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US 11,117,915 B2Granted
Antibacterial aminoglycoside analogs
AssigneeCipla USA, Inc.
InventorsJames Bradley Aggen, Adam Aaron Goldblum, Martin Sheringham Linsell, Paola Dozzo, Heinz Ernst Moser, Darin James Hildebrandt, Micah James Gliedt
Life of this patent
Estimating the term…
Abstract
Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Claims30
A compound having the following structure (I):
- or a stereoisomer, or a pharmaceutically acceptable salt thereof,
- wherein:
- Q1 is hydrogen;
- Q2 is hydrogen, optionally substituted aryl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, —C(═NH)NR4R5, —(CR10R11)pR12,
- Q3 is hydrogen, optionally substituted aryl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, —C(═NH)NR4R5, —(CR10R11)pR12,
- each R1, R2, R3, R4, R5, R8 and R10 is, independently, hydrogen or C1-C6 alkyl, or R1 and R2 together with the atoms to which they are attached can form a heterocyclic ring having from 4 to 6 ring atoms, or R2 and R3 together with the atoms to which they are attached can form a heterocyclic ring having from 4 to 6 ring atoms, or R1 and R3 together with the atoms to which they are attached can form a carbocyclic ring having from 4 to 6 ring atoms, or R4 and R5 together with the atom to which they are attached can form a heterocyclic ring having from 4 to 6 ring atoms;
- each R6 and R7 is, independently, hydrogen, hydroxyl, amino or C1-C6 alkyl, or R6 and R7 together with the atoms to which they are attached can form a heterocyclic ring having from 4 to 6 ring atoms;
- each R9 is, independently, hydrogen or methyl;
- each R11 is, independently, hydrogen, hydroxyl, amino or C1-C6 alkyl;
- each R12 is, independently, hydroxyl or amino;
- each n is, independently, an integer from 0 to 4;
- each m is, independently, an integer from 0 to 4;
- and
- each p is, independently, an integer from 1 to 5, and
- wherein at least one of Q2 and Q3 is —C(═NH)NR4R5.
12 more elements
Dependencies are inferred from the claim text.