cerlapirdine (PF-5212365) / Pfizer - LARVOL DELTA

Exploring Synthetic Strategies for 1H-Indazoles and Their N-Oxides: Electrochemical Synthesis of 1H-Indazole N-Oxides and Their Divergent C-H Functionalizations. (PubMed, Angew Chem Int Ed Engl) - "Owing to the rich reactivity of 1H-indazole N-oxides, diverse C-H functionalization reactions were performed. We demonstrated the synthetic utility of 1H-indazole N-oxides by synthesizing the pharmaceutical molecules lificiguat and YD (3); key intermediates for bendazac, benzydamine, norepinephrine/serotonin reuptake inhibitors, SAM-531, and gamendazole analogues; and a precursor for organic light-emitting diodes."

Journal

Progress in Investigational Agents Targeting Serotonin-6 Receptors for the Treatment of Brain Disorders. (PubMed, Biomolecules) - "Several 5-HT receptor antagonists (idalopirdine, intepirdine and latrepirdine) showed efficacy in alleviating cognitive deficits associated with AD in the proof-of-concept clinical studies; however, the outcomes of the subsequent phase 3 studies were largely disappointing...Masupirdine, a selective 5-HT receptor antagonist, reduced agitation/aggression-like behaviors in animal models, and a post hoc analysis of a phase 2 trial suggested potential beneficial effects on agitation/aggression and psychosis in AD. This agent will be assessed in additional trials, and the outcome of the trials will inform the use of 5-HT receptor antagonists in the treatment of agitation in dementia of the Alzheimer's type."

Journal • Review • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Dementia • Psychiatry • Schizophrenia

To evaluate the relationship between plasma drug levels and receptor binding in brain using PET (positron emission tomography) in healthy volunteers (3193A1-1103) (clinicaltrials.gov) - P1, N=6

Schizophrenia

Pfizer pipeline (Pfizer) - Pipeline discontinued at P2 on Feb 28,2011

Pipeline update • Schizophrenia