Cinnamamide derivatives and drug compositions containing the same
    1.
    发明授权
    Cinnamamide derivatives and drug compositions containing the same 失效
    肉桂酰胺衍生物和含有它们的药物组合物

    公开(公告)号:US06413995B1

    公开(公告)日:2002-07-02

    申请号:US09856419

    申请日:2001-05-21

    IPC分类号: C07D21340

    CPC分类号: C07D213/40

    摘要: The invention relates to cinnamamide derivatives having the following formula wherein R1 represents a hydroxyl group, a C1-6-alkoxy group, an arylalkoxy group or a substituted or unsubstituted amino group; R2 and R3 are same or different, each of which represents a hydrogen atom, a halogen atom or a C1-4-alkyl group; R4 represents a hydrogen atom or a C1-6-alkyl group; R5 represents a hydrogen atom, a C1-6-alkyl group or an aryl group; R6 represents a hydrogen atom, a C1-6-alkyl group, a cyano group or a C1-6-alkoxy-carbonyl group; W represents an oxygen atom, a sulfur atom, an imino group, a methylene group, a hydroxymethylene group or a carbonyl group; X and Y are same or different, each of which represents an oxygen atom or a sulfur atom; m represents an integer of 0 to 2; n represents an integer of 1 to 3; and when m is 0, a group: —C(R2)(R3)—W— may represent a vinylene group; or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the above compound, in particular, an immunomodulatory agent and a prophylactic or therapeutic agent for nephrotic syndrome, circulatory disorders or respiratory diseases.

    摘要翻译: 本发明涉及具有下列化学式的肉桂酰胺衍生物:R1表示羟基,C1-6-烷氧基,芳基烷氧基或取代或未取代的氨基; R2和R3相同或不同,各自表示氢原子, 卤素原子或C 1-4 - 烷基; R 4表示氢原子或C 1-6 - 烷基; R 5表示氢原子,C 1-6 - 烷基或芳基; R 6表示氢原子, C 1-6 - 烷基,氰基或C 1-6 - 烷氧基 - 羰基; W表示氧原子,硫原子,亚氨基,亚甲基,羟基亚甲基或羰基; X和 Y相同或不同,各自表示氧原子或硫原子; m表示0〜2的整数,n表示1〜3的整数, 并且当m为0时,基团-C(R 2)(R 3)-W-可以表示亚乙烯基;或其药学上可接受的盐; 以及含有上述化合物,特别是免疫调节剂,肾病综合征,循环障碍或呼吸系统疾病的预防或治疗剂的药物组合物。

    Compositions and methods for treating nephritis and inhibiting TGF -&bgr; related conditions using pyridylacrylamide derivatives
    2.
    发明授权
    Compositions and methods for treating nephritis and inhibiting TGF -&bgr; related conditions using pyridylacrylamide derivatives 失效
    使用吡啶基丙烯酰胺衍生物治疗肾炎和抑制TGF-β相关病症的组合物和方法

    公开(公告)号:US06313153B1

    公开(公告)日:2001-11-06

    申请号:US09463511

    申请日:2000-01-21

    IPC分类号: C07D21342

    CPC分类号: C07D213/56

    摘要: The present invention relates to an agent for treating nephritis and a TGF-&bgr; inhibiting agent comprising as an effective ingredient a pyridylacrylamide derivative represented by the following formula (I): wherein Ar1 is a substituted or unsubstituted pyridyl group, Ar2 is a substituted or unsubstituted phenyl group, R1 is a hydrogen atom, an alkyl group or an aryl group, R2 is a hydrogen atom, an alkyl group, a cyano group or an alkoxycarbonyl group, R3 is a hydrogen atom or an optionally substituted alkyl group, X is an oxygen or sulfur atom, A and B are same or different and each represent a hydrogen atom, a hydroxyl group, an alkoxy group or an alkylthio group, or A and B together form an oxo or thioxo group, or a group represented by the formula: ═N—Y in which Y is a dialkylamino, hydroxyl, aralkyloxy or alkoxy group, or a group represented by the formula: —Z1—M—Z2— which Z1 and Z2 are same or different and each represent an oxygen or sulfur atom or an imino group optionally substituted by an alkyl group, and M is an alkylene group or a 1,2-phenylene group, or A is a hydroxyl group and B is a 1-alkylimidazol-2-yl group, and n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof; as well as the pyridylacrylamide derivatives.

    摘要翻译: 本发明涉及治疗肾炎的药剂和TGF-β抑制剂,其包含作为有效成分的下式(I)表示的吡啶基丙烯酰胺衍生物:其中Ar1为取代或未取代的吡啶基,Ar2为取代或未取代的 苯基,R 1为氢原子,烷基或芳基,R 2为氢原子,烷基,氰基或烷氧基羰基,R 3为氢原子或任选取代的烷基,X为 氧或硫原子,A和B相同或不同,各自表示氢原子,羟基,烷氧基或烷硫基,或A和B一起形成氧代或硫代基,或由式 := NY,其中Y是二烷基氨基,羟基,芳烷氧基或烷氧基,或由式-Z1-M-Z2-表示的基团,其中Z1和Z2相同或不同,各自表示氧或硫原子或 亚胺基可选择地 由烷基取代,M为亚烷基或1,2-亚苯基,或A为羟基,B为1-烷基咪唑-2-基,n为1〜3的整数, 或其药学上可接受的盐; 以及吡啶基丙烯酰胺衍生物。