Patent ID: 6919441
Filing Date: 2005-07-19
Classification: A61K,C07H,C07K

Abstract:
1. A polyamide-oligonucleotide derivative of the formula Ia or a physiologically tolerated salt thereof wherein q=r=s=1 and t=zero; R B is, independently of one another, a base customary in nucleotide chemistry or a prodrug form thereof, and the “curved bracket” indicates that R Nu is a radical of the formulae IIa or IIb wherein R U is hydroxyl, mercapto, C R R R V is oxy, thio or imino; W is oxo or thioxo; Y is oxy, thio, methylene or imino; m is zero to 20; o is zero to 20; D is a radical of the formula III wherein B is as defined above; n is zero to 20; p is zero to 20; Li where, independently of one another, ε is 1 to 5, V′ is oxygen, NH, a bond or a radical of the formula VI wherein U, V, W and Y are as defined above; G is C G′ is oxy, thio, imino, —C(O)—, —C(O)NH—, a bond or a radical of the formula VI in which U, V, W and Y are as defined above; and F and F′ are linked by a bond to form cyclic compounds, or F and F′ are end groups that cleave or crosslink nucleic acids; or F is R F′ is -(Q) R R A and Q are, independently of one another, the residue of a natural or unnatural amino acid; Q V is as defined above; V′ is a bond or V; k is zero to 10; I is zero to 10; with the proviso that a) if in the compound of the formula Ia t is zero and s is 1, and Li b) if in the compound of the formula Ia s=t=zero, Li where each nucleotide can be in its D configuration, and the base can be in the α or β position.