[EN] QUINOLINE DERIVATIVES<br/>[FR] DÉRIVÉS DE QUINOLINE
申请人:CHRONOGEN INC
公开号:WO2008014602A1
公开(公告)日:2008-02-07
[EN] The invention relates to new quinoline derivatives which are active CLK-1 inhibitors. More specifically, the CLK-1 inhibitors of the invention are compounds of formula (A). The invention also relates to pharmaceutical compositions comprising such compounds and to methods for the prophylaxis and/or treatment of disorders or their associated symptoms for which the inhibition of CLK-1 is beneficial. [FR] L'invention concerne de nouveaux dérivés de quinoline constituant des inhibiteurs actifs de CLK-1. Les inhibiteurs de CLK-1 de l'invention sont, plus spécifiquement, des composés représentés par la formule (A). L'invention concerne également des compositions pharmaceutiques contenant lesdits composés et des méthodes prophylactiques et/ou thérapeutiques de troubles ou des symptômes associés dans lesquels l'inhibition de CLK-1 est bénéfique.
[EN] SMALL MOLECULE INHIBITORS OF GRP78 AND USES THEREOF<br/>[FR] INHIBITEURS À PETITES MOLÉCULES DE GRP78 ET LEURS UTILISATIONS
申请人:[en]THE REGENTS OF THE UNIVERSITY OF MICHIGAN
公开号:WO2022169834A2
公开(公告)日:2022-08-11
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules as defined within Formula I (as defined herein) which function as inhibitors of glucose-regulated protein 78 (GRP78) within cancer cells and/or immune cells, and which function as effective therapeutic agents for treating, ameliorating, and preventing various forms of cancer (e.g., pancreatic cancer), viral infections (e.g. SARS-CoV-2), and inflammatory diseases. In addition, this invention also relates to a new class of PROTACs having Formulas II, III and IV (as defined herein) which function as degraders of GRP78 within cancer and/or immune cells. Pharmaceutical compositions comprising said compounds of Formulas I, II, III, or IV are also within the scope of the present invention.