109254-16-2Relevant articles and documents
NOVEL SULFONAMIDE DERIVATIVE
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, (2010/11/25)
A compound of the formula (1): wherein m, n and p is independently an integer of 0 to 4 with the proviso that 3 a?| m + n a?| 8; X is the formula: NR4, etc.; R1, R3 and R4 are a substituted or unsubstituted aryl group, etc.; R2 is a hydrogen atom, etc.; a, b, c, d, e and f are a hydrogen atom or a substituted or unsubstituted alkyl group, etc.; Y is the formula: -SO2-, etc.; and Z is an oxygen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt of the same has an activity of potentiating an expression of a low density lipoprotein receptor and thus is useful as an agent for treating hyperlipidemia or arteriosclerosis.
Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists
Burkholder, Timothy P.,Kudlacz, Elizabeth M.,Maynard, George D.,Liu, Xiao-Gao,Le, Tieu-Binh,Webster, Mark E.,Horgan, Stephen W.,Wenstrup, David L.,Freund, David W.,Boyer, Fred,Bratton, Larry,Gross, Raymond S.,Knippenberg, Robert W.,Logan, Deborah E.,Jones, Bryan K.,Chen, Teng-Man,Geary, Julie L.,Correll, Melinda A.,Poole, J. Chuck,Mandagere, Arun K.,Thompson, Thomas N.,Hwang, Kin-Kai
, p. 2531 - 2536 (2007/10/03)
We recently described the synthesis and characterization of MDL 105,212, a non peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors. Here we report the synthesis and structure-activity relationships for a series of analogs of MDL 105,212 with regards to: NK1 and NK2 receptor binding affinity, physical-chemical characterization; in vitro absorption potential; in vitro metabolic stability; and efficacy in a capsaicin-challenge conscious guinea pig model after oral administration.
