322 results about "Carboxamide" patented technology

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.

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 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.

Certain substituted pyrazine-2-carboxamides of formula (I), and pharma- ceutically acceptable salts thereof, are disclosed, along with compositions containing them, and their use in therapy. The compounds are inhibitors of hematopoietic progenitor kinase 1 (HPK1), and are therefore particularly useful in the treatment or prevention of cancer. [Case 1] TIFF2024527623000305.tif30161

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.

The application relates to quinoline and quinazoline carboxamide derivatives of the general formula (I) that have activity as cluster of differentiation 38 (CD38) inhibitors, and to pharmaceutical compositions comprising such compounds. The compounds are useful for preventing or treating diseases and disorders such as, for example, diseases and disorders of metabolism.

The invention discloses a crystal form of carboxamide triazole. The crystal form I shows characteristic peaks at the positions of 20.3 degrees + / -0.2 degrees, 22.1 degrees + / -0.2 degrees, 23.4 degrees + / -0.2 degrees, 25.2 degrees + / -0.2 degrees, 28.6 degrees + / -0.2 degrees and 28.9 degrees + / -0.2 degrees in an X-ray powder diffraction pattern expressed by a 2theta diffraction angle; the crystal form II shows characteristic peaks at the positions of 3.8 degrees + / -0.2 degrees, 14.9 degrees + / -0.2 degrees, 19.2 degrees + / -0.2 degrees, 22.3 degrees + / -0.2 degrees, 25.4 degrees + / -0.2 degrees and 28.9 degrees + / -0.2 degrees in an X-ray powder diffraction pattern represented by a 2theta diffraction angle; the crystal form III shows characteristic peaks at the positions of 3.4 degrees + / -0.2 degrees, 3.7 degrees + / -0.2 degrees, 12.1 degrees + / -0.2 degrees, 14.8 degrees + / -0.2 degrees, 20.2 degrees + / -0.2 degrees and 24.3 degrees + / -0.2 degrees in an X-ray powder diffraction pattern expressed by a 2theta diffraction angle.

The invention discloses a preparation method of an optically pure mepivacaine hydrochloride intermediate. According to the method, N-(2, 6-dimethylphenyl) pyridine carboxamide is used as a starting material, hydrogenation reduction is carried out in the presence of a ligand and a catalyst to obtain the mepivacaine hydrochloride intermediate ((S)-N-(2, 6-dimethylphenyl) piperidine-2-carboxamide), the ee value of the obtained mepivacaine hydrochloride intermediate can reach 93%, the yield can reach 95%, post-treatment is simple, and the method is suitable for industrial production. The method is very suitable for large-scale workshop production. The ligand used in the invention is cheap and easily available, and can be refined and recovered through column chromatography, and the catalytic effect of the recovered ligand is consistent with that of a newly purchased ligand.

The present invention relates to fungicidal compositions comprising a carboxamide (Compound I) and at least one active compound II. The invention also relates to an agrochemical composition comprising the composition and a solvent of a solid carrier. In addition, the invention relates to the non-therapeutic use of the composition of the invention to control phytopathogenic harmful fungi.

To provide a compound that expands the spectrum of pesticides.SOLUTION: Provided is a compound represented by formula (b*): (in the formula, E is hydrogen or a C1-C6 alkyl group; A is -CN, chlorine, or fluorine; and L is S, SO, or SO2).SELECTED DRAWING: None

New derivatives of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl) phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo [3,4c] pyridine-3-carboxamide (Apixaban) able to increase its water solubility. These derivatives are cocrystals derivatives ofApixaban of different acids, from which the most outstanding are the following: Apixaban Malonic Acid derivative, Apixaban-a-Ketoglutaric Acid derivative, Apixaban-Gallic Acid derivative, Apixaban-Maleic Acid derivative, Apixaban-L-Tartaric Acid derivative, and Apixaban Citric Acid derivative.

The invention relates to a synthesis method of 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, which comprises the following four steps: carrying out a Knoevenagel condensation reaction, carrying out a Hantzsch dihydropyridine synthesis method, carrying out an O-ethylation reaction and carrying out a deprotection reaction to synthesize the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, and carrying out a reaction to obtain the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide. The preparation method of the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide has the advantages that the selectivity is high, the post-treatment is simple, the yield and the purity of the product are high, a new synthesis route and method are developed for synthesizing the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, the amplified production is conveniently realized, and the method is suitable for industrial production. The method has good application potential and research value.

