申请人:Texas Biotechnology Corporation
公开号:US06545014B2
公开(公告)日:2003-04-08
Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds that include those of the formula:
where X is selected from groups that include O, S, and NH; Y is selected from O+ and N, and R1 and R2 are each selected independently from among alkyl, lower alkenyl, lower alkynyl, lower haloalkyl, halide, pseudohalide or H, except that R2 is not halide. R3, R4 and R5 are selected from among groups that include hydrogen, halide, alkoxy, alkyl, haloalkyl; and R7 is selected from groups that include (CH2)rR18, in which r is 0 to 6 and R18 is selected from groups that include aryl, particularly pyrmidinyl and phenyl. The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.
提供了用于调节内皮素肽活性的方法、组合物和化合物。该方法使用含有化合物的组合物,其中化合物的公式如下:其中X从包括O、S和NH的基团中选择;Y从O+和N中选择;R1和R2各自独立地从烷基、低烯基、低炔基、低卤代烷基、卤素、伪卤素或H中选择,但R2不是卤素。R3、R4和R5从包括氢、卤素、烷氧基、烷基、卤代烷基的基团中选择;R7从包括(CH2)rR18的基团中选择,其中r为0到6,R18从包括芳基、特别是吡啶基和苯基的基团中选择。该方法通过在与内皮素肽接触之前、同时或之后将内皮素受体与一个或多个化合物或含有一个或多个化合物的组合物接触来实现。