754219-11-9

Upstream product

• 108-69-0 3,5-dimethylaminoaniline 
• 38521-46-9 3-carboxy-2-mercaptopyridine 
• 97936-36-2 1,2-dihydro-2-thioxo-3-pyridinecarbonyl chloride 

Downstream Products

• 864494-46-2 2-(2-aminopyridin-4-ylmethylthio)-N-(3,5-dimethylphenyl)pyridine-3-carboxamide 

Relevant academic research and scientific papers

Pyridylmethylthio derivatives as VEGF inhibitors: Part 2

Optimization of compounds 5 and 6 led to the discovery of VEGF inhibitor 10g which reduced CYP inhibition. It was highly active in vitro (VEGF induced HUVEC proliferation assay) and showed efficacies in three disease models in vivo (cancer, RA, and AMD).

NOVEL CYCLIC COMPOUND HAVING PYRIMIDINYLALKYLTHIO GROUP

The present invention has its object to study synthesis of novel cyclic compounds having a pyrimidinylalkylthio group and to find pharmacological actions of the compounds. According to the present invention, a compound represented by the formula (1) or a

NOVEL CYCLIC COMPOUND HAVING 4-PYRIDYLALKYLTHIO GROUP HAVING (UN)SUBSTITUTED AMINO INTRODUCED THEREIN

A novel cyclic compound having a 4-pyridylalkylthio group having an (un) substituted amino group introduced therein or a salt thereof. They are useful as a medicine. The cyclic compound is a compound represented by the following formula (1), which is useful for the treatment of diseases in which angiogenesis participates. In the following formula (1), ring A represents a benzene ring or a 5- or 6-membered aromatic heterocycle optionally fused with a cycloalkane ring; B represents alkylene; R1 and R2 each represents H, (substituted) aryl, (substituted) heterocyclic group, etc.; R3 and R4 each represents H; (substituted) alkyl, (substituted) cycloalkyl, -Z-R5, etc.; R5 represents (substituted) alkyl, (substituted) aryl, (substituted) heterocyclic group, etc.; X and Y each represents H, etc.; Z represents -CO-, -COO-, -CONR 6- -SO2-, etc.; R6 represents H, etc.; p is 0, 1, or 2; and q is 0 or 1.

NOVEL COMPOUND HAVING 4-PYRIDYLALKYLTHIO GROUP AS SUBSTITUENT

A subject of the present invention is to provide a novel aromatic five- or six-memberd heterocyclic derivative having 4-pyridylalkylthio as a substituent or a salt thereof which is useful as a pharmaceutical. Compound represented by the following general formula [I] or salts thereof are useful as therapeutic agents for diseases in which angiogenesis or augmentation of vascular permeability is involved. In the formula, ring "A" is a benzene ring or an aromatic five- or six-memberd heterocycle which can be fused with a cycloalkane ring, "B" is alkylene, R1 and R2, the same or different, are H, OH, substituted or unsubstituted alkoxy and the like, X and Y, the same or different, are group(s) selected from H, halogen, OH, substituted or unsubstituted alkoxy and the like respectively, p is 0, 1 or 2, and q is 0 or 1.