Massachusetts Institute of Technology

Eagle Biologics, Inc.

Novartis Ag

Living Proof, Inc.

Kevin Thomas Love

Robert Samuel Langer

Daniel Griffith Anderson

Alexander M Klibanov

Alan Crane

Alyssa M Larson

Alisha K Weight

Delai Chen

Christopher G Levins

Kathryn Ann Whitehead

Kerry Peter Mahon

Andrew John Geall

Frederic Zecri

Luis Brito

Akinleye C Alabi

Thomas Zabawa

Gabriel Grant Gamber

Yi Heng Chen

Arturo Jose Vegas

Yizhou Dong

Yunlong Zhang

David Thomas Puerta

Lorna Nagamoottoo-Casse

Robert S Langer, Jr

Robert S Langer

Akinleye Alabi

Yi Chen

Concentrated, low-viscosity, low-volume liquid pharmaceutical formulations of proteins have been developed. Such formulations can be rapidly and conveniently administered by subcutaneous or intramuscular injection, rather than by lengthy intravenous infusion. These formulations include low-molecular-weight and/or high-molecular-weight proteins, such as mAbs, and viscosity-reducing ionic liquids.

Liquid protein formulations containing 4-ethyl-4-methylmorpholinium methylcarbonate (EMMC)

Concentrated, low-viscosity, low-volume liquid pharmaceutical formulations of proteins have been developed. Such formulations can be rapidly and conveniently administered by subcutaneous (SC) or intramuscular (IM) injection, rather than by lengthy intravenous infusion. These formulations include low-molecular-weight and/or high-molecular-weight proteins, such as mAbs, and organophosphates. The viscosity of the formulation is significantly reduced by the addition of one or more organophosphates.

Liquid protein formulations containing cyclic adenosine monophosphate (cAMP) or adenosine triphosphate (ATP)

Concentrated, low-viscosity, low-volume liquid pharmaceutical formulations of polysaccharides and nucleic acids have been developed. Such formulations can be rapidly and conveniently administered by subcutaneous or intramuscular injection, rather than by lengthy intravenous infusion. These formulations include low-molecular-weight and/or high-molecular-weight polysaccharides and nucleic acids, and viscosity-lowering agents.

Polysaccharide and nucleic acid formulations containing viscosity-lowering agents

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as 'APPLs'. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R', R, R, R, R, R, R, Z, W, Y, and Z are as defined herein.

Amino acid-, peptide- and polypeptide-lipids, isomers, compositions, and uses thereof

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R-R, L, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Lipids and lipid compositions for the delivery of active agents

Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

Aminoalcohol lipidoids and uses thereof

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R-R, n, p, Land Lare defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Concentrated, low-viscosity, low-volume liquid pharmaceutical formulations of proteins have been developed. Such formulations can be rapidly and conveniently administered by subcutaneous or intramuscular injection, rather than by lengthy intravenous infusion. These formulations include low-molecular-weight and/or high-molecular-weight proteins, such as mAbs, and viscosity-lowering agents that are typically bulky polar organic compounds, such as many of the GRAS (US Food and Drug Administration List of compounds generally regarded as safe) and inactive injectable ingredients and FDA approved therapeutics.

Liquid Protein Formulations Containing Thiamine

Liquid protein formulations containing 4-(3-butyl-1-imidazolio)-1-butane sulfonate (BIM)

Liquid protein formulations containing thiamine pyrophosphate (TPP)

Liquid protein formulations containing cimetidine

This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R-R, n, p, Land Lare defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues. 

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Boston, MA, United States of America

Kevin Thomas Love