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公开(公告)号：KR1019970003501B1
公开(公告)日：1997-03-18
申请号：KR1019920006546
申请日：1992-04-18
Applicant: 동화약품주식회사
IPC: C07D401/14
Abstract: This invention provides quinolone derivatives represented by the structural formula (I) wherein X is N or C-H. The derivatives are produced by reacting a fluorine-substituted quinolinecarbonic acid, 1-cycloprophyl-6,7,8- trifluoro-1,4-dihydro-4-oxo-3-quinolinecarbonic acid, with one of substituted piperazines, 1-(2,6-diaminoprymidine-4-yl)-piperazine and 1-(4,6-diamino-1,3,5-triazine-2-yl)-piperazine, in a polar solvent. These quinolone derivatives have high antimicrobial activity especially against gram-positive bacteria.
Abstract translation: 本发明提供由结构式（I）表示的喹诺酮衍生物，其中X为N或C-H。 衍生物通过氟取代的喹啉碳酸1-环丙基-6,7,8-三氟-1,4-二氢-4-氧代-3-喹啉碳酸与一个取代的哌嗪，1-（2 ，6-二氨基丙内酰胺-4-基） - 哌嗪和1-（4,6-二氨基-1,3,5-三嗪-2-基） - 哌嗪。 这些喹诺酮衍生物具有高抗微生物活性，特别是针对革兰氏阳性菌。
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公开(公告)号：KR1019960037643A
公开(公告)日：1996-11-19
申请号：KR1019950008856
申请日：1995-04-15
Applicant: 동화약품주식회사
IPC: C07C233/80
Abstract: 본 발명은 2-(4-시클로펜톡시벤조일아미노)벤즈아미드유도체에 관한 것으로 더욱 자세하게는 새로운 2-(4-시클로펜톡시벤조일아미노)벤즈 아미드 유도체 및 이들의 제조방법과 그것의 용도에 관한 것이다.
종래의 천연물성분인 멜란드린과 그의 에스테르유도체들은 진통작용이 다소약한 문제점이 있어 이러한 구조에 여러 작용기를 도입하여 진통 및 소염작용이 우수하고 독성과 위장장해등의 부작용이 거의 없는 약리학적 및 생리학적으로 탁월한 하기 구조식(Ⅰ)의 2-(4-시클로펜톡시벤조일아미노)벤즈아미드유도체 및 그 제조방법을 제공한다.
상기의 구조식(Ⅰ)의 화합물은 우수한 소염진통작용을 나타내는 화합물로 기존에 널리 쓰이고 있는 소염진통제들의 흔한 문제점인 위장장해등의 부작용과 독성이 거의 없는 안정성이 탁월한 화합물이다.-
公开(公告)号：KR1019960037642A
公开(公告)日：1996-11-19
申请号：KR1019950008823
申请日：1995-04-14
Applicant: 동화약품주식회사
IPC: C07C233/80
Abstract: 본 발명에 따르면, 하기 일반식(Ⅰ)로 표시되는 2-(4-알콕시벤조일아미노)벤즈아미드 유도체 및 그의 제조방법이 제공된다.
상기 식에서, R
1 은 수소, 탄소수 1-4의 히드록시 치환기를 가질 수 있는 저급 알킬기, 벤질기, 저급 아실기 또는 저급 알콕시카르보닐이고 ; R
2 , R
3 의 하나는 수소 원자, 다른 하나는 치환기를 가질 수도 있는 탄소수 1∼7의 직쇄 또는 분지쇄 알킬기 또는 고리형 알킬기, 또는 벤질기이거나 ; R
2 및 R
3 는 인접한 질소원자와 함께 헤테로고리를 형성할 수 있으며 ; R
4 는 탄소수 1∼4의 직쇄 또는 분지쇄 알킬기 또는 벤질기이다.
본 발명의 화합물은 소염 진통작용이 우수하고 독성과 위장장해 등의 부작용이 거의 없으므로 소염진통제로서 매우 유용하다.-
公开(公告)号：KR100420616B1
公开(公告)日：2004-05-17
申请号：KR1019960072384
申请日：1996-12-26
Applicant: 동화약품주식회사
IPC: C07D401/14
Abstract: PURPOSE: Terephthalic acid amide derivatives are provided, which have improved antiviral activity to hepatitis B virus and no toxicity, so that they can be useful for prevention and treatment of hepatitis B. CONSTITUTION: The terephthalic acid amide derivatives containing substituted phenylpiperazine group represented by formula (1), and pharmaceutically acceptable salts thereof are provided, wherein R1 is hydrogen, halogen, C1-C3 lower alkyl, lower alkoxy or lower acyl, trifluoromethyl, amino or nitro. The method for preparing the terephthalic acid amide derivatives of formula (1) comprises the steps of: (a) reacting a compound of formula (2) with a compound of formula (3) to prepare a compound of formula (4); (b) hydrolysis of benzoic acid methylester of formula (4) to prepare a compound of formula (5); and (c) reacting the compound of formula (5) with acid chloride to prepare acid anhydride and reacting the acid anhydride with a compound of formula (6).
