756771-71-8Relevant academic research and scientific papers
4-Aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators
Xiong, Hui,Brugel, Todd A.,Balestra, Michael,Brown, Dean G.,Brush, Kelly A.,Hightower, Caprice,Hinkley, Lindsay,Hoesch, Valerie,Kang, James,Koether, Gerard M.,McCauley Jr., John P.,McLaren, Francis M.,Panko, Laura M.,Simpson, Thomas R.,Smith, Reed W.,Woods, James M.,Brockel, Becky,Chhajlani, Vijay,Gadient, Reto A.,Spear, Nathan,Sygowski, Linda A.,Zhang, Minli,Arora, Jalaj,Breysse, Nathalie,Wilson, Julie M.,Isaac, Methvin,Slassi, Abdelmalik,King, Megan M.
scheme or table, p. 7381 - 7384 (2011/02/26)
Positive allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) is regarded as a potential novel treatment for schizophrenic patients. Herein we report the synthesis and SAR of 4-aryl piperazine and piperidine amides as potent mGluR5 positive allosteric modulators (PAMs). Several analogs have excellent activity and desired drug-like properties. Compound 2b was further characterized as a PAM using several in vitro experiments, and produced robust activity in several preclinical animal models.
BISAMLDE DERIVATIVES AND USE THEREOF AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 161, (2008/12/05)
A compound of formula I, or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus,
