215797-81-2Relevant articles and documents
Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease
Panarese, Joseph D.,Engers, Darren W.,Wu, Yong-Jin,Bronson, Joanne J.,Macor, John E.,Chun, Aspen,Rodriguez, Alice L.,Felts, Andrew S.,Engers, Julie L.,Loch, Matthew T.,Emmitte, Kyle A.,Castelhano, Arlindo L.,Kates, Michael J.,Nader, Michael A.,Jones, Carrie K.,Blobaum, Anna L.,Conn, P. Jeffrey,Niswender, Colleen M.,Hopkins, Corey R.,Lindsley, Craig W.
supporting information, p. 255 - 260 (2018/10/25)
Herein, we report the discovery of a novel potent, selective, CNS penetrant, and orally bioavailable mGlu4 PAM, VU0652957 (VU2957, Valiglurax). VU2957 possessed attractive in vitro and in vivo pharmacological and DMPK properties across species.
ISOQUINILINE AND NAPTHALENE-SUBSTITUTED COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOUNDS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION
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Page/Page column 67; 68, (2016/08/23)
Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treat
ARYL LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
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Page/Page column 36, (2015/06/03)
The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhbiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.