On September 22, 2016, Conn, P. Jeffrey; Lindsley, Craig W.; Emmitte, Kyle A.; Felts, Andrew S.; Bollinger, Katrina A. published a patent.Formula: C7H6F3NO The title of the patent was Pyridine derivatives as negative allosteric modulators of metabotropic glutamate receptor 2 and their preparation. And the patent contained the following:
Described are pyridine derivatives of formula I as neg. allosteric modulators of metabotropic glutamate receptor 2 (mGlu2), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer’s disease, or autism spectrum disorders in a subject. Compounds of formula I wherein R1 is aryl, heteroaryl, heterocyclyl and cycloalkyl; R2a and R2b are independently H, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl and C1-4 haloalkoxy; R3 is X-(C(R5)2)0-2-Z-(C(R5)2)0-2-N(R6)2, X-(C(R5)2)0-2-Z-(C(R5)2)0-2-Y-A, A’-X-(C(R5)2)0-2-Z-(C(R5)2)0-2-N(R6)2, etc.; X, Y and Z are independently C(R5)2, O, S, CO, OCO, etc.; each R5 are independently H, F, C1-4 alkyl, C1-4 alkoxy, etc.; each R6 are independently C1-6 alkyl, C1-6 haloalkyl, cycloalkyl, C1-6 heteroalkyl and heterocyclyl; N(R6)2 may be taken together form heterocyclyl; A and A’ are independently (un)substituted aryl, (un)substituted heteroaryl, (un)substituted cycloalkyl and (un)substituted heterocyclyl; R4 is CONH2 and CN; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their mGlu2 receptor modulatory activity. From the assay, it was determined that compound II exhibited IC50 value of 6850 nM and a maximum response of 5.12 %. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Formula: C7H6F3NO
The Article related to pyridine preparation mglu2 receptor neg allosteric modulator, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Formula: C7H6F3NO
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