143 results about "Pyrazolylchalcone" patented technology

The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-TH-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

The invention provides an epoxy adhesive solution composition, a preparation method of an epoxy adhesive solution and a modified cellular board. The epoxy adhesive liquid composition comprises the following components in parts by weight: 53-58 parts of epoxy resin, 2-10 parts of a silane coupling agent, 1-10 parts of a curing agent, 1-5 parts of blocked isocyanate and 60-70 parts of water, wherein a blocking group of the blocked isocyanate is selected from hydroxyl, oximido, acylamino, amino, imidazolyl, pyrazolyl or piperazinyl. By introducing the blocked isocyanate with the specific structure, the epoxy adhesive liquid can be subjected to pre-crosslinking reaction in the early drying treatment process, the modulus and high temperature resistance of a formed dry film are improved, and the phenomenon of glue overflow in the subsequent curing stage is inhibited; therefore, the structural integrity and the bonding strength of the adhesive layer in the modified cellular board under the high-temperature condition are improved.

Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I):and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

Described herein is the farnesoid X receptor agonist, 4-((4-(1-(tert-butyl)-1H-pyrazol-4-yl)pyridin-2-yl)((4-(4-methoxy-3-methylphenyl)bicyclo[2.2.2]octan-1-yl)methyl)carbamoyl)cyclohexyl 3-hydroxyazetidine-trans-1-carboxylate, including crystalline forms and pharmaceutically acceptable salts, solvates, and formulations thereof.

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 invention relates to the technical field of 3D printing, in particular to two-component photo-thermal dual-curing 3D printing resin and a preparation method thereof. Comprising a component A and a component B, the component B is a chain extender; the component A is prepared from the following raw materials in parts by weight: 60 to 95 parts of polyurethane acrylic resin; 0.1-30 parts of an acrylic monomer; 0.5-30 parts of a blocked isocyanate modified acrylic monomer; 0.5 to 5 parts of a photoinitiator; 1-6 parts of an auxiliary agent; the acrylic monomer is polyethylene glycol acrylate and / or an acrylate monomer containing other active groups; the blocked isocyanate modified acrylic monomer is one or a composition of more of pyrazolyl carbonyl amino group-containing acrylic ester, ketoxime carbonyl amino group-containing acrylic ester and ester carbonyl amino group-containing acrylic ester. After the 3D printing resin prepared by the technical scheme is printed and cured, relatively good printing performance, mechanical property and durability are obtained.

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.

This disclosure relates to N 2 -(3-(2-(2H-1,2,3-triazol-2-yl)propan-2-yl)-1-cyclopropyl-1H-pyrazol-5-yl)-N 4 The present invention relates to crystalline and amorphous forms of -ethyl-5-(trifluoromethyl)pyrimidine-2,4-diamine (compound of formula I), co-crystals, pharmaceutical compositions, and preparations thereof. TIFF2026504627000045.tif4857

The present invention refers to compounds of formula (I). The present invention also relates to compounds of formula (I) for use as G Protein coupled Receptor 139 (GPR139) antagonists in methods of medical treatment of e.g. depression, Alzheimer's disease, schizophrenia, drug addiction, sleep disorders, pain, and attention deficit hyperactivity disorder. Exemplary compounds are e.g. 3-((1H-pyrazol-4-yl)methyl)-6′-(phenyl)-2H-(1,2′-bipyridin)-2-one derivatives and related compounds. The present description discloses the synthesis and characterisation of exemplary compounds, pharmacological data thereof, as well as exemplary tablet formulations comprising the compounds of the invention (e.g. page 83 to page 110; examples 1 to 33; reference example 1; test examples 1 and 2; tables 1 to 4).

This article describes pharmaceutical formulations of the farnesol X receptor agonist 3-hydroxyazacyclobutane-trans-1-carboxylic acid 4-((4-(1-(tert-butyl)-1H-pyrazol-4-yl)pyridin-2-yl)((4-(4-methoxy-3-methylphenyl)bicyclo[2.2.2]octane-1-yl)methyl)carbamoyl)cyclohexyl ester, and methods of using such pharmaceutical formulations to treat conditions, diseases, or symptoms associated with farnesol X receptor activity.