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.

N-[(S)-[3-[1-(2,2-difluoropropylcarbamoyl)-3-hydroxy-3-methyl- cyclobutyl]imidazo[1,2-b][1,2,4]triazin-6-yl]-[4-(trifluoromethyl)cyclohexyl]methyl]-4-5 methyl-1,2,5-oxadiazole-3-carboxamide, or a pharmaceutically acceptable salt and / or solvate thereof, being a potent modulator of human IL-17 activity, is accordingly of benefit in the treatment and / or prevention of various human ailments, including inflammatory and autoimmune disorders.

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.

[Problem] To provide a substance having an activity of antagonizing the binding of histamine to histamine-H3 receptor, or having an activity of inhibiting the homeostatic activity of histamine-H3 receptor. [Means for Solution] A compound of the following formula (I) is provided: [wherein X, Y, Z and W each independently represent a methine group optionally having 1 or 2 substituents, or a nitrogen atom (provided that a case where all of X, Y, Z and W are an optionallysubstituted methine group); A, B and D represent C(0)-, etc.; Q represents a methine group or a nitrogen atom; R represents an optionallysubstituted group of the following formula (II-1): (wherein R7 and R8 each independently represent a lower alkyl group, etc.)].

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 invention belongs to the technical field of biological medicines, and particularly relates to a pharmaceutical composition containing carboxamide triazole or pharmaceutically acceptable salts thereof and application of the pharmaceutical composition in preparation of medicines for preventing or treating fibrosis-related diseases. Specifically, the invention discovers that the carboxylamine triazole orotate (CTO) can directly inhibit fibroblast collagen generation and cross-linking maturation, so that the fibrosis degree is reduced; when the polypeptide is combined with a PD-1 antibody, collagen deposition in tumor tissues can be reduced by inducing normalization of a tumor matrix in a synergistic manner, the tumor permeation concentration of chemotherapeutic drugs is remarkably enhanced, and the anti-tumor curative effect is improved. The invention can be applied to the treatment of various matrix dense solid tumors including pancreatic cancer, breast cancer, colorectal cancer and lung adenocarcinoma, and is expanded for intervention of fibrosis-related diseases, thereby providing a new treatment strategy for improving the efficacy of chemotherapeutic drugs and improving immunotherapy response through targeted matrix remodeling.

Disclosed are crystalline salt Forms C and D of 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide. Form C is a MSA salt and Form D is a sulfate salt of Compound (I). Characterization data for the Forms are disclosed.

The present invention relates to fungicidal compositions comprising at least one compound selected from the group consisting (I-1) N-[1,3-dimethyl-1-(phenylmethyl)butyl]-8-fluoro-3- quinolinecarboxamide, (I-2) N-[(1R)-1-benzyl-1,3-dimethyl-butyl]-8-fluoro-quinoline-3- carboxamide, (I-3) N-[(1S)-1-benzyl-1,3-dimethyl-butyl]-8-fluoro-quinoline-3-carboxamide, as active component 2) at least one compound, or an N-oxide, or an agriculturally useful salt thereof, selected from the group consisting of (II-1) 2-fluoro-4-[5-(trifluoromethyl)-1,2,4- oxadiazol-3-yl]benzanilide, (II-2) metarylpicoxamid,(II-3) N-methoxy-N-[[4-[5-(trifluoromethyl)- 1,2,4-oxadiazol-3-yl]phenyl]methyl]cyclopropanecarboxamide, (II-4) N,2-dimethoxy-N-[[4-[5- (trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]propenamide,(II-5) methyl (Z)-3-methoxy-2- (2-methyl-5-phenyl-phenoxy)prop-2-enoate, wherein the weight ratio of compound I to compound II is from 10:1 to 1:10. The invention also relates to an agrochemical composition comprising the composition and a solvent of solid carrier. Further, the invention relates to a non- therapeutic use of the inventive compositions controlling phytopathogenic harmful fungi.