103258-38-4Relevant articles and documents
Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors
Papillon, Julien P. N.,Adams, Christopher M.,Hu, Qi-Ying,Lou, Changgang,Singh, Alok K.,Zhang, Chun,Carvalho, Jose,Rajan, Srinivan,Amaral, Adam,Beil, Michael E.,Fu, Fumin,Gangl, Eric,Hu, Chii-Whei,Jeng, Arco Y.,LaSala, Daniel,Liang, Guiqing,Logman, Michael,Maniara, Wieslawa M.,Rigel, Dean F.,Smith, Sherri A.,Ksander, Gary M.
, p. 4749 - 4770 (2015/06/25)
CYP11B2, the aldosterone synthase, and CYP11B1, the cortisol synthase, are two highly homologous enzymes implicated in a range of cardiovascular and metabolic diseases. We have previously reported the discovery of LCI699, a dual CYP11B2 and CYP11B1 inhibi
ORGANIC COMPOUNDS
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Page/Page column 58, (2008/06/13)
The present invention provides a compound of formula (I):said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, cardiac fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.
Sparteine-mediated enantioselective [2,3]-Wittig rearrangement of allyl ortho-substituted benzyl ethers and ortho-substituted benzyl prenyl ethers
Kawasaki, Takeshi,Kimachi, Tetsutaro
, p. 6847 - 6862 (2007/10/03)
The (-)-sparteine-mediated enantioselective [2,3]-Wittig rearrangement of N,N-dialkyl-o-allyloxymethylbenzamides and o-substituted benzyl prenyl ethers has been investigated. Enantiomeric excess up to 60% was observed as for the reaction with N,N-diethyl-o-allyloxymetylbenzamide. From the mechanistic investigations, it was suggested that the stereoinformation was introduced at the deprotonation step. Substoichiometric amount of (-)- sparteine (0.2 equiv.) did not decrease the enantioselectivity. Introduction of functional groups other than carbamoyl group did not enhance the enantioselectivity in this rearrangement.