On June 6, 2013, Aebi, Johannes; Amrein, Kurt; Chen, Wenming; Hornsperger, Benoit; Kuhn, Bernd; Liu, Yongfu; Maerki, Hans P.; Mayweg, Alexander V.; Mohr, Peter; Tan, Xuefei; Wang, Zhanguo; Zhou, Mingwei published a patent.Application of 58142-46-4 The title of the patent was New bicyclic dihydroisoquinolin-1-one derivatives as aldosterone synthase inhibitors and their preparation. And the patent contained the following:
The invention provides compounds having formula I, compositions including the compounds and methods of using the compounds as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome. Compounds of formula I wherein E is absent and CR3R4; A1 is CR8 and N; A2 is CR9 and N; A3 is CR10 and N; A4 is CR11 and N; A5 is CR6 and N; R1, R2, R3 and R4 are independently H, alkyl, cycloalkyl, haloalkyl, etc.; R2R4 can be taken together to form a double bond, then R5 is H; R1R2, R3R4 or R1R3 can be taken together to form substituted cycloalkyl and heterocycloalkyl; R5, R6, R7 and R8 are independently halo, CN, alkoxy, hydroxyalkoxy, etc.; R9 is H, halo, OH, CN, alkyl, etc.; R10 is (un)substituted alkoxy and substituted alkyl; R11 is H; and with proviso; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by N-arylation of 6-chloro-3,4-dihydroisoquinolin-1(2H)-one with 3-bromopyridine. The invention compounds were evaluated for their aldosterone synthase inhibitory activity. From the assay, it was determined that compound II exhibited EC50 values of 0.0860 μM and 4.6072 μM towards CYP11B2 and CYP11B1, resp. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Application of 58142-46-4
The Article related to dihydroisoquinolinone preparation aldosterone synthase inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 58142-46-4
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem