-
71.发明公开2-메틸-2'-하이드록시메틸-6-아미도벤조피란 유도체 또는 약제학적으로 허용 가능한 그의 염을 유효성분으로 함유하는 알레르기 질환 치료제 无效含有2-甲基-2'-羟基甲基-6-氨基苯并噻吩衍生物及其药学上可接受的盐的过敏性疾病的治疗
公开(公告)号：KR1020090022398A
公开(公告)日：2009-03-04
申请号：KR1020070087718
申请日：2007-08-30
Applicant: 한국화학연구원
IPC: A61K31/353 , A61P27/14
Abstract: A 2-methyl-2-hydroxymethyl-6-amido benzopyran derivative and its salt are promote Th1 differentiation with high activity in a T-bet promotor assay, thereby effectively curing bronchial asthma, atopic dermatitis, and allergic rhinitis. A 2-methyl-2-hydroxymethyl-6-amido benzopyran derivative is represented by the formula 1. In the formula 1, R1 indicates a C1-C5 alkyl group, benzyl or substituted benzyl group, phenethyl group, 2- pyrimidyl methyl group, thiophene group, 2-methyl thiophene methyl group, 5-methyl-2-thiophene methyl group, 3-thiophene methyl group, indolyl methyl group, naphthalene ylmethyl group, or a furanylmethyl group.
Abstract translation: 2-甲基-2-羟甲基-6-氨基苯并吡喃衍生物及其盐在T-bet启动子测定中促进Th1分化的高活性，从而有效地治愈了支气管哮喘，特应性皮炎和过敏性鼻炎。 2-甲基-2-羟甲基-6-氨基苯并吡喃衍生物由式1表示。在式1中，R1表示C1-C5烷基，苄基或取代苄基，苯乙基，2-嘧啶基甲基， 噻吩基，2-甲基噻吩甲基，5-甲基-2-噻吩甲基，3-噻吩甲基，吲哚基甲基，萘基甲基或呋喃基甲基。
-
72.发明授权염증억제 활성을 가지는Ｎ-[1'-치환술폰아미드-스파이로(2Ｈ-1-벤조피란-2,4-피페리딘)-6-일]치환아민 유도체, 그의 약학적으로허용가능한 염, 그의 제조방법 및 그의 용도 失效염증억제활성을가지는N- [1'-치환술폰아미드 - 스파이로（2H-1-벤조피란-2,4-피페리딘）-6-일]치환아민유도체，그의약학적으로허용가능한염， 그의제조방법및그의용도
公开(公告)号：KR100746939B1
公开(公告)日：2007-08-07
申请号：KR1020060073546
申请日：2006-08-04
Applicant: 한국화학연구원
IPC: C07D491/107 , A61K31/407 , A61P29/00
Abstract: N-[1'-substituted sulfonamide-spiro(2H-1-benzopyrane-2,4-piperidin)-6-yl]substituted amine derivatives, a process for preparation of the same compounds and use thereof are provided to inhibit 5-lipoxygenase and improve simplicity and yield of preparation, so that the compounds are useful for prevention and treatment of diseases caused by activation of leukotriens. The N-[1'-substituted sulfonamide-spiro(2H-1-benzopyrane-2,4-piperidin)-6-yl]substituted amine derivatives represented by the formula(1) and pharmaceutically acceptable salts thereof are provided, wherein R^1 is C1-C10 alkyl group, benzyl or substituted benzyl group, 2-pyrimidylmethyl group, thiophene group, 2-methylthiophenemethyl group, 5-methyl-2-thiophenemethyl group, indolylmethyl group, benzo dioxolanylmethyl group, naphthalenylmethyl group or furanylmethyl group; and R^2 is C1-C10 alkyl group, phenyl or substituted phenyl group, or hetero atom-containing 5- to 7-membered hetero ring and corresponding sulfonyl group.
Abstract translation: 提供了N- [1'-取代的磺酰胺 - 螺（2H-1-苯并吡喃-2,4-哌啶）-6-基]取代的胺衍生物，制备相同化合物的方法及其用途，以抑制5-脂氧合酶 并且提高制剂的简单性和收率，因此该化合物可用于预防和治疗由白三烯激活引起的疾病。 提供由式（1）表示的N- [1'-取代的磺酰胺 - 螺（2H-1-苯并吡喃-2,4-哌啶）-6-基]取代的胺衍生物及其药学上可接受的盐， 图1是C1-C10烷基，苄基或取代苄基，2-嘧啶甲基氧基，噻吩基，2- methylthiophenemethyl基，5-甲基-2- thiophenemethyl基，吲哚基，苯并二氧戊环基，萘基甲基氧基或呋喃基甲基; 和R ^ 2为C1-C10烷基，苯基或取代的苯基，或含杂原子的5至7元杂环和相应的磺酰基。
-
公开(公告)号：KR100524701B1
公开(公告)日：2005-10-31
申请号：KR1020030057713
申请日：2003-08-20
Applicant: 한국화학연구원
IPC: C07D239/54 , A61K31/505
Abstract: 본 발명은 5-이미노메틸기가 치환된 2,4-피리미딘다이온 유도체에 관한 것으로서, 더욱 상세하게는 2,4-피리미딘다이온 모핵의 C-5 위치에 다양한 이미노메틸기가 치환되어 있는 신규 화합물로서 수용체 티로신 키나제(RTK)로서의 상피세포 성장인자 수용체(EGFR)에 대한 우수한 억제활성을 나타내는 5-이미노메틸기가 치환된 2,4-피리미딘다이온 유도체에 관한 것이다.
상기 화학식 1에서, R
1 , R
2 , R
3 , R
4 및 R
5 는 각각 발명의 상세한 설명에서 정의한 바와 같다.-
公开(公告)号：KR100470958B1
公开(公告)日：2005-03-08
申请号：KR1020010084740
申请日：2001-12-26
Applicant: 한국화학연구원
IPC: C07D311/74 , C07D215/40
Abstract: 본 발명은 고체 지지체에 연결된 탄소-탄소 이중결합 화합물의 고효율 하이드로 알콕시 부가방법에 관한 것으로서, 더욱 상세하게는 메타-클로로과벤조산(
m -cpba)의 유기 산화제 존재하에서 고체 지지체에 연결된 탄소-탄소 이중결합 화합물에 하이드로 알콕시를 부가하는 반응을 수행함에 있어, 특정의 용매계와 유기 산화제 및 알코올을 한 반응용기에 투입하여 일용기반응(one-pot reaction)을 수행하여 목적하는 하이드로 알콕시 부가 생성물을 효과적으로 수득하도록 하는 고체 지지체에 연결된 탄소-탄소 이중결합 화합물의 고효율 하이드로알콕시 부가방법에 관한 것이다.
본 발명에 따른 방법은 분자내에 다양한 알콕시기 도입이 가능하고 인접하는 탄소에 하이드록시기가 있으면 에스테르, 에테르 등의 다양한 관능기의 도입으로 조합화학 합성기술을 이용한 선도물질 탐색에 유용한 다양한 분자합성에 유용하다.-
公开(公告)号：KR1020050020066A
公开(公告)日：2005-03-04
申请号：KR1020030057713
申请日：2003-08-20
Applicant: 한국화학연구원
IPC: C07D239/54 , A61K31/505
Abstract: PURPOSE: Derivatives of 5-(iminomethyl)-2,4-pyrimidinedione are provided, which derivatives have activity inhibiting EGFR(epidermal growth factor receptor), so that they can be useful for treatment of cancer. CONSTITUTION: The derivatives of 5-(iminomethyl)-2,4-pyrimidinedione represented by formula (1) are provided, wherein R1 and R2 are independently hydrogen, optionally substituted C1-C10 alkyl or C3-C6 cycloalkyl, or optionally substituted C7-C15 benzyl; R3 and R4 are independently hydrogen, allyl, optionally substituted C1-C10 alkyl or C3-C6 cycloalkyl, optionally substituted C7-C15 benzyl, optionally substituted C6-C15 aryl, optionally substituted C6-C15 hetero atom containing ring, optionally substituted C3-C20 acyl, optionally substituted C3-C20 amide, or optionally substituted C3-C20 thioamide; and R5 is optionally substituted C1-C20 alkyl or C3-C6 cycloalkyl, optionally substituted C7-C15 benzyl, optionally substituted C6-C15 aryl, optionally substituted C6-C15 hetero atom containing ring, optionally substituted C1-C10 alkoxy, optionally substituted C7-C15 benzyloxy, optionally substituted C1-C10 amine, or cyano, provided that the substituent of R1, R2, R3, R4 and R5 is selected from halogen atom, cyano, amide, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, alkylsulfone and arylsulfone, and a case that R3 and R4 are hydrogen simultaneously, and R5 is methyl, hydroxy, phenyl or phenylamine is excluded.
