92501-98-9Relevant academic research and scientific papers
Novel 1,8-naphthyridin-2(1h)-one derivatives
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, (2008/06/13)
The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety. A compound of the formula (1): wherein: A is an unsubstituted or optionally substituted 5 or 6 membered heteroaryl group or a fused benzene ring in which any of the above-defined heteroaryl groups is fused to a benzene ring, B is carbon or nitrogen, R1 is hydrogen, lower alkyl, trifluoromethyl, hydroxyl, lower alkoxy, a residue derived from a carboxylic acid or a derivative thereof, amino, or an amino nitrogen-containing group, R2 is hydrogen, halogen, cyano, nitro, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, trifluoromethyl, hydroxyl, lower alkoxy, a residue derived from a carboxylic acid or a derivative thereof, amino, or an amino nitrogen-containing group, and m is an integer of from 1 to 8, both inclusive; or a pharmaceutically acceptable salt thereof possesses selective PDE IV inhibition and is useful as a pharmaceutical drug, preferably an anti-asthmatic, etc.
Design of a new class of orally active fibrinogen receptor antagonists
Klein, Scott I.,Molino, Bruce F.,Czekaj, Mark,Gardner, Charles J.,Chu, Valeria,Brown, Karen,Sabatino, Ralph D.,Bostwick, Jeffrey S.,Kasiewski, Charles,Bentley, Ross,Windisch, Vincent,Perrone, Mark,Dunwiddie, Christopher T.,Leadley, Robert J.
, p. 2492 - 2502 (2007/10/03)
The integrin receptor recognition sequence Arg-Gly-Asp was successfully used as a template from which to develop a series of potent, selective, orally active, peptide-based fibrinogen receptor antagonists with a long duration of action. Simple modifications centered on the Arg and Gly residues quickly led to a modified peptide (1) with significantly enhanced ability to inhibit in vitro platelet aggregation. Substitution of the guanidino group in 1 by piperidine provided 3, which showed not only a further increase in potency but also a modest degree of oral efficacy. Finally, exploration of the nature of the C-terminal amino acid, with respect to its side-chain functionality and the carboxy terminus, yielded a group of molecules that showed excellent in vitro potency for inhibiting platelet aggregation, excellent integrin selectivity, a high level of oral efficacy, and an extended duration of action.
Tartronic acids, their acetalic ethers and O-esters
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, (2008/06/13)
Tartronic acid acetalic ethers and esters of the general formula: STR1 are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C2 -C12 acyl group, R is phenyl and n is 0-12.
