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公开(公告)号：KR1020010061857A
公开(公告)日：2001-07-07
申请号：KR1019990064403
申请日：1999-12-29
Applicant: 동화약품주식회사
IPC: C07D213/72
Abstract: PURPOSE: The 3-nitropyridine derivatives and a pharmaceutical composition containing the same are provided, which are useful for inhibiting the growth of hepatitis B virus(HBV) and human immunodeficiency virus(HIV). CONSTITUTION: The 3-nitropyridine derivatives are represented by formula (1), in which R1: is H; hydroxy; C2 to C6 dialkylamino; C2 to C6 linear or branched hydroxyalkyl; C3 to C6 linear or branched dihydroxyalkyl; C3 to C6 alkoxyalkyl; saturated or unsaturated hetero ring compound of 5 or 6 atoms that contains 1 to 3 hetero atoms selected from N, O or S and substituted or unsubstituted by C1 to C3 alkyl; and R1 contains as an asymmetric carbon, R2: is H; or C1 to C4 linear or branched alkyl, or R1 and R2 together form saturated membered hetero ring of 5 or 6 atoms, wherein the 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 3. The pharmaceutical composition contains effective amounts of 3-nitropyridine derivatives.
Abstract translation: 目的：提供3-硝基吡啶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。 构成：3-硝基吡啶衍生物由式（1）表示，其中R1：是H; 羟基; C2〜C6二烷基氨基; C2至C6直链或支链羟烷基; C3至C6直链或支链二羟基烷基; C3至C6烷氧基烷基; 含有1至3个选自N，O或S的杂原子并且被C1至C3烷基取代或未取代的5或6个原子的饱和或不饱和杂环化合物; R1含有不对称碳，R2为H; 或C1至C4直链或支链烷基，或R1和R2一起形成5或6个原子的饱和元杂环，其中该杂环含有1至3个选自N，O和S的杂原子并且被C1至C5取代或未取代 直链或支链烷基，C2至C5直链或支链羟烷基或羟基，R3为吲唑-5-基或吲唑-6-il，n为0至3的整数。该药物组合物含有有效量的3- 硝基吡啶衍生物。
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公开(公告)号：KR1020010048569A
公开(公告)日：2001-06-15
申请号：KR1019990053294
申请日：1999-11-27
Applicant: 동화약품주식회사
IPC: C07D239/10
Abstract: PURPOSE: Novel 5-pyrimidinecarboxamide derivatives inhibiting the growth of HBV and HIV, a pharmaceutically acceptable salt thereof, a preparation thereof and an antiviral composition containing the compound as an effective component are provided, which show less adverse effects and can be effectively used for prevention and treatment of HBV and HIV. CONSTITUTION: The novel 5-pyrimidinecarboxamide derivatives of formula 1 are prepared by the following processes: 4-chloro-2-methylthio-5-pyrimidinecarboxylic acid ethyl ester of formula 2 and 5-aminoindazole or 6-aminoindazole of the formula; R2-NH2 are reacted in the presence of a base to produce 5-pyrimidine carboxylic acid ethyl ester derivative of formula 4; and the obtained 5-pyrimidine carboxylic acid ethyl ester derivative is reacted with an amine compound(R1-NH2). In formula, R1 is H, C1-4 straight or branched alkyl, C3-6 cycloalkyl or C2-3 hydroxyalkyl; R2 is indazole-5-yl or indazole-6-yl.
Abstract translation: 目的：提供抑制HBV和HIV生长的新型5-嘧啶甲酰胺衍生物，其药学上可接受的盐，其制备方法和含有该化合物作为有效成分的抗病毒组合物，其效果较差，可有效用于预防 以及治疗HBV和HIV。 构型：式1的新型5-嘧啶甲酰胺衍生物通过以下方法制备：式2的4-氯-2-甲硫基-5-嘧啶羧酸乙酯和下式的5-氨基吲唑或6-氨基吲唑; R2-NH2在碱的存在下反应，生成式4的5-嘧啶羧酸乙酯衍生物; 并将所得的5-嘧啶羧酸乙酯衍生物与胺化合物（R1-NH2）反应。 在式中，R 1是H，C 1-4直链或支链烷基，C 3-6环烷基或C 2-3羟基烷基; R2是吲唑-5-基或吲唑-6-基。
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公开(公告)号：KR1020010111346A
公开(公告)日：2001-12-17
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：KR1020010096176A
公开(公告)日：2001-11-07
申请号：KR1020000020137
申请日：2000-04-17
Applicant: 동화약품주식회사
IPC: C07D417/06
Abstract: PURPOSE: 6-methylnicotineamide derivatives useful as antiviral agents are provided, thereby inhibiting the growth of hepatitis B virus(HBV), hepatitis C virus(HCV) and human immunodeficiency virus(HIV). CONSTITUTION: The 6-methylnicotineamide derivatives are represented by formula(1), in which R1 is hydroxy, C1 to C5 linear or branched alkyl, C3 to C6 cyclo alkyl, C2 to C6 dialkylamino, or saturated or unsaturated hetero ring having 5 or 6 atoms, in which the hetero ring comprises 1 to 2 hetero atoms selected from N, O or S, and unsubstituted or substituted with C1 to C3 alkyl; and m is an integer of 0 or 1; R2 is hydrogen or C1 to C4 alkyl; or both R1 and R2 form hetero ring having 5 to 6 atoms, in which the hetero ring comprises 1 to 2 hetero atoms selected from N, O or S; and n is an integer of 0 to 4.
