59 results about "Pyrazolopyrimidine" patented technology

Methods for treating patients with wAIHA comprising administering at least one compound chosen from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (rilzabrutinib) and pharmaceutically acceptable salts thereof are disclosed.

The present invention relates to a pharmaceutical composition for preventing or treating tumors, which contains a novel pyrazolopyrimidine compound or a pharma- ceutical acceptable salt thereof as an active ingredient, and which can be usefully used as a composition for preventing or treating cancer by administering it in combination with other anticancer agents.

The invention discloses a pyrazolo [1, 5-alpha] pyrimidine compound as well as a synthesis method and application thereof, the structural general formula of the pyrazolo [1, 5-alpha] pyrimidine compound is shown in the specification, R is 4-NO2-Ph-, 3-NO2-Ph-, 2-NO2-Ph-, 3-F-Ph-or 4-F-Ph-, and the invention also specifically discloses a pyrazolo [1, 5-alpha] pyrimidine compound as well as a preparation method and application of the pyrazolo [1, 5-alpha] pyrimidine compound. The invention relates to a synthesis method of a [1, 2, 5-alpha] pyrimidine compound and application of the compound in preparation of medicines for preventing or / and treating liver cancer. The pyrazol [1, 5, a] pyrimidine compound synthesized by the invention has a good inhibition effect on liver cancer HepG2 cells, the antitumor activity of the pyrazol [1, 5, a] pyrimidine compound in the liver cancer HepG2 cells is superior to that of a positive control drug CX-4945 and a compound I-1, and particularly, compounds I-2 and I-5 have excellent liver cancer HepG2 cell proliferation inhibition performance.

The present invention provides a compound of formula (I), or a pharmaceutically acceptable salt thereof, for the treatment of diseases, disorders or conditions associated with NLRP3, including diseases, disorders or conditions associated with heterozygous gain-of-function mutations in the NLRP3 gene, such as cryopyrin-associated periodic syndromes (CAPS). JPEG2026514121000054.jpg2770[wherein L, X, Y, R 7 , 8 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined in the specification]

A method for treating pruritus in patients with atopic dermatitis (AD) and / or nodular prurigo (PN) is disclosed, comprising administering a therapeutically effective amount of at least one compound selected from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-carbonyl]-4-methyl-4-[4-(oxecyclobutane-3-yl)piperazin-1-yl]pent-2-enonitrile (rezabrutinib) and pharmaceutically acceptable salts thereof.

The present disclosure relates to antibody-drug conjugates, wherein the drug is a pyrazolo[1,5-a][1,3,5]triazine derivative or a pyrazolo[1,5-a]pyrimidine derivative. In particular, the drug may be a 2-substituted 8-halogeno-N4-(4-(pyridine-2-yl)benzyl)pyrazolo[1,5-a][1,3,5]triazine-2,4-diamine. Such antibody-drug conjugates are particularly useful in treating proliferative diseases, including cancer.

The invention relates to pyrazolo [3, 4-d] pyrimidine-hydroxamic acid derivatives as well as a synthesis method and application thereof. The pyrazolo [3, 4-d] pyrimidine-hydroxamic acid derivatives have structural general formulas I and II. The pyrazolo [3, 4-d] pyrimidine-hydroxamic acid derivative disclosed by the invention shows remarkable inhibitory activity on phosphatidylinositol-3-kinase and histone deacetylase. The pyrazolo [3, 4-d] pyrimidine-hydroxamic acid derivative disclosed by the invention can be used as a phosphatidylinositol-3-kinase / histone deacetylase double-target inhibitor, and is used for preparing medicines for treating various malignant tumors jointly mediated by phosphatidylinositol-3-kinase and histone deacetylase.

The invention relates to a pharmaceutical formula of a Bruton's tyrosine kinase inhibitor. Described herein are pharmaceutical formulations of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo [3, 4-d] pyrimidin-1-yl) piperidin-1-yl) prop-2-en-1-one. Also disclosed are methods of using Btk inhibitors, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

To provide a new compound useful for treatment, prevention and / or diagnosis of seizure or the like in diseases accompanied by epileptic seizure or convulsive seizure (including multidrug-resistant seizure, intractable seizure, acute symptomatic seizure, febrile seizure and status epilepticus).SOLUTION: There are provided a compound represented by formula [I] and a salt thereof. Ring C is selected from pyridazine, pyrimidine, indole, pyrrolopyridine, indazole, pyrazolopyridine, imidazopyridine, imidazopyrazine, imidazopyridazine, triazolopyridine, pyrazolopyrimidine, imidazopyrimidine, triazolopyrimidine, isoquinoline, naphthyridine, quinazoline, quinoxaline, benzodioxole, oxazine, oxazepine, benzothiazole, and triazolopyridazine, with the proviso that pyrimidine-2, 4-dione and dihydropyrimidine-2, 4-dione are excluded.SELECTED DRAWING: None

