FATTY ACIDS AND USE IN CONJUGATION TO BIOMOLECULES THEREOF

• Main Authors: LOUISE CLARE KIRMAN, AIMEE RICHARDSON USERA, LOU CHANGGANG, ALOKESH DUTTAROY, AVIRUP BOSE, YAMADA TAKESHI, CHIKWENDU IBEBUNJO, YUAN JUN, AARON KANTER, ALEXANDRA MARSHALL BRUCE, FREDERIC ZECRI, DAVID WENINGER BARNES
• Format: Patent
• Language: English; Japanese
• Published: 11.07.2023
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS THEREOF; CULTURE MEDIA; ENZYMOLOGY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPIRITS; VINEGAR; WINE

To provide novel fatty acids and their use in extending the half-life of biomolecules via conjugation.SOLUTION: The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker, the fatty acid having the following formula A1, A2 or A3, or an amide, an ester, or a pharmaceutically acceptable salt thereof, wherein R1 is CO2H or H, R2, R3, and R4 independently represent H, OH, CO2H, -CH=CH2, or -C≡CH, Ak is branched C6-C30 alkylene, and n, m, and p independently represent an integer of 6-30.SELECTED DRAWING: None 【課題】新規な脂肪酸、および生体分子の半減期をコンジュゲーションによって延長する際のその使用を提供する。【解決手段】リンカーを介して脂肪酸に連結している生体分子を含み、脂肪酸は、下式のＡ１、Ａ２、またはＡ３を有する、コンジュゲート、またはそのアミド、エステル、もしくは薬学的に許容される塩。［式中、Ｒ１は、ＣＯ２ＨまたはＨ、Ｒ２、Ｒ３、Ｒ４は互いに独立して、Ｈ、ＯＨ、ＣＯ２Ｈ、－ＣＨ＝ＣＨ２、または－Ｃ≡ＣＨであり、Ａｋは、分枝状Ｃ６～Ｃ３０アルキレンであり、ｎ、ｍ、およびｐは、互いに独立して、６～３０の間の整数である］JPEG2023099133000225.jpg45139【選択図】なし