公开(公告)号：WO2017049383A1

公开(公告)日：2017-03-30

申请号：PCT/CA2016/000232

申请日：2016-09-14

Applicant: CYCLENIUM PHARMA INC.

Inventor： WAHHAB, Amal ,  THOMAS, Helmut ,  RICHARD, Luc ,  PETERSON, Mark L. ,  MACDONALD, Dwight ,  DUBÉ, Daniel

IPC: C40B40/04 ,  C07D498/08 ,  C40B30/00 ,  C40B30/04 ,  C40B30/06 ,  C40B30/08 ,  C40B50/00 ,  G01N33/48

CPC classification number: C07D498/08 ,  C40B40/04 ,  C40B50/00

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.

Abstract translation: 本公开涉及新的大环化合物及其含有杂芳基部分的文库，其可用作药物发现工作的研究工具。 本公开还涉及制备这些化合物的方法和文库以及使用这些文库的方法，例如在高通量筛选中。 特别地，这些文库可用于评估现有和新鉴定的药理学相关靶标（包括G蛋白偶联受体，核受体，酶，离子通道，转运蛋白，转录因子，蛋白质 - 蛋白质相互作用和核酸 - 蛋白质相互作用）的生物活性 。 因此，这些图书馆可以应用于寻找新的药剂，用于治疗和预防一系列医疗条件。

公开(公告)号：WO2018232506A1

公开(公告)日：2018-12-27

申请号：PCT/CA2018/050749

申请日：2018-06-20

Applicant: CYCLENIUM PHARMA INC.

Inventor： WAHHAB, Amal ,  DUBÉ, Daniel ,  MACDONALD, Dwight ,  PETERSON, Mark L. ,  RICHARD, Luc ,  THOMAS, Helmut

IPC: C40B40/04 ,  A61K31/395 ,  C07D487/18 ,  C12Q1/00 ,  C40B50/00 ,  G01N33/48

Abstract: The present disclosure relates to novel pyridine-containing macrocyclic compounds and libraries thereof that are useful as research tools for drug discovery efforts. This 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：WO2017197488A1

公开(公告)日：2017-11-23

申请号：PCT/CA2017/000128

申请日：2017-05-16

Applicant: CYCLENIUM PHARMA INC.

Inventor： MACDONALD, Dwight ,  DUBÉ, Daniel ,  WAHHAB, Amal ,  THOMAS, Helmut ,  RICHARD, Luc ,  PETERSON, Mark L.

IPC: C40B40/04 ,  C40B30/00 ,  C40B30/04 ,  C40B30/06 ,  C40B30/08 ,  C40B50/00 ,  G01N33/48 ,  C12Q1/00

Abstract: The present disclosure relates to novel macrocyclic compounds and libraries thereof that are useful as research tools for drug discovery efforts. This 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.

Abstract translation: 本公开涉及新的大环化合物及其文库，其可用作用于药物发现工作的研究工具。 本公开还涉及制备这些化合物和文库的方法以及使用这些文库的方法，例如高通量筛选。 特别是，这些文库可用于评估现有和新鉴定的药理学相关靶点的生物活性，包括G蛋白偶联受体，核受体，酶，离子通道，转运蛋白，转录因子，蛋白质 - 蛋白质相互作用和核酸 - 蛋白质相互作用 。 因此，这些文库可以用于寻找治疗和预防一系列医疗状况的新药物。