US2016206680A1PendingUtilityA1
Anti-trypanosome compounds and treatments
Est. expiryMar 20, 2029(~2.7 yrs left)· nominal 20-yr term from priority
A61K 38/08A61P 33/02A61K 31/185C07K 7/06A61K 31/155A61K 38/00A61K 31/555Y02A50/30A61P 33/00
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Claims
Abstract
A novel structural class of highly N-methylated linear lipopeptide compounds useful for the treatment of parasitic disease.
Claims
exact text as granted — not AI-modified1 - 13 . (canceled)
14 . A method for affecting the physiology of a trypanosome, the method comprising exposing the pathogen to an almiramide compound, the almiramide compound comprising a linear lipopeptide having the following structure
but specifically excluding compounds (1), (2) and (3)
wherein for (1), R 1 consists of
R 2 consists of Me, R 3 consists of H, and R 4 consists of NH2;
and wherein for (2), R 1 consists of
R 2 consists of Me, R 3 consists of H, and R 4 consists of NH2;
and wherein for (3), R 1 consists of
R 2 consists of Me, R 3 consists of H, and R 4 consists of NH2.
15 . The method of claim 14 wherein R 1 is selected from one of the following moieties:
and wherein R 2 is selected from one of the following moieties: Me or H
and wherein R 3 is selected from one of the following moieties: Me or H
and wherein R 4 is selected from one of the following moieties: NH 2 , NMe 2 , OH, OMe.
16 . The method of claim 14 wherein the almiramide compound is selected from the group consisting of compounds 2, 3, 11, 12, 13, 14, 15 and 16 as shown below:
Compound
R 1
R 2
R 3
R 4
2
Me
H
NH 2
3
Me
H
NH 2
11
Me
Me
NH 2
12
Me
Me
NMe 2
13
H
Me
NMe 2
14
H
Me
NMe 2
15
H
Me
NMe 2
16
H
Me
NMe 2
17 - 20 . (canceled)
21 . The method of claim 14 wherein the almiramide possesses anti-trypanosome properties.
22 . The method of claim 21 wherein the almiramide possesses anti-pathogenic properties against Trypanosoma gambiense.
23 . The method of claim 21 wherein the almiramide possesses anti-pathogenic properties against Trypanosoma rhodesiense.
24 . The method of claim 21 wherein the almiramide possesses anti-pathogenic properties against Trypanosoma brucei.
25 . The method of claim 21 wherein the almiramide molecule is selected from the group consisting of compound 13, compound 14, and compound 16.
26 . The method of claim 22 comprising additionally administering pentamidine.
27 . The method of claim 23 comprising additionally administering suramin.
28 . The method of claim 24 comprising additionally administering melarsoprol.Cited by (0)
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