Novel selective cannabinoid CB2 receptor ligands, primarily agonists, have a number of biological and pharmacological activities, including bronchial action, immunomodulatory action and analgesia. Hence, they are useful for treating diseases or conditions characterized by pain, inflammation and immunological dysregulation. Examples of this class of novel compounds are 4 chloro-N-[1-(2-morpholin-4-ylethyl)-1H-benzimidazol-2-yl]benzamide and 4-chloro-N-[7 methoxy-1-(2-morpholin-4-ylethyl)-1H-benzimidazol-2-yl]benzamide. Other examples of the novel compounds are 4-derivatives of 3-amino and 3-carboxy-1,2-dihydro-1-substitutedquinazol-2-ones, including 2-chloro-N (1,2-dihydro-1-(2-morpholinoethyl)-2-oxoquinoxalin-3-yl)benzamide, 3-chloro-N-(1,2-dihydro-1-(2-morpholinoethyl)-2-oxoquinoxalin-3-yl)benzamide, tert-butyl 1,2-dihydro-1-(2-morpholinoethyl)-2-oxoquinoxalin-3-ylcarbamate and N-benzyl-3,4-dihydro-4-(2-morpholinoethyl)-3-oxoquinoxaline-2-carboxamide. The compounds bind specifically to a cell-bound or cell-free CB2 receptor with an affinity (Kd) ≤ 100 µM. As agonists, these compounds stimulate a CB2-related post-binding signal transduction event, e.g., inhibition of adenylyl cyclase activity, after binding to a CB2 receptor on a cell. These compounds are used to treat inflammatory conditions, cell proliferative disorders, or an immune disorder, and may be administered in combination with agents that are also useful for the treatment of the symptoms or cause of the underlying disease or condition.
展开▼
