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US 2017/0247423 A1Published application
Stapled intracellular-targeting antimicrobial peptides to treat infection
AssigneeDana-Farber Cancer Institute, Inc.
InventorsLoren D. Walensky, Rida Mourtada
Life of this patent
Estimating the term…
Abstract
Structurally stabilized, e.g., stapled, peptides with the ability to translocate through microbial cell membranes to the interior of microbial cells and exert a biological activity there are provided, as are methods of designing, making and using such peptides.
Claims36
A compound having the formula:
- or a pharmaceutically acceptable salt thereof,
- wherein;
- each R1 and R2 is independently H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkylalkyl, heteroarylalkyl, or heterocyclylalkyl, any of which is substituted or unsubstituted;
- each R3 is independently alkylene, alkenylene, or alkynylene, any of which is substituted or unsubstituted;
- each x is independently 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- each w and y is independently 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20;
- z is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- and
- each Xaa is independently an amino acid,
- wherein the compound exhibits an intracellular antimicrobial effect against at least one microbe.
7 more elements
A method of treating an infection caused by a microbe, the method comprising administering a therapeutically-effective amount of a compound having the formula:
- or a pharmaceutically acceptable salt thereof,
- wherein;
- each R1 and R2 is independently H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkylalkyl, heteroarylalkyl, or heterocyclylalkyl, any of which is substituted or unsubstituted;
- each R3 is independently alkylene, alkenylene, or alkynylene, any of which is substituted or unsubstituted;
- each x is independently 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- each w and y is independently 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20;
- z is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- and
- each Xaa is independently an amino acid,
- to a subject having, or at risk of having, the infection caused by the microbe, wherein the compound exhibits an intracellular antimicrobial effect against at least one microbe.
7 more elements
A pharmaceutical composition comprising a compound having the formula:
- or a pharmaceutically acceptable salt thereof,
- wherein;
- each R1 and R2 is independently H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkylalkyl, heteroarylalkyl, or heterocyclylalkyl, any of which is substituted or unsubstituted;
- each R3 is independently alkylene, alkenylene, or alkynylene, any of which is substituted or unsubstituted;
- each x is independently 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- each w and y is independently 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20;
- z is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;
- and
- each Xaa is independently an amino acid,
- wherein the compound exhibits an intracellular antimicrobial effect against at least one microbe.
7 more elements
Dependencies are inferred from the claim text.