314 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.

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 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.

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 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.

[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.)].

Described herein are modified monoterpene TRPM8 activating compounds. In particular, provided herein are compounds that affect intracellular ion channel function, and are useful as or in conjunction with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and disorders, including inflammatory eye diseases (e.g., uveitis), cardiovascular diseases, inflammatory diseases, and diseases characterized by aberrant hyperplasia (e.g., cancer).

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 provides a weeding composition which comprises a component A and a component B. The component A is one of a compound 1, a compound 2 and a compound 3, the component B is selected from one of tembotrione, isoxaflutole, dicamba, foramsulfuron, nicosulfuron, rimsulfuron, topramezone, 2, 4-D isooctyl ester, fenoxaprop-p-ethyl and MCPA, and the component B is one of tembotrione, isoxaflutole, dicamba, foramsulfuron, nicosulfuron, rimsulfuron, topramezone, 2, 4-D isooctyl ester, fenoxaprop-p-ethyl and MCPA. The component A and the component B in the composition have a good synergistic effect, and the composition has a good application prospect.

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.

Methods of treating non-metastatic castration-resistant prostate cancer in a subject having severe liver damage are provided.SOLUTION: Provided are methods of treating non-metastatic castration-resistant prostate cancer in a subject with severe hepatic impairment with an androgen receptor inhibitor comprising 4 - [7 - (6-cyano-5-trifluoromethylpyridin-3-yl) - 8-oxo-6-thioxo-5, 7-diazaspiro [3.4] oct-5-yl] - 2-fluoro-N-methylbenzamide (apalutamide).SELECTED DRAWING: None

This invention relates to the prevention and / or treatment of protein tyrosine kinase-mediated diseases, particularly phosphatidylinositol 3-kinase (PI3Ks)-mediated diseases. PI3Ks are well known as oncological targets, and several PI3K inhibitors have been developed that inhibit numerous class 1A PI3K isoforms. The development of selective inhibitors of PI3K-α may enable sufficient targeted inhibition while avoiding some of the known toxic drawbacks of pan-PI3K inhibitors. The inventors have discovered that a novel carbamoti-oil-pyrrolidine-carboxamide compound of formula (I) exhibits advantageous PI3K inhibitory activity, particularly with high selectivity for the isoform PI3K-α. In particular, this invention relates to the compound of formula (I), or deuterated or tritiated forms of the compound of formula (I), and pharmaceutically acceptable salts thereof. [Formula 1] The present invention also relates to pharmaceutical compositions containing a compound of formula (I) for use in the treatment and / or prevention of protein tyrosine kinase-mediated diseases, and to a compound of formula (I).