779329-61-2Relevant academic research and scientific papers
Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865)
Owen, Robert M.,Blakemore, David,Cao, Lishuang,Flanagan, Neil,Fish, Rebecca,Gibson, Karl R.,Gurrell, Rachel,Huh, Chan Woo,Kammonen, Juha,Mortimer-Cassen, Elisabeth,Nickolls, Sarah A.,Omoto, Kiyoyuki,Owen, Dafydd,Pike, Andy,Pryde, David C.,Reynolds, David S.,Roeloffs, Rosemarie,Rose, Colin,Stead, Clara,Takeuchi, Mifune,Warmus, Joseph S.,Watson, Christine
supporting information, p. 5773 - 5796 (2019/05/15)
The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABAA ligand-gated ion channel are described. From a set of initial hits multiple subseries were designed and evaluated based on binding affinity and functional activity. As designing in the desired level of functional selectivity proved difficult, a probability-based assessment was performed to focus the project's efforts on a single subseries that had the greatest odds of delivering the target profile. These efforts ultimately led to the identification of two precandidates from this subseries, which were advanced to preclinical safety studies and subsequently to the identification of the clinical candidate PF-06372865.
Chemical Compounds
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Paragraph 0498; 0499; 0500, (2014/06/25)
The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
NOVEL COMPOUNDS
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Page 44, (2010/02/09)
The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation
