C07D277/62

Quinone-masked probes as labeling reagents for cell uptake measurements

Provided are labeling reagents and methods of using the reagents for cell uptake measurements. The labeling reagents can be quinone-masked probes including fluorophores and/or luminophores.

URAT1 INHIBITOR

Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R.sup.1a, R.sup.2a, R.sup.6a, and R.sup.7a represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, R.sup.3a and R.sup.8a form a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which R.sup.3a and R.sup.8a are bonded, R.sup.4a and R.sup.5a form a benzene ring together with two carbon atoms to which R.sup.4a and R.sup.5a are bonded or represent any of the groups represented by R.sup.1a described above, W.sup.a represents CR.sup.10a or N, and where, R.sup.10a represents any of the groups represented by R.sup.1a, X.sup.a represents an oxygen atom or a sulfur atom, Y.sup.a represents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Z.sup.a represents CO.sub.2H.)

##STR00001##

Flap modulators

The present invention relates to compounds of Formula (I), or a form thereof wherein ring A.sub.1, R.sub.1, R.sub.2, R.sub.3, R.sub.3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention. ##STR00001##

Flap modulators

The present invention relates to compounds of Formula (I), or a form thereof wherein ring A.sub.1, R.sub.1, R.sub.2, R.sub.3, R.sub.3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention. ##STR00001##

NOVEL SULFONYLAMINOBENZAMIDE COMPOUNDS AS ANTHELMINTICS
20170226053 · 2017-08-10 · ·

The present invention relates to a new compound of formula (I) wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endoparasites, in and on vertebrates.

##STR00001##

NOVEL MITOCHONDRIAL UNCOUPLERS FOR TREATMENT OF METABOLIC DISEASES AND CANCER

2-hydroxy-benzoic anilide compounds and derivatives, compositions thereof, and methods for treating metabolic diseases and cancer through uncoupling mitochondria.

Labeling composition for intraocular tissue, labeling method of intraocular tissue, and screening method

The invention provides a labeling composition for an intraocular tissue of a living individual, which specifically labels the intraocular tissue without need of an invasive operation such as exposure of an ocular tissue or injection of a staining agent into the ocular tissue or a nerve tissue linking to the ocular tissue, a method of noninvasively labeling an intraocular tissue of a living individual, and a screening method using the labeling composition for the intraocular tissues. The composition contains a compound capable of labeling at least a photoreceptor cell layer of a retina, wherein the compound is a staining compound having a particular structure as a partial structure thereof.

Antibacterial compounds

The present invention relates to the following compounds for use in the treatment of a bacterial infection ##STR00001##
wherein the integers are as defined in the description. The invention also relates to compounds for use as medicaments, pharmaceutical compositions and some novel compounds.

NADPH OXIDASE 4 INHIBITORS

The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I)

##STR00001##

wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.

NADPH OXIDASE 4 INHIBITORS

The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I)

##STR00001##

wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.