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公开(公告)号：KR100661081B1
公开(公告)日：2006-12-26
申请号：KR1020000031926
申请日：2000-06-10
Applicant: 동화약품주식회사
IPC: C07D401/12
Abstract: 본 발명은 항바이러스제로 유용한 신규의 6-메틸니코틴아미드 유도체, 그의 제조방법 및 그를 포함하는 약학적 조성물에 관한 것으로서, 구체적으로 비핵산계 화합물인 하기 화학식 1로 표시되는 6-메틸니코틴아미드 유도체는 HBV (Hepatitis B Virus) 및 HCV (Hepatitis C virus)의 증식 뿐만 아니라 HIV (Human Immunodeficiency Virus) 증식을 억제하는 효과도 나타내므로 B형 간염과 C형 간염 및 후천성 면역 결핍증의 치료제 및 예방제로 유용하게 사용될 수 있다.
상기 화학식 1에서, R 및 n은 명세서에 기재된 바와 같다.-
公开(公告)号：KR100566193B1
公开(公告)日：2006-03-29
申请号：KR1019990053295
申请日：1999-11-27
Applicant: 동화약품주식회사
IPC: C07D213/16
Abstract: 본 발명은 신규의 3-니트로피리딘 유도체, 그의 제조방법 및 그를 포함하는 약학적 조성물에 관한 것으로서, 구체적으로 비핵산계 화합물인 하기 화학식 1로 표시되는 3-니트로피리딘 유도체는 HBV (Hepatitis B Virus) 증식 뿐만 아니라 HIV (Human Immunodeficiency Virus) 증식을 억제하는 효과를 나타내므로 B형 간염 및 후천성 면역 결핍증의 치료제 및 예방제로서 유용하게 사용될 수 있다.
상기 식에서, R 및 R
2 는 명세서에 기재된 바와 같다.-
公开(公告)号：KR100566189B1
公开(公告)日：2006-03-29
申请号：KR1019990064402
申请日：1999-12-29
Applicant: 동화약품주식회사
IPC: C07D239/38
Abstract: 본 발명은 신규의 5-피리미딘카르복스아미드 유도체, 그의 제조방법 및 그를 포함하는 약학적 조성물에 관한 것으로서, 구체적으로 비핵산계 화합물인 하기 화학식 1로 표시되는 5-피리미딘카르복스아미드 유도체는 HBV (Hepatitis B Virus) 증식 뿐만 아니라 HIV (Human Immunodeficiency Virus) 증식을 억제하는 효과를 나타내므로 B형 간염 및 후천성 면역 결핍증의 치료제 및 예방제로서 유용하게 사용될 수 있다.
상기 식에서, R
1 , R
2 , R
3 및 n은 명세서에 기재된 바와 같다.Abstract translation: 本发明涉及包含其特别通过下述通式（1）中所示的一种新颖的嘧啶-5-甲酰胺衍生物，制造的方法，并且他，5-嘧啶甲酰胺衍生物的药物组合物，非核系化合物是HBV （B型肝炎病毒）的增殖，以及显示出抑制HIV（人类免疫缺陷病毒）的增殖可以被有效地用作乙型肝炎和AIDS的治疗和预防剂的效果。
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公开(公告)号：KR100491100B1
公开(公告)日：2005-11-29
申请号：KR1019970036589
申请日：1997-07-31
Applicant: 동화약품주식회사
IPC: C07D401/04 , A61K31/395 , C07D401/14 , C07D413/14 , C07D417/14
Abstract: 본 발명은 신규 테레프탈산아미드 유도체에 관한 것으로서, 더욱 상세하게는 HIV 및 HBV를 비롯한 각종 바이러스의 증식억제 효과가 우수하여 항바이러스제로서 유효한 다음 화학식 1로 표시되는 신규 테레프탈산아미드 유도체와 그의 약제학적으로 허용가능한 염, 그리고 그의 제조방법에 관한 것이다.