Abstract translation: 目的：提供5-（亚氨基甲基）-2,4-嘧啶二酮的衍生物，该衍生物具有抑制EGFR（表皮生长因子受体）的活性，因此可用于治疗癌症。 构成：提供由式（1）表示的5-（亚氨基甲基）-2,4-嘧啶二酮的衍生物，其中R1和R2独立地为氢，任选取代的C 1 -C 10烷基或C 3 -C 6环烷基，或任选取代的C7- C15苄基; R 3和R 4独立地是氢，烯丙基，任选取代的C 1 -C 10烷基或C 3 -C 6环烷基，任选取代的C 7 -C 15苄基，任选取代的C 6 -C 15芳基，任选取代的C 6 -C 15杂原子的环，任选取代的C 3 -C 20 酰基，任选取代的C 3 -C 20酰胺或任选取代的C 3 -C 20硫代酰胺; 并且R 5是任选取代的C 1 -C 20烷基或C 3 -C 6环烷基，任选取代的C 7 -C 15苄基，任选取代的C 6 -C 15芳基，任选取代的C 6 -C 15杂原子的环，任选取代的C 1 -C 10烷氧基， C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6卤代烷基， 烷氧基，C1-C6卤代烷氧基，C1-C6烷硫基，烷基砜和芳基砜，以及R3和R4同时为氢，R5为甲基，羟基，苯基或苯基胺的情况。
-
Patent Agency Ranking76.发明公开
公开(公告)号：KR1020040000320A
公开(公告)日：2004-01-03
申请号：KR1020030037668
申请日：2003-06-11
Applicant: 한국화학연구원
IPC: C07D311/22
Abstract: PURPOSE: Provided are 2,2-dimethyl-3-alkylether-4-alkoxy-6-alkyl amino benzopyran derivatives synthesized in higher yield by using parallel synthesis on the solid-phase. The synthesized derivatives inhibit lipid peroxidation. CONSTITUTION: 2,2-dimethyl-3-alkylether-4-alkoxy-6-alkyl amino benzopyran derivatives are characterized by the formula(5), wherein R1 and R2 are the same or different each other, and represent a C1-C10 alkyl group, a benzyl group or a substituted benzyl group, or a penethyl group; and R3 represents a C1-C10 alkyl group, a C2-C10 alkenyl group, a C2-C10 alkynyl group, a benzyl group or a substituted benzyl group, or a naphthylmethyl group; wherein the substituted benzyl group has 1-4 substituents selected from a halogen atom, a nitro group, C1-C10 alkyl group, C1-C10 alkoxy group and C1-C10 haloalkyl group.
