127056-57-9Relevant academic research and scientific papers
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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, (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.
ORGANIC COMPOUNDS AS AGENTS FOR THE TREATMENT OF ALDOSTERONE MEDIATED CONDITIONS
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Page 44, (2010/02/06)
Compounds of formula (I), provide pharmacological agents which are inhibitors of the P450 enzyme, aldosterone synthase, and thus may be employed for the treatment of aldosterone mediated conditions. Accordingly, the compounds of formula (I) may be employe
3-Aminopyrrolidinone farnesyltransferase inhibitors: Design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency
Bell, Ian M.,Gallicchio, Steven N.,Abrams, Marc,Beese, Lorena S.,Beshore, Douglas C.,Bhimnathwala, Hema,Bogusky, Michael J.,Buser, Carolyn A.,Culberson, J. Christopher,Davide, Joseph,Ellis-Hutchings, Michelle,Fernandes, Christine,Gibbs, Jackson B.,Graham, Samuel L.,Hamilton, Kelly A.,Hartman, George D.,Heimbrook, David C.,Homnick, Carl F.,Huber, Hans E.,Huff, Joel R.,Kassahun, Kelem,Koblan, Kenneth S.,Kohl, Nancy E.,Lobell, Robert B.,Lynch Jr., Joseph J.,Robinson, Ronald,Rodrigues, A. David,Taylor, Jeffrey S.,Walsh, Eileen S.,Williams, Theresa M.,Zartmant, C. Blair
, p. 2388 - 2409 (2007/10/03)
A series of macrocyclic 3-aminopyrrolidinone farnesyltransferase inhibitors (FTIs) has been synthesized. Compared with previously described linear 3-aminopyrrolidinone FTIs such as compound 1, macrocycles such as 49 combined improved pharmacokinetic prope
Inhibitors of prenyl-protein transferase
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, (2008/06/13)
The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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, (2008/06/13)
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras
THE SYNTHESIS OF VIRIDAMINE, A PENICILLIUM VIRIDICATUM MYCOTOXIN
Bond, Roy F.,Bredenkamp, Martin W.,Holzapfel, Cedric W.
, p. 2551 - 2566 (2007/10/02)
The synthesis of viridamine, involving the condensation of 2-(3,3-dimethylallyl)-4(5)-formylimidazole with cyclo-glycyl-L-valyl is described.Different methods for the preparation of the imidazole intermediate were investigated.
