19353-97-0Relevant academic research and scientific papers
Surveying heterocycles as amide bioisosteres within a series of mGlu7 NAMs: Discovery of VU6019278
Reed, Carson W.,Washecheck, Jordan P.,Quitlag, Marc C.,Jenkins, Matthew T.,Rodriguez, Alice L.,Engers, Darren W.,Blobaum, Anna L.,Jeffrey Conn,Niswender, Colleen M.,Lindsley, Craig W.
, p. 1211 - 1214 (2019/03/26)
This letter describes a diversity-oriented library approach to rapidly assess diverse heterocycles as bioisosteric replacements for a metabolically labile amide moiety within a series of mGlu7 negative allosteric modulators (NAMs). SAR rapidly
TRIAZOLE DERIVATIVES AS WNT SIGNALING PATHWAY INHIBITORS
-
Page/Page column 45, (2012/06/30)
The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear β-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.
Design, synthesis, and pharmacological and pharmacokinetic evaluation of 3-phenyl-5-pyridyl-1,2,4-triazole derivatives as xanthine oxidoreductase inhibitors
Sato, Takahiro,Ashizawa, Naoki,Iwanaga, Takashi,Nakamura, Hiroshi,Matsumoto, Koji,Inoue, Tsutomu,Nagata, Osamu
scheme or table, p. 184 - 187 (2009/05/26)
In an effort to find a potent xanthine oxidoreductase (XO) inhibitor, we discovered the best compound 2-[2-(2-methoxy-ethoxy)-ethoxy]-5-[5-(2-methyl-pyridin-4-yl)-1H-[1,2,4]triazol-3-yl]-benzonitrile 28. Here, we describe the following: (1) the design, synthesis, and structure-activity relationship of a series of 3-phenyl-5-pyridyl-1,2,4-triazole derivatives by in vitro studies of XO inhibitory activity in bovine milk and in vivo studies of serum uric acid (UA) reductive activity in rats, (2) a drug interaction study by a cytochrome P450 3A4 (CYP3A4) assay, and (3) a pharmacokinetic (PK) study. Compound 28 exhibits potent XO inhibitory activity, serum UA-lowering activity in rats, weak CYP3A4 inhibitory activity, and moderate PK profile.
MGLUR5 MODULATORS
-
Page/Page column 59, (2008/06/13)
The present invention is directed to compounds of formula (I) Wherein R1 to R5, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compounds and to intermediates used in
MGLUR5 MODULATORS II
-
Page/Page column 20, (2008/06/13)
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
MGluR5 modulators IV
-
Page/Page column 12, (2008/06/13)
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
mGluR5 modulators III
-
Page/Page column 14, (2008/06/13)
The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
POLYHETEROCYCLIC COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS
-
Page/Page column 69, (2010/02/13)
The present invention relates to new compounds of formula (I), wherein P, Q, X1, X2, X3, X4, X5, X6, R1, R2, R3, m, n, and p are as defined as in formula (I), or salts, or hydrates thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