[화학식 1]
상기 화학식 1에서,
R
1 , R
2 및 R
3 은 발명의 상세한 설명에서 설명한 바와 같다.-
公开(公告)号：KR100438482B1
公开(公告)日：2004-08-18
申请号：KR1019960051939
申请日：1996-11-05
IPC: C07D403/12 , A61K31/41
Abstract: PURPOSE: Diarylsulfonyl imidazolone derivative and a preparation method thereof are provided. The derivative has improved anticancer activity and do not form aniline derivative causing side-effects. CONSTITUTION: The 4-phenyl-1-(N-carbamoylindoline-5-sulfonyl)- 4,5-dihydro-2-imidazolone derivative is represented by the formula (I), wherein X is oxygen or sulfur; R is C1-C6 alkyl, chloroacetyl, benzyl, phenyl, methoxyphenyl, fluorophenyl, methylphenyl, aminophenyl or thiomethylphenyl; and R' is hydrogen or chlorine. An anticancer pharmaceutical composition comprises the diarylsulfonyl imidazolone derivative of the formula (I) and pharmaceutically acceptable salts thereof as effective components. The method for preparing the 4-phenyl-1-(N-carbamoylindoline-5-sulfonyl)- 4,5-dihydro-2-imidazolone derivative represented by the formula (I) comprises reacting a compound of the formula (II) with a compound of the formula (III).
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Patent Agency Ranking
公开(公告)号：KR1020020034759A
公开(公告)日：2002-05-09
申请号：KR1020000065270
申请日：2000-11-03
Applicant: 동화약품주식회사
IPC: C12N7/01
CPC classification number: C12N7/00 , C12N2710/14011 , C12Q1/68
Abstract: PURPOSE: Provided are a detecting method of hepatitis C virus(HCV) using recombinant mixed antigens derived from HCV and a diagnostic kit thereof, particularly by immuno chromatography using recombinant mixed antigens including core, NS3 and NS5A proteins of HCV gene as main components. CONSTITUTION: A recombinant Baculovirus(KCCM 10218) is manufactured by cotransfection of Baculovirus transfer vector including HCV derived core protein gene. HCV derived core protein is expressed from the recombinant Baculovirus(KCCM 10218) and has amino acid sequence of SEQ ID NO: 8. A recombinant Baculovirus(KCCM 10219) is manufactured by cotransfection of Baculovirus transfer vector including HCV derived NS3 protein gene. HCV derived NS3 proteins expressed from the recombinant Baculovirus(KCCM 10219) and has amino acid sequence of SEQ ID NO:9. An E.coli transformant(KCCM 10217) is transformed with a recombinant expression vector including HCV derived NS5A protein gene. HCV derived NS5A protein is expressed from the transformant and has amino acid sequence of SEQ ID NO: 10. The HCV diagnostic kit contains a mixed antigen consisting of core, NS3 and NS5A proteins derived from HCV.
Abstract translation: 目的：提供使用HCV衍生的重组混合抗原的丙型肝炎病毒（HCV）的检测方法及其诊断试剂盒，特别是使用包含HCV基因的核心，NS3和NS5A蛋白的重组混合抗原的免疫色谱作为主要成分。 构成：通过共转染包括HCV衍生的核心蛋白基因的杆状病毒转移载体来制备重组杆状病毒（KCCM 10218）。 HCV衍生的核心蛋白由重组杆状病毒（KCCM 10218）表达并具有SEQ ID NO：8的氨基酸序列。通过共转染包含HCV衍生的NS3蛋白基因的杆状病毒转移载体来制备重组杆状病毒（KCCM 10219）。 由重组杆状病毒（KCCM 10219）表达的HCV衍生的NS3蛋白，具有SEQ ID NO：9的氨基酸序列。 用包含HCV衍生的NS5A蛋白基因的重组表达载体转化大肠杆菌转化体（KCCM 10217）。 HCV衍生的NS5A蛋白由转化体表达，并具有SEQ ID NO：10的氨基酸序列。HCV诊断试剂盒含有由核心，NS3和源自HCV的NS5A蛋白组成的混合抗原。
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7.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。
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公开(公告)号：KR1020010011926A
公开(公告)日：2001-02-15
申请号：KR1019990031532
申请日：1999-07-31
Applicant: 동화약품주식회사
IPC: A61K38/15
Abstract: PURPOSE: A composition containing destruxin derivatives for prevention and treatment of osteoporosis is provided, inwhich cyclodepsipeptide derived from fungi shows excellent osteoclast activity-inhibition effect regardless of presence of PTH(parathyroid hormone) in osteoclast, therefore being used for prevention and treatment of osteoporosis. CONSTITUTION: The various destruxin derivatives can be prepared by a well known method, which is cyclodepsipeptides separated from various fungi(e.g., Metarhizium anisopliae). The composition containing destruxin derivatives for prevention and treatment of osteoporosis can be prepared in the form of tablets, capsules, troches, solution, suspension, or injections, dried powder for injection, a spray, suppositories, or a patch preparation by mixing with pharmaceutically acceptable carriers, and which can be administrated by oral path and parenteral path(e.g., in vein, under subcutaneous, abdominal cavity, or nasal cavity). The composition containing destruxin derivatives can be also administrated in the dosage of 0.1μg-100mg, desirably 100μg-1mg per day.
