# US 9,872,849 B2 · Diterpenoid membranolide compounds having anti-leishmania activity and uses thereof

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- Number: US 9,872,849 B2
- Document ID: US9872849B2
- Status: Granted
- Kind: B2
- Application number: 14/811,341
- Filed: 2015-07-28
- Published: 2016-02-04
- Granted: 2018-01-23
- Earliest claimed: 2014-08-01
- Assignees: University of South Florida
- Applicants: Bill J. Baker; Christopher G. Witowski; John Alan Maschek; Brian Vesely; Dennis E. Kyle
- Inventors: Bill J. Baker; Christopher G. Witowski; John Alan Maschek; Brian Vesely; Dennis E. Kyle
- Web page: https://patentgrep.com/patent/US9872849B2

## CPC

- A61K 31/365: Lactones
- A61K 31/343: condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
- A61K 31/366: having six-membered rings, e.g. delta-lactones
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

In a screening program, the Antarctic sponge Dendrilla membranosa was found to produce diterpenoid secondary metabolites with activity against the leishmaniasis-causing parasite Leishmania donovani. The present invention concerns compositions useful for control of Leishmania spp. parasites in vitro and in vivo and treatment of leishmaniasis; methods for treatment of leishmaniasis; and methods for controlling Leishmania spp. parasites in vitro and in vivo.

## Claims

### Claim 1

A composition comprising at least one anti-Leishmania agent; and at least one other compound having the following chemical structure:
or a pharmaceutically acceptable salt thereof; or,
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the at least one anti-Leishmania agent is an antimonial, amphotericin B, miltefosine, pentamidine, aminoglycoside-amino-cyclitol antibiotic, azole, 4-methyl-6-methoxy-8-aminoquinoline, or nucleoside analogue, or a combination thereof.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the at least one other compound has the following chemical structure:
or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 3)

The composition of claim 3, wherein the at least one anti-Leishmania agent is an antimonial, amphotericin B, miltefosine, pentamidine, aminoglycoside-amino-cyclitol antibiotic, azole, 4-methyl-6-methoxy-8-aminoquinoline, or nucleoside analogue, or a combination thereof.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the at least one other compound has the following chemical structure:
or a pharmaceutically acceptable salt thereof.

### Claim 6 (depends on 5)

The composition of claim 5, wherein the at least one anti-Leishmania agent is an antimonial, amphotericin B, miltefosine, pentamidine, aminoglycoside-amino-cyclitol antibiotic, azole, 4-methyl-6-methoxy-8-aminoquinoline, or nucleoside analogue, or a combination thereof.

### Claim 7 (depends on 1)

The composition of claim 1, wherein the at least one other compound comprises a compound having the chemical structure:
or a pharmaceutically acceptable salt thereof; and a compound having the chemical structure:
or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 7)

The composition of claim 7, wherein the at least one anti-Leishmania agent is an antimonial, amphotericin B, miltefosine, pentamidine, aminoglycoside-amino-cyclitol antibiotic, azole, 4-methyl-6-methoxy-8-aminoquinoline, or nucleoside analogue, or a combination thereof.
