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1. (CA2288946) MODIFIED ANTISENSE NUCLEOTIDES COMPLEMENTARY TO A SECTION OF THE HUMAN HA-RAS GENE

Office : Canada
Application Number: 2288946 Application Date: 30.04.1998
Publication Number: 2288946 Publication Date: 12.11.1998
Publication Kind : A1
Prior PCT appl.: Application Number:EP1998002546 ; Publication Number: Click to see the data
IPC:
C12N 15/11
A61K 31/70
A61K 45/06
C07H 21/00
A61K 38/00
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15
Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09
Recombinant DNA-technology
11
DNA or RNA fragments; Modified forms thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06
Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21
Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
CPC:
C07H 21/02
A61K 38/00
C12N 15/1135
C12N2310/11
C12N2310/315
C12N2310/322
C12N2310/345
C12N2310/351
C12N2310/3531
Applicants: HOECHST MARION ROUSSEL DEUTSCHLAND GMBH
Inventors: UHLMANN, EUGEN
PEYMAN, ANUSCHIRWAN
WILL, DAVID WILLIAM
CHANG, ESTHER
PIROLLO, KATHLEEN
RAIT, ANTONINA
Priority Data: 97107404.2 05.05.1997 DE
Title: (EN) MODIFIED ANTISENSE NUCLEOTIDES COMPLEMENTARY TO A SECTION OF THE HUMAN HA-RAS GENE
(FR) NUCLEOTIDES ANTISENS MODIFIES COMPLEMENTAIRES D'UNE SECTION DU GENE HUMAIN HA-RAS
Abstract:
(EN) The invention relates to a specific modified oligonucleotide complementary to a section of the human Ha-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 abnormal expression of the Ha-ras gene, in particular in combination with chemotherapy and radiotherapy. The modified oligodeoxynucleotide according to the invention has the sequence: 5'-TxAxTxTxCxCxGxTxCxAxT-3'-O-PO2-O-R, wherein X is o or s, with the proviso that x is 4 to 9 times equal to s and o means a phosphodiester internucleoside linkage, s means a phosphorothioate internucleoside linkage, R means a C8-C21 alkyl group, -(CH2-CH2O)n-(CH2)m-CH3 or -CH2-CH(OH)CH2O-(CH2)q-CH3 wherein n is an integer from 1 to 6, m is an integer from 0 to 20 and q is an integer from 7 to 20 and A is 2'- deoxyadenosine, G is 2'-deoxyguanosine, C is 2'-deoxycytidine and T is thymidine.


Also published as:
CZPV1999-3910MXPA/a/1999/010132KR1020010012238EP0979273US20030064514US20050020523
JP2002501505 CN1255164AU1998077602WO/1998/050540