1129-66-4Relevant articles and documents
The compound, composition, and display device
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Paragraph 0207-0209, (2017/07/26)
PROBLEM TO BE SOLVED: To provide a compound capable of elevating an upper limit temperature where a SmC (smectic-C) phase of a liquid crystal can exist, broadening a temperature width of the SmC phase or enlarging a tilt angle of the SmC phase, and to provide a liquid crystal composition comprising the compound and a display element including the liquid crystal composition.SOLUTION: [1] The compound is expressed by general formula (i) shown below. In general formula (i), R and R' each independently represent a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, or an alkoxy group having 1 to 9 carbon atoms; A1, A2 and A3 each independently represent a 1,4-phenylene group or a 2,3-difluoro-1,4-phenylene group; m represents an integer of 1 to 10; and Y represents a cyclohexylene group, a phenylene group, a bicyclooctylene group or a dialkylsilylene group.
Disubstituted beta-lactones as inhibitors of N-acylethanolamine acid amidase (NAAA)
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Page/Page column 112, (2016/06/28)
The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.
3-Aminoazetidin-2-one derivatives as N-acylethanolamine acid amidase (NAAA) inhibitors suitable for systemic administration
Fiasella, Annalisa,Nuzzi, Andrea,Summa, Maria,Armirotti, Andrea,Tarozzo, Glauco,Tarzia, Giorgio,Mor, Marco,Bertozzi, Fabio,Bandiera, Tiziano,Piomelli, Daniele
supporting information, p. 1602 - 1614 (2014/07/21)
N-Acylethanolamine acid amidase (NAAA) is a cysteine hydrolase that catalyzes the hydrolysis of endogenous lipid mediators such as palmitoylethanolamide (PEA). PEA has been shown to exert anti-inflammatory and antinociceptive effects in animals by engaging peroxisome proliferator-activated receptor α (PPAR-α). Thus, preventing PEA degradation by inhibiting NAAA may provide a novel approach for the treatment of pain and inflammatory states. Recently, 3-aminooxetan-2-one compounds were identified as a class of highly potent NAAA inhibitors. The utility of these compounds is limited, however, by their low chemical and plasma stabilities. In the present study, we synthesized and tested a series of N-(2-oxoazetidin-3-yl)amides as a novel class of NAAA inhibitors with good potency and improved physicochemical properties, suitable for systemic administration. Moreover, we elucidated the main structural features of 3-aminoazetidin-2-one derivatives that are critical for NAAA inhibition. Stability is the key: α-Amino-β-lactams were synthesized as amide derivatives, and the effect of the azetidin-2-one ring, the stereochemistry at the α-position, and the functionalization of the α-amino group were studied with regard to N-acylethanolamine acid amidase inhibitory potency and hydrolytic and plasma stability.
