293 results about "Pyrazolylchalcone" patented technology

This invention relates to a crystalline 19-nor C3,3-disubstituted C21-pyrazolyl steroid of Formula (I),and compositions thereof. Also disclosed herein are methods of making the same and methods of using the same.

The invention discloses an anthraquinone-based MOF photocatalytic material as well as a preparation method and application thereof. The anthraquinone-based MOF photocatalytic material is prepared by carrying out solvothermal reaction on a ligand DPAq and a nickel source in a mixed solvent, wherein the ligand DPAq is 2, 6-bis (pyrazol-4-yl)-9, 10 anthraquinone, and the mixed solvent is a composition of N, N-dimethylformamide and water. The anthraquinone-based MOF photocatalytic material shows an appropriate band gap and good ROS generation efficiency and shows excellent catalytic activity and selectivity when applied to benzylamine coupling reaction, the reaction selectivity reaches 100%, the product yield can reach 97%, and the catalytic reaction efficiency is high; the product can be recycled, and the yield of the product can still reach 92% after the product is recycled for 5 times.

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 a 4 (1H-pyrazol-3-yl) piperidinyl derivative, the structural formula of the 4 (1H-pyrazol-3-yl) piperidinyl derivative is shown as a formula I, # imgabs0 #, R1 is an aromatic ring or a substituted aromatic ring, the substituted aromatic ring is a substituent group on the aromatic ring, and R2 is a hydrogen atom or a hydrogen atom or a substituent group on the substituted aromatic ring, so that the structural formula of the 4 (1H-pyrazol-3-yl) piperidinyl derivative is shown as a formula I; the substituent groups are selected from C1-C6 alkyl groups, C1-C6 halogenated alkyl groups, C1-C6 alkylamino groups, C1-C6 alkoxy groups, five-membered to six-membered heterocyclic groups, halogen, hydroxyl groups, cyano groups, nitryl groups, amino groups and carbonyl substituted five-membered to six-membered heterocyclic groups containing 1-2 nitrogen atoms; and R2 is H or a C1-C6 alkyl group. The 4 (1H-pyrazol-3-yl) piperidinyl derivative has MNK1 and / or MNK2 inhibitory activity, and has anti-cancer and anti-inflammatory activity; the invention also provides a preparation method of the 4 (1H-pyrazol-3-yl) piperidinyl derivative, an application of the 4 (1H-pyrazol-3-yl) piperidinyl derivative in preparation of MNK1 and / or MNK2 inhibitors, and an application of the 4 (1H-pyrazol-3-yl) piperidinyl derivative in preparation of anti-inflammatory and anti-cancer drugs.

The invention relates to a deuterated pyrazolyl formamide compound as well as a preparation method and application thereof. Specifically, the compound has a structure as shown in a formula I, and has a more excellent bactericidal effect and an effect of increasing the yield. # imgabs0 #

The present invention provides a pharmaceutical composition containing Compound 1, which has excellent disintegrability and bioavailability. The present invention relates to a pharmaceutical composition comprising: a granulated material containing 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo [3, 4-b] pyridin-1-yl} benzamide or a pharmaceutically acceptable salt thereof, and a crystalline cellulose, the granulated material being characterized in that: the granulated material contains a compound represented by general formula (1); the pharmaceutical composition has a disintegration time within 360 seconds in a coated tablet state.

Provided herein are optionally substituted pyrazolylacetamides, pharmaceutical compositions comprising a therapeutically effective amount of such compounds and a pharmaceutically acceptable excipient, and methods of treating diseases or disorders, such as, epilepsy, amyotrophic lateral sclerosis, various types of pain, hyperexcitability, a dyskinesia, dystonia, mania, tinnitus, neurodevelopmental diseases or disorders, a smooth muscle contractility disorder, Dravet syndrome, posttraumatic stress disorder (PTSD), with such compounds and pharmaceutical compositions.

The invention discloses 4-(1H-pyrazol-4-yl) pyridine derivatives targeting a gram-negative bacteria lipoprotein transport pathway, a composition and application of the 4-(1H-pyrazol-4-yl) pyridine derivatives and belongs to the technical field of chemical medicines. The invention provides 4-(1H-pyrazol-4-yl)-2, 6-dimethyl pyridine and 4-(1H-pyrazol-4-yl) pyridine derivatives with the following structures: # imgabs0 #, the compounds can target a key protein machine of Gram's inner and outer membranes, and have remarkable antibacterial activity; meanwhile, the polypeptide can target key protein machines of gram inner and outer membranes, has good affinity with target protein LolCDE, and provides a new way for specific antibacterial treatment of gram-negative bacteria.

