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EP0169787B1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Use of oligonucleotides bonded to an intercalating agent as drugs

Assignee: Centre National de la Recherche Scientifique
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Filing: 1985-07-22
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Granted: 1989-09-06
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Expires: 2005-07-22
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Abstract

Abstract 1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Drugs, in the form of oligonucleotide compounds bonded to an intercalating agent and comprising an oligonucleotide or an oligodesoxynucleotide made up of a chain of natural or modified nucleotides and complementary with a nucleic acid sequence to which an intercalating group is attached by a covalent bond, the nucleic acid sequence constituting all or part of a sequence involved in initiation, propagation or termination of the replication of a nucleic acid and of transcription and/or translation of one or more genes. 1. Claims for the Contracting State : AT A method of manufacturing drugs comprising oligonucleotide compounds bonded to an intercalating agent consisting of an oligonucleotide or oligodesoxynucleotide made up of a chain of natural or modified nucleotides complementary with a nucleic acid sequence, characterised in that an intercalating group is attached by a covalent bond to the aforementioned nucleic acid sequence which constitutes all or part of a sequence involved in initiation, propagation or termination of replication of a nucleic acid, and of transcription and/or translation of one or more genes.

Inventors

  • 👤 Claude Helene
  • 👤 Thanh Thuong Nguyen

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-05 00:37
CPC Classifications
C; C07; C07H; C07H21/00; A; A61; A61P; A61P31/00; A61P31/04; A61P31/12; A61P33/00; A61P33/10; A61P35/00

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 81 words
Drugs, in the form of oligonucleotide compounds bonded to an intercalating agent and comprising an oligonucleotide or an oligodesoxynucleotide made up of a chain of natural or modified nucleotides and complementary with a nucleic acid sequence to which an intercalating group is attached by a covalent bond, the nucleic acid sequence constituting all or part of a sequence involved in initiation, propagation or termination of the replication of a nucleic acid and of transcription and/or translation of one or more genes.
Claim 2
Dependent Claim 81 words
Drugs, in the form of oligonucleotide compounds bonded to an intercalating agent and comprising an oligonucleotide or an oligodesoxynucleotide made up of a chain of natural or modified nucleotides and complementary with a nucleic acid sequence to which an intercalating group is attached by a covalent bond, the nucleic acid sequence constituting all or part of a sequence involved in initiation, propagation or termination of the replication of a nucleic acid and of transcription and/or translation of one or more genes.
Claim 3
Dependent Claim 32 words
Drugs according to claim 1, in the form of compounds characterised in that the oligonucleotide or oligodesoxynucleotide is complementary with a sequence for replicating or developing a virus or bacterium or parasite.
Claim 4
Dependent Claim 31 words
Drugs according to claim 2, in the form of compounds characterised in that the sequence of oligonucleotides or oligodesoxynucleotides is complementary with a region for regulation, initiation or propagation of replication.
Claim 5
Dependent Claim 45 words
Drugs according to claim 1, in the form of compounds characterised in that the sequence of oligonucleotides or oligodesoxynucleotides is complementary with a nucleic acid sequence for expressing a gene which codes for a factor giving resistance to antibiotics or antiviral agents or antiparasitic agents.
Claim 6
Dependent Claim 25 words
Drugs according to claim 2 or 3, in the form of compounds characterised in that the virus is the influenza virus or the herpes virus.
Claim 7
Dependent Claim 31 words
Drugs according to claim 1, in the form of compounds characterised in that the sequence of oligonucleotides or oligodesoxynucleotides is complementary with a nucleic acid sequence for expressing an oncogenic gene.
Claim 8
Dependent Claim 186 words
Drugs according to any of claims 1 to 6, in the form of compounds having the formula: in which: the radicals B can be identical or different and each denote a natural or modified nucleic acid base, the radicals X, which can be identical or different, each represent an oxoanion O ⊖ or a thioanion S 9 or an alkyl group or an alkoxy, aryloxy, alkoxy or alkyl group substituted by a nitrogen-containing heterocycle, or an aminoalkyl group or an aminoalkoxy group or a thioalkyl group or a -Y-Z group; R and R', which can be identical or different, each represent a hydrogen atom or a -Y-Z group in which: Y represents a straight-chain or branched alkylene radical -alk- or a radical in which E can have the same meanings as X except Y-Z; or a radical -Y"-0-Y' where Y" and Y' can have the meanings given for Y, Z is a radical corresponding to an intercalating agent; only one out of X, R and R' is a Y-Z group; J represents a hydrogen atom or a hydroxy group, and n is an integer including O.
Claim 9
Dependent Claim 27 words
Drugs according to claim 7, in the form of compounds characterised in that the intercalating agent Z is chosen from among polycyclic compounds having a plane configuration.
Claim 10
Dependent Claim 22 words
Drugs according to claim 8, in the form of compounds characterised in that Z is chosen from among acridine, furocoumarin or ellipticine.
Claim 11
Dependent Claim 86 words
Drugs according to any of claims 1 to 9, in the form of compounds characterised in that the radical B is a radical corresponding to thymine, adenine, 2-aminoadenine and derivatives thereof substituted e.g. on the N 6 by an aminoalkylene group or by an azidophenylalkylene group, cytosine, guanine or guanine substituted on the 0 6 e.g. by an (ω-alkylene)-9-acridine group, or 8-(ω-aminoalkyl)-aminoadenine and derivatives thereof substituted on the NH 2 at ω by an acridine group; uracil, 5-bromo-uracil, 8-azidoadenine or a photoactivatable derivative of the bases.
Claim 12
Dependent Claim 24 words
Drugs according to any of claims 1 to 10, in the form of compounds characterised in that the radical Z is chosen from among:
Claim 13
Dependent Claim 47 words
Drugs according to any of claims 1 to 11, in the form of compounds characterised in that B is chosen from among T, G, A, C and U; X is chosen from among O - , methyl, ethyl, propyl, methoxy, ethoxy and propoxy, and J = H.
Claim 14
Dependent Claim 26 words
Drugs according to claim 1, in the form of compounds characterised in that the compounds are chosen from among: in which Z is an intercalating agent.
Claim 15
Dependent Claim 28 words
A pharmaceutical composition characterised in that the active principle therein is at least one drug according to any of claims 1 to 13 and a pharmaceutically acceptable excipient.
Claim 16
Dependent Claim 25 words
A pharmaceutical composition according to claim 14, characterised in that it also comprises an antibiotic, an antiparasitic agent, an antiviral agent or an antitumor agent.

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