Abstract translation: 目的：提供用作抗病毒药物的6-甲基烟酰胺衍生物，从而抑制乙型肝炎病毒（HBV），丙型肝炎病毒（HCV）和人类免疫缺陷病毒（HIV）的生长。 构成：6-甲基烟酰胺衍生物由式（1）表示，其中R1是羟基，C1至C5直链或支链烷基，C3至C6环烷基，C2至C6二烷基氨基或饱和或不饱和杂环，具有5或6 原子，其中杂环包含1至2个选自N，O或S的杂原子，未取代或被C 1至C 3烷基取代; m为0或1的整数; R2是氢或C1-C4烷基; 或者R 1和R 2都形成具有5至6个原子的杂环，其中杂环包含1至2个选自N，O或S的杂原子; n为0〜4的整数。
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公开(公告)号：KR1020010048570A
公开(公告)日：2001-06-15
申请号：KR1019990053295
申请日：1999-11-27
Applicant: 동화약품주식회사
IPC: C07D213/16
Abstract: PURPOSE: Novel 3-nitropyridine derivatives inhibiting the growth of HBV and HIV, a pharmaceutically acceptable salt thereof, a preparation thereof and an antiviral composition containing the compound as an effective component are provided, which show less adverse effects and can be effectively used for prevention and treatment of hapatitis B and HBV and HIV. CONSTITUTION: The novel 3-nitropyridine derivatives of formula 1 are prepared by the following processes: 2-chloro-6-methoxy-3-nitropyridine of formula 2 and 5-aminoindazole or 6-aminoindazole of the formula; R2-NH2 are reacted in the presence of a base to produce 3-nitropyridine derivative of formula 1a and the obtained 3-nitropyridine derivative is reacted with an amine compound(R1-NH2). In formula, R1 is H, C1-4 straight or branched alkylamino or C3-6 cycloalkylamino; R2 is indazole-5-yl or indazole-6-yl.
Abstract translation: 目的：提供抑制HBV和HIV生长的新型3-硝基吡啶衍生物，其药学上可接受的盐，其制备方法和含有该化合物作为有效成分的抗病毒组合物，其具有较少的副作用并可有效地用于预防 和乙型肝炎和乙型肝炎病毒和艾滋病毒的治疗。 构型：式1的新型3-硝基吡啶衍生物通过以下方法制备：式2的2-氯-6-甲氧基-3-硝基吡啶和下式的5-氨基吲唑或6-氨基吲唑; R2-NH2在碱的存在下反应，得到式1a的3-硝基吡啶衍生物，将得到的3-硝基吡啶衍生物与胺化合物（R1-NH2）反应。 在式中，R 1是H，C 1-4直链或支链烷基氨基或C 3-6环烷基氨基; R2是吲唑-5-基或吲唑-6-基。
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Patent Agency Ranking
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：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：KR100609490B1
公开(公告)日：2006-08-09
申请号：KR1020000020137
申请日：2000-04-17
Applicant: 동화약품주식회사
IPC: C07D417/06
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 식에서, R
1 , R
2 및 n은 명세서에 기재된 바와 같다.Abstract translation: 本发明是在小说-6-甲基 - 烟酰胺衍生物的抗病毒剂是有用的，它涉及一种药物组合物，包括制造和他的方法，由通式-6-甲基 - 烟酰胺衍生物（1）具体地，核类化合物是HBV （乙肝病毒）和HCV增殖的（丙型肝炎病毒），以及HIV（人类免疫缺陷病毒），因此也表明抑制乙型肝炎和丙型肝炎的增殖的作用，并且可以是在爱滋病使用的有用的治疗和预防剂 有。
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