Cyanoguanidines as cell proliferation inhibitors
    1.
    发明授权
    Cyanoguanidines as cell proliferation inhibitors 有权
    氰基胍作为细胞增殖抑制剂

    公开(公告)号:US06346541B1

    公开(公告)日:2002-02-12

    申请号:US09424632

    申请日:1999-11-26

    IPC分类号: A61K3144

    CPC分类号: C07D213/75

    摘要: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C4-C20 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino and Y stands for benzylene or phenylene and R2 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, C1-C4 alkyl, hydroxyalkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl, nitro, amino, carboxy, alkoxycarbonyl or benzyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.

    摘要翻译: 本发明涉及迄今为止未知的式(I)化合物或其互变异构形式,其中吡啶环位于3-或4-位,其中R 1表示一个或多个可相同的取代基或 不同的并且选自氢,卤素,三氟甲基,羧基,C 1 -C 4烷基,烷氧基或烷氧基羰基,硝基,氨基或氰基,Q代表可以是直链,支链,环状的C 4 -C 20二价烃基 ,饱和或不饱和的,X代表羰基,羰基氨基,氨基羰基,氧羰基氧基,氧羰基,羰基氧基,氨基羰基氧基,氨基硫代羰基氧基,氧羰基氨基或氧硫基羰基氨基,Y代表亚苄基或亚苯基,R2代表一个或多个相同或不同的取代基, 选自:氢,C 1 -C 4烷基,羟基烷基或烷氧基,羟基,卤素,三氟甲基,氰基,甲酰胺基,氨磺酰基,硝基,氨基 不,羧基,烷氧基羰基或苄氧基; 和其药学上可接受的无毒盐和N-氧化物。 本化合物在人类和兽医实践中是有价值的。

    Cyanoguanidines as cell proliferation inhibitors
    2.
    发明授权
    Cyanoguanidines as cell proliferation inhibitors 失效
    氰基胍类作为细胞增殖抑制剂

    公开(公告)号:US06197797B1

    公开(公告)日:2001-03-06

    申请号:US09424630

    申请日:1999-11-26

    IPC分类号: A61K3144

    CPC分类号: C07D213/75

    摘要: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl nitro, amino, cyano, carboxy, or alkyl, alkoxy, or alkoxycarbonyl, the C-content of which can be from 1 to 4; X stands for a straight or branched C9-C20 carbon chain, saturated or unsaturated or Q—Ar—R; in which formula Ar stands for phenyl, Q stands for a C5-C20 divalent hydrocarbon radical which can be straight, branched, saturated or unsaturated and R stands for hydrogen or for one or more substituents which can be the same or different and are selected from the group consisting of: hydroxy, amino, halogen, trifluoromethyl, cyano, nitro, carboxy, carbamoyl, or alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 4; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.

    摘要翻译: 本发明涉及迄今为止未知的式(I)化合物或其互变异构形式,其中吡啶与3-或4-位的连接,式R1代表一个或多个可相同或不同的取代基 并且选自:氢,卤素,硝基三氟甲基,氨基,氰基,羧基或烷基,烷氧基或烷氧基羰基,其C含量可以为1至4; X代表饱和或不饱和的直链或支链C 9 -C 20碳链或Q-Ar-R; 其中式Ar代表苯基,Q代表可以是直链,支链,饱和或不饱和的C 5 -C 20二价烃基,R代表氢或一个或多个相同或不同的取代基,选自 由羟基,氨基,卤素,三氟甲基,氰基,硝基,羧基,氨基甲酰基或烷基,烷氧基,烷硫基,烷基氨基或烷氧基羰基组成的基团,其C含量可以为1至4; 和其药学上可接受的无毒盐和N-氧化物。 本化合物在人类和兽医实践中是有价值的。

    Cyanoguanidines as cell proliferation inhibitors
    3.
    发明授权
    Cyanoguanidines as cell proliferation inhibitors 有权
    氰基胍作为细胞增殖抑制剂

    公开(公告)号:US06346520B1

    公开(公告)日:2002-02-12

    申请号:US09424631

    申请日:1999-11-26

    IPC分类号: A61K3144

    CPC分类号: C07D213/75 C07D405/12

    摘要: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C5-C14 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carboxy, C1-C4 alkoxycarbonyl, di(C1-C4 alkoxy)phosphinoyloxy, amino, C1-C4 alkoxycarbonylamino or tetrahydropyranyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.

    摘要翻译: 本发明涉及迄今为止未知的式(I)化合物或其互变异构形式,其中吡啶环在3-或4-位上的连接,其中式R代表一个或多个可相同的取代基或 不同的并且选自氢,卤素,三氟甲基,羧基,C 1 -C 4烷基,烷氧基或烷氧基羰基,硝基,氨基或氰基,Q代表C5-C14二价烃基,其可以是直链,支链,环状 ,饱和或不饱和的,X代表羧基,C 1 -C 4烷氧基羰基,二(C 1 -C 4烷氧基)膦酰氧基,氨基,C 1 -C 4烷氧羰基氨基或四氢吡喃氧基; 和其药学上可接受的无毒盐和N-氧化物。 本化合物在人类和兽医实践中是有价值的。

    Cyanoguanidines as cell proliferation inhibitors
    5.
    发明授权
    Cyanoguanidines as cell proliferation inhibitors 有权
    氰基胍作为细胞增殖抑制剂

    公开(公告)号:US06646129B2

    公开(公告)日:2003-11-11

    申请号:US10061204

    申请日:2002-02-04

    IPC分类号: C07D40512

    CPC分类号: C07D213/75 C07D405/12

    摘要: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C5-C14 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carboxy, C1-C4 alkoxycarbonyl, di(C1-C4 alkoxy)-phosphinoyloxy, amino, C1-C4 alkoxycarbonylamino or tetrahydropyranyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.

    摘要翻译: 本发明涉及迄今为止未知的式(I)化合物或其互变异构形式,其中吡啶环在3-或4-位上的连接,其中式R代表一个或多个可相同的取代基或 不同的并且选自氢,卤素,三氟甲基,羧基,C 1 -C 4烷基,烷氧基或烷氧基羰基,硝基,氨基或氰基,Q代表C 5 -C 14二价烃基,其可以是直链,支链,环状 ,饱和或不饱和的,X代表羧基,C 1 -C 4烷氧基羰基,二(C 1 -C 4烷氧基) - 膦酰氧基,氨基,C 1 -C 4烷氧羰基氨基或四氢吡喃氧基; 和其药学上可接受的无毒盐和N-氧化物。 本化合物在人类和兽医实践中是有价值的。