653 results about "Methylamide" patented technology

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

Disclosed are mixtures and compositions for controlling invertebrate pests relating to combinations comprising (a) 3-bromo-N-[4-chloro-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide, and its N-oxides, and suitable salts thereof

and a component (b) wherein the component (b) is at least one compound or agent selected from neonicotinoids, cholinesterase inhibitors, sodium channel modulators, chitin synthesis inhibitors, ecdysone agonists, lipid biosynthesis inhibitors, macrocyclic lactones, GABA-regulated chloride channel blockers, juvenile hormone mimics, ryanodine receptor ligands, octopamine receptor ligands, mitochondrial electron transport inhibitors, nereistoxin analogs, pyridalyl, flonicamid, pymetrozine, dieldrin, metaflumizone, biological agents, and suitable salts of the foregoing. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a mixture or composition of the invention.

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.

Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof,

are useful as kinase modulators, including Btk modulation.

The invention relates to processes for preparing compounds having the formula,

• • and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R₂, R₃, R₄, and R₅, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.

As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.

The invention relates to processes for preparing compounds having the formula,

and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R₂, R₃, R₄, and R₅, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith.

The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

The invention pertains to cooling agents comprising N-substituted p-menthane-3-carboxamides, menthyl acetate and solubilizer, and methods for making the cooling agents. The invention also concerns pharmaceutical compositions comprising the cooling agents, including tablets, suspensions and liquid solutions having active pharmaceutical agents for treating upper gastrointestinal tract distress, and methods for treating upper gastrointestinal tract distress in humans.

The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.

The subject invention provides 5-chloro-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide, its salts and uses.

The present invention relates to bioavailable pharmaceutical formulations of heterocyclic compounds, such as such as N-(3,5-dichloropyrid-4-yl)-4-difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide (oglemilast) and pharmaceutically acceptable salts thereof, to processes for their preparation and to methods of treatment using the same. The present invention also relates to substantially pure amorphous forms of heterocyclic compounds, such as oglemilast. The invention is particularly directed to bioavailable pharmaceutical oral dosage forms containing amorphous oglemilast.

The invention is directed to processes for preparing 2-aminothiazole-5-carboxamides of formula I

• • wherein R₁, R₂, R₃, R₄ and R₅ are as defined as set forth in the specification herein.

Compounds of the formula

wherein R₁, R₂, R₃, R₄, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis, and the like; allergic diseases such as asthma, or disorders of male or female genital function and the like.

Inhibitors of HBV replication of Formula (I)

including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X, R¹, R², R³ and R⁴ have the meaning as defined herein.

The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

A cooling topical cosmetic or dermatological preparation which comprises (1R,2S,5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2-yl)ethyl)cyclohexane carboxamide and/or (1R,2S,5R)-N-(4-cyanomethyl-phenyl)-2-isopropyl-5-methylcyclohexane carboxamide, in combination with menthoxypropanediol.

The invention discloses a 2-aryl quinazoline or 2-heterocyclic aryl quinazoline derivative and a preparation method thereof. The structural formula of the product is shown in a formula (i), wherein Ar represents aryl, substituted aryl, heterocyclic aryl or substituted heterocyclic aryl. The preparation method of the 2-aryl quinazoline or 2-heterocyclic aryl quinazoline derivative comprises the following steps of: reacting aromatic formaldehyde or heterocyclic aromatic formaldehyde with ortho-amino toluamide at high temperature to obtain a 2-aryl quinazoline-4(3H)-ketone derivative or a 2-heterocyclic aryl quinazoline-4(3H)-ketone derivative; subsequently reducing the 2-aryl quinazoline-4(3H)-ketone derivative or the 2-heterocyclic aryl quinazoline-4(3H)-ketone derivative into a 2-aryl-3,4-dihydro quinazoline derivative or a 2-heterocyclic aryl-3,4-dihydro quinazoline derivative by using an appropriate reducing agent; and finally synthesizing the 2-aryl quinazoline or 2-heterocyclic aryl quinazoline derivative by using an oxidizing agent in an oxidation mode. Compared with the conventional synthesis method, the preparation method has the advantages of easy and available raw material, simple synthesis method, temperate reaction condition, high yield and the like, is easy to purify, and is a synthesis method applicable to industrial production.