Abstract: A new class of ligands derived from benzo[h]quinoline are described and these ligands are used to prepare several novel transition metal complexes. The complexes are preferably of the group VIII transition metals iron, ruthenium or osmium, with the benzo[h]quinolone ligands acting as tridentate ligands. The complexes described are proved to be very active catalysts for the reduction of ketones and aldehydes to alcohols, via hydrogen transfer and hydrogenation reactions. These compounds hence can be usefully employed as catalysts in said reduction reactions.

Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.

Abstract: The invention provides analgesic conjugates having a mu opioid receptor agonist linked to a mGluR5 antagonist, and to methods for producing analgesia using such compounds.

Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: Malonic ester derivatives of the formula (I) in which the symbols A1, A2, Y, R10, p, X, R2, G, Q, L2 and R1 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

Abstract: The invention provides simple small molecule, non-heme iron catalyst systems with broad substrate scope that can predictably enhance or overturn a substrate's inherent reactivity preference for sp3-hybridized C—H bond oxidation. The invention also provides methods for selective aliphatic C—H bond oxidation. Furthermore, a structure-based catalyst reactivity model is disclosed that quantitatively correlates the innate physical properties of the substrate to the site-selectivities observed as a function of the catalyst. The catalyst systems can be used in combination with oxidants such as hydrogen peroxide to effect highly selective oxidations of unactivated sp3 C—H bonds over a broad range of substrates.

Abstract: The invention relates to a method for producing a hydrazine of general formula (I) and the pharmaceutically acceptable salts thereof from an amine of formula (II), characterised in that said method uses a urea of formula (III) as a synthesis intermediate.

Abstract: A composition and method are disclosed for capturing CO2. A pollutant/greenhouse gas can be converted into a valuable organic compound using a nontoxic reducing agent. CO2 may be economically captured from the atmosphere, from products of combustion, or from byproducts of various chemical processes. The method reduces CO2 in a three-step reaction cycle, in which a binuclear metal-organic compound converts CO2 to oxalate in a redox cycle under mild conditions.

Abstract: The present invention relates to a process for the preparation of Compound (A): wherein the process comprises contacting atazanavir base (Compound (II)) with sulphuric acid in a combination of two or more solvents and isolating compound (A). The present invention also relates to substantially pure Compound (A), and to Compound (A) devoid of mesityl oxide impurity.

Abstract: Methods of producing a sulfilimine compound, such as N-cyano-S-methyl-S-[1-(6-trifluoromethyl-3-pyridinyl)ethyl]sulfilimine or other substituted sulfilimine compound. The method includes combining a sulfide compound, cyanamide, a hypochlorite compound, and a base, and oxidizing the sulfide compound to form the sulfilimine compound. The sulfide compound may include a 2-trifluoromethyl-5-(1-substituted)alkyl-thiopyridine compound. The base may include sodium hydroxide. A buffer, such as a phosphate buffer, may, optionally, be used in the reaction.

Abstract: Disclosed herein is a cost effective and environmentally friendly process to prepare 1-hydroxy-6-substituted pyridones from 2,6-dichloropyridine.

Abstract: The present invention provides a new forms of (R)-N-methylnaltrexone, and compositions thereof, useful as a peripheral mu opioid receptor antagonist.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

Abstract: The disclosure relates to Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein Ar1, Ar2, L1, L2, X, R3, R22, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I), and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I).

Abstract: The present invention provides a composition for controlling pests having an excellent control efficacy on pests. A composition for controlling pests comprising a compound represented by the formula (1): wherein each of symbols are the same as defined in the Description, or N-oxide thereof; and a compound represented by the formula (2): wherein each of symbols are the same as defined in the Description; shows an excellent controlling efficacy on pests.

Abstract: The present application describes a novel type of picolinamide-cinchona organocatalyst that allows for the successful transformation of ketimines to chiral amines with very high enantioselectivities and with the highest TOFs reported for any particular organocatalyst to date. These organocatalysts have also been immobilized to a variety of solid supports, including magneto-nanoparticles.

Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.

Abstract: Provided herein are processes and intermediate compounds useful for the preparation of 2-carboxamide cycloamino urea derivatives, and useful intermediates therefore.

Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, {[(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibittors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

Abstract: Provided is a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder and the like. The present invention relates to a compound represented by the formula wherein ring A is a 4- to 7-membered ring optionally having substituent(s); L is —O—, —S—, —SO— or —SO2—; R1 is a C1-6 alkyl group optionally having substituent(s) (provided that when L is —O—, R1 is not a C1-6 alkyl group optionally substituted by halogen atom(s)), or a cyclic group optionally having substituent(s); X1 is —CRa? or —N?; X2 is —CRb? or —N?; X3 is —CRc= or —N?; Ra, Rb and Rc are each a C1-6 alkyl group, C2-6 alkenyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, C3-6 cycloalkoxy group or C6-14 aryl group, each of which optionally having substituent(s), H or halogen, or a salt thereof.