Abstract translation: 目的：提供含有用于预防和治疗骨质疏松症的destruxin衍生物的组合物，其中来自真菌的环缩酚肽显示出破骨细胞中存在PTH（甲状旁腺激素）的极好的破骨细胞活性抑制作用，因此用于预防和治疗骨质疏松症。 构成：各种destruxin衍生物可以通过众所周知的方法制备，该方法是从各种真菌（例如，Metarhizium anisopliae）分离的环糊精肽。 含有用于预防和治疗骨质疏松症的destruxin衍生物的组合物可以以片剂，胶囊剂，锭剂，溶液，悬浮液或注射剂的形式，注射用干燥粉末，喷雾剂，栓剂或贴剂制剂的形式制备， 载体，并且其可以通过口服途径和肠胃外途径施用（例如，在静脉，皮下，腹腔或鼻腔）。 含有destruxin衍生物的组合物也可以以0.1μg-100mg，优选每天100μg-1mg的剂量施用。
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公开(公告)号：KR1020000031735A
公开(公告)日：2000-06-05
申请号：KR1019980047918
申请日：1998-11-10
Applicant: 동화약품주식회사
IPC: C07D401/14
Abstract: PURPOSE: 2,5-pyrimidinedicarboxylic acids and the method for manufacturing it are provided, which have effect on restraining the proliferation of HBV(Hepatitis B Virus) and HIV(Human Immunodeficiency Virus). CONSTITUTION: In the formula 1, R1 represents hydrogen, alkyl group, hydroxy alkyl group, alkoxy alkyl group, dihydroxy alkyl group and dialkoxy alkyl group and R2 represents hydrogen and alkyl group. 2,5-pyridinedicarboxylic acids(formula 1) can form organic or inorganic salt such as chloric acid, phosphoric acid, oxalic acid, maleic acid and tartaric acid which is admitted pharmaceutically. 2,5-pyridinedicarboxylic acids are prepared from following reaction(reaction 1). Piperazines are piperazine(R1=hydrogen), 1-methylpiperazine(R1=methyl group), 1-ethylpiperazine(R1=ethyl group), 1-(2-hydroxyethyl)piperazine(R1=2-hydroxyethyl group. Nicotinic acids(formula 2) are reacted with acyl chloride, product of this reaction is reacted with piperazine compounds and 2,5-pyrimidinedicarboxylic acids are prepared from this reaction.
Abstract translation: 目的：提供2,5-嘧啶二羧酸及其制备方法，其具有抑制HBV（乙型肝炎病毒）和HIV（人类免疫缺陷病毒）增殖的作用。 构成：在式1中，R 1表示氢，烷基，羟基烷基，烷氧基烷基，二羟基烷基和二烷氧基烷基，R 2表示氢和烷基。 2,5-吡啶二羧酸（式1）可以形成有机或无机盐，例如药学上允许的氯酸，磷酸，草酸，马来酸和酒石酸。 从以下反应制备2,5-吡啶二羧酸（反应1）。 哌嗪是哌嗪（R1 =氢），1-甲基哌嗪（R1 =甲基），1-乙基哌嗪（R1 =乙基），1-（2-羟乙基）哌嗪（R1 = 2-羟乙基）烟酸（式2 ）与酰氯反应，将该反应产物与哌嗪化合物反应，并从该反应制备2,5-嘧啶二羧酸。
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