203186-29-2Relevant academic research and scientific papers
MCH antagonists for the treatment of obesity
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Page/Page column 11, (2010/02/10)
The present invention discloses methods of using antagonists for melanin-concentrating hormone (MCH), to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes, as well as novel compounds which are antagonists for melanin-concentrating hormone (MCH). In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods for preparing such compounds. Compounds of the invention generally have the structure: where the substituents are as defined herein.
Synthesis and structure-Activity relationships of M2-Selective muscarinic receptor ligands in the 1-[4-(4-Arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family
McCombie, Stuart W.,Lin, Sue-Ing,Tagat, Jayaram R.,Nazareno, Dennis,Vice, Susan,Ford, Jennifer,Asberom, Theodros,Leone, Daria,Kozlowski, Joseph A.,Zhou, Guowei,Ruperto, Vilma B.,Duffy, Ruth A.,Lachowicz, Jean E.
, p. 795 - 798 (2007/10/03)
The synthesis and muscarinic binding properties of compounds based on the 1-[4-(4-arylsulfonyl)phenylmethyl]-4-(1-aroyl-4-piperidinyl)-piperazine skeleton are described. For compounds, substituted with appropriately configured methyl groups at the benzylic center and at the piperazine 2-position, high levels of selective, M2 subtype affinity could be obtained, particularly when the terminal N-aroyl residue was ortho-substituted.
