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US 8,765,722 B2Granted
Inhibitors of flaviviridae viruses
AssigneeGilead Sciences, Inc.
InventorsAesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
Life of this patent
Estimating the term…
Abstract
Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
Claims27
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is -(L1)m-(L2)n-X1;
- L1 is selected from the group consisting of alkynylene and arylene;
- m is 1;
- L2 is selected from the group consisting of —NHC(O)— and alkylene;
- n is 0 or 1;
- X1 is selected from the group consisting of
- a) —P(O)RxRy,
- b) —P(O)ORxRy,
- c) —OP(O)RxRy and
- d) optionally substituted C1-12 alkyl, and 5-10 membered heteroaryl comprising one to three nitrogen atoms;
- each of Rx and Ry independently is selected from the group consisting of H, C1-12 alkyl, and C6-14 aryl;
- when X1 is selected from d) and is substituted, X1 is substituted with one or more halogen;
- R2 is optionally substituted C3-12 cycloalkyl;
- wherein, when R2 is substituted, R2 is substituted with one or more Q2;
- where each Q2 individually is selected from the group consisting of —OH, and optionally substituted C1-6 alkyl;
- when Q2 is substituted, Q2 is substituted with one or more halogen;
- R3 is -(L3)p-(L4)q-(X3);
- L3 is selected from the group consisting of optionally substituted C1-12 alkylene, optionally substituted C3-12 cycloalkylene and optionally substituted 5-6 membered N-containing heterocyclylene;
- p is 0 or 1;
- when L3 is substituted, L3 is substituted with one or more Q3,
- each Q3 individually is selected from the group consisting of —OH and C1-6 alkyloxy;
- L4 is selected from the group consisting of —NH—, and C1-12 alkylene;
- q is 0, 1 or 2;
- X3 is selected from the group consisting of:
- e) —P(O)RxRy,
- f) —P(O)ORxRy,
- g) —OP(O)RxRy,
- h) —P(O)(ORx)(ORy),
- wherein each A is a 4 to 6 membered ring, including the depicted P atom, and
- k) optionally substituted C3-12 cycloalkyl, and optionally substituted 3-12 membered heterocyclyl;
- each of Rx and Ry individually is as defined above;
- and
- when X3 is selected from k) and is substituted, X3 is substituted with one —OH;
- provided that when X1 is selected from d), then X3 is selected from the group consisting of e), f), g), h), and i).
32 more elements
Dependencies are inferred from the claim text.