The application discloses a preparation method of baricitinib, and belongs to the technical field of drug synthesis. The method comprises the following steps: firstly, 2-[1-(ethylsulfonyl)-3-azetidinyl]acetonitrile and 4-pyrazole boron pinacol ester are subjected to a Michael addition reaction to obtain 1-(ethylsulfonyl)-3-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]-3-azetidine acetonitrile as an intermediate I; secondly, a protection group is introduced on the amino group of 4-chloropyrrolopyrimidine to obtain an intermediate II; finally, the intermediate I and the intermediate II are subjected to a Suzuki coupling process by adopting a method of combining a nickel pre-catalyst with a supporting ligand to obtain the baricitinib. The preparation method creatively realizes cross coupling of the baricitinib by adopting the cheap metal nickel as a catalyst, avoids the use of a heavy metal palladium catalyst, and has the advantages of low cost, low toxicity, small pollution, green environmental protection and the like.

The present application provides compounds of Formula (I), or a stereoisomer thereof, or a atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of a atropisomer thereof; methods of making the compounds and therapeutic uses thereof. The present application further provides combinations of pharmacologically active agents and pharmaceutical compositions comprising the compounds.

Provided herein are solid forms, e.g., polymorphs, of 2-(3-((7R,8aS)-7-fluorohexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl)-1-(5-methyl-2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)azetidin-3-yl)acetonitrile, which are useful for treating kinase-related diseases or disorders. The solid forms, and compositions thereof, are useful for treating diseases in a subject, including, but not limited to, ocular diseases such as glaucoma, ocular hypertension, ocular wound repair, neurodegenerative ocular diseases, retinal detachment, and non-ocular diseases such as nerve injury, or skin wound repair, or inflammatory diseases, among others. (Compound 1) TIFF2026501674000028.tif4839

One aspect of the present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is a phenyl group or a 5- or 6-membered heteroaryl group; Ring B is absent or is phenyl, pyridinyl, pyrazidinyl, pyrazinyl, pyrimidinyl, oxazolyl, isoxazolyl, thiadiazolyl, pyrazolyl, isothiazolyl or thiazolyl; Ring C is a fused bicyclic group of formula: (AA), wherein X1 to X9 form a substituted heteroaryl group containing at least one N and at least one NH; X-Y is -(CH2) m NR 21 CO; L is a direct bond or a linker group; Z is selected from alkyl, cycloalkyl, aryl, heteroaryl and heterocycloalkyl, each of which may be substituted; each R a and each R b is independently selected from alkyl, halo, haloalkyl, alkoxy, cycloalkoxy, haloalkoxy, cyano, NR 23 COR 25 、NR 24 -SO2R 26 、(CH2) q SR 27 、(CH2) q SOR 28 、(CH2) q SO2R 29 、SO2NR 30 R 31 、(CH2) q OH、(CH2) q OR 32 、NR 33 R 34 、CONR 35 R 36 、cycloalkyl and (CH q 2)-heterocycloalkyl; R 10 、R 11 、R 21 、R 22 、R 23 and R 24 are each independently selected from H and alkyl; R 12 ~R 20 、and R 25 ~R36 Each of the following is independently selected from H, alkyl, aralkyl, alkoxy, alkoxyalkyl, hydroxyalkyl, and cycloalkyl; each of m, n, and p is independently an integer from 0 to 4; and each of q is independently an integer from 0 to 4. Further aspects of the present invention relate to pharmaceutical compositions comprising the compounds according to the present invention and the use of the compounds in the treatment of various GPR35-related disorders. [Formula 1] TIFF2026510355000540.tif56170

The present invention relates to novel 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as potent inhibitors of transforming growth factor-beta receptor I (also known as activin receptor-like kinase 5) (TGFβRI) / ALK5. Other objects of the present invention are to provide processes for preparing these compounds; pharmaceutical compositions comprising an effective amount of these compounds; the use of said compounds for the preparation of a medicament for the treatment of pathological conditions or diseases which can be ameliorated by the inhibition of transforming growth factor-beta receptor I (TGFβRI) / ALK5, such as respiratory diseases, including idiopathic pulmonary fibrosis, asthma, COPD and lung cancer and skin and ocular fibrotic disorders.

