1284199-22-9Relevant academic research and scientific papers
Synthesis of a stable triformylmethane synthon and its scalable application to 7-acylamino-3-formylquinoline syntheses
Sawai, Yasuhiro,Mizuno, Masahiro,Ito, Tatsuya,Yamano, Mitsuhisa
, p. 2370 - 2377 (2014/04/03)
Novel 2-iminiomethylvinamidinium trihalides were isolated as stable crystals and found to be useful triformylmethane synthons with non-deliquescent nature in air. They were easier to manufacture, handle, and store than the known 2-iminiomethylvinamidinium
BICYCLIC COMPOUND
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Paragraph 1325; 1326; 1327, (2014/09/03)
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
8-benzamidochromen-4-one-2-carboxylic acids: Potent and selective agonists for the orphan G protein-coupled receptor GPR35
Funke, Mario,Thimm, Dominik,Schiedel, Anke C.,Müller, Christa E.
, p. 5182 - 5197 (2013/07/25)
8-Amido-chromen-4-one-2-carboxylic acid derivatives were identified as novel agonists at the G protein-coupled orphan receptor GPR35. They were characterized by a β-arrestin recruitment assay and optimized to obtain agonists with nanomolar potency for the
Synthesis, structure-activity relationship, and pharmacological studies of novel melanin-concentrating hormone receptor 1 antagonists 3- aminomethylquinolines: Reducing human ether-a-go-go-related gene (hERG) associated liabilities
Kasai, Shizuo,Kamata, Makoto,Masada, Shinichi,Kunitomo, Jun,Kamaura, Masahiro,Okawa, Tomohiro,Takami, Kazuaki,Ogino, Hitomi,Nakano, Yoshihide,Ashina, Shuntarou,Watanabe, Kaoru,Kaisho, Tomoko,Imai, Yumi N.,Ryu, Sunghi,Nakayama, Masaharu,Nagisa, Yasutaka,Takekawa, Shiro,Kato, Koki,Murata, Toshiki,Suzuki, Nobuhiro,Ishihara, Yuji
, p. 4336 - 4351 (2012/07/01)
Recently, we discovered 3-aminomethylquinoline derivative 1, a selective, highly potent, centrally acting, and orally bioavailable human MCH receptor 1 (hMCHR1) antagonist, that inhibited food intake in F344 rats with diet-induced obesity (DIO). Subsequent investigation of 1 was discontinued because 1 showed potent hERG K+ channel inhibition in a patch-clamp study. To decrease hERG K+ channel inhibition, experiments with ligand-based drug designs based on 1 and a docking study were conducted. Replacement of the terminal p-fluorophenyl group with a cyclopropylmethoxy group, methyl group introduction on the benzylic carbon at the 3-position of the quinoline core, and employment of a [2-(acetylamino)ethyl]amino group as the amine portion eliminated hERG K+ channel inhibitory activity in a patch-clamp study, leading to the discovery of N-{3-[(1R)-1-{[2-(acetylamino)ethyl]amino} ethyl]-8-methylquinolin-7-yl}-4-(cyclopropylmethoxy)benzamide (R)-10h. The compound (R)-10h showed potent inhibitory activity against hMCHR1 and dose-dependently suppressed food intake in a 2-day study on DIO-F344 rats. Furthermore, practical chiral synthesis of (R)-10h was performed to determine the molecule's absolute configuration.
HETEROCYCLIC COMPOUND
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Page/Page column 38, (2010/12/30)
The present invention provides to a compound having melanin-concentrating hormone receptor antagonistic action and low toxicity, and useful as a agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound re
