192069-85-5Relevant articles and documents
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors
Zhan, Wenhu,Xu, Lei,Dong, Xiaowu,Dong, Jun,Yi, Xiao,Ma, Xiaodong,Qiu, Ni,Li, Jia,Yang, Bo,Zhou, Yubo,Hu, Yongzhou
, p. 47 - 58 (2016/05/11)
A series of novel pyrazol-furan carboxamide analogues were designed, synthesized and biologically evaluated for their Akt1 inhibitory activities, as well as anti-proliferative efficacies against HCT116 and OVCAR-8 cell lines. Most compounds exhibited mode
SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES
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Page/Page column 88-89, (2011/02/18)
The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds. These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.
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.