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    • 4. 发明申请
    • 4-[4-(4-MORPHOLINO)ANILINO]PYRIMIDINE DERIVATIVES, METHOD FOR PREPARING THEREOF AND ANTIVIRAL PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
    • 4- [4-(4-吗啉基)苯胺基]吡啶衍生物,其制备方法和包含其的抗病毒药物组合物
    • WO2004108068A3
    • 2005-02-17
    • PCT/KR2004001297
    • 2004-06-01
    • B & C BIOPHARM CO LTDKIM JONG-WOOLEE SANG-WOOKLEE GEUN-HYUNGHAN JAE-JINPARK SANG-JINPARK EUL-YONGSHIN JOONG-CHUL
    • KIM JONG-WOOLEE SANG-WOOKLEE GEUN-HYUNGHAN JAE-JINPARK SANG-JINPARK EUL-YONGSHIN JOONG-CHUL
    • C07D413/12A61K20060101
    • C07D239/47
    • The present invention relates to 4-[4-(4-morpholino)anilino]pyrimidine derivatives useful as an antiviral agent, and more particularly novel 4-[4-(4-morpholino)anilino]pyrimidine derivatives having an excellent inhibitory effect on replication of Hepatitis C virus (HCV), represented by the following formula I: in which R1 represents C1-C4 straight or branched alkoxy group, -NR2R3 group or 4-(R4)-piperazin-l-yl group; R2 represents hydrogen or C1-C4 straight or branched alkyl group; R3 represents C1-C4 straight or branched alkyl group, C1-C4 straight or branched hydroxyalkyl group, C1-C4 straight or branched alkyl group substituted by C2-C6 straight or branched dialkylamino group or C1-C4 straight or branched alkyl group substituted by heterocyclic ring; R4 represents C1-C4 straight or branched alkoxycarbonylmethyl group, carboxymethyl group or -CH2-CO-NH-R5 group; and R5 represents C1-C4 straight or branched alkyl group, C1-C4 straight or branched hydroxyalkyl group, C3-C6 cycloalkyl group or C1-C4 straight or branched alkyl group substituted by heterocyclic ring; and pharmaceutically acceptable salts thereof, a preparation method thereof, and an antiviral pharmaceutical composition comprising the compound as an effective component. The 4-[4-(4-morpholino)anilino]pyrimidine derivatives according to the present invention have an excellent inhibitory effect on replication of Hepatitis C virus (HCV) and thus can be advantageously used as a therapeutic or prophylactic agent of hepatitis C.
    • 本发明涉及可用作抗病毒剂的4- [4-(4-吗啉代)苯胺基]嘧啶衍生物,更特别地涉及对复制具有优异抑制作用的更具体的新型4- [4-(4-吗啉代)苯胺基]嘧啶衍生物 由下式I表示的丙型肝炎病毒(HCV):其中R1表示C1-C4直链或支链烷氧基,-NR2R3基或4-(R4) - 哌嗪-1-基; R2表示氢或C1-C4直链或支链烷基; R3表示C1-C4直链或支链烷基,C1-C4直链或支链羟烷基,被C2-C6直链或支链二烷基氨基取代的C1-C4直链或支链烷基或被杂环取代的C1-C4直链或支链烷基 环; R4表示C1-C4直链或支链烷氧基羰基甲基,羧甲基或-CH2-CO-NH-R5基团; R5表示C1-C4直链或支链烷基,C1-C4直链或支链羟烷基,C3-C6环烷基或被杂环取代的C1-C4直链或支链烷基; 及其药学上可接受的盐,其制备方法和包含该化合物作为有效成分的抗病毒药物组合物。 根据本发明的4- [4-(4-吗啉代)苯胺基]嘧啶衍生物对丙型肝炎病毒(HCV)的复制具有优异的抑制作用,因此可有利地用作丙型肝炎的治疗或预防剂。
