625437-38-9Relevant articles and documents
COMPOUNDS AS INHIBITORS OF RENIN
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Page/Page column 19, (2013/06/27)
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
Practical synthesis of a renin inhibitor via a diastereoselective dieckmann cyclization
Gauvreau, Danny,Hughes, Greg J.,Lau, Stephen Y. W.,McKay, Daniel J.,O'Shea, Paul D.,Sidler, Rick R.,Yu, Bing,Davies, Ian W.
supporting information; experimental part, p. 5146 - 5149 (2011/02/23)
A scalable synthesis of a potent renin inhibitor (1) is described. The absolute stereochemistry is set via an unprecedented diastereoselective Dieckmann cyclization directed by a remote chiral protecting group. This transformation enables preparation of chiral 1,3-[3.3.1]-diazabicyclononenes by desymmetrization of alkyl-esters, with selectivities ranging from 4 to 17:1.
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.
A PROCESS FOR PREPARING DIAZABICYCLO[3.3.1] NONANE COMPOUNDS
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Page/Page column 11; 15-16; 52-53, (2008/12/07)
The invention is a process for preparing a diazabicyclo compound of formula (I) process for preparing a diazabicyclo compound of formula (I):where X is selected from the group consisting of hydrogen, C1-C6 alkoxycarbonyl, and carbobenzyloxy; R6 is selected from the group consisting of C1-C6 alkyl, C2-C6 alkenyl, and benzyl; and R9, R 10, and R11 are independently selected from the group consisting of hydrogen, halogen, and C1-C6 alkyl. wherein the process involves cyclizing I-I, formula (II).
RENIN INHIBITORS
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Page/Page column 28, (2008/06/13)
The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.
7- {4- [2- (2 , 6-DICHL0R0-4-METHYLPHEN0XY) ETHOXY] PHENYL}-3 , 9-DIAZABICYCLO [3 .3 . 31] NON - 6-ENE- S- CARBOXYLIC ACID CYCLOPROPYL- (2 , 3-DIMETHYLBENZYD AMIDE AS INHIBITORS OF RENIN FOR THE TREATMENT OF HYPERTENSION
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Page/Page column 10; 16-17, (2008/06/13)
The invention relates to a novel 3,9-diazabicyclα [3.3. ljnonene derivative of formula (I) and the enantiomers thereof and the use thereof as active ingredients in the preparation of pharmaceutical compositions . The invention also concerns related aspects including pharmaceutical compositions containing at least one compound of formula (I) or (I') and especially their use as inhibitors of renin.(I).