Dual NK2/NK3-antagonists, pharmaceutical compositions comprising them, and processes for their preparation
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.
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Page/Page column 23-24
(2010/11/28)
NOVEL DUAL NK2/NK3-ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND PROCESSES FOR THEIR PREPARATIONS
The present invention relates to novel dual NK2/NK3-antagonists of formula (I) wherein the meaning of X and R1 to R5 is defined in the claims and in the description and also to pharmaceutical compositions comprising these compounds. Furthermore, the invention relates to processes for the preparation of the novel dual NK2/NK3-antagonists and to their uses.
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Page/Page column 59
(2010/11/28)
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
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.
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)
PIPERAZINE UREA DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS
Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders r
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(2010/11/30)
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