Vancomycin derivatives with siderophore modification as novel repurposed antibiotics to combat gram-negative bacterial infection
AssigneeResearch Triangle Institute
InventorsChunyang JIN, Bruce Edward BLOUGH, Dongliang GUAN
Life of this patent
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Abstract
The present disclosure provides novel vancomycin derivatives that act as antimicrobials against Gram-negative bacteria. The compounds of the present disclosure are believed to be useful for the treatment of diseases caused by antimicrobial resistant bacteria, including Acinetobacter baumannii and Escherichia coli.
Claims57
A compound of Formula (1) or a pharmaceutically acceptable salt thereof:
- wherein:
- (i) R1 is
- and each of R2, R3, and R4, is H;
- (ii) R1 is
- and each of R2, R3, and R4, is H;
- (iii) R1 is
- and each of R2, R3, and R4, is H;
- (iv) R1 is
- and each of R2, R3, and R4, is H;
- (v) R1 is OH;
- R2 is
- and each of R3 and R4 are H;
- (vi) R1 is OH;
- R3 is
- and each of R2 and R4 are H;
- or
- (vii) R1 is OH;
- R4 is
- and each of R2 and R3 are H;
- and wherein:
- X1 is a bond or
- X2 is a bond or
- X3 is a bond or
- X4 is a bond or
- Y1 is C(O) or SO2;
- Y2 is C(O) or SO2;
- Y3 is C(O) or SO2;
- n1 is 1-5;
- n2 is 1-10;
- n3 is 0-5;
- n4 is 1-5;
- n5 is 1-5;
- n6 is 1-10;
- n7 is 0-5;
- n8 is 0-5;
- n9 is 0-5;
- n10 is 0-5;
- n11 is 0-5;
- R5 is selected from the group consisting of hydrogen, halogen, and OH;
- R6 is selected from the group consisting of hydrogen, halogen, and OH;
- R7 is selected from the group consisting of hydrogen, halogen, and OH;
- R8 is selected from the group consisting of hydrogen, halogen, and OH;
- R9 is selected from the group consisting of hydrogen, halogen, and OH;
- R10 is selected from the group consisting of hydrogen, halogen, and OH;
- R11 is selected from the group consisting of hydrogen, halogen, and OH;
- R12 is selected from the group consisting of hydrogen, halogen, and OH;
- R13 is selected from the group consisting of hydrogen, halogen, and OH;
- R14 is selected from the group consisting of hydrogen, halogen, and OH;
- R15 is selected from the group consisting of hydrogen, halogen, and OH;
- R16 is selected from the group consisting of hydrogen, halogen, and OH;
- R17 is selected from the group consisting of hydrogen, halogen, and OH;
- R18 is selected from the group consisting of hydrogen, halogen, and OH;
- R19 is selected from the group consisting of hydrogen, halogen, and OH;
- R20 is selected from the group consisting of hydrogen, halogen, and OH;
- and R21 is selected from the group consisting of hydrogen, halogen, and OH.
The compound of claims 1 and 39, wherein n10 is 1, n11 is 0, X4 is a bond, R19 is Cl, R20 is OH, R21 is OH, R22 is H, and R23 is H.
A compound or a pharmaceutically acceptable salt thereof selected from the group consisting of
- Com-
- pound #
- Compound
- 1
- 2
- 3
- 4
- 5
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- 8
- 9
- 10
- 11
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- 19
- 20
- 21
- 22
- 23
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- 25
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- 31
- 32
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.