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公开(公告)号：KR100592920B1
公开(公告)日：2006-06-23
申请号：KR1020000008695
申请日：2000-02-23
Applicant: 동화약품주식회사
IPC: A61K31/196
Abstract: 본 발명은 디클로페낙나트륨 및 폴록사머 혼합물을 포함하고 폴리에틸렌옥사이드 또는 폴리비닐피롤리돈 중에서 선택되어진 1종 이상의 고분자를 포함하는 직장 투여용 조성물로서 직장 투여시 이물감이나 불편함이 없고 투약이 용이하며 투약 후 항문에서 빠져나오지 않고 대장말단으로 이행되지 않는 디클로페낙나트륨을 포함하는 직장 투여용 조성물에 관한 것이다.
직장 투여용 조성물, 디클로페낙나트륨, 폴록사머-
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。
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公开(公告)号：KR100416120B1
公开(公告)日：2004-05-07
申请号：KR1019970060255
申请日：1997-11-15
Applicant: 동화약품주식회사
IPC: C07D493/04
Abstract: PURPOSE: An anti-tumor lignan compound isolated from Anthriscus sylvestris HOFFMANN(Umbelliferae) is provided, which compound has similar or improved anti-tumor activity to the prior anti-tumor compounds and no toxicity. CONSTITUTION: The anti-tumor lignan compound isolated from Anthriscus sylvestris HOFFMANN(Umbelliferae) represented by formula (1) is provided. The method for isolating the Anti-tumor lignan compound isolated from Anthriscus sylvestris HOFFMANN(Umbelliferae) of formula (1) comprises the steps of: cutting roots of Anthriscus sylvestris HOFFMANN(Umbelliferae); extracting the cut roots of Anthriscus sylvestris HOFFMANN(Umbelliferae) with methanol in 5 times; fractioning the methanol extract of Anthriscus sylvestris HOFFMANN(Umbelliferae) with solvent of hexane, chloroform, acetic acid ethyl, butanol and water to obtain an active fraction; subjecting the active fraction to silica gel, Sephadex and RP-18 chromatography to obtain anti-tumor compounds; and isolating and purifying an anti-tumor compound, Angeloyl podophyllotoxin, by subjecting the anti-tumor compounds to prep HPLC.
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公开(公告)号：KR100343943B1
公开(公告)日：2002-11-16
申请号：KR1019970032177
申请日：1997-07-11
Applicant: 동화약품주식회사
IPC: A61K31/495
Abstract: PURPOSE: A pteridine derivative is provided which is obtained by culturing Streptomyces sp. DWJJ 839 and purification, and shows excellent inhibiting effect on HBV polymerase. Therefore, it can be effectively used as a therapeutic agent for B type hepatitis and formulated into injection, ointment, cream, liquid, etc. CONSTITUTION: Streptomyces sp. DWJJ 839(KFCC 10974) separated from soil is cultured, the culture solution thereof is heat treated and centrifuged to separate a supernatant, the concentrated supernatant is extracted in butanol, purified with column chromatography and separated with HPLC to produce a pteridine derivative of the formula(1-1). In formula, R5 and R6 are CH3; X1 and X2 are nitrogen; X3 and X4 are oxygen. The therapeutic agent for B type hepatitis contains a pteridine derivative of the formula(1) or a salt thereof. In formula, R1 and R2 are each H, C1-4 alkyl or lower alkoxy or can form a benzene ring by binding R1 and R2.
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Patent Agency Ranking
公开(公告)号：KR1020010061856A
公开(公告)日：2001-07-07
申请号：KR1019990064402
申请日：1999-12-29
Applicant: 동화약품주식회사
IPC: C07D239/38
Abstract: PURPOSE: A 5-pyrimidine carboxamide derivatives and a pharmaceutical composition containing the same are provided, which are useful in the inhibition of the growth of hepatitis B virus(HBV) and human immunodeficiency virus(HIV). CONSTITUTION: The 5-pyrimidine carboxamide derivatives are represented by formula(1), in which R1 is hydroxy, C1 to C6 linear or branched alkyl, C1 to C5 linear or branched alkoxy, C2 to C6 linear or branched hydroxyalkyl, C2 to C6 dialkylamino, C2 to C6 linear or branched alkyl substituted by C2 to C5 alkoxycarbonyl and/or hydroxy, saturated or unsaturated 5 or 6 atoms membered hetero ring compounds containing 1 to 3 hetero atoms selected from N, O or S and substituted or unsubstituted by C1 to C3 alkyl and optionally containing asymmetric carbon; R2 is H or C1 to C4 linear or branched alkyl; R1 and R2 form together saturated 5 or 6 atoms membered hetero ring, wherein hetero ring contains 1 to 3 hetero atoms selected from N, O and S and substituted or unsubstituted by C1 to C5 linear or branched alkyl, C2 to C5 linear or branched hydroxyalkyl, or hydroxy; R3 is indazole-5-il or indazole-6-il; and n is an integer of 0 to 4. The pharmaceutical composition contains an effective amount of 5-pyrimidine carboxamide.
