826 results about "Carboxamide" patented technology

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.

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 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.

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.

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.

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 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 invention belongs to the technical field of perovskite materials, and particularly relates to application of triazole formamide, a perovskite precursor solution and a preparation method and application of the perovskite precursor solution, triazole formamide serves as an additive to be added into perovskite, and triazole formamide is 1, 2, 4 triazole-3-formamide. According to the method, the homogenization of the large-area film is realized and the defects in the perovskite polycrystalline film are effectively passivated in the nucleation and crystallization process in the process of preparing the large-area perovskite polycrystalline film by using the small-molecule triazole formamide as the multi-active-site additive regulation and control solution method; therefore, the photoelectric conversion efficiency and the stability of the perovskite photovoltaic miniature module are improved.

The present disclosure relates generally to crystalline forms of (1S,2S)-N-(2-(4,6- bis(methoxy-d 3)pyrimidin-5-yl)-1-methyl-1H-pyrrolo[2, 3-c]pyridin-5-yl)-2- fluorocyclopropane-1-carboxamide (Compound 1), compositions thereof, and methods of using any of the foregoing.

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 invention relates to compounds of formula (I) as RAS-PI3K modulators for use in methods of treatment of cancer, immunological disorders and wound healing. Preferred compounds are e.g. l-(([l,l'-biphenyl]-2-yl)sulfonyl)-4-fluoro-N-(3-(methylsulfonyl)allyl)piperidine-4-carboxamide derivatives.

Provided herein are compounds, preferably (R)-N-(4-(chlorodifluoromethoxy) phenyl)-2-(difluoromethyl)-1-(1-hydroxypropan-2-yl)-7-(pyrimidin-5-yl)-1H-benzo[d]imidazole-5-carboxamide having the Formula Ior a pharmaceutically acceptable salt or tautomer thereof, that inhibits tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and / or symptomology of the disease.

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 invention relates to crystalline particles of N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazol-3-carboxamide (I) having a specific surface area (SSA) in the range of from about 8 to about 16 m2 / g, preferably from about 10 to about 15 m2 / g, and to a process for preparing said particles. Compound (I) is potent androgen receptor (AR) modulators, which are useful as medicaments, for example in the treatment of prostate cancer.

The invention discloses a synthesis method of an inner piroxostat key intermediate and a synthesis method of inner piroxostat. The invention provides a novel synthesis method of an inner piroxostat key intermediate 5, 7-difluoro-1, 2, 3, 4-tetrahydronaphthalene-2-amine, which comprises the following steps: taking 3, 5-difluorobenzyl bromide as a raw material, carrying out substitution reaction on the 3, 5-difluorobenzyl bromide and methane tricarboxylic acid triethyl ester, then carrying out hydrolysis decarboxylation, adding 1, 2, 3, 4-tetrahydronaphthalene-2-amine, and carrying out reaction to obtain the 5, 7-difluoro-1, 2, 3, 4-tetrahydronaphthalene-2-amine. The preparation method comprises the following steps: substituting 1, 2-diiodoethane, catalyzing carbon-hydrogen activation and ring closing by tetrakis (triphenylphosphine) palladium, hydrolyzing and decarboxylating, amidating, and carrying out Hofmann degradation reaction to obtain a target intermediate. The method has the advantages of cheap and easily available raw materials, simple synthesis and high yield, avoids the use of ethylene, sodium azide and other reagents, and is green and safe. The invention provides a method for further synthesizing the endopiroxostat based on the synthesis method, the method comprises a novel endopiroxostat hydrochloride chiral resolution method, the chiral pure endopiroxostat is conveniently prepared through a chiral preparative column, and the ee value is 100%.

Disclosed are a crystal of the compound (S)—N—((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazacycloheptane-2-carboxamide salt or a salt thereof, a preparation method therefor, and the uses thereof in pharmaceutical compositions and in medicine.