Disclosed are compounds, which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.本發明揭示結合VLA-4之化合物。某些該等化合物亦抑制白血球黏附,且尤其抑制由VLA-4所調節之白血球黏附。該等化合物可用於治療人類或動物受檢者中之發炎性疾病,諸如,哮喘、阿耳滋海默症(Alzheimer's disease)、動脈粥樣硬化、AIDS癡呆、糖尿病、發炎性腸道疾病、克羅恩氏病(Crohn's disease)、類風濕性關節炎、組織移植、腫瘤轉移及心肌局部缺血。亦可投予該等化合物用於治療發炎性腦病,諸如,多發性硬化症。