To provide a crystal of 2 - (4-acetylbenzyl) - 3 - ((4-fluorophenyl) amino) - 577 - trimethyl-7, 8-dihydro-pyrazolo-imidazo [1, 2-a] 2H [4, 3-e] pyrimidin-4 (5H) - one.SOLUTION: Provided is a crystal of an acid addition salt form selected from, for example, succinate form, citrate form, adipate form, tartrate form (e.g., L-tartrate form), malate form, gluconate form (e.g., D-gluconate form), maleate form, fumarate form, aspartate form (e.g., L-aspartate form), hippurate form, sebacate form, glycolate form, galactarate form, benzoate form, pamoate form, oxalate form and malonate form.SELECTED DRAWING: None

The present invention provides a crystalline form Form I of a pyrazolopyrimidine ester compound of the structure of formula (I)This crystalline form has been characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). The present invention also provides methods of preparing the crystalline form Form I of the pyrazolopyrimidine ester compound. This crystalline form allows long-term storage without special requirements in respect of temperature, light, humidity or oxygen presence and is significantly advantageous in terms of stability. Moreover, the methods involve simple steps and provide good reproducibility and excellent purity. Therefore, they have a promising prospect of extensive application.

The invention provides a silicon dioxide and amorphous indium tin oxide selective etching solution. The silicon dioxide and amorphous indium tin oxide selective etching solution comprises an alcohol substance, a fluorine-containing substance, a corrosion inhibitor, a surfactant and the balance of water. The alcohol is one or a combination of more of ethylene glycol, polyethylene glycol, glycerol, isooctanol or isopropanol. The fluorine-containing substance is one or a combination of more of hydrofluoric acid, ammonium fluoride or ammonium bifluoride. The etching inhibitor is one or a combination of more of N, N-diisopropylethylamine, 2-hexylbenzimidazole, hydroxyethylidene-1, 1-diphosphonic acid, 5-oxo-4, 5-dihydropyrazolo [1, 5-a] pyrimidine-3-formonitrile or 5-chloro-[1, 2, 4] triazolo [1, 5-a] pyrimidine. The surfactant is one or a combination of more of polyethylene glycol mono-p-tert-octylphenyl ether, polyethylene glycol-propylene glycol monobutyl ether or coconut oil fatty acid diethanolamide. The etching solution can quickly remove a silicon dioxide deposition layer on the premise that the etching rate of amorphous indium tin oxide is smaller than or equal to 0.03 nm / min, the etched surface of silicon dioxide is smooth after etching, and etching of silicon dioxide and amorphous indium tin oxide has a high selection ratio.

The present invention relates to a novel pyrazolopyrimidine compound, its composition, its preparation method, and its use as an anticancer agent due to its antitumor activity. The novel pyrazolopyrimidine compound has the following general formula (I), and as an ATR inhibitor, it has excellent tumor inhibitory activity, high selectivity, good water solubility, low toxicity, and is applicable to oral or intravenous administration. TIFF2025503771000083.tif36170

The invention belongs to the technical field of pesticides, and particularly relates to a pyridyl-substituted triazole ring compound as well as a composition and application thereof. The compound is shown as a general formula I, wherein Y1 represents O or N-Y3; y2 represents an alkyl group, a haloalkyl group, an alkenyl group, a haloalkenyl group, or the like; y3 each independently represents hydrogen, an alkyl group, a haloalkyl group, or the like; m1 and M2 respectively and independently represent N or CX4; r1, R3, R4, R5, X1, X3, and X4 each independently represent hydrogen, cyano, nitro, halogen, alkyl, alkenyl, or the like; r2 represents a halogenated alkyl group; and X2 represents a halogenated alkoxy group. The compound has excellent prevention and treatment effects on spodoptera frugiperda, armyworm, prodenia litura and the like.

The invention discloses an energetic compound based on pyrazolo [1, 5-a] pyrimidine and a synthesis method of the energetic compound. The synthesis method comprises the following steps: (1) reacting 2-oxime ethyl cyanoacetate, potassium permanganate and potassium hydroxide to prepare potassium salt of 2-cyano-2-nitroethyl acetate; (2) enabling the potassium salt of the 2-cyano-2-nitroethyl acetate to react with hydrazine hydrate, so as to prepare 5-amino-4-nitro-1, 2-dihydro-3-pyrazolone; and (3) carrying out a reaction on the 5-amino-4-nitro-1, 2-dihydro-3-pyrazolone, potassium permanganate and potassium hydroxide, so as to prepare the potassium salt of the 5-hydroxy-3, 6-dinitropyrazolo [1, 5-a] pyrimidine-2, 7 (1H, 4H)-diketone. The synthesis process is mild in condition and high in safety, the raw materials are easy to prepare, the product yield is high, and the synthesized energetic compound has good detonation performance and low sensitivity and has potential application value in the field of energetic materials.

