177338-13-5Relevant articles and documents
TRIAZOLE FURAN COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR
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Paragraph 0248; 0424; 0427, (2018/06/12)
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula (I) and Formula (II) have the following structures: (I); (II). Intermediates (V) are also claimed.
BICYCLIC-PYRIMIDINEDIONE COMPOUNDS
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Paragraph 0223; 0224, (2016/07/27)
The present invention provides novel bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.
Asymmetric Synthesis of Spiroketals with Aminothiourea Catalysts
Yoneda, Naoki,Fukata, Yukihiro,Asano, Keisuke,Matsubara, Seijiro
supporting information, p. 15497 - 15500 (2016/01/26)
Chiral spiroketal skeletons are found as core structures in a range of bioactive compounds. These natural compounds and their analogues have attracted much attention in the field of drug discovery. However, methods for their enantioselective construction are limited, and easily available optically active spiroketals are rare. We demonstrate a novel catalytic asymmetric synthesis of spiroketal compounds that proceeds through an intramolecular hemiacetalization/oxy-Michael addition cascade mediated by a bifunctional aminothiourea catalyst. This results in spiroketal structures through the relay formation of contiguous oxacycles, in which multipoint recognition by the catalyst through hydrogen bonding imparts high enantioselectivity. This method offers facile access to spiroketal frameworks bearing an alkyl group at the 2-position, which are prevalent in insect pheromones. Optically active (2S,5S)-chalcogran, a pheromone of the six-spined spruce bark beetle, and an azide derivative could be readily synthesized from the bicyclic reaction product. Around and around: A catalytic asymmetric synthesis of spiroketals through an intramolecular hemiacetalization/oxy-Michael addition cascade with a bifunctional aminothiourea catalyst was developed. This method offers facile access to spiroketal frameworks bearing an alkyl group at the 2-position. Optically active (2S,5S)-chalcogran, a pheromone from the six-spined spruce bark beetle, and a derivative were readily synthesized from the bicyclic reaction product.