C07C233/06

Compounds Which Have a Protective Activity with Respect to the Action of Toxins and of Viruses with an Intracellular Mode of Action

The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.

Synthetic ligands that modulate the activity of the RhlR quorum sensing receptor

RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where —W— is —CO—NH—, —SO.sub.2—NH—, —CO—NH—CH.sub.2—, or —SO.sub.2—NH—CH.sub.2— are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in Pseudomonas. Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria.

Synthetic ligands that modulate the activity of the RhlR quorum sensing receptor

RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where —W— is —CO—NH—, —SO.sub.2—NH—, —CO—NH—CH.sub.2—, or —SO.sub.2—NH—CH.sub.2— are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in Pseudomonas. Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria.

Compositions for preventing and/or treating degenerative disorders of the central nervous system and/or lysosomal storage disorders
11358926 · 2022-06-14 · ·

The present invention provides novel compounds as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system and/or lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease, Alzheimer's disease and/or Gaucher's disease.

Compositions for preventing and/or treating degenerative disorders of the central nervous system and/or lysosomal storage disorders
11358926 · 2022-06-14 · ·

The present invention provides novel compounds as well as compositions and methods using the same for preventing and/or treating degenerative disorders of the central nervous system and/or lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Parkinson's disease, Alzheimer's disease and/or Gaucher's disease.

LIPIDS FOR USE IN LIPID NANOPARTICLE FORMULATIONS

Compounds are provided having the following structure:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.3, L.sup.1, L.sup.2, G.sup.1, G.sup.2 and G.sup.3 are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

Modulators of Liver Receptor Homologue 1 (LRH-1) and Uses

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.

POLY-LYSINE DERIVATIVE STABILIZE SOLID-BASED COMPOSITIONS COMPRISING ONE OR MORE SALTS

Described herein is a polymeric stabilizing agent selected from poly-lysine derivatives obtained by process including heating an aqueous lysine solution to boiling, increasing a temperature of the aqueous lysine solution to a reaction temperature in the range of about 105° C. to about 180° C., and keeping the reaction temperature in the range of about 105° C. to about 180° C. until a melt viscosity of the reaction mixture is in the range of about 350 mPa*s to about 6,500 mPa*s, and (ii) an amine number in the range of about 100 mg KOH/g to about 500 mg KOH/g is achieved. The process also includes adding alkyl-carboxylic acid or alkenyl-carboxylic acid in amounts of 2.5 mol % to 10 mol %, and increasing or keeping the reaction temperature in the range of about 105° C. to about 180° C. until number of free alkyl-carboxylic acid or alkenyl-carboxylic acid is ≤9% by weight.

POLY-LYSINE DERIVATIVE STABILIZE SOLID-BASED COMPOSITIONS COMPRISING ONE OR MORE SALTS

Described herein is a polymeric stabilizing agent selected from poly-lysine derivatives obtained by process including heating an aqueous lysine solution to boiling, increasing a temperature of the aqueous lysine solution to a reaction temperature in the range of about 105° C. to about 180° C., and keeping the reaction temperature in the range of about 105° C. to about 180° C. until a melt viscosity of the reaction mixture is in the range of about 350 mPa*s to about 6,500 mPa*s, and (ii) an amine number in the range of about 100 mg KOH/g to about 500 mg KOH/g is achieved. The process also includes adding alkyl-carboxylic acid or alkenyl-carboxylic acid in amounts of 2.5 mol % to 10 mol %, and increasing or keeping the reaction temperature in the range of about 105° C. to about 180° C. until number of free alkyl-carboxylic acid or alkenyl-carboxylic acid is ≤9% by weight.

POLY-LYSINE DERIVATIVE AND ITS USE IN SOLID-BASED COMPOSITIONS

Described herein is a poly-lysine derivative obtained by a process including heating an aqueous lysine solution to boiling, increasing a temperature of the aqueous lysine solution to a reaction temperature in the range of about 105° C. to about 180° C., and keeping the reaction temperature in the range of about 105° C. to about 180° C. until (i) a melt viscosity of the reaction mixture is in the range of about 350 mPa*s to about 6,500 mPa*s, and (ii) an amine number in the range of about 100 mg KOH/g to about 500 mg KOH/g is achieved. The process also includes adding alkyl-carboxylic acid or alkenyl-carboxylic acid in amounts of 2.5 mol % to 10 mol %, and increasing or keeping the reaction temperature in the range of about 105° C. to about 180° C. until number of free alkyl-carboxylic acid or alkenyl-carboxylic acid is ≤9% by weight.