790663-45-5Relevant academic research and scientific papers
NOVEL COMPOUNDS AS INHIBITORS OF RENIN
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Page/Page column 10, (2012/05/20)
The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to
NOVEL COMPOUNDS AS INHIBITORS OF RENIN
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Page/Page column 21, (2010/11/05)
The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors
Bezen?on, Olivier,Bur, Daniel,Weller, Thomas,Richard-Bildstein, Sylvia,Remeň, Lubo?,Sifferlen, Thierry,Corminboeuf, Olivier,Grisostomi, Corinna,Boss, Christoph,Prade, Lars,Delahaye, Stéphane,Treiber, Alexander,Strickner, Panja,Binkert, Christoph,Hess, Patrick,Steiner, Beat,Fischli, Walter
supporting information; experimental part, p. 3689 - 3702 (2010/04/02)
Starting from known piperidine renin inhibitors, a new series of 3,9-diazabicyclo[3.3.1]nonene derivatives was rationally designed and prepared. Optimization of the positions 3, 6, and 7 of the diazabicyclonene template led to potent renin inhibitors. The substituents attached at the positions 6 and 7 were essential for the binding affinity of these compounds for renin. The introduction of a substituent attached at the position 3 did not modify the binding affinity but allowed the modulation of the ADME properties. Our efforts led to the discovery of compound (+)-26g that inhibits renin with an IC 50 of 0.20 nM in buffer and 19 nM in plasma. The pharmacokinetics properties of this and other similar compounds are discussed. Compound (+)-26g is well absorbed in rats and efficacious at 10 mg/kg in vivo.
ORGANIC COMPOUNDS
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Page/Page column 165, (2008/06/13)
3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that cla
AZABICYCLONONENE DERIVATIVES AS RENIN INHIBITORS
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Page/Page column 36, (2010/11/08)
The invention relates to novel bicyclononene derivatives, related compounds and use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the
AZABICYCLONONENE DERIVATIVES
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Page 24, (2008/06/13)
The invention relates to novel 9-azabicyclo[3.3.1 ]nonene derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the prep
DIAZABICYCLONONENE AND TETRAHYDROPYRIDINE DERIVATIVES AS RENIN INHIBITORS
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Page 36, (2010/02/09)
The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives, tetrahydropyridine derivatives, and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspe
