Patent ID: 7550582
Filing Date: 2009-06-23
Classification: A61K,A61P,C07K,Y10T

Abstract:
1. A process for preparing a PNA derivative of Formula I wherein q is 0; D′ is, independently of each other, hydroxyl, mercapto, amino, alkylamino, or acylamino; V is oxygen, sulfur, or NR V′ is, independently of any other V′, oxygen, sulfur, NR U is, independently of any other U, oxygen, sulfur, or NH; u′ is, independently of any other u′, from 1 to 10; W and W′ are, independently of each other, oxygen, sulfur, or NR Y and Y′ are, independently of each other, hydroxyl, mercapto, oxyanion, thioate, or NR X and X′ are, independently of each other, Z and Z′ are, independently of each other, R R n is from 0 to 10; m is from 0 to 10; and wherein {POLY} is described by Formula II wherein {BLOCK} is, independently of any other {BLOCK}, a group selected from Formula IIIA, Formula IIIB, and Formulae IV A to IV G, wherein each {BLOCK} building block can be different, and wherein z″ is from 0 to 100; G is (CR A is, independently of any other A, a group (CR B is, independently of any other B, either an aromatic radical, a heteroaromatic radical, hydrogen, hydroxyl, or C D is, independently of any other D, a group (CR E is, independently of any other E, a group (CR R wherein R and physiologically tolerated salts of the PNA derivative of Formula I, with the provisos that at least one Y, Y′, Z, or Z′ radical is hydroxyl, mercapto, oxyanion, or thioate, and that at least one B radical is a nucleobase; said process comprising