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Patent Agency Ranking86.发明公开
公开(公告)号：KR1020030008654A
公开(公告)日：2003-01-29
申请号：KR1020010043490
申请日：2001-07-19
IPC: A61K31/426
CPC classification number: A61K31/426 , Y10S514/878
Abstract: PURPOSE: Provided are 4-((4-thiazolyl)phenoxy)alkoxy-benzamidine derivatives(DW1350 and DW1352) acting as leukotriene-B4 receptor antagonistic action. The compounds exhibit an excellent inhibition effect on a differentiation, formation, fusion process and bone absorption function of osteoclast cells, therefore they can be effectively used as an prophylaxis and treatment of osteoporosis. CONSTITUTION: The agent for prophylaxis and treatment of osteoporosis contains an effective amount of 4-((4-thiazolyl)phenoxy)alkoxy-benzamidine derivative of formula(1) or a salt thereof. In formula, R is H or OH. The agent is excellent in an inhibition of osteoclast cells as compared to any compound such as DW1349 and DW1351 having structural similarity as well as HS-1141 and CGS-25019C and has increased efficacy in increasing the activity of osteoblast cells.
Abstract translation: 目的：提供作为白三烯-B4受体拮抗作用的4 - （（4-噻唑基）苯氧基）烷氧基 - 苄脒衍生物（DW1350和DW1352）。 该化合物对破骨细胞的分化，形成，融合过程和骨吸收功能具有优异的抑制作用，因此可有效用于预防和治疗骨质疏松症。 构成：用于预防和治疗骨质疏松症的药物含有有效量的式（1）的4 - （（4-噻唑基）苯氧基）烷氧基 - 苄脒衍生物或其盐。 在式中，R是H或OH。 与具有结构相似性的DW1349和DW1351以及HS-1141和CGS-25019C的化合物相比，该试剂在破骨细胞抑制方面优异，并且在增加成骨细胞活性方面具有增加的功效。
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公开(公告)号：KR1020020068148A
公开(公告)日：2002-08-27
申请号：KR1020010008424
申请日：2001-02-20
Applicant: 동화약품주식회사
IPC: C12N15/866
CPC classification number: C12N15/866 , C07K1/22 , C07K14/005 , C07K2319/00 , C12N5/0601 , C12N2730/10134 , C12N2760/10134
Abstract: PURPOSE: Provided is a divalent vaccine against hepatitis B and hepatitis D and a method for preparing it in high yield, thereby preventing hepatitis B and hepatitis D simultaneously. CONSTITUTION: Baculovirus transition vector, pVLHBs(WT)-HDs, contains HBV surface antigen coding gene having 158-836 nt region of SEQ ID NO:1 and HDV delta antigen coding gene having 1601-1016 nt region of SEQ ID NO:7. Recombinant baculovirus is prepared by transfection with the baculovirus transition vector. The divalent vaccine is expressed in a transfected insect cells by recombinant baculovirus.
Abstract translation: 目的：提供一种针对乙型肝炎和丙型肝炎的二价疫苗及其高产率制备方法，从而同时预防乙肝和丙型肝炎。 构成：杆状病毒转移载体pVLHB（WT）-HDs含有具有SEQ ID NO：1具有158-836nt区域的HBV表面抗原编码基因和具有SEQ ID NO：7的1601-1016nt区域的HDVδ抗原编码基因。 通过用杆状病毒转染载体转染制备重组杆状病毒。 二价疫苗通过重组杆状病毒在转染的昆虫细胞中表达。
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88.发明公开
公开(公告)号：KR1020010029698A
公开(公告)日：2001-04-06
申请号：KR1020000024657
申请日：2000-05-09
Applicant: 동화약품주식회사
IPC: C07D403/04
Abstract: PURPOSE: Provided is a method for manufacturing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative which has antibacterial effects on both gram positive and negative bacteria so that the derivative is useful for medical purposes. And Its pharmaceutically acceptable salt and its solvate are also provided. CONSTITUTION: A method for producing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative comprises the following steps of: i) reacting the compound of the formula (3) with ketal compound of the formula (2a) in the presence of acid receptor, for 1-24 hours at 0-150 deg.C, preferably from room temperature to 90 deg.C, to manufacture optically active quinoline carboxylic acid derivative of the formula (4); ii) deketalizing the quinoline carboxylic acid derivative to manufacture pyrrolidinone of the formula (5) at from room temperature to 100 deg.C; and iii) reacting the pyrrolidinone with alkoxylamine in the presence of base at 0-90 deg.C. In the formula (1), Q is C-H, C-F, C-CL, or N. Y is H or NH2. R is a C1-C4 linear or branched alkyl, aryl, or benzyl group. * is an optically pure asymmetric carbon.
