- NOVEL COMPOUNDS USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS
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The present invention relates to novel morpholine, oxazapane and piperidine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 81
(2010/07/08)
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- Synthesis and evaluation of ligands for D2-like receptors: The role of common pharmacophoric groups
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Arylcycloalkylamines, such as phenyl piperidines and piperazines and their arylalkyl substituents, constitute pharmacophoric groups exemplified in several antipsychotic agents. A review of previous reports indicates that arylalkyl substituents can improve
- Sikazwe, Donald M.N.,Nkansah, Nancy T.,Altundas, Ramazan,Zhu, Xue Y.,Roth, Bryan L.,Setola, Vincent,Ablordeppey, Seth Y.
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scheme or table
p. 1716 - 1723
(2009/08/07)
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- Haloperidol analogs
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Haloperidol analogs that conforms to the structural formulae: wherein: R is H, or —(CH2)n—OH, n is an integer from 0 to 2, and A is a heterocyclic bridging group, consisting essentially of carbon and at least one nitrogen atom, which effectively maintains the distance between the moieties connected thereby such that the compound (1) is incapable of metabolizing to BCPP+ like species, (2) has an affinity for the D2 receptor subtype of 151 is H, or —(CH2)n—OH, n is an integer from 0 to 2, B is an aza- or diaza-bicyclo group, which effectively maintains the distance between the moieties connected thereby such that the compound is incapable of metabolizing to BCPP+ like species; and Z is —CH— or N; and pharmaceutically acceptable salts, esters, derivatives, metal complexes, conjugates and prodrugs thereof.
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Page/Page column 5
(2008/06/13)
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- Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan- 1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol
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Enantiomeric separation of the racemic 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan- 1-one, a pyrrolidine analog of haloperidol, {(±)-SYA 09}, and subsequent binding studies revealed that most of the binding affinity at dopamine
- Ablordeppey, Seth Y.,Lyles-Eggleston, Margaret,Bricker, Barbara,Zhang, Wang,Zhu, Xue,Goodman, Carl,Roth, Bryan L.
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p. 3219 - 3223
(2007/10/03)
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