Processing

Please wait...

Settings

Settings

1. WO1992003452 - NOVEL NUCLEOSIDE ANALOGS

Publication Number WO/1992/003452
Publication Date 05.03.1992
International Application No. PCT/US1991/005713
International Filing Date 12.08.1991
Chapter 2 Demand Filed 21.02.1992
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
7
Compounds containing elements of the 4th Group of the Periodic System
02
Silicon compounds
08
Compounds having one or more C-Si linkages
18
Compounds having one or more C-Si linkages as well as one or more C-O-Si linkages
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
06
Pyrimidine radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
06
Pyrimidine radicals
10
with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
16
Purine radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21
Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
C07D 405/04 (2006.01)
C07D 405/14 (2006.01)
C07F 7/18 (2006.01)
C07H 19/04 (2006.01)
C07H 19/06 (2006.01)
C07H 19/10 (2006.01)
CPC
C07D 405/04
C07D 405/14
C07F 7/1804
C07H 19/04
C07H 19/06
C07H 19/10
Applicants
  • ISIS PHARMACEUTICALS, INC. [US/US]; 2280 Faraday Avenue Carlsbad, CA 92008, US
Inventors
  • COOK, Philip, Dan; US
  • SANGHVI, Yogesh, Shantilal; US
Agents
  • CALDWELL, John, W. ; Woodcock Washburn Kurtz Mackiewicz & Norris One Liberty Place - 46th Floor Philadelphia, PA 19103, US
Priority Data
566,83613.08.1990US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NOVEL NUCLEOSIDE ANALOGS
(FR) NOUVEAUX ANALOGUES DE NUCLEOSIDE
Abstract
(EN)
Novel oligonucleotide analogs are provided having improved cellullar uptake, improved resistance to nucleases, and good hybridization to target RNA. Such analogs are provided having substantially non-chiral, non-ionic linking functionalities between the sugars and sugar analogs thereof. In accordance with preferred embodiments, the 4' position of a sugar or sugar analog at one nucleoside is linked to the 3' position of a second sugar or sugar analog of a second nucleoside by a linking function that comprises a two- or three- carbon backbone chain. In accordance with preferred embodiments, the linking functions comprise the formula O-R1-O where R1 comprises a two or three carbon backbone. Such linking functions also, preferably comprise ether functionalities to effect such linkage. Processes for the automated synthesis of oligonucleotide analogs are also provided.
(FR)
Nouveaux analogues d'oligonucléotide présentant une absorption cellulaire améliorée, une meilleure résistance aux nucléases, ainsi qu'une bonne hybridation avec l'ARN cible. Lesdits analogues présentent des fonctionnalités non chirales de liaison non ionique entre les sucres et leurs analogues de sucre. Selon les modes de réalisation préférés, la position 4' d'un sucre ou d'un analogue de sucre au niveau d'un nucléoside est liée à la position 3' d'un second sucre ou analogue de sucre d'un second nucléoside par une fonction de liaison comprenant une chaîne de squelettes à deux ou trois atomes de carbone. Selon les modes de réalisation préférés, les fonctions de liaison comprennent la formule O-R1-O dans laquelle R1 comprend un squelette à deux ou trois atomes de carbone. Lesdites fonctions de liaison présentent également, de préférence, des fonctionnalités éther afin d'effectuer ladite liaison. L'invention concerne également des procédés de synthèse automatique d'analogues d'oligonucléotides.
Latest bibliographic data on file with the International Bureau