Imidazo[2,1-b]thiazoles and their use as pharmaceuticals: Sanofi-Aventis EP 1 923 062 A1 (equivalent to WO2008058641)

Background: Imidazothiazoles are well-known compounds and many derivatives of this fused ring system have been evaluated for potential biological activity. Objectives: The present application is focused on imidazo[2,1-b]thiazoles with pharmacological ability to stimulate the expression (transcription) of the enzyme endothelial nitric oxide (NO) synthase. This invention contains two types of claims. First, several imidazo[2,1-b]thiazoles (and compositions thereof) that were not previously reported in chemical literature are claimed (claims 6 - 15). Second, the use of the claimed compounds in the treatment of several different diseases is claimed (claims 1 - 5 and 16). Methods: The claimed imidazo[2,1-b]thiazoles are synthesized by the condensation of 2-aminothiazole with an α-halo ketone. Evaluation of pharmacological activity of the claimed compounds is based on previously reported methodo-logies. Results are at their best reported in descriptive terms. Conclusion: The descriptive presentation of results in this application does not allow a critical evaluation of the claims. However, this does not diminish the potential commercial importance of this application. Because of the importance of nitric oxide regulation in physiological systems, more research in this area of medicinal chemistry can be anticipated.