487 results about "Methylamide" patented technology

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 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 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 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.

The utility model relates to the technical field of mixing devices, and discloses a mixing device for synthesizing an anthranilamide compound, which comprises a reaction kettle, a feeding pipe is arranged on the upper surface of the reaction kettle, a discharging pipe is arranged at the center of the bottom of the reaction kettle, and a support frame is arranged on the lower surface of the reaction kettle; the motor is arranged on the upper surface of the bottom plate of the supporting frame, a rotating rod is coaxially mounted on a rotor of the motor, a stirring frame is mounted at the bottom, penetrating through the reaction kettle, of the rotating rod, and mixing rods are mounted on the inner walls of the two sides of the stirring frame; the rotating directions of the additionally arranged driving rod and the rotating rod are opposite, so that the stirring rod can be driven to rotate anticlockwise along the inner cavity of the reaction kettle, and an anthranilamide compound in the reaction kettle is stirred in two different directions, so that the compound can be prevented from forming a vortex to be accumulated at the bottom or the edge of the inner cavity of the reaction kettle; and the compounds can be fully mixed.

The subject of the invention is N-substituted derivatives of l-(l-phenyl-3-aryl)-lH-pyrazol-4-yl)methanamine with the general formula 1, where ¥ represents CH or N, R1 represents hydrogen, R2 represents no substituent, R3 represents hydrogen, while R4 represents N-propylbenzamide, benzo[b]furan, dihydrobenzo [b] furan, methylenedioxybenzene, ethyl benzoate, or propyl benzoate, substituted accordingly, their method of production and application, and the method of obtaining and application of N-substituted derivatives of l-(l-phenyl-3-aryl)-IH-pyrazol-4-yl)methanamine with the general formula 1, where Y represents C, CH, or N, R1 represents hydrogen or a methyl group, R2 represents a methyl group or no substituent, R3 represents hydrogen or a methyl group, while R4 represents dimethylpyrazole, methylpyrazole, dimethylimidazo[l,2-a]pyrimidine, or isopropoxybenzene, substituted accordingly. The compounds that are the subject of the invention are obtained through reductive amination using borohydride derivatives as the reducing agent, advantageously sodium triacetoxyborohydride, in the amount of 1.4-2.0 eq, amine in the amount of 1.0-1.1 eq, advantageously in slight excess, base, advantageously triethylamine in the amount of 1.0-1.1 eq (in the case of using amine in the form of hydrochloride), and the starting aldehyde. The reaction is conducted in a nonpolar solvent environment, advantageously dichloroethane at a concentration of about 0.1 M. The crude product is purified by column chromatography on silica gel using a methanol in dichloromethane mixture as the eluent, in concentration ranges from 2% to 5%. In order to obtain a solid form and improve the physicochemical parameters, the free bases are converted into hydrochloride form, and then crystallized from a polar solvent, advantageously ethanol or propanol.

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 present application provides: a phosphoribosylaminoimidazole-succinoylcarboxamide synthase variant; a microorganism comprising the variant; a composition for producing a purine nucleotide, the composition comprising the microorganism; and a method of producing a purine nucleotide, the method comprising the step of culturing the microorganism.

The invention discloses a 4-amino-2-methylbenzamide HBV capsid protein inhibitor as well as a preparation method and application thereof. The compound has a structure as shown in a general formula I. The invention further discloses a preparation method and application of the 4-amino-2-methylbenzamide HBV capsid protein inhibitor. The invention also relates to a preparation method of the compound with the structure as shown in the general formula I, a pharmaceutical composition and application of the compound in preparation of anti-HBV drugs.

The present disclosure relates, in part, to solid forms of (S)-N-(8-(2-chloro-5-fluorophenyl)-3-(methylcarbamoyl)-6-oxo-5, 6, 7, 8-tetrahydroimidazo [1, 5-a] pyrazin-1-yl) benzo [d] isothiazol-3-carboxamide, salts thereof, crystalline forms thereof, and variants thereof.

The invention belongs to the technical field of biological medicines, relates to application of a compound 1 in treatment or prevention of diseases related to RET fusion and / or RET mutation, and provides application of N (3-chloro-5 (trifluoromethyl) phenyl) 3 ((6 (4-hydroxypiperidine-1-yl) imidazo [1, 2-a] pyridin-2-yl)-1, 3, 4-triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4 The invention relates to application of (2R, 2R, 2b) pyridazin-3-yl) ethynyl) 2-methylbenzamide or pharmaceutically acceptable salts thereof in treatment or prevention of RET fusion and / or RET mutation related diseases, and application of the (2R, 2R, 2b) pyridazin-3-yl) ethynyl) 2-methylbenzamide or pharmaceutically acceptable salts thereof in treatment or prevention of RET fusion and / or RET mutation related diseases in treatment or prevention of RET fusion and / or RET mutation related diseases by utilizing broad-spectrum and efficient RET inhibition activity, excellent drug-resistant mutation covering ability and higher safety The technical problems of drug resistance, off-target toxicity, high medication frequency and the like of the existing RET inhibitor are solved, and a new effective means is provided for accurate treatment of RET-driven tumors.

Disclosed herein is a novel tool to associate protein cargo molecules to the inside and / or outside of a Hepatitis B Virus (HBV) virus-like particle (VLP). The novel tool being composed of a sulfamoylbenzamide (SBA) antiviral, linker, and protein.

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.