- Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8- trifluoromethyl[1,2,4]triazolo[4,3- a ]pyridine (JNJ-42153605): A positive allosteric modulator of the metabotropic glutamate 2 receptor
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Advanced leads from a series of 1,2,4-triazolo[4,3-a]pyridines with mGlu2 receptor PAM activity are reported. By modification of the analogous imidazo[1,2-a]pyridine series, the newly reported leads have improved potency, in vitro ADMET, and hERG as well
- Cid, Jose María,Tresadern, Gary,Vega, Juan Antonio,De Lucas, Ana Isabel,Matesanz, Encarnación,Iturrino, Laura,Linares, María Lourdes,Garcia, Aránzazu,Andrés, José Ignacio,MacDonald, Gregor J.,Oehlrich, Daniel,Lavreysen, Hilde,Megens, Anton,Ahnaou, Abdellah,Drinkenburg, Wilhelmus,MacKie, Claire,Pype, Stefan,Gallacher, David,Trabanco, Andrés A.
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p. 8770 - 8789
(2013/01/15)
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- 1,2,3-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OR PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 ("mGluR2"), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
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Page/Page column 109
(2010/12/17)
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