181283-43-2Relevant articles and documents
AGENT FOR OVERCOMING RESISTANCE TO ANTI-CANCER AGENT
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Page/Page column 6, (2009/04/23)
An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenox
1- [3- (MONOCYCLIC AMINO) PROPYL] - 4, 5, 6, 7-TETRAHYDRO-1H-PYRAZOLO [4, 3-C] -PYRIDINES AS MODULATORS OF CATHEPSIN S
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Page/Page column 25, (2008/12/08)
Monocyclic aminopropyl tetrahydro-pyrazolo-pyridine compounds of formula (I) are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, a
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole α(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH)
Meyer, Michael D.,Altenbach, Robert J.,Basha, Fatima Z.,Carroll, William A.,Condon, Stephen,Elmore, Steven W.,Kerwin Jr., James F.,Sippy, Kevin B.,Tietje, Karin,Wendt, Michael D.,Hancock, Arthur A.,Brune, Michael E.,Buckner, Steven A.,Drizin, Irene
, p. 1586 - 1603 (2007/10/03)
In search of a uroselective agent that exhibits a high level of selectivity for the α(1A) receptor, a novel series of tricyclic hexahydrobenz[e]isoindoles was synthesized. A generic pharmacophoric model was developed requiring the presence of a basic amine core and a fused heterocyclic side chain separated by an alkyl chain. It was shown that the 6- OMe substitution with R, R stereochemistry of the ring junction of the benz[e]isoindole and a two-carbon spacer chain were optimal. In contrast to the highly specific requirements for the benz[e]isoindole portion and linker chain, a wide variety of tricyclic fused heterocyclic attachments were tolerated with retention of potency and selectivity. In vitro functional assays for the α1 adrenoceptor subtypes were used to further characterize these compounds, and in vivo models of vascular vs prostatic tone were used to assess uroselectivity.