N-Acylphenylalanines as antagonists of VLA-4/VCAM-1

Abstract

Within the entitled patents, a series of N-acylphenylalanine derivatives are disclosed that inhibit the binding interaction of the leukocyte cell surface integrin α4β1 (also known as VLA-4, very late antigen-4) with the adhesion molecule vascular cell adhesion molecule-1 (VCAM-1). These antagonists are expected to be useful as therapeutic agents for the treatment of chronic inflammatory diseases such as rheumatoid arthritis (RA), inflammatory bowel disease (IBD), multiple sclerosis (MS), and pulmonary inflammation (asthma).

• α4β1
• adhesion
• cell adhesion molecule (CAM)
• integrin
• vascular cell adhesion molecule-1 (VCAM-1)
• very late antigen-4 (VLA-4)