The present application relates to compounds of formula (A), wherein R1 is selected from formula (II) and formula (III) and R2 is selected from formula (IV), formula (V) and formula (VI), as IRAK4 inhibitors for use in methods of treating, for example, asthma and chronic obstructive pulmonary disease (COPD), cancer, inflammatory diseases and autoinflammatory / autoimmune diseases such as systemic lupus erythematosus, rheumatoid arthritis, myositis, Sjogren's syndrome, systemic sclerosis, gout, endometriosis, atopic dermatitis and psoriasis. Preferred compounds of the present application are, for example: N-(imidazo[l,2-b]pyridazin-3-yl)-l-cyclohexyl-2H-indazole-5-carboxamide, N-(pyrazolo[l,5-a]pyrimidin-3-yl)-l-cyclohexyl-2H-indazole-5-carboxamide, N-(imidazo[l,2-b]pyridazin-3-yl)-l-azaspiro[4.5]dec-8-yl-2H-indazole-5-carboxamide and N-(pyrazolo[l,5-a]pyrimidin-3-yl)-l-azaspiro[4.5]dec-8-yl-2H-indazole-5-carboxamide derivatives. An exemplary compound of the present application is, for example: N-(imidazo[l,2-b]pyridazin-3-yl)-6-methoxy-2-((5r,8r)-l-methyl-2-oxo-l-azaspiro[4.5]dec-8-yl)-2H-indazole-5-carboxamide (Example 1): formula (VII).

The present invention provides compounds having NF - κ B-inducing kinase inhibitory activity.SOLUTION: The present invention provides a compound of the following formula [I] or a pharmaceutically acceptable salt thereof.SELECTED DRAWING: None

Disclosed herein are methods for treating pemphigus in a human patient in need thereof comprising administering to the human patient a dose of at least 400 mg of (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (PRN1008) once a day (QD) or twice a day (BID).

The present invention provides a compound having NF-κB-inducing kinase inhibitory activity. The present invention provides the compound in formula [I] and a pharmaceutically acceptable salt thereof.

The application discloses a preparation method of a 7-position-hydrogen-substituted pyrazolo[1,5-a]pyrimidine compound. The preparation method comprises the following steps: contacting a compound shown in a formula (I) with a compound shown in one of formula (II) or formula (III), a thiocyanate, an iodine-containing oxidant and a solvent to react. The preparation method has the characteristics of simple operation, low cost of raw materials, wide application range of substrates and high yield, and the obtained product is an important pharmaceutical intermediate.

A pyrazolopyrimidinone compound of formula I: (I), a method for inhibiting a Wee1A kinase or both a Wee1A kinase and a Myt1 kinase.

The invention discloses a benzofuro [3, 2-d] pyrazolo [1, 5-a] pyrimidine compound as well as a synthesis method and application thereof, and relates to the technical field of organic synthesis and medicinal chemistry, the synthesis method of the compound comprises the following steps: in the presence of a catalyst and alkali, mixing a salicylaldehyde compound, a terminal alkyne compound and an alpha-aminoazole compound in a solvent for reaction, and separating to obtain the benzofuro [3, 2-d] pyrazolo [1, 5-a] pyrimidine compound. The benzofuro [3, 2-d] pyrazolo [1, 5-a] pyrimidine compound is obtained through the reaction. The furo [3, 2-d] pyrimidine compound is prepared by taking a salicylaldehyde compound, a terminal alkyne compound and an alpha-aminoazole compound as initial raw materials through a one-pot method, the reaction condition is mild, the raw materials are cheap and easy to obtain, the operation is simple and convenient, the production cost can be greatly reduced, and the production efficiency is improved; the furo [3, 2-d] pyrimidine compound has remarkable antifungal activity on plant pathogenic fungi, and can be applied to inhibition of fungi such as apple black beetle fungus and rhizoctonia solani.

The invention belongs to the technical field of pesticides, and particularly relates to a substituted imidazole ring compound as well as a composition and application thereof. The compound is shown as a general formula I, wherein Q1 and Q2 respectively and independently represent CH, C-halogen or N; x represents fluorine; y represents alkyl; r1 represents hydrogen, halogen, alkyl, alkenyl or the like; r2 represents hydrogen, an alkyl group, an alkenyl group, an alkynyl group or the like; the compound has excellent prevention and treatment effects on spodoptera frugiperda, armyworms and the like.

A method for treating patients with moderate to severe asthma is disclosed, comprising administering a therapeutically effective amount of at least one compound selected from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-carbonyl]-4-methyl-4-[4-(oxocyclobutane-3-yl)piperazin-1-yl]pent-2-enonitrile (rizabrutinib) and pharmaceutically acceptable salts thereof.

The present invention provides a crystalline form Form II of a pyrazolopyrimidine ester compound of the structure of formula (I)This crystalline form has been characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and infrared (IR) spectroscopy. The present invention also provides a method of preparing the crystalline form Form II of the pyrazolopyrimidine ester compound. This crystalline form allows long-term storage without special requirements in respect of temperature, light, humidity or oxygen level and is significantly advantageous in terms of stability. Moreover, the method involves simple steps and provides good reproducibility and excellent purity. It has a promising prospect of extensive application.

The application relates to pharmaceutically acceptable salts and polymorphs of substituted pyrazolo[1,5-a]pyrimidin-7-amine derivatives as shown in formula (I), pharmaceutical compositions containing the same, methods of preparation, and use of the pharmaceutically acceptable salts and polymorphs in the treatment or prevention of diseases associated with or mediated by CDK9 activity.