中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

57 records (took 0.029 seconds)

    Chemical compound and assay
    1.
    发明申请
    Chemical compound and assay 审中-公开
    化学化合物和化验

    公开(公告)号：US20070048215A1

    公开(公告)日：2007-03-01

    申请号：US10575523

    申请日：2004-10-18

    Applicant: Brian Springthorpe ,  Gert Strandlund

    Inventor： Brian Springthorpe ,  Gert Strandlund

    IPC: A61K51/00 ,  C07D471/04 ,  A61K31/4745

    CPC classification number: C07D471/08

    Abstract: The present invention relates to a labelled ligand compound that is useful in a method of identifying, testing and/or screening of compounds modulating ion channels, in particular myocardial I?Kr# 191 channels such as those encoded by ERG, including hERG. The ligand compound is therefore of use to evaluate the affinity of preclinical compounds at the ERG potassium channel. The or salts, hydrates or solvates thereof and comprising at least one radiolabel: Formula (I).

    Abstract translation: 本发明涉及标记的配体化合物，其可用于鉴定，测试和/或筛选调节离子通道的化合物，特别是心肌IκKr＃191通道（例如由ERG编码的那些，包括hERG）的化合物。 因此，配体化合物可用于评估临床前化合物在ERG钾通道的亲和力。 其盐或其盐，水合物或溶剂合物并且包含至少一种放射性标记：式（I）。

    Aromatic compounds
    9.
    发明授权
    Aromatic compounds 失效
    芳香族化合物

    公开(公告)号：US4883804A

    公开(公告)日：1989-11-28

    申请号：US932473

    申请日：1986-11-19

    Applicant: Francis Ince ,  Brian Springthorpe ,  John Dixon

    Inventor： Francis Ince ,  Brian Springthorpe ,  John Dixon

    IPC: C07C323/25 ,  C07D213/38

    CPC classification number: C07C323/25 ,  C07D213/38 ,  Y10S514/821 ,  Y10S514/822 ,  Y10S514/824

    Abstract: There are described compounds of formula I, ##STR1## in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O).sub.n, wherein n is 0, 1 or 2;Y represents O or NH,l and m each independently represent 2, 3 or 4,R.sub.10 represents phenyl substituted by one or more substituents R.sub.23, which may be the same or different; or R.sub.10 represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,R.sub.15 represents hydrogen or together with R.sub.23 forms a (CH.sub.2).sub.p chain, wherein p represents 0, 1 or 2;R.sub.20, R.sub.21, R.sub.22 and R.sub.23, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR.sub.25, SH, NO.sub.2, halogen, CF.sub.3, SO.sub.2 R.sub.30, CH.sub.2 OH or OH, wherein R.sub.25 represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO.sub.2 alkyl C 1 to 6, and R.sub.30 represents alkyl C 1 to 6 or NH.sub.2,provided that when X represents an uninterrupted C4 alkylene chain, Y represents NH, m represents 2, l represents 2, R.sub.10 represents phenyl, R.sub.15 represents hydrogen, and R.sub.21, R.sub.22 and R.sub.23 represent hydrogen, then R.sub.20 does not represent hydrogen or 4-OH,and pharmaceutically acceptable salts and solvates thereof.There are also described processes for the preparation of the compounds of formula I and pharmaceutical compositions containing them. The compounds of the invention may be used in the treatment or prophylaxis of renal failure or cardiovascular disorders.

    Abstract translation: 描述式I的化合物，其中X表示任选被双键中断的C 2至8亚烷基链或S（O）n，其中n为0,1或2; Y表示O或NH，l和m各自独立地表示2,3或4，R10表示被一个或多个可以相同或不同的取代基R 23取代的苯基; 或R 10表示吡啶基，饱和碳环基，C 1-6烷基或氢，R 15表示氢或与R 23一起形成（CH 2）p链，其中p表示0,1或2; R 20，R 21，R 22和R 23可以相同或不同，独立地表示氢，烷基C1至6，NHR25，SH，NO2，卤素，CF3，SO2R30，CH2OH或OH，其中R25表示氢，烷基C1 如果X表示不间断的C 4亚烷基链，则Y表示NH，m表示2，l表示2，表示2至6的烷基，C 1至6的烷酰基或C 2至C 6的烷基，R 30表示烷基C 1-6， R10表示苯基，R15表示氢，R21，R22和R23表示氢，则R20不表示氢或4-OH及其药学上可接受的盐和溶剂化物。 还描述了制备式I化合物的方法和含有它们的药物组合物。 本发明的化合物可用于治疗或预防肾衰竭或心血管疾病。

Patent Agency Ranking