A61K31/381

TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.

COMPOSITIONS AND METHODS OF TREATING CARDIAC HYPERTROPHY AND HEART FAILURE
20230087562 · 2023-03-23 ·

A method of treating cardiac hypertrophy and/or heart failure in a subject includes administering to the subject a therapeutically effective amount of a REV-ERBα agonist.

COMPOSITIONS AND METHODS OF TREATING CARDIAC HYPERTROPHY AND HEART FAILURE
20230087562 · 2023-03-23 ·

A method of treating cardiac hypertrophy and/or heart failure in a subject includes administering to the subject a therapeutically effective amount of a REV-ERBα agonist.

METHODS OF INHIBITING TUMOR METASTASIS
20230090578 · 2023-03-23 ·

Thromboxane A2 receptor antagonists, such as ifetroban, inhibit solid tumor metastasis. The formation of surface and microscopic lung metastases are inhibited. Thromboxane A2 receptor antagonists can inhibit the tumor metastasis process without affecting the growth or development of a primary tumor.

INHIBITORS OF HUMAN DEUBIQUITINASES FOR THE TREATMENT OF CORONAVIRAL INFECTIONS
20230087388 · 2023-03-23 ·

The present application relates to small molecule inhibitors of human deubiquitinases for use in the prevention or treatment of a coronaviral infection. It relates in particular to small molecule inhibitors of USP7 and USP47. Pharmaceutical compositions, respective advantageous formulation techniques and a method of treatment are disclosed.

INHIBITORS OF HUMAN DEUBIQUITINASES FOR THE TREATMENT OF CORONAVIRAL INFECTIONS
20230087388 · 2023-03-23 ·

The present application relates to small molecule inhibitors of human deubiquitinases for use in the prevention or treatment of a coronaviral infection. It relates in particular to small molecule inhibitors of USP7 and USP47. Pharmaceutical compositions, respective advantageous formulation techniques and a method of treatment are disclosed.

METHODS OF TREATING OR SELECTING A TREATMENT FOR A SUBJECT RESISTANT TO TNF INHIBITOR USING A NLRP3 ANTAGONIST

Provided herein are methods of treating a subject that include administering a therapeutically effective amount of an NLPR3 antagonist or a pharmaceutically acceptable salt, solvate, or co-crystal thereof to a subject identified as having a cell that has an elevated level of NLRP3 inflammasome activity and/or expression as compared to a reference level. Provided herein are methods of treating a subject, methods of selecting a treatment for a subject, methods of selecting a subject for treatment, and methods of selecting a subject for participation in a clinical study that include the administration of a therapeutically effective amount of an NLRP3 antagonist. Also provided are methods of treating a subject having resistance to an anti-TNFα agent and methods of determining the efficacy of treatment with an anti-TNFα agent. Also provided are methods of treating a subject with a combination of an NLRP3 antagonist and an anti-TNFα agent.

LIPOSOMAL TROPONOID COMPOUND FORMULATIONS
20220339136 · 2022-10-27 ·

The present disclosure is concerned with liposomal formulations comprising troponoid compounds and methods of using same in the treatment of, for example, viral infections, antimicrobial infections, cancer, inflammatory diseases, and cardiovascular diseases. 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.

LIPOSOMAL TROPONOID COMPOUND FORMULATIONS
20220339136 · 2022-10-27 ·

The present disclosure is concerned with liposomal formulations comprising troponoid compounds and methods of using same in the treatment of, for example, viral infections, antimicrobial infections, cancer, inflammatory diseases, and cardiovascular diseases. 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.

INHIBITOR AGAINST EXPRESSION OF IMMUNE CHECKPOINT MOLECULE
20220340665 · 2022-10-27 · ·

The present invention provides a novel use of a compound having a plasminogen activator inhibitor-1 (PAI-1) inhibitory effect. Specifically, a compound having a PAI-1 inhibitory effect is used as an intranostimulator, an immune checkpoint inhibitor, an inhibitor for exacerbation of tumor cells caused by PD-L1, or an enhancer of immunotherapy for tumors, based on the inhibitory effect of the compound on expression induction of immune checkpoint molecules.