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    3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
    34.
    发明申请
    3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents 失效
    具有用作抗炎剂的3,4-二芳基噻吩及其类似物

    公开(公告)号：US20030153602A1

    公开(公告)日：2003-08-14

    申请号：US10329332

    申请日：2002-12-27

    申请人： G.D. Searle & Co.

    发明人： John J. Talley ,  Stephen R. Bertenshaw ,  Paul W. Collins ,  Thomas D. Penning ,  David B. Reitz ,  Roland S. Rogers

    IPC分类号： A61K031/4436 ,  A61K031/40 ,  A61K031/381 ,  A61K031/34

    CPC分类号： C07D307/38 ,  A61K31/341 ,  A61K31/365 ,  C07D307/58 ,  C07D333/16 ,  C07D333/18 ,  C07D333/28 ,  C07D333/38 ,  C07D409/04

    摘要： A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: 1 wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 一类3,4-二芳基取代的噻吩，呋喃和吡咯衍生物及其类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。 特别感兴趣的化合物由式I定义：其中Y选自O，S和NR1; 其中R1选自氢和低级烷基; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选在可取代的位置被一个或多个选自磺酰胺基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

    Imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
    36.
    发明申请
    Imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 审中-公开
    用于治疗高血压的咪唑基/苯并咪唑基封端的烷基氨基乙炔基丙氨酸氨基二醇化合物

    公开(公告)号：US20030130329A1

    公开(公告)日：2003-07-10

    申请号：US10290944

    申请日：2002-11-08

    申请人： G.D. Searle & Co.

    发明人： Gunnar J. Hanson ,  Robert E. Manning

    IPC分类号： A61K031/4184 ,  A61K031/4172 ,  A61K031/416 ,  A61K031/415

    CPC分类号： C07D233/64 ,  C07D231/12 ,  C07D233/56 ,  C07D233/68 ,  C07D235/06 ,  C07D235/14 ,  C07D249/08

    摘要： Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I 1 wherein A is selected from CO and SO2; wherein X is selected from oxygen atom and methylene; wherein B is selected from imidazolyl and benzimidazolyl groups; wherein R1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R2 is phenylmethyl; wherein each of R3 and R5 is hydrido; wherein R4 is selected from 2 wherein V is selected from hydrido and methyl; wherein R6 is cyclohexylmethyl; wherein R7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 通常表示咪唑基/苯并咪唑基封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是其中A选自CO和SO 2的式I的化合物; 其中X选自氧原子和亚甲基; 其中B选自咪唑基和苯并咪唑基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。