专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2018148745-A1 优先权日:2015-05-26 标题:Hemoprotein catalysts for improved enantioselective enzymatic synthesis of ticagrelor 发明人:ARNOLD FRANCIS H; RENATA HANS; MCINTOSH JOHN A; LEWIS RUSSELL D; KAN SEK BIK JENNIFER; HERNANDEZ KARI; COELHO PEDRO; ROZZELL DAVID; ZHANG CHEN 权利人:CALIFORNIA INST OF TECHN; PROVIVI INC 摘要:The present invention provides methods by which trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine and related cyclopropane compounds are prepared using synthetic strategies that include a biocatalytic cyclopropanation step.
专利号:US-8093381-B2 优先权日:2007-05-24 标题:Method of synthesis of fluoroquinolones 发明人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS 权利人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS; BIOCODEX 摘要:The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and X are as defined in Claim 1.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-7632944-B2 优先权日:2007-01-24 标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same 发明人:HARMS ARTHUR E 权利人:BAUSCH & LOMB 摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
专利号:US-8227597-B2 优先权日:2006-10-06 标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same 发明人:HARMS ARTHUR E 权利人:HARMS ARTHUR E; BAUSCH & LOMB 摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
1: Wang H, Lekkala S, Ren Y, Tay AJH, Neighbors J, Ebetino FH, Sun S, Joseph NM, Schwarz EM, Xie C. Effects of hydroxybisphosphonates-conjugated sitafloxacin on fracture healing and skeletal growth in mice. JBMR Plus. 2025 Dec 24;10(2):ziaf195. doi: 10.1093/jbmrpl/ziaf195. 2: Mori H, Saito Y, Ando H, Masaoka T, Matsuzaki J, Nakano M, Kanai T. Third- Line and Later Susceptibility-Guided Helicobacter pylori Eradication Therapies: A Multicenter Study of Vonoprazan-Amoxicillin-Sitafloxacin/Rifabutin Regimens. J Clin Med. 2026 Jan 6;15(2):434. doi: 10.3390/jcm15020434. 3: Urabe N, Sakamoto S, Tokita N, Kanokogi T, Tsunehara R, Kishi K. Clinical efficacy of sitafloxacin-containing regimens for Mycobacterium avium complex pulmonary disease. BMC Pulm Med. 2025 Nov 18;25(1):532. doi: 10.1186/s12890-025-04004-1.