# US 11,028,114 B2 · Amphotericin B derivatives with improved therapeutic index

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- Number: US 11,028,114 B2
- Document ID: US11028114B2
- Status: Granted
- Kind: B2
- Application number: 16/530,109
- Filed: 2019-08-02
- Published: 2020-01-02
- Granted: 2021-06-08
- Earliest claimed: 2013-10-07
- Assignees: The Board of Trustees of the University of Illinois
- Applicants: The Board of Trustees of the University of Illinois
- Inventors: Martin D. Burke; Stephen Davis; Brice E. Uno; Justin Struble; Ian Dailey; Kaitlyn C. Gray; David M. Knapp; Pulin Wang; Nagarjuna Palyam
- Web page: https://patentgrep.com/patent/US11028114B2

## CPC

- C07H 17/08: Hetero rings containing eight or more ring members, e.g. erythromycins
- A01N 43/90: having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
- A61P 31/10: Antimycotics
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- A01N: PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF (preservation of food or foodstuff A23); BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES (preparations for medical, dental or toiletry purposes which kill or prevent the growth or proliferation of unwanted organisms A61K); PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3′ or C4′ modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

## Claims

### Claim 1

A compound, or a pharmaceutically acceptable salt thereof, selected from the group consisting of:

### Claim 2 (depends on 1)

The compound of claim 1, wherein the compound is represented by:

### Claim 3 (depends on 1)

The compound of claim 1, wherein the compound is represented by:

### Claim 4 (depends on 1)

The compound of claim 1, wherein the compound is represented by:

### Claim 5 (depends on 1)

The compound of claim 1, wherein the compound is represented by:

### Claim 6 (depends on 1)

The compound of claim 1, wherein the compound is represented by:

### Claim 7 (depends on 1)

The compound of claim 1, wherein the compound is represented by:

### Claim 8 (depends on 1)

The compound of claim 1, wherein the compound is represented by:

### Claim 9 (depends on 1)

A pharmaceutical composition, comprising a compound of claim 1;
and a pharmaceutically acceptable carrier.

### Claim 10 (depends on 9)

The pharmaceutical composition of claim 9, wherein the pharmaceutical composition is an oral or intravenous dosage form.

### Claim 11 (depends on 9)

The pharmaceutical composition of claim 9, wherein the pharmaceutical composition is an oral dosage form.

### Claim 12 (depends on 9)

The pharmaceutical composition of claim 9, wherein the pharmaceutical composition is an intravenous dosage form.