167298-54-6Relevant articles and documents
PYRAZINE COMPOUNDS AND USES THEREOF
-
Page/Page column 116; 150-151, (2020/03/05)
The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
Novel pyrrolyl 2-aminopyridines as potent and selective human β-secretase (BACE1) inhibitors
Malamas, Michael S.,Barnes, Keith,Hui, Yu,Johnson, Matthew,Lovering, Frank,Condon, Jeff,Fobare, William,Solvibile, William,Turner, Jim,Hu, Yun,Manas, Eric S.,Fan, Kristi,Olland, Andrea,Chopra, Rajiv,Bard, Jonathan,Pangalos, Menelas N.,Reinhart, Peter,Robichaud, Albert J.
scheme or table, p. 2068 - 2073 (2010/06/19)
The proteolytic enzyme β-secretase (BACE1) plays a central role in the synthesis of the pathogenic β-amyloid in Alzheimer's disease. Recently, we reported small molecule acylguanidines as potent BACE1 inhibitors. However, many of these acylguanidines have a high polar surface area (e.g. as measured by the topological polar surface area or TPSA), which is unfavorable for crossing the blood-brain barrier. Herein, we describe the identification of the 2-aminopyridine moiety as a bioisosteric replacement of the acylguanidine moiety, which resulted in inhibitors with lower TPSA values and superior brain penetration. X-ray crystallographic studies indicated that the 2-aminopyridine moiety interacts directly with the catalytic aspartic acids Asp32 and Asp228 via a hydrogen-bonding network.
PROKINETICIN 2 RECEPTOR ANTAGONISTS
-
Page/Page column 98, (2010/11/28)
The present invention relates to certain novel compounds of Formula (I): and methods for the treatment of prokineticin 2 or prokinetin 2 receptor mediated disorders.