DK2558478T3 - Pyrimidiner modificeret ved 5-positionen og deres anvendelse - Google Patents
Pyrimidiner modificeret ved 5-positionen og deres anvendelse Download PDFInfo
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- DK2558478T3 DK2558478T3 DK11769451.3T DK11769451T DK2558478T3 DK 2558478 T3 DK2558478 T3 DK 2558478T3 DK 11769451 T DK11769451 T DK 11769451T DK 2558478 T3 DK2558478 T3 DK 2558478T3
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- modified
- oligonucleotide
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- C—CHEMISTRY; METALLURGY
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- 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
- C12N15/115—Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith ; Nucleic acids binding to non-nucleic acids, e.g. aptamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
- C07H19/167—Purine radicals with ribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
- C07H19/173—Purine radicals with 2-deoxyribosyl as the saccharide radical
-
- 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
- C07H21/04—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
-
- 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
- C12N2310/10—Type of nucleic acid
- C12N2310/16—Aptamers
-
- 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
- C12N2310/33—Chemical structure of the base
- C12N2310/335—Modified T or U
Claims (9)
1. Forbindelse udvalgt blandt forbindelserne med den følgende struktur eller et salt deraf:
hvor Rer-(CH2)n-Rx1; RX1 er:
*Betegner bindingspunkt af RX1 -gruppen til (CH2)n -forbindelsesgruppen RX4 er en halogen (F, Cl, Br, I); n = 0-10; X er udvalgt fra gruppen bestående af -H, -OFI, -OMe, -O-allyl, -F, -OEt, -OPr, - OCFI2CFI2OCFl3 og -azido; R' er udvalgt fra gruppen bestående af -Ac; -P(N(iPr)2(0(CFI2)2)CN; -Bz og -SiMe2tBu; R" er udvalgt fra gruppen bestående af H, DMT og triphosphat (-P(0)(0H)-0P(0)(0H)-0-P(0)(0H)2) eller et salt deraf.
2. Forbindelse ifølge krav 1 med den følgende struktur eller et salt deraf:
eller
3. Forbindelse ifølge krav 1 med den følgende struktur eller et salt deraf:
4. Oligonukleotid omfattende mindst et modificeret nukleotid med den følgende struktur:
hvor Rer -(CH2)n-Rx1; RX1 er:
‘Betegner bindingspunkt af RX1 -gruppen til (CH2)n -forbindelsesgruppen RX4 er udvalgt fra gruppen bestående af halogen (F, Cl, Br, I); n = 0-10; X er udvalgt fra gruppen bestående af -H, -OFI, -OMe, -O-allyl, -F, -OEt, -OPr, - OCFI2CFI2OCFl3 og -azido;
5. Oligonukleotid ifølge krav 4 omfattende mindst et modificeret nukleotid med den følgende struktur:
hvor X er udvalgt fra gruppen bestående af -H, -OH, -OMe, -O-allyl, -F, -OEt, -OPr, - OCH2CH2OCH3 og -azido.
6. Oligonukleotid ifølge krav 5, hvor oligonukleotidet er udvalgt blandt en ri-bonukleinsyre eller en deoxyribonukleinsyre, eventuelt hvor oligonukleotidet yderligere omfatter mindst en kemisk modifikation omfattende en kemisk substitution ved en eller flere positioner uafhængigt udvalgt blandt en riboseposition, en deoxyriboseposition, en phos-phatposition og en baseposition, eventuelt hvor den kemiske modifikation er uafhængigt udvalgt fra gruppen bestående af en 2'-position sukkermodifikation, en 2'-amino (2'-NH2), en 2'-fluor (2'-F), en 2'-0-methyl (2'-OMe), 2'-0-ethyl (2'-OEt), 2'-0-propyl (2'-OPr), 2'-0-CH2CH20CH3, en 5-position pyrimidinmodifikation, en ryggradsmodifikation, methylering, en 3'-cap og en 5'-cap.
7. Aptamer omfattende mindst et modificeret nukleotid med den følgende struktur:
hvor Rer -(CH2)n-Rx1; RX1 er:
*Betegner bindingspunkt af RX1 -gruppen til (CH2)n -forbindelsesgruppen RX4 er en halogen (F, Cl, Br, I); n = 0-10; X er udvalgt fra gruppen bestående af -H, -OH, -OMe, -O-allyl, -F, -OEt, -OPr, - OCH2CH2OCH3 og -azido;
8. Aptamer ifølge krav 7 omfattende mindst et modificeret nukleotid med den følgende struktur:
9. Aptamer ifølge krav 8, hvor aptameren er udvalgt blandt en ribonukleinsyre eller en deoxyribonukleinsyre, eventuelt hvor aptameren yderligere omfatter mindst en kemisk modifikation omfattende en kemisk substitution ved en eller flere positioner uafhængigt udvalgt blandt en riboseposition, en deoxyriboseposition, en phosphatposi-tion og en baseposition, eventuelt hvor den kemiske modifikation er uafhængigt udvalgt fra gruppen bestående af en 2'-position sukkermodifikation, en 2'-amino (2'-NH2),en 2'-fluor (2'-F), en 2'-0-methyl (2'-OMe), 2'-0-ethyl (2'-OEt), 2’-0-propyl (2’-OPr), 2'-0-CH2CH20CH3, en 5-position pyrimidinmodifi-kation, en ryggradsmodifikation, methylering, en 3'-cap og en 5'-cap.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US32314510P | 2010-04-12 | 2010-04-12 | |
PCT/US2011/032143 WO2011130289A1 (en) | 2010-04-12 | 2011-04-12 | 5-position modified pyrimidines and their use |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2558478T3 true DK2558478T3 (da) | 2018-05-22 |
Family
ID=44798979
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK11769451.3T DK2558478T3 (da) | 2010-04-12 | 2011-04-12 | Pyrimidiner modificeret ved 5-positionen og deres anvendelse |
Country Status (23)
Country | Link |
---|---|
US (7) | US8598140B2 (da) |
EP (3) | EP3345915B1 (da) |
JP (4) | JP6012591B2 (da) |
KR (4) | KR101952671B1 (da) |
CN (4) | CN104069512A (da) |
AR (1) | AR081452A1 (da) |
AU (2) | AU2011240774B2 (da) |
BR (2) | BR122021003805B8 (da) |
CA (3) | CA2797188C (da) |
CO (1) | CO6630139A2 (da) |
DK (1) | DK2558478T3 (da) |
EA (1) | EA022429B1 (da) |
ES (3) | ES2905656T3 (da) |
HK (2) | HK1201740A1 (da) |
IL (5) | IL222339A (da) |
MX (3) | MX2012011771A (da) |
MY (1) | MY160608A (da) |
NO (1) | NO2558478T3 (da) |
NZ (1) | NZ602618A (da) |
SG (3) | SG184089A1 (da) |
TW (6) | TWI505833B (da) |
UA (1) | UA105290C2 (da) |
WO (2) | WO2011130289A1 (da) |
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