University of Alberta

Wisconsin Alumni Research Foundation

Glen S. Kwon

Afsaneh Lavasanifar

John Samuel

Abdullah Mahmud

Glen S Kwon

Dennis Hall

Michael Weinfeld

Sylvain Bernard

Tristan Verdelet

Timothy Morgan

Vikie Lamontagne

Zahra Shire

Anthony Ernest Bolton

Mahmud Abdullah

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

Imidopiperidine compounds as inhibitors of human polynucleotide kinase phosphatase

The present invention relates to micelle-forming poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups on the polyester block therein. The biodegradability of these copolymers and their biocompatibilities with a large number of bioactive agents make them suitable as carriers for various bioactive agents. The bioactive agents, such as DNA, RNA, oligonucleotide, protein, peptide, drug and the like, can be coupled to the reactive groups on the polyester block of the copolymer.

Poly(ethylene oxide)-block-poly(ester) block copolymers

Provided are methods and compositions for reducing the toxicity of certain hydrophobic therapeutic agents, especially polyene antibiotics, in particular, Amphotericin B (AmB), and therapeutics such as paclitaxel, tamoxifen, an acylated prodrug or an acylated cis-platin, by incorporating these agents within micelles comprising an amphiphilic block-forming copolymer. Where the polyene is amphotericin B, desirably the spacer is an alkyl molecule of aabout 2 to about 8 carbon atoms, desirably 6 carbon atoms, and the core is an N-alkyl molecule of about 8 to about 28 carbon atoms, desirably 12 to 22 carbon atoms, advantageously, 12 to 18 carbon atoms, and as specifically embodied, 18 carbon atoms (stearate moiety). For the formulation of a larger polyene, the spacer and core are proportionately larger than those for amphotericin B. As specifically exemplified herein, the polymer backbone is a PEO of about 270 units with about 10-30 core-forming PLAA subunits, and advantageously about 14-24. Desirably the stearate moiety has a substitution level on the copolymer from about 35 percent to about 70 percent.

Methods and compositions for polyene antibiotics with reduced toxicity

Growing community of inventors

Edmonton, Canada

Afsaneh Lavasanifar