170282-19-6Relevant academic research and scientific papers
ULTRAVIOLET LIGHT ABSORBERS
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, (2017/10/10)
The present invention relates to compounds that have ultraviolet light absorbing properties, and which can also have mesogenic properties. The present invention also relates to compositions that include one or more such compounds, and to articles of manufacture that include one or more such compounds, such as optical elements that include an optical substrate and a layer that includes at least one compound of the present invention.
Substituted phenyl compounds
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, (2008/06/13)
Compounds of formula (I) are described wherein R1is hydrogen, -(lower alkyl)q(CO2R6or OH), —CN, —C(R7)═NOR8, NO2, —O(lower alkyl)R9, —C≡C—R10, —CR11═C(R12)(R13), —C(═O)CH2C(═O)CO2H, —CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4and R5are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.
Selective endothelin a receptor antagonists. 3. Discovery and structure- activity relationships of a series of 4-phenoxybutanoic acid derivatives
Astles, Peter C.,Brealey, Clive,Brown, Thomas J.,Facchini, Vincenzo,Handscombe, Caroline,Harris, Neil V.,McCarthy, Clive,McLay, Iain M.,Porter, Barry,Roach, Alan G.,Sargent, Carol,Smith, Christopher,Walsh, Roger J. A.
, p. 2732 - 2744 (2007/10/03)
The third in this series of papers describes our further progress into the discovery of a potent and selective endothelin A (ET(A)) receptor antagonist for the potential treatment of diseases in which a pathophysiological role for endothelin has been implicated. These include hypertension, ischemic diseases, and atherosclerosis. In earlier publications we have outlined the discovery and structure-activity relations of two moderately potent series of nonpeptide ET(A) receptor antagonists. In this paper, we describe how a pharmacophore model for ET(A) receptor binding was developed which enabled these two series of compounds to be merged into a single class of 4-phenoxybutanoic acid derivatives. The subsequent optimization of in vitro activity against the ET(A) receptor led to the discovery of (R)-4-[2-cyano-5-(3-pyridylmethoxy)phenoxy]-4-(2- methylphenyl)butanoic acid (12m). This compound exhibits low-nanomolar binding to the ET(A) receptor and a greater than 1000-fold selectivity over the ET(B) receptor. Data are presented to demonstrate that 12m is orally bioavailable in the rat and is a functional antagonist in vitro and in vivo of ET-1-induced vasoconstriction.
