The University of British Columbia

Provincial Health Services Authority

British Columbia Cancer Agency Branch

David Perrin

François Bénard

Zhibo Liu

Chengcheng Zhang

Kuo-Shyan Lin

Kuo-shyan Lin

Hsiou-ting Kuo

Mihajlo Todorovic

Richard Ting

Zhengxing Zhang

Hsiou-Ting Kuo

Jinhe Pan

Aron Roxin

Mathieu Lepage

Rajaguru Kandasamy

Sungjoon Huh

Francois Bénard

Maral Pourghiasian

Christopher Overall

A compound or molecular complex. The compound or molecular complex comprises: a metal chelator configured for chelation with a radioactive isotope or a non-radioactive isotope; and a trifluoroborate (BF)-containing moiety configured forF/F exchange or a precursor thereof; and optionally a cell-targeting domain.

Dual mode 18F-labelled theranostic compounds and uses thereof

The invention described herein is based in part on the discovery of a protein/peptide crosslink, which introduces fluorescent properties, and which has been applied to synthesize analogues of melanocortin and amanitin as choice peptides to be explored in the context of isoindole peptides. Without limitation, it is expected that those trained in the art of peptide synthesis and stapling would appreciate the consequences of this invention such that other peptides of varied length can be similarly constrained by isoindole staples as featured herein.

Cyclic peptide analogs of melanocortin and amanitin and methods of making such

A compound comprising a prostate specific membrane antigen (PSMA)-targeting moiety of the following formula or of a salt or a solvate thereof. Ris O or S. Each of R, Rand Rmay be &#x2014;COH, &#x2014;SOH, &#x2014;SOH, &#x2014;POH, or &#x2014;POH, for example. Rmay be methylene or a derivative thereof, propylene or a derivative thereof, or a derivative of ethylene, optionally substituted. Ris a linker. When the PSMA-targeting moiety is linked to a radiolabeling group, the compound may be used as an imaging agent or therapeutic agent for PSMA-expressing diseases/conditions. 

Radiolabeled compounds targeting the prostate-specific membrane antigen

Fluoridated organofluoroborates comprising at least oneF atom and precursors thereto, for use in PET scanning.

Substituted organofluoroborates as imaging agents

This disclosure relates to novel compounds comprising a zwitterionic trifluoroborate prosthetic group which target prostate-specific membrane antigen (PSMA), e.g. in prostate cancer. The compounds have Formula I, wherein each R1 is an anionic group, L is a linker and R2B-F3 is &#x2014;N(R)CHBF, a pyridinium group substituted with BFor methyl BF, or an azole group substituted with methyl BF3. Methods and uses of imaging and treating PSMA-expressing cancers are also disclosed. 

18/19F-labelled compounds which target the prostate specific membrane antigen

Somatostatin derivative compounds of general formula (I) that may be readily labelled with the isotope fluorine-18 and that have affinity and selectivity for cellular somatostatin receptors are provided. The labelled compounds are useful clinically as radioactive tracers in various in vivo imaging applications (for example, using positron emission tomography (PET) and related techniques) to detect somatostatin-expressing cells and tissues, including tumors, or as therapeutic agents.

Compositions and methods for imaging cancer

Substituted aryl-boron compounds comprising at least oneF atom, as illustrated by the formula (I), where at least one of Yor YisF and Ais a substituted aromatic ring, with Gbeing, independently, C or N, and where the substitutents of the aromatic ring or polycyclic moiety (other than boron) comprise at least one electron-withdrawing group (EWG), providing that sigma total (&#x3c3;) for all substituents on the aromatic ring or polycyclic moiety except B is about 0.06 or more when said at least one EWG is positioned ortho to B, or about 0.2 or more when no EWG is positioned ortho to B. The compounds include neutral (N=1) and ionic borate (N=2) embodiments. The compounds are useful as positron emission tomography (PET) imaging agents. 

Substituted aryl-fluoroborates as imaging agents

Positron emitting compounds and methods of their production are provided. The compounds have the formula: (F)m G (R)n wherein each R is a group comprising at least one carbon, nitrogen, phosphorus or sulfur atom and G is joined to R through said carbon, nitrogen, phosphorus or sulfur atom; G is silicon or boron; m is 2 to 5 and n is 1 to 3 with m+n=3 to 6 when G is silicon; m is 1 to 3 and n is 1 to 3 with m+n=3 to 4 when G is boron; and wherein the compound further comprises one or more counterions when the above formula is charged; and wherein at least one F is 18F.

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Vancouver, Canada

David Perrin