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1. (WO1998050540) MODIFIED ANTISENSE NUCLEOTIDES COMPLEMENTARY TO A SECTION OF THE HUMAN Ha-Ras GENE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/050540 International Application No.: PCT/EP1998/002546
Publication Date: 12.11.1998 International Filing Date: 30.04.1998
Chapter 2 Demand Filed: 28.11.1998
IPC:
A61K 38/00 (2006.01) ,C12N 15/11 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
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
Applicants:
HOECHST MARION ROUSSEL DEUTSCHLAND GMBH [DE/DE]; Brüningstrasse 50 D-65929 Frankfurt am Main, DE (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CU, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, GW, HU, ID, IE, IL, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW)
UHLMANN, Eugen [DE/DE]; DE (UsOnly)
PEYMAN, Anuschirwan [DE/DE]; DE (UsOnly)
WILL, David, William [GB/DE]; DE (UsOnly)
CHANG, Esther [US/US]; US (UsOnly)
PIROLLO, Kathleen [US/US]; US (UsOnly)
RAIT, Antonina [US/US]; US (UsOnly)
Inventors:
UHLMANN, Eugen; DE
PEYMAN, Anuschirwan; DE
WILL, David, William; DE
CHANG, Esther; US
PIROLLO, Kathleen; US
RAIT, Antonina; US
Priority Data:
97107404.205.05.1997EP
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.
(FR) L'invention concerne un oligonucléotide modifié spécifique, complémentaire d'une section du gène humain Ha-ras et mARN, et son utilisation pour réguler, moduler ou inhiber de manière spécifique, l'expression du gène Ha-ras. L'invention concerne également son utilisation comme produit pharmaceutique pour traiter les conditions provenant de l'expression anormale du gène Ha-ras, en particulier, en association avec la chimiothérapie et la radiothérapie. L'oligodésoxynucléotide modifié, selon l'invention, présente la séquence 5'-TxAxTxTxCxCxGxTxCxAxT-3'-O-PO2-O-R x représente o ou s, à condition que x soit 4 à 9 fois égal à s et o représente une liaison d'internucléoside de phosphodiester, s représente une liaison d'internucléoside de phosphorothioate. R représente un groupe alkyle C8-C21, -(CH2-CH2O)n-(CH2)m-CH3 ou -CH2-CH(OH)CH2O-(CH2)q-CH3 où n est un nombre entier compris entre 1 et 6, m est un nombre entier compris entre 0 et 20 et q est un nombre entier compris entre 7 et 20 et A représente 2'-désoxyadénosine, G représente 2'-désoxyguanosine, C est 2'-désoxycytidine et T est thymidine.
Designated States: AL, AU, BA, BB, BG, BR, CA, CN, CU, CZ, EE, GE, GW, HU, ID, IL, IS, JP, KP, KR, LC, LK, LR, LT, LV, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, SL, TR, TT, UA, US, UZ, VN, YU
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
CZPV1999-3910MXPA/a/1999/010132KR1020010012238EP0979273US20030064514US20050020523
JP2002501505 CN1255164CA2288946AU1998077602