A61K31/542

Multilayer Biodegradable Microparticles for Sustained Release of Therapeutic Agents

Microparticles are prepared by a method that includes: (a) forming a layer comprising a first polymer on a solid surface by depositing a first composition one or more times on the solid surface, wherein the first composition comprises the first polymer and a first solvent, and evaporating the first solvent in the first composition; (b) forming one or more layers comprising a second polymer and a therapeutic agent by depositing a second composition on all or part of the layer formed in step (a), wherein the second composition comprises the second polymer, the therapeutic agent, and a second solvent; and evaporating the second solvent in the second composition; and (c) forming an additional layer comprising a third polymer by depositing a third composition one or more times on a previously formed layer, wherein the third composition comprises the third polymer and a third solvent; and evaporating the third solvent in the third composition.

Condensed heterocyclic derivates as BCL-2 inhibitors for the treatment of neoplastic diseases
11680072 · 2023-06-20 · ·

The disclosure includes compounds of Formula (A): ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, and R.sub.12, j, k, m, n, Y, W, W.sub.1, W.sub.2, W.sub.3, V, L, Z.sub.1, Q.sub.1, Q.sub.2, Q.sub.3, and Q.sub.4, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neurodegenerative disease with these compounds.

Condensed heterocyclic derivates as BCL-2 inhibitors for the treatment of neoplastic diseases
11680072 · 2023-06-20 · ·

The disclosure includes compounds of Formula (A): ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, and R.sub.12, j, k, m, n, Y, W, W.sub.1, W.sub.2, W.sub.3, V, L, Z.sub.1, Q.sub.1, Q.sub.2, Q.sub.3, and Q.sub.4, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neurodegenerative disease with these compounds.

Use of condensed benzo[B]thiazine derivatives as cytoprotectants
09827249 · 2017-11-28 · ·

The present invention relates to arylthiazine compounds, metabolites, N-oxides, amides, esters, pharmaceutically acceptable salts, hydrates and solvates thereof and their use as cytoprotectants in the treatment or prophylaxis of diseases or states, either acute or chronic, involving aberrant cellular lipid peroxidation in the central nervous system or in the periphery of the body. The present invention also relates to a method for their preparation and to pharmaceutical composition comprising as an active ingredient one or more of the aforementioned compounds.

Use of condensed benzo[B]thiazine derivatives as cytoprotectants
09827249 · 2017-11-28 · ·

The present invention relates to arylthiazine compounds, metabolites, N-oxides, amides, esters, pharmaceutically acceptable salts, hydrates and solvates thereof and their use as cytoprotectants in the treatment or prophylaxis of diseases or states, either acute or chronic, involving aberrant cellular lipid peroxidation in the central nervous system or in the periphery of the body. The present invention also relates to a method for their preparation and to pharmaceutical composition comprising as an active ingredient one or more of the aforementioned compounds.

METHODS OF EXTENDING LIFESPAN BY ADMINISTERING FERROPTOSIS INHIBITORS

Provided herein is a method of extending the lifespan of an organism comprising administering to the organism an effective amount of a ferroptosis inhibitor. Also provided are compositions for extending lifespan comprising ferroptosis inhibitors.

METHODS OF EXTENDING LIFESPAN BY ADMINISTERING FERROPTOSIS INHIBITORS

Provided herein is a method of extending the lifespan of an organism comprising administering to the organism an effective amount of a ferroptosis inhibitor. Also provided are compositions for extending lifespan comprising ferroptosis inhibitors.

Sustained Release Formulation and Use Thereof

Provided herein are extended release polymers. In one aspect, a composition for sustained release of active ingredients comprises a block polymer having formula: PEG-PCL-PLA-PCL-PEG or PGA-PCL-PEG-PCL-PGA. The extended release block polymers modulate drug release rate based on the hydrophobicity of the PTSgel polymer irrespective of the nature of drug. PTSgel polymers are biodegradable, thermosensitive, and compatible with hydrophilic, hydrophobic, and combinations thereof, biologic or chemical active agents.

ANTIMICROBIAL FUSION PEPTIDES
20220054584 · 2022-02-24 ·

Antimicrobial peptides, compositions and methods are described that are useful for treating infectious disease, including those caused by drug resistant Gram-negative bacteria (e.g., Pseudomonas and Acinetobacter) and parasite-caused disease such as malaria. The peptides include a modular kinocidin gamma-core connected directly, or through a short spacer, to a kinocidin C-terminal alpha-helix.

LIQUID PENTABLOCK CO-POLYMER FORMULATIONS FOR SUSTAINED DELIVERY OF THERAPEUTICS

Provided herein are amphiphilic polymers compositions for making aqueous formulations. In one aspect, a solution composition for delivery and release of active ingredients comprises a block co-polymer having formula: PEG-PCL-PLA-PCL-PEG or PGA-PCL-PEG-PCL-PGA or PLA-PCL-PEG-PCL-PLA or PCL-PLA-PEG-PLA-PCL or PCL-PGA-PEG-PGA-PCL. The block co-polymers are biodegradable, stable and compatible with hydrophilic, hydrophobic, and combinations thereof, biologic or chemical active agents. In some embodiments, the block co-polymers enable sustained and/or continuous release of various active agents. In certain embodiments, the block co-polymers can be used to make an artificial tear preparation, a lubricant for joints or wound cover or adhesive.