This invention relates to the solid form of propionic acid (1R,3S)-3-[3-({[3-(methoxymethyl)-1-methyl-1H-pyrazol-5-yl]carbonyl}amino)-1H-pyrazol-5-yl]cyclopentyl ester, pharmaceutical compositions comprising such solid forms, and the use of such solid forms and pharmaceutical compositions for the treatment of cancer.

The present invention relates to fungicidal mixtures comprising at least one substituted pyridyl / pyrazidyl dihydrobenzothiazepine compounds (compound I) and at least one active compound II in a weight ratio of from 100:1 to 1 :100; to a method for controlling phytopathogenic harmful fungi using mixtures of at least one compound I and at least one compound II in a weight ratio of from 100:1 to 1:100; to the use of mixtures comprising compounds I and compounds II for controlling phytopathogenic harmful fungi; to agrochemical compositions comprising these mixtures; and to agrochemical compositions further comprising seed.

The invention relates to a 4-hydroxy-5-(3-(4-methoxyphenyl)-5-methyl-1-phenyl-1H-pyrazol-4-yl) cyanobenzene compound and an application of the 4-hydroxy-5-(3-(4-methoxyphenyl)-5-methyl-1-phenyl-1H-pyrazol-4-yl) cyanobenzene compound in a medicine for treating diabetes mellitus. The compound as shown in the following formula (1) is obtained through virtual screening in combination with experimental verification, and the compound has remarkable alpha-glucosidase inhibitory activity. In-vitro and in-vivo experiments prove that the compound effectively reduces the generation of glucose and delays the digestion and decomposition of starch by inhibiting the activity of alpha-glucosidase. The invention discloses the compound and the application thereof in the field of preparation of anti-diabetic drugs for the first time, the alpha-glucosidase inhibitory activity of the compound is high, and a new direction is provided for development of diabetes treatment drugs. Formula (1) below

The present invention provides a process for the preparation of aminopyridazine derivatives, and novel pyridazine-based and pyrazole-based compounds which are useful as either starting materials or intermediates in said process.

A method for controlling phytopathogenic pests on cereals, wherein the pest, their habitat, breeding grounds, their locus or the plants to be protected against pest attack, the soil or plant propagation material are treated with an effective amount of a fungicidal mixture comprising, as active components, 1) 1-[2-[[1-(4-chlorophenyl)pyrazol-3-yl]oxymethyl]-3-methyl-phenyl]-4-methyl-tetrazol-5-one as compound I, and 2) one fungicidal compound II selected from [2, 2-bis(4-fluorophenyl)-1-methyl-ethyl]2-[(3-acetoxy-4-methoxy-pyridine-2-carbonyl)amino]propanoate (compound 11-1) and [(1S)-2,2-bis(4-fluorophenyl)-1-methyl-ethyl](2S)-2-[(3-acetoxy-4-methoxy-pyridine-2-carbonyl)amino]propanoate (compound II-2).

A 2-piperidyl or 2-pyrazolyl substituted pyrimidine compound, which is a compound represented by formula (I) or a pharmaceutically acceptable salt, an isotopic variant, a tautomer, a stereoisomer, a prodrug, a polymorph, a hydrate or a solvate thereof. A pharmaceutical composition comprising the compound, and a use of the pharmaceutical composition in the treatment of diseases mediated by an EGFR protein and mutants thereof.

The application discloses a nickel-based metal organic framework and a preparation method and detection application thereof. The nickel-based metal organic framework is formed by coordination of 2,6-bis(1H-pyrazol-1-yl) isonicotinic acid (H2BPIA) and nickel ions Ni(II). The H2BPIA and NiCl2·6H2O are prepared by a hydrothermal / solvothermal method in a water-acetonitrile mixed solvent, and the obtained nickel-based metal organic framework has high thermal stability and can be used for detection of marbofloxacin and has the advantages of high selectivity, strong anti-environmental interference capability and fast response speed.

Telomerase inhibitor compounds are provided. Some compounds contain a lactone or lactam group covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In other examples, a sulfonamide-containing moiety is covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In some embodiments, the telomerase inhibitor compounds have an amide moiety and a vinyl sulfonamide group bonded to an aromatic group. In other examples, the inhibitor compounds have an isothiazolidine 1,1-dioxide core bonded to a phenyl group. Aspects of the present invention also include pharmaceutical compositions containing the telomerase inhibitor compounds of the present invention, as well as methods for treating telomerase-related diseases or conditions.

