122844-73-9

Upstream product

• 67-56-1 methanol 
• 122844-85-3 3-benzyl-1,2,3,4,5,8,9,9a-octahydro-7H-3-benzazepin-7-one 
• 122844-79-5 1-benzyl-1,2,3,5,6,7-hexahydro-5-(3-oxobutyl)-4H-azepin-4-one 
• 74-83-9 methyl bromide 

Downstream Products

• 50351-80-9 7-methoxy-2,3,4,5-tetrahydro-1H-benz[d]azepine 

Relevant academic research and scientific papers

Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists

SCH 58261 is a reported adenosine A2A receptor antagonist which is active in rat in vivo models of Parkinson's Disease upon ip administration. However, it has poor selectivity versus the A1 receptor and does not demonstrate oral activity. Quinoline analogs have improved upon the selectivity and pharmacokinetics of SCH 58261, but were difficult to handle due to poor aqueous solubility. We report the design and synthesis of fused heterocyclic analogs of SCH 58261 with aqueous solubility as well as improved A2A receptor binding selectivity and pharmacokinetic properties. In particular, the tetrahydronaphthyridine 4s has excellent A2A receptor in vitro binding affinity and selectivity, is active orally in a rat in vivo model of Parkinson's Disease, and has aqueous solubility of 100 μM at physiological pH.

NITROGENOUS FUSED HETEROCYCLE COMPOUNDS, PROCESS FOR THE PREPARATION THEREOF AND AGENTS CONTAINING THE SAME

A nitrogen-containing condensed heterocyclic derivative of the present invention, which is a compound represented by the formula: wherein ring A represents benzene ring optionally having a further substituent, -L-represents -O-, -NR3a-, -S-, -SO-, -SO2-, -SO2NR3a-, -SO2NHCONR3a-, -SO2NHC(=NH)NR3a-, -C(=S)-, or -CONR3a- (wherein R3a and R3b represent independently hydrogen atom, cyano group, hydroxy group, amino group, a C1-6 alkyl group or a C1-6 alkoxy group), n represents an integer of 0 to 6, R is hydrogen atom or a hydrocarbon group optionally having a substituent, and may be different in repetition of n, R1 represents a hydrocarbon group optionally having a substituent or a group represented by the formula: (wherein R7 represents a hydrocarbon group optionally having a substituent), R2 represents hydrogen atom, an acyl group, a hydrocarbon group optionally having a substituent or a heterocyclic group optionally having a substituent, X represents a bond, O, S, SO, SO2 or NR4 (wherein R4 represents hydrogen atom, an acyl group or a hydrocarbon group optionally having a substituent), k and m represent independently an integer of 0 to 5, and 1k+m5, or a salt thereof, and the like, has an excellent thermal production promoting activity and the like, and is useful as an agent for preventing or treating obesity and obesity-based diseases.