727 results about "Methylamide" patented technology

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.

Telomerase reverse transcriptase (TERT) expression enhancing isoxazole-3-carboxamide compounds, and methods for using the same, are provided. These compounds and methods find use in a variety of applications in which increased expression of telomerase reverse transcriptase is desired.

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 invention discloses a super-smooth, anti-corrosion and anti-coagulation hydrogel composite coating on the surface of a medical instrument as well as a preparation method and application of the super-smooth, anti-corrosion and anti-coagulation hydrogel composite coating, and the super-smooth, anti-corrosion and anti-coagulation hydrogel composite coating is a surface hydrogel composite coating formed by taking N-(3, 4-dihydroxyphenethyl)-2-benzoylbenzamide (BPDA) as a primer and grafting a hydrophilic polymer on the primer. BPDA is deposited on the surface of the substrate, then hydrophilic monomer surface graft polymerization is initiated by light, and a hydrogel coating is constructed on the surface of the BPDA substrate. The BPDA primer provides excellent corrosion resistance, the corrosion rate of a metal substrate is effectively reduced, and benzophenone derivatives with photoreaction activity on BPDA molecules can mediate firm combination of the hydrogel layer; after meeting water, a stable and compact hydrated layer is formed, the super-lubricating property is achieved, adhesion of protein and cells can be remarkably inhibited, and thrombus formation is effectively prevented. The anti-corrosion and anti-blood coagulation coating has excellent anti-corrosion and anti-blood coagulation properties, and is widely applicable to anti-blood coagulation and anti-corrosion surface modification in the fields of medical instruments and the like.

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 invention provides an N-(hydroxyalkyl pyridyl) tetrahydrofuran carboxamide compound, a prodrug, an oxide, a salt, a metal complex or a stereochemical isomer of a sodium channel regulator and a pharmaceutical composition containing the N-(hydroxyalkyl pyridyl) tetrahydrofuran carboxamide compound, the prodrug, the oxide, the salt, the metal complex or the stereochemical isomer. And their use as Nav inhibitors and their use in the preparation of medicaments for the treatment and / or alleviation of pain and pain-related diseases. The compound provided by the invention has the advantages of high metabolic stability, high oral absorption, better bioavailability, better activity, higher selectivity, better pharmacokinetic property, quicker effect, low cardiac side effect and the like.

The invention discloses a gamma-aminobutyric acid gated chloride ion channel allosteric modifier compound and an application thereof, namely (S)-4-(5-(3-chloro-5-(trifluoromethyl) phenyl)-5-(trifluoromethyl)-4, 5-dihydroisoxazole-3-yl)-2-methyl-N-(2-oxo-2-((2, 2, 2-trifluoroethyl) amino) ethyl) benzamide, and a preparation method of the gamma-aminobutyric acid gated chloride ion channel allosteric modifier compound. The compound has an excellent control effect on pests of thysanoptera, acarina, lepidoptera and the like, is very friendly to bees and high in environmental ecological safety, can be used for preparing efficient, low-toxicity and safe insecticides, and has a wide application prospect in agricultural production.

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 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.

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.

This invention relates to N-(3-(6-Amino-5-(2-(N-methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide drug substance substantially free of a nitrosamine impurity, e.g. the nitrosamine impurity N-(3-(6-amino-5-(2(methyl)(nitroso)amino)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide and novel processes of preparation thereof. The invention further relates to pharmaceutical composition comprising N-(3-(6-Amino-5-(2-(N- methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide, wherein the composition is substantially free of a nitrosamine impurity, e.g. the nitrosamine impurity N-(3-(6-amino-5-(2(methyl)(nitroso)amino)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide. Pharmaceutical products containing said drug substance and compositions are also disclosed, as well as methods for preparing said drug substance, pharmaceutical compositions and products.

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.

In some embodiments, the present disclosure provides a compound(S) or (R)-N-(4.6-difluorobenzo[d]thiazol-2-yl)-1-(2-(dimethylamino)ethyl) piperidine-3-carboxamide, as described herein, or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising the compound, and methods of treating. e.g., metabolic diseases using the compound are also provided.

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.

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.

The invention provides an application of a compound based on a 3-phenyl-1, 2, 4-oxadiazole-5-formamide skeleton in preparation of a medicine for treating pathological retinal neovascular diseases, and belongs to the technical field of biological medicines. The compound based on the 3-phenyl-1, 2, 4-oxadiazole-5-formamide skeleton developed by the invention can be used as an inhibitor of PPT1, and the palmitoylation modification level of a substrate is improved by inhibiting the enzyme activity of the PPT1. According to the compound, the palmitoylation modification of Gpx1 is improved by inhibiting PPT1, so that the generation of pathological retinal neovascularization is inhibited.

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 disclosure relates to a series of substituted imidazolecarboxamide compounds of formula I as BTK (Bruton's Tyrosine Kinase) inhibitors, and the methods of using the same for the treatment of autoimmune disease, inflammatory disease, cancer and potentially allergies.

The compound cis)-N—((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4 methyl-6-(5-methyl-1H-pyrazol-3-ylamino)pyrimidin-2-yl)cyclohexanecarboxamide can be prepared as a free base in various crystalline solid forms, and in various salt forms each having one or more solid forms.

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 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.