152811-86-4

Upstream product

• 152811-87-5 N-[(1-benzylpiperidin-4-yl)methyl]indole-3-carboxamide 
• 627-18-9 1-bromo-3-propanol 
• 88915-26-8 4-aminomethyl-1-benzylpiperidine 
• 203585-25-5 methyl 3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxylate 

Relevant academic research and scientific papers

5-HTX MODULATORS

This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT2 or 5-HT7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.

MODULATORS OF PERIPHERAL 5-HT RECEPTORS

Novel modulators of 5-HT4 receptors have been developed which have a selectivity for peripheral receptors rather than those of the central nervous systems. Theses include novel derivatives of known modulators as well as entirely novel entities. Surprisingly, the derivatised compounds of the known modulators maintain a high binding affinity to 5-HT4 receptors, despite the presence of an acidic moiety at the end of an optional chain. The entirely novel entities also exhibit good binding affinity to 5-HT4 receptors. All of the compounds of the invention have a common motif which includes a basic nitrogen moiety and an acidic moiety. The compounds of the invention, due at least in part to their high ionisation potential at physiological pH, have the unique properties of selectively for peripheral 5HT4 receptors over those of the CNS, good binding affinity, and selectively of 5HT4 receptors over other serotonin receptors.

Piperidine derivatives as 5-HT4 receptor antagonists

Compounds of formula (I): STR1 wherein Xg is O, S, SO, SO2, CH2, CH, N or NR wherein R is hydrogen or C1-6 alkyl; A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms; R1g and R2g are hydrogen or C1-6 alkyl; R3g is hydrogen, halo, C1-6 alkyl, amino, nitro or C1-6 alkoxy; R4g is hydrogen, halo, C1-6 alkyl or C1-6 alkoxy, Y is O or NH, or CO--Y together are a heterocyclic bioisostere; Z is of sub-formula: STR2 wherein --(CH2)n1 is attached at carbon; and n1 is 0, 1, 2, 3 or 4; q is 0, 1, 2 or 3; Ra is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R7 wherein R7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R7 is C2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C1-6 alkyl; and R6 is hydrogen or C1-6 alkyl; are useful as 5HT4 receptor antagonists.