CYTIDINE-5-CARBOXAMIDE MODIFIED NUCLEOTIDE COMPOSITIONS AND METHODS RELATED THERETO

• Main Authors: NEBOJSA JANJIC, BHARAT NATHU GAWANDE, JOHN ROHLOFF
• Format: Patent
• Language: English; Japanese
• Published: 13.05.2021
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS OR TEST PAPERS THEREFOR; COMPOSITIONS THEREOF; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES; CULTURE MEDIA; DERIVATIVES THEREOF; ENZYMOLOGY; HUMAN NECESSITIES; HYGIENE; MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROCESSES OF PREPARING SUCH COMPOSITIONS; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPIRITS; SUGARS; VINEGAR; WINE

To provide 5-position modified cytosines and phosphoramidites thereof, and triphosphate derivatives thereof, and methods of making and using the same, and compositions and uses of the modified nucleosides as part of a nucleic acid molecule (e.g., aptamer).SOLUTION: The present disclosure provides a compound having a structure represented by the following formula I. (R independently represents -(CH2) n-, n is an integer of 0-10; R' is independently selected from the group consisting of -H, -OAc, -OBz, -P(NiPr2)(OCH2CH2CN), and -OSiMe2 tBu; R'' is independently selected from the group consisting of hydrogen, 4,4'-dimethoxytrityl (DMT) and triphosphate (-P(O)(OH)-O-P(O)(OH)-O-P(O)(OH)2) or a salt thereof).SELECTED DRAWING: None 【課題】５位修飾シトシン及びそのホスホルアミダイト、ならびにトリホスフェート誘導体、それの製造及び使用方法、及び核酸分子（例えば、アプタマー）の一部としての組成物ならびに修飾ヌクレオシドの使用を提供する。【解決手段】下記式Ｉに示される構造を含む化合物。（Ｒは独立して−（ＣＨ２）ｎ−であって、ｎは０〜１０の整数であり；Ｒ'は−Ｈ、−ＯＡｃ、−ＯＢｚ、−Ｐ（ＮｉＰｒ２）（ＯＣＨ２ＣＨ２ＣＮ）、及び−ＯＳｉＭｅ２ｔＢｕから成る群から独立して選択され；Ｒ''は水素、４，４'−ジメトキシトリチル（ＤＭＴ）及びトリホスフェート（−Ｐ（Ｏ）（ＯＨ）−Ｏ−Ｐ（Ｏ）（ＯＨ）−Ｏ−Ｐ（Ｏ）（ＯＨ）２）またはそれらの塩から成る群から独立して選択される。）【選択図】なし