363191-03-1Relevant articles and documents
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist
Hong, Qingmei,Bakshi, Raman K.,Palucki, Brenda L.,Park, Min K.,Ye, Zhixiong,He, Shuwen,Pollard, Patrick G.,Sebhat, Iyassu K.,Liu, Jian,Guo, Liangqin,Cashen, Doreen E.,Martin, William J.,Weinberg, David H.,MacNeil, Tanya,Tang, Rui,Tamvakopoulos, Constantin,Peng, Qianping,Miller, Randy R.,Stearns, Ralph A.,Chen, Howard Y.,Chen, Airu S.,Strack, Alison M.,Fong, Tung M.,MacIntyre, D. Euan,Wyvratt, Matthew J.,Nargund, Ravi P.
scheme or table, p. 2330 - 2334 (2011/05/15)
We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
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.
PIPERAZINE UREA DERIVATIVES AS MELANOCORTIN-4 RECEPTOR AGONISTS
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, (2010/11/30)
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