Universitéde Montreal

Yves Chantigny

Anne Marinier

Guy Sauvageau

Stéphane Gingras

Bruno Simoneau

Michel Bouvier

Gaoqiang Yang

Yves Gareau

Patricia René

Réjean Ruel

Philippe Dagneau

Irène Baccelli

Jonathan Yeh

Heterocyclic compounds of Formula (I) and pharmaceutically acceptable salt thereof are disclosed. The use of such heterocyclic compounds and pharmaceutically acceptable salt thereof for the treatment of cancers, and more particularly cancers sensitive to mitochondrial activity inhibition and increased reactive oxygen species (ROS) levels, is also disclosed. Such cancers include acute myeloid leukemia (AML), preferably AML characterized by certain features, such as high level of expression of one or more Homeobox (HOX)-network genes, high and/or low expression of specific genes, the presence of one or more cytogenetic or molecular risk factors such as intermediate cytogenetic risk, Normal Karyotype (A/K), mutated NPM1, mutated CEBPA, mutated FLT3, mutated DNMT3A, mutated TET2, mutated IDH1, mutated IDH2, mutated RUNX1, mutated WT1, mutated SRSF2, intermediate cytogenetic risk with abnormal karyotype (intern(abnK)), trisomy 8 (+8) and/or abnormal chromosome (5/7), and/or a high leukemic stem cell (LSC) frequency.

Heterocyclic mitochondrial activity inhibitors and uses thereof

The invention relates to compounds as described herein and pharmaceutical compositions containing them. Also, the invention relates to methods for expanding stem cells and/or progenitor cells and methods for treating a hematopoietic disorder/malignancy, an autoimmune disease and/or an inherited immunodeficient disease.

Compounds and use thereof in the expansion of stem cells and/or progenitor cells

Disclosed herein is a compound of Formula I: wherein X, R, R, and Rare as defend herein, or a pharmaceutically acceptable salt thereof to allow the drug to penetrate the cell membrane; or a prodrug, or the compound is labeled with a detectable label or an affinity tag thereof. Also disclosed is a pharmaceutical composition, a method of treating a disorder mediated by melanocortin-4 receptors, and a method of treating obesity using the compounds described. 

Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators

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Pincourt, CA, United States of America

Yves Chantigny