Publications by authors named "Adriana I Velter"

3 Publications

  • Page 1 of 1

Anilinotriazoles as potent gamma secretase modulators.

Bioorg Med Chem Lett 2014 Dec 18;24(24):5805-5813. Epub 2014 Oct 18.

Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium. Electronic address:

The design and synthesis of a novel series of potent gamma secretase modulators is described. Exploration of various spacer groups between the triazole ring and the aromatic appendix in 2 has led to anilinotriazole 28, which combined high in vitro and in vivo potency with an acceptable drug-like profile.
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http://dx.doi.org/10.1016/j.bmcl.2014.10.024DOI Listing
December 2014

Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators.

Bioorg Med Chem Lett 2013 Sep 11;23(17):4794-800. Epub 2013 Jul 11.

Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.

The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a γ-secretase modulator is described. This is a potential disease modifying anti-Alzheimer's drug which demonstrated high in vitro and in vivo potency against Aβ42 peptide, reduced lipophilicity and enhanced brain free fraction compared to the previous series.
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http://dx.doi.org/10.1016/j.bmcl.2013.06.100DOI Listing
September 2013

Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.

ACS Med Chem Lett 2013 Apr 12;4(4):419-22. Epub 2013 Mar 12.

Janssen Research and Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.

The synthesis and preclinical characterization of two novel, brain penetrating P2X7 compounds will be described. Both compounds are shown to be high potency P2X7 antagonists in human, rat, and mouse cell lines and both were shown to have high brain concentrations and robust receptor occupancy in rat. Compound 7 is of particular interest as a probe compound for the preclinical assessment of P2X7 blockade in animal models of neuro-inflammation.
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http://dx.doi.org/10.1021/ml400040vDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4027403PMC
April 2013