Abstract translation: 目的：提供5-嘧啶甲酰胺衍生物和含有它们的药物组合物，其可用于抑制乙型肝炎病毒（HBV）和人类免疫缺陷病毒（HIV）的生长。 构型：5-嘧啶甲酰胺衍生物由式（1）表示，其中R 1是羟基，C 1至C 6直链或支链烷基，C 1至C 5直链或支链烷氧基，C 2至C 6直链或支链羟烷基，C 2至C 6二烷基氨基 由C2至C5烷氧基羰基和/或羟基取代的C2至C6直链或支链烷基，和/或羟基，含有1至3个选自N，O或S的杂原子的饱和或不饱和的5或6元杂环化合物，并由C1至 C3烷基和任选含有不对称碳; R2是H或C1-C4直链或支链烷基; R 1和R 2一起形成饱和的5或6个原子元环，其中杂环含有1至3个选自N，O和S的杂原子，并且被C1至C5直链或支链烷基取代或未取代，C2至C5直链或支链羟烷基 ，或羟基; R3是吲唑-5-基或吲唑-6-il; n为0〜4的整数。该药物组合物含有有效量的5-嘧啶甲酰胺。
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公开(公告)号：KR1020000027306A
公开(公告)日：2000-05-15
申请号：KR1019980045212
申请日：1998-10-28
Applicant: 동화약품주식회사
IPC: A61K31/34
CPC classification number: A61K31/343 , A61K36/53 , A61K2236/30 , A61K2236/51
Abstract: PURPOSE: A medicinal composition, which is useful for treating hepatitis B, and a method for recovering trapezoid compound are provided. CONSTITUTION: The medicinal composition for treating hepatitis B contains tanshinol B of a following formula 1, tanshinone IIB of a following formula 2, przewaquinone A of a following formula 3, Salvia militarize Bunge extract, Salvia militarize Bunge separated materials as an effective ingredient. The method for recovering tanshinol B of the following formula 1, tanshinone IIB of the following formula 2 and przewaquinone A of the following formula 3 comprises steps of: (i) obtaining Salvia militarize Bunge extract by using water, organic solvent or a mixture solvent thereof as an extracting solvent; (ii) concentrating the extract of step (i); and (iii) performing solvent separation and column chromatography of step (ii) to separate and purify.
Abstract translation: 目的：提供一种可用于治疗乙型肝炎的药物组合物和回收梯形化合物的方法。 构成：用于治疗乙型肝炎的药物组合物含有下式1的丹参醇B，下式2的丹参酮IIB，下式3的靛红醌A，丹参黄芪提取物，丹参麻黄素Bunge分离物作为有效成分。 用于回收下式1的丹宁醇B，下式2的丹参酮IIB和下式3的柚子醌A的方法包括以下步骤：（i）通过使用水，有机溶剂或其混合溶剂来获得丹参武装提取物 作为提取溶剂; （ii）浓缩步骤（i）的提取物; 和（iii）进行步骤（ii）的溶剂分离和柱色谱以分离和纯化。
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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。
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公开(公告)号：KR1020000013029A
公开(公告)日：2000-03-06
申请号：KR1019980031662
申请日：1998-08-04
Applicant: 동화약품주식회사
IPC: C07D211/58
Abstract: PURPOSE: An N-(4-piperidine)benzamide has a physiological activity for the stimulating gastrointestinal system and a pharmaceutically accepted additional salt thereof. CONSTITUTION: An N-(4-piperidine)benzamide represented by the formula (1) having a physiological activity for the stimulating gastrointestinal system and a pharmaceutically accepted additional salt thereof: wherein L is aralkyl or aryloxyalkyl, wherein the alkyl moiety is C1-C6 alkyl and the aryl moieties are up to three substituents each independently selected from the group consisting of halo, C1-C6 low alkyl and C1-C6 low alkoxy; and R is C1-C6 low alkyl.
Abstract translation: 目的：N-（4-哌啶）苯甲酰胺具有刺激胃肠系统的生理活性和药学上可接受的另外的盐。 构成：由式（1）表示的具有刺激胃肠系统的生理活性的N-（4-哌啶）苯甲酰胺及其药学上可接受的另外的盐：其中L是芳烷基或芳氧基烷基，其中烷基部分是C1-C6 烷基和芳基部分是至多三个独立地选自卤素，C 1 -C 6低级烷基和C 1 -C 6低级烷氧基的取代基; 且R为C1-C6低级烷基。
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公开(公告)号：KR1019990079559A
公开(公告)日：1999-11-05
申请号：KR1019980012218
申请日：1998-04-07
Applicant: 동화약품주식회사
IPC: C07D401/10
Abstract: 본 발명은 신규의 4-치환된 피페리디노테레프탈산 유도체에 관한 것으로서, 더욱 상세하게는 HBV(Hepatitis B virus ; B형 간염 바이러스) 및 HIV(Human Immunodeficiency virus ; 인체 면역결핍 바이러스)에 대한 증식억제효과가 우수하여 항바이러스제로서 유효한 다음 화학식 1로 표시되는 신규의 4-치환된 피페리디노테레프탈산 유도체와 그의 약제학적으로 허용가능한 염, 그리고 그의 제조방법에 관한 것이다.
상기 화학식 1에서
R
1, R
2 및R
3 은 발명의 상세한 설명에서 설명한 바와 같다.
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