专利号:US-2025170267-A1 优先权日:2022-02-28 标 题 :Antibody-drug conjugate precursor and intermediate for synthesis thereof 发明人:TSUZAKI YASUNORI; MIZUNO GEN; KASHIWAGI TAKAMASA; TANAKA MASAYUKI; SHIMIZU HAYATO; NONOUCHI SHIMPEI; MATSUSHITA TAKASHI; KIMURA TOMIO 权利人:UBE CORP 摘要:A method for improving the stability of an antibody-drug conjugate in a living body, and a conjugate precursor for producing a stabilized antibody-drug conjugate. An antibody-drug conjugate precursor represented by the following general formula (I) or a salt thereof, a synthetic intermediate thereof or a salt thereof, n Z-L-D  (I)n n where Z is a reactive group which can react with a functional group present in an antibody or a modified antibody; D is an antitumor drug residue in which one hydrogen atom or one hydroxy group is removed from any position of an antitumor drug molecule or an analog thereof or a derivative thereof; L is a linker which links Z to D; and at least any one of D and L has one or more lactonyl group(s) at any position(s) as substituent(s) or protecting group(s).
1: Masuda N, Takahashi Y, Otsuki M, Ibuki E, Miyoshi H, Nishino T. In vitro and in vivo antibacterial activities of CS-940, a new 6-fluoro-8-difluoromethoxy quinolone. Antimicrob Agents Chemother. 1996 May;40(5):1201-7. doi: 10.1128/AAC.40.5.1201. 2: Biedenbach DJ, Sutton LD, Jones RN. Antimicrobial activity of CS-940, a new trifluorinated quinolone. Antimicrob Agents Chemother. 1995 Oct;39(10):2325-30. doi: 10.1128/AAC.39.10.2325. 3: Schmitz FJ, Jones ME. Antibiotics for treatment of infections caused by MRSA and elimination of MRSA carriage. What are the choices? Int J Antimicrob Agents. 1997 Jun;9(1):1-19. doi: 10.1016/s0924-8579(97)00027-7. 41(11):2582-5. doi: 10.1128/AAC.41.11.2582.
合成参考文献
摘要:Yamane N, Chilima BZ, Tosaka M, Okazawa Y, Tanno K. [Determination of antimycobacterial activities of fluoroquinolones against clinical isolates of Mycobacterium tuberculosis: comparative determination with egg-based Ogawa and agar-based Middlebrook 7H10 media]. Kekkaku. 1996 Aug;71(8):453–8. 摘要:Tanimura H, Ohnishi H. [Transfer of cadrofloxacin, a novel fluoroquinolone antibacterial, into the gallbladder tissue and bile]. Jpn J Antibiot. 2004 Feb;57(1):118–23.