Patent ID: 9029569
Filing Date: 2015-05-12
Classification: A61K,A61M,A61P,C07B,C07D

Abstract:
1. A method of reducing a reduction-activated prodrug, the method comprising contacting the reduction-activated prodrug with a compound of formula I, or a dimer thereof, wherein the reduction-activated prodrug is tretazicar (5-(aziridin-1-yl)-2,4-dinitrobenzamide), and wherein the reduction-activated prodrug tretazicar (5-(aziridin-1-yl)-2,4-dinitrobenzamide) is reduced to give more 5-(aziridin-1-yl)-4-hydroxylamino-2-nitrobenzamide than 5-(aziridin-1-yl)-2-hydroxylamino-4-nitrobenzamide, and wherein the compound of formula I has the structure: wherein R wherein R wherein aryl is a C wherein Het is a 4- to 14-membered heterocyclic group comprising one, two, or three rings, and comprising one or more heteroatoms independently selected from oxygen, nitrogen, and sulfur, wherein the heterocyclic group is optionally substituted by one or more substituents selected from halo, C wherein the compound of formula I is capable of forming a cyclic dimer of formula Ia: wherein R wherein the reduction is carried out at a temperature from ambient to 70° C.; and: