A61K47/542

ENZYME AND RECEPTOR MODULATION

Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

Methods of Treating Multiple Sclerosis
20180000770 · 2018-01-04 ·

Provided herein are methods of treating multiple sclerosis with a fumarate, wherein the fumarate is a dialkyl fumarate, a monoalkyl fumarate, a combination of a dialkyl fumarate and a monoalkyl fumarate, a prodrug of monoalkyl fumarate, a deuterated form of any of the foregoing, or a pharmaceutically acceptable salt, clathrate, solvate, tautomer, or stereoisomer of any of the foregoing, or a combination of any of the foregoing. The methods provided herein improve the safety of treatment by informing and monitoring patients undergoing treatment regarding progressive multifocal leukoencephalopathy, and/or by monitoring lymphocyte count.

Amino Acid and Peptide Conjugates and Uses Thereof

The present invention relates to peptides, and amino acid and peptide conjugates, methods for making amino acid and peptide conjugates, conjugates produced by the methods, pharmaceutical compositions comprising the peptides and conjugates, methods of eliciting immune responses in a subject and methods of vaccinating a subject, uses of the peptides and conjugates for the same, and uses of the peptides and conjugates in the manufacture of medicaments for the same.

LIPID NANOPARTICLE COMPOSITIONS
20180000953 · 2018-01-04 ·

Disclosed herein are nanoparticle compositions including an mRNA and a lipid component and methods of using the same. The present invention provides compositions and methods involving lipid-containing nanoparticle compositions to deliver mRNA to cells. In one aspect, the invention provides a nanoparticle composition including (i) a lipid component including a phospholipid (which may or may not be unsaturated), a PEG lipid, a structural lipid, and a compound of formula (I) and (ii) an mRNA encoding a polypeptide of interest.

USE OF PLL FOR IMPROVING THE STABILITY OF MOLECULES IN SOLUTION
20180008722 · 2018-01-11 ·

The invention relates to a molecular complex comprising at least one polylysine conjugate (PLL), comprising a main PLL straight chain and at least one molecule F having an average molecular weight of between 50 daltons and 1000 daltons that is covalently bonded to said main chain, and at least one molecule M that is unstable in solution, the conjugate(s) and the molecule(s) M being bonded by means of a non-covalent bond. The invention also relates to a composition comprising a complex of this kind, to a method for obtaining said composition and use thereof, and to the use of one or more PLL-based conjugates for improving the hydrophilicity, the effectiveness, and the activity of a molecule that is unstable in solution, over a time period that is compatible with the use of said molecule. The invention also relates to a method for identifying a PLL-based conjugate or a combination of a plurality of PLL-based conjugates that makes it possible to improve the hydrophilicity, the effectiveness, and the activity of a molecule that is unstable in solution, and to a kit for implementing said method.

Ligand capable of multivalently binding to glutamine transporter, and composition comprising same

The present invention pertains to a ligand that contains a plurality of groups represented by formula (1) and is capable of multivalently binding to a glutamine transporter expressed in excess in a cancer cell compared to a normal cell.

PHARMACEUTICAL COMPOSITION WITH ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY
20180008717 · 2018-01-11 ·

A composition comprising a compound having a formula I:

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wherein T is derivative of a terpene and R is a derivative of a neurotransmitter acids, wherein the neurotransmitter acids are selected form GABA, glycine, and taurine. Pharmaceutical formulations for oral and topical use as analgesics and anti-inflammatories are also provided. A process for preparing the composition and the formulations are also provided.

Multi-Tyrosine Kinase Inhibitors Derivatives and Methods of Use
20180009758 · 2018-01-11 ·

The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.

Method for Treating Psoriasis
20230233505 · 2023-07-27 ·

A method for treating psoriasis including the steps of applying an isothiocyanate functional surfactant to an area affected by psoriasis, wherein the isothiocyanate functional surfactant comprises at least one isothiocyanate functional group associated with an aliphatic and/or aromatic carbon atom of the isothiocyanate functional surfactant.

CONTACT LENS PRODUCT WITH CORNEA REPAIR FUNCTION
20230233602 · 2023-07-27 ·

A contact lens product having a cornea repair function includes a composition in the form of a solution. The composition includes gold nanoparticles and at least one auxiliary repairing ingredient. The gold nanoparticles are present in an effective concentration from 0.01 ppm to 3000 ppm and have an average particle size from 0.01 nm to 100 nm. The at least one auxiliary repairing ingredient is selected from the group consisting of chondroitin sulfate, α-lipoic acid, 2-aminoethanesulfonic acid, and potassium L-aspartate and present in an amount greater than 0 wt % and less than 20 wt % based on the composition being 100 wt %.