ANTIVIRAL PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    2.
    发明公开
    ANTIVIRAL PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
    抗病毒嘧啶二酮衍生物及其制造方法

    公开(公告)号:EP1100786A1

    公开(公告)日:2001-05-23

    申请号:EP00921122.8

    申请日:2000-04-08

    IPC分类号: C07D239/54

    摘要: The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or tri-substituted phenyl with a group selected from hydroxy, C1-C4 alkyl, C1-C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1-C4 alkyl, C1-C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1-C4 alkoxycarbonyl; C1-C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1-C4 alkyl, R2 and R3 represent independently hydrogen or C1-C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.

    ANTIVIRAL PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    3.
    发明授权
    ANTIVIRAL PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
    抗病毒嘧啶二酮衍生物及其制造方法

    公开(公告)号:EP1100786B1

    公开(公告)日:2004-07-21

    申请号:EP00921122.8

    申请日:2000-04-08

    IPC分类号: C07D239/54

    摘要: The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or tri-substituted phenyl with a group selected from hydroxy, C1-C4 alkyl, C1-C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1-C4 alkyl, C1-C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1-C4 alkoxycarbonyl; C1-C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1-C4 alkyl, R2 and R3 represent independently hydrogen or C1-C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.

    PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    5.
    发明公开
    PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
    哌嗪及其制备方法

    公开(公告)号:EP1075469A1

    公开(公告)日:2001-02-14

    申请号:EP00908085.4

    申请日:2000-03-03

    摘要: The present invention relates to a novel compound of general formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antitumor activities and very low toxicity, wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 hydroxyalkyl, C1-C4 aminoalkyl or C1-C4 hydroxyiminoalkyl, or R1 and R2 are fused to form C3-C4 unsaturated ring; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, amino, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy or C1-C4 thioalkoxy; R8 is C1-C4 alkyl; Y is oxygen, sulphur, amino, substituted amino or C1-C4 thioalkyl; Z is C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino or C1-C4 thioalkoxy; X1 and X2 are independently carbon or nitrogen; and -N--C- and -C--Y- may form a single bond or a double bond provided that if -N--C- forms a single bond, -C--Y- forms a double bond, and if -C--Y- forms a single bond, -N--C- forms a double bond and R8 is nonexistent.

    PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    7.
    发明授权
    PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 有权
    哌嗪及其制备方法

    公开(公告)号:EP1075469B1

    公开(公告)日:2004-05-26

    申请号:EP00908085.4

    申请日:2000-03-03

    摘要: The present invention relates to a novel compound of general formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antitumor activities and very low toxicity, wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 hydroxyalkyl, C1-C4 aminoalkyl or C1-C4 hydroxyiminoalkyl, or R1 and R2 are fused to form C3-C4 unsaturated ring; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, amino, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy or C1-C4 thioalkoxy; R8 is C1-C4 alkyl; Y is oxygen, sulphur, amino, substituted amino or C1-C4 thioalkyl; Z is C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino or C1-C4 thioalkoxy; X1 and X2 are independently carbon or nitrogen; and -N--C- and -C--Y- may form a single bond or a double bond provided that if -N--C- forms a single bond, -C--Y- forms a double bond, and if -C--Y- forms a single bond, -N--C- forms a double bond and R8 is nonexistent.

    PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    9.
    发明授权
    PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 失效
    哌嗪衍生物和工艺及其

    公开(公告)号:EP0850222B1

    公开(公告)日:2003-05-28

    申请号:EP97930868.1

    申请日:1997-06-28

    摘要: The present invention relates to novel compound having strong antitumor activities of general formula (I), wherein R1 and R2 are independently hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted C3-C6 cycloalkyl, substituted or unsubstituted C2-C8 unsaturated alkyl, ketone, substituted or unsubstituted aryl, substituted or unsubstituted C1-C4 alkoxy, substituted or unsubstituted arylhydroxy, substituted or unsubstituted amino, C1-C4 lower ester, C1-C4 lower thioester, thiol, substituted or unsubstituted carboxyl, epoxy, substituted or unsubstituted C1-C4 lower thioalkoxy; or R1 and R2 are fused to form C3-C4 saturated or unsaturated chain; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, C1-C4 lower ester, C1-C4 lower alkyl, C1-C4 lower thioalkyl, substituted or unsubstituted C3-C6 cycloalkyl, C1-C4 lower alkoxy, C1-C4 lower thioalkoxy, substituted or unsubstituted aryl, substituted or unsubstituted lower arylalkoxy, substituted or unsubstituted lower alkylamino, or lower alkyl substituted or unsubstituted carbamate; or among R3, R4, R5, R6 and R7, two adjacent groups are bonded with each other to form 1,2-phenylene or 2,3-naphthylene; X is oxygen, sulfur, or substituted or unsubstituted imino; Y is bonded at the 3-position or 4-position of the aromatic ring part wherein Y is oxygen or -NR8- (wherein, R8 is the same with the above-mentioned R3); Z is hydroxy, C1-C4 lower alkoxy, C1-C4 lower thioalkoxy, substituted or unsubstituted aryloxy, C1-C4 lower alkylamino, substituted or unsubstituted cycloamino containing 1-5 nitrogen atoms; A is nitrogen or -CH=; its pharmaceutically acceptable acid addition salts and process for the preparation thereof.

    9-AMINOACRIDINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    10.
    发明公开
    9-AMINOACRIDINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
    9-氨基吖啶衍生物AND PROCESS FOR THEIR

    公开(公告)号:EP1062207A1

    公开(公告)日:2000-12-27

    申请号:EP99959999.6

    申请日:1999-12-17

    IPC分类号: C07D219/10

    CPC分类号: C07D219/10 Y02P20/55

    摘要: The present invention relates to new 9-aminoacridine derivatives of general formula (I), wherein A is hydrogen or (II) (wherein X is oxygen or sulfur, R1, R2, R3, R4 and R5 are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkyloxycarbonyl and m and n are independently an integer of 0, 1 or 2), R6, R7, R8 and R9 are independently C1-C8 alkyl or C1-C4 lower alkoxy, and Y is hydrogen, amino, -N=CHR'(wherein R' is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino), (III) (wherein R'' is hydrogen, benzyl, C1-C8 alkyl or C1-C6 lower alkylamino, and R''' is hydrogen, benzyl, C1-C8 alkyl or amino protecting group) or (IV) (wherein, X is as defined above, R1', R2', R3', R4' and R5' are independently hydrogen, halogen, nitro, amino, hydroxy, C1-C4 lower alkylhydroxy, C1-C4 lower alkylamino, C1-C8 alkyl, C1-C4 lower alkoxy or C1-C4 lower alkylcarboxy, and q and r are independently an integer of 0, 1 or 2) or its pharmaceutically acceptable salt, and process for the preparation thereof.