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US 12,552,820 B2Granted
Benzyloxy phosph(on)ate compounds
AssigneeLigand Pharmaceuticals Incorporated
InventorLin Zhi
Life of this patent
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Abstract
Provided herein are 2-substituted benzyloxy phosph(on)ate compounds, their preparation and their uses, such as treating liver diseases or conditions.
Claims22
A compound of Formula I:
- wherein:
- R1 is selected from the group consisting of —CH(OR6)2, —C(O)N(R6)2, —CH2OR7, CH2SR7, —CH2N(R7)2, —CH2OCH2OR6, —COOR5, and
- each R2 is independently selected from the group consisting of halogen, an optionally substituted alkyl, and an optionally substituted alkyloxy;
- R3 is selected from the group consisting of H, an optionally substituted aryl, and a therapeutic or diagnostic moiety;
- R4 is selected from a nucleoside or a nucleoside base or analog thereof, or alternatively, R4 and R3 together with the atoms to which they are attached form a monocyclic heterocyclyl substituted with a nucleoside base or analog thereof, or R4 and R5 together with the atoms to which they are attached form a heterocyclyl substituted with a nucleoside base or analog thereof, wherein the nucleoside base or analog thereof is selected from the group consisting of:
- R5 is H or an optionally substituted alkyl;
- each R6 is independently an optionally substituted alkyl;
- R7 is selected from the group consisting of H, an optionally substituted C1-C10 acyl, an optionally substituted C1-C10 alkyl-OC(O)—, an optionally substituted (C6-10 aryl)-C(O)—, and an optionally substituted (C6-10 aryl)-OC(O)—;
- R9 is H, halo, or an optionally substituted C1-C10 alkyl;
- R10 is selected from the group consisting of H, an optionally substituted C1-C10 alkyl, an optionally substituted C1-C10 alkyl-OCH2—, an optionally substituted C1-C10 alkyl-NHCH2—, an optionally substituted C1-C10 acyl, an optionally substituted C1-C10 alkyl-OC(O)—, an optionally substituted (C6-10 aryl)-CH2OCH2—, an optionally substituted (C6-10 aryl)-OCH2—, an optionally substituted (C6-10 aryl)-C(O)—, and an optionally substituted (C6-10 aryl)-OC(O)—;
- R11 is selected from the group consisting of OH, NH2, NHOR7, an optionally substituted C1-C10 alkyloxy, an optionally substituted C1-C10 alkylamino, an optionally substituted C1-C10 acyloxy, an optionally substituted C1-C10 acylamino, an optionally substituted C1-C10 alkyl-OC(O)NH—, an optionally substituted (C6-10 aryl)-C(O)O—, an optionally substituted (C6-10 aryl)-C(O)NH—, an optionally substituted (C6-10 aryl)-OC(O)NH—, an optionally substituted C1-C10 alkyl-OCH2NH—, and an optionally substituted C1-C10 alkyl-OCH2O—;
- and
- R12 is selected from a group of H, NH2, an optionally substituted C1-C10 alkylamino, an optionally substituted C1-C10 acylamino, an optionally substituted C1-C10 alkyl-OC(O)NH—, an optionally substituted (C6-10 aryl)-C(O)NH—, an optionally substituted (C6-10 aryl)-OC(O)NH—, and an optionally substituted C1-C10 alkyl-OCH2NH—;
- and
- n is 0, 1, 2, or 3;
- or a stereoisomer or pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.