Abstract: The present invention relates to oligonucleotide derivatives which are at least partly double-stranded and which have a 2′5′-linked oligonucleotide residue on at least one 3′ end and to the use thereof for specific inhibition of gene expression.

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 specific modified oligonucleotide complementary to a section of the human Hs-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 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 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 an oligonucleotide or a derivative thereof which has a sequence that corresponds to a particular fragment of a nucleic acid sequence which encodes human eg5 or a mutant form thereof; the invention further relates to a method of making the oligonucleotide and the use thereof.

Abstract: Oligonucleotides of the formula

Abstract: The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II) with a compound of Formula (III) a compound of Formula (V) B′—CH2—CO—R2  (V), a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII) B′—CH2—CO—R3  (VII), and converting the resulting compounds to that of Formula I.

Abstract: The invention relates to novel stabilized oligonucleotides in which at least one non-terminal pyrimidine nucleoside is modified, and to their use as a diagnostic or pharamaceutical for the treatment of viral infections, cancer or diseases in which integrins or cell-cell adhesion receptors are active.

Abstract: Novel oligonucleotide analogs of the formulae I and II in which A, B, D, R1, R2, T, U, V, W, X, Y, Z, a, b, m, m′, n and n′ have the meanings stated in the description, with valuable physical, biological and pharmacological properties, and a process for the preparation thereof are described. Application thereof relates to the use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex forming oligonucleotides), as probes for detecting nucleic acids and as aids in molecular biology.

Abstract: The invention provides compounds and processes for synthesis of peptide nucleic acids (PNA). The compounds include temporary amino protecting groups that are base-labile, and protection groups for the exocyclic amino function of the nucleotide base that is compatible with the base-labile amino protecting group. Cleavage of an oligomer comprising these compounds from a solid support can be achieved using weak or medium strength acids.

Abstract: VEGF (vascular endothelial growth factor) is a key regulator of angiogenesis, and agents that selectively decrease the VEGF levels may be used to treat malignancies and other angiogenic diseases characterized by high degree of vascularization or vascular permeability. A short oligonucleotide, or a derivative thereof, which has a sequence that corresponds to a particular part of a nucleic acid sequence which encodes VEGF, and which has a maximum length of 15 nucleotides, selectively inhibits VEGF expression. The invention further relates to a method of making the oligonucleotide and the use thereof.

Abstract: The preparation of L-2-amino-4-methylphosphinobutyric acid (L-PPT) by transamination of (3-carboxy-3-oxo-propyl)-methylphosphinic acid with the aid of the L-PPT-specific transaminase from E. coli DH 1 is very much more efficient when the gene coding for this enzyme is isolated, incorporated into the plasmid and then a microorganism is transformed therewith.

Abstract: Novel oligonucleotide analogs of the formula [I] are described, ##STR1## in which A, B, D, G, L, P, Q, Q', R.sup.5, R.sup.6, X, Y, Z and n are as defined in the description, which have useful physical, biological and pharmacological properties, as well as a process for their preparation. Their application relates to use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex-forming oligonucleotides), as probes for the detection of nucleic acids and as auxiliaries in molecular biology.

Abstract: Oligonucleotides of the formula:5'-(CAP)-(Oligo)-(CAP)-3'are disclosed where (oligo) is a nucleotide sequence of from 10 to 40 nucleotides in length, and CAP is G.sub.m, where m is an integer of from zero to ten, the two CAP's which are present in the molecule can be defined independently of each other and must be different in the case where m is zero at the 5' or 3' end and the end of the oligo sequence is other than guanine. The oligonucleotides can be synthesized chemically. The oligonucleotides are used to diagnose or treat cancer, restenosis, a disease caused by a virus, a disease affected by integrins or cell-cell adhesion receptor or a disease triggered by diffusible factors.

Abstract: PNA synthesis using a base-labile amino protecting group Processes are described for preparing PNA oligomers, ##STR1## in which R.sup.0 is hydrogen, alkanoyl, alkoxycarbonyl, cycloalkanoyl, aroyl, heteroaroyl, or a group which favors the intracellular uptake of the oligomer, A and Q are amino acid residues, k and 1 are 0 to 20, n is 1-50, B is a nucleotide base which is customary in nucleotide chemistry, and Q.sup.0 is OH, NH.sub.2, or alkylamino which can be substituted by OH or NH.sub.2. In these processes, the amino acid residues and the structural components ##STR2## in which PG is a base-labile amino protecting group and B' is a nucleotide base which is protected on its exocyclic amino function, are coupled step-wise, in accordance with the solid-phase method, onto a polymeric support which is provided with an anchor group, and, after the construction is complete, the target compounds are cleaved from the polymeric support using a cleaving reagent.

Abstract: There are described N-ethylglycine derivatives of the formula I ##STR1## in which PG is a urethane-type or trityl-type amino protective group which is labile to weak acids, X is NH, O or S, Y is CH.sub.2, NH or O, and B' are bases customary in nucleotide chemistry, the exocyclic amino or hydroxyl groups of which being protected by suitable, known protective groups, or are base substitute compounds, and their salts with tert-organic bases, as well as a process for their preparation. The N-ethylglycine derivatives of the formula I are used in the preparation of PNA and PNA/DNA hybrids.

Abstract: The present invention relates to a novel advantageous process for amplifying nucleic acids using DNA/PNA primers and a temperature-stable polymerase enzyme.

Abstract: The preparation of L-2-amino-4-methylphosphinobutyric acid (L-PPT) by transamination of (3-carboxy-3-oxopropyl)-methylphosphinic acid with the aid of the L-PPT-specific transaminase from E. coli DH 1 is very much more efficient when the gene coding for this enzyme is isolated, incorporated into a plasmid and then a microorganism is transformed therewith.

Abstract: PNA synthesis using an amino protective group which is labile to weak acids.