273378-16-8Relevant articles and documents
Dual NK2/NK3-antagonists, pharmaceutical compositions comprising them, and processes for their preparation
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Page/Page column 23-24, (2010/11/28)
Dual NK2/NK3-antagonists corresponding to formula I: and physiologically compatible salts of such compounds in which X and R1 to R5 have specific defined meanings, pharmaceutical compositions containing such compounds, methods of using such compounds to treat or inhibit disorders mediated by tachykinin receptors, and a process for preparing such compounds.
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino] carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl] -4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist
Palucki, Brenda L.,Park, Min K.,Nargund, Ravi P.,Ye, Zhixiong,Sebhat, Iyassu K.,Pollard, Patrick G.,Kalyani, Rubana N.,Tang, Rui,MacNeil, Tanya,Weinberg, David H.,Vongs, Aurawan,Rosenblum, Charles I.,Doss, George A.,Miller, Randall R.,Stearns, Ralph A.,Peng, Qianping,Tamvakopoulos, Constantin,McGowan, Erin,Martin, William J.,Metzger, Joseph M.,Shepherd, Cherrie A.,Strack, Alison M.,MacIntyre, D. Euan,Van Der Ploeg, Lex H.T.,Patchett, Arthur A.
, p. 171 - 175 (2007/10/03)
We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. Further in vivo development of lead agonist, MB243, is disclosed.