The present invention relates to a methionine sulfoxide reductase B1 inhibitor and an anticancer composition comprising same. More specifically, the present invention relates to 4-[3-(4-ethylphenyl)-5-(4-hydroxyphenyl) -4,5-dihydro -1 H-pyrazol-1-yl]benzene-1-sulfonamide or 6-chloro-10-(4-ethylphenyl)-4-hydroxypyrimido[4,5-b]quinolin-2(10H)-one, which is a MsrB1 inhibitor, and an anticancer composition comprising same. The MsrB1 inhibitor of the present invention has been confirmed to inhibit differentiation into tumor-friendly M2 macrophages and to suppress tumor growth. In addition, the MsrB1 inhibitor of the present invention was found to exhibit anticancer effects through immune regulation within the tumor microenvironment, and thus can be usefully applied as a composition for cancer treatment.

The present disclosure relates to a process for the synthesis of a heterocyclic ketone compound, and in particular a 3'-substituted-3-hydroxy-(8-azabicyclo[3.2.1]oct-8-yl)-[5-(1 h-pyrazol-4-yl)-thiophen-3-yl]-methanone compound and azabicyclic intermediates thereof. In particular, the present disclosure also relates to a process for the synthesis of Xanamem. The present disclosure also relates to a process for the synthesis of optionally protected azabicyclic intermediate compounds. The present disclosure also relates to 3'-substituted-3-hydroxy-(8-azabicyclo[3.2.1]oct-8-yl)-[5-(1 h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds and azabicyclic intermediate compounds thereof.

This invention discloses a method for preparing and applying o-pyrazolylphenylacetone olefin derivatives. The method involves dispersing o-pyrazolylphenylpropenol compounds, aryl aldehyde compounds, and a catalyst in an organic solvent to react and obtain o-pyrazolylphenylacetone derivatives. The method for synthesizing o-pyrazolylphenylacetone derivatives of this invention has advantages such as inexpensive raw materials, simplicity and efficiency, mild reaction conditions, high atom economy, easy product purification, and green economy. The obtained products can be directly applied as potential drugs in the pharmaceutical field, showing broad application prospects.

The present disclosure relates to choline salts, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3- (trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment and prevention of a Retroviridae viral infection including an infection caused by the HIV virus.

The application belongs to the technical field of pest control, and discloses application of a nitrogen-containing heterocyclic compound in the prevention and treatment of apple snails. The application takes the arginine kinase of the apple snail as an action target, and screens out a nitrogen-containing heterocyclic compound with the activity of killing the apple snail, which is N-[4-(3,5-diphenyl-4,5-dihydro-1H-pyrazol-1-yl)benzyl]-N-(1-hexyl-1H-benzimidazol-2-yl)amine. The nitrogen-containing heterocyclic compound is prepared into a suspension agent or a granule as an active ingredient, and both of them have excellent killing effects on the apple snails. Compared with the existing arginine kinase inhibitor quercetin, the nitrogen-containing heterocyclic compound has higher activity, better selectivity, lower toxicity to vertebrates, and great application potential.

Provided herein are compounds and pharmaceutical compositions thereof for inhibiting emopamil binding protein (EBP), and the use of the compounds and pharmaceutical compositions thereof in the treatment of demyelinating diseases, such as multiple sclerosis.

The application discloses a pyrazolyl porous organic polymer loaded ruthenium nanocluster material and a preparation method and application thereof, relates to the field of nanometer material synthesis and the field of energy electrocatalysis technology. The pyrazolyl porous organic polymer (Pz-POP) material is prepared through a polycondensation reaction of 2,4,6-triformylphloroglucinol and 1H-pyrazole-3,5-diamine. Subsequently, the Pz-POP material loaded with ruthenium (Ru) nanoclusters (Ru@Pz-POP) is prepared by using a liquid phase sodium borohydride reduction method. The Pz-POP material synthesized by the application presents a nanowire morphology, the particle size of the Ru nanoclusters is about 2.5 nm, the preparation method is simple and the condition is mild, and the obtained Ru@Pz-POP material exhibits excellent electrocatalytic hydrogen evolution reaction performance and has a potential application prospect.