KR930702374A - 안티 센스 핵산 유도체 - Google Patents
안티 센스 핵산 유도체Info
- Publication number
- KR930702374A KR930702374A KR1019930701512A KR930701512A KR930702374A KR 930702374 A KR930702374 A KR 930702374A KR 1019930701512 A KR1019930701512 A KR 1019930701512A KR 930701512 A KR930701512 A KR 930701512A KR 930702374 A KR930702374 A KR 930702374A
- Authority
- KR
- South Korea
- Prior art keywords
- group
- carbon atoms
- substituent
- alkyl
- atom
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
- 230000000692 anti-sense effect Effects 0.000 title 1
- 150000007523 nucleic acids Chemical class 0.000 title 1
- 102000039446 nucleic acids Human genes 0.000 title 1
- 108020004707 nucleic acids Proteins 0.000 title 1
- 239000002773 nucleotide Substances 0.000 claims abstract 211
- 125000003729 nucleotide group Chemical group 0.000 claims abstract 211
- 125000000217 alkyl group Chemical group 0.000 claims abstract 194
- 125000001424 substituent group Chemical group 0.000 claims abstract 184
- 125000003118 aryl group Chemical group 0.000 claims abstract 114
- 150000001875 compounds Chemical class 0.000 claims abstract 109
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 98
- 230000000295 complement effect Effects 0.000 claims abstract 74
- 125000004434 sulfur atom Chemical group 0.000 claims abstract 74
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 claims abstract 60
- 125000005843 halogen group Chemical group 0.000 claims abstract 60
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 60
- 108090000623 proteins and genes Proteins 0.000 claims abstract 54
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 claims abstract 50
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical compound O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 claims abstract 50
- RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 claims abstract 50
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 36
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims abstract 34
- 125000003396 thiol group Chemical group [H]S* 0.000 claims abstract 29
- 241000700605 Viruses Species 0.000 claims abstract 27
- 229940104302 cytosine Drugs 0.000 claims abstract 25
- 229940113082 thymine Drugs 0.000 claims abstract 25
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 claims abstract 23
- 229930024421 Adenine Natural products 0.000 claims abstract 23
- 229960000643 adenine Drugs 0.000 claims abstract 23
- 150000003839 salts Chemical class 0.000 claims abstract 17
- 206010028980 Neoplasm Diseases 0.000 claims abstract 14
- 239000002246 antineoplastic agent Substances 0.000 claims abstract 3
- 229940034982 antineoplastic agent Drugs 0.000 claims abstract 2
- 239000003443 antiviral agent Substances 0.000 claims abstract 2
- 230000003612 virological effect Effects 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 433
- -1 methylenedioxy group Chemical group 0.000 claims 124
- 125000004430 oxygen atom Chemical group O* 0.000 claims 93
- 229910052717 sulfur Inorganic materials 0.000 claims 93
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 89
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 73
- 125000004104 aryloxy group Chemical group 0.000 claims 59
- 229910052760 oxygen Inorganic materials 0.000 claims 50
- 239000001301 oxygen Substances 0.000 claims 50
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 38
- 108700020796 Oncogene Proteins 0.000 claims 32
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 27
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 27
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 27
- 125000003710 aryl alkyl group Chemical group 0.000 claims 24
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 24
- 230000014621 translational initiation Effects 0.000 claims 22
- 108091034117 Oligonucleotide Proteins 0.000 claims 20
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 20
- 239000011593 sulfur Chemical group 0.000 claims 20
- 125000002103 4,4'-dimethoxytriphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)(C1=C([H])C([H])=C(OC([H])([H])[H])C([H])=C1[H])C1=C([H])C([H])=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 19
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical class [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 18
- 241000725303 Human immunodeficiency virus Species 0.000 claims 17
- 239000005373 porous glass Substances 0.000 claims 17
- 125000004423 acyloxy group Chemical group 0.000 claims 12
- 125000006239 protecting group Chemical group 0.000 claims 11
- 238000000034 method Methods 0.000 claims 9
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 8
- 108010087776 Proto-Oncogene Proteins c-myb Proteins 0.000 claims 8
- 125000001624 naphthyl group Chemical group 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 7
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 7
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 7
- 239000003795 chemical substances by application Substances 0.000 claims 6
- 108020004414 DNA Proteins 0.000 claims 5
- 241000124008 Mammalia Species 0.000 claims 5
