A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/70 (2006.01) A61K 31/165 (2006.01) A61K 31/47 (2006.01) A61K 31/4709 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 31/505 (2006.01) A61K 31/506 (2006.01) A61K 31/519 (2006.01) A61K 31/55 (2006.01) A61K 31/551 (2006.01) A61K 31/5513 (2006.01) A61K 31/66 (2006.01)
Patent
CA 2373672
The invention concerns the use of nucleotide analogues, defined as molecules acceptable as substrate of the reverse-transcription response and enabling the addition of at least one supplementary nucleotide to the polynucleotide chain during the reverse transcription to affect and/or to control the fidelity and execution of the reverse transcription. The invention also concerns a pharmaceutical composition containing said nucleotide analogues preferably selected among dUTP, dITP, C7dGTP and C7dATP or characterised in that they have modified bases 6H, 8H-3,4-dihydropyrimido[4,5c][1,2]oxazin-7-one (P) and N methoxy-2,6-diaminopurine (K) alone or mixed with 3'-azido-3'deoxythimidine(AZT), 2',3'-dideoxyinosine-(ddI), 2',3'-dideoxycytidine (ddC), (-)2',3'-dideoxy-3'-theacytidine (3TC), 2',3'-didehydro-2',3'-dideoxythymidine (d4T) and (-)2'-deoxy-5-fluoro-3'-theacytidine (FTC), TIBO (tetrahydroimidazo-(4,5,1-1,jk) (1,4)-benzodiapezine-2-(1H)-one, HEPT (1-[(2-hydroxyethoxy)-methyl]-6-phenylthiothymine), TSAO([2', 5'-bis-O-(tert-butylmethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-dioxide), .alpha.-APA (alpha-anilinophenylacetamide), neviparine, BAHP (bis(etheroaryl)-piperazine) or phosphonoformic acid (PFA), indinavir, saquinavir.
La présente invention porte sur l'utilisation d'analogues de nucléotides, définis comme des molécules capables d'être prises comme substrat de la réaction de reverse transcription et de permettre l'addition d'au moins un nucléotide supplémentaire à la chaîne polynucléotidique en cours de synthèse pour affecter et/ou prendre le contrôle de la fidélité et la processivité de la reverse transcription. Elle concerne également la composition pharmaceutique contenant ces analogues nucléotidiques préférentiellement choisis parmi le dUPT, le dITP, le C7dGTP et le C7dATP, ou caractérisés en ce qu'ils possèdent les bases modifiés 6H, 8H-3, 4-dihydropyrimido [4,5c] [1,2] oxazin-7-one(P) et N méthoxy-2,6-diaminopurine (K) seuls ou en mélange avec la 3'-azido-3'déoxythymidine (AZT), le 2', 3'-didéoxyinosine-(ddI), le 2', 3'- didéoxycytidine (ddC), le (-)2', 2'-didéoxy-3'-théacytidine (3TC), le 2', 3'- didéhydro-2', 3'didéoxythymidine (d4T) et le (-)2'-déoxy-5-fluoro-3'- théacytidine (FTC), le TIBO (Tétrahydroimidazo-(4,5,1-1,jk) (1,4)- benzodiapézine-2(1H)-one), le HEPT (1-[(2-hydroxyéthoxy)-méthyl]-6- phénylthiothymine), le TSAO ([2', 5'-bis-O-(tert-butyldiméthylsilyl)-béta-D- ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide), l'alpha-APA (alpha-anilinophénylacétamide), la névirapine, le BAHP (bis(étheroaryl)-pipérazine) ou l'acide phosphonoformique (PFA), l'indinovir, le saquinovir (INDINAVIR).
Derrien Valerie
Reiss Claude
Centre National de La Recherche Scientifique
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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