Abstract translation: 目的：通过在固相上使用平行合成，提供以更高收率合成的2,2-二甲基-3-烷基醚-4-烷氧基-6-烷基氨基苯并吡喃衍生物。 合成的衍生物抑制脂质过氧化。 构成：2,2-二甲基-3-烷基醚-4-烷氧基-6-烷基氨基苯并吡喃衍生物的特征在于式（5），其中R 1和R 2相同或不同，表示C1-C10烷基 基团，苄基或取代的苄基，或苯乙基; R 3表示C1-C10烷基，C2-C10链烯基，C2-C10炔基，苄基或取代苄基或萘基甲基; 其中取代的苄基具有1-4个选自卤素原子，硝基，C 1 -C 10烷基，C 1 -C 10烷氧基和C 1 -C 10卤代烷基的取代基。
-
公开(公告)号：KR1020020005213A
公开(公告)日：2002-01-17
申请号：KR1020000035729
申请日：2000-06-27
Applicant: 한국화학연구원
Inventor： 공영대
IPC: C07F9/09
CPC classification number: C07F9/65031
Abstract: PURPOSE: Provided is a preparation method in making 3-trifluoromethyl-5-hydroxylpyrazole phosphoric acid ester derivatives using water as a solvent in place of organic solvent. Using water facilitates the easy separation of side products such as 3-trifluoromethyl-5-hydroxylpyrazole and halophosphate in the esterification reaction between derivatives of 3-trifluoromethyl-5-hydroxylpyrazole and halophosphate with catalysts such as dimethylaminopyridine and strong inorganic bases like hydroxides of alkali metal. The reaction process shortens the reaction time and offers high yield because the pure product is obtained by a simple extraction method. CONSTITUTION: The preparation method of the compound represented by the formula 1 comprises: adding 0.01 mole of 1-methyl-3-trifluoromethyl-5-hydroxylpyrazole and 0.02 mole of sodium hydroxide in 50mL of water; adding 0.01 mole of diethylchlorothiophosphate and 0.8 mmole of 4-dimethylaminopyridine to the above mixture; stirring the reactants at room temperature for 48 hours; and extracting the reaction mixture with 30mL of dichloromethane two times, drying the mixture with MgSO4 and evaporating the solvent to obtain the over 95% pure product, O,OO,O-diethyl-OO-(1-methyl-3-trifluoromethyl- 5-pyrazoyl)thiophosphoric ester in 88% yield. In the formula 1, R1 is hydrogen or halogen atom; R2 is straight or branched low alkyl group of C1-C6; R3 is C1-C6 low alkoxy, C1-C6 straight or branched low alkylthio, phenoxy or thiophenoxy group; R4 is hydrogen atom, C1-C6 straight or branched low alkyl, or substituted or unsubstituted phenyl group where the substituents are halogen atom, trifluoromethyl, or C1-C6 straight or branched low alkoxy group; and X is oxygen or sulfur atom.
Abstract translation: 目的：提供使用水作为溶剂代替有机溶剂的3-三氟甲基-5-羟基吡唑磷酸酯衍生物的制备方法。 使用水有助于在3-三氟甲基-5-羟基吡唑和卤代磷酸酯的衍生物与催化剂如二甲基氨基吡啶和强无机碱如碱金属的氢氧化物之间的酯化反应中容易地分离副产物如3-三氟甲基-5-羟基吡唑和卤代磷酸酯 。 反应过程缩短反应时间并提供高产率，因为纯产物通过简单的萃取方法获得。 构成：由式1表示的化合物的制备方法包括：在50mL水中加入0.01摩尔1-甲基-3-三氟甲基-5-羟基吡唑和0.02摩尔氢氧化钠; 向上述混合物中加入0.01摩尔氯代硫代磷酸二乙酯和0.8毫摩尔的4-二甲基氨基吡啶; 在室温下搅拌反应物48小时; 并用30mL二氯甲烷萃取反应混合物两次，用MgSO 4干燥混合物并蒸发溶剂，得到超过95％的纯产物，O，OO，O-二乙基-OO-（1-甲基-3-三氟甲基-5 - 吡唑基）硫代磷酸酯，收率88％。 在式1中，R 1是氢或卤素原子; R2是C1-C6的直链或支链低级烷基; R3是C1-C6低级烷氧基，C1-C6直链或支链低级烷硫基，苯氧基或硫代苯氧基; R4是氢原子，C1-C6直链或支链低级烷基或取代或未取代的苯基，其中取代基是卤素原子，三氟甲基或C 1 -C 6直链或支链低级烷氧基; X为氧或硫原子。