- 125000003277 amino group Chemical group 0.000 claims 5
- 239000003937 drug carrier Substances 0.000 claims 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims 5
- QGJOPFRUJISHPQ-UHFFFAOYSA-N Carbon disulfide Chemical compound S=C=S QGJOPFRUJISHPQ-UHFFFAOYSA-N 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000007800 oxidant agent Substances 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims 2
- 239000007791 liquid phase Substances 0.000 claims 2
- 150000003018 phosphorus compounds Chemical class 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- JLCPHMBAVCMARE-UHFFFAOYSA-N [3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methyl [5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Polymers Cc1cn(C2CC(OP(O)(=O)OCC3OC(CC3OP(O)(=O)OCC3OC(CC3O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c3nc(N)[nH]c4=O)C(COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3CO)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cc(C)c(=O)[nH]c3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O JLCPHMBAVCMARE-UHFFFAOYSA-N 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- 229940059260 amidate Drugs 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 239000011324 bead Substances 0.000 claims 1
- 238000006482 condensation reaction Methods 0.000 claims 1
- 125000001891 dimethoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000005982 diphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 239000001177 diphosphate Substances 0.000 claims 1
- 235000011180 diphosphates Nutrition 0.000 claims 1
- NPUKDXXFDDZOKR-LLVKDONJSA-N etomidate Chemical compound CCOC(=O)C1=CN=CN1[C@H](C)C1=CC=CC=C1 NPUKDXXFDDZOKR-LLVKDONJSA-N 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- YACKEPLHDIMKIO-UHFFFAOYSA-N methylphosphonic acid Chemical compound CP(O)(O)=O YACKEPLHDIMKIO-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000000962 organic group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-N phosphoric acid Substances OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- 239000001226 triphosphate Substances 0.000 claims 1
- 235000011178 triphosphate Nutrition 0.000 claims 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 claims 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 description 2
- 241000713772 Human immunodeficiency virus 1 Species 0.000 description 1
- 102100034343 Integrase Human genes 0.000 description 1
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 description 1
- 239000000427 antigen Substances 0.000 description 1
- 102000036639 antigens Human genes 0.000 description 1
- 108091007433 antigens Proteins 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/31—Chemical structure of the backbone
- C12N2310/312—Phosphonates
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/31—Chemical structure of the backbone
- C12N2310/312—Phosphonates
- C12N2310/3125—Methylphosphonates
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/31—Chemical structure of the backbone
- C12N2310/314—Phosphoramidates
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/31—Chemical structure of the backbone
- C12N2310/315—Phosphorothioates
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/32—Chemical structure of the sugar
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/32—Chemical structure of the sugar
- C12N2310/321—2'-O-R Modification
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/32—Chemical structure of the sugar
- C12N2310/322—2'-R Modification
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/352—Nature of the modification linked to the nucleic acid via a carbon atom
- C12N2310/3527—Other alkyl chain
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/353—Nature of the modification linked to the nucleic acid via an atom other than carbon
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/353—Nature of the modification linked to the nucleic acid via an atom other than carbon
- C12N2310/3531—Hydrogen
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Biomedical Technology (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Engineering & Computer Science (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Plant Pathology (AREA)
- Biophysics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Physics & Mathematics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Microbiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP90-315007 | 1990-11-20 | ||
| JP31500790 | 1990-11-20 | ||
| PCT/JP1991/001572 WO1992008729A1 (en) | 1990-11-20 | 1991-11-18 | Antisense nucleic acid derivative |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR930702374A true KR930702374A (ko) | 1993-09-08 |
Family
ID=18060297
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019930701512A Ceased KR930702374A (ko) | 1990-11-20 | 1991-11-18 | 안티 센스 핵산 유도체 |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP0558749A1 (enExample) |
| JP (1) | JPH05213986A (enExample) |
| KR (1) | KR930702374A (enExample) |
| CA (1) | CA2096658A1 (enExample) |
| HU (1) | HUT64554A (enExample) |
