1,6- Diazabicyclo [3,2,1] octan-7-one derivatives and their use in the treatment of bacterial infections
申请人:Patel Mahesh Vithalbhai
公开号:US20140148431A1
公开(公告)日:2014-05-29
Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.
公式(I)的化合物,其制备和在预防或治疗细菌感染中的应用被披露。
[EN] 1,3,4-OXADIAZOLE AND THIADIAZOLE COMPOUNDS AS IMMUNOMODULATORS<br/>[FR] COMPOSÉS 1,3,4-OXADIAZOLES ET THIADIAZOLES UTILISÉS COMME IMMUNOMODULATEURS
申请人:AURIGENE DISCOVERY TECH LTD
公开号:WO2016142852A1
公开(公告)日:2016-09-15
The present invention relates to 1,3,4-oxadiazole and thiadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.
作者:Eunhwa Ko、Jing Liu、Lisa M. Perez、Genliang Lu、Amber Schaefer、Kevin Burgess
DOI:10.1021/ja1071916
日期:2011.1.26
This paper concerns peptidomimetic scaffolds that can present side chains in conformations resembling those of amino acids in secondary structures without incurring excessive entropic or enthalpic penalties. Compounds of this type are referred to here as minimalist mimics. The core hypothesis of this paper is that small sets of such scaffolds can be designed to analogue local pairs of amino acids (including noncontiguous ones) in any secondary structure; i.e., they are universal peptidomimetics. To illustrate this concept, we designed a set of four peptidomimetic scaffolds. Libraries based on them were made bearing side chains corresponding to many of the protein-derived amino acids. Modeling experiments were performed to give an indication of kinetic and thermodynamic accessibilities of conformations that can mimic secondary structures. Together, peptidomimetics based on these four scaffolds can adopt conformations that resemble almost any combination of local amino acid side chains in any secondary structure. Universal peptidomimetics of this kind are likely to be most useful in the design of libraries for high-throughput screening against diverse targets. Consequently, data arising from submission of these molecules to the NIH Molecular Libraries Small Molecule Repository (MLSMR) are outlined.