228246-84-2Relevant academic research and scientific papers
1,3,8-triazaspiro[4,5]decan-4-one derivatives
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, (2008/06/13)
The present invention relates to compounds of the formula wherein R1 and R2 are each independently hydrogen, lower alkyl, lower alkoxy or halogen; R3 is phenyl, which is unsubstituted or substituted by lower alkyl, CF3, lower alkoxy or halogen; R4 is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylene-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF3, phenyl or benzyl, R5 and R6 are each independently hydrogen, phenyl, lower alkyl or di-lower alkyl or R5 and R6 together with the carbon atoms to which they are bound form a phenyl ring, or R5 and one of R1 or R2 together with the carbon atoms to which they are bound form a saturated or unsaturated 6 membered ring, A is a 4-7 membered saturated ring, their racemates and the enantiomers thereof, and the pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.
8-Acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists
Wichmann, Juergen,Adam, Geo,Roever, Stephan,Cesura, Andrea M.,Dautzenberg, Frank M.,Jenck, Francois
, p. 2343 - 2348 (2007/10/03)
A series of 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4- one derivatives 1 was studied with respect to the binding affinity for the orphanin FQ (OFQ) and opioid (μ, κ, δ) receptors. The influence of stereochemistry as well as the substitution pattern of the phenyl-ring in position 1 on the affinity for the orphanin FQ receptor and selectivity to opioid (μ, κ, δ) receptors is discussed. The most interesting compound 1c was tested for its anxiolytic-like properties in vivo.
