-
公开(公告)号：KR100713137B1
公开(公告)日：2007-05-02
申请号：KR1020010037547
申请日：2001-06-28
Applicant: 동화약품주식회사
IPC: C07D401/12
CPC classification number: C07D249/08 , C07D231/12 , C07D231/56 , C07D233/56 , C07D401/12 , C07D403/12
Abstract: 본 발명은 신규의 2,4-디플루오로벤즈아미드 유도체에 관한 것으로서, 더욱 상세하게는 HBV(Hepatitis B Virus) 증식 뿐만 아니라 HCV(Hepatitis C Virus) 증식을 억제하는 효과가 우수하여 B형 간염 및 C형 간염의 치료제 및 예방제로 유용한 비핵산계 화합물인 다음 화학식 1로 표시되는 2,4-디플루오로벤즈아미드 유도체와 그의 약학적으로 허용가능한 염, 그리고 그의 제조방법에 관한 것이다.
상기 화학식 1에서 : R
1 , R
2 , R
3 및 n은 각각 발명의 상세한 설명에서 정의한 바와 같다.
2,4-디플루오로벤즈아미드 유도체, B형 간염, C형 간염, 치료제, 예방제-
公开(公告)号：KR1020030001167A
公开(公告)日：2003-01-06
申请号：KR1020010037547
申请日：2001-06-28
Applicant: 동화약품주식회사
IPC: C07D401/12
CPC classification number: C07D249/08 , C07D231/12 , C07D231/56 , C07D233/56 , C07D401/12 , C07D403/12
Abstract: PURPOSE: Provided are novel 2,4-difluorobenzamide derivatives which are excellent in inhibition of the growth of both HBV and HCV, and thus used as prevention and treatment agents for HBV hepatitis and HCV hepatitis. also, provided are their pharmaceutically acceptable salts and their manufacturing method. CONSTITUTION: The 2,4-difluorobenzamide derivative is represented by the formula(1), wherein R1 is C1-C4 linear or branched alkyl group, hydroxy group, a C2-C6 alkylamino group, a 4-sulfamoylphenyl group, or a saturated or unsaturated 5 or 6 membered hetero cycle having 1-2 of hetero atoms selected from N, O and S; R2 is H or a C1-C3 linear or branched alkyl group; or R1 and R2 are bound together with 1-2 of hetero atoms selected from N, O and S to form a saturated or unsaturated 5, 6 or 7 membered hetero cycle, wherein the hetero cycle is a C1-C4 linear or branched alkyl group, or substituted or unsubstituted with a C1-C3 hydroxyalkyl group; and R3 is a 5-indazolyl group; and n is an integer of 0-4.
Abstract translation: 目的：提供对HBV和HCV的生长抑制优异的新型2,4-二氟苯甲酰胺衍生物，因此用作HBV肝炎和HCV肝炎的预防和治疗剂。 还提供了它们的药学上可接受的盐及其制造方法。 构成：2,4-二氟苯甲酰胺衍生物由式（1）表示，其中R1是C1-C4直链或支链烷基，羟基，C2-C6烷基氨基，4-氨磺酰基苯基或饱和或 具有1-2个选自N，O和S的杂原子的不饱和5或6元杂环; R2是H或C1-C3直链或支链烷基; 或R 1和R 2与1-2个选自N，O和S的杂原子结合在一起以形成饱和或不饱和的5,6或7元杂环，其中杂环是C 1 -C 4直链或支链烷基 或者被C1-C3羟烷基取代或未取代; 并且R 3是5-吲唑基; n为0-4的整数。
-
公开(公告)号：KR100798579B1
公开(公告)日：2008-01-28
申请号：KR1020010017143
申请日：2001-03-31
Applicant: 동화약품주식회사
IPC: C07D413/14
CPC classification number: C07D403/14 , C07D401/14 , C07D403/12 , C07D413/14
Abstract: 본 발명은 신규의 메톡시-1,3,5-트리아진 유도체, 제조방법 및 그를 포함하는 약학적 조성물에 관한 것으로서, 구체적으로 비핵산계 화합물인 하기 화학식 1로 표시되는 메톡시-1,3,5-트리아진 유도체는 HBV (Hepatitis B Virus) 증식뿐만 아니라 HCV (Hepatitis C Virus) 증식을 억제하는 효과를 나타내므로 B형 간염 및 C형 간염의 치료제 및 예방제로서 유용하게 사용될 수 있다.
