Ahmad, Saleem et al. published their patent in 2010 |CAS: 386704-04-7

The Article related to aza pyridone preparation melanin concentrating hormone receptor antagonist, obesity diabetes depression anxiety mchr1 antagonist pyrimidinone preparation, inflammatory bowel disease mchr1 antagonist pyridazinone preparation and other aspects.Synthetic Route of 386704-04-7

On September 16, 2010, Ahmad, Saleem published a patent.Synthetic Route of 386704-04-7 The title of the patent was Preparation of aza-pyridone derivatives as antagonists of melanin concentrating hormone receptor-1 (MCHR1). And the patent contained the following:

Title compounds I [A1 and A2 independently = C or N; E = C or N; Q1, Q2 and Q3 independently = C or N provided that only one of them is N; D1 = bond, CC, 1,2-cyclopropyl, etc; R1, R2 and R3 independently = H, halogen, (un)substituted alkyl, etc; G = O, S or NR15; where R15 = H or (un)substituted alkyl; D2 = (un)substituted alkyl, cycloalkyl, cycloalkoxy, etc; Z1 and Z2 independently = H, (un)substituted alkyl, cycloalkyl, etc; R5, R6 and R7 independently = H, halogen, (un)substituted alkyl, etc], and their pharmaceutically acceptable salts or prodrugs, are prepared and disclosed. Thus, e.g., II was prepared by coupling reaction of (E)-4-chlorostyrylboronic acid with 6-chloro-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)pyrimidin-4(3H)-one (preparation given). Compounds of the invention were evaluated for their antagonistic activity of peptide agonist binding to human melanin concentrating hormone receptor-1 (MCHR1), e.g., II exhibited Ki value of 23 nM. The invention compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, inflammatory bowel disease, depression, and anxiety. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Synthetic Route of 386704-04-7

The Article related to aza pyridone preparation melanin concentrating hormone receptor antagonist, obesity diabetes depression anxiety mchr1 antagonist pyrimidinone preparation, inflammatory bowel disease mchr1 antagonist pyridazinone preparation and other aspects.Synthetic Route of 386704-04-7

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