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US 11,535,648 B2Granted
Isolated darobactin A analog compounds and compositions thereof
AssigneeNortheastern University
InventorsKim Lewis, Yu Imai, Quentin Favre-Godal, Akira Iinishi, Kirsten Meyer
Life of this patent
Estimating the term…
Abstract
Embodiments of the present invention relate to a novel compound of Formula (I) or stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, for use in treatment of infection caused by Gram-negative bacteria.
Claims7
A compound of Formula (I):
- and/or a pharmaceutically acceptable salt, stereoisomer, tautomer, or hydrate thereof, wherein:
- R1, R2, R3, R4, R5, and R6 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, halogen, —CN, —O-alkyl, —C(O)-alkyl, —C(O)O-alkyl, —C(O)OH, —C(O)NH2, —C(O)NH-alkyl, —NH2, —NO2, —CF3, —NH-alkyl, —N-(alkyl)2, —NHC(O)-alkyl and aryl, wherein said alkyl, alkenyl, alkynyl and aryl are each optionally substituted;
- R7 and R8 are each independently selected from the group consisting of hydrogen, straight or branched C1-C5 alkyl, straight or branched C2-C6 alkenyl, straight or branched C2-C6 alkynyl;
- wherein said alkyl, alkenyl and alkynyl are each optionally substituted;
- R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19 and R20 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl, heteroaryl, haloalkyl, hydroxyl, hydroxyalkyl, halogen, —CN, —O-alkyl, —C(O)-alkyl, —C(O)O-alkyl, —C(O)OH, —C(O)N H2, —C(O)NH-alkyl, —NH2, —NO2, —CF3, —NH-alkyl, —NHC(O)-alkyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl, heteroaryl, haloalkyl are each optionally substituted;
- A is a bond or —(CH2)n—, wherein n is an integer between 0 and 10;
- and X is —C(O)—, —CH2—, —C(OH)—, —C(O)O-alkyl, —C((O)alkyl)-, with the provision that the compound of formula (I) is isolated in a substantially pure form from a microorganism;
- is encoded by a darA gene comprising at least one non-natural nucleotide substitution;
- and is neither naturally occurring nor the compound of formula (II):
6 more elements
Dependencies are inferred from the claim text.