(상기 식에서 R
1 , R
2 , R
3 및 n은 명세서에 기재된 바와 같다.)
메톡시-1,3,5-트리아진 유도체, B형 간염, C형 간염, 치료제, 예방제-
4.发明授权
公开(公告)号：KR100497942B1
公开(公告)日：2005-06-29
申请号：KR1020017014647
申请日：2000-05-18
Applicant: 동화약품주식회사
IPC: C07D471/04
CPC classification number: C07D401/04 , C07D471/04 , C07D487/10
Abstract: 본 발명은 광학활성의 퀴놀린 카르복실산 유도체, 이의 약학적으로 허용되는 염, 이의 용매화물 및 이의 제조방법에 관한 것으로, 구체적으로 본 발명은 퀴놀론 모핵의 7-위치에 광학활성을 유발하는 4-아미노메틸-4-메틸-3-(Z)-알콕시이미노피롤리딘 치환체를 갖는 광학활성의 퀴놀린 카르복실산 유도체에 관한 것으로, 본 발명의 화합물은 그의 거울상 이성질체, 라세믹 혼합물 및 기존의 항균제에 비하여 항균 효과가 매우 우수하고 약동력학적 특성이 우수할 뿐만 아니라 광독성도 거의 나타내지 않기 때문에 항균제로서 효과적으로 사용될 수 있다.
-
公开(公告)号：KR100579792B1
公开(公告)日：2006-05-12
申请号：KR1019990005100
申请日：1999-02-12
Applicant: 동화약품주식회사
IPC: C07D401/06
Abstract: 본 발명은 신규의 2,5-피리딘디카복실산 유도체에 관한 것으로서, 더욱 상세하게는 HBV 및 HIV에 대한 증식억제효과가 우수하여 항바이러스제로서 유효한 다음 화학식 1로 표시되는 신규의 2,5-피리딘디카복실산 유도체와 그의 약제학적으로 허용가능한 염, 그리고 그의 제조방법에 관한 것이다.
상기 화학식 1에서 : R
1 , R
2 , R
3 및 n은 각각 발명의 상세한 설명에서 설명한 바와 같다.
2,5-피리딘디카복실산 유도체, 항바이러스Abstract translation: 本发明涉及有效作为抗病毒剂的新颖的2,5-吡啶二羧酸衍生物，更具体地讲，由下式表示的新的2,5-吡啶（1），并且具有以HBV和HIV二优良增殖抑制效果 羧酸衍生物及其药学上可接受的盐及其制备方法。
-
Patent Agency Ranking
公开(公告)号：KR1020000020792A
公开(公告)日：2000-04-15
申请号：KR1019980039546
申请日：1998-09-24
Applicant: 동화약품주식회사
IPC: C07D401/14
Abstract: PURPOSE: Title derivatives are provided which has an inhibition effect against HBV(Hepatitis B Virus) and HIV(Human Immunodeficiency Virus) growth. CONSTITUTION: Nicotinic derivatives(formula 2; R4 is H or C1-C4 straight chain or branched alkyl group) and amine compound(formula 3; R1 is C1-C4 straight chain or branched alkoxy or amino group; R2 is H, C1-C4 straight chain or branched alkyl, C1-C3 straight chain or branched hydroxy alkyl, C2-C4 alkyl thioalkyl, phenyl, benzyl or hydroxy benzyl group; R3 is H or methyl group; n is 0-1) are reacted to give the derivatives(formula 1). Thus, 2 g of 6-£1-£3-isopropyl amino)-2-pyridyl|piperazin-4-yl-carbonyl|nicotine acid and 0.8 ml of triethyl amine are dissolved in 30 ml of methylene chloride, and slowly added 0.7 ml of pivaloyl chloride at 0- 5°C. Reactant is reacted at 5°C for 1 hour, followed by addition of 2.5 ml of N,N-diisopropyl ethyl amine and 0.83 g of glycine ethyl ester at 10°C for 2 hour to give 1.89 g of N-(ethoxycarbonyl methyl)-6-£1-£3-isopropyl amino)-2-pyridyl|piperazin-4-yl-carbonyl|nicotine amide hydrochloride.
