91591-69-4

Usage

Chemical Properties

Light yellow powder

InChI:InChI=1/C7H6ClNO/c1-5-2-3-6(4-10)7(8)9-5/h2-4H,1H3

Upstream product

• 18368-63-3 6-chloro-2-picoline 
• 68-12-2 N,N-dimethyl-formamide 
• 30529-70-5 2-chloro-6-methyl nicotinic acid 
• 109-94-4 formic acid ethyl ester 
• 4241-27-4 1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile 
• 28900-10-9 2-chloro-6-methylnicotinonitrile 
• 1057667-23-8 2-chloro-N-methoxy-N,6-dimethylpyridine-3-carboxyamide 

Downstream Products

• 1352396-72-5 3-iodine-6-methyl-1H-pyrazolo[3,4-b]pyridine 

Relevant academic research and scientific papers

Site-Selective γ-C(sp3)?H and γ-C(sp2)?H Arylation of Free Amino Esters Promoted by a Catalytic Transient Directing Group

The first selective PdII-catalysed γ-C(sp3)?H and γ-C(sp2)?H arylation of free amino esters using a commercially available catalytic transient directing group. A variety of free amino esters, including α-amino esters and β-amino esters, amino monoesters and amino bis-esters, are shown to react with a diverse range of simple aryl and heteroaryl iodide reagents.

KINASE INHIBITOR

[Problem] To provide a novel PIM-3 inhibitor and a novel cancer therapeutic drug, in particular, a therapeutic drug for pancreatic cancer. [Solution] A PIM-3 kinase inhibitor comprising a compound represented by general formula (I) or a pharmacologically acceptable salt, hydrate or solvate thereof.

PYRROLOPYRAZINE KINASE INHIBITORS

The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

NOVEL PYRIMIDINE COMPOUNDS HAVING BENZYL (HETEROCYCLIC METHYL) AMINE STRUCTURE AND MEDICAMENT COMPRISING THE SAME

A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halogen atom, a lower alkyl group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7 and R8 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group and the like, R9 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, R10 and R11 represent hydrogen atom, a lower alkyl group, a lower alkoxy group, a halo(lower alkyl) group and the like, and A represents a heterocyclic ring constituted by 6 to 10 atoms, which has potent inhibitory activity on cholesterol ester transfer protein (CETP).

Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor

Benzylamine and pyridinemethylamine derivatives were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC4R). These compounds were also profiled in rodents for their pharmacokinetic properties. Two compounds with diversified profiles in chemical structure, pharmacological activities, and pharmacokinetics, 10 and 12b, showed efficacy in an established murine cachexia model. For example, 12b had a Ki value of 3.4 nM at MC4R, was more than 200-fold selective over MC3R, and had a good pharmacokinetic profile in mice, including high brain penetration. Moreover, 12b was able to stimulate food intake in the tumor-bearing mice and reverse their lean body mass loss. Our results provided further evidence that a potent and selective MC4R antagonist with appropriate pharmacokinetic properties might potentially be useful for the treatment of cancer cachexia.