专利名称 | 化学化合物 | ||
申请号 | TW107131085 | 申请日 | |
公开(公告)号 | TW201922721A | 公开(公告)日 | |
申请(专利权)人 | 英商葛兰素史克智慧财产发展有限公司 | 发明人 | 麦迪娜 吉萨斯; 田 新荣; 盖瑞比尔 陶德; 赫尔丁 德克; 李 海康; 门格特 比竹; 马特尔 卡斯柏特; 里韦罗 拉斐尔; 德马克 克里斯汀娜 |
专利来源 | 国家知识产权局 | 转化方式 | |
摘要 |
本发明系关於经取代之苯并咪唑衍生物特别地,本发明系关於根据式Ib之化合物:其中R’、R 2’ 、R 3’ 、R 4’ 、R 5’ 、R 6’ 、R 7’ 、和X 1’ 如本文中所定义;或其盐,包括医药上可接受的盐; 本发明化合物减少细胞中之MYC蛋白(c-MYC)及/或抑制p300/CBP组织蛋白乙醯基移转酶且可用於治疗心肥大、糖尿病、肥胖与非酒精性脂肪肝疾病、HIV、多囊性肾病、发炎性疾病、关节黏连性脊椎炎、牛皮癣、牛皮癣性关节炎、类风湿性关节炎、克隆氏病、多发性硬化症、癌症和癌前期症候群、和与Myc失调或抑制p300/CBP组织蛋白乙醯基移转酶有关的疾病因此,本发明进一步关於包含本发明化合物之医药组成物本发明又进一步关於使用本发明化合物或包含本发明化合物的医药组成物减少细胞中之MYC蛋白(c-MYC)及/或抑制p300/CBP组织蛋白乙醯基移转酶活性及治疗与其相关的病症之方法 The invention is directed to substituted benzimidazole derivatives. Specifically, the invention is directed to compounds according to Formula Ib : wherein R’, R 2’ , R 3’ , R 4’ , R 5’ , R 6’ , R 7’ , and X 1’ are as defined herein; or a salt thereof including a pharmaceutically acceptable salt thereof.; The compounds of the invention decrease MYC protein (c-MYC) in cells and/or inhibit p300/CBP histone acetyltransferase and can be useful in the treatment of cardiac hypertrophy, diabetes, obesity与nonalcoholic fatty liver disease, HIV, polycystic kidney disease, inflammatory diseases, ankylosing spondylitis, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn’s disease, multiple sclerosis, cancer and pre-cancerous syndromes, and diseases associated with dysregulation of Myc or inhibition of p300/CBP histone acetyltransferase. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of reducing MYC protein (c-MYC) in cells and inhibiting p300/CBP histone acetyltransferase activity, and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention. |
主管部门:海南中小企业服务 | 建设单位:海南商业联合会
版权所有:海南商业联合会 | 备案号:粤ICP备13083911号(ICP加挂服务)@2017