- Synthesis of spirolactams and spiropiperidines as CCR4 receptor antagonists
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The synthesis of racemic and non-racemic spirocyclic lactams that display high binding affinity toward CCR4 is described. Two distinct series of spirocycles were prepared from the common intermediate 9.
- Hansen, Joshua D.,Newhouse, Bradley J.,Allen, Shelley,Anderson, Aaron,Eary, Todd,Schiro, Justin,Gaudino, John,Laird, Ellen,Allen, Andrew C.,Chantry, David,Eberhardt, Christine,Burgess, Laurence E.
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- Racemic and chiral lactams as potent, selective and functionally active CCR4 antagonists
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A series of racemic and chiral, nonracemic lactams that display high binding affinities, functional chemotaxis antagonism, and selectivity toward CCR4 are described. Compound 41, which provides reasonably high blood levels in mice when dosed intraperitoneally, was identified as a useful pharmacological tool to explore the role of CCR4 antagonism in animal models of allergic disease. A series of racemic and chiral, nonracemic lactams that display high binding affinities, functional chemotaxis antagonism, and selectivity toward CCR4 are described. Compound 41, which provides reasonably high blood levels in mice when dosed intraperitoneally, was identified as a useful pharmacological tool to explore the role of CCR4 antagonism in animal models of allergic disease.
- Newhouse, Bradley,Allen, Shelley,Fauber, Benjamin,Anderson, Aaron S.,Eary, C. Todd,Hansen, Joshua D.,Schiro, Justin,Gaudino, John J.,Laird, Ellen,Chantry, David,Eberhardt, Christine,Burgess, Laurence E.
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p. 5537 - 5542
(2007/10/03)
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