A61K31/4015

ALKALOIDS FROM SPONGE, SCAFFOLDS FOR THE INHIBITION OF HUMAN IMMUNODEFICIENCY VIRUS (HIV)

Anti-viral compounds with low cytotoxicity are identified from screening of products found in Red Sea sponges, including the sponge Stylissa carteri. The identified compounds can be brominated pyrrole-2-aminoimidazole alkaloids and derivatives thereof. Specific examples of identified compounds include oroidin, hymenialdisine, and debromohymenialdisine, as well as derivatives thereof. The compounds also can be useful scaffolds or pharmacores for further chemical modification and derivatization. Selected compounds, particularly oroidin, show selective anti-viral HIV-1 activity coupled with reduced cytotoxicity. The compounds can function as HIV reverse-transcriptase inhibitors, and molecular modeling can be used to confirm inhibition.

COVALENT INHIBITORS OF CDK-7
20180008604 · 2018-01-11 ·

The disclosure includes compounds of Formula (I)

##STR00001## wherein R.sub.0, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

Phenylpyrrolidinone formyl peptide 2 receptor agonists

The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. ##STR00001##

Phenylpyrrolidinone formyl peptide 2 receptor agonists

The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. ##STR00001##

METHODS OF PERMEABILIZING THE BLOOD BRAIN BARRIER
20230233481 · 2023-07-27 ·

The present invention relates to using monoterpene or sesquiterpene to permeabilize the blood brain barrier.

METHODS OF PERMEABILIZING THE BLOOD BRAIN BARRIER
20230233481 · 2023-07-27 ·

The present invention relates to using monoterpene or sesquiterpene to permeabilize the blood brain barrier.

METHODS AND COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF HEARING LOSS

In one aspect, pharmaceutical compositions comprising a CDK2 inhibitor and one or more of at least one agent known to treat a hearing impairment and at least one agent known to prevent a hearing impairment, and methods of treating and/or preventing hearing impairments or disorders using the compositions are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

METHODS AND COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF HEARING LOSS

In one aspect, pharmaceutical compositions comprising a CDK2 inhibitor and one or more of at least one agent known to treat a hearing impairment and at least one agent known to prevent a hearing impairment, and methods of treating and/or preventing hearing impairments or disorders using the compositions are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Gasdermin D (GSDMD) Succination for the Treatment of Inflammatory Disease

Described herein are compositions and methods for treating inflammation, and inflammation-related conditions, using fumarate or fumarate analogs or inhibitors of fumarate hydratase (FH).

Gasdermin D (GSDMD) Succination for the Treatment of Inflammatory Disease

Described herein are compositions and methods for treating inflammation, and inflammation-related conditions, using fumarate or fumarate analogs or inhibitors of fumarate hydratase (FH).