The present disclosure relates to substituted thiophene carboxamides derivatives of formula (I) and (II), their use for controlling phytopathogenic microorganisms and compositions comprising thereof.

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This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

The present invention provides a thiophene carboxamide compound of the following General Formula (I), which is a novel fluorine-substituted biphenyl carboxamide-based compound, and provides a useful compound, as an agricultural and horticultural plant disease control agent, exhibiting an excellent control effect at a low dose. ##STR00001## wherein, R, R1, R2, R3, Xm, and Y are each as defined in the specification.

The present invention provides a thiophene carboxamide compound of the following General Formula (I), which is a novel fluorine-substituted biphenyl carboxamide-based compound, and provides a useful compound, as an agricultural and horticultural plant disease control agent, exhibiting an excellent control effect at a low dose. ##STR00001## wherein, R, R1, R2, R3, Xm, and Y are each as defined in the specification.

A use of a diarylamide compound having the structure as shown in formula (I) or a pharmaceutically acceptable salt thereof in preparing a drug which acts as a urea transporter protein inhibitor, and a novel diarylamide compound. The diarylamide compound has urea transporter protein inhibitor effect, and can produce urea selective diuresis in the body without obvious toxicity.

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A use of a diarylamide compound having the structure as shown in formula (I) or a pharmaceutically acceptable salt thereof in preparing a drug which acts as a urea transporter protein inhibitor, and a novel diarylamide compound. The diarylamide compound has urea transporter protein inhibitor effect, and can produce urea selective diuresis in the body without obvious toxicity.

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The invention provides 2-(substituted phenylhetero) aromatic formate FTO inhibitors, a preparation method thereof, and applications thereof. Specifically, disclosed in the present invention are a 2-(substituted phenylhetero) aromatic formate compound represented by the following formula (I), and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, which can be used as an FTO targeting inhibitor for treating diseases associated with FTO targets, including obesity, metabolic syndrome (MS), type 2 diabetes (T2D), Alzheimer's diseases, and cancers such as breast cancers, small-cell lung cancers, human bone marrow rhabdomyosarcoma, pancreatic cancer, malignant glioblastoma and the like. ##STR00001##

The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

Provided herein are compounds of Formula (I), Formula (II), and Formula (III), and compositions comprising the same, as well as methods of use thereof for controlling or inhibiting the formation of calcium oxalate kidney stones, inhibiting the production of glyoxylate and/or oxalate, and/or inhibiting hydroxyproline dehydrogenase (HYPDH).

Provided herein are compounds of Formula (I), Formula (II), and Formula (III), and compositions comprising the same, as well as methods of use thereof for controlling or inhibiting the formation of calcium oxalate kidney stones, inhibiting the production of glyoxylate and/or oxalate, and/or inhibiting hydroxyproline dehydrogenase (HYPDH).