Abstract: Provided are a phenanthroimidazole derivative, and a preparation method therefor, and an application thereof. The phenanthroimidazole derivative has a structural formula as shown in Formula (I), R being an electron donor group, wherein by taking a phenanthroimidazole group containing a trifluoromethyl phenyl group as an electron acceptor, and in virtue of the properties of the specific electron donor group R, the phenanthroimidazole derivative containing a light-absorbing photosensitive group of a series D-?-A structure is synthesized, and can be used as a photoinitiator, which is used in the technical field of UV light-curing systems or 3D printing.

Abstract: A structural analog of Cyclotheonellazole A, and a synthetic method therefor and an application method thereof are provided. A compound with a structure of formula (I) and a pharmaceutically acceptable salt thereof are provided. The formula (I) is as follows: R1, R2, R3 and R4 are independently selected form the group consisting of H, a C1-C6 alkyl group, a C1-C6 alkoxy group, a halogen group, a hydroxyl group, an amino group, a nitro group, a cyano group, and a sulfydryl group. Based on the total synthetic route of Cyclotheonellazole A, the classical reverse synthesis analysis is utilized, the structural modification is purposefully carried out, a mother nucleus of the natural product remains unchanged, and the structural analog 1a is obtained by replacing a left side chain with a simple formylamine, thereby confirming the excellent protease inhibitory activity thereof, and having a strong application prospect in the pharmaceutical industry.

Abstract: A ketoamide compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically, the ketoamide compound shown in formula (A), a racemate, an enantiomer, or a diastereoisomer thereof, or any mixture of same, or a pharmaceutically active metabolite thereof, or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The ketoamide compound can effectively inhibit coronavirus or Ebola virus, and thereby implement the prevention or treatment of diseases related to coronavirus or diseases related to Ebola virus.

Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including autoimmune diseases, inflammatory diseases, chronic inflammatory diseases, diabetes, and infectious diseases, such as lupus, Sjögren's syndrome, rheumatoid arthritis, type 1 diabetes, inflammatory bowel disease, viral diseases, and nonalcoholic steatohepatitis. The compounds can also be used to generate cells, such as immune cells, for treating the conditions.

Abstract: Compositions and methods for the treatment of tuberculosis, as well as other mycobacterial and gram positive bacterial infections are disclosed. These compositions contain a highly potent and selective oxazolidinone encapsulated with high efficiency to maximize dosing potential of low toxicity drugs, and are stable in the presence of plasma. The compositions are long circulating and retain their encapsulated drug while in the circulation following intravenous dosing to allow for efficient accumulation at the site of the bacterial or mycobacterial infection. The high doses that can be achieved when combined with the long circulating properties and highly stable retention of the drug allow for a reduced frequency of administration when compared to daily or twice daily administrations of other drugs typically utilized to treat these infections.

Abstract: The present invention relates to a compound of the Formula: and pharmaceutically salts thereof. The compound of the present invention inhibits Pol?. This novel therapeutic compound is therefore useful for the treatment and/or prevention of diseases and conditions in which Pol? activity is implicated, such as, for example but not limited to, the treatment and/or prevention of cancer. The present invention also relates to pharmaceutical compositions comprising the novel therapeutic compound defined herein, to processes for synthesising the compound and to their use for the treatment of diseases and/or conditions in which Pol? activity is implicated.

Abstract: Described herein are MK2 inhibitors 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: 6,7-Dihydrothiazolo[5,4-c]pyridines substituted in the 5-position with heterocyclic rings are positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted benzothiazole compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.

Abstract: Provided herein are compounds, compositions including them, and methods of modulating GPR120 activity and treating diseases mediated by GPR120 by administering such compounds and compositions.

Abstract: Compositions and methods for the treatment of tuberculosis, as well as other mycobacterial and gram positive bacterial infections are disclosed. These compositions contain a highly potent and selective oxazolidinone encapsulated with high efficiency to maximize dosing potential of low toxicity drugs, and are stable in the presence of plasma. The compositions are long circulating and retain their encapsulated drug while in the circulation following intravenous dosing to allow for efficient accumulation at the site of the bacterial or mycobacterial infection. The high doses that can be achieved when combined with the long circulating properties and highly stable retention of the drug allow for a reduced frequency of administration when compared to daily or twice daily administrations of other drugs typically utilized to treat these infections.

Abstract: Disclosed herein are WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds including a WDR5 ligand, a degradation/disruption tag, and a linker, and methods of using such compounds in the treatment of WDR5-mediated diseases.

Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

Abstract: This disclosure is drawn to pyridine derivatives, compositions thereof, and associated methods, useful for inhibition of SARM1 activity and/or for treating or preventing neurological disorders.

Abstract: Compounds of formula (I), or the pharmaceutically acceptable salts and/or the solvates thereof, wherein m, n, R1, R2, R3, R4, R5, L, Ar1 and Ar2 are as defined as disclosed, which are useful as inhibitors of METTL3 (N6-adenosine-methlytransferase subunit) activity, in particular for the treatment of proliferative diseases such as cancers.

Abstract: The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

Abstract: Described herein are KAT6A inhibitors of Formula (Ia) and pharmaceutical compositions comprising said inhibitors.

Abstract: The present disclosure relates to calixpyrrole compounds and compositions thereof. The calixpyrrole compounds are chemical groups which are located in such a manner so as to be useful for the selective extraction of specific salts. Also provided herein are compositions and methods of use thereof.

Abstract: Disclosed herein are compounds and methods of treating diseases and/or conditions associated with FGFR inhibition.

Abstract: The present invention relates to a heterocyclic amide inhibiting RIP1 kinase and the use thereof, and specifically, to a compound of formula I, its pharmaceutically acceptable salts, stereoisomers, enantiomers, diastereomers, atropisomers, optical isomers, racemates, polymorphs, solvates or isotopically labeled compounds, a pharmaceutical composition comprising the compound, and the pharmaceutical use thereof. The compound is particularly effective for treatment of diseases or disorders mediated by RIP1 kinase.