The University of Mississippi

L'université Catholique De Louvain

Leland Stanford Junior University

Christopher R McCurdy

Christophe Mesangeau

Sanjiv Sam Gambhir

Rae Matsumoto

Michelle Louise James

Bin Shen

Frederick T Chin

Jacques Henri Poupaert

Sandip Biswal

Bonnie Ann Avery

Deepak Behera

Ahmed Hassan Amin Abdelazeem

Sanju Narayanan

A method for localizing and quantifying S1R role in nociceptive processing; for providing a guide to providing an analgesic therapy; of using an S1R selective ligand as a biomarker for pathphysiological study of memory deficits and cognitive disorders; or of detecting increased S1R density at the site of nerve injury arising from neuropathic pain comprising using as a probe at least one SR1 selective compound or radioligand of the general formula III', or IV&#x2032;: 

Highly selective sigma receptor ligands and radioligands as probes in nociceptive processing and the pathphysiological study of memory deficits and cognitive disorders

Compounds having the general formula III', or IV&#x2032; wherein Rcan be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: Rcan each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, S&#x2014;R or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; 'n' can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging Rand N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C-Ccycloalkyl group, aromatic, and heterocyclic group; and wherein X is C-Cradiohaloalkyl.

Highly selective sigma receptor radioligands

A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which Rcan be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): Rcan each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH, O, S, OCH, N&#x2014;R, N&#x2014;Ar, C&#x2014;R, C&#x2014;Ar; Z can be either H, O, S, S&#x2014;R or NR. R groups can be either H, aryls, alkyls, or cycloalkyls; 'n' can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging Rand N can be optionally substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C-Ccycloalkyl group, aromatic and heterocyclic group.

Highly selective sigma receptor ligands

Compounds having the general formula II, III, or IV wherein Rcan be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: Rcan each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH, O, S, OCH, N&#x2014;R, N&#x2014;Ar, C&#x2014;R, C&#x2014;Ar; Z can be either H, O, S, S&#x2014;R or NR. R groups can be either H, aryls, alkyls, or cycloalkyls; 'n' can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging Rand N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C-Ccycloalkyl group, aromatic, and hetercocyclic group; wherein X' is halogen, or C-Chaloalyl; wherein the Ris a C-Cstraight chain or branched chain alkyl or a C-Cstraight chain or branched chain haloalkyl.

Growing community of inventors

Oxford, MS, United States of America

Christopher R McCurdy