Compounds
AssigneesCantab Anti-Infectives Limited, Novacta Biosystems Limited
InventorsMona Saadi, Esther Duperchy, Pamela Brown, Michael John Dawson, Sjoerd Nicolaas Wadman
Life of this patent
Estimating the term…
Abstract
Provided are compounds, the use of the said compounds in treatment, for example treatment of microbial infections, particularly by Gram negative bacteria. The compounds are polymyxin-based and are represented by the formula (I): and pharmaceutically acceptable salts thereof, where X is —NHC(O)—, —C(O)—, —OC(O)—, —CH2— or —SO2—; R5 represents C0-12 alkyl(C4-6 heterocyclyl), or C2-12 alkyl or C0-12 alkyl(C3-8 cycloalkyl). and the alkyl or cycloalkyl bears one, two or three hydroxyl groups, or a —NR6R7 group, or one —NR6R7 group and one or two hydroxyl groups; and R1 to R4 and R6 to R8 are as defined in the description.
Claims16
A compound of the formula (I):
- wherein:
- X represents an —NHC(O)—, —C(O)—, —OC(O)—, —CH2— or —SO2—;
- and
- R1 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, represents a phenylalanine, leucine or valine residue;
- R2 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, represents a leucine, iso-leucine, phenylalanine, threonine, valine or nor-valine residue;
- R3 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, represents a threonine or leucine residue;
- R4 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, represents α,γ-diaminobutyric acid or a serine residue;
- R5 represents
- C0-12 alkyl(C4-6 heterocyclyl), or
- C2-12 alkyl or C0-12 alkyl(C3-8 cycloalkyl) wherein the alkyl or cycloalkyl bears:
- i) one, two or three hydroxyl groups, or
- ii) a —NR6R7 group, or
- iii) one —NR6R7 group and one or two hydroxyl groups,
- R6 represents hydrogen or C1-4 alkyl;
- and
- R7 represents hydrogen or C1-4 alkyl,
- R8 represents hydrogen or methyl, or
- a pharmaceutically acceptable salt thereof.
-14. (canceled)
A method according to claim 17 where the bacterium is multidrug resistant.
A method according to claim 17 where the bacterium is Gram negative.
Dependencies are inferred from the claim text.