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NOVEL TIGHT-BINDING INHIBITORS OF LEUKOTRIENE A4 HYDROLASE

机译:白三烯A4水解酶的新型紧密结合抑制剂

摘要

Inhibitors of leukotriene A4 hydrolase are disclosed, as are processes for making and using the same. A contemplated inhibitor has a structure corresponding to formula (I), wherein the depicted -NH2 group is in the (S) configuration; -W is -CH2SH, -CH2NH2 or C(=Z)-Y, wherein =Z is =O, or -H and -OH; and -Y is selected from the group consisting of (a) phenyl, (b) trifluoromethylphenyl, (c) carboxyphenyl, (d) benzyl, (e) C1-C6 alkylenecarboxyl, (f) C1-C6 alkyl, (g) C2-C6 alkenyl, (h) C1-C6 alkylenephenyl and (i) -C(=O)-X-R1 wherein X is O or NH and, R1 is selected from the group consisting of C?1?-C6 alkyl, C1-C6 alkylenecarboxyl, and benzyl, with the proviso that -Y is other than (i) when =Z is -H and -OH; and R?2? is hydrogen, benzyloxy or 2-naphthylmethyloxy, and a pharmaceutically acceptable acid addition salt thereof.
机译:公开了白三烯A4水解酶的抑制剂,以及其制备和使用方法。预期的抑制剂具有对应于式(I)的结构,其中所示的-NH 2基团为(S)构型; -W是-CH 2 SH,-CH 2 NH 2或C(= Z)-Y,其中= Z是= O或-H和-OH。 -Y选自:(a)苯基,(b)三氟甲基苯基,(c)羧苯基,(d)苄基,(e)C 1 -C 6亚烷基羧基,(f)C 1 -C 6烷基,(g)C 2。 -C 6烯基,(h)C 1 -C 6亚烷基苯基和(i)-C(= O)-X-R 1,其中X是O或NH,且R 1选自C 1〜C 6烷基,C 1。 -C 6亚烷基羧基和苄基,条件是当= Z为-H和-OH时,-Y不同于(i)。 R 2是氢,苄氧基或2-萘甲氧基,及其药学上可接受的酸加成盐。

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