- Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor
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The discovery, of a series of 2-Cl-5-heteroaryl-benzamide antagonists of the P2X7 receptor via parallel medicinal chemistry is described. Initial analogs suffered from poor metabolic stability and low Vdss. Multi parametric optimizat
- Subramanyam, Chakrapani,Duplantier, Allen J.,Dombroski, Mark A.,Chang, Shang-Poa,Gabel, Christopher A.,Whitney-Pickett, Carrie,Perregaux, David G.,Labasi, Jeff M.,Yoon, Kwansik,Shepard, Richard M.,Fisher, Michael
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p. 5475 - 5479
(2011/10/12)
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- BENZAMIDE INHIBITORS OF THE P2X7 RECEPTOR
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The present invention provides benzamide inhibitors of the P2X7 receptor of the formula (I), wherein R1 -R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, incl
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- Thiazolyl benzoic acid compounds
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m-(thiazol-4-yl) benzoic acids substituted in 2- and optionally 5-position of the thiazol ring by lower alkyl, phenylalkyl, phenyl, halo-phenyl, lower alkylphenyl or lower alkoxyphenyl, and on the phenyl ring of the benzoic acid moiety by halogen, hydroxyl, lower alkyl or lower alkoxy. These compounds possess fibrinolytic, platelet stickiness decreasing and antiulcer properties and have an impact on the immunological processes.
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