US 2026/0103491 A1 · ARYL SUBSTITUTED POLYMYXIN DERIVATIVES

Abstract

The invention provides a polymyxin compound of formula (1) and salts, solvates and protected forms thereof, pharmaceutical compositions comprising the compounds of formula (1), and the use of the compounds and compositions in methods of treatment, such as methods for the treatment of microbial infections. The compounds of formula (1) are represented thus: wherein —R15 is a group: and —R16 is hydrogen; —R17 is hydrogen -L- is a covalent bond or methylene; and —Ar is optionally substituted aryl. The groups —X—, —R1, —R2, —R3, —R4, and —R8 are as defined herein.

Claims20

Dependent claims

A compound of formula (i):

wherein:
—X— represents —C(O)—;
—R1 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, is phenylalanine, leucine, norleucine, valine or norvaline residue;
—R2 is C1-4 alkyl optionally substituted with one hydroxyl group;
—R3 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, is a threonine residue;
—R4 together with the carbonyl group and nitrogen alpha to the carbon to which it is attached, is Dap;
—R8 is hydrogen or methyl;
and
—R15 is a group:
where:
—R16 is hydrogen;
—R17 is hydrogen:
-L- is a covalent bond or methylene;
—Ar is optionally substituted aryl, such as substituted phenyl
and salts, solvates and protected forms thereof.

12 more elements

Dependencies are inferred from the claim text.

Aryl substituted polymyxin derivatives

Life of this patent

Aryl substituted polymyxin derivatives

Life of this patent

Abstract

Claims20