University of Alberta

Alberta Health Services

Greencentre Canada

Dennis Hall

Michael Weinfeld

Todd Randall Mereniuk

Edan Foley

Feridoun Karimi-Busheri

Gary Kenneth Freschauf

Afsaneh Lavasanifar

Sylvain Bernard

Timothy Morgan

Raed Al-Zoubi

Vikie Lamontagne

Nicolas Gernigon

Zahra Shire

Raed M Al-Zoubi

Tristan Verdelet

Paul D Thornton

Olivier Marion

There is described herein imidopiperidine compounds as inhibitors of human polynucleotide kinase phosphatase.

Imidopiperidine compounds as inhibitors of human polynucleotide kinase phosphatase

There is described herein compounds, compositions and methods for inducing synthetic lethality in a cancer cell(s).

Synthetic lethality in cancer

The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions.

Small molecule inhibitors of polynucleotide kinase/phosphatase, poly(ADP-ribose) polymerase and uses thereof

The present application provides methods and catalysts for activation of carboxylic acids for organic reactions. In particular, methods are disclosed for direct nucleophilic addition reactions, such as, amidation reactions with amines, cycloadditions, and conjugate additions, using boronic acid catalysts of formula I, II or III: Also included are novel boronic acid catalysts of formula IV, V and III: 

Boronic acid catalysts and methods of use thereof for activation and transformation of carboxylic acids

The present disclosure describes operationally simple methods for the low temperature, catalytic activation of carboxylic acids for organic reactions, in particular for direct amidation reactions with amines. The methods involve the use of orthosubstituted arylboromc acids of the formula (I), wherein the groups Rto Rare as defined herein. In preferred embodiments Ris halogen. The arylboromc acids catalyze nucleophilic 1,2-addition reactions, conjugate 1,4-addition reactions, and cycloaddition reactions, including Diels-Alder reactions involving &#x3b1;,&#x3b2;-unsaturated carboxylic acids. 

Method for the organocatalytic activation of carboxylic acids for chemical, reactions using orthosubstituted arylboronic acids

The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.

Preparation and uses of conjugated solid supports for boronic acids

Growing community of inventors

Edmonton, Canada

Dennis Hall