The University of British Columbia

Ab Science

Tekmira Pharmaceuticals Corporation

Centre National De La Recherche Scientifique

Universite Claude Bernard – Lyon1

Pierre Fabre Dermo-cosmetique

Arbutus Biopharma Corporation

Aviragen Therapeutics, Inc.

Nanovation Therapeutics Inc.

Obe Therapy Biotechnology

Alnylam Pharmaceuticals, Inc.

Anaconda Pharma

Marco A Ciufolini

Pieter Rutter Cullis

Marcel B Bally

Igor V Jigaltsev

Norbert Maurer

Pieter R Cullis

Barbara Mui

Jianxin Chen

Michael J Hope

Alain Moussy

Thomas D Madden

Bruno Giethlen

Camille Georges Wermuth

Sean C Semple

Barbara Low Shoud Mui

Muthiah Manoharan

Kallanthottathil G Rajeev

Muthusamy Jayaraman

Marta Blumenfeld

David Butler

Pascal Bordat

Kim F Wong

Jayaprakash K Narayanannair

Delphine Compere

Willy Picoul

Roger Tarroux

Itzik Harosh

Fariba Saadati

Deaglan Arnold

Sandrine Braud

Huy Tran

Nagavenkata Durga Prasad Atmuri

Norbert Mauer

Joshua Zaifman

Yuen Yi Tam

Srinivasulu Masuna

Masunu Srinivasulu

Provided herein is an ionizable, cationic amino lipid or a pharmaceutically acceptable salt thereof. The ionizable, cationic amino lipid has:

Sulfur-containing ionizable lipids for the delivery of nucleic acids and other therapeutic agents

This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.

Lipid-linked prodrugs

The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

Amino lipids and methods for the delivery of nucleic acids

Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.

Modified drugs for use in liposomal nanoparticles

The invention relates to a method for producing a hydrazine of general formula (I) and the pharmaceutically acceptable salts thereof from an amine of formula (II), characterised in that said method uses a urea of formula (III) as a synthesis intermediate. 

Method for the synthesis of a hydrazine that can be used in the treatment of the papilloma virus

Novel compounds, particularly derivatives of boroarginine, boroornithine and borolysine that selectively modulate, regulate, and/or inhibit enteropeptidase. Compositions, particularly pharmaceutical compositions, as well as methods to treat excess weight, obesity and diseases associated with an abnormal fat metabolism.

Boropeptide inhibitors of enteropeptidase and their uses in treatment of obesity, overweight and/or diseases associated with an abnormal fat metabolism

Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.

2-(3-aminoaryl) amino-4-aryl-thiazoles and their use as c-kit inhibitors

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures XIV or XVII. 

Lipids and compositions for the delivery of therapeutics

Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.

Growing community of inventors

Vancouver, Canada

Marco A Ciufolini