The invention discloses a preparation method and application of a reactive flame retardant containing double DOPO groups and nitrogen heterocycles, and the preparation method of the reactive flame retardant comprises the following steps: adding an amino compound R-NH2 and terephthalaldehyde into a reactor with a stirring device, adding a solvent, adding an acid to adjust the pH value to 6, then heating until the solvent is refluxed, keeping the refluxing temperature to react for a period of time, and cooling to room temperature to obtain the reactive flame retardant containing double DOPO groups and nitrogen heterocycles. Reaction liquid containing an imine intermediate product is obtained; then adding DOPO, controlling the reaction temperature to be the solvent reflux temperature, and keeping the reflux temperature to react for a period of time; after the reaction is finished, cooling, carrying out suction filtration, washing and drying to obtain a reaction type flame retardant containing double DOPO groups and nitrogen heterocyclic rings; the reaction formula is as follows: # imgabs0 # amino compound R-NH2 is 4-aminopyridine or 3-aminopyrazole, namely R is pyridyl or pyrazolyl. The synthesis and purification method of the flame retardant is simple, the reaction yield is high, and the flame retardant effect of epoxy resin can be remarkably improved by adding the flame retardant into bisphenol A epoxy resin through modification.

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.

The invention belongs to the field of environmental protection, and discloses a method for synthesizing a metal organic framework material by a water-phase one-pot method. The method comprises the following steps: mixing a pyrazolyl derivative containing an amino group or an aldehyde group, a linker containing the aldehyde group or the amino group, a copper salt and pyruvic acid, adding an acid solution of water into the mixture, and performing ultrasonic treatment or stirring at room temperature to obtain the high-crystalline-state metal organic framework material, the dosage of the pyruvic acid being 0 or not 0; when the pyrazolyl derivative containing the amino group is selected as the raw material, the corresponding linker is a linker containing an aldehyde group; when a pyrazolyl derivative containing an aldehyde group is selected as a raw material, a corresponding linker containing an amino group is selected. When the water-phase one-pot synthesis method provided by the invention is used for preparing the metal organic framework material, the use of an organic solvent is eliminated, so that the influence on the environment is greatly reduced. Meanwhile, batch amplification synthesis can be achieved, repeatability is good, the synthesis process is simple, operability is high, and wide application prospects are achieved.

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.

Provided is a method of treating malignant tumor by an azabicyclic compound, particularly, with eye disorder reduced. The present invention provides a method for treating malignant tumor, comprising administering an effective amount of 3-ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide (compound 1) or a salt thereof to a patient in need thereof according to a dosing regimen, wherein the dosing regimen comprises administering the compound 1 or the salt thereof at a dose from 40 mg / body / day to 240 mg / body / day in terms of the amount of the compound 1 for consecutive days, and then providing a withdrawal period of at least 2 days.

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.

Provided herein is a method of preventing or treating an immune disorder, autoimmune disorder or an inflammatory condition in a person in need thereof, comprising administering to the person a therapeutically effective amount of an LDH inhibitor. Specifically, provided herein are substituted pyrazolyl compounds as Lactate dehydrogenase A (LDHA) inhibitors, methods and uses of the LDHA inhibitors and / or a pharmaceutically acceptable salt thereof in preventing or treating an immune disorder, an inflammatory condition, or a fibrosis disease.

Provided herein are high strength / high drug load tablets comprising 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (“Compound 1”), dispersible tablets comprising Compound 1, processes of manufacturing such tablets, and methods for treating patients with the tablets. Compound 1 is useful for treating hematological disorders such as sickle cell disease, pulmonary disease such as idiopathic pulmonary fibrosis, and hypoxia and hypoxemia conditions.

The invention relates to a compound of formula (I)which is 6-((1H-pyrazol-4-yl)sulfonyl)-2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one; or a salt and / or solvate thereof;and to its use in treating or preventing an inflammatory disease, a disease associated with an undesirable immune response, cancer, obesity, a diabetic disease or a blood disorder.

The invention belongs to the technical field of pest control, and discloses application of a nitrogen-containing heterocyclic compound in control of ampullaria gigas. According to the invention, a nitrogen-containing heterocyclic compound with the activity of killing ampullaria gigas is screened by taking ampullaria gigas arginine kinase as an action target, and the nitrogen-containing heterocyclic compound is N-[4-(3, 5-diphenyl-4, 5-dihydro-1H-pyrazole-1-yl) benzyl]-N-(1-hexyl-1H-benzimidazole-2-yl) amine. The nitrogen-containing heterocyclic compound is used as an active component to be prepared into a suspending agent or a granule, the suspending agent or the granule has an excellent killing effect on ampullaria gigas, and compared with an existing arginine kinase inhibitor quercetin, the nitrogen-containing heterocyclic compound is higher in activity, good in selectivity, low in toxicity to vertebrates and huge in application potential.

