8-(Heteroaryl)phenalkyl-1-Phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as Opioid Receptor Modulators

A. D. Jordan; M. J. Orsini; S. A. Middleton; P. J. Connolly; D. E. Brenneman; K. Pan; A. B. Reitz

doi:10.2174/157340605774598207

ISSN: 1573-4064
E-ISSN: 1875-6638

8-(Heteroaryl)phenalkyl-1-Phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as Opioid Receptor Modulators
Authors: A. D. Jordan¹, M. J. Orsini², S. A. Middleton³, P. J. Connolly⁴, D. E. Brenneman⁵, K. Pan⁶ and A. B. Reitz⁷
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¹ Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, LLC, aP.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA. ² Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, LLC, aP.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA. ³ Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, LLC, aP.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA. ⁴ Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, LLC, aP.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA. ⁵ Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, LLC, aP.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA. ⁶ Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, LLC, aP.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA. ⁷ Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, LLC, aP.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA.
Source: Medicinal Chemistry, Volume 1, Issue 6, Nov 2005, p. 601 - 610
DOI: https://doi.org/10.2174/157340605774598207
- Available online: 01 Nov 2005

Abstract

A series of N-biarylalkyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-ones were prepared and evaluated for biological activity at opioid (μ, δ, κ) and opioid receptor like-1 (ORL-1) G-protein coupled receptors. Substitution on the biaryl moiety produced enhanced affinity for the μ-opioid receptor.

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2005-11-01

2025-12-07

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Article Type: Review Article

Keyword(s): 1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one; [35s]gtpγs binding assay; delta receptor; heteroarylphenylalkyl; kappa receptor; mu receptor; nociceptin receptor; pain; sar; suzuki reaction

8-(Heteroaryl)phenalkyl-1-Phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as Opioid Receptor Modulators

Abstract

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