BENZIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS

To provide novel compounds which have prolyl hydroxylase inhibitory activity and are useful in treating anemia, hypoxia, ischemia, peripheral vascular disease, myocardial infarction, stroke, diabetes, obesity, inflammatory bowel disease, ulcerative colitis, Crohn's disease, wounds, infection, burns, fractures, and the like.SOLUTION: The present invention is directed to benzimidazole derivatives represented by the formula (I) in the figure. (Each R1 is independently C1-4 alkyl, -NO2, -NH2, -NH-C1-4 alkyl, -NH-SO2-C3-8 cycloalkyl, -NH-SO2-C1-4 alkyl, -NH-C(O)-C1-4 alkyl, -CN, -CO2H, -OC1-4 alkyl, -NH-(CH2)2-morpholine, -NH(CO)CH2-morpholine, -NHC(O)-CH2-piperidine, -NHC(O)-CH2-(N-methylpiperazine), -NH-C1-4 alkyl-morpholine, pyrrolidine, piperidine, morpholine, or the like; R2 and R3 are H; and each Z is C or, in the case of two pieces of Z, N.)SELECTED DRAWING: None 【課題】プロリルヒドロキシラーゼ阻害作用を有し、貧血、低酸素症、虚血、末梢血管疾患、心筋梗塞、脳卒中、糖尿病、肥満、炎症性腸疾患、潰瘍性大腸炎、クローン病、創傷、感染症、火傷、骨折等の治療に有用な新規化合物を提供する。【解決手段】下記式（Ｉ）で表されるベンゾイミダゾール誘導体である。（Ｒ1は各々独立に、Ｃ1〜4アルキル、−ＮＯ2、−ＮＨ2、−ＮＨ−Ｃ1〜4アルキル、−ＮＨ−ＳＯ2−Ｃ3〜8シクロアルキル、−ＮＨ−ＳＯ2−Ｃ1〜4アルキル、−ＮＨ−Ｃ（Ｏ）−Ｃ1〜4アルキル、−ＣＮ、−ＣＯ2Ｈ、−ＯＣ1〜4アルキル、−ＮＨ−（ＣＨ2）2−モルホリン、−ＮＨ（ＣＯ）ＣＨ2−モルホリン、−ＮＨＣ（Ｏ）−ＣＨ2−ピペリジン、−ＮＨＣ（Ｏ）−ＣＨ2−（Ｎ−メチルピペラジン）、−ＮＨ−Ｃ1〜4アルキル−モルホリン、ピロリジン、ピペリジン、モルホリン等；Ｒ2及びＲ3はＨ；各ＺはＣ又はＺが２つの場合Ｎ。）【選択図】なし