonyl piperazine of chemical formula 3 by alkylating.

    Abstract translation: 目的：提供新颖的1,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮以抑制癌细胞。 构成：1,6-二取代-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-7-酮化合物由化学式1表示。用于抗癌的药物组合物含有化合物 的化学式1或其药学上可接受的盐作为活性成分。 制备化学式1的化合物的方法包括通过烷基化将化学式2的3-氨基化合物与化学式3的卤代烷基羰基哌嗪烷基化的步骤。

    신규한 세팔로스포린계 화합물 및 약제학적으로 허용되는염과 그의 제조 방법
    30.
    发明公开
    신규한 세팔로스포린계 화합물 및 약제학적으로 허용되는염과 그의 제조 방법 失效
    具有改善抗微生物活性，特别是耐甲氧西林金黄色葡萄球菌（MRSA）菌株及其药学上可接受的盐及其制备方法的CEPHOROSPORIN衍生物

    公开(公告)号：KR1020050001245A

    公开(公告)日：2005-01-06

    申请号：KR1020030042826

    申请日：2003-06-27

    Applicant: 영진약품 주식회사 ,  한국과학기술연구원

    Inventor： 김성규 ,  이정민 ,  전종옥 ,  손상권 ,  최경일 ,  김중협 ,  남길수

    IPC: C07D501/24

    CPC classification number: C07D501/00 ,  Y02P20/55

    Abstract: PURPOSE: Cephalosporin derivatives, its pharmaceutically acceptable salts and a manufacturing process thereof are provided, which cephalosporin derivatives have improved anti-microbial activity, particularly, for methicillin-resistant Staphylococcus aureus(MRSA) strain, so that they can be useful for antibiotics. CONSTITUTION: The cephalosporin derivatives represented by formula (I), or pharmaceutically acceptable salts thereof are provided, wherein X, Y and Z are the same or different, and independently hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 halogenoalkyl, C1-6 alkoxy alkyl or C3-6 cycloalkyl; R1 is an isoxazol compound in which the 3-site is substituted with a compound of formula (A), wherein Q is a substituent useful for cephalosporin-based compound, and is selected from hydrogen, halogen, hydroxyl, mercapto, cyano, carboxy, carboxylic acid, ester, carbamoyloxy, carbamoyl, N,N-dimethylcarbamoyl, C1-4 alkyl, C1-4 alkyloxy, halogen substituted alkyl, aryl or hetero ring substituent; and R2 is hydrogen, an ester-forming group as an ester of carboxy group, salt-forming atom or carboxy-protecting group. The process for preparing the cephalosporin derivatives represented by formula (I), or pharmaceutically acceptable salts thereof comprises reacting an ilide compound of formula (VI) with an aldehyde compound of formula (VII) in the presence of base and organic solvent at -40 to 25 deg. C.

    Abstract translation: 目的：提供头孢菌素衍生物及其药学上可接受的盐及其制备方法，其头孢菌素衍生物具有改善的抗微生物活性，特别是耐甲氧西林金黄色葡萄球菌（MRSA）菌株，因此它们可用于抗生素。 构成：提供由式（I）表示的头孢菌素衍生物或其药学上可接受的盐，其中X，Y和Z相同或不同，独立地是氢，卤素，C 1-6烷基，C 1-6烷氧基， 6卤代烷基，C 1-6烷氧基烷基或C 3-6环烷基; R1是其中3-位被式（A）化合物取代的异恶唑化合物，其中Q是可用于头孢菌素类化合物的取代基，并且选自氢，卤素，羟基，巯基，氰基，羧基， 羧酸，酯，氨基甲酰氧基，氨基甲酰基，N，N-二甲基氨基甲酰基，C 1-4烷基，C 1-4烷氧基，卤素取代的烷基，芳基或杂环取代基; 并且R 2是氢，作为羧基的酯形成基团，成盐原子或羧基保护基。 制备由式（I）表示的头孢菌素衍生物或其药学上可接受的盐的方法包括：在碱和有机溶剂的存在下，使式（VI）的铱化合物与式（Ⅶ）的醛化合物在-40至 25度 C。

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