The invention relates to compounds of Formula (I)

##STR00001##

wherein X.sup.1, X.sup.2, X.sup.3, Y, R.sup.1, R.sup.2A, R.sup.2B, R.sup.3, and R.sup.4 are as described in the description; to their preparation, to pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing one or more compounds of Formula (I), and to the use of such compounds as medicaments, especially as Kv7 openers.

Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants.

Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants.

The present invention relates to the compound of formula (I), and a stereoisomer, a tautomer, a stable isotopic variation, a pharmaceutically acceptable salt or a solvate thereof, a pharmaceutical composition containing the compound, a method for using the compound for treating or preventing an RORγ-related disease, and use of the compound in the preparation of a drug for treating or preventing the RORγ-related disease.

##STR00001##

The present invention relates to the compound of formula (I), and a stereoisomer, a tautomer, a stable isotopic variation, a pharmaceutically acceptable salt or a solvate thereof, a pharmaceutical composition containing the compound, a method for using the compound for treating or preventing an RORγ-related disease, and use of the compound in the preparation of a drug for treating or preventing the RORγ-related disease.

##STR00001##

The present invention relates in certain aspects to the discovery of novel 2-naphthimidamide compounds that are capable of binding Type II Transmembrane Serine Proteases (TTSPs). In certain embodiments, the compounds of the invention can be used to treat or prevent Influenza A viral infection in a mammal.

The present invention relates to a novel and improved process for preparing butyl (5S)-5-({2-[4-(butoxycarbonyl)phenyl]ethyl}[2-(2-{[3-chloro-4′-(trifluoromethyl)[biphenyl]-4-yl]methoxy}phenyl)ethyl]amino)-5,6,7,8-tetrahydroquinoline-2-carboxylate of the formula (XII)

##STR00001##

to novel precursors for preparation thereof, and to use for preparation of (5S)-5-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)[biphenyl]-4-yl]methoxy}phenyl)ethyl]amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid.

A process of making Roxadustat of the following formula:

##STR00001##

comprising converting a compound of formula VI:

##STR00002##

to Roxadustat, wherein R is a C.sub.1-C.sub.20 alkyl group, and PG is a protective group.

A process of making Roxadustat of the following formula:

##STR00001##

comprising converting a compound of formula VI:

##STR00002##

to Roxadustat, wherein R is a C.sub.1-C.sub.20 alkyl group, and PG is a protective group.

The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR.sub.11R.sub.11′, OH, SO.sub.2-alkyl, CO.sub.2-alkyl, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR.sub.11R.sub.11′, OH, alkyl, haloalkyl, and aralkyl; Y and Z are each independently CR10R.sub.10′, wherein R.sub.10 and R.sub.10′ are each independently selected from H, F, alkyl, and haloalkyl; R.sub.1, R.sub.4, and R.sub.5 are each independently selected from H, F, Cl, Br, I and haloalkyl; R.sub.2 and R.sub.3 are each independently selected from H, F, Cl, Br, I, CN, and haloalkyl; wherein at least two of R.sub.2, R.sub.3 and R.sub.4 are other than H; and R.sub.11 and R.sub.11′ are each independently selected from H, alkyl, haloalkyl, COR.sub.12, and SO.sub.2R.sub.13, wherein R.sub.12 and R.sub.13 are both alkyl; wherein the compound is other than: N-(3,4-Dichlorophenyl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxamide; N-(3,4-Dichlorophenyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxamide; N-(4-Chloro-3-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-dichlorophenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-Dichlorophenyl)-6,7-dihydroisoxazolo[4,5-c]pyridine-5(4H)-carboxamide; and N-(3,4-Dichlorophenyl)-4-methyl-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-carboxamide. Further aspects of the invention relate to such compounds for use in the field of immunooncology, immunology, and related applications.

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