346416-55-5

Upstream product

• 120-43-4 4-ethoxycarbonylpiperazine 
• 37167-62-7 bromo-phenyl-acetic acid methyl ester 
• 346416-54-4 4-(Methoxycarbonyl-phenyl-methyl)-piperazine-1-carboxylic acid ethyl ester 

Downstream Products

• 346417-00-3 4-[2-(3,5-dimethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-carboxylic acid ethyl ester 
• 346417-02-5 4-[2-(3,5-di-tert-butyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-carboxylic acid ethyl ester 
• 346417-16-1 4-[2-(3,4-dichloro-benzyloxy)-1-phenyl-ethyl]-piperazine-1-carboxylic acid ethyl ester 
• 346417-04-7 4-[2-(2-methoxy-benzyloxy)-1-phenyl-ethyl]-piperazine-1-carboxylic acid ethyl ester 
• 346417-14-9 4-[2-(3,5-dichloro-benzyloxy)-1-phenyl-ethyl]-piperazine-1-carboxylic acid ethyl ester 
• 346417-10-5 4-[1-phenyl-2-(3,4,5-trimethoxy-benzyloxy)-ethyl]-piperazine-1-carboxylic acid ethyl ester 
• 346417-08-1 4-[1-phenyl-2-(2-trifluoromethoxy-benzyloxy)-ethyl]-piperazine-1-carboxylic acid ethyl ester 
• 346416-99-7 4-[2-(2,4-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Discovery of orally bioavailable NK1 receptor antagonists

Benzyloxyphenethylpiperazines are a new class of high affinity NK1 receptor antagonists. Oral bioavailability and selectivity can be fine tuned by the nature of the substituents on the basic nitrogen atom. Addition of substituents with a carboxylic acid group led to very selective and orally active NK1 antagonists free of interaction with L-type calcium channels.

Alpha-arylethylpiperazine derivatives as neurokinin antagonists

The invention relates to new α-arylethylpiperazine derivatives, which are useful as neurokinin receptor antagonists (NK1antagonists). It also relates to processes for the preparation of said α-arylethylpiperazine derivatives, to their use for the prevention and/or treatment of a condition associated with pathogical levels of substance P in a patient and to pharmaceutical compositions containing them.