475655-24-4Relevant academic research and scientific papers
Efficient solid-phase synthesis of 2,3-substituted indoles
Wacker, Dean A,Kasireddy, Padmaja
, p. 5189 - 5191 (2002)
The development of the solid-phase version of the modified Madelung indole synthesis is reported. The chemistry was initiated with the reductive amination of Bal resin using an ortho substituted aniline. The resin bound aniline was acylated with a variety of acid chlorides followed by cyclization with base to provide the desired indole after TFA-promoted cleavage from the resin.
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects
Papillon, Julien P. N.,Lou, Changgang,Singh, Alok K.,Adams, Christopher M.,Ksander, Gary M.,Beil, Michael E.,Chen, Wei,Leung-Chu, Jennifer,Fu, Fumin,Gan, Lu,Hu, Chii-Whei,Jeng, Arco Y.,Lasala, Daniel,Liang, Guiqing,Rigel, Dean F.,Russell, Kerry S.,Vest, John A.,Watson, Catherine
, p. 9382 - 9394 (2015/12/23)
Human clinical studies conducted with LCI699 established aldosterone synthase (CYP11B2) inhibition as a promising novel mechanism to lower arterial blood pressure. However, LCI699's low CYP11B1/CYP11B2 selectivity resulted in blunting of adrenocorticotropic hormone-stimulated cortisol secretion. This property of LCI699 prompted its development in Cushing's disease, but limited more extensive clinical studies in hypertensive populations, and provided an impetus for the search for cortisol-sparing CYP11B2 inhibitors. This paper summarizes the discovery, pharmacokinetics, and pharmacodynamic data in preclinical species and human subjects of the selective CYP11B2 inhibitor 8.
ORGANIC COMPOUNDS
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, (2011/04/19)
The present invention provides novel organic compounds of Formula (I): methods of use, and pharmaceutical compositions thereof.
