Abstract: The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates compounds useful as reagents for the diazomethylation reaction, their preparation and the use thereof as reagents in a method for the diazomethylation reaction of aromatic substrates. It relates in particular to a compound of formula (I) wherein E is an electron withdrawing group.

Abstract: Provided herein is a process for the preparation of 4-((6-bromopyridin-3-yl)oxy)benzonitrile.

Abstract: The present disclosure is directed to disclosed compounds that modulate e.g., address underlying defects in cellular processing of CFTR activity.

Abstract: The invention relates to a method for producing 5-hydroxymethylfurfural (HMF) in a continuous process, which leads to the obtainment of an HMF fraction, a carbohydrate/acid fraction, a fructose fraction, and a levulinic-acid and formic-acid fraction and advantageously makes it possible, because of the purity of the obtained fractions, to return the fructose fraction obtained by means of the method directly to the production process and to use the other fractions in further-processing processes without the need for complex, additional purification steps.

Abstract: The present invention relates to a urea compound and a preparation method and an application thereof. The structure of the present compound is represented by formula (I), the definition of each variable in the formula being as described in the description. The compound can block interaction between the PD-1/PD-L1 signalling pathways. The compound of the present invention can be used for treating or preventing diseases related to the signalling pathways, such as cancer, autoimmune disease, chronic infectious disease, and other diseases.

Abstract: Crystalline Forms of Compound I: and pharmaceutically acceptable salts thereof are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

Abstract: Disclosed are compounds of Formula 1, N-oxides of the compounds and salts of the compounds and N-oxides: wherein R1, R2, R3, R4, R5, R6, Q1, Q2, J, Y1, and Y2 are as defined in the disclosure. Also disclosed are compositions containing the compounds, N-oxides and salts, and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of such a compound, N-oxide, salt or composition.

Abstract: An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof. The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof. wherein the symbols in the formula are defined below: R1: e.g., a C1-C6 alkyl group; R2: a C1-C6 alkyl group; A: e.g., an oxygen atom; and R3: e.g., a C1-C6 alkyl group.

Abstract: A compound of general formula I: is disclosed. The compound be used to prevent or treat hepatitis B virus infection.

Abstract: An inhibitor of a wild type and Y641F mutant of human histone methyltransferase EZH2 is provided herein. Particularly, the inhibitor is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The inhibitor can be used to treat a cancer or precancerous condition related to EZH2 activity.

Abstract: Oligomeric compounds useful as organic conjugated materials in electronic devices. Oligomeric compounds contain three or more or four or more of certain PDI units bonded to an organic core. The organic core contains one, two or more thiophene rings. The organic core can contain two or more thiophene rings separated by a linker group; two or more thiophene rings directly fused to each other or indirectly fused to each other through an optionally substituted aromatic or non-aromatic carbocylic ring system or an optionally substituted aromatic heterocyclic or non-aromatic heterocyclic ring system; or each of two or more thiophene rings is fused to an aromatic or non-aromatic carbocylic ring system or an aromatic heterocyclic or non-aromatic heterocyclic ring system and the resulting fused rings containing a thiophene ring are each separated by a linker group M. Methods for making oligomeric compounds by direct heteroarylation are provided.

Abstract: The present invention provides salts of (E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide represented by the formula I and acids, and crystals thereof, possessing a potential to be used as drug substance in pharmaceuticals.

Abstract: The present invention provides a compound having a TrkA inhibitory activity or a pharmaceutically acceptable salt thereof. The present invention relates to a compound represented by Formula (I): wherein -L- is —C(?X)—, or the like, —Z— is —NR5—, or the like, —ZA— is —NR5A—, or the like, B is substituted or unsubstituted aromatic carbocyclyl, or the like, Y is a single bond, or the like, the ring C is a substituted or unsubstituted aromatic heterocycle, or the like, R2 is a hydrogen atom, or the like, and the group represented by is a group represented by Formula: or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.

Abstract: The compound according to the present embodiment is represented by the following formula (1): Q-L-CHR2??(1) (wherein, Q is a non-cationic aliphatic group that does not contain nitrogen but contains oxy; L is a single bond or an aliphatic group containing no nitrogen; Rs are C12-C24 aliphatic group, the same or different; and at least one R contains, in the main chain or side chain thereof, a linking group LR selected from the group consisting of —C(?O)—O—, —O—C(?O)—, —O—C(?O)—O—, —S—C(?O)—, —C(?O)—S—, —C(?O)—NH—, and —NH—C(?O)—).

Abstract: To provide novel pesticides, especially insecticides or acaricides. A condensed heterocyclic compound represented by the formula (1) or its salt, or N-oxide thereof: wherein Q is a structure represented by Q1, Q2 or the like, D substituted with —S(O)nR1 is a structure represented by D1 or D2, A1 is N(A1a) or the like, A1a is C1-C6 alkyl or the like, A4 is a nitrogen atom or C(R4), A5 is a nitrogen atom or C(R5), R1 is C1-C6 alkyl or the like, each of R2, R5 and R6 is independently a hydrogen atom or C1-C6 alkyl, each of R3, R4, Y1, Y2, Y3 and Y4 is independently a halogen atom, halo (C1-C6) alkyl or the like, and n is an integer of 0, 1 or 2.

Abstract: The present invention provides unified synthesis of the CI-CI 9 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hydridized carbon. The provided efficient selective coupling reactions can allow easy access to the CI-CI 9 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.

Abstract: The present invention relates to an improved process for the preparation of [(1S,2R)-3-[[(4-aminophenyl)sulfonyl] (2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-carbamic acid (3R,3aS,6aR)hexahydrofuro[2,3-b]furan-3-yl ester compound of formula-1 represented by the following structural formula:

Abstract: A problem to be solved by the present invention is to provide a novel preventive or therapeutic agent for pulmonary hypertension containing as an active ingredient a compound that has not been known for a therapeutic effect on pulmonary hypertension heretofore. The present invention provides a preventive or therapeutic agent for pulmonary hypertension containing an ingredient having a selenoprotein P activity-inhibiting action.

Abstract: This disclosure relates to polymersomes comprising a crosslinked polymer and their use as drug delivery vehicles. Specifically, polymersomes comprising a polymer of Formula I: wherein each R is independently C1-6 alkyl; and n is an integer between 1 and 50.