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US 2019/0055252 A1Published application
Compounds and methods for the treatment of malaria
AssigneeThe Broad Institute, Inc.
InventorsEAMON COMER, NOBUTAKA KATO, CHRISTINA SCHERER, JESSICA BASTIEN, JEREMY DUVALL, TIMOTHY LEWIS, MORGANE SAYES, MATTHEW LEIGHTY, JUN PU, JENNIFER BEAUDOIN, BERTRAND BRAIBANT, BENITO MUNOZ
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Abstract
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of malaria.
Claims19
A compound according to formula (VII):
- wherein o and p are independently 0, 1, 2, 3, 4, or 5;
- and
- Z is absent, C1-C6 alkylene, or C1-C6 heteroalkylene;
- R3 is hydrogen, —NR5R6′—C(O)R7, or C2-C9 heterocyclyl;
- R4 is hydrogen or C1-C6 alkyl;
- R5 and R6 are independently hydrogen, C1-C6 alkyl, or C1-C6 acyl;
- R7 is hydroxyl, C1-C6 heteroalkyl, or C2-C9 heterocyclyl;
- and
- R8 and R9 are independently hydrogen, halogen, or C1-C6 heteroalkyl.
6 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound having the structure:
- wherein the dotted line represents an optional double bond;
- m is 0 or 1;
- n is 0, 1, or 2;
- A is CH or N;
- X is absent or —C≡C—;
- R1 is hydrogen, C1-C6 alkyl, C1-C6 heteroalkyl, C6-C10 aryl, C3-C10 carbocyclyl, or C2-C9 heteroaryl;
- Y is C1-C6 alkylene, —C(O)NR4—;
- —SO2—, or —C(O)—;
- R2 is C1-C6 perfluoroalkyl, C6-C10 aryl, C6-C10 aryl C1-C6 alkyl, C3-C10 carbocyclyl, or C2-C9 heteroaryl;
- Z is absent, C1-C6 alkylene, or C1-C6 heteroalkylene;
- R3 is hydrogen, hydroxyl, —NR5R6, —C(O)R7, or C2-C9 heterocyclyl;
- R4 is hydrogen or C1-C6 alkyl;
- R5 and R6 are independently hydrogen, C1-C6 alkyl, or C1-C6 acyl;
- and
- R7 is hydroxyl, C1-C6 heteroalkyl, or C2-C9 heterocyclyl;
- or a pharmaceutically acceptable salt thereof;
- and
- a pharmaceutically acceptable excipient.
15 more elements
Dependencies are inferred from the claim text.