Research Topics
| Martin H BolliSummaryAffiliation: Actelion Pharmaceuticals Ltd Country: Switzerland Publications
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Detail Information
Publications
Synthetic sphingosine 1-phosphate receptor modulators--opportunities and potential pitfallsMartin H Bolli
Drug Discovery Chemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil, Switzerland
Curr Top Med Chem 11:726-57. 2011..In particular, the complexity of discovering a molecule akin to FTY720 but with an improved side-effect profile will be discussed...
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonistsMartin H Bolli
Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
Bioorg Med Chem Lett 13:955-9. 2003..g., 70 and 75). The propargyl derivative 26 significantly reduced blood pressure in in vivo model studies with hypertensive salt-sensitive Dahl rats...
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonistsMartin H Bolli
Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil, Switzerland
J Med Chem 47:2776-95. 2004..In this animal model, the efficacy of the benzo[e][1,4]diazepin-2-one derivative rac-39au was superior to that of racemic ambrisentan, rac-2...
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonistsMartin H Bolli
Drug Discovery Chemistry, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
J Med Chem 53:4198-211. 2010..At a dose of 100 mg/kg, the effect on lymphocyte counts was fully reversible within less than 36 h. Pharmacokinetic investigation of 8bo in beagle dogs suggests that the compound is suitable for once daily dosing in humans...
Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonistMarc Iglarz
Drug Discovery Department, Actelion Pharmaceuticals Ltd, Allschwil, Switzerland
J Pharmacol Exp Ther 327:736-45. 2008..This profile makes macitentan a new agent to treat cardiovascular disorders associated with chronic tissue ET system activation...
Bis-sulfonamides as endothelin receptor antagonistsChristoph Boss
Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH 4123 Allschwil BL, Switzerland
Bioorg Med Chem Lett 13:951-4. 2003..This allowed to prepare dual ET(A)/ET(B) as well as ET(B) receptor selective antagonists, which could serve as tools to investigate the pharmacological consequences of selective ET(B) receptor blockade...
The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammationLuca Piali
Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland
J Pharmacol Exp Ther 337:547-56. 2011..Immunomodulation with a rapidly reversible S1P(1)-selective agonist may represent a new therapeutic approach in lymphocyte-mediated autoimmune diseases...
