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2-amino-benzimidazole derivatives and their use as 5-lipoxygenase and / or prostaglandin synthase inhibitors
专利权人:
INSTITUT PASTEUR KOREA;QURIENT CO., LTD.
发明人:
DONGSIK PARK,DOOHYUNG LEE,GAHEE CHOI,JAESEUNG KIM,JEONGJEA SEO,JEONGJUN KIM,JIYE AHN,JUNG HWAN KIM,KIYEAN NAM,MINJUNG SEO,MOOYOUNG SEO,SAE YEON LEE,SANGCHUL LEE,SEOHYUN AHN,SUNG-JUN HAN,SUNHEE KANG,YE
申请号:
BR112017001918
公开号:
BR112017001918A2
申请日:
2015.07.31
申请国别(地区):
BR
年份:
2017
代理人:
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 C 1 -C 6 alkylene, wherein alkylene is optionally substituted with one or two C 1 -C 3 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 C 1 -C 6 alkoxy, C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 1 -C 3 haloalkyl, -c (o) nhr 11, aryl, heteroaryl and heterocyclyl, wherein each of said cycloalkyl, aryl, heteroaryl and heterocyclyl is optionally and independently substituted with one to four groups ra; 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 ia shown below, and their use in the treatment diseases, in particular inflammatory diseases, cancer, stroke and / or alzheimer's disease.a presente invenção refere-se derivados de benzimidazol tendo a fórmula geral i, em que n é 0 ou 1; x1 e x2 são independentemente, em cada ocorrência, cr5 ou n; y é c1-c6 alquileno, em que alquileno é opcionalmente substituído com um ou dois grupos c1-c3 alquila; r1 é selecionado do grupo consistindo em hidrogênio, halogênio, c1-c6 alcóxi, -nh2, -nhr6, -nr7r8 e ?nh-(r9)n-r10, n sendo 0 ou 1; r2 é selecionado do grupo consistindo em hidrogênio, halogênio, c1-c6 alquila, -nh2, -nhr6, -nr7r8 e ?nh-(r9)n-r10, r3 é selecionado do grupo consistindo em hidrogênio, hidroxila, or11, -nr7r8, c1-c6 alcóxi, c1-c6 alquila, c3-c10 cicloalquila, c1-c3 haloalquila, -c(o)nhr11, arila, heteroarila e heterociclila, em que cada uma das ditas cicloalquila, arila, heteroarila e heterociclila é opcionalmente e independentemente substituída com um a quatro grupos ra; e r4 é selecio
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