申请人:E. R. Squibb & Sons, Inc.
公开号:US04906667A1
公开(公告)日:1990-03-06
Phenyl hydroxamic acids are disclosed having the general formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is NR, oxygen, sulfur, ##STR2## or a single bond, and Y is NR, oxygen, sulfur, ##STR3## or a single bond, where R can be hydrogen or lower alkyl, g can be 1 or 2, and with the proviso that at least one of X and Y is other than a single bond; Z is aryl, aralkyl or cycloalkyl; R.sub.1 is hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl or aryl; R.sub.2 is hydrogen, lower alkyl, aroyl or acyl; m is 0 to 4 carbon atoms; and, n is 0 to 4 carbon atoms further providing that if one of X or Y is oxygen, the other of X or Y must be oxygen and further that when X and Y are oxygen Z cannot be aralalkyl. These new compounds have been found to be inhibitors or arachidonic acid 5-lipoxygenase and are therefore useful as antiallergy agents and antipsoriatics.
揭示了具有一般公式##STR1##或其药用可接受的盐的苯基羟肟酸,其中X为NR、氧、硫、##STR2##或单键,Y为NR、氧、硫、##STR3##或单键,其中R可以是氢或较低的烷基,g可以是1或2,并且至少X和Y中的一个不是单键;Z为芳基、芳基烷基或环烷基;R.sub.1为氢、取代或未取代的较低烷基、环烷基、较低烯基或芳基;R.sub.2为氢、较低烷基、芳酰基或酰基;m为0至4个碳原子;n为0至4个碳原子,进一步提供如果X或Y中的一个是氧,则另一个X或Y必须是氧,并且当X和Y均为氧时,Z不能是芳基烷基。已发现这些新化合物是花生四烯酸5-脂氧合酶的抑制剂,因此可用作抗过敏药物和抗银屑病药物。