183 results about "Pyrazolopyrimidine" patented technology

Methods for treating immune thrombocytopenia 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.

Methods for treating patients with moderate-to-severe asthma comprising administering a therapeutically effective amount of 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.

There is provided a process for preparing 5,7-dimethyl-N-((1R,4R)-4- (pentyloxy)cyclohexyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide, said process comprising at least a step of amide coupling a 5,7-Dimethylpyrazolo[1,5-a]pyrimidine-3-carboxylic acid with trans-4-(pentyloxy)cyclohexanamine using carbonyldiimidazole (CDI).

Described herein are pharmaceutical formulations of 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 the Btk inhibitor, 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.

Disclosed herein are novel methods for preparing 2-[(3R)-2-[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, including various solvate forms and intermediates thereof. Also disclosed herein are novel solvate forms and intermediates of 2-[(3R)-2-[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.

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.

Methods for treating immune thrombocytopenia 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 (PRN1008) and pharmaceutically acceptable salts thereof are disclosed. Pharmaceutical compositions comprising at least one compound chosen from PRN1008 and pharmaceutically acceptable salts thereof are also disclosed.

Disclosed herein are novel formulations of 2-[(3R)-2-[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, including formulations including various solid forms thereof. Also disclosed are processes for preparing formulations of 2-[(3R)-2-[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.

The invention belongs to the technical field of medicine, and particularly relates to an NLRP3 inhibitor, a preparation method thereof and application of the NLRP3 inhibitor in medicine. The invention provides an NLRP3 inhibitor as shown in a formula (I) as well as a composition and application thereof. The NLRP3 inhibitor can be used for treating or preventing diseases or symptoms related to abnormal expression of an NLRP3 signal channel. # imgabs0 #

Compounds and salts thereof that are useful as JAK kinase inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.

A series of pyrazolopymidine derivatives, and use thereof in the preparation of a medicament for treating disease associated with FGFR and c-Met. The pyrazolopymidine derivative is a compound represented by formula (I), a tautomer, or a pharmaceutically acceptable salt thereof.

The application discloses application of a chiral tetrahydropyrazolo[1,5-a]pyrimidine derivative in preparation of an antitumor drug for treating HER2 positive colorectal cancer. Through in vitro and in vivo experiments, it is confirmed that the compound has a significant inhibitory effect on proliferation and migration of HER2 positive colorectal cancer cells, and shows antitumor activity. The application provides a new idea for developing a novel tyrosine kinase inhibitor for treating HER2 positive colorectal cancer in clinic.

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.

A substituted pyrazolo[1,5-a]pyrimidine-7-amine derivative having a structure as shown in formula (I) or a pharmaceutically acceptable salt, solvate, stereoisomer, prodrug, or pharmaceutical composition thereof. The derivative has significant CDK9 selective inhibitory activity. #imgabs0#

The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and pyrazolo[1,5-a]pyrimidine derivatives and / or pharmaceutically acceptable salts thereof, and the use of these derivatives as pharmaceutically active agents, particularly for the prevention and / or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases, and infectious diseases. Furthermore, the present invention relates to pharmaceutical compositions comprising at least one of the pyrazolo[1,5-a][1,3,5]triazine derivatives and pyrazolo[1,5-a]pyrimidine derivatives and / or pharmaceutically acceptable salts thereof.

Provided herein are formulations, processes, solid forms and methods of use relating to (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide.

The invention provides an aminomethylation reaction method based on a pyrazolo [1, 5-a] pyrimidine nitrogen-containing fused heterocycle substrate, a product and application, and belongs to the technical field of chemistry. Pyrazolo [1, 5-a] pyrimidine nitrogen-containing fused heterocycle, secondary amine and glyoxylic acid are used as raw materials, an aminomethylation reaction is achieved at the C3 site of pyrazolo [1, 5-a] pyrimidine through heating for the first time, a transition metal catalyst or a chemical oxidizing agent is not needed, the drug purification problem caused by metal residues and oxidation byproduct pollution are avoided, and the purity of the product is improved. The method is a novel efficient, simple, convenient and environment-friendly nitrogen-containing fused heterocyclic aromatic hydrocarbon functionalization strategy, the reaction can be directly carried out at the temperature of 100-120 DEG C, shielding gas does not need to be filled, and compared with some reactions needing high-temperature or high-pressure conditions, the mild reaction conditions are easier to control, side reactions are reduced, and the yield of the target product is increased. Meanwhile, the reaction conditions are also beneficial to reducing energy consumption, and conform to the concept of green chemistry.

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]

The invention belongs to the technical field of medicinal chemistry, and discloses application of pyrazolo [3, 4-d] pyrimidine-4-ketone derivatives with the following structure or pharmaceutically acceptable salts thereof in prevention or treatment of pain diseases, # imgabs0 # R1 represents a substituent group selected from hydrogen, halogen or alkyl; m is an integer of 3-5; n is an integer of 0-2; x is a carbon atom, an oxygen atom or a nitrogen atom; and R2 represents a substituent selected from hydrogen, phenyl, and substituted or unsubstituted alkyl.

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.

This disclosure relates to 1H-pyrazolo[3,4-d]pyrimidine ribonucleoside compounds of Formula (I) and pharmaceutically acceptable salts thereof, which activate LACTB and are useful for treating diseases or disorders, such as cancer.

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 provides pyrazolotriazine and pyrazolopyrimidine derivatives as well as a preparation method, a pharmaceutical composition and application thereof. Specifically, the invention provides pyrazolo [1, 5-a] [1, 3, 5] triazine and pyrazolo [1, 5-a] pyrimidine derivatives as shown in a general formula (I) and / or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and application of the derivatives as pharmaceutical active agents in drugs for preventing and / or treating diseases related to abnormal activity of CDKs, it is indicated that the compound has a good cell proliferation inhibition effect on solid tumors and hematologic tumors, and potential for treating related cancers and autoimmune diseases is achieved. # imgabs0 #

The present invention belongs to the technical field of drug synthesis, and in particular to a method for preparing ibrutinib. The present invention uses 3-bromo-1H-pyrazolo[3,4-D]pyrimidine-4-amine as a raw material, and reacts with 4-phenoxyphenylboronic acid under amine catalysis to obtain 4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine; 4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine is reacted with 1-[(S)-3-hydroxy-1-piperidinyl]-2-propylene-1-one under the catalysis of phosphine oxide to obtain ibrutinib through Mitsunobu reaction. This process uses amine catalysts instead of precious metal palladium to catalyze the Suzuki coupling reaction, which solves the problems of low yield and expensive catalysts in traditional reactions of this type. It uses phosphine oxide as a catalyst to catalyze the Mitsunobu reaction, avoiding the use of equivalent triphenylphosphine in the Mitsunobu reaction, and solves the harsh conditions of the reaction itself that require the acidity of the nucleophilic reagent. The process is simple to operate, and the target product obtained is of high purity, which is suitable for industrial production.

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