1052 results about "Carboxamide" patented technology

The present invention relates to four specific macrocyclic compounds for use as inhibitors of KRAS mutant for the treatment of cancer. Example (1): 1-[4-(dimethylamino)-4-methyl-pent-2-ynoyl]-N-[(1S)-1-[[(6S,8S,14S)-22-ethyl-25-fluoro-(21M)-21-[2-[(1S)-1-methoxyethyl]-3-pyridyl]-18,18-dimethyl-9,15-dioxo-5,16-dioxa-2,10,22,28-tetrazapentacyclo[18.5.2.12,6.110,14.023,27]nonacosa-1(26),20,23(27),24-tetraen-8-yl]carbamoyl]-2-methyl-propyl]-4-fluoro-N-methyl-piperidine-4-carboxamide.

The invention relates to the field of prevention and treatment of plant filamentous fungal diseases, in particular to an application of a compound NSC-32 (N-[(5Z)-4-oxo-5-(phenylmethylidene-1, 3-thiazolidin-3-yl) pyridin-4-carboxamide) in prevention and treatment of magnaporthe oryzae, and a preparation method of the compound NSC-32 (N-[(5Z)-4-oxo-5-(phenylmethylidene-1, 3-thiazolidin-3-yl) pyridin-4-carboxamide). MoPex19 protein is used as a target spot, a compound NSC-32 is obtained through screening, and it is proved that the compound can inhibit growth of magnaporthe oryzae and reduce pathogenicity of the magnaporthe oryzae. In addition, the application object, the use method, the target specificity and the action mechanism of the compound NSC-32 are further explored, and a new green pesticide and a new thought are provided for preventing and treating the magnaporthe oryzae.

Disclosed are naphthyl compounds comprising either a ureido piperidine-1 -carboxamide or a ureido piperidine-1 -carboxylate moiety, compositions thereof, and methods of use thereof, for treating or preventing a disease or disorder associated with abnormal levels of amino acids by modulation of SLC6A19 transport, such as phenylketonuria, hyperphenylalaninemia, diabetes and chronic kidney disease.

The invention relates to the field of organic chemical synthesis, in particular to a synthetic method and application of pyrimidone compounds. The invention provides a synthesis method, reactants are o-amino heterocyclic formamide and triethyl orthoformate respectively, a solvent system is a hexafluoroisopropanol solvent, and a product is a heterocyclic pyrimidone compound. The reaction does not need strong acid or strong alkali conditions, does not need additional reducing agents or oxidizing agents, does not need transition metal catalysis, is economical and practical, the reaction conditions are relatively mild, and the synthesized pyrimidone compound has a good antibacterial effect.

Stable and bioavailable formulations and dosage forms comprising a dispersion (e.g., spray-dried dispersion) of solid amorphous 6-(cyclopropancamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide (Formula (I): BMS-986165) in a solid polymer matrix are provided for the treatment of auto-immune and auto-inflammatory diseases such as an inflammatory bowel disease (IBD) and psoriasis.

The present disclosure provides compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, wherein X1, R1, R2, R3, R4, R5 and R6 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; the use of such compounds and salts for the treatment or prevention of prolyl endopeptidase fibroblast activation protein (FAP) mediated disorders; kits comprising such compounds and salts; and processes for preparing such compounds and salts. # imgabs0 #

The combination of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or pharmaceutically acceptable salt thereof, and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4′-piperidine]-1′-carbonyl)-6-methoxypyridin-2-yl)benzoic acid or pharmaceutically acceptable salt thereof, for treatment of diseases, including non-alcoholic steatohepatitis (NASH), in mammals are described herein.

