Patent ID: 6420546
Filing Date: 2002-07-16
Classification: A61P,C07H

Abstract:
An oligoribonucleotide of the formula I in which R1 is hydrogen or a radical of the formula II R2 is hydrogen or a radical of the formula III â€ƒbut where at least one of the radicals R1 or R2 is a radical of the formula II or III; B is a base such as, for example, natural bases such as adenine, thymine, cytosine, guanine or unnatural bases such as, for example, purine, 2,6-diaminopurine, 7-deazaadenine, 7-deazaguanine, N4,N4-ethanocytosine or their prodrug forms; R3 is, independently of one another, OH, hydrogen, O(C1-C18)alkyl, O(C2-C18)alkenyl, F, NH2 or its prodrug forms and N3, but at least one R3 radical is different from H, and R3 is preferably OH, hydrogen, O(C1-C6)alkyl, O(C2-C6)alkenyl, F, NH2 and very preferably OH; W and Wâ€² are, independently of one another, oxygen or sulfur; Z and Zâ€² are, independently of one another, Oâˆ’; Sâˆ’; C1-C18-alkoxy, preferably C1-C8-alkoxy, particularly preferably C1-C3-alkoxy, especially methoxy; C1-C18-alkyl, preferably C1-C8-alkyl, particularly preferably C1-C3-alkyl, especially methyl; NHR4, with R4=preferably C1-C18-alkyl, particularly preferably C1-C8-alkyl, especially C1-C4-alkyl or C1-C4-alkoxy-C1-C6-alkyl, preferably methoxyethyl; NR4R5, in which R4 is as defined above and R5 is preferably C1-C18-alkyl, particularly preferably C1-C8-alkyl, especially C1-C4-alkyl, or in which R4 and R5 are, together with the nitrogen atom carrying them, a 5-6-membered heterocyclic ring which may additionally contain another hetero atom from the series comprising O, S and N, such as, for example, morpholine; where X is OH, H, F, Cl, Br, NH2, N3, Oâ€”C(O)â€”(C1-C18)-alkyl, Oâ€”C(O)â€”(C2-C18)-alkenyl, Oâ€”C(O)â€”(C2-C18)alkynyl, Oâ€”C(O)â€”(C6-C18) aryl, Oâ€”(C1-C18)-alkyl, Oâ€”(C2-C18)-alkenyl, Oâ€”(C2-C18)alkynyl, Oâ€”(C1-C18)aryl, P(O)YYâ€², where Y and Yâ€² are defined as Z and Zâ€². R3 and X in formula II can together form a cyclic phosphoric diester; X is preferably OH, H, F, particularly preferably OH; n is an integer from 5-60, preferably 10-40 and especially preferably 15-25, and its physiologically tolerated salts.