Abstract: 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.

Abstract: Oligonucleotides of the formula5'-(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: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

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: A process for the preparation of 1-hydroxy-2-pyridones is described in which a pyrone is reacted with a hydroxyl-ammonium salt in the presence of basic compounds, solvents and organic acids or salts thereof.

Abstract: The invention concerns prodrugs of enzyme inhibitors in which at least one OH-- group in the enzyme inhibitor has been converted into a derivative grouping of the formula III, IV or V: ##STR1## in which the groups R.sup.11 to R.sup.25 and s,l, m, o, q, and r are as defined in the description. Such prodrugs exhibit an improved solubility in water and improved pharmaco-kinetic characteristics.

Abstract: The invention relates to a process for the preparation of 1-hydroxy-2-pyridones of the formula I ##STR1## by reaction of a pyrone of the formula II ##STR2## with a hydroxylammonium salt in the presence of basic compounds, which comprises carrying out the reaction in the presence of a distillable, filterable or extractable acid or a salt thereof in an amount of 0.01 to 20 equivalents with respect to the pyrone of the formula II, and employing as the basic compounds an alkali metal carbonate and/or alkali metal bicarbonate in an amount of 0.8 to 5 equivalents with respect to the hydroxylammonium salt, the radicals R.sup.1 and R.sup.2 in the formulae I and II are described herein.

Abstract: Compounds of the formula I, ##STR1## in which the symbols or substituents A, B, D, D*, E and E* have the meanings given in the specification, inhibit aspartyl proteases and are suitable for controlling viral diseases.

Abstract: Novel oligonucleotide analogs of the formulae I and II ##STR1## in which A, B, D, R.sup.1, R.sup.2, 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 present invention relates to a compound of the formula ##STR1## in which A, Q, R.sup.2, R.sup.3 and R.sup.4, and also the corresponding, asterisked radicals, are defined as indicated in the description, to a process for their preparation, and also to their use for inhibiting retroviral proteases.

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

Abstract: The present invention relates to compounds of the formula I ##STR1## in which A, Q, R.sup.2, R.sup.3, R.sup.4 and the corresponding radicals with an * are defined as indicated in the description, a process for the preparation thereof, and the use thereof for inhibiting retroviral proteases.

Abstract: Novel bis(aminomethyl)phosphinic acid derivatives and process for the preparation of bis(aminomethyl)phosphinic acid derivativesCompounds of the formula VI ##STR1## can be prepared by reaction of a compound of the formula IV ##STR2## with a base to give a compound of the formula Va or Vb ##STR3## and subsequent reaction with carbon nucleophiles; alternatively the compound of the formula VI is prepared by direct reaction of the compound of the formula IV e.g. with R.sup.2 Cu(CN)Li.sub.2, the above substituents having the meanings mentioned.

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

Abstract: A process for the preparation of .alpha.- or .alpha.,.alpha.'-substituted derivatives of the bis(aminomethyl)phosphinic acid of the formula I and their acid or basic salts, ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are defined as in the description, wherein a bis(aminomethyl)phosphinate is converted into the corresponding bisimine, which is alkylated by R.sup.2 and R.sup.3 in the .alpha.- and/or .alpha.,.alpha.'-position after reaction with a base, and is converted into a compound of the formula I by subsequent treatment with an acid.

Abstract: 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, orR.sup.1 and R.sup.2 together form a cyclic diester,R.sup.3 and R.sup.4 are alkyl, alkenyl, alkynyl, cycloalkyl, hydrogen, alkoxy or halogen, R.sup.5 and R.sup.8 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, alkoxy, phenyl, cyanide, hydroxyl or hydrogen, and X, Y or Z are oxygen or sulfur, or prodrug forms of the compound of the formula I can be used for the treatment of diseases caused by viruses.The preparation of these compounds and pharmaceutical preparations containing them and their use is described.

Abstract: 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.