Universitéde Montreal

Zealand Pharma A/s

Angiochem Inc.

Gaoqiang Yang

James Gillard

Marc-André Poupart

Andrew Roughton

Manuel Perez Vazquez

Jennifer L Hickey

Adam Paul Kafal

M Monzur Morshed

Anne Marinier

Michel Demeule

Guy Sauvageau

Stéphane Gingras

Yves Gareau

Irène Baccelli

Sasmita Tripathy

Christian Che

Yves Andre Chantigny

Reinhard Gabathuler

Alain Larocque

Sai Kumar Chakka

Yves Chantigny

Narendra Patel

Andrew L Roughton

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 (NK), 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

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.

There is described herein antagonists of &#x3b1;4&#x3b2;7 integrin, and more particularly to cyclic peptide antagonists. Accordingly, there is described herein a compound of formula (I) wherein R, R, R, R, R, R, Rand Rare various substituents; stereocentres 1*, 2* and 3* are each independently selected from R and S; n is 1, 2, 3, or 4 and where n is 2-4, Z is an amino terminus of an amino acid; &#x2014;C&#x2550;O&#x2014; adjacent L is the carboxy terminus of an amino acid; and L along with Z and &#x2014;C&#x2550;O&#x2014; is a peptide. 

Cyclic peptides targeting alpha-4-beta-7 integrin

There is described herein use of a compound of formula (I) below to make cyclic peptides. 

Fragment synthesis of substituted cyclic peptides

The invention relates to dendrimers conjugated to multiple targeting peptides and one or more therapeutic, diagnostic, or imaging agents for delivery of such agents across the blood-brain barrier and into certain cell types including, cells expressing the LRP-1 receptor. Also described are methods of making compounds that comprise dendrimers conjugated to targeting peptides and therapeutic, diagnostic, or imaging agents.

Peptide-dendrimer conjugates and uses thereof

The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptides having a hydrolyzable covalent bond to a therapeutic agent that includes, etoposide, etoposide 4'-dimethylglycine or doxorubicin. These polypeptide conjugates can be used as vectors to transport the podophyllotoxin derivative across the blood brain barrier (BBB) or into particular cell types such as ovary, liver, lung, or kidney. The invention also relates to pharmaceutical compositions that include the compounds of the invention and to uses thereof in methods of treatment.

Etoposide and doxorubicin conjugates for drug delivery

Growing community of inventors

Montreal, Canada

Gaoqiang Yang