Wednesday, September 8, 2010

Patent of the week

In an issued patent 7772223 (pub date 08/10/2010) Pfizer has disclosed a series of carboxamide analogs as antimuscrinic agents. The most preferred structures are shown here.
The compounds appear to be of interest for asthma, COPD and other related uses. There is still a need for improved M3 receptor antagonists that would have an appropriate pharmacological profile, for example in term of potency, pharmacokinetics or duration of action. In this context, the patent relates to novel M3 receptor antagonists. In particular, there is a need for M3 receptor antagonists that would have a pharmacological profile suitable for an administration by the inhalation route. 
The application provides a description of the synthetic protocols but only minimal biological information as could be expected.
Some of the most potent compounds in these series are in the subnanomolar range, in a cell based assay according to the patent.
Even these traditional receptor families clearly continue to attract attention in big pharma.

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