申请人:Gottlieb Eyal
公开号:US20090005437A1
公开(公告)日:2009-01-01
The present invention relates generally to the field of pharmaceuticals and medicine. More particularly, the present invention relates to certain compounds (e.g., α-ketoglutarate compounds; compounds that activate HIFα hydroxylase; compounds that increases the level of α-ketoglutarate, etc.) and their use in medicine, for example, in the treatment of cancer (e.g., cancer in which the activity of one of the enzymes in the tricarboxylic acid (TCA) cycle is down regulated), in the treatment of angiogenesis (e.g., hypoxia-induced angiogenesis). One preferred class of compounds are α-ketoglutarate compounds having a hydrophobic moiety that is, or is part of, an ester group formed from one of the acid groups of α-ketogluartic acid; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof.
本发明一般涉及制药和医学领域。更具体地说,本发明涉及某些化合物(例如α-酮戊二酸化合物;激活HIFα羟化酶的化合物;增加α-酮戊二酸水平的化合物等)及其在医学上的应用,例如治疗癌症(例如三羧酸循环中的酶活性被下调的癌症),治疗血管生成(例如缺氧诱导的血管生成)。一种首选的化合物类别是具有亲水性基团的α-酮戊二酸化合物,该亲水性基团是α-酮戊二酸的酸基之一形成的酯基或其一部分;以及其药学上可接受的盐、溶剂化物、酰胺、酯、醚、N-氧化物、化学保护形式和其前药。