119 results about "Carboxamide" patented technology

The application relates to the field of agricultural disease control technology, and particularly relates to the use of indole compounds and pharmaceutically acceptable salts, solvates, crystal forms, prodrugs, stereoisomers and tautomers thereof for preparing a medicine for inhibiting pathogenic key protein kinase CgSlt2 of pathogenic fungi. The application first proposes a new type of CgSlt2-targeted inhibitor, specifically, indole compounds ((S)-N-(1-(1H-indol-3-yl)-4-(methylamino)-4-oxobutan-2-yl)-8-bromo-1,6-naphthyridine-2-carboxamide) and ((S)-N-(2-((1H-indol-3-yl)-1-(methylamino)-1-oxopropyl)-8-bromo-1,6-naphthyridine-2-carboxamide) are used as CgSlt2 inhibitors, have the characteristics of high target specificity and high activity, and exhibit excellent pathogenicity inhibition of a strain of the complex group of Colletotrichum gloeosporioides.

The technology herein provides various embodiments that relate to a method of treating pulmonary hypertension in a subject in need thereof, comprising administering to the subject an effective amount of BX-912 (N-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]-2-pyrimidinyl]amino]phenyl]pyrrolidine-1-carboxamide).

The present disclosure relates to nanoemulsions of 5-amino-[4-(4-chlorobenzoyl)-3,5-dichlorobenzyl]-1,2,3-triazole-4-carboxamide (carboxy-amido-triazole or CAI), methods of preparing thereof, and their use in the treatment of inflammatory optic neuropathies.

The present disclosure relates to 1-(2-(4-cyclopropyl-1H-1,2,3-triazol-1-yl)acetyl)-4- hydroxypyrrolidine-2-carboxamide derivatives and structurally related compounds of formula (I) as VHL inhibitors for the treatment of e.g. anemia (e.g. chronic anemia or anemia associated with chronic kidney disease, dialysis or cancer chemotherapy), ischemia, stroke or injury to the cardiovascular system during ischemia, or for enhancing wound healing, reducing scarring or enhancing angiogenesis or arteriogenesis.

A process for preparing (R)-N-((S)-1-(4-(3,3-dimethyl-2-oxoindolin-1-yl)piperidin-1-yl)-1-oxo-4-phenylbutan-2-yl)piperidine-3-carboxamide HCl-salt Crystalline Form A, wherein the HCl-salt Crystalline Form A is characterized by an X-ray powder diffraction (XRPD) pattern obtained by irradiation with copper K-alpha (Cu Kα) radiation comprising peaks at 14.7±0.2 and 17.5±0.2 degrees two-theta, which comprises the step of crystallizing the crystalline form from a solvent.

Provided herein are compounds having the following structure: (I), or an N-oxide thereof, or a pharmaceutically acceptable salt, stereoisomer, tautomer, or a deuterated analog thereof, wherein the substituents are as defined herein, their pharmaceutical compositions and uses for modulating the activity of PRMT5 in cooperation with methylthioadenosine (MTA) in tumors bearing MTAPDEL mutations, and their pharmaceutical compositions and methods of use.

The present invention relates to agricultural methods and the use of an active carboxamide derivative as an insecticide in seed treatment and soil application methods. The carboxamide derivative as an insecticide is highly suitable, alone or in combination with other active agricultural ingredients, for controlling animal pests, such as insects, mites, and / or nematodes, by treating the soil / growing substrate through soaking, drip application, immersion, or soil injection.

Provided herein is (R)-7-chloro-2-((1r,4R)-4-(3-methoxyaetidin-1-yl)cyclohexyl)-2,4-dimethyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide, or a pharmaceutically acceptable salt thereof for use in methods of treating certain cancers having at least one BAP1 mutation.

The present disclosure relates to PI3Kα inhibitors, their crystalline forms, solvates, compositions, and methods of use. For example, the present disclosure describes solid forms of compounds including the crystalline solid form of the following compounds: N-((1S,2R,4S)-4-(((S)-(3-chloro-2,6-difluorophenyl)(4-fluorobicyclo[2.2.1]heptane-1-yl)methyl)carbamoyl)-2-hydroxycyclopentyl)pyrimidine-5-carboxamide; and (1S,3S,4R)-3-acetamido-N-((S)-(3-chloro-2,6-difluorophenyl)(4-fluorobicyclo[2.2.1]heptane-1-yl)methyl)-4-hydroxycyclopentane-1-carboxamide.

The present invention relates to combinations of a compound of formula (A-1) with a compound selected from the group consisting of dimpropyridaz, emamectin and isocycloseram, bentioflumin, pioxaniliprole, isoflualanam, cybenzoxasulfyl, vinylfluthrin, cyclobunofen, flupymezotiaz, fentiazoluron, 1-(1,2-dimethylpropyl)-5-methyl-N-prop-2-ynyl-N-(3-pyridyl)pyrazole-4-carboxamide, 1 -[4- [5-ethylsulfonyl-1-methyl-4-[3-methyl-6-(trifluoromethyl)imidazo[4,5-b]pyridin-2-yl]imidazol-2- yl]phenyl]cyclopropanecarbonitrile, [(Z)-[[3-ethylsulfonyl-5-[4-(trifluoromethoxy)phenyl]-2-pyridyl]-[[5- (trifluoromethyl)-2-pyridyl]amino]methylene]amino] acetate, 3-[3-ethylsulfonyl-5-[4- (trifluoromethoxy)phenyl]-2-pyridyl]-4-[5-(trifluoromethyl)-2-pyridyl]-1,2,4-oxadiazol-5-one, 1-(4- chlorophenyl)-2-fluoro-4-methyl-5-(2,2,2-trifluoroethylsulfanyl)benzene, and emamectin benzoate; and to methods of controlling or preventing damage to plants using such combinations; and to formulations, concentrates and seed treatments comprising such combinations.

