# US 8,772,247 B2 · Anti-parasitic compounds

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- Number: US 8,772,247 B2
- Document ID: US8772247B2
- Status: Granted
- Kind: B2
- Application number: 13/256,498
- Filed: 2010-03-20
- Published: 2012-05-03
- Granted: 2014-07-08
- Earliest claimed: 2009-03-20
- Assignees: The Regents of the University of California
- Applicants: Roger Linington; Laura Sanchez
- Inventors: Roger Linington; Laura Sanchez
- Web page: https://patentgrep.com/patent/US8772247B2

## CPC

- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61P 33/00: Antiparasitic agents
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/185: Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids (hydroxamic acids A61K31/16; peroxy acids A61K31/327)
- A61K 31/555: containing heavy metals, e.g. hemin, hematin, melarsoprol
- A61P 33/02: Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- C07K 7/06: having 5 to 11 amino acids
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

A novel structural class of highly N-methylated linear lipopeptide compounds useful for the treatment of parasitic disease.

## Claims

### Claim 1

1 An almiramide molecule, comprising a linear lipopeptide having the following structure
but specifically excluding compounds (1), (2) and (3)
wherein for (1), R1 consists of
R2 consists of Me, R3 consists of H, and R4 consists of NH2:
and wherein for (2), R1 consists of
R2 consists of Me, R3 consists of H, and R4consists of NH2;
and wherein for (3), R1 consists of
R2 consists of Me, R3 consists of H, and R4 consists of NH2, and further,
wherein R1 is selected from one of the following moieties:
and wherein R2 is selected from one of the following moieties: Me or H
and wherein R3 is selected from one of the following moieties: Me or H
and wherein R4 is selected from one of the following moieties: NH2 , NMe2 , OH, OMe.

### Claim 2

An almiramide molecule, comprising a linear lipopeptide having the following structure
but specifically excluding compounds (1), (2) and (3)
wherein for (1), R1 consists of
R2 consists of Me, R3 consists of H, and R4 consists of NH2:
and wherein for (2), R1 consists of
R2 consists of Me, R3 consists of H, and R4 consists of NH2;
and wherein for (3), R1 consists of
R2 consists of Me, R3 consists of H, and R4 consists of NH2, and further, wherein said almiramide molecule is selected from the group consisting of compounds 4, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, and 24 as shown below:
Comp.
R1
R2
R3
R4
4
Me
H
NH2
11
Me
Me
NH2
12
Me
Me
NMe2
13
H
Me
NMe2
14
H
Me
NMe2
15
H
Me
NMe2
16
H
Me
NMe2
17
H
Me
OH
18
H
Me
OH
19
H
Me
OH
20
H
Me
OH
21
H
Me
OMe
22
H
Me
OMe
23
H
Me
OMe
24
H
Me
OMe.

### Claim 3 (depends on 2)

The almiramide molecule of claim 2 comprising an N—N-dimethyl-amide C-terminus.

### Claim 4 (depends on 2)

The almiramide molecule of claim 2 comprising at least one unsaturated terminus.