Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

Abstract: Provided is a degradation inhibitor that delays the progress of the degradation reaction of 2ccPA and has an excellent stabilization effect by using a carbacyclic phosphatidic acid compound represented by formula (1): wherein R1 represents hydrogen, alkali metal, alkyl, arylalkyl, or aryl; bonds indicated by solid and dotted lines represent single or double bonds; wavy lines represent single bonds; and when the single bond is adjacent to a double bond, the steric configuration is E-configuration, Z-configuration, or any mixture thereof.

Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

Abstract: A reversible photo-switchable isomerization of novel sterically hindered 2,2?,6,6?-tetraisopropyl-4,4?-diethynylazobenzene and its synthesis.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where X1; X2; R1 and R4 are as defined herein.

Abstract: Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

Abstract: A process for preparing, 1,1,3-trioxo-1,2-benzothiazole-6-carboxamide of formula (I) comprising: (a) oxidizing 2,5-dimethyl-benzenesulfonamide of formula (II) in the presence of an oxidizing agent to receive 2-sulfamoyl-terephthalic acid of formula (III); (b) converting the formed 2-sulfamoyl-terephthalic acid of formula (III) to receive 2-sulfonoyl-terephthalic acid derivative of formula (IV); and (c) reacting the resulting 2-sulfamoyl-terephthalic acid derivative of formula (IV) with ammonia (NH3) or ammonium containing-salt; wherein R represents OR? or CI and R? represents a branched or non-branched C1-C12 alkyl.

Abstract: An 6-(5-(3-fluorophenyl)-4-phenyl-4H-1,2,4-triazol-3-ylthio)hexanoic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

Abstract: An 4-(2,4,5-tris(4-chlorophenyl)-1H-imidazol-1-yl)benzoic acid compound, its synthesis, and its use as an antimicrobial agent.

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the following formula (I): wherein X1 represents a nitrogen atom or CR9, R1 represents a hydrogen atom, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a halogen atom, R3 represents a hydrogen atom or a halogen atom, R4 represents a hydrogen atom or a halogen atom, and R5 represents a C1-C3 alkylsulfonyl group, a substituted C1-C6 alkyl group, a substituted C1-C6 haloalkyl group, a substituted C1-C6 alkoxy group, or a substituted C1-C6 alkylamino group, or a pharmacologically acceptable salt thereof.

Abstract: Disclosed herein are cyclic thiol prodrugs, and pharmaceutical compositions thereof. The prodrugs and pharmaceutical compositions thereof may be used to treat or prevent medical disorders such as, for example, cystinuria, cystinosis, cancer, neurodegenerative disease, Parkinson's disease, Huntington's disease, malaria, nonalcoholic fatty liver disease, radiation poisoning, arsenic poisoning, radioprotection, Wilson's disease or rheumatoid arthritis.

Abstract: Provided is a compound represented by formula (1). In formula (1), Ar1, Ar2, and Ar3 represent a 1,4-phenylene group or a divalent sulfur-containing aromatic heterocyclic group optionally having a substituent, and at least one of Ar1 and Ar2 has a fluorine atom as a substituent; n represents 1 or 2; R1 represents a single bond or a group selected from the group consisting of —OC(?O)—, —C(?O)O—, —C?C—, —CH?CH—, —CH?N—, and —N?CH—; R2 represents an alkylamino group or an alkoxy group; R3 represents a group selected from the group consisting of an alkanediyl group, an alkanediyloxy group, an alkanediyloxycarbonyl group, and an alkanediylcarbonyloxy group; and R4 represents a polymerizable group or a hydrogen atom.

Abstract: Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

Abstract: The present invention discloses a phthalide derivative, the structure of said derivative is represented by Formula (I) or Formula (II). The present invention also discloses the preparation method and use of said derivative. The phthalide compound obtained through structure modifications in the present invention enhances the chemical stability and pharmacological activity of the phthalide compound, facilitating the improvement of the druggability of such compounds.

Abstract: A 7-(4-((5-(2-bromobenzylideneamino)-2-thioxo-1,3,4-thiadiazol-3(2H)-yl)methyl)piperazin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid compound, its synthesis, and its use as an anti-inflammation agent.

Abstract: A drug or agent containing a compound having an agonistic activity to STING as an active ingredient, where the compound is represented by the following general formula (I-1): wherein all symbols represent the same meanings as described in the specification, and the compound can be used as an active ingredient of an agent for suppressing the progression of, suppressing the recurrence of and/or treating cancer or infectious disease.

Abstract: A P2X3 and/or P2X2/3 receptor antagonist of formula (I), a pharmaceutical composition comprising the same, and a use thereof in preparing a drug for preventing or treating a disease mediated by the P2X3 and/or P2X2/3 receptor antagonist.

Abstract: The present disclosure describes novel compounds that are somatostatin receptor type 4 agonists.

Abstract: This disclosure relates to salt forms of compounds capable of activating PPAR? for use in drug substance and drug product development, and related compositions and methods.