The present invention relates to a ternary insecticidal composition of 3-[benzoyl(methyl)amino]-N-[2-bromo-4-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)- 6-(trifluoromethyl)phenyl]-2-fluorobenzamide (Component A), 4-chloro-5-ethyl-2-methyl-N-[[4-(4-methylphenoxy)phenyl]methyl] pyrazole-3-carboxamide (Component B) and at least one insecticide (Component C) demonstrating an effective and synergistic broad spectrum control of insects-pests and mites with one shot application by developing delay in resistance of hard to kill and resistant towards insects-pests and mites Further, the ternary insecticidal composition provides residual control and increases yield of treated plants due to protection against insect-pests and mites. The ternary insecticidal composition of present invention increases overall health and plant vigor and is environmentally safe.

The present invention relates to a process for the preparation of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of formula (I) and to the preparation and use of crystalline modification I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of formula (I).

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.

There is provided a process for preparing 5,7-dimethyl-N-((1R,4R)-4- (pentyloxy)cyclohexyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide, said process comprising at least a step of amide coupling a 5,7-Dimethylpyrazolo[1,5-a]pyrimidine-3-carboxylic acid with trans-4-(pentyloxy)cyclohexanamine using carbonyldiimidazole (CDI).

The present invention relates to a process for preparing acyloxymethyl esters of (4S)-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxylic acid of the formula (IIa) by optical resolution of the compound of the formula (II) using a hydrolase. The invention also relates to a process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (Ia), wherein the process comprises the optical resolution of the compound of the formula (II) using a hydrolase. The invention additionally also relates to the use of a hydrolase in a process for preparing a compound of formula (IIa). The invention further relates to the use of a hydrolase in a process for preparing a compound of formula (Ia).

The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

The present disclosure relates to solid-state forms and corresponding pharmaceutical compositions of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, and methods of treatment, including treatment of rheumatoid arthritis and juvenile idiopathic arthritis using the same. The treatment methods generally comprise administering to a patient (e.g., a pediatric patient) a therapeutically effective amount of upadacitinib as a stable liquid pharmaceutical composition or a solid dosage form, at a dose based on patient body weight.

Provided herein is a process for the preparation of (R)—N-(5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)-1-methyl-1H-pyrazole-4-carboxamide, intermediates thereof, and salts of the foregoing.

The present disclosure relates to PI3K-alpha inhibitors, the crystalline forms, the solvates thereof, and the compositions and methods of use thereof. For example, the present disclosure describes compounds in solid form, including crystalline solid forms of compounds: N-((1S,2R,4S)-4-(((S)-(3-chloro-2,6-difluorophenyl)(4-fluorobicyclo[2.2.1]heptan-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]heptan-1-yl)methyl)-4-hydroxycyclopentane-1-carboxamide.

Pyridine carboxamide compounds for inhibiting NaV1.8 and methods for treating a condition, disease, or disorder associated with an increased NaV1.8 activity or expression are disclosed.

This invention relates to formula I: This relates to the compounds of JPEG2026512972000438.jpg4271, methods for their manufacture, pharmaceutical compositions containing them, and their use in the treatment of conditions related to the function of metabotropic glutamate receptor subtype 4 (mGluR4), in particular, and / or in the prevention of such conditions. A, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 The terms have the meanings provided herein.

The present application relates to novel substituted heterocyclic carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and / or prevention of diseases and to their use for producing medicaments for the treatment and / or prevention of diseases, in particular for the treatment and / or prevention of breathing difficulties including sleep-induced breathing difficulties such as central and obstructive sleep apnoea, snoring (primary and obstructive snoring), dysphagia, peripheral and cardiac vascular disorders including diabetic microangiopathies and disorders of the peripheral and central nervous system including neurodegenerative and neuroinflammatory disorders.

The present invention relates to pharmaceutical compositions containing N-(1,3-dimethylpyrazol-4-yl)sulfonyl-6-[3-(3,3, 3-trifluoro-2,2-dimethyl-propoxy)pyrazol-1-yl]-2-[(4S)-2,2,4-trimethylpyrrolidin-1-yl]pyridine-3-carboxamide, a solid dispersion of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-7V-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-en indol-5-yl)cyclopropanecarboxamide, and a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-quinoline-3-carboxamide, including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical compositions.

Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

The invention provides a novel covalent organic framework-based all-solid-state Z-type heterojunction photocatalyst and a preparation method and application thereof.According to the photocatalyst, a two-dimensional triazinyl covalent organic framework material (CTF) and a two-dimensional Ag / TiO2 nanosheet are compounded through electrostatic self-assembly for the first time, then heating is conducted in an inert gas atmosphere at the temperature of 200-350 DEG C, and the photocatalyst is obtained. Nitrogen vacancy is introduced while the interfacial interaction is enhanced, and the covalent organic framework-based all-solid-state Z-type heterojunction photocatalyst is obtained; the two-dimensional triazinyl covalent organic framework material is prepared by mixing and reacting 1, 4-benzenedimethanol, 1, 4-benzene dicarboxamide hydrochloride (1: 2) and Cs2CO3; experiments show that the photocatalyst provided by the invention not only can improve the separation and transfer efficiency of photo-induced electrons-holes in CTF, but also can reduce the CO2 reduction reaction energy barrier and promote the CO2 adsorption and activation ability, thereby showing excellent CO2 catalytic reaction activity and cycle stability.

Provided herein are solid forms and methods of prepapation relating to (R) -3- (tert-butyl) -N-(1- (4- (6- (6- (4- ( (1- (4- (2, 4-dioxotetrahydropyrimidin-1 (2H) -yl) phenyl) piperidin-4-yl) methyl) piperazin-1-yl) pyridin-3-yl) -7H-pyrrolo [2, 3-d] pyrimidin-4-yl) -2-methylphenyl) ethyl) -1,2,4-oxadiazole-5-carboxamide.

Disclosed are processes for the preparation of the pesticide N-(1-methylcyclopropyl)-2-(3-pyridinyl)-2H-indazole 4-carboxamide. Also disclosed are methods for the preparation of intermediates of thereof N-(1-methylcyclopropyl)-2-(3-pyridinyl)-2H-indazole 4-carboxamide.

This document relates to crystalline or amorphous forms of oxoisoindole-5-carboxamide compounds, or salts or solvates thereof. It also discloses compositions containing the crystalline or amorphous forms, as well as methods for preparing and using the crystalline or amorphous forms. The resulting crystalline or amorphous forms have excellent solid-state stability and are of great value in drug development, formulation development, and production.

The present invention relates to salts and crystalline forms of 2-(3-(8-Amino-6-(trifluoromethyl)imidazo[1,2-a]pyrazin-3-yl)-4-methylphenyl)-3,3,3-trifluoro-2-hydroxypropanamide, crystalline forms of 8-amino-N-(2-hydroxy-2-methylpropyl)-3-(2-methyl-5-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide, and crystalline forms of 8-amino-N-(2-hydroxy-2-methylpropyl)-3-(2-(methyl-d3)-5-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide, which are PI3K inhibitors useful in the treatment of cancer and other diseases.

The present disclosure provides intermediates of 1-(1-oxo-1, 2-dihydrophthalazin-6-yl) cycloalkyl-1-carboxamide derivatives, and methods of synthesis thereof. The present invention relates to a 1-(1-oxo-1, 2-dihydrophthalazin-6-yl) cycloalkyl-1-carboxamide derivative compound, which can be used to selectively inhibit the synergistic activity of PRMT5 and MTA in a tumor carrying an MTAPDEL mutation, and a pharmaceutical composition comprising the compound as a therapeutic agent for various diseases, including cancer.

The invention discloses a pyrazolecarboxamide compound and application of the pyrazolecarboxamide compound. Specifically, the invention discloses a compound shown as a formula I or a pharmaceutically acceptable salt thereof. The compounds of the present invention are IL-17 small molecule modulators, and can be used for the treatment or prevention of IL-17 mediated diseases, such as autoimmune diseases.

The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.