Abstract: Disclosed herein, inter alia, are compounds and methods of use thereof for the modulation of certain chemokine receptor activity.

Abstract: Provided herein are novel ligands and pharmaceutical compositions thereof which modulate IL-17A. Also provided are methods for preparing the IL-17A modulators. Such compounds may be useful in the treatment and/or prevention of, for example, inflammation, cancer or autoimmune disease.

Abstract: The present invention provides compounds inhibiting eIF4E activity, and compositions and methods of using thereof.

Abstract: Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides prodrugs of compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both, according to formula (I) as described herein. Formula I compounds are useful in the treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. The invention also provides pharmaceutical compositions of Formula I compounds.

Abstract: Lysyl oxidase (LOX) inhibitors, lysyl oxidase-like (LOXL) inhibitors, or pharmaceutically acceptable salts thereof and methods for the treatment of myeloid malignancies, comprising administering a therapeutically effective amount of those inhibitors alone or optionally in combination with a second therapeutic agent.

Abstract: Co-crystals of itanapraced; methods of preparation of the co-crystals; uses of the co-crystals as APIs; formulations containing the co-crystals; uses of the co-crystals and formulations for prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries; and methods of prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries are described.

Abstract: This invention relates to the use of agomelatine (or a prodrug or salt thereof) in the treatment of major depressive disorder or bipolar disorder, including the selection of patients who would most benefit from agomelatine.

Abstract: The present invention provides a compound represented by a following formula. A compound represented by, wherein R1 is hydrogen, hydroxy, or the like; R2a and R2b may be taken together with an adjacent carbon atom to form ring B, ring B is a substituted or unsubstituted non-aromatic carbocycle or a substituted or unsubstituted non-aromatic heterocycle; R3a is hydrogen, halogen, hydroxy, or the like; R3b is hydrogen, halogen, hydroxy, or the like; R4a is a group represented by formula: L3 is a single bond or substituted or unsubstituted alkylene, R7 is hydrogen, halogen, hydroxy, or the like, and R4b is halogen, cyano, carboxy, or the like, or its pharmaceutically acceptable salt.

Abstract: Provided herein are compounds, compositions, and methods useful for reducing, preventing, and/or inhibiting germination of C. difficile spores, including methods for inhibiting C. difficile germination to prevent or treating C. difficile-associated diseases and disorders such as, for example, severe diarrhea and colitis in a subject. 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.

Abstract: The instant invention provides for inositol derivatives, analogs, methods of preparation and uses that inhibit oncogenic signaling pathways and genes. In particular, the compounds disclosed selectively inhibit one or two classes and or isoforms of PI3K. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting KRAS by administering the compound to a patient in need of treatment of cancer.

Abstract: The present invention relates to stable pharmaceutical compositions comprising apixaban or its pharmaceutically acceptable salts thereof. The present invention further relates to a capsule composition comprising a therapeutically effective amount of apixaban solubilized or dispersed in a pharmaceutically acceptable carrier, wherein the therapeutically effective amount of apixaban ranges from about 0.5 mg/unit dosage form to about 50 mg/unit dosage form. The present invention also provides manufacturing processes thereof and use of the said compositions for prevention, treatment or prophylaxis of disorders in human patients in need thereof.

Abstract: This patent document reveals a class of pleiotropic pathway modifier (known as PPM) compounds that facilitate the degradation of multiple targeted proteins and regulate various signaling events involved in cancer cell survival and proliferation, as well as immune response. These compounds effectively recruit disease-causing proteins for swift destruction through the ubiquitin-proteasome pathway, exhibiting potent anti-cancer, immunomodulatory, and anti-inflammatory properties. Additionally, disclosed herein are methods for treating diseases encompassing cancers, autoimmune disorders, infections, inflammations, and other ailments.

Abstract: The current methods and compositions provide for a novel therapeutic method for treating patients diagnosed with melanoma, especially those that have become resistant to certain other therapies. Accordingly, certain aspects of the disclosure relate to a method for treating melanoma in a subject, the method comprising administering a composition comprising a ferroptosis-inducing agent or other dedifferentiated melanoma-targeting agent to the subject.

Abstract: Disclosed are substituted aminoquinoline and aminopyridine compounds and their use as bacterial nitric oxide synthase (bNOS) inhibitors. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject having or at risk for developing a disease or disorder that is associated with bNOS activity.

Abstract: The present disclosure provides polymorphs of 3-(2,3,5,6-tetrafluoro-3?-trifluoromethoxy-biphenyl-4-ylcarbamoyl)-thiophene-2-carboxylic acid, and methods of making such polymorphs. The present disclosure further provides pharmaceutical compositions and kits comprising polymorphs of the invention, and methods of treating, preventing, or ameliorating a disease or condition comprising administering a polymorph of the invention.

Abstract: Compounds, pharmaceutical compositions, and methods for treating tinnitus in a subject in need thereof. The methods include administering a therapeutically effective amount of a compound having a structure represented by Formula I as described herein. The compounds and compositions are administered transdermally or orally, preferably via a sustained release mechanism. The compounds and compositions reduce at least one behavioral correlate of tinnitus and/or at least one neurophysiological correlate of tinnitus. The compounds and compositions reduce hyperactivity in the auditory system.

Abstract: The present invention relates to a process for the preparation of a chiral prostaglandin enol intermediate of formula 1, comprising the steps of: separating a compound of formula 16-(R,S)-10 into its diastereomers by fractional crystallisation, reducing the 15-oxo group of the compound of formula 16-(R)-10, thereby obtaining a compound of formula 15-(R,S), 16-(R)-11, followed by removing the protecting group of the compound of formula 15-(R,S), 16-(R)-11, and isolating the compound of formula 1, and optionally, crystallizing the compound of formula 1. Optionally, the undesired isomer formed during fractional crystallization can be epimerized and further amount of the desired isomer can be recovered from the resulting mixture. The present invention also provides novel intermediates useful in the process. The invention further relates to a process for fractional crystallization of the compound of formula 16-(R,S)-10.

Abstract: The present invention relates to chemical compounds which can be used in particular as structural mimetics of proline-rich peptides. The compounds of the present invention are capable of selectively inhibiting Ena/VASP-EVH1-mediated protein-protein interactions. The invention further relates to the use of these compounds as pharmaceutical agents and the use of the pharmaceutical agents for the treatment of tumor diseases.

Abstract: The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (ROR?) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of ROR?-mediated diseases or disorders.

Abstract: The present disclosure discloses a micromolecular compound specifically degrading tau protein, and an application thereof. The chemical structure of the micromolecular compound specifically degrading tau protein is TBM-L-ULM or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph or N-oxide thereof, TBM being a tau protein-binding moiety, L being a linking group, and ULM being a ubiquitin ligase-binding moiety, the tau protein-binding moiety and the ubiquitin ligase-binding moiety being connected by means of the linking group. The micromolecular compound specifically degrading tau protein may increase tau protein degradation in a cell, thereby decreasing tau protein content.