Patent ID: 8642535
Filing Date: 2014-02-04
Classification: A61K,A61P,C07K,C12Q,G01N,Y02A

Abstract:
1. A polymyxin derivative of formula (I): wherein: A is a polymyxin ring moiety having the following formula: wherein R4 of the polymyxin ring moiety is an amino acid residue selected from the group consisting of lysine, hydroxylysine, ornithine, glutamate, aspartate, an α,γ-diamino-n-butyryl residue, diaminopropionic acid, threonine, cysteine and serine; R6 is an amino acid residue selected from the group consisting of D-phenylalanine, D-leucine and D-tryptophan; R7 is an amino acid residue selected from the group consisting of leucine, threonine, phenylalanine, isoleucine, serine, alanine, valine, norvaline, and tryptophan; R10 is an amino acid residue selected from the group consisting of leucine, threonine, serine, O-acetyl-threonine, O-propionyl-threonine and O-butyryl-threonine; and wherein R5, R8 and R9 are amino acid residues independently selected from the group consisting of an α,γ-diamino-n-butyryl residue, lysine, 2-amino-4-guanido butyric acid, an α-aminobutyryl residue, and threonine; D is R m Q W R R and pharmaceutically acceptable prodrugs and salts thereof wherein said derivative has three positive charges at physiological pH; and provided that at least one of m