Provided herein are optionally substituted pyrazolylacetamides, pharmaceutical compositions comprising a therapeutically effective amount of such compounds and a pharmaceutically acceptable excipient, and methods of treating diseases or disorders, such as, epilepsy, amyotrophic lateral sclerosis, various types of pain, hyperexcitability, a dyskinesia, dystonia, mania, tinnitus, neurodevelopmental diseases or disorders, a smooth muscle contractility disorder, Dravet syndrome, posttraumatic stress disorder (PTSD), with such compounds and pharmaceutical compositions.

The invention discloses a preparation method of a pyrazol type metal Salen-based MOF (Metal Organic Framework) material. The preparation method comprises the following steps: chelating a pyrazol functionalized Salen ligand with cobalt salt, nickel salt, copper salt and iron salt to generate corresponding M-pyrazol Salen; dispersing and dissolving the obtained M-pyrazolyl Salen and Zn (OAc) 2.2 H2O by using a mixed solution of an organic solvent and H2O; and carrying out hydrothermal reaction on the obtained mixed solution, washing and drying to obtain the M-SalenMOFs. The pyrazole type metal Salen-based MOF synthesized by the invention is novel and unique in structure, easy to regulate and control and high in stability, and has good stability under a strong alkaline condition; the obtained M-SalenMOFs can flexibly change the ligand center metal so as to realize different catalysis.

The invention discloses a micron-level block-shaped stable tri-metal MOF oxygen evolution catalyst and a preparation method and application thereof.The preparation method of the catalyst comprises the steps that pyrazolyl Salen and nickel salt are stirred in methyl alcohol at the normal temperature to react overnight, after the reaction is finished, sediment is obtained through filtering and washed, then methyl alcohol pulping treatment is conducted, finally vacuum drying is conducted, Ni-pyrazolyl Salen is obtained, and the micron-level block-shaped stable tri-metal MOF oxygen evolution catalyst is obtained. The preparation method comprises the following steps: dispersing Ni-pyrazolyl Salen obtained from # imgabs0 # and Zn salt in a reaction solvent, reacting at 100-140 DEG C for 60-80 hours, precipitating, washing, drying, and carrying out ion exchange reaction with bivalent Fe salt, thereby finishing the preparation. The catalyst is used for water electrolysis under a strong alkali condition, has good oxygen evolution performance and electrochemical stability, and is superior to a commercial RuO2 catalyst and most original MOF oxygen evolution catalysts.

The invention relates to a 2N type manganese complex and a preparation method thereof, and a preparation method of phenylalkyl disiloxane. The invention discloses a 2N-type manganese complex and a preparation method thereof, and the preparation method comprises the following steps: (1) adding 2-bromo-pyridine, a ligand, potassium carbonate and cuprous iodide into a dimethyl sulfoxide solution, and reacting at 110-130 DEG C for 20-28 hours to obtain an N, N bidentate ligand; the ligand is 1-(pyridine-2-yl)-1H-indole, or 2-(1H-pyrazole-1-yl) pyridine, or 2-(2H-1, 2, 3-triazole-2-yl) pyridine, and the ligand is one or more of 1-(pyridine-2-yl)-1H-indole, 2-(1H-pyrazole-1-yl) pyridine, 2-(2H-1, 2 And (2) dissolving the N, N bidentate ligand and Mn (CO) 5Br in a tetrahydrofuran solution, and reacting at 65-75 DEG C for 10-14 hours to obtain the 2N type manganese complex. According to the 2N-type manganese complex, the preparation method thereof and the preparation method of the phenyl alkyl disiloxane, the 2N-type manganese complex is used as a catalyst for hydrosilylation reaction of pentamethyldisiloxane, styrene and derivatives thereof to prepare the phenyl alkyl disiloxane.

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 to a pharmaceutically acceptable salt of a 3, 4-dihydro-2H-chromene [8, 7-d] isoxazole derivative, and a crystalline form thereof. Specifically, the invention provides a pharmaceutically acceptable salt of N-(5-((1H-pyrazol-1-yl) methyl)-3, 4-dihydro-2H-chromene [8, 7-d] isoxazol-9-yl)-2-methoxybenzenesulfonamide, a crystal form and a preparation method thereof, and the corresponding salt has good stability and can be better used for clinical treatment.

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 relates to a series of novel pyrazolylmethylurea derivatives, and the use thereof for the inhibition of capsid assembly and the prevention or treatment of viral diseases through the inhibition.

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.