Abstract: The invention relates to functionalised dioxaborolane or dioxaborinane derivatives of formula (I), wherein R1 is covalently bonded to the boron atom by a carbon atom; one of R2, R3, R?3 or R4 is a radical of formula —X; or one of R1, R2, R3, R?3 or R4 is a radical of formula —X; and X is a functionalised radical. The invention relates to the method for preparing same and the uses thereof.

Abstract: Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.

Abstract: Provided are methods useful for preventing and mitigating radiation injury, including acute radiation syndrome, comprising administering to a subject a therapeutically effective amount of a compound represented by formula I or a pharmaceutically acceptable salt thereof, wherein Z is —O— or —N(H)—.

Abstract: Disclosed crystalline Siponimod fumaric acid, solid state forms (polymorphs) thereof, processes for preparation thereof and pharmaceutical compositions thereof.

Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

Abstract: One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N?-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 ?M) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 ?M), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 ?M (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.

Abstract: The present invention sets forth new compounds that potently block activation of ABA receptors. In some aspects, these compounds can be used to enhance germination of crop seeds to stand establishment and to increase transpiration and photosynthetic yields when water is not limiting plant growth.

Abstract: Provided herein are azo prodrugs of small-molecule isoindoline-1,3-diones and isoindoles anti-inflammatory inhibitors according to formula IA, in particular PDE4 inhibitors, which prodrugs can be administered orally to a subject in need thereof, whereby the prodrugs are cleaved in the colon and the PDE4 inhibitor released.

Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein A, Q, R1, R2, R3, R4, W and Y are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: The present invention provides a novel dosage principle for compounds of formula I and pharmaceutically acceptable derivatives thereof as defined in the claims, wherein said compound or pharmaceutically acceptable derivative thereof is intravenously administered to said patient over a period of at least about 8 hours, wherein the dose of the compound of formula I or pharmaceutically acceptable derivative thereof is at least the molar equivalent of about 45 mg/m2 of the dihydrochloride salt of the compound of formula I-B as defined in the claims.

Abstract: The compounds of the present invention are represented by the following compounds having Formula (I): where the substituents R, R1-R5, k, m, n, and q are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders, infectious disease, or for providing immunosuppression for transplanted organs or tissues.

Abstract: The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Abstract: Provided herein are unsymmetrical bis(azolium) salts, unsymmetrical CCC-NHC metal complexes, and methods of forming the same. The unsymmetrical bis(azolium) salts include a central aryl ring that is substituted with two heterocyclic rings in an ortho, meta, or para fashion. The unsymmetrical CCC-NHC metal complexes include metalated unsymmetrical bis(azolium) salts. The method of forming the unsymmetrical CCC-NHC metal complexes includes reacting a dihalogenated benzene with a first azole to form a mono(azole)benzene, reacting the mono(azole)benzene with a second azole to form an unsymmetrical bis(azole)benzene, alkylating the unsymmetrical bis(azole)benzene to form an unsymmetrical bis(azolium) salt, and metalating the unsymmetrical bis(azolium) salt to form the unsymmetrical CCC-NHC metal complex. Also provided are a bis-ligated CCC-NHC metal complex and an unsymmetrical bimetallic complex.

Abstract: The present invention generally relates to 6-amino-2,4-dihydropyrano [2,3-c] pyrazoles as a ubiquitin specific protease 7 (USP7) inhibitor useful for the treatment of diseases mediated by malfunction of USP7, such as inflammation, cancer, and immunological disorders. The invention described herein also pertains to pharmaceutical compositions and methods for treating diseases mediated by malfunction of USP7, in mammals using compounds disclosed herein.

Abstract: Provides herein are novel compounds, compositions, and methods useful for inhibiting bacteria, such as Mycobacterium tuberculosis. These compositions and methods find many uses in medicine and research, e.g., treating subjects afflicted with active or latent bacterial infections.

Abstract: Provided is a method for inhibiting the growth of Gram-positive bacteria, including contacting said bacteria with a first compound and a second compound, wherein the first compound is a compound of Formula I: and the second compound is an antibiotic other than a compound of Formula I. Also provided is a composition including the first compound and the second compound.

Abstract: A method of preparing bilirubin IX? from biliverdin IX? diester, the method including: 1) adding sodium hydroxide dissolved in a first methanol solution to biliverdin IX? diester dissolved in a second methanol solution, to yield a first mixture; adding water to the first mixture to hydrolyze biliverdin IX? diester; adding an acid to the first mixture to adjust the pH value thereof; removing a first solvent of the first mixture through rotary evaporation, and removing an inorganic salt through rinsing, and vacuum drying, to yield biliverdin IX?; and 2) dissolving the biliverdin IX? in an alcoholic solution, and adding a radical scavenger and borohydride to the alcoholic solution, to yield a second mixture; adding a ketone to the second mixture to decompose excess borohydride; adding the acid to the second mixture to adjust the pH value thereof; and removing a second solvent of the second mixture through rotary evaporation.

Abstract: Disclosed are crystalline salts of Compound I, methods of preparing them, and related pharmaceutical preparations thereof. Also disclosed are methods of treatment using the crystalline salts of the invention.