65076-02-0Relevant articles and documents
Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors
Fernandez, Maria-Carmen,Escribano, Ana,Mateo, Ana I.,Parthasarathy, Saravanan,Martin De La Nava, Eva M.,Wang, Xiaodong,Cockerham, Sandra L.,Beyer, Thomas P.,Schmidt, Robert J.,Cao, Guoqing,Zhang, Youyan,Jones, Timothy M.,Borel, Anthony,Sweetana, Stephanie A.,Cannady, Ellen A.,Stephenson, Gregory,Frank, Scott,Mantlo, Nathan B.
scheme or table, p. 3056 - 3062 (2012/06/17)
This Letter describes the discovery and SAR optimization of 1,5-tetrahydronaphthyridines, a new class of potent CETP inhibitors. The effort led to the identification of 21b and 21d with in vitro human plasma CETP inhibitory activity in the nanomolar range (IC50 = 23 and 22 nM, respectively). Both 21b and 21d exhibited robust HDL-c increase in hCETP/hApoA1 dual heterozygous mice model.
Heterocyclic fused pyridone carboxylic acid M1 positive allosteric modulators
Kuduk, Scott D.,Di Marco, Christina N.,Chang, Ronald K.,Ray, William J.,Ma, Lei,Wittmann, Marion,Seager, Matthew A.,Koeplinger, Kenneth A.,Thompson, Charles D.,Hartman, George D.,Bilodeau, Mark T.
scheme or table, p. 2533 - 2537 (2010/08/05)
The phenyl ring in a series of quinolone carboxylic acid M1 positive allosteric modulators was replaced with a variety of heterocycles in order to reduce protein plasma binding and enhance CNS exposure.
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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Page/Page column 49-50, (2009/01/20)
The present invention relates to modulators of ATP-B inding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators
Antiviral agents
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Page 17, (2010/02/07)
The invention provides a compound of formula I: wherein G, R2, and R3 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or salts, and methods of treating a herpesvirus infection using such compounds or salts.
Synthesis and antibacterial activity of 4,7-dihydro-4-ethyl-7-oxothieno(3,2-b)pyridine-6-carboxylic acids
Malicorne,Bompart,Giral,Despaux
, p. 3 - 11 (2007/10/02)
The synthesis of some new 4,7-dihydro-4-ethyl-7-oxothieno(3,2-b)pyridine-6-carboxylic acids with various substituents on position 2 is described. The evaluation of the anti-bacterial activity of some compounds shows an activity different to those of the thieno(2,3-b)pyridine series.
THE PREPARATION OF 2-(HETEROCYCLIC)THIENOPYRIDINE DERIVATIVES
Elliot, Richard, L.,O'Hanlon, Peter J.,Rogers, Norman H.
, p. 3295 - 3302 (2007/10/02)
The preparation of a series of 2-(heterocyclic)-4-ethyl-4,7-dihydro-7-oxothienopyridine-6-carboxylic acids (5j-l) by aminolysis of the corresponding 2-bromo derivative (5i) is described.None of the compounds (5j-l) showed any interesting antibacterial activity.
Thienopyridines. Part 4. The Preparation of Some Dithienopyridine Derivatives.
Barker, John M.,Huddleston, Patrick R.,Keenan, Guy J.
, p. 1726 - 1746 (2007/10/02)
Reaction of 6-ethoxycarbonyl-7-hydroxythienopyridin-5(4H)-one (1) with phosphoryl chloride produced the corresponding 5,7-dichloro- (2) and 7-chloro- (3) derivatives.With alkyl thioglycolate-base these led to angularly fused dithienopyridines; the nature of the products was demonstrated (through reductive dehalogenation) by correlation with dithienopyridines synthesised by an unambiguous route.
