N-substituted spiropiperidine compounds as ligands for ORL-1...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S017000

Reexamination Certificate

active

06869960

ABSTRACT:
A compound of the formula:or a pharmaceutically acceptable salt, ester or ether thereof, wherein R1through R12are independently hydrogen or the like; X1and X2are independently CH2or the like; R13is hydrogen or the like; or R12and R13taken together with three ring atoms of the quinoline ring separating said substituents form a heterocyclic ring; R14and R15are hydrogen or the like or these groups taken together form oxo; and the dotted line represents a single or double bond. These compounds are ligands for ORL-1 receptor and especially are antagonists for said receptor.

REFERENCES:
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patent: 0006545 (2000-02-01), None
patent: WO 2002085354 (2002-10-01), None
patent: WO 03 000677 (2003-01-01), None
Meunier et al., “Isolation and structure of the endogenous agonist of opioid receptor-like ORL, receptor”,Nature, vol. 377, 1995, pp. 532-535.
Reinscheid et al., “Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor”,Science, vol. 270, 1995, pp. 792-794.
S. Rover, et al., “Orl 1 Receptor Ligands Structure-Activity Relationships of 8-Cycloalkyl-1-phenyl-1,3,8-triaza-spiro [4.5]decan-4-ones”, Bioogan & Med Chem Ltrs, vol. 10,pp 831-834 (2000).
D. Barlocco, et al., “The opioid receptor like 1 (ORL 1) as a potential target for new analgesics”, Eur J of Med Chem, vol. 35, pp 275-282 (2000).
N. Zaveri, et al., “Characterization of opiates, neuroleptics, and synthetic analogs at ORL 1 and opioid receptors”, Eur J of Pharma, vol. 428, pp 29-36 (2001).
S. Ronzoni, et al., “Lead generation and lead optimisation approaches in the discovery of selective, non-peptide ORL 1 receptor agonists and antagonists”, Expert Opinion on Therap Patents, vol. 525, pp 525-546 (2001).

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