461720-22-9Relevant academic research and scientific papers
Discovery of selective biaryl ethers as PDE10A inhibitors: Improvement in potency and mitigation of Pgp-mediated efflux
Rzasa, Robert M.,Hu, Essa,Rumfelt, Shannon,Chen, Ning,Andrews, Kristin L.,Chmait, Samer,Falsey, James R.,Zhong, Wenge,Jones, Adrie D.,Porter, Amy,Louie, Steven W.,Zhao, Xiaoning,Treanor, James J.S.,Allen, Jennifer R.
, p. 7371 - 7375 (2013/02/21)
We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure-activity studies improved the potency and decreased Pgp-mediated efflux found in the initial compound 4. X-ray crystallographic studies revealed two novel binding modes to the catalytic site of the PDE10A enzyme.
1, 4-DISUBSTITUTED PIPERIDINES AS VASOPRESSIN RECEPTOR VIA ANTAGONISTS
-
Page/Page column 40; 43, (2010/09/17)
The present invention provides compounds of formula (1) compositions comprising such compounds; the use of such compounds in therapy (such as in the treatment of dysmenorrhoea); and methods of treating patients with such compounds; wherein A and G are as defined herein.
ARYL-SUBSTITUTED ALICYCLIC COMPOUND AND MEDICAL COMPOSITION COMPRISING THE SAME
-
Page 42, (2008/06/13)
An aryl-substituted alicyclic compound of the formula (I): wherein U is 1,4,5,6-tetrahydropyrimidin-2-yl, etc., A is phenylene, etc., B is piperidine-1,4-diyl, etc., Z is -CONH-, etc., R3 is hydrogen, etc., R5 is hydrogen, aryl, etc.
Preparation of a series of aryl isonipecotic acids using microwave irradiation
Antane, Schuyler
, p. 2145 - 2149 (2007/10/03)
Rapid parallel synthesis of arylisonipecotic acids was achieved using microwave irradiation of a palladium catalyzed amination reaction.
