1202577-82-9Relevant articles and documents
NOVEL SALTS
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Paragraph 0058; 0059; 0060; 0061, (2016/10/27)
Salts of 1-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid of the formula (I), in particular amino acid salts such as the lysine salt and alkali metal salts such as the sodium salt and the potassium salt, processes for their preparation, medicaments comprising them and their use for controlling diseases.
Optimization of 3-aryl-3-ethoxypropanoic acids and discovery of the potent GPR40 agonist DS-1558
Takano, Rieko,Yoshida, Masao,Inoue, Masahiro,Honda, Takeshi,Nakashima, Ryutaro,Matsumoto, Koji,Yano, Tatsuya,Ogata, Tsuneaki,Watanabe, Nobuaki,Hirouchi, Masakazu,Kimura, Takako,Toda, Narihiro
supporting information, p. 5546 - 5565 (2015/11/11)
GPR40 agonists stimulate insulin secretion only under the presence of high glucose concentration. Based on this mechanism, GPR40 agonists are believed to be promising novel insulin secretagogues with low risk of hypoglycemia. The optimizations of 3-aryl-3-ethoxypropanoic acids were performed to improve in vitro activity. We discovered compound 29r (DS-1558), (3S)-3-ethoxy-3-(4-{[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]oxy}phenyl)propanoic acid, which was confirmed to have an enhancing effect on glucose-dependent insulin secretion after intravenous glucose injection in SD rats.
INDANYLOXYPHENYLCYCLOPROPANECARBOXYLIC ACIDS
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Paragraph 0389, (2014/01/07)
The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.