473732-83-1Relevant academic research and scientific papers
New quinoline NK3 receptor antagonists with CNS activity
Smith, Paul W.,Wyman, Paul A.,Lovell, Peter,Goodacre, Caroline,Serafinowska, Halina T.,Vong, Antonio,Harrington, Frank,Flynn, Sean,Bradley, Daniel M.,Porter, Rod,Coggon, Sara,Murkitt, Graham,Searle, Kirsten,Thomas, David R.,Watson, Jeannette M.,Martin, William,Wu, Zining,Dawson, Lee A.
scheme or table, p. 837 - 840 (2009/09/06)
Lead optimisation starting from the previously reported selective quinoline NK3 receptor antagonists talnetant 2 (SB-223412) and 3 (SB-222200) led to the identification of 3-aminoquinoline NK3 antagonist 10 (GSK172981) with excellent CNS penetration. Investigation of a structurally related series of sulfonamides with reduced lipophilicity led to the discovery of 20 (GSK256471). Both 10 and 20 are high affinity, potent NK3 receptor antagonists which despite having different degrees of CNS penetration produced excellent NK3 receptor occupancy in an ex vivo binding study in gerbil cortex.
3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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Page 135, (2008/06/13)
There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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Page 135-136, (2008/06/13)
There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
