264123-70-8

Usage

InChI:InChI=1/C6H4Cl3N/c7-1-4-5(8)2-10-3-6(4)9/h2-3H,1H2

Upstream product

• 159783-46-7 3,5-dichloro-4-hydroxymethylpyridine 
• 136590-83-5 3,5-dichloropyridine-4-carboxaldehyde 
• 13958-93-5 3,5-dichloropyridine-4-carboxylic acid 

Downstream Products

• 1064677-00-4 N-(3,5-dichloro-4-chloromethyl-pyridin-2-yl)-N-methyl-acetamide 

Relevant academic research and scientific papers

Compound with kinase inhibition activity and its preparation method and use

The invention discloses a compound shown in the general formula I or its pharmaceutically acceptable salt, enantiomer, diastereomer or raceme, and a preparation method and pharmacal use thereof. All groups are defined in the patent specification. The comp

Novel small molecule bradykinin B2 receptor antagonists

Blockade of the bradykinin B2 receptor provides therapeutic benefit in hereditary angioedema (HAE) and potentially in many other diseases. Herein, we describe the development of highly potent B2 receptor antagonists with a molecular weight of approximately 500 g/mol. First, known quinoline-based B2 receptor antagonists were stripped down to their shared core motif 53, which turned out to be the minimum pharmacophore. Targeted modifications of 53 resulted in the highly water-soluble lead compound 8a. Extensive exploration of its structure-activity relationship resulted in a series of highly potent B2 receptor antagonists, featuring a hydrogen bond accepting functionality, which presumably interacts with the side chain of Asn-107 of the B2 receptor. Optimization of the microsomal stability and cytochrome P450 inhibition eventually led to the discovery of the highly potent and orally available B2 receptor antagonist 52e (JSM10292), which showed the best overall properties.

8-OXY-QUINOLINE DERIVATIVES AS BRADYKININ B2 RECEPTOR MODULATORS

The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.

TRIAZOLOTRIAZINES AND PYRAZOLOTRIAZINES AND METHODS OF MAKING AND USING THE SAME

The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson’s disease. In one embodiment, the invention features a compound of formula I: (I)