Hoechst Aktiengesellschaft

Hoescht Aktiengesellschaft

Matthias Helsberg

Irvin Winkler

Eugen Uhlmann

Anuschirwan Peyman

Gerard J O'Malley

Gerhard Kretzschmar

Christoph Meichsner

Matthias Mag

Gerhard Jaehne

Jochen Knolle

Hans-Wolfram Fehlhaber

Herbert Kogler

Elmar Schrinner

Bimal N Ganguli

Michael Limbert

Joachim Betz

Laslo Vertesy

Ramaiyer R Chandran

Dieter-Andreas Sukatsch

Gerhard Gross

Thomas Scholl

Heinz H Anel

Gerhard J Ahne

Karlheinz Budt

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.

Stabilized oligonucleotides and their use

The invention relates to compounds of the formula I ##STR1## where R.sup.1 is H, alkyl, acyl, aryl, or a phosphate residue; R.sup.2 is H, OH, alkoxy, NH.sub.2, or halogen; B is a base customary in nucleotide chemistry; a is O or CH.sub.2 ; n is an integer from 1 to 100; W=O, S or Se; V=O, S, or NH; Y=O, S, NH, or CH.sub.2 ; Y'=O, S, NH, or alkylene; X=OH or SH; U=OH, SH, SeH, alkyl, alkoxy, aryl, aryloxy, or amine, and Z=OH, SH, SeH, an optionally substituted radical from the group comprising alkyl, aryl, heteroaryl, alkoxy, or amino, or a group which favors intracellular uptake or serves as the label of a DNA probe or attacks the target nucleic acid during hybridization, where if Z=OH, SH, CH.sub.3, or OC.sub.2 H.sub.5, at least one of the groups X, Y, Y', V, or W is not OH or O or R.sup.1 is not H; a process for their preparation and their use as inhibitors of gene expression, as probes for detecting nucleic acids and as aids in molecular biology.

Oligonucleotide analogs, their preparation and use

The present invention relates to novel oligonucleotide analogs with valuable physical, biological and pharmacological properties, and a process for their preparation.

3'-derivatized oligonucleotide analogs with non-nucleotidic groupings,

Cycloalkyltriols containing heterocyclic substituents, in particular cyclopentyl- and cyclohexyltriols containing heterocyclic substituents Compounds of the formulae I and II ##STR1## in which the substituents A, R.sup.1, R.sup.2 and R.sup.3 and n have the meanings given, have an antiviral and antiparasitic action.

Cycloalkltriols containing cyclic substituents, processes and

The invention relates to novel antisense oligonucleotides having the sequences ##STR1## and their mixtures, homologs or modified forms, against HSV 1.

Antisense oligonucleotides against HSV 1, and their preparation

Compounds 31668P and 31668U, a process for their production and their use. Compound 31668P and compound 31668U with the formulae ##STR1## have an antibiotic and an antitumor action.

Compounds 31668P and 31668U, a process for their production and their use

N1-Substituted 1H-1,2,3-triazolo[4,5-d]pyrimidine compounds of the formula I ##STR1## in which the substituents X, Y, R.sup.1, R.sup.2 and R.sup.3 have the meanings recited in the specification, are described as pharmaceutical compositions containing them and processes for their preparation. The compounds are effective antiviral agents.

N1-substituted 1H-1,2,3-triazolo[4,5,-D]pyrimidines, a process for their

The compound of the formula I ##STR1## in which R is an aldehyde group or a group which can be converted into an aldehyde, R.sup.1 and R.sup.2 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, hydrogen, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium or triethylamnonium, or

2-formylbenzylphosphonic acid derivatives useful for the treatment of

The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.

Use of benzylphosphonic acid derivatives for the treatment of diseases

A pharmaceutical combination product containing or composed of

Growing community of inventors

Kelkheim, Germany

Matthias Helsberg