102676-87-9Relevant academic research and scientific papers
R-FADROZOLE FOR USE IN THE TREATMENT OF ALDOSTONERISM
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, (2019/11/19)
The present invention relates to a composition for use in the treatment of a disease or disorder, wherein said disease or disorder is preferably a disease or disorder in which aldosterone overexposure contributes to the symptoms of said disease or disorder, said composition comprises a compound which is (R)-(+)-5-(p-cyanophenyl)-5,6,7,8- tetrahydroimidazo[1,5-a]pyridine or a pharmaceutically acceptable salt thereof, wherein preferably said compound is (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazolium[1,5- a]pyridine dihydrogen phosphate, and wherein said compound has an enantiomeric excess (ee) of the (R) form higher than or equal to 97%, and wherein said composition is administered once daily to a subject in need thereof. The invention further relates to a pharmaceutical composition comprising a daily dosage of said compound in a fixed-unit dosage form and to a combination comprising (i) said pharmaceutical composition or said compound; and (ii) instructions for administration of said pharmaceutical composition or said compound once per day.
ALDOSTERONE SYNTHASE INHIBITOR
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, (2018/05/24)
The present invention relates to a compound selected from (R)-(+)-5-(p-cyanophenyl)- 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine and a pharmaceutically acceptable salt thereof, and in particular to the phosphate salt of (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, both having preferably an enantiomeric excess of the (R) form higher than or equal to 97%. Furthermore, the present invention relates to pharmaceutical compositions comprising the same, their use as a medicament and in methods of treatment of diseases and disorders in humans including women of child bearing potential and pediatric patients in which aldosterone over-exposure contributes to the deleterious effects of said diseases or disorders, as well as processes for preparing said inventive compounds.
Aromatase inhibitors: Synthesis, biological activity, and binding mode of azole-type compounds
Furet,Batzl,Bhatnagar,Francotte,Rihs,Lang
, p. 1393 - 1400 (2007/10/02)
The enantiomers of the potent nonsteroidal inhibitor of aromatase fadrozole hydrochloride 3 have been separated and their absolute configuration determined by X-ray crystallography. On the basis of a molecular modeling comparison of the active enantiomer
Fedrazole Hydrochloride: A Potent, Selective, Nonsteroidal Inhibitor ofAromatase for the Treatment of Estrogen-Dependent Disease
Browne, L. J.,Gude, C.,Rodriguez, H.,Steele, R. E.
, p. 725 - 736 (2007/10/02)
A new class of potent, selective, nonsteroidal inhibitors of aromatase have been discovered.The most potent member of this series is fadrozole hydrochloride, CGS 16949 A, 4-(5,6,7,8-tetrahydroimidazopyridin-5-yl)benzonitrile monohydrochloride, 26a.
