C - Chemistry – Metallurgy – 12 – N
Patent
C - Chemistry, Metallurgy
12
N
C12N 15/11 (2006.01) A61K 31/70 (2006.01) A61P 9/00 (2006.01) A61P 35/00 (2006.01) C07H 21/00 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2339340
The present invention relates to an oligonucleotide or a derivative thereof which has a sequence that corresponds to a part of a nucleic acid which encodes VEGF (vascular endothelial growth factor) and which has the ability to inhibit tumor growth in animal tumor models, the invention further relates to the preparation of such oligonucleotide and the use thereof. An oligonucleotide or a derivative thereof which has the sequence SEQ ID NO. 4 or a part thereof, wherein SEQ ID NO. 4 is 3'-GTACCTACAGATAGTCGCGTCGATGACGGTAGG- 5', with the first proviso, that not all internucleoside bridges in the oligonucleotide are phosphodiester internucleoside bridges and not all phosphodiester internucleoside bridges are replaced by phosphorothioate internucleoside bridges and/or the second proviso, that the oligonucleotide contains no modified nucleosides selected from C5-propynyl uridine, C5- propynyl cytidine, C5-hexynyl uridine, C5-hexynyl cytidine, 6-aza uridine and 6-aza cytidine.
L'invention concerne un oligonucléotide ou un dérivé de celui-ci, lequel possède une séquence correspondant à une partie d'un acide nucléique codant pour VEGF (facteur de croissance des cellues endothéliales vasculaires) et capable d'inhiber la croissance tumorale dans des modèles de tumeurs animales; elle concerne en outre la préparation d'un tel oligonucléotide et l'utilisation de celui-ci. Cet oligonucléotide ou un dérivé de celui-ci possède la séquence SEQ ID NO.4 ou une partie de celle-ci, représentée par 3'-GTACCTACAGATAGTCGCGTCGATGACGGTAGG-5', à la première condition que tous les ponts entre les nucléosides ne soient pas des ponts phosphodiester et que tous les ponts phosphodiester entre les nucléosides ne soient remplacés par des ponts phosphorothioate, et/ou à la seconde condition que l'oligonucléotide ne contienne pas des nucléosides modifiés choisis dans le groupe constitué par C5-propynyl-uridine, C5-propynyl-cytidine, C5-hexynyl-uridine, C5-hexynyl-cytidine, 6-aza-uridine et 6-aza-cytidine.
Bitonti Alan
Peyman Anuschirwan
Uhlmann Eugen
Woessner Richard
Aventis Pharma Deutschland Gmbh
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
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