Abstract translation: 目的：提供对革兰氏阳性细菌和阴性细菌都具有抗菌作用的4-氨基甲基-4-甲基-3-（Z） - 烷氧基氨基衍生物的制备方法，因此该衍生物可用于医疗目的。 还提供其药学上可接受的盐及其溶剂合物。 构成：4-氨基甲基-4-甲基-3-（Z） - 烷氧基氨基衍生物的制备方法包括以下步骤：i）使式（3）的化合物与式（2a）的缩酮化合物反应于 存在酸受体，在0-150℃，优选室温至90℃下进行1-24小时，以制备式（4）的光学活性喹啉羧酸衍生物; ii）将喹啉羧酸衍生物缩酮化，制备式（5）的吡咯烷酮，室温至100℃; 和iii）在0-90℃下，在碱的存在下使吡咯烷酮与烷氧基胺反应。 在式（1）中，Q是C-H，C-F，C-CL或N.Y是H或NH 2。 R是C1-C4直链或支链烷基，芳基或苄基。 *是光学纯的不对称碳。
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公开(公告)号：KR1020000020793A
公开(公告)日：2000-04-15
申请号：KR1019980039547
申请日：1998-09-24
IPC: C07D211/58
Abstract: PURPOSE: An N-(4-piperidine) benzamide is prepared by the reaction of thioester and is-piperidine amine derivatives which has gastroenteric irritative physiological activities. CONSTITUTION: Carboxylic derivatives and alkyl chloroformate are reacted to give an intermediate(formula 5), and reacted with 2-mercaptobenzimidazole to give the novel active thioester(formula 3). Active thioester and is-piperidine amine derivatives(formula 2) are reacted to give benzamide derivatives(formula 1; R is C1-C6 lower alkyl; L is an alkyl or aryloxyalkyl). Thus, 376 mg of triethyl amine and 280 mg of ethyl chloroformate are drop in 500 mg of 4-amino-5-chloro-2-methoxybenzoic acid and reacted at 0-10°C for 1.5 hours, adding 396 mg of 2-mercaptobenzimidazole at room temperature for 6 hour. A mixed solution of 630 mg of is-4-amino-3-method-1-£3-(4-fluorophenoxy) propyl|piperidine and 1 ml of N,N-dimethyl form amide is drop at room temperature for 5 hours in the reactant to give 963 mg of is-2-method-4-amino-5-chloro-N-£1-£3-(4- fluorophenoxy)propyl|-3-method-4-piperidinyl|benzamide1 hydrate.
Abstract translation: 目的：通过具有胃肠刺激性生理活性的硫酯和异哌啶胺衍生物的反应制备N-（4-哌啶）苯甲酰胺。 组成：羧酸衍生物和氯甲酸烷基酯反应得到中间体（式5），并与2-巯基苯并咪唑反应得到新的活性硫酯（式3）。 使活性硫酯和哌啶胺衍生物（式2）反应得到苯甲酰胺衍生物（式1; R是C 1 -C 6低级烷基; L是烷基或芳氧基烷基）。 因此，将376mg三乙胺和280mg氯甲酸乙酯滴加到500mg 4-氨基-5-氯-2-甲氧基苯甲酸中，并在0-10℃下反应1.5小时，加入396mg 2-巯基苯并咪唑 在室温下放置6小时。 将630mg的is-4-氨基-3-方法1-（3-氟苯氧基）丙基|哌啶和1ml N，N-二甲基甲酰胺的混合溶液在室温下滴加5小时， 反应物得到963mg的is-2-方法-4-氨基-5-氯-N- {3-（4-氟苯氧基）丙基| 3-方法-4-哌啶基|苯甲酰胺1水合物。
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公开(公告)号：KR1020000008471A
公开(公告)日：2000-02-07
申请号：KR1019980028294
申请日：1998-07-14
Applicant: 동화약품주식회사
IPC: C07D211/58
Abstract: PURPOSE: A method for preparing N-(4-piperidine)benzamide is provided in which high purity of compound can be obtained in high yield and a side reaction product is easily separated from an object product. CONSTITUTION: A benzamide derivatives of formula I is obtained by reacting an active ester compound of formula II and a piperidine amine compound of formula III. The active ester compound of formula II is obtained by reacting a compound of formula VI and a compound of formula IV and the piperidine amine compound of formula III is obtained by using a ketone compound of formula VII. The compound of formula VI is obtained by reacting a carboxylic acid compound of formula II` and an ethylchloroformate or an isobytylchloroformate of formula V.
Abstract translation: 目的：提供一种制备N-（4-哌啶）苯甲酰胺的方法，其中可以高产率获得高纯度的化合物，并且副反应产物容易与目标产物分离。 构成：式I的苯甲酰胺衍生物通过使式II的活性酯化合物与式III的哌啶胺化合物反应获得。 式Ⅱ的活性酯化合物是通过使式Ⅵ化合物与式Ⅳ化合物反应得到的，通过使用式Ⅶ的酮化合物得到式Ⅲ的哌啶胺化合物。 式VI化合物通过使式II'的羧酸化合物与氯甲酸乙酯或式V的氯代甲酸异丁酯反应而得到。
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