Development of dihydropyridone indazole amides as selective rho-kinase inhibitors
Rho kinase (ROCK1) mediates vascular smooth muscle contraction and is a potential target for the treatment of hypertension and related disorders. Indazole amide 3 was identified as a potent and selective ROCK1 inhibitor but possessed poor oral bioavailabi
Goodman, Krista B.,Cui, Haifeng,Dowdell, Sarah E.,Gaitanopoulos, Dimitri E.,Ivy, Robert L.,Sehon, Clark A.,Stavenger, Robert A.,Wang, Gren Z.,Viet, Andrew Q.,Xu, Weiwei,Ye, Guosen,Semus, Simon F.,Evans, Christopher,Fries, Harvey E.,Jolivette, Larry J.,Kirkpatrick, Robert B.,Dul, Edward,Khandekar, Sanjay S.,Yi, Tracey,Jung, David K.,Wright, Lois L.,Smith, Gary K.,Behm, David J.,Bentley, Ross,Doe, Christopher P.,Hu, Erding,Lee, Dennis
Enantioselective synthesis of dihydropyridinones via NHC-Catalyzed Aza-Claisen reaction
N-Heterocyclic carbene catalyzed aza-Claisen annulations of enals or their α-hydroxyenone surrogates with vinylogous amides afford dihydropyridinones. The reaction proceeds with a broad range of substrates, and no nitrogen protecting group is required.
Wanner, Benedikt,Mahatthananchai, Jessada,Bode, Jeffrey W.
supporting information; experimental part
p. 5378 - 5381
(2011/12/02)
NOVEL COMPOUNDS
Novel inhibitors of Rho-kinases are disclosed.
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Page/Page column 25-26
(2008/06/13)
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