142001-75-0

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 152298-54-9 N-[2-(S)-(3,4-dichlorophenyl)-4-hydroxybutyl]-N-methylamine 
• 152298-51-6 2-(2-Hydroxyethyl)-2-(3,4-dichlorobenzene)ethanamine 

Downstream Products

• 178914-34-6 N-{1-[3-(3,4-Dichloro-phenyl)-4-methylamino-butyl]-4-phenyl-piperidin-4-yl}-acetamide 
• 173942-48-8 C₃₀H₃₁Cl₂N₃O₄ 
• 173943-90-3 (+/-)-1'-<3-(3,4-dichlorophenyl)-4-methylaminobutyl>spiro 
• 173943-89-0 tert-butyl (+/-)-N-[2-(3,4-dichlorophenyl)-4-(spiro[isobenzofuran-1(3H),4'-piperidine]-1'-yl)butyl]-N-methylcarbamate 

Relevant academic research and scientific papers

Spiro-substituted piperidines as neurokinin receptor antagonists. II. Syntheses and NK2 receptor-antagonistic activities of N-[2-aryl-4-(spiro- substituted piperidin-1'-yl)butyl]carboxamides

In the course of our research on spiro-compounds as neurokinin receptor antagonists, N-[2-aryl-4-spiro-substituted piperidin-1'-yl)butyl]carboxamides were designed, based on YM-35375 (3) as a lead compound, and evaluated for NK2 receptor-antagonistic activities. Some derivatives inhibited the binding of radio-labeled neurokinin A to the NK2 receptor with IC50 values at the level of 10-9. Among these compounds, (±)-1'-[4-(N-benzoyl-N-methylamino)- 3-(3,4-dichlorophenyl)butyl]spiro[benzo[c]thiophene-1(3H), 4'-piperidine] 2- oxide (58, YM-38336) showed 10 times more potent NK2 receptor binding affinity than compound 3 (IC50 values of 8.9 and 84nM, respectively). It showed more potent inhibitory activity (ID50 20μg/kg (i.v.)) against [β- Ala8]-NKA(4 - 10)-induced bronchoconstriction in guinea pigs than compound 3 (ID50 41 μg/kg (i.v.)). This compound was also effective intraduodenally in the same model, exhibiting an ID50 value of 0.41 μg/kg.

Parallel-compound synthesis: Methodology for accelerating drug discovery

Parallel compound synthesis enables large numbers of individual compounds to be prepared simultaneously using semiautomated techniques. This fast and efficient methodology has an important role to play in accelerating lead optimisation and hence the whole drug discoveIy process. The potential of this strategy to rapidly optimise chemical leads an.d provide structureactivity relationship (SAR) information was demonstrated in two therapeutic areas, antiviral agents (herpes simplex virus), and neurokinin-2 receptor antagonists.

Arylalkylamines, process for preparing them and pharmaceutical compositions containing them

The invention relates to compounds of formula: STR1 in which Y represents--either a group Cy--N in which Cy represents a phenyl, optionally substituted; a C3 -C7 cycloalkyl group; a pyrimidinyl group or a pyridyl group; or a group ST