130205-06-0Relevant academic research and scientific papers
Lead-discovery of bis-aromatic alkynes: A novel class of herbicides
Glock, Jutta,Allen, James,Niderman, Thierry,Haas, Hans Ulrich,Chollet, Renold,Eberle, Martin,Renold, Peter,Lutz, William,Ehrler, Jürg,Valentini, Marian,Walti, Markus,Sieger, Evelyne,Vettiger, Thomas,Brunner, Hans,Penzotti, Julie E.,Grootenhuis, Peter D. J.,Bondy, Steven,Comer, Daniel D.,Cheng, Soan,Steiger, Arthur,Zeller, Martin,Laue, Grit,Friedmann, Adrian,Jacob, Olivier,Nina, Mafalda,Widmer, Hans-Jürg,Kreuz, Klaus,Craig, G. Wayne
, p. 23 - 28 (2008/09/20)
The search for new active molecules with novel modes of action and desirable physical properties is an ongoing endeavour.[1,2] This publication describes the follow-up chemistry of a biological hit discovered in the screening system of Novartis
Dual-Acting Thromboxane Receptor Antagonist/Synthase Inhibitors: Synthesis and Biological Properties of alkenoic Acids
Faull, Alan W.,Brewster, Andrew G.,Brown, George R.,Smithers, Michael J.,Jackson, Ruth
, p. 686 - 694 (2007/10/02)
The design, synthesis, and pharmacology of a new class of compounds possessing bith thromboxane receptor antagonist and thromboxane synthase inhibitory properties are described.Replacement of the phenol group of the known thromboxane antagonist series 4(Z)-6-hex-4-enoic acid by a 3-pyridyl group led to a series of compounds, 5, which were potent thromboxane synthase inhibitors and weak thromboxane antagonists.Further modifications at the dioxane C2 position led to compounds, 7, which were potent dual-acting agents.In the case of compound 7w, the dual activity was shown to reside almost exclusively in the (-)-enantiomer, 7x.Following oral dosing to rats and dogs, 7x (3 mg/kg) displayed significant dual activity over a period of at least 8 h.
Pyridine derivatives
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, (2008/06/13)
The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A1 is alkylene, the substituents R1 and R2 at position 2 of the dioxane ring have a variety of values defined hereinafter, and R4 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
