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US 2013/0157979 A1Published application
Phosphate esters of gyrase and topoisomerase inhibitors
AssigneeVertex Pharmaceuticals Incorporated
InventorsYoussef Laafiret Bennani, Paul S. Charifson, Anne-Laure Grillot, Arnaud Le Tiran, Hardwin O'Dowd
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Abstract
The present invention relates to phosphate esters of compounds that inhibit bacterial gyrase and/or Topoisomerase IV and pharmaceutical compositions thereof. These phosphate esters are useful for treating bacterial infections.
Claims20
A compound of the formula (I):
- or a pharmaceutically acceptable salt thereof, wherein
- X is —PO(OH)O—R1, or —PO(O−M+)O—R1;
- M+ is a pharmaceutically acceptable monovalent cation;
- R1 is (C1-C20)-alkyl, (C2-C20)-alkenyl, —(CH2CH2O)nCH3, or R2;
- wherein said alkyl or alkenyl is optionally substituted with R2, —OR9, —N(R9)2, —CN, —C(O)OR9, —C(O)N(R9)2, —N(R9)—C(O)—R9, halogen, —CF3, or —NO2;
- each R2 is independently a 5-6 membered carbocyclic or heterocyclic aliphatic ring system;
- wherein any of said heterocyclic ring systems contains one or more heteroatoms selected from O, N, and N(R9);
- and wherein any of said ring systems optionally contains 1 to 4 substituents independently selected from —OH, C1-C4 alkyl, and —O—(C1-C4)-alkyl;
- each R9 is independently H or a C1-C4 alkyl group;
- and
- n is an integer 1 to 5.
8 more elements
Dependencies are inferred from the claim text.