228246-71-7Relevant academic research and scientific papers
High-affinity, non-peptide agonists for the ORL1 (Orphanin FQ/nociceptin) receptor
R?ver, Stephan,Adam, Geo,Cesura, Andrea M.,Galley, Guido,Jenck, Fran?ois,Monsma Jr., Frederick J.,Wichmann, Jürgen,Dautzenberg, Frank M.
, p. 1329 - 1338 (2000)
The discovery of 8-(5,8-dichloro-1,2,3,4-tetrahydro-napthalene-2-yl)-1- phenyl-1,3,8-triazaspiro[4.5]decan-4-one, 1a, as a high-affinity ligand for the human ORL1 (orphanin FQ/nociceptin) receptor led to the synthesis of a series of optimized ligands. The
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.
