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发明公开
EP3177597A1 2-AMINO-BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS 5-LIPOXYGENASE AND/OR PROSTAGLANDIN E SYNTHASE INHIBITORS 审中-公开
2-氨基 - 苯并咪唑衍生物及其作为5-脂氧合酶和/或前列腺素E合成酶抑制剂的用途

2-AMINO-BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS 5-LIPOXYGENASE AND/OR PROSTAGLANDIN E SYNTHASE INHIBITORS
摘要：
The present invention relates to benzimidazole derivatives having the general formula I, wherein n is 0 or 1; X1 and X2 are independently, at each occurrence, CR5 or N; Y is C1-C6 alkylene, wherein alkylene is optionally substituted with one to two C1-C3 alkyl groups; R1 is selected from the group consisting of hydrogen, halogen, C1-C6 alkoxy, -NH2, -NHR6, -NR7R8 and -NH-(R9)n-R10, n being 0 or 1; R2 is selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, -NH2, -NHR6, - NR7R8 and -NH-(R9)n-R10; R3 is selected from the group consisting of hydrogen, hydroxyl, OR11, -NR7R8, C1-C6 alkoxy, C1-C6 alkyl, C3-C10 cycloalkyl, C1-C3 haloalkyl, -C(O)NHR11, aryl, heteroaryl and heterocyclyl, wherein each of said cycloalkyl, aryl, heteroaryl and heterocyclyl is optionally and independently substituted with one to four Ra groups; and R4 is selected from the group consisting of -NH2, -N(R12)(V)pR13, - NH(V)p-OR14, -NHC(O)R15, and groups of formula la shown below, and their use in the treatment of diseases, in particular inflammatory diseases, cancer, stroke and/or Alzheimer's disease.
摘要（中）：

本发明涉及具有通式I的苯并咪唑衍生物，其中n是0或1; X1和X2在每次出现时独立地为CR5或N; Y是C 1 -C 6亚烷基，其中亚烷基任选被一个至两个C 1 -C 3烷基取代; R1选自氢，卤素，C1-C6烷氧基，-NH2，-NHR6，-NR7R8和-NH-（R9）n-R10，n为0或1; R2选自氢，卤素，C1-C6烷基，-NH2，-NHR6，-NR7R8和-NH-（R9）n-R10; R3选自氢，羟基，OR11，-NR7R8，C1-C6烷氧基，C1-C6烷基，C3-C10环烷基，C1-C3卤代烷基，-C（O）NHR11，芳基，杂芳基和杂环基， 其中所述环烷基，芳基，杂芳基和杂环基中的每一个任选且独立地被1至4个Ra基团取代; 并且R4选自-NH2，-N（R12）（V）pR13，-NH（V）p-OR14，-NHC（O）R15和下面所示的式Ia的基团，以及它们在 治疗疾病，特别是炎性疾病，癌症，中风和/或阿尔茨海默氏病。

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