The present application relates to the formula shown with BCA Tm agonist effect 2- (amino carbonyl) -1H-indole-5-carboxamide derivatives, its racemate or optical isomer, its solvate, or its pharmaceutically acceptable salt, and its use in the preparation of treating metabolic syndrome or obesity drugs and the use of pharmaceutical compositions containing them. Wherein, R1 is the following substituent group amide, methanol, methyl sulfonamide.

This invention relates to deuterated 3-oxo-2,3-dihydropyridazine-4-carboxamide inhibitors, their preparation methods, and applications. Specifically, the compounds of this invention have the structure shown in formula (I). This invention also discloses the preparation method of the compounds and their use as AhR inhibitors. The compounds of this invention exhibit excellent selective inhibition of AhR and possess better pharmacodynamic and pharmacokinetic properties, as well as lower toxicity.

The invention relates to processes for producing racemic (4R,4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carboxamide of formula (I) from the enantiomers (Ia) or (Ib); a process for producing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carboxamide of formula (Ia); a process for producing racemic (4R,4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carboxamide of formula (I) from the pyridine of formula (II). The subjects of the invention have in common the irradiation of the compound of formulas (Ia), (Ib) and / or (II) with light in a suitable solvent, or solvent mixture, in the presence of a base. The compounds of formulas (Ia), (Ib) and / or (II) are intermediate products, by-products or target compounds in the synthesis of finerenone (compound according to formula (Ia)).

The application relates to the technical field of drug synthesis, in particular to a synthesis method and application of a 2-(cyclopropylamide)thiazole-4-amide derivative. The thiazole structure is shown in formula I. The preparation method of the 2-(cyclopropylamide)thiazole-4-amide derivative is as follows: the compound shown in formula I is obtained by reacting the compound shown in formula II in the presence of HATU, DIPEA, a primary amine or a secondary amine and tetrahydrofuran. The 2-(cyclopropylamide)thiazole-4-amide derivative has the effect of relieving Alzheimer's disease, and is characterized by strong cholinesterase inhibition activity.

The present invention provides pyridazine-3-carboxamide compounds of general formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, racemate, solvate, hydrate, polymorph, prodrug or isotopic variant thereof. The present invention also provides pharmaceutical compositions comprising said compounds, processes for their preparation and their use in the treatment or prevention of TYK2 kinase-mediated diseases.

The application provides a 4-(2,4-dihydroxyphenyl)thiazole-2-carboxylic amide derivative and a preparation method and application thereof, and relates to the technical field of organic chemistry.The application provides a 4-(2,4-dihydroxyphenyl)thiazole-2-carboxylic amide derivative compound.The 4-(2,4-dihydroxyphenyl)thiazole-2-carboxylic amide derivative has the functions of inhibiting tyrosinase and melanin production, and has the characteristics of low toxicity and high safety.The preparation method can obtain the 4-(2,4-dihydroxyphenyl)thiazole-2-carboxylic amide derivative at a high yield.

The present invention relates to compounds of formula (I) with STAT6 inhibitory activity for use in methods of treatment of inflammatory or allergic diseases, such as e.g. atopic dermatitis.

The application discloses a pyrazole hexacyclic-5-formamide compound containing an aromatic (ethyl) amide group and a preparation and application thereof. A structural general formula of the compound is shown as formula I. The compound is prepared through an amide condensation reaction, and the preparation method is simple. The pyrazole hexacyclic-5-formamide compound containing the aromatic (ethyl) amide group has an obvious inhibiting effect on growth and development of agricultural pests and growth and development of monocotyledonous or dicotyledonous plants. After application, the pests show symptoms of individual atrophy, skin wrinkling, abnormal molting of insect body deformity and even death, and the plants show that the growth of roots and stems is inhibited. The formula I compound can be applied in agriculture as an insecticide and / or herbicide.

The present disclosure relates to a compound of Formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or tautomer thereof, wherein the variable are as defined herein. The invention further provides modulators or inhibitors of STAT6 activity, processes for their preparation, pharmaceutical compositions, and medicaments containing them, and their use in diseases and disorders mediated by IL-4 and / or IL-13.

The disclosure is in part directed to crystalline free base forms of N-(4-((2-methoxy-3-(1-(methyl-d / 3)-1H,2,4-triazol-3-yl)phenyl) amino)-5-(propanoyl-3,3,3-d / 3)pyridin-2-yl) cyclopropane carboxamide, pharmaceutical compositions thereof, and methods of use.

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

The present invention provides solid forms of N-[(1S,2E)-1-cyclopropyl-3- (methanesulfonyl)prop-2-en-1-yl]-2-(1,1-difluoroethyl)-4-phenoxypyrimidine-5-carboxamideide and solvates thereof, as well as therapeutic uses thereof and pharmaceutical composition comprising them.

Disclosed in the present invention are a pyrazole carboxamide compound and a use thereof. Specifically, disclosed is the compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention is an IL-17 small molecule modulator, and can be used for treating or preventing IL-17-mediated diseases, such as autoimmune diseases.

The present invention provides pyridazine-3-carboxamide compounds of general formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, racemate, solvate, hydrate, polymorph, prodrug or isotopic variant thereof. The present invention also provides pharmaceutical compositions comprising said compounds, processes for their preparation and their use in the treatment or prevention of TYK2 kinase-mediated diseases.