-
-
公开(公告)号：KR1020000077495A
公开(公告)日：2000-12-26
申请号：KR1020000041991
申请日：2000-07-21
Applicant: 한국화학연구원
IPC: A61L33/00
Abstract: PURPOSE: Quantitative analysis method of CCS products is provided which uses X-ray Photoelectron Spectroscopy(XPS) effectively to track the extent of progress of synthetic reaction in a solid support. CONSTITUTION: In the analysis method of products by CCS on the solid support, a CCS process wherein Wang resin halide is used as a solid support and processed through organic synthesis, peptide synthesis or carbohydrate synthesis is analyzed by XPS atomic spectroscopy quantitatively. The Wang resin are shown in a chemical formula 1 wherein P is polystyrene-divinyl benzene, X is selected from a halogen atom and n is an integer from 1 to 4 which indicates the number of substituted by halogen atom.
Abstract translation: 目的：提供CCS产品的定量分析方法，可以有效地利用X射线光电子能谱（XPS）来跟踪固体支持中合成反应进程的程度。 构成：在CCS对固体支持物的分析方法中，通过XPS原子光谱定量分析了王树脂卤化物用作固体支持物并通过有机合成，肽合成或碳水化合物合成进行处理的CCS方法。 Wang树脂以化学式1表示，其中P是聚苯乙烯 - 二乙烯基苯，X选自卤素原子，n是1至4的整数，表示被卤素原子取代的数目。
-
公开(公告)号：KR1020000055019A
公开(公告)日：2000-09-05
申请号：KR1019990003428
申请日：1999-02-02
Applicant: 한국화학연구원
IPC: C08G83/00
Abstract: PURPOSE: A resin containing vinyl ether that functions as a protecting group as well as a linker is provided. A method of combination chemical synthesis for hetero atom-containing compound derivatives is also provided. CONSTITUTION: A resin containing vinyl ether linker for use in organic reactions on a solid support according to the present invention has the formula (1): £formula 1| wherein P is polystyrene-divinylbenzene and n is an integer of 1 to 5. The resin according to the present invention is prepared by the method comprising the steps: a) reducing methyl(4-hydroxybenzyl)ester of the formula 2 to obtain 4-hydroxy phenethyl alcohol of the formula 3; b) reacting the compound of the formula 3 with ethylvinyl ether of the formula 4 to obtain 4-(2-vinyloxyethyl)phenol of the formula 5; and c) reacting the compound of the formula 5 with Merrifield resin of the formula 6 to obtain the resin containing vinyl ether linker: £formula 2-6| wherein P is polystyrene-divinylbenzene and n is an integer of 1 to 5.
Abstract translation: 目的：提供一种含乙烯基醚作为保护基的树脂以及连接体。 还提供了含杂原子的化合物衍生物的组合化学合成方法。 构成：根据本发明的用于固体支持物上的有机反应的含乙烯基醚接头的树脂具有式（1）：式1 | 其中P为聚苯乙烯 - 二乙烯基苯，n为1至5的整数。本发明的树脂通过包括以下步骤的方法制备：a）还原式2的（4-羟基苄基） 式3的羟基苯乙醇; b）使式3的化合物与式4的乙基乙烯基醚反应，得到式5的4-（2-乙烯氧基乙基）苯酚; 和c）使式5的化合物与式6的Merrifield树脂反应，得到含乙烯基醚接头的树脂： 其中P是聚苯乙烯 - 二乙烯基苯，n是1至5的整数。
-
-
-
-
-
-
-
-
-
Search Results
107
records
(took 0.03 seconds)
