937263-71-3

Usage

Uses

Used in Pharmaceutical Industry:
4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylaniline is used as a potential therapeutic agent for the treatment of brain cancer. Its unique molecular structure allows it to interact with specific biological targets, such as receptors or enzymes, that play a role in the development and progression of brain tumors. By modulating these targets, the compound may help to inhibit tumor growth, reduce metastasis, and improve patient outcomes.
Additionally, 4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylaniline may also be utilized in the development of novel drug delivery systems, which could enhance its bioavailability, target specificity, and therapeutic efficacy. This could lead to the design of more effective treatments for brain cancer and other related conditions, ultimately improving patient care and quality of life.

Upstream product

• 99-53-6 2-methyl-4-nitrophenol 
• 65370-42-5 4-chloro-2-nitropyridine 
• 864244-98-4 4-(2-methyl-4-nitrophenoxy)pyridin-2-amine 
• 937263-44-0 7-(2-methyl-4-nitrophenoxy)-[1,2,4]triazolo[1,5-a] pyridine 
• 10201-73-7 2-amino-4-methoxypyridine 
• 53750-66-6 4-chloro-pyridine-2-carbonyl chloride 
• 98-98-6 2-Picolinic acid 
• 99586-65-9 4-chloropicolinamide 
• 2835-96-3 4-amino-2-methylphenol 
• 1427452-48-9 7-chloro-[1,2,4]triazolo[1,5-a]pyridine 
• 19798-80-2 2-Amino-4-chloropyridine 
• 455-88-9 5-nitro-2-fluorotoluene 
• 1033810-70-6 [1,2,4]triazolo[1,5-a]pyridin-7-ol 

Downstream Products

• 937263-43-9 tucatinib 

Relevant academic research and scientific papers

[1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS

The present invention relates to new [1,3]diazino[5,4-d]pyrimidines and derivatives of Formula (I), wherein the groups R1, R2, R3 and R4 have the meanings given in the claims and specification, their use as inhibitors of HER2 and its mutants, pharmaceutical compositions which contain such compounds and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

Preparation method of Tucatinib intermediate

The invention discloses a preparation method of a tucatinib intermediate, which comprises the following steps: firstly, reacting 4-chloropyrido-2-amine with N,N-dimethylformamide dimethyl acetal, and then adding hydroxylamine hydrochloride for reaction to

ALKYNYL QUINAZOLINE COMPOUNDS

The present disclosure relates to compounds of Formula (I'): and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the prevention or treatment of abnormal cell growth in mammals, especially humans.

PYRROLO[2,1-F][1,2,4]TRIAZINE DERIVATIVES SERVING AS SELECTIVE HER2 INHIBITORS AND APPLICATION THEREOF

The present invention relates to a group of pyrrolo[2, 1-f][1,2,4]triazine derivatives serving as selective HER2 inhibitors and an application thereof in the preparation of a drug that serves as an HER2 inhibitor. Specifically, the present invention relates to a compound represented by formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof.

[1,3]DIAZINO[5,4-D]PYRIMIDINES AS HER2 INHIBITORS

The present invention relates to new [1,3]diazino[5,4-d]pyrimidines and derivatives of Formula (I) wherein the groups R1, R2, R3 and R4 have the meanings given in the claims and specification, their use as inhibitors of HER2 and its mutants, pharmaceutical compositions which contain such compounds and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

Synthesis method of Tucatinib and intermediate product thereof

The invention discloses a synthesis method of Tucatinib, and the method comprises the following step: carrying out substitution reaction on halate of a compound shown in a formula VI or free alkali thereof serving as a raw material and a compound shown in a formula VII under an alkaline condition to obtain a compound shown in a formula VIII. The raw materials used in the whole synthesis route areeasy to obtain, expensive catalysts are not needed, and the method is suitable for large-scale production and beneficial to industrial production of the Tucatinib.

Preclinical activity of HER2-selective tyrosine kinase inhibitor tucatinib as a single agent or in combination with trastuzumab or docetaxel in solid tumor models

HER2 is a transmembrane tyrosine kinase receptor that mediates cell growth, differentiation, and survival. HER2 is overexpressed in approximately 20% of breast cancers and in subsets of gastric, colorectal, and esophageal cancers. Both antibody and smallm

NITROGENOUS HETEROCYCLIC COMPOUND, PREPARATION METHOD, INTERMEDIATE, COMPOSITION, AND APPLICATION

A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target. (I)

New Synthetic Route to Tucatinib

A new and improved synthetic route to tucatinib is described that involves three key intermediates. The first of these, 4-([1,2,4]triazolo[1,5- a ]pyridin-7-yloxy)-3-methylaniline, was prepared on a 100 g scale in 33percent yield over five steps and 99percent purity. Next, N 4 -(4-([1,2,4]triazolo[1,5- a ]pyridin-7-yloxy)-3-methylphenyl)quinazoline-4,6-diamine was isolated in 67percent yield over three steps and >99percent purity. Then, 4,4-dimethyl-2-(methylthio)-4,5-dihydrooxazole trifluoromethanesulfonate was prepared under mild conditions in 67percent yield over two steps. Finally, tucatinib was obtained in 17percent yield over nine steps and in >99percent purity (HPLC). Purification methods used to isolate the product and the intermediates involved in the route are also reported.