公开(公告)号：EP2083005A1

公开(公告)日：2009-07-29

申请号：EP09004388.6

申请日：2001-09-27

申请人： TopoTarget UK Limited

发明人： Watkins, Clare J. ,  Romero-Martin, Maria-Rosario ,  Moore, Kathryn G. ,  Ritchie, James ,  Finn, Paul W ,  Kalvinsh, Ivars ,  Loza, Einars ,  Starchenkov, Igor ,  Dikovska, Klara ,  Bokaldere, Rasma Melita ,  Gailite, Vija ,  Vorona, Maxim ,  Andrianov, Victor ,  Lolya, Daina ,  Semenikhina, Valentina ,  Amolins, Andris ,  Harris, John C ,  Duffy, James E S

IPC分类号： C07D207/40 ,  C07D209/14 ,  C07D213/06 ,  C07D233/04 ,  C07D233/08 ,  C07D235/24 ,  C07D307/34 ,  C07D333/24 ,  C07D333/60 ,  A61K31/426 ,  A61K31/381 ,  A61K31/38 ,  A61K31/277 ,  A61K31/198 ,  A61K31/195 ,  A61K31/16 ,  A61P31/20

CPC分类号： C07D207/337 ,  A61K31/16 ,  A61K31/195 ,  A61K31/198 ,  A61K31/277 ,  A61K31/38 ,  A61K31/381 ,  A61K31/426 ,  C07C233/49 ,  C07C233/83 ,  C07C235/34 ,  C07C237/36 ,  C07C255/57 ,  C07C259/06 ,  C07C259/08 ,  C07C2603/18 ,  C07D207/40 ,  C07D207/404 ,  C07D209/14 ,  C07D209/16 ,  C07D209/18 ,  C07D209/22 ,  C07D213/06 ,  C07D213/55 ,  C07D213/56 ,  C07D233/04 ,  C07D233/08 ,  C07D235/14 ,  C07D235/24 ,  C07D271/06 ,  C07D307/34 ,  C07D307/54 ,  C07D317/60 ,  C07D333/24 ,  C07D333/60 ,  C07D403/12 ,  Y02A50/411

摘要： This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula:

wherein: A is an aryl group; Q 1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: -NR 1 (=O)- and -C(=O)NR 1 -; R 1 is an amido substituent; and, Q 2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, and ethers thereof, for use in the treatment of a fibroproliferative disorder; liver fibrosis; smooth muscle proliferative disorder; atherosclerosis; restenosis; a neurodegenative disease; Alzheimer's; Parkinson's; Huntington's chorea; amyotropic lateral sclerosis; spino-cerebellar degeneration; an inflammatory disease; osteoarthritis; rheumatoid arthritis; a diseases involving angiogenesis; diabetic retinopathy; a haematopoietic disorder; anaemia; sickle cell anaemia; thalassaeimia; a fungal infection; a parasitic infection; trypanosomiasis; helminthiasis; a protozoal infection; a bacterial infection; a viral infection; a condition treatable by immune modulation; multiple sclerosis; autoimmune diabetes; lupus; atopic dermatitis; an allergy; asthma; allergic rhinitis; or inflammatory bowel disease.

摘要翻译： 本发明涉及抑制HDAC活性的某些活性氨基甲酸化合物，其具有下式：其中：A为芳基; Q 1是具有至少2个碳原子的主链的芳基前导基团; J是选自：-NR 1（= O） - 和-C（= O）NR 1 - 的酰胺键; R 1是酰氨基取代基; Q 2是酸性引导基团; 和其药学上可接受的盐，溶剂合物，酰胺，酯和醚，用于治疗纤维增生性疾病; 肝纤维化; 平滑肌增生障碍; 动脉粥样硬化; 再狭窄; 神经退行性疾病 老年痴呆症; 帕金森氏; 亨廷顿舞蹈 肌萎缩性侧索硬化; 脊髓小脑变性; 炎性疾病; 骨关节炎; 类风湿关节炎; 涉及血管生成的疾病 糖尿病性视网膜病变; 造血障碍 贫血; 镰状细胞性贫血 thalassaeimia; 真菌感染; 寄生虫感染; 锥虫病; 蠕虫病; 原生动物感染; 细菌感染; 病毒感染; 通过免疫调节治疗的病症; 多发性硬化症 自身免疫性糖尿病 狼疮; 特应性皮炎; 过敏; 哮喘; 过敏性鼻炎; 或炎症性肠病。