Abstract: The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging; wherein the inhibitors of NLRP3 inflammasomes are compounds of Formula VII: or a Pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to picolinic acid derivatives that are useful in treating fungal diseases, particularly in plants.

Abstract: The present disclosure relates to a compound having an AhR inhibitory effect as shown in FIG. (I), and a use thereof and a preparation method thereof.

Abstract: Acquired hearing loss due to chemotherapy or noise exposure is a major health problem, and Cisplatin chemotherapy often causes permanent hearing loss in cancer patients. However, there are no FDA-approved drugs for the treatment or prevention of Cisplatin- or noise-induced hearing loss. In one aspect, use of Niclosamide, Ingenol, and Elesclomol as an active agent to treat a hearing impairment and 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.

Abstract: Disclosed are bifunctional compounds (degraders) that target FAK or FAK and ALK for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat disease.

Abstract: Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

Abstract: The present disclosures provides surprising insight into new technologies for treatment and/or prevention of certain types of hair loss (also known as alopecia), including androgenetic alopecia, alopecia areata, frontal fibrosing alopecia, and senescent alopecia. Among other things, the present disclosure provides surprising insight that plasminogen activator inhibitor-1 (PAI-1) inhibitors may be surprisingly effective and/or useful in the treatment and/or prevention of certain types of hair loss, including androgenetic alopecia, alopecia areata, frontal fibrosing alopecia, and senescent alopecia. Furthermore, the present disclosure provides insight that provided new technologies may not be particularly effective and/or useful in the treatment and/or prevention of other types of alopecia such as radiation-induced alopecia, chemotherapy-induced alopecia, and alopecia due to chronic discoid lupus erythematosus.

Abstract: Provided herein are compounds, crystalline free forms, crystalline salt forms, and pharmaceutical compositions of Compound 1. Also provided are methods of preparing and methods of using the same, e.g., for inhibiting a kinase and/or for treating various diseases or disorders, such as autoimmune diseases.

Abstract: The present disclosure provides a compound comprising a modified tetracycline derivative, covalently coupled through a linker to a low-hydrophobicity bioactive molecule useful for treating neurodegenerative diseases, wherein the modified tetracycline derivative is optionally defined by the following formula:

Abstract: Provided herein are substituted indole compounds. In certain embodiments, the compounds are inhibitors of the alternative pathway of the complement system, and in particular, inhibitors of complement factor B (CFB). Also provided are compositions comprising the compounds and methods of use thereof. The compounds provided are useful in the treatment, prevention or amelioration of a disease, condition or disorder through inhibition of the complement alternative pathway.

Abstract: The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer, wherein the compounds have the formula:

Abstract: Provided herein are amorphous and crystalline hemisulfate salt forms of the formula. Also provided are pharmaceutical compositions comprising the amorphous and crystalline hemisulfate salt forms, methods for their manufacture, and uses thereof for treating conditions associated with pyruvate kinase such as e.g., pyruvate kinase deficiency.

Abstract: Disclosed herein is a compound of Formula (I) for inhibiting TYK2 and treating disease associated with undesirable tyk-2 activity (tyk-2 related diseases), a method of using the compounds disclosed herein for treating inflammatory or autoimmune disease, and a pharmaceutical composition comprising the same.

Abstract: The invention relates to a combination comprising a carotenoid, a carotenoid metabolite, a carotenoid derivative, analogue or an ester or salt thereof and a second component selected from the group consisting of an inhibitor of one or more members of the BCL-2 anti-apoptotic protein family, an activator of pro-apoptotic BCL-2 family members, a senolytic agent and a senomorphic agent. The invention also relates to a food, a cosmeceutical, a nutraceutical, a cosmetic or pharmaceutical composition comprising the combination of the invention and its use in a cosmetic method and it medical uses.

Abstract: An iridium complex which has a phenylpyridine bidentate ligand containing a group represented by the following general formula (A): (In the general formula (A), X represents a cyano group or a halogenated alkyl group. L represents a single bond or a divalent linking group. R represents a substituent. n represents an integer of 0 to 4. * represents a binding site to a phenylpyridine bidentate ligand.

Abstract: Pharmaceutical compositions of the invention comprise functionalized lactam derivatives of formula (I) having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity, wherein A is selected from a group consisting of:

Abstract: The invention relates to novel heteroaryl compounds of Formula (I), and pharmaceutically acceptable salts thereof; and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cardiovascular diseases, and methods treating sepsis or septic shock, using the novel heterocyclic compounds disclosed herein.

Abstract: Described herein are MK2 inhibitors of Formula (II) and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of autoimmune disorders, chronic inflammatory disorders, acute inflammatory disorders, auto-inflammatory disorders, fibrotic disorders, metabolic disorders, neoplastic disorders, and cardiovascular or cerebrovascular disorders.

Abstract: Disclosed is crystalline Form A of 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl) amino)-N-(methyl-d3)pyridazine-3-carboxamide. Form A is a neat crystalline form. Characterization data for Form A are disclosed.

Abstract: An isoindoline derivative of formula wherein X is N, C—CN or C—COR2; Y is a radical having an acidic group or a basic group; R1 is independently from one another halogen or C1-C4-alkyl, said alkyl is unsubstituted or substituted with halogen; R2 is C1-C4-alkyl, said alkyl is unsubstituted or substituted with halogen; and n is 0, 1, 2, 3 or 4, with the proviso that Y does not include an acidic group if X is C—CN or C—COR2, and compositions containing the same are provided. The isoindoline derivative and the pigment composition are suitable, for example, for coloring high molecular mass organic material, especially paints, printing inks, resist formulations for color filter applications, electrophotographic toners, cosmetics, plastics, films or fibers.