1132941-00-4Relevant articles and documents
High potency improvements to weak aryl uracil HCV polymerase inhibitor leads
Donner, Pamela,Randolph, John T.,Huang, Peggy,Wagner, Rolf,Maring, Clarence,Lim, Ben Hock,Colletti, Lynn,Liu, Yaya,Mondal, Rubina,Beyer, Jill,Koev, Gennadiy,Marsh, Kennan,Beno, David,Longenecker, Kenton,Pilot-Matias, Tami,Kati, Warren,Molla, Akhter,Kempf, Dale
, p. 4367 - 4369 (2013)
Described herein is the development of a potent non-nucleoside, small molecule inhibitor of genotype 1 HCV NS5B Polymerase. A 23 μM inhibitor that was active against HCV polymerase was further elaborated into a potent single-digit nanomolar inhibitor of HCV NS5B polymerase by additional manipulation of the R and R1 substituents. Subsequent modifications to improve physical properties were made in an attempt to achieve an acceptable pharmacokinetic profile.
URACIL OR THYMINE DERIVATIVE FOR TREATING HEPATITIS C
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Page/Page column 184; 200-201; 209, (2009/04/25)
Present application relates to the compounds of formula I useful to treat hepatitis C (HCV) infections. In the structure of the disclosed compounds is the uracil or thymine derivative linked via a phenylene into either fused 2-ring cyclic system (R6) or alternatively via additional two-atom linker (L) to a 5-6 membered monocycle (R6). Application further discloses polymorphs and pseudopolymorphs of two specific compounds: N-(6(3-t-butyl-5-(2>4-dioxo-3,4-dihydropyrimidin-1 (2H)- y!)2-methoxy-phenyl)naphthalen-2-yl)methanesulfonamide and (E)-N-(4(3-t- butyl-5-(2,4-dioxo-3)4-dihydropyrimidin-1 (2H)-yl)2-methoxy-styryl- phenyl)methanesulfonamide.
N-PHENYL-DIOXO-HYDROPYRIMIDINES USEFUL AS HEPATITIS C VIRUS (HCV) INHIBITORS
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Page/Page column 105, (2009/04/25)
This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such interm