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9 条记录 (耗时 0.014 秒)

    Substituted pyrimidin-2-ones and the salts thereof
    1.
    发明公开
    Substituted pyrimidin-2-ones and the salts thereof 失效
    取代的吡咯烷二酮及其盐

    公开(公告)号：EP0056319A3

    公开(公告)日：1982-10-27

    申请号：EP82300106

    申请日：1982-01-08

    申请人： NYEGAARD & CO. A/S

    发明人： Benneche, Tore ,  Undheim, Kjell

    IPC分类号： C07D239/36 ,  C07D403/12 ,  C07D409/12 ,  A61K31/505 ,  C07D239/38

    CPC分类号： C07D239/36 ,  C07D239/38

    摘要： Compounds of the general formula:
    (wherein
    X represents a halogen atom or a trifluoromethyl group; R 1 and R 2 independently represent a hydrogen atom or a lower alkyl group; Z is -0-, -S-, -SO-, -SO 2 - or the group -NR 4 -wherein R 4 is as defined for R hereinafter or represents the group COR 5 in which R 5 represents a hydrogen atom or an optionally substituted aryl, heterocyclic, aralkyl, lower alkyl or lower alkoxy group; R represents a C 6-10 carbocyclic aromatic group or a heterocyclic group containing a 5-9 membered unsaturated or aromatic heterocyclic ring which ring contains one or more heteroatoms selected from 0, N and S and optionally carries a fused ring which carbocyclic or heterocyclic group may carry one or more C 1-4 alkyl or phenyl groups, said groups being optionally substituted; or, where Z represents the group >R 4 , the group -ZR may represent a heterocyclic ring optionally carrying a fused ring and/or optionally substituted as defined for R; and R 3 represents a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl, lower alkanoyl, lower alkenoyl, C 7-16 aralkyl or C 6-10 aryl group or a 5-9 membered unsaturated or aromatic heterocyclic ring); and, where acid or basic groups are present, the salts thereof; are useful in combating abnormal cell proliferation. The compounds of the invention are prepared by inter alia alkylation, ring closure and oxidation.

    5-Halo-pyrimidin-2-ones, the salts thereof, processes for their preparation and pharmaceutical compositions containing them
    3.
    发明公开
    5-Halo-pyrimidin-2-ones, the salts thereof, processes for their preparation and pharmaceutical compositions containing them 失效
    5-卤代 - 嘧啶-2-酮，它们的盐，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0032131A1

    公开(公告)日：1981-07-15

    申请号：EP81300031.2

    申请日：1981-01-06

    申请人： NYEGAARD & CO. A/S

    发明人： Gacek, Mikkel Josef ,  Undheim, Kjell

    IPC分类号： C07D409/06 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  A61K31/505

    CPC分类号： C07D239/30 ,  C07D243/08 ,  C07D277/42 ,  C07D277/56 ,  C07D333/16 ,  C07D333/28

    摘要： Compounds of the formula :-
    (wherein

    X represents a halogen atom;
    R' and R 2 , which may be the same or different, each represents a hydrogen atom, or a C 1-4 alkyl group;
    Het represents a C-attached 3-9 membered, saturated, unsaturated or aromatic heterocyclic ring containing one or more hetero atoms selected from 0,N and S and optionally carrying a fused ring and/or optionally substituted by one or more substituents; and
    alk represents a C 1-4 saturated or unsaturated, straight or branched chain, divalent aliphatic hydrocarbyl group optionally substituted and, where an acidic or basic group is present, the salts thereof have been found to possess metaphase arresting ability which by virtue of its reversibility is of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered whilst the abnormal cells are in a phase susceptible to attack and whilst the normal cells are in a non-susceptible phase.

    The compounds of the invention are prepared by alkylation, ring closure of the pyrimidine ring, halogenation, ring closure of the heterocyclic ring Het or dehydrazination.

    Substituted pyrimidin-2-ones and the salts thereof
    6.
    发明公开
    Substituted pyrimidin-2-ones and the salts thereof 失效
    取代的嘧啶-2-酮及其盐。

    公开(公告)号：EP0056319A2

    公开(公告)日：1982-07-21

    申请号：EP82300106.0

    申请日：1982-01-08

    申请人： NYEGAARD & CO. A/S

    发明人： Benneche, Tore ,  Undheim, Kjell

    IPC分类号： C07D239/36 ,  C07D403/12 ,  C07D409/12 ,  A61K31/505

    CPC分类号： C07D239/36 ,  C07D239/38

    摘要： Compounds of the general formula:
    (wherein

    X represents a halogen atom or a trifluoromethyl group;
    R 1 and R 2 independently represent a hydrogen atom or a lower alkyl group;
    Z is -0-, -S-, -SO-, -SO 2 - or the group -NR 4 -wherein R 4 is as defined for R hereinafter or represents the group COR 5 in which R 5 represents a hydrogen atom or an optionally substituted aryl, heterocyclic, aralkyl, lower alkyl or lower alkoxy group;
    R represents a C 6-10 carbocyclic aromatic group or a heterocyclic group containing a 5-9 membered unsaturated or aromatic heterocyclic ring which ring contains one or more heteroatoms selected from 0, N and S and optionally carries a fused ring which carbocyclic or heterocyclic group may carry one or more C 1-4 alkyl or phenyl groups, said groups being optionally substituted; or, where Z represents the group >R 4 , the group -ZR may represent a heterocyclic ring optionally carrying a fused ring and/or optionally substituted as defined for R; and
    R 3 represents a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl, lower alkanoyl, lower alkenoyl, C 7-16 aralkyl or C 6-10 aryl group or a 5-9 membered unsaturated or aromatic heterocyclic ring); and, where acid or basic groups are present, the salts thereof; are useful in combating abnormal cell proliferation.

    The compounds of the invention are prepared by inter alia alkylation, ring closure and oxidation.

    Substituted pyrimid-2-ones, the salts thereof, processes for their preparation and pharmaceutical compositions containing them
    9.
    发明公开
    Substituted pyrimid-2-ones, the salts thereof, processes for their preparation and pharmaceutical compositions containing them 失效
    取代的嘧啶-2-酮，它们的盐，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0074820A1

    公开(公告)日：1983-03-23

    申请号：EP82304780.8

    申请日：1982-09-10

    申请人： NYEGAARD & CO. A/S

    发明人： Benneche, Tore ,  Gacek, Mikkel Josef ,  Undheim, Kjell

    IPC分类号： C07D239/36 ,  A61K31/505

    CPC分类号： C07D239/36 ,  A61K31/70 ,  C07D401/12 ,  C07D409/12 ,  A61K31/505 ,  A61K2300/00

    摘要： Compounds of general formula:
    (wherein X represents a halogen atom or a trifluoromethyl group; R 1 and R 2 , which may be the same or different, each represents a hydrogen atom, or a C 1-4 alkyl group, and R 3 represents a hydrogen atom or a C 1-5 saturated or unsaturated, straight or branched acyclic aliphatic group; a C34 saturated or unsaturated cyclic aliphatic group; a heterocyclic substituted aliphatic group; an araliphatic group; or a heterocyclic or carbocyclic aryl group; any of said groups optionally carrying one or more substituents selected from halogen, oxo, hydroxy, mercapto, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyloxy and amino) and, where an acidic or basic group is present, physiologically compatible salts thereof have been found to be of use in combating abnormal cell proliferation.
    The compounds of formula I may be prepared by reaction of a 5-halo- or 5-trifluoromethyl-pyrimidin-2-one with an appropriate isocyanate.