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US 10,016,436 B2Granted
Animal and human anti-malarial agents
AssigneeCelgene Corporation
InventorsStacie S. Canan, Natalie Anne Hawryluk
Life of this patent
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Abstract
Provided herein are Purine Comounds of Formula (I) or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.
Claims21
A Purine Compound of formula (I),
- or a pharmaceutically acceptable salt, tautomer, isotopologue, or stereoisomer thereof, wherein
- R1 is CR1aR1bR1c, wherein R1a and R1b are (C1-4)alkyl and R1c is H or (C1-4)alkyl;
- or R1a and R1b form a 3-6 membered cycloalkyl or 3-6 membered heterocyclyl, and R1c is H or (C1-4)alkyl;
- R2 is L-R2a or L-R2b,
- L is a bond or (C1-2 alkyl);
- R2a is 3-6 membered N-containing heterocyclyl or heteroaryl, each optionally substituted with one or more (C1-4)alkyl, or (C1-4)alkyl-NR2,
- R2b is (C1-4 branched or unbranched alkyl)-NR2,
- R3 is phenyl or pyridyl, substituted with at least one halogen, CN, (C1-4)alkyl, or O(C1-4)alkyl, wherein the alkyl is optionally fluorinated;
- and
- R is H or (C1-4) alkyl;
- provided the Purine Compound is not
- 4-(2-(isopropylamino)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-9-yl)pyrrolidin-2-one;
- N2-cyclopentyl-N8-(2-fluorophenyl)-9-(piperidin-4-yl)-9H-purine-2,8-diamine;
- or
- N2-cyclohexyl-N8-(2-fluorophenyl)-9-(piperidin-4-ylmethyl)-9H-purine-2,8-diamine.
12 more elements
Dependencies are inferred from the claim text.