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    ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    1.
    发明授权
    ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
    ANIVIRALE 2.4嘧啶二酮衍生物及其生产工艺

    公开(公告)号：EP1159271B1

    公开(公告)日：2004-08-25

    申请号：EP00908087.0

    申请日：2000-03-03

    申请人： Korea Research Institute of Chemical Technology

    发明人： SON, Jong, Chan ,  SHIN, Seun, Shil ,  KIM, Shin, Keol ,  LEE, Chong, Kyo ,  KIM, Hae, Soo

    IPC分类号： C07D239/04 ,  A61K31/495 ,  A61P31/18

    CPC分类号： C07D239/54 ,  C07D239/545 ,  C07D239/62 ,  C07D239/66 ,  C07D401/06

    摘要： 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C¿6-10? aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-6 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O-(C1-6 alkyl)-substituted oximino, C-1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethyl, C1-6 alkoxymethyl, C1-6 acyloxymethyl, carbamoyloxymethyl, aminomethyl, N-(C1-3 alkyl) aminomethyl, N,N-di(C1-3 alkyl) aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl) amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl) carbamoyl, aminocarbamoyl, dimethylaminocarbamoyl, hydrazino, 1,1-dimethylhydrazino, imidazolyl, triazolyl and tetrazolyl; a tetrahydropyridyl or piperidyl group optionally substituted with a C1-6 alkyl or C1-6 alkoxycarbonyl group; a tetrahydropyranyl group; or a tetrahydrofuryl group; R?2¿ is hydrogen, halogen, nitro, cyano, C¿1-3? alkoxycarbonyl, C1-3 alkylamino, di(C1-3 alkyl) amino, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl, C1-6 alkyl, C3-6 cycloalkyl or benzyl; R?3 and R4¿ are each independently hydrogen, halogen, hydroxy, cyano, nitro, amino, acetamido, trifluoroacetamido, azido, C¿1-3? alkyl, C1-3 alkyl substituted with one or more halogen atoms, C1-3 alkoxycarbonyl, carbamoyl, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl or C1-3 alkoxy; A is O or S; and Z is O, S, C=O, NH or CH2.

    ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    4.
    发明公开
    ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
    ANIVIRALE 2.4嘧啶二酮衍生物及其生产工艺

    公开(公告)号：EP1159271A1

    公开(公告)日：2001-12-05

    申请号：EP00908087.0

    申请日：2000-03-03

    申请人： Korea Research Institute of Chemical Technology

    发明人： SON, Jong, Chan ,  SHIN, Seun, Shil ,  KIM, Shin, Keol ,  LEE, Chong, Kyo ,  KIM, Hae, Soo

    IPC分类号： C07D239/04 ,  A61K31/495

    CPC分类号： C07D239/54 ,  C07D239/545 ,  C07D239/62 ,  C07D239/66 ,  C07D401/06

    摘要： 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C¿6-10? aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-6 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O-(C1-6 alkyl)-substituted oximino, C-1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethyl, C1-6 alkoxymethyl, C1-6 acyloxymethyl, carbamoyloxymethyl, aminomethyl, N-(C1-3 alkyl) aminomethyl, N,N-di(C1-3 alkyl) aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl) amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl) carbamoyl, aminocarbamoyl, dimethylaminocarbamoyl, hydrazino, 1,1-dimethylhydrazino, imidazolyl, triazolyl and tetrazolyl; a tetrahydropyridyl or piperidyl group optionally substituted with a C1-6 alkyl or C1-6 alkoxycarbonyl group; a tetrahydropyranyl group; or a tetrahydrofuryl group; R?2¿ is hydrogen, halogen, nitro, cyano, C¿1-3? alkoxycarbonyl, C1-3 alkylamino, di(C1-3 alkyl) amino, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl, C1-6 alkyl, C3-6 cycloalkyl or benzyl; R?3 and R4¿ are each independently hydrogen, halogen, hydroxy, cyano, nitro, amino, acetamido, trifluoroacetamido, azido, C¿1-3? alkyl, C1-3 alkyl substituted with one or more halogen atoms, C1-3 alkoxycarbonyl, carbamoyl, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl or C1-3 alkoxy; A is O or S; and Z is O, S, C=O, NH or CH2.

