专利号:US-2023286915-A1 优先权日:2020-10-07 标 题 :Synthesis of pyrrole acid derivatives 发明人:WILKINSON ANDREW; COOPER LAN; ORR DAVID; FINLAYSON JONATHAN; BUNT ADAM; KIRKHAM JAMES; LYTH DAVID; BLADES KEVIN 权利人:INFEX THERAPEUTICS LTD 摘要:This invention relates to the synthesis of compounds that can be used to treat bacterial infections in combination with other antibacterial agents, and more specifically in combination with a class of antibacterial agents known as carbapenems. The compounds resulting from the novel methods of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.
专利号:US-7728135-B2 优先权日:2005-01-06 标 题:Synthesis of CCR5 receptor antagonists 发明人:SHI XIONGWEI; ZHU MAN; LEONG WILLIAM; DAHANUKAR VILAS; ZAVIALOV ILIA A; PROIETTI CECELIA; ZHAO SHANNON; LEE HONG-CHANG; LIU YI; NGUYEN HOA N; WU WENXUE; D SA BOSCO; LIANG FENG; TRAN LOC THANH 权利人:SCHERING CORP 摘要:The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.
专利号:US-11028123-B2 优先权日:2018-04-10 标题 :Capping of unprotected amino groups during peptide synthesis 发明人:HENKEL BERND; METZENTHIN TOBIAS; GERKEN MANFRED; FIEDLER WOLFGANG 权利人:SANOFI AVENTIS DEUTSCHLAND 摘要:The present invention relates to a method for the synthesis of a polypeptide comprising a pre-determined amino acid sequence. The method according to the invention comprises coupling cycles of coupling an N-terminally protected amino acid building block C-terminally at an unprotected N-terminal amino group of an amino acid chain, wherein at least one coupling cycle comprises a coupling step (a), a capping step (b), and a de-protecting step (c).
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:WO-2013136265-A1 优先权日:2012-03-13 标 题:Synthesis of an intermediate of an antiviral compound 发明人:ATTOLINO EMANUELE; BOVE ALESSIO; BRUNOLDI ENRICO; ALLEGRINI PIETRO 权利人:DIPHARMA FRANCIS SRL 摘要:Process for the preparation of a cyclopropylamide compound which is useful as a structural unit in a process for the preparation of a viral protease inhibitor.
专利号:US-6307071-B1 优先权日:1998-03-02 标 题:Synthesis of paclitaxel from baccatin III by protection of the 7-hydroxyl of baccatin III using a strong base and an electrophile 发明人:GIBSON FRANCIS S 权利人:BRISTOL MYERS SQUIBB CO 摘要:Process for synthesizing paclitaxel by treating baccatin III with a strong base in a solvent, adding an electrophile to the solution to form a 7-O-protected baccatin III derivative, reacting the 7-O-protected baccatin III derivative with a protected paclitaxel sidechain in a solvent such that the protected paclitaxel sidechain is coupled to the 13-hydroxyl of the 7-O-protected baccatin III, and subsequently deprotecting the protected paclitaxel sidechain and the 7-O protecting group to form paclitaxel, and intermediates used therein.