Diphenylurea derivatives and their use as chloride channel blockers
    72.
    发明申请
    Diphenylurea derivatives and their use as chloride channel blockers 失效
    二苯基脲衍生物及其作为氯通道阻断剂的用途

    公开(公告)号:US20060178413A1

    公开(公告)日:2006-08-10

    申请号:US10561189

    申请日:2004-06-15

    IPC分类号: C07D257/02 A61K31/41

    CPC分类号: C07D257/04

    摘要: The present invention relates to novel diphenylurea derivatives useful as chloride channel blockers. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.

    摘要翻译: 本发明涉及可用作氯化物通道阻断剂的新型二苯基脲衍生物。 在其他方面,本发明涉及这些化合物在治疗方法中的用途,以及包含本发明化合物的药物组合物。

    Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers

    公开(公告)号:US06417393B1

    公开(公告)日:2002-07-09

    申请号:US09194083

    申请日:1999-01-22

    IPC分类号: C07C24100

    摘要: The present patent application relates to compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein one of R1, R2 and R3 is a non-cyclic acidic group having a pKa value below 8 or a group which is in vivo convertible to such a group; R4, R5 and the other two of the substituents R1, R2 and R3 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amnino, and aryl, aralkyl, arylamino, aryloxy, aryl—CO—, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or R3 and R4 or R4 and R5 together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R1, R2, R3, R4 and R5 are as defined above; Y is —CO—, —CS—, —SO2—, or —C(═N—R8)—, wherein R8 is hydrogen, alkyl, or cyano; X is —NH—, —CH2—NH—, or —SO2—NH—; Z is NR6, O, —CH═CH—, —C═C—, —N═CH—, or —CH═N—; wherein R6 is hydrogen, or alkyl; R11, R12, R13, R14 and R15 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, —NHSO2—R7, —COOR7, —SO2N(R7)2, —SO2OR7 and —CO—R7, wherein R7 is hydrogen alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or aralkyl; and aryl, aralkyl, arylamino, aryloxy, aryl-CO—, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or one of R11 and R12, R12 and R13, R13 and R14 or R14 and R15 together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R11, R12, R13, R14 and R15 are as defined above. The compounds are useful for the treatment of diseases and disorders responsive to the blockage of chloride channels.

    Patch clamp apparatus and technique having high throughput and low fluid
volume requirements
    80.
    发明授权
    Patch clamp apparatus and technique having high throughput and low fluid volume requirements 失效
    具有高通量和低流体体积要求的贴片钳装置和技术

    公开(公告)号:US6063260A

    公开(公告)日:2000-05-16

    申请号:US836094

    申请日:1997-04-25

    摘要: Apparatus for carrying out patch clamp technique utilized in studying the effect of certain materials on ion transfer channels in biological tissue, and more particularly patch clamp apparatus utilizing an autosampler, such as those utilized with HPLC apparatus, to provide high throughput, is disclosed. The invention additionally includes novel microperfusion chamber assemblies capable of utilizing only small amounts of material to be tested and only small amounts of liquid carrier, thereby enabling many tests to be completed in a short period of time. The invention more broadly relates to a novel electrophysiology drug handling and application set up for screening of chemical substances while providing high throughput and requiring only low volume of solutions and samples to be tested. The invention also comprises several novel procedures for utilizing the apparatus of the invention.

    摘要翻译: PCT No.PCT / EP95 / 02204 Sec。 371日期1997年04月25日 102(e)日期1997年4月25日PCT提交1995年6月7日PCT公布。 第WO96 / 13721号公报 日期1996年5月9日用于研究某些材料对生物组织中的离子转移通道的影响的膜片钳技术的装置,更具体地,使用利用HPLC装置的自动进样器的膜片钳装置,以提供高通量, 被披露。 本发明另外包括能够仅使用少量待测试材料和仅少量液体载体的新型微灌注室组件,从而使得能够在短时间内完成许多试验。 本发明更广泛地涉及一种用于筛选化学物质的新型电生理学药物处理和应用,同时提供高通量并且仅需要低体积的溶液和样品进行测试。 本发明还包括利用本发明装置的若干新颖程序。