Competitive Technologies, Inc.

Ciba-Geigy Corporation

University Patents, Inc.

Novartis Corporation

Competitve Technologies, Inc.

Wolfgang K-d Brill

Marvin H Caruthers

John Nielsen

Eric K Yau

Michael Ma

Pascal Furet

Peter Traxler

William S Marshall

Yun-Xi Ma

The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumor diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0,

Pyrrolopyrimidine derivatives having pharmacological activity

The present invention relates to new and useful nucleoside thiophosphoroamidites and polynucleotide phosphorodithioate compounds as well as the processes whereby these compounds may be used for synthesizing new mononucleotides and polynucleotides having phosphorothioate and phosphorodithioate internucleotide linkages.

Polynucleotide phosphorodithioate compounds

The present invention describes a method for the inhibition of reverse transcriptase by contacting said reverse transcriptase with oligonucleotides having have at least one phosphorodithioate internucleotide linkage of the formula ##STR1## within the phosphorus backbone of the oligonucleotide.

Inhibition of reverse transcriptase by phosphorodithioates

The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumour diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0,

Nucleoside thiophosphoramidites

The invention relates to nucleosides, nucleotides and oligonucleotides carrying in their basic structure a primary hydroxyl group protected by tris-4,4',4'-tert-butylphenylmethyl, to processes for the preparation of said nucleosides and nucleotides, to a process for the preparation of oligonucleotides, and to the use of said protected nucleosides, nucleotides and oligonucleotides.

TTTr as protective group in nucleotide synthesis

Dinucleoside phosphorodithioate phosphoramidite precursors useful in the synthesis of oligonucleotide phosphorodithioate which can be used as antisense inhibitors of translation.

Oligonucleotides having at least one phosphorodithioate internucleotide linkage. Phosphorodithioate oligonucleotides exhibit stronger antiviral activity than the corresponding phoshorothioate derivatives.

Polynucleotide phosphorodithioate

A process for the preparation of natural or synthetic nucleosides, nucleoside analogs or oligonucleotides from at least two such nucleosides and/or nucleoside analogs whose basic molecule contains an unsubstituted or substituted radical of a nucleic base B and a protected hydroxyl group of formula R.sub.1 --O--, wherein R.sub.1 is a protective group, or which are linked to the oxygen atom of a hydroxyl group direct or to a solid support through a linking group, from nucleoside monomers or from oligonucleotides to the basic molecule of which, in addition to said radicals, a group of formula I, Ia or Ib ##STR1## is attached, by converting the group of formula I, Ia or Ib into a hydroxyl group --OH by reacting the nucleosides or oligonucleotides, in the absence or presence of an inert organic solvent, with an excess of an aliphatic, cycloaliphatic araliphatic or aromatic alcohol containing 1 to 30 carbon atoms, a polyol containing 2 to 50 carbon atoms or a polymeric polyol, in the presence of at least a catalytic amount of an inorganic base or of an organic nitrogen base, which base has a pK value of 4 to 10.

Process for the preparation of nucleosides

The present invention relates to new and useful nucleside thiophosphoramidite, polynucleotide dithioate phosphoramidite and polynucleotide phosphorothioamidate phosphoramidite compounds as well as the process whereby these compounds can be used for synthesizing new monoucleotides and polynucleotides having phosphorodithioate, phosphorothioamidate, phosphorothiotriesters and phosphorothioate internucleotide linkages.

Growing community of inventors

Schopfheim, Germany

Wolfgang K-d Brill