494863-86-4Relevant academic research and scientific papers
Novel hexahydrospiro[piperidine-4,1′-pyrrolo[3,4-c]pyrroles: Highly selective small-molecule nociceptin/orphanin FQ receptor agonists
Kolczewski, Sabine,Adam, Geo,Cesura, Andrea M.,Jenck, Fran?ois,Hennig, Michael,Oberhauser, Thomas,Poli, Sonia M.,R?ssler, Felix,R?ver, Stephan,Wichmann, Jürgen,Dautzenberg, Frank M.
, p. 255 - 264 (2007/10/03)
Novel hexahydrospiro[piperidine-4,1′-pyrrolo[3,4-c]pyrroles that act as potent and selective orphanin FQ/nociceptin (N/OFQ) receptor (NOP) agonists were identified. The best compound, (+)-5a, potently inhibited 3H-N/OFQ binding to the NOP recep
Spiro[piperidine-4,1'-pyrrolo [3,4-C] pyrrole]derivatives
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, (2008/06/13)
The present invention relates to compounds of the general formula wherein R1 is C5-12-cycloalkyl, optionally substituted by lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl; octahydro-inden-2-yl; 1,2,3,4-tetrahydro-naphthalen-1-yl; 1,2,3,4-tetrahydro-naphthalen-2-yl; naphthalen-lower alkyl-1-yl; naphthalen-lower alkyl-2-yl; acenaphthen-1-yl; and 5-isopropyl-2-methyl-bicyclo[3.1.0]hex-3-yl; R2, R3 are hydrogen; hydroxy; lower alkyl; =O; or phenyl, optionally substituted by lower allyl, halogen or alkoxy; R4 is hydrogen; lower alkyl; -(CH2)nCH(OH)CF3; -(CH2)nC3-6-cycloalkyl; phenyl; benzyl; tetrahydrofuran-3-yl; -(CH2)nOCH2C6H5; -(CH2)nmorpholinyl; 3-methyl-oxetan-3-yl-methyl; -(CH2)nCH2OH; -S(O)2-lower alkyl; -C(O)-lower alkyl; -C(O)CF3; -C(O)(CH2)nOCH3; -(CH2)nC(O)N(lower alkyl)2; -S(O)2heteroaryl; -C(O)heteroaryl; -S(O)2-phenyl; -S(O)2-N(lower alkyl)2; -C(O)-C3-6-cycloalkyl; -C(O)O-phenyl; or -C(O)O-lower alkyl: R5 is hydrogen; halogen; lower alkyl; trifluoromethyl or lower alkoxy; n is 0-3; and to pharmaceutically acceptable acid addition salts thereof The compounds of formula I and their salts are useful as in the treatment of psychiatric, neurological and physiological disorders.
