Staple oligonucleotides and medicaments comprising the same

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 15/11 (2006.01) A61K 31/713 (2006.01) A61K 48/00 (2006.01) A61P 1/04 (2006.01) A61P 9/00 (2006.01) A61P 13/02 (2006.01) A61P 13/08 (2006.01) A61P 13/10 (2006.01) A61P 13/12 (2006.01) A61P 17/00 (2006.01) A61P 37/00 (2006.01)

Patent

CA 2538215

It is intended to provide an oligonucleotide and a drug to thereby solve problems occurring in existing oigonucleotides, for example, being unstable because of being opened at both ends, and showing toxicity caused by phosphorothioate when modified with phosphorothioate (S-modification) to elevate the stability to digesting enzymes. More specifically speaking, a staple type oligonucleotide and a drug containing the same as the active ingredient. More particularly, a transcriptional factor inhibitor, an antisense oligonucleotide or an siRNA, in greater detail, a drug for preventing, treating or improving inflammation, autoimmune diseases, central diseases, reperfusion injury in ischemic diseases, worsened prognosis after organ transplantation or organ operation or restenosis after PTCA. Still specifically speaking, a drug for preventing, treating or improving arthritis, dermatitis, nephritis, hepatitis, renal failure, cystitis, prostatitis, urethritis, ulcerative colitis, Crohn~s disease, rheumatoid arthritis or arthritis deformans, atopic dermatitis, contact dermatitis, prosiasis, skin ulcer or bed sore.

L'invention a pour but de fournir un oligonucléotide et un médicament destinés à résoudre les problèmes se présentant dans les oligonucléotides existants, par exemple, l'instabilité en raison de l'ouverture aux deux extrémités, et la présence d'une toxicité causée par un phosphorothioate, dans le cas où le produit est modifié avec un phosphorothioate (modification S) afin d'élever la stabilité à la digestion d'enzymes. Plus spécifiquement, l'invention concerne un oligonucléotide du type en agrafe et un médicament comprenant celui-ci, en tant qu'ingrédient actif. Plus particulièrement, l'invention concerne un inhibiteur de facteur de transcription, un oligonucléotide anti-sens ou un ARNSi, de façon plus détaillée, un médicament pour la prévention, le traitement ou l'amélioration d'une inflammation, de maladies auto-immunitaires, de maladies centrales, lésion de reperfusion dans des maladies ischémiques, pronostic d'aggravation après transplantation d'organe ou opération d'organe ou resténose après PTCA. Plus spécifiquement, l'invention concerne un médicament pour la prévention, le traitement ou l'amélioration des maladies ci-après : arthrite, dermatite, néphrite, hépatite, défaillance rénale, cystite, prostatite, uréthrite, rectocolite hémorragique, maladie de Crohn, polyarthrite rhumatoïde ou arthrite deformans, desmatite atopique, eczéma de contact, prosiasis, ulcère de la peau, escarre.

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