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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
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。
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公开(公告)号：KR1020070119422A
公开(公告)日：2007-12-20
申请号：KR1020060054040
申请日：2006-06-15
Abstract: A method for preparing a novel D-erythro-2-deoxy-2,2-difluoro-1-oxoribose compound is provided to synthesize the compound with high purity and high yield selectively, which is able to be used as an intermediate for preparing beta-2,2-difluoro nucleoside. A D-erythro-2-deoxy-2,2-difluoro-1-oxoribose compound is represented by the formula(1), wherein R1 is piperonyloyl, 2,3-dimethoxybenzoyl or 2,4-dimethoxybenzoyl; and R2 is benzoyl, biphenylcarbonyl, naphthoyl, benzyloxycarbonyl, para-methoxy benzyloxycarbonyl, or para-nitrobenzyloxycarbonyl substituted by a substituent selected from the group consisting of acetyl, monochloroacetyl, dichloroacetyl, pivaloyl, nitro, methyl, trifluoromethyl, chloro, fluoro, hydroxy and methoxy. A method for preparing the compound of the formula(1) comprises the steps of: reacting a compound represented by the formula(4) with piperonyloyl, 2,3-dimethoxybenzoyl or 2,4-dimethoxybenzoyl compound to prepare a compound represented by the formula(3); reacting the compound of the formula(3) with an acid to prepare a compound represented by the formula(2); and protecting 5-hydroxy of the compound of the formula(2). In the formulae(2) to (4), R is the same as defined above.
Abstract translation: 提供了一种制备新型D-赤式-2-脱氧-2,2-二氟-1-氧代核糖化合物的方法，可以选择性地合成具有高纯度和高产率的化合物，其能够用作制备β的中间体 -2,2-二氟核苷。 D-赤式-2-脱氧-2,2-二氟-1-氧代核糖化合物由式（1）表示，其中R 1是哌嗪基，2,3-二甲氧基苯甲酰基或2,4-二甲氧基苯甲酰基; R2是由选自乙酰基，一氯乙酰基，二氯乙酰基，新戊酰基，硝基，甲基，三氟甲基，氯，氟，羟基的取代基取代的苯甲酰基，联苯基羰基，萘甲酰基，苄氧基羰基，对甲氧基苄氧基羰基或对硝基苄氧基羰基。 甲氧基。 制备式（1）化合物的方法包括以下步骤：使式（4）表示的化合物与哌嗪基，2,3-二甲氧基苯甲酰或2,4-二甲氧基苯甲酰化合物反应，制备式 （3）; 使式（3）的化合物与酸反应以制备由式（2）表示的化合物; 并保护式（2）化合物的5-羟基。 式（2）〜（4）中，R与上述相同。
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公开(公告)号：KR100428703B1
公开(公告)日：2004-04-30
申请号：KR1020000005140
申请日：2000-02-02
Applicant: 한국과학기술연구원
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：提供一种对幽门螺杆菌生长具有抑制活性的新型大环内酯化合物，其不易被胃酸分解。 构成：大环内酯类化合物由式（1）表示，其中R1为氢，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一起或独立地形成氧代-OR 4和氢，其中R 4是氢。 它对幽门螺杆菌的生长具有抑制活性，引起多种胃病。
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公开(公告)号：KR100377787B1
公开(公告)日：2003-03-26
申请号：KR1020000086254
申请日：2000-12-29
IPC: C07D471/04
Abstract: PURPOSE: Provided are novel pyridopyrimidine derivatives which inhibit phosphodiesterase IV activity and TNF production. Also, provided are preparing process thereof and a pharmaceutical composition containing the same. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkyl amino, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl; R is hydrogen, methyl, C3-7 lower alkyloxy, phenyl, benzyl, substituted phenyl(wherein a substituent group includes cyano, halogen, carboxylalkyl, nitro, methyl, trihalogenated ethyl or alkyloxy; and substitution site can be ortho-, meta-, or para- site), alkyloxy, C3-7 lower alkyloxy ethyl, benzyloxy, benzyloxyethyl, phenyloxyethyl, carboxyalkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.
Abstract translation: 目的：提供抑制磷酸二酯酶IV活性和TNF产生的新型吡啶并嘧啶衍生物。 另外，提供了其制备方法和含有其的药物组合物。 构成：新的吡啶并嘧啶衍生物由式（1）表示，其中R1为C1-3低级烷基，C3-7环烷基，环烷氧基，环烷基氨基，环烷基低级烷基，C1-3低级烷氧基，甲酰基，羟基低级烷基或 羧基; （其中取代基包括氰基，卤素，羧基烷基，硝基，甲基，三卤代乙基或烷氧基;取代位置可以是邻位，间位， 烷氧基，C 3-7低级烷氧基乙基，苄氧基，苄氧基乙基，苯氧基乙基，羧基烷基或氰基; 并且R4是氢或甲基，条件是R2和R3不相同。
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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
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。
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Patent Agency Ranking
公开(公告)号：KR1020200142215A
公开(公告)日：2020-12-22
申请号：KR1020190069154
申请日：2019-06-12
Applicant: 한국과학기술연구원
IPC: C07D471/04 , C07F5/02 , G01N33/533 , G01N33/68 , C09K11/06
Abstract: 본발명은타우응집체에높은선택성을가지는화합물및 이의제조방법, 상기화합물을포함하는타우표적형광탐침자, 상기형광탐침자를유효성분으로포함하는타우섬유단백질검출용조성물, 및상기조성물의타우병증진단용도에관한것이다. 특히, 본발명의화합물은아밀로이드베타단백질에는결합하지않고, 특이적으로타우병증의초기상태의병인으로보고된타우응집체에높은선택성을가지므로, 알츠하이머병을포함한타우병증의조기진단을위한타우섬유단백질검출용형광탐지자로서유용하게활용될수 있다.
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公开(公告)号：KR101851323B1
公开(公告)日：2018-04-23
申请号：KR1020160055552
申请日：2016-05-04
Abstract: 본발명은향오일점착제조성물및 그제조방법에관한것이다. 본발명의일 실시예에따른향오일점착제조성물제조방법은. (a) 키토산(Chitosan) 고분자를포함하는고분자수용액을제조하는단계(S10), (b) 고분자수용액에향오일(Fragrance Oil)을혼합하여향오일에멀젼을제조하는단계(S20), 및 (c) 상기향오일에멀젼을아크릴계점착제와혼합하는단계(S30)를포함한다.
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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
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.
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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
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
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20.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
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。
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