Abstract: The present invention relates to bi-functional compounds which function to recruit endogenous proteins to an E3 ubiquitin ligase for degradation, and methods for using same. More specifically, the present disclosure provides specific proteolysis targeting chimera (PROTAC) molecules which find utility as modulators of targeted ubiquitination of a variety of polypeptides and other proteins, in particular the androgen receptor of a slice variant of AR which lacks the LBD, labelled as AR-V7, which are then degraded and/or otherwise inhibited by the compounds as described herein.

Abstract: The present invention relates to a compound of formula (I) or a tautomer thereof, wherein R1, R2, R3, R4 and R5, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of epilepsy and/or neurodegenerative diseases.

Abstract: A method of treating and/or preventing disease wherein retinal pigment epithelium, including administering compound of formula (I) or pharmaceutically acceptable salt, racemic mixture, corresponding enantiomer or, if applicable, corresponding diastereomer, wherein: X is either NH or O, R11, R12 and R13 are independently selected from consisting hydrogen group, fluoro, chloro, trifluoromethyl, methyl and difluoromethoxy, A is selected from consisting residue group of formula (II)-(VII) or (VIII) “*” denotes point of attachment to molecule remainder, and R2, R3, R4, R5, R2I, R3I, R4I, R5I, R2II, R3II, R4II, R5II, R2III, R3III, R4III, R5III, R2IV, R3IV, R4IV, R5IV, R2V, R3V, R4V, R5V, R2VI, R3VI, R4VI and R5VI are independently selected from hydrogen consisting group, linear or branched alkyl having 1-3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, trifluoromethyl, 2,2,2-trifluoroethyl and difluoromethoxy and R6 is selected from hydrogen consisting group, linear or branched alkyl having

Abstract: An empirical Screen for Anti-infectives using Fluorescence microscopy of IntracellulaR Enterobacteriaceae (SAFIRE) was developed. Using this methodology, a library of small molecules and identified antimicrobials that are cell permeable and non-host-toxic were screened. Inhibitors of bacterial efflux pumps were identified as being implicated in antibiotic resistance and are attractive therapeutic targets for antimicrobials.

Abstract: Prodigiosin analogs which reactivate the p53 pathway are provided, as well as compositions of these compounds, and methods for reactivation of the p53 pathway using these compounds are provided. The prodigiosin analogs may be used to treat cancer in which p53 mutation plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others.

Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.

Abstract: The present disclosure relates to a novel tetrazole azasydnone, a method of making the novel tetrazole azasydnone, and a method of using the novel tetrazole azasydnone as a primary explosive. In one aspect, the novel tetrazole azasydnone has a structure of formula I: wherein A? represents a cation with a 1+ charge.

Abstract: A method of fixating CO2 to form a substituted oxazolidinone is described. The method includes mixing a nickel-based metal-organic framework (Ni-MOF) catalyst of formula [Ni3(BTC)2(H2O)3]·(DMF)3(H2O)3, a cocatalyst, an aromatic amine, and at least one epoxide to form a reaction mixture, and further contacting the reaction mixture with a gas stream containing carbon dioxide to react the carbon dioxide in the gas stream with the epoxide and the aromatic amine to form a substituted oxazolidinone mixture. The method further includes adding a polar protic solvent to the substituted oxazolidinone mixture, centrifuging, and filtering to produce a recovered Ni-MOF; and further washing the recovered Ni-MOF with an organochloride solvent and drying for at least 5 hours to produce a recycled Ni-MOF.

Abstract: The present invention is a method of treating or preventing Mycobacterium tuberculosis infection in a subject by administering to the subject an effective amount of oxazolidinone, specifically (N—(((S)-3-(dibenzo[b,e][1,4]dioxin-7-yl)-2-oxooxazolidin-5-yl)methyl)acetamide) or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof.

Abstract: Aldoketo reductase (AKR) inhibitors having formulas I-III are used to treat disorders associated with NO/SNO deficiency.

Abstract: The present invention relates to a brivaracetam intermediate, a preparation method therefor, and a preparation method for brivaracetam. The steps of the method for preparing brivaracetam described in the present invention are short and the raw materials are cheap, moreover, the method is simple and highly effective without requiring isomer separation by means of column chromatography or asymmetric synthesis, being suitable for industrial large-scale production. In addition, disclosed by the present invention is a compound as shown in formula (II), which may be used for the synthesis of brivaracetam.

Abstract: A method of inhibiting a rise in intraneuronal calcium concentration includes administering an effective amount of a cyclic amine derivative represented by formula (I) or a pharmacologically acceptable salt thereof to a subject in need thereof: wherein A represents formula (IIa), (IIb) or (IIc):

Abstract: Provided herein are protein translation inhibitors and pharmaceutical compositions thereof that bind to an RNA Recognition motif in heterogeneous ribonucleoprotein A18 to inhibit binding to mRNA transcripts thereby inhibiting protein synthesis. Also provided is a method for treating a cancer by administering a pharmaceutically acceptable amounts of at least one of the protein translation inhibitors.

Abstract: The present invention is related to the development of therapeutics and prophylactics for the treatment and/or prevention of bacterial infections in humans and other mammals. A new class of small molecules is disclosed that inhibits the bacterial trans-translation/ribosome rescue mechanism and thus blocks infection of host cells by bacteria. Also disclosed are methods of using the small molecule inhibitors in the treatment/prevention of bacterial infections.

Abstract: The present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as T-cell immunoglobulin and mucin-domain containing-3 (TIM-3) inhibitors or as dual inhibitors of TIM-3 and the programmed cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal induced by TIM-3, PD-1, PD-L1, and/or PD-L2.

Abstract: Disclosed are a cannabinoid composition and an application of the same in preparing a medicine for treating neurodegenerative diseases, so as to solve the drawbacks of conventional medicines such as serious side effects and degraded therapeutic effect after long-term administration. The cannabinoid composition includes: cannabidiol and cannabigerol, a mass ratio of the cannabidiol to the cannabigerol ranging from 1:1 to 1:10, or from 1:0.3 to 1:0.5, or from 1:0.5 to 1:0.7, or from 1:07 to 1:1.

Abstract: An object is to provide a compound having ?-lactamase inhibitory activity. The object is achieved by a compound represented by formula (1), typified by a compound in which specific positions of a 5-membered ring having planarity are replaced by sulfamoyl and carboxy groups.

Abstract: Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, such as oxazole compounds, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.

Abstract: Provided herein are methods of treating or preventing a viral infection in a subject comprising administering a compound of Formula I, Formula Ia, or Formula Ib, or a pharmaceutically acceptable salt thereof, wherein the subject is not being treated with chloroquine, or an analog or salt thereof.

Abstract: This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.