    • 5. 发明申请
    • 4-[4-(4-MORPHOLINO)ANILINO]PYRIMIDINE DERIVATIVES, METHOD FOR PREPARING THEREOF AND ANTIVIRAL PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
    • 4- [4-(4-吗啉基)苯胺基]吡啶衍生物,其制备方法和包含其的抗病毒药物组合物
    • WO2004108068A2
    • 2004-12-16
    • PCT/KR2004/001297
    • 2004-06-01
    • B & C BIOPHARM CO., LTD.KIM, Jong-WooLEE, Sang-WookLEE, Geun-HyungHAN, Jae-JinPARK, Sang-JinPARK, Eul-YongSHIN, Joong-Chul
    • KIM, Jong-WooLEE, Sang-WookLEE, Geun-HyungHAN, Jae-JinPARK, Sang-JinPARK, Eul-YongSHIN, Joong-Chul
    • A61K
    • C07D239/47
    • The present invention relates to 4-[4-(4-morpholino)anilino]pyrimidine derivatives useful as an antiviral agent, and more particularly novel 4-[4-(4-morpholino)anilino]pyrimidine derivatives having an excellent inhibitory effect on replication of Hepatitis C virus (HCV), represented by the following formula I: in which R 1 represents C 1 -C 4 straight or branched alkoxy group, -NR 2 R 3 group or 4-(R 4 )-piperazin-l-yl group; R 2 represents hydrogen or C 1 -C 4 straight or branched alkyl group; R 3 represents C 1 -C 4 straight or branched alkyl group, C 1 -C 4 straight or branched hydroxyalkyl group, C 1 -C 4 straight or branched alkyl group substituted by C 2 -C 6 straight or branched dialkylamino group or C 1 -C 4 straight or branched alkyl group substituted by heterocyclic ring; R 4 represents C 1 -C 4 straight or branched alkoxycarbonylmethyl group, carboxymethyl group or -CH 2 -CO-NH-R 5 group; and R 5 represents C 1 -C 4 straight or branched alkyl group, C 1 -C 4 straight or branched hydroxyalkyl group, C 3 -C 6 cycloalkyl group or C 1 -C 4 straight or branched alkyl group substituted by heterocyclic ring; and pharmaceutically acceptable salts thereof, a preparation method thereof, and an antiviral pharmaceutical composition comprising the compound as an effective component. The 4-[4-(4-morpholino)anilino]pyrimidine derivatives according to the present invention have an excellent inhibitory effect on replication of Hepatitis C virus (HCV) and thus can be advantageously used as a therapeutic or prophylactic agent of hepatitis C.
    • 本发明涉及可用作抗病毒剂的4- [4-(4-吗啉代)苯胺基]嘧啶衍生物,更特别地涉及对复制具有优异抑制作用的更具体的新型4- [4-(4-吗啉代)苯胺基]嘧啶衍生物 由下式I表示的丙型肝炎病毒(HCV):其中R1表示C1-C4直链或支链烷氧基,-NR2R3基或4-(R4) - 哌嗪-1-基; R2表示氢或C1-C4直链或支链烷基; R3表示C1-C4直链或支链烷基,C1-C4直链或支链羟烷基,被C2-C6直链或支链二烷基氨基取代的C1-C4直链或支链烷基或被杂环取代的C1-C4直链或支链烷基 环; R4表示C1-C4直链或支链烷氧基羰基甲基,羧甲基或-CH2-CO-NH-R5基团; R5表示C1-C4直链或支链烷基,C1-C4直链或支链羟烷基,C3-C6环烷基或被杂环取代的C1-C4直链或支链烷基; 及其药学上可接受的盐,其制备方法和包含该化合物作为有效成分的抗病毒药物组合物。 根据本发明的4- [4-(4-吗啉代)苯胺基]嘧啶衍生物对丙型肝炎病毒(HCV)的复制具有优异的抑制作用,因此可有利地用作丙型肝炎的治疗或预防剂。