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Patrick Hess

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Articles 43
Citations 963
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Recent Articles
21.
Rey M, Hess P, Clozel M, Delahaye S, Gatfield J, Nayler O, et al.
PLoS One . 2013 Sep; 8(9):e74285. PMID: 24069292
Ponesimod, a selective S1P1 receptor modulator, reduces the blood lymphocyte count in all tested species by preventing egress of T and B cells from thymus and peripheral lymphoid organs. In...
22.
Bolli M, Boss C, Binkert C, Buchmann S, Bur D, Hess P, et al.
J Med Chem . 2012 Aug; 55(17):7849-61. PMID: 22862294
Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy. This...
23.
Rey M, Hess P, Clozel M
Curr Protoc Pharmacol . 2012 Feb; Chapter 5:Unit 5.56. PMID: 22294402
Pulmonary arterial hypertension (PAH) is a debilitating and often fatal disease characterized by a progressive increase in pulmonary vascular resistance that leads to right ventricular failure. Described in this unit...
24.
St-Jacques R, Toulmond S, Auger A, Binkert C, Cromlish W, Fischli W, et al.
J Renin Angiotensin Aldosterone Syst . 2011 Mar; 12(3):133-45. PMID: 21393355
Introduction: The hypertensive double-transgenic (dTG) rat strain, expressing human renin and angiotensinogen, develops severe hypertension and organ damage and 50% of individuals die by 7 weeks of age. Here, we...
25.
Bauer Y, Hess P, Qiu C, Klenk A, Renault B, Wanner D, et al.
Hypertension . 2011 Mar; 57(4):795-801. PMID: 21357272
The renin-angiotensin system is a well-known regulator of blood pressure and plays an important role in the pathogenesis of cardiovascular disease and renal damage. Genetic factors, including single nucleotide polymorphisms...
26.
Piali L, Froidevaux S, Hess P, Nayler O, Bolli M, Schlosser E, et al.
J Pharmacol Exp Ther . 2011 Feb; 337(2):547-56. PMID: 21345969
Lymphocyte exit from lymph nodes and their recirculation into blood is controlled by the sphingolipid sphingosine 1-phosphate (S1P). The cellular receptor mediating lymphocyte exit is S1P(1), one of five S1P...
27.
Corminboeuf O, Bezencon O, Remen L, Grisostomi C, Richard-Bildstein S, Bur D, et al.
Bioorg Med Chem Lett . 2010 Sep; 20(21):6291-6. PMID: 20843690
The optimization of the 4-position of recently described new 3,4-disubstituted piperidine-based renin inhibitors is reported herein. The synthesis and characterization of compounds leading to the discovery of 11 (ACT-178882, MK-1597),...
28.
Corminboeuf O, Bezencon O, Grisostomi C, Remen L, Richard-Bildstein S, Bur D, et al.
Bioorg Med Chem Lett . 2010 Sep; 20(21):6286-90. PMID: 20843686
The discovery of a new series of piperidine-based renin inhibitors is described herein. SAR optimization upon the P3 renin sub-pocket is described, leading to the discovery of 9 and 41,...
29.
Morrison K, Ernst R, Hess P, Studer R, Clozel M
J Pharmacol Exp Ther . 2010 Jul; 335(1):249-55. PMID: 20660124
Selexipag [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide] is an orally available prostacyclin (PGI(2)) receptor (IP receptor) agonist that is chemically distinct from PGI(2) and is in clinical development for the treatment of pulmonary arterial hypertension....
30.
Bolli M, Abele S, Binkert C, Bravo R, Buchmann S, Bur D, et al.
J Med Chem . 2010 May; 53(10):4198-211. PMID: 20446681
Sphingosine-1-phosphate (S1P) is a widespread lysophospholipid which displays a wealth of biological effects. Extracellular S1P conveys its activity through five specific G-protein coupled receptors numbered S1P(1) through S1P(5). Agonists of...