公开(公告)号：EP3177597A1

公开(公告)日：2017-06-14

申请号：EP15748009.6

申请日：2015-07-31

申请人： Institut Pasteur Korea ,  Qurient Co. Ltd.

发明人： KIM, Jaeseung ,  AHN, Seohyun ,  JEON, Yeejin ,  PARK, Dongsik ,  YANG, Young-In ,  LEE, Doohyung ,  LEE, SaeYeon ,  AHN, Jiye ,  KIM, Jeongjun ,  NAM, Kiyean ,  KANG, Sunhee ,  SEO, MinJung ,  SEO, Mooyoung ,  SEO, Jeongjea ,  HAN, Sung-Jun ,  KIM, Jung Hwan ,  LEE, Sangchul ,  CHOI, Gahee ,  LEE, Yunmi

IPC分类号： C07D235/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/4184

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.

摘要翻译： 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。

公开(公告)号：EP2730576A3

公开(公告)日：2014-09-03

申请号：EP13198407.2

申请日：2009-06-17

申请人： Institut Pasteur Korea ,  INSERM (Institut National de la Santé et de la Recherche Médicale)

发明人： Brodin, Priscille ,  Christophe, Thierry ,  No, Zaesung ,  Kim, Jaeseung ,  Genovesio, Auguste ,  Fenistein, Denis, Philippe, Cedric ,  Jeon, Heekyoung ,  Ewann, Fanny, Anne ,  Kang, Sunhee ,  Lee, Saeyeon ,  Seo, Min, Jung ,  Park, Eunjung ,  Contreras Dominguez, Monica ,  Nam, Ji, Youn ,  Kim, Eun, Hye

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P31/06

CPC分类号： C12Q1/18 ,  C07C255/66 ,  C07C335/40 ,  C07D223/24 ,  C07D233/84 ,  C07D251/52 ,  C07D251/66 ,  C07D271/113 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04

摘要： The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.

公开(公告)号：EP2307568A2

公开(公告)日：2011-04-13

申请号：EP09769011.9

申请日：2009-06-25

申请人： Institut Pasteur Korea ,  Institut Pasteur

发明人： EMANS, Neil ,  GENOVESIO, Auguste ,  WINDISCH, Marc P. ,  KWON, Yong Jun ,  JUNG, Sungyong ,  KIM, Hi Chul ,  KIM, Hi Chul ,  YEON, Choi Seo ,  NEHRBASS, UIf

IPC分类号： C12Q1/68

CPC分类号： C12Q1/6876 ,  C12Q1/703 ,  C12Q2600/136 ,  C12Q2600/158

摘要： The present invention relates to the identification of human host factors involved in the early stage of HIV infection. Furthermore, it relates to the use of the identified genes for the elucidation of the mechanism of HIV-infection, as drug targets, and for identifying a compound useful in the treatment of HIV.

公开(公告)号：EP1865320A2

公开(公告)日：2007-12-12

申请号：EP07252322.8

申请日：2007-06-08

申请人： Institut Pasteur Korea

发明人： Emans, Neil ,  Altschuler, Yoram c/o Institut Pasteur Korea ,  Kwon, Yongjun

IPC分类号： G01N33/50 ,  G01N33/74 ,  C07K14/705

CPC分类号： G01N33/5035 ,  G01N33/5008 ,  G01N33/566 ,  G01N2333/5754 ,  G01N2333/70571 ,  G01N2333/726 ,  G01N2800/12 ,  G01N2800/32

摘要： A method for identifying a compound that modifies the cellular distribution of a GPCR in a population of cells comprising:
a) taking a population of cells expressing a GPCR
b) incubating said cells with a candidate compound and with a ligand of the GPCR
c) determining distribution of said GPCR in cells treated according to step b) and comparing with distribution of GPCR in cells incubated with a ligand of the GPCR in the absence of the candidate compound;

wherein altered distribution in cells incubated with the candidate compound is indicative that the candidate compound modifies GPCR cellular distribution.

摘要翻译： 一种用于鉴定修饰细胞群中GPCR的细胞分布的化合物的方法，包括：a）取表达GPCR的细胞群b）用候选化合物和GPCR的配体将所述细胞孵育c）确定 所述GPCR在根据步骤b）处理的细胞中的分布并与不存在候选化合物时与GPCR配体孵育的细胞中GPCR的分布进行比较; 其中与候选化合物孵育的细胞中分布改变指示候选化合物修饰GPCR细胞分布。