Gijsen HJM - Search Results

1

Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.

Gijsen HJM, Alonso de Diego SA, De Cleyn M, García-Molina A, Macdonald GJ, Martínez-Lamenca C, Oehlrich D, Prokopcova H, Rombouts FJR, Surkyn M, Trabanco AA, Van Brandt S, Van den Bossche D, Van Gool M, Austin N, Borghys H, Dhuyvetter D, Moechars D. Gijsen HJM, et al. J Med Chem. 2018 Jun 28;61(12):5292-5303. doi: 10.1021/acs.jmedchem.8b00304. Epub 2018 Jun 11. J Med Chem. 2018. PMID: 29809004

2

5-Sulfonyl-benzimidazoles as selective CB2 agonists.

Verbist BM, De Cleyn MA, Surkyn M, Fraiponts E, Aerssens J, Nijsen MJ, Gijsen HJ. Verbist BM, et al. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2574-9. doi: 10.1016/j.bmcl.2008.03.048. Epub 2008 Mar 20. Bioorg Med Chem Lett. 2008. PMID: 18394887

3

Analogues of morphanthridine and the tear gas dibenz[b,f][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel.

Gijsen HJ, Berthelot D, Zaja M, Brône B, Geuens I, Mercken M. Gijsen HJ, et al. J Med Chem. 2010 Oct 14;53(19):7011-20. doi: 10.1021/jm100477n. J Med Chem. 2010. PMID: 20806939

4

γ-Secretase modulators as potential disease modifying anti-Alzheimer's drugs.

Oehlrich D, Berthelot DJ, Gijsen HJ. Oehlrich D, et al. J Med Chem. 2011 Feb 10;54(3):669-98. doi: 10.1021/jm101168r. Epub 2010 Dec 9. J Med Chem. 2011. PMID: 21141968 Review. No abstract available.

5

Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors.

Tresadern G, Delgado F, Delgado O, Gijsen H, Macdonald GJ, Moechars D, Rombouts F, Alexander R, Spurlino J, Van Gool M, Vega JA, Trabanco AA. Tresadern G, et al. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7255-60. doi: 10.1016/j.bmcl.2011.10.050. Epub 2011 Oct 20. Bioorg Med Chem Lett. 2011. PMID: 22071305

6

A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators.

Borghys H, Tuefferd M, Van Broeck B, Clessens E, Dillen L, Cools W, Vinken P, Straetemans R, De Ridder F, Gijsen H, Mercken M. Borghys H, et al. J Alzheimers Dis. 2012;28(4):809-22. doi: 10.3233/JAD-2011-111475. J Alzheimers Dis. 2012. PMID: 22072214

7

5-sulfonyl-benzimidazoles as selective CB2 agonists-part 2.

Gijsen HJ, De Cleyn MA, Surkyn M, Van Lommen GR, Verbist BM, Nijsen MJ, Meert T, Wauwe JV, Aerssens J. Gijsen HJ, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):547-52. doi: 10.1016/j.bmcl.2011.10.091. Epub 2011 Nov 6. Bioorg Med Chem Lett. 2012. PMID: 22130134

8

Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists.

Gijsen HJ, Berthelot D, De Cleyn MA, Geuens I, Brône B, Mercken M. Gijsen HJ, et al. Bioorg Med Chem Lett. 2012 Jan 15;22(2):797-800. doi: 10.1016/j.bmcl.2011.12.068. Epub 2011 Dec 22. Bioorg Med Chem Lett. 2012. PMID: 22222037

9

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

Bischoff F, Berthelot D, De Cleyn M, Macdonald G, Minne G, Oehlrich D, Pieters S, Surkyn M, Trabanco AA, Tresadern G, Van Brandt S, Velter I, Zaja M, Borghys H, Masungi C, Mercken M, Gijsen HJ. Bischoff F, et al. J Med Chem. 2012 Nov 8;55(21):9089-106. doi: 10.1021/jm201710f. Epub 2012 Jun 8. J Med Chem. 2012. PMID: 22650177

10

Comment on "ApoE-directed therapeutics rapidly clear β-amyloid and reverse deficits in AD mouse models".

Tesseur I, Lo AC, Roberfroid A, Dietvorst S, Van Broeck B, Borgers M, Gijsen H, Moechars D, Mercken M, Kemp J, D'Hooge R, De Strooper B. Tesseur I, et al. Science. 2013 May 24;340(6135):924-e. doi: 10.1126/science.1233937. Science. 2013. PMID: 23704554

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