[EN] BENZIMIDAZOLE COMPOUNDS THAT ARE VITRONECTIN RECEPTOR ANTAGONISTS<br/>[FR] COMPOSES DE BENZIMIDAZOLE UTILISES COMME ANTAGONISTES DU RECEPTEUR DE LA VITRONECTINE
                        
                            
                                申请人:SCHERING CORP
                            
                            
                                公开号:WO2000032578A1
                            
                            
                                公开(公告)日:2000-06-08
                            
                            The present invention provides compounds having formula (I) wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y' each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, -CF3, and -C(O)OH; R?1, R2, R3 and R4¿ are H or specified substituents; R?5, R6, R7, R8, R9, R10, R11 and R12¿ are independently selected from H or C¿1?-C3 alkyl; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.
                            本发明提供具有式(I)的化合物,其中n,p,q和r各自独立地选自0或1;a,b,c和d各自独立地表示碳或氮原子,但a,b,c和d中不超过两个是氮原子;Y和Y'各自独立地表示从烷基,烷氧基,卤素,-
CF3和-C(O)OH中选择的1-4个可选取代基;R?1,R2,R3和R4¿为H或指定的取代基;R?5,R6,R7,R8,R9,R10,R11和R12¿各自独立地选自H或C¿1?-C3烷基;或其
生物可降解酯或其药学上可接受的盐。还提供使用这些化合物治疗
玻璃蛋白酶介导的疾病的方法,例如癌症,视网膜病变,动脉粥样硬化,血管再狭窄和骨质疏松症。