193635-07-3Relevant academic research and scientific papers
BCL6 INHIBITORS
-
, (2019/11/04)
The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity Formula (I) wherein X1, X2, R1, R2, R30, R31 and Ring A are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
3-[2-((2S)-2-Cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramid e analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes
Coumar, Mohane Selvaraj,Chang, Chung-Nien,Chen, Chiung-Tong,Chen, Xin,Chien, Chia-Hui,Tsai, Ting-Yueh,Cheng, Jai-Hong,Wu, Hsin-Yi,Han, Chia-Hung,Wu, Ssu-Hui,Huang, Yu-Wen,Hsu, Tsu,Hsu, Li-Jen,Chao, Yu-Sheng,Hsieh, Hsing-Pang,Jiaang, Weir-Torn
, p. 1274 - 1279 (2008/02/02)
Based on the structures of NVP-DPP728 (1) and NVP-LAF237 (Vildagliptin, 2), three series of DPP-IV inhibitors were synthesized by linking substituted anilines, benzylamines, and phenylethylamines to (2S)-cyanopyrrolidine through a linker. More than 20 compounds were evaluated for their in vitro DPP-IV inhibition and selectivity profile over DPP-II, DPP8, and FAP enzymes. Selected compounds 5f and 7i showed in vivo plasma DPP-IV inhibition and inhibited glucose excursion in OGTT after oral administration in Wistar rats. Compound 5f (DPP-IV IC50 = 116 nM) has the potential for development as antidiabetic agent.
(S,S)-(+)-pseudoephedrine as chiral auxiliary in asymmetric aza-Michael reactions. Unexpected selectivity change when manipulating the structure of the auxiliary
Etxebarria, Juan,Vicario, Jose L.,Badia, Dolores,Carrillo, Luisa,Ruiz, Nerea
, p. 8790 - 8800 (2007/10/03)
The asymmetric aza-Michael reaction of metal benzylamides to α,β-unsaturated amides derived from the chiral amino alcohol (S,S)-(+)-pseudoephedrine has been studied in detail. A deep study of the most important experimental parameters (solvent, temperatur
