公开(公告)号：US10981931B2

公开(公告)日：2021-04-20

申请号：US16521904

申请日：2019-07-25

Applicant: CYCLENIUM PHARMA INC.

Inventor： Amal Wahhab ,  Helmut Thomas ,  Luc Richard ,  Mark L. Peterson ,  Dwight MacDonald ,  Daniel Dubé

IPC: C07D498/00 ,  C07D497/00 ,  C07D497/02 ,  C07D498/08 ,  C40B40/04 ,  C07D498/02 ,  G01N33/50 ,  C40B50/00 ,  C40B30/04 ,  C40B30/06

Abstract: The present disclosure relates to novel macrocyclic compounds and libraries thereof containing heteroaryl moieties that are useful as research tools for drug discovery efforts. The present disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.

公开(公告)号：US10407442B2

公开(公告)日：2019-09-10

申请号：US15761371

申请日：2016-09-14

Applicant: CYCLENIUM PHARMA INC.

Inventor： Amal Wahhab ,  Helmut Thomas ,  Luc Richard ,  Mark L. Peterson ,  Dwight Macdonald ,  Daniel Dubé

IPC: C07D497/00 ,  C07D497/02 ,  C07D498/00 ,  C07D498/02 ,  C07D498/08 ,  G01N33/50 ,  C40B50/00 ,  C40B40/04 ,  C40B30/04 ,  C40B30/06

Abstract: The present disclosure relates to novel macrocyclic compounds and libraries thereof containing heteroaryl moieties that are useful as research tools for drug discovery efforts. The present disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.