193755-84-9

Upstream product

• 167262-37-5 3-(3,4-dichloro-phenyl)-1-(benzoyl)-3-(2-hydroxy-ethyl)-pyrrolidine 
• 3218-49-3 3,4-dichloro-benzeneacetonitrile 
• 135936-16-2 α-[2-(Tetrahydropyran-2-yloxy)ethyl]-3,4-dichlorophenyl-acetonitrile 
• 155308-39-7 4-(3,4-dichloro-phenyl)-4-[2-(tetrahydro-pyran-2-yloxy)-ethyl]-pyrrolidine 
• 155308-38-6 4-(3,4-dichloro-phenyl)-4-[2-(tetrahydro-pyran-2-yloxy)-ethyl]-pyrrolidin-2-one 
• 155308-37-5 3-cyano-3-(3,4-dichloro-phenyl)-5-(tetrahydro-pyran-2-yl-oxy)-pentanoic acid ethyl ester 
• 193755-82-7 1-Benzoyl-3-(3,4-dichlorophenyl)-3-(2-[tetrahydropyran-2-yloxy]ethyl)pyrrolidine 

Relevant academic research and scientific papers

4-Amino-2-(aryl)-butylbenzamides and their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK2) receptor

A library, evaluating a range of piperazines, piperidines and acyclic amines, as replacements for the 4-hydroxy-4-phenylpiperidine moiety in lead (1b) was prepared. These efforts identified the 4-((N)-benzimidazolone)piperidine analogue (2a) which was further optimised using classical single-compound synthesis to yield the 3-((N)-morpholino)azetidine (2j). Conformationally constrained analogues of (2j), generally offered no potency advantage in this particular series.

3-Azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists

The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.