Abstract: The present invention relates to oligoribonucleotide derivatives which have a 2?5?-linked oligoribonucleotide residue without a 5?-phosphate residue on the 3? end and to the use thereof for specific inhibition of gene expression.

Abstract: The invention relates to a class of CpG immunostimulatory oligonucleotides containing a CpG immunostimulatory motif and a second motif which is capable of forming secondary structure, including duplex and higher order structures, in vitro and in vivo. The oligonucleotides of the invention are useful as adjuvants in vaccination. The oligonucleotides are also useful for inducing an immune response, inducing expression of a type I interferon (IFN), inducing expression of gamma interferon (IFN-?), and for treating a variety of conditions, including allergy, asthma, infection, and cancer.

Abstract: Novel oligonucleotides having immune inhibitory effects, and methods for their use, are provided. The inhibitory oligonucleotides include those that specifically inhibit certain Toll-like receptors, including TLR7, TLR8, and TLR9. Certain of the immunoinhibitory oligonucleotides inhibit a combination of TLRs selected from TLR7, TLR8, and TLR9. Inhibitors of TLR9 are characterized by a 5? CC dinucleotide appropriately spaced upstream of a G-rich oligomer. Inhibitors of TLR8 include specific simple dinucleotides and oligonucleotides ending at their 3? termini with the specific dinucleotides. TLR7 inhibitors include oligonucleotides having a phosphorothioate backbone. Also provided are combinations and conjugates involving the inhibitory oligonucleotides of the invention and other agents, where the other agents include TLR agonists and antigens.

Abstract: The invention provides polyamide-oligonucleotide derivatives of the formula: F[(DNA-Li)q(PNA-Li)r(DNA-Li)s(PNA)t]xF?. In the formula, q, r, s, and t are, independently of one another, zero or 1, where the total of two or more adjacent q, r, s, and t is greater than or equal to 2; and x is 1 to 20. In the formula, DNA is a nucleic acid such as DNA or RNA or a known derivative thereof. Li is a covalent linkage between DNA and PNA, where the covalent linkage comprises a bond or an organic radical with at least one atom from the series consisting of C, N, O, or S. PNA is a polyamide structure which contains at least one nucleotide base that is different from thymine. F and F? are end groups and/or are linked together by a covalent bond. The invention also provides physiologically tolerated salts of the above formula. The invention further provides a process for preparation of the polyamide-oligonucleotide derivatives of the invention as well as their use as pharmaceuticals, as gene probes, and as primers.

Abstract: Antisense oligonucleotides against tenascin for the treatment of vitiligo The invention relates to specific, optionally modified oligonucleotides having a length of up to 18 nucleotides, which correspond to sections of tenascin-coding sequences or can bind to these sequences, to their preparation and to the use thereof, for example for the specific inhibition of the expression of tenascin and for the production of pharmaceuticals which can be used for the treatment of vitiligo.

Abstract: The invention relates to a nucleic acid-lipophilic conjugates and methods for modulating an immune response using the conjugates. The lipophilic moiety associated with an immunostimulatory nucleic acid.

Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.

Abstract: The invention relates to specific, optionally modified oligonucleotides with a length of up to 17 nucleotides. Said oligonucleotides correspond to segments of tenascin-coding sequences or can bind to these sequences. The invention also relates to the production and use of the oligonucleotides, for example for the specific inhibition of the expression of tenascin and for producing medicaments used to treat vitiligo.

Abstract: A mini-proinsulin, in which the amino acid Arg bridges the A and the B chain instead of the C chain, shows insulin activity and is suitable for the preparation of pharmaceuticals for the treatment of diabetes mellitus. It can furthermore be converted into an insulin derivative simply using trypsin, the B chain of which is lengthened by Arg. This can be converted into insulin using carboxypeptidase B. Advantageously, however, the mini-proinsulin can also be converted to insulin directly in a one-pot process.

Abstract: The invention relates to a class of soft or semi-soft CpG immunostimulatory oligonucleotides that are useful for stimulating an immune response.

Abstract: Polyamide-oligonucleotide derivatives of the formula F[(DNA-Li)q(PNA-Li)r(DNA-Li)s(PNA)t]xF? wherein q, r, s, t are, independently of one another, zero or 1, where the total of two or more adjacent q, r, s and t?2; x is 1 to 20; DNA is a nucleic acid such as DNA or RNA or a known derivative thereof; Li is a covalent linkage between DNA and PNA, where the covalent linkage comprises a bond or an organic radical with at least one atom from the series consisting of C, N, O or S; PNA is a polyamide structure which contains at least one nucleotide base which is different from thymine; and F and F? are end groups and/or are linked together by a covalent bond, and the physiologically tolerated salts thereof, a process for their preparation and their use as pharmaceutical, as gene probe and as primer, are described.

Abstract: The invention relates to a specific modified oligonucleotide complementary to a section of the human Ha-ras gene and mRNA, and its use to specifically regulate, modulate or inhibit expression of the HA-ras gene, and its use as a pharmaceutical for the treatment of conditions arising from the abnormal expression of the Ha-Ras gene, in particular in combination with chemotherapy and radiotherapy.

Abstract: The present application relates to oligonucleotides which inhibit expression of the OB-RGRP protein and to uses thereof for preventing and/or treating leptin-related pathological conditions. It also relates to a method for detecting compounds which modify the interaction between proteins of the OB-RGRP family and the leptin receptor. This detection may be carried out by measuring the energy transfer between fusion proteins composed of these proteins and of energy-donor and -acceptor proteins.

Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.

Abstract: The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.

Abstract: The invention relates to a class of CpG immunostimulatory oligonucleotides containing a 5′TCG motif or a CG at or near the 5′ end that are useful for stimulating an immune response.

Abstract: The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.

Abstract: The invention relates to a specific modified oligonucleotide complementary to a section of the human Ha-ras gene and mRNA, and its use to specifically regulate, modulate or inhibit expression of the HA-ras gene, and its use as a pharmaceutical for the treatment of conditions arising from the abnormal expression of the Ha-Ras gene, in particular in combination with chemotherapy and radiotherapy.

Abstract: Polyamide-oligonucleotide derivatives of the formula

Abstract: The present invention relates to an antisense oligonucleotide or a derivative thereof which has a sequence that corresponds to a part of a nucleic acid which encodes an integrin &agr;v subunit and which has the ability to induce apoptosis, the preparation and the use thereof.