690264-82-5Relevant academic research and scientific papers
BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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Page/Page column 20, (2009/07/17)
The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and/or diabetes.
NOVEL N-ARYL AND N-HETEROARYL SUBSTITUTED PYRIDINONE DERIVATIVES FOR USE IN MCH-1 MEDIATED DISEASES
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Page/Page column 31, (2008/06/13)
The present invention concerns N-aryl and N-heteroaryl substituted pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.
Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists
Dyck, Brian,Zhao, Liren,Tamiya, Junko,Pontillo, Joseph,Hudson, Sarah,Ching, Brett,Heise, Christopher E.,Wen, Jenny,Norton, Christi,Madan, Ajay,Schwarz, David,Wade, Warren,Goodfellow, Val S.
, p. 4237 - 4242 (2007/10/03)
A series of substituted chromones were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor 1. Compounds with subnanomolar binding affinity and 66% oral bioavailability in rats were discovered.
2- (3-AMINOPYRROLIDIN-1-YL) PYRIDINES AS MELANIN-CONCENTRATING HORMONE RECEPTOR AN TAGONISTS
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Page/Page column 24, (2010/02/14)
Melanin-concentrating hormone (MCH) receptor antagonists are disclosed having utility for the treatment of MCH receptor-based disorders such as obesity. The compounds of this invention have the following structure: including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein R1, R2, R5, Het, X and Cyc are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.
Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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, (2008/06/13)
The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