Abstract translation: 目的：提供对HBV（乙型肝炎病毒）和HIV（人类免疫缺陷病毒）生长具有抑制作用的标题衍生物。 构型：烟碱衍生物（式2; R4为H或C1-C4直链或支链烷基）和胺化合物（式3; R1为C1-C4直链或支链烷氧基或氨基; R2为H，C1-C4 直链或支链烷基，C1-C3直链或支链羟基烷基，C2-C4烷基硫代烷基，苯基，苄基或羟基苄基; R3是H或甲基; n为0-1）反应，得到衍生物 公式1）。 因此，将2g 6- {1- {3-异丙基氨基）-2-吡啶基|哌嗪-4-基羰基|尼古丁酸和0.8ml三乙胺溶于30ml二氯甲烷中，并缓慢加入0.7 ml的新戊酰氯在0-5℃。 反应物在5℃下反应1小时，然后在10℃下加入2.5ml N，N-二异丙基乙基胺和0.83g甘氨酸乙酯2小时，得到1.89g N-（乙氧基羰基甲基） -6- {1- {3-异丙基氨基} -2-吡啶基}哌嗪-4-基 - 羰基}烟碱酰胺盐酸盐。
-
7.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。
-
公开(公告)号：KR1019990087861A
公开(公告)日：1999-12-27
申请号：KR1019990005100
申请日：1999-02-12
Applicant: 동화약품주식회사
IPC: C07D401/06
CPC classification number: C07D213/82 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
Abstract: 본발명은신규의 2,5-피리딘디카복실산유도체에관한것으로서, 더욱상세하게는 HBV 및 HIV를비롯한레트로바이러스에대한증식억제효과가우수하여항레트로바이러스제로서유효한다음화학식 1로표시되는신규의 2,5-피리딘디카복실산유도체와그의약제학적으로허용가능한염, 그리고그의제조방법에관한것이다. 상기화학식 1에서 : R, R, R및 n은각각발명의상세한설명에서설명한바와같다.
-
公开(公告)号：KR1020020076920A
公开(公告)日：2002-10-11
申请号：KR1020010017143
申请日：2001-03-31
Applicant: 동화약품주식회사
IPC: C07D413/14
CPC classification number: C07D403/14 , C07D401/14 , C07D403/12 , C07D413/14
Abstract: PURPOSE: Provided are a methoxy-1,3,5-triazine derivative which inhibit the growth of Hepatitis C virus(HCV) and a pharmaceutical composition containing the same, therefore it can be useful for the prevention and treatment of hepatitis type B and hepatitis type C. CONSTITUTION: The methoxy-1,3,5-triazine derivative is represented by formula(1) and its pharmaceutically acceptable salt are provided. In the formula(1), R1 is H or C1-C8 alkyl; R2 is H, hydroxy, C1-C4 linear or branched chain alkyl, C1-C3 linear or branched chain alkoxy, C1-C3 hydroxyalkyl, C2-C6 dialkylamino, C3-C6 cycloalkyl, lactam, saturated or unsaturated 5 or 6 atom hetero ring compound optionally substituted with C1-C3 linear or branched chain alkyl substituted or unsubstituted, and containing one or two hetero atom selected from N, O and S; or bicyclo compound containing one or two hetero atom selected from N, O and S; n is an integer of 0 to 4; and R3 is 5-indazolyl or 6-indazolyl. The method for producing the methoxy-1,3,5-triazine derivative comprises the steps of: reacting 2,4-dichloro-6-methoxy-1,3,5-triazine of formula(4) with 5-aminoindazole or 6-aminoindazole of formula(5) in the presence of base to prepare aminoindazole substituted 2-chloro-6-methoxy-1,3,5-triazine derivative of formula(6); and reacting the compound of formula(6) with amine compound of formula(7) in the presence of amine to prepare methoxy-1,3,5-triazine derivative of formula(1).
