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1. WO2003005822 - ENHANCEMENT OF THE STABILITY OF OLIGONUCLEOTIDES COMPRISING PHOSPHOROTHIOATE LINKAGES BY ADDITION OF WATER-SOLUBLE ANTIOXIDANTS

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Publication Number WO/2003/005822
Publication Date 23.01.2003
International Application No. PCT/US2002/022038
International Filing Date 11.07.2002
Chapter 2 Demand Filed 10.02.2003
IPC
A61K 31/7125 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
7125Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
A61K 47/18 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
16containing nitrogen
18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
A61K 47/20 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
20containing sulfur, e.g. dimethyl sulfoxide , docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/22 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
CPC
A61K 31/7125
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
7125Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
A61K 47/20
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
20containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/22
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 9/0014
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0014Skin, i.e. galenical aspects of topical compositions
A61P 39/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
39General protective or antinoxious agents
06Free radical scavengers or antioxidants
Applicants
  • ISIS PHARMACEUTICALS, INC. [US]/[US] (AllExceptUS)
  • KROTZ, Achim, H. [DE]/[US] (UsOnly)
  • MEHTA, Rahul [IN]/[US] (UsOnly)
Inventors
  • KROTZ, Achim, H.
  • MEHTA, Rahul
Agents
  • DAILEY, Emma, R.
Priority Data
09/902,95311.07.2001US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) ENHANCEMENT OF THE STABILITY OF OLIGONUCLEOTIDES COMPRISING PHOSPHOROTHIOATE LINKAGES BY ADDITION OF WATER-SOLUBLE ANTIOXIDANTS
(FR) AMELIORATION DE LA STABILITE D'OLIGONUCLEOTIDES COMPRENANT DES LIAISONS PHOSPHOROTHIOATE PAR ADDITION D'ANTIOXYDANTS SOLUBLES DANS L'EAU
Abstract
(EN) Compositions and methods for inhibition of desulfurization in oligonucleotides comprising one or more phosphorothioate linkages. Antioxidants which partition into the aqueous phase of bi-phasic or multi-phasic topical pharmaceutical formulations inhibit desulfurization of phosphorothioate oligonucleotides, resulting in enhanced oligonucleotide stability.
(FR) L'invention concerne des compositions et des procédés pour inhiber la désulfuration dans des oligonucléotides comprenant une ou plusieurs liaisons phosphorothioate. Les antioxydants qui se séparent à l'intérieur de la phase aqueuse de formulations pharmaceutiques topiques biphasiques ou multiphasiques inhibent la désulfuration des oligonucléotides à liaisons phosphorothioate, ce qui améliore la stabilité de ces oligonucléotides.
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