    NOVEL ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
    6.
    发明公开
    NOVEL ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF 失效
    新的抗病毒2.4嘧啶二酮衍生物及其制造方法

    公开(公告)号：EP0736015A1

    公开(公告)日：1996-10-09

    申请号：EP95903455.0

    申请日：1994-12-20

    申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

    发明人： SON, Jong, Chan ,  LEE, Ill, Young ,  BAE, Byung, Il ,  HAN, Jeong, Sik ,  CHOI, Joong, Kwon ,  CHAE, Yung, Bok

    IPC分类号： C07D239 ,  A61K31 ,  A61P31

    CPC分类号： C07D239/54 ,  C07D239/60

    摘要： Novel 2,4-pyrimidinedione compounds, and pharmaceutically acceptable salts thereof which possess good antiviral activities, and specifically represented by formula (I) wherein: R1 represents an unsubstituted or substituted alkyl group represented by CH¿2?CH=CR?5R6¿ or an unsubstituted or substituted propargyl group represented by CH¿2?C CR?7¿ wherein R?5, R6 and R7¿ are each independently a hydrogen atom; a methyl group optionally substituted with a halogen atom, or a C¿1-10? carbonyloxy, hydroxy, azido, cyano, optionally substituted amino, optionally substituted phosphonyl, optionally substituted phenyl, C3-10 heteroaryl, C1-3 alkoxy or benzyloxy radical; a C2-10 alkyl or alkenyl group; a cyclopropyl group; an optionally substituted phenyl group; a C3-10 heteroaryl group; a C1-10 ester group; or an optionally substituted C1-10 alkylamide group; R?2¿ represents a halogen atom, an optionally substituted C¿1-5? alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl group or a benzyl group; R?3 and R4¿ represent independently a hydrogen or halogen atom, or a hydroxy, C¿1-3? alkyl, fluoromethyl, C1-3 alkoxy, amino, C2-6 alkylester or C2-7 alkylamide group; A represents an oxygen or sulfur atom; Z represents an oxygen or sulfur atom; a carbonyl group; an amino group; or a methylene group optionally substituted with at least one selected from the group consisting of a halogen atom, and a cyano, hydroxy, azido, amino, C1-3 alkylamide, C1-4 ester, and nitro groups.

    ANTIVIRAL 2,4-PYRIMIDINDIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
    9.
    发明授权
    ANTIVIRAL 2,4-PYRIMIDINDIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF 失效
    抗病毒2.4嘧啶二酮衍生物和工艺及其

    公开(公告)号：EP0736015B1

    公开(公告)日：2001-03-07

    申请号：EP95903455.4

    申请日：1994-12-20

    申请人： KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

    发明人： SON, Jong, Chan ,  LEE, Ill, Young ,  BAE, Byung, Il ,  HAN, Jeong, Sik ,  CHOI, Joong, Kwon ,  CHAE, Yung, Bok

    IPC分类号： C07D239/60 ,  C07D239/54 ,  A61K31/505

    CPC分类号： C07D239/54 ,  C07D239/60

    摘要： Novel 2,4-pyrimidinedione compounds, and pharmaceutically acceptable salts thereof which possess good antiviral activities, and specifically represented by formula (I) wherein: R1 represents an unsubstituted or substituted alkyl group represented by CH¿2?CH=CR?5R6¿ or an unsubstituted or substituted propargyl group represented by CH¿2?C CR?7¿ wherein R?5, R6 and R7¿ are each independently a hydrogen atom; a methyl group optionally substituted with a halogen atom, or a C¿1-10? carbonyloxy, hydroxy, azido, cyano, optionally substituted amino, optionally substituted phosphonyl, optionally substituted phenyl, C3-10 heteroaryl, C1-3 alkoxy or benzyloxy radical; a C2-10 alkyl or alkenyl group; a cyclopropyl group; an optionally substituted phenyl group; a C3-10 heteroaryl group; a C1-10 ester group; or an optionally substituted C1-10 alkylamide group; R?2¿ represents a halogen atom, an optionally substituted C¿1-5? alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl group or a benzyl group; R?3 and R4¿ represent independently a hydrogen or halogen atom, or a hydroxy, C¿1-3? alkyl, fluoromethyl, C1-3 alkoxy, amino, C2-6 alkylester or C2-7 alkylamide group; A represents an oxygen or sulfur atom; Z represents an oxygen or sulfur atom; a carbonyl group; an amino group; or a methylene group optionally substituted with at least one selected from the group consisting of a halogen atom, and a cyano, hydroxy, azido, amino, C1-3 alkylamide, C1-4 ester, and nitro groups.