# US 9,775,348 B2 · Composition comprising a sesterterpene and use thereof as antibiotic and antifungal adjuvant

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- Number: US 9,775,348 B2
- Document ID: US9775348B2
- Status: Granted
- Kind: B2
- Application number: 14/408,553
- Filed: 2013-06-25
- Published: 2015-07-16
- Granted: 2017-10-03
- Earliest claimed: 2012-06-25
- Assignees: Rode Pharma S.R.L.
- Applicants: Rode Pharma S.R.L.
- Inventors: Luigi Amelotti; Lorenzo Secondini
- Web page: https://patentgrep.com/patent/US9775348B2

## CPC

- A01N 37/08: containing carboxylic groups or thio analogues thereof, directly attached by the carbon atom to a cycloaliphatic ring; Derivatives thereof
- A01N 35/06: containing keto or thioketo groups as part of a ring, e.g. cyclohexanone, quinone; Derivatives thereof, e.g. ketals
- A01N 43/653: 1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 31/04: Antibacterial agents
- A61P 31/10: Antimycotics
- A61P 31/12: Antivirals
- 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
- 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
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention relates to a composition comprising at least a sesterterpene for use as medicament like antibiotic or antifungal. Furthermore, the present invention relates to the use of at least a sesterterpene for increasing, assisting and/or enhancing the bacteriostatic and/or bactericidal activity of an antibiotic or the fungicidal activity of an antifungal compound.

## Claims

### Claim 1

A method for treating a subject, the method comprising: administering to the subject a terpene selected from the group consisting of gascardic acid and a salt thereof, geranyl pyrophosphate and geranylfarnesol pyrophosphate in an effective amount to treat bacteria, fungi or infections caused therefrom in the subject, wherein the bacteria are selected from the group consisting of Staphylococcus aureus, Staphylococcus aureus subsp rosen and Staphylococcus epidermidis, Pseudomonas, Escherichia coli, Bacillus, Proteus vulgaris, Legionella, Salmonella, Listeria monocytogenes, Clostridium difficile, Streptococcus pyogenes, Enterococcus fecaiis, Enterococcus hirae, and Kiebsielia pneumoniae; and the fungi are selected from the group consisting of Aspergillus niger, Aspergillus versicolor and Aspergillus clavatus, Candida albicans, Trichoderma, Peniciiiiurn funirolosum, Chaetoimium giobosum, Fusarium rubrum, Fusarium oxysoorum, Fusarium solani, Puliularia fermantans and Rhizoous spp.

### Claim 2 (depends on 1)

The method of claim 1, wherein said terpene is combined with an antibiotic for increasing a bacteriostatic or bactericidal activity or efficacy of said antibiotic.

### Claim 3 (depends on 1)

The method of claim 1, wherein the terpene is in combination with an antifungal for increasing a fungicidal activity or efficacy of said antifungal.

### Claim 4 (depends on 1)

The method of claim 1, wherein said terpene is combined with at least a second terpene selected from ophiobolin A, ophiobolin B and ceroplastol.

### Claim 5 (depends on 1)

The method of claim 1, wherein said terpene is combined with betulinic acid or a salt thereof.

### Claim 6 (depends on 5)

The method of claim 5, wherein said terpene and said betulinic acid or a salt thereof are in a weight ratio from 1:5 to 5:1.

### Claim 7 (depends on 1)

The method of claim 1, wherein said terpene is combined with a steroidal pentacyclic triterpene.

### Claim 8 (depends on 1)

The method of claim 1, wherein said terpene is combined with friedelin or a salt thereof, and, wherein said terpene or a salt thereof and said friedelin or a salt thereof are in a weight ratio from 1:5 to 5:1.

### Claim 9 (depends on 1)

The method of claim 1, wherein said terpene is combined with betulinic acid or a salt thereof, and with a steroidal pentacyclic triterpene.

### Claim 10 (depends on 9)

The method of claim 9, wherein said terpene, said betulinic acid or a salt thereof and said steroidal pentacyclic triterpene are in a weight ratio of 1:1:1.

### Claim 11 (depends on 4)

The method of claim 4, wherein the second terpene is ophiobolin A.

### Claim 12 (depends on 6)

The method of claim 6, wherein said terpene or a salt thereof or a derivative thereof and said betulinic acid or a salt thereof are in a weight ratio from 1:3 to 3:1.

### Claim 13 (depends on 7)

The method of claim 7, wherein the steroidal pentacyclic triterpene is friedelin or a salt thereof.

### Claim 14 (depends on 8)

The method of claim 8, wherein said terpene or a salt thereof and said friedelin or a salt thereof are in a weight ratio from 1:3 to 3:1.

### Claim 15 (depends on 1)

The method of claim 1, wherein the Pseudomonas is Pseudomonas aeruginosa, the Bacillus is Bacillus cereus and the Trichoderma is Trichoderma viride or Trichoderma viridescens.