| WO (1) | WO1992008729A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2114355A1 (en) * | 1993-01-29 | 1994-07-30 | Hidehiko Furukawa | Modified oligodeoxyribonucleotides, their preparation and their therapeutic use |
| US5994320A (en) * | 1995-02-06 | 1999-11-30 | Regents Of The University Of Minnesota | Antisense oligonucleotides and methods for treating central nervous system tumors |
| CN105524104B (zh) * | 2015-12-03 | 2018-10-02 | 清华大学 | 硫代磷酸酯衍生物与过量溴乙酮基芳环物的反应及产物 |
| IL319933A (en) * | 2019-05-08 | 2025-05-01 | Biogen Ma Inc | Convergent Syntheses of Oligonucleotides in Liquid Phase |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4469863A (en) * | 1980-11-12 | 1984-09-04 | Ts O Paul O P | Nonionic nucleic acid alkyl and aryl phosphonates and processes for manufacture and use thereof |
| US5276019A (en) * | 1987-03-25 | 1994-01-04 | The United States Of America As Represented By The Department Of Health And Human Services | Inhibitors for replication of retroviruses and for the expression of oncogene products |
| WO1989008146A1 (en) * | 1988-02-26 | 1989-09-08 | Worcester Foundation For Experimental Biology | Inhibition of htlv-iii by exogenous oligonucleotides |
| DE68929361T2 (de) * | 1988-04-27 | 2002-06-20 | Isis Pharmaceuticals, Inc. | Oligoribonukleotid-Derivate und Verwendung davon als Antiviral Arzneimittel |
-
1991
- 1991-11-18 HU HU9301453A patent/HUT64554A/hu unknown
- 1991-11-18 EP EP91919641A patent/EP0558749A1/en not_active Withdrawn
- 1991-11-18 JP JP3301744A patent/JPH05213986A/ja active Pending
- 1991-11-18 CA CA002096658A patent/CA2096658A1/en not_active Abandoned
- 1991-11-18 WO PCT/JP1991/001572 patent/WO1992008729A1/ja not_active Ceased
- 1991-11-18 KR KR1019930701512A patent/KR930702374A/ko not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| JPH05213986A (ja) | 1993-08-24 |
| CA2096658A1 (en) | 1992-05-21 |
| EP0558749A1 (en) | 1993-09-08 |
| WO1992008729A1 (en) | 1992-05-29 |
| HU9301453D0 (en) | 1993-09-28 |
| EP0558749A4 (enExample) | 1995-07-05 |
| HUT64554A (en) | 1994-01-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US5955599A (en) | Process for making oligonucleotides containing o- and s- methylphosphotriester internucleoside linkages | |
| US6140482A (en) | Primary phosphoramidate internucleoside linkages and oligonucleotides containing the same | |
| EP2361921B1 (en) | Bicyclo-oligonucleotide analogues | |
| US5955591A (en) | Phosphotriester oligonucleotides, amidites and method of preparation | |
| EP0570514A1 (en) | Methylene phosphonate nucleoside analogs and oligonucleotide analogs made therefrom | |
| EP0963997B1 (en) | Novel nucleotide analogues | |
| EP0506242B1 (en) | Method and compounds for solid phase synthesis of oligonucleotides and oligonucleotide analogs | |
| EP0680969B1 (de) | Modifizierte Oligonukleotide, deren Herstellung sowie deren Verwendung | |
| US5449769A (en) | Method and reagent for sulfurization of organophosphorous compounds | |
| CA2106819C (en) | Oligoribonucleotide and ribozyme analogs with terminal 3'-3' and/or 5'-5' linkages | |
| KR920002625A (ko) | 말단에 3'-3' 또는 5'-5' 뉴클레오타이드간 결합을 갖는 올리고뉴클레오타이드 유사체 | |
| KR100273824B1 (ko) | 비뉴클레오티드성 그룹을 갖는 3'-유도된 올리고뉴클레오티드 동족체, 이의 제조방법 및 이를 함유하는 약제학적 제제 | |
| AU716391B2 (en) | Solid phase synthesis of oligonucleotides | |
| Moody et al. | Regiospecific inhibition of DNA duplication by antisense phosphate-methylated oligodeoxynucleotides | |
| JPH10195098A (ja) | 新規ヌクレオチド類縁体 | |
| JP2000506849A (ja) | オリゴヌクレオチド類似体 | |
| WO1998029429A1 (en) | Method for the synthesis of nucleotide or oligonucleotide phosphoramidites | |
| KR930702374A (ko) | 안티 센스 핵산 유도체 | |
| WO1990012022A1 (en) | Polynucleotide phosphorodithioates as therapeutic agents for retroviral infections | |
| US20040033967A1 (en) | Alkylated hexitol nucleoside analogues and oligomers thereof | |
| EP0739899B1 (en) | Novel oligoribonucleotide derivatives and application thereof to antiviral agents | |
| Stec et al. | Stereospecific Synthesis of P-chiral Analogs of oligonucleotides | |
| WO1995031470A2 (en) | Antisense inhibitors of gene expression | |
| US6486313B1 (en) | Oligonucleotides having alkylphosphonate linkages and methods for their preparation | |
| JPH069682A (ja) | レトロウイルス感染用治療薬としてのポリヌクレオチドホスホロジチオエート |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0109 | Patent application |
Patent event code: PA01091R01D Comment text: Patent Application Patent event date: 19930520 |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 19961014 Comment text: Request for Examination of Application Patent event code: PA02011R01I Patent event date: 19930520 Comment text: Patent Application |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 19981029 Patent event code: PE09021S01D |
|
| E601 | Decision to refuse application | ||
| PE0601 | Decision on rejection of patent |
Patent event date: 19990123 Comment text: Decision to Refuse Application Patent event code: PE06012S01D Patent event date: 19981029 Comment text: Notification of reason for refusal Patent event code: PE06011S01I |