Abstract translation: 目的：提供抑制丙型肝炎病毒（HCV）生长的甲氧基-1,3,5-三嗪衍生物和含有该丙氨酸病毒（HCV）的药物组合物，因此可用于预防和治疗乙型肝炎和肝炎 C型。构成：提供甲氧基-1,3,5-三嗪衍生物由式（1）表示，并提供其药学上可接受的盐。 在式（1）中，R 1是H或C 1 -C 8烷基; R2是H，羟基，C1-C4直链或支链烷基，C1-C3直链或支链烷氧基，C1-C3羟基烷基，C2-C6二烷基氨基，C3-C6环烷基，内酰胺，饱和或不饱和的5或6原子杂环 任选被取代或未取代的C 1 -C 3直链或支链烷基取代的，含有一个或两个选自N，O和S的杂原子的化合物; 或含有一个或两个选自N，O和S的杂原子的双环化合物; n为0〜4的整数。 并且R 3是5-吲唑基或6-吲唑基。 制备甲氧基-1,3,5-三嗪衍生物的方法包括以下步骤：使式（4）的2,4-二氯-6-甲氧基-1,3,5-三嗪与5-氨基吲唑或6- 式（5）的氨基吲唑在碱的存在下反应，制备式（6）的氨基吲唑取代的2-氯-6-甲氧基-1,3,5-三嗪衍生物; 并在胺的存在下使式（6）的化合物与式（7）的胺化合物反应，制得式（1）的甲氧基-1,3,5-三嗪衍生物。
-
10.发明公开
公开(公告)号：KR1020020002461A
公开(公告)日：2002-01-09
申请号：KR1020017014647
申请日：2000-05-18
Applicant: 동화약품주식회사
IPC: C07D471/04
CPC classification number: C07D401/04 , C07D471/04 , C07D487/10
Abstract: PURPOSE: Provided are optically active quinoline carboxylic acid derivatives, pharmaceutically acceptable salts thereof, solvates thereof, and a process for preparation thereof, which are useful for an antibacterial agent. CONSTITUTION: The optically active quinoline carboxylic acid derivatives are represented by the following formula(1), and contains optical activity-causing 4-aminomethyl-4-methyl-3 (Z)-alkoxyiminopyrrolidine substituents at the 7-position of the quinolone nuclei, their pharmaceutically acceptable salts, and their solvates. In the formula(1), Q is C-H, C-F, C-Cl or N; Y is H or NH2; R is a straight or branched alkyl group of Cl-C, an allyl group or a benzyl group, and * represents optically pure chiral carbon atom. Their preparation process comprises the steps of: condensing the quinolone nuclei-containing compound of formula(3), with the ketal compound of formula(2a), in the presence of an acid acceptor to give the optically active quinoline carboxylic acid derivative of formula(4); deketalizing the optically active quinoline carboxylic acid derivative of formula(4) to give the pyrrolidinone compound of formula(5); and reacting the pyrrolidinone compound of formula(5) with an alkoxylamine in the presence of a base to obtain the desired compound of formula(1).
Abstract translation: 目的：提供可用于抗菌剂的光学活性喹啉羧酸衍生物，其药学上可接受的盐，溶剂合物及其制备方法。 构成：光学活性喹啉羧酸衍生物由下式（1）表示，并且在喹诺酮核的7-位含有光学活性的4-氨基甲基-4-甲基-3（Z） - 烷氧基亚氨基吡咯烷取代基， 其药学上可接受的盐及其溶剂合物。 在式（1）中，Q是C-H，C-F，C-Cl或N; Y为H或NH 2; R是Cl-C，烯丙基或苄基的直链或支链烷基，*表示光学上纯的手性碳原子。 它们的制备方法包括以下步骤：在酸受体存在下将式（3）的喹诺酮核含有化合物与式（2a）的缩酮化合物缩合，得到式（3）的光学活性喹啉羧酸衍生物 4）; 对式（4）的光学活性喹啉羧酸衍生物进行缩酮化，得到式（5）的吡咯烷酮化合物; 并在碱的存在下使式（5）的吡咯烷酮化合物与烷氧基胺反应，得到所需的式（1）化合物。
-
-
-
-
-
-
-
-
-
Search Results
11
records
(took 0.023 seconds)
