Patent of the Week - Vasopressin Inhibitors

A series of V3 antagonists were disclosed in patent 7807686 by Organon, which after a couple of mergers (what's new) is now part of the Merck/ Merck Sharp Dohme organization. The compounds share a common scaffold as shown on the left.

The compounds are aimed to CNS disorders which are characterized by abnormal hypothalamo-pituitary-adrenal axis negative feedback mechanisms, among them depression. V₃ receptor does play a functional role in control of pituitary adrenocorticotropic hormone release. The V_1a receptor, predominantly found on liver and vascular tissue and the V₂ receptor, predominantly found on kidney tissue have peripheral activity. Interaction at these receptors mediate the pressor and antidiuretic actions of Vasopressin.Only a qualitative sense of the affinity is provided. 

Patent of the week - New Antibiotic

Merck Sharp & Dohme in Spain has disclosed in US patent 7807445 anew antibacterial compound. The compound was isolated from  Streptomyces sp.

The compound appreas to have activity against a variety of microbes including S. Aureus, S pneumoniae, E. Coli, etc.. As well as some MRSA resistant S Aureus and Vancomycin resistant (VRE) enterococcus. The minimum inhibitory concentration (MIC) ranged from 5 to 32 ug/mL.