专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:US-9409945-B2 优先权日:1999-10-04 标 题 :Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery 发明人:DESLONGCHAMPS PIERRE; DORY YVES; BERTHIAUME GILLES; OUELLET LUC; LAN RUOXI 权利人:OCERA THERAPEUTICS INC 摘要:A library of macrocyclic compounds of the formula (I) n n n n n n n n n n n n where part (A) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) y — bivalent radical or a covalent bond; n where part (B) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) z — bivalent radical, or a covalent bond; n where part (C) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) t — bivalent radical, or a covalent bond; and n where part (T) is a —Y-L-Z— radical wherein Y is CH 2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.
专利号:US-4003916-A 优先权日:1975-12-22 标 题:Total synthesis of steganacin and derivatives thereof 发明人:KENDE ANDREW S; LIEBESKIND LANNY S 权利人:KENDE ANDREW S; LIEBESKIND LANNY S 摘要:Steganacin and Steganangin, dibenzocyclooctadiene lignan lactones, have been reported to possess antileukemic activity. This invention describes the first total synthesis of these compounds and other relevant intermediates.
专利号:US-4059593-A 优先权日:1975-12-22 标 题:Synthesis of steganacin and derivatives thereof 发明人:KENDE ANDREW S; LIEBESKIND LANNY S 权利人:UNIV ROCHESTER 摘要:Steganacin and Steganangin, dibenzocyclooctadiene lignan lactones, have been reported to possess anti-leukemic activity. This invention describes the first total synthesis of these compounds and other relevant intermediates.
专利号:US-4448724-A 优先权日:1982-12-20 标题 :Synthesis of 4-demethoxydaunomycinone 发明人:CAVA MICHAEL P; DOMINGUEZ DOMINGO 权利人:UNIV PENNSYLVANIA 摘要:A synthesis of 4-demethoxydaunomycinone and its derivatives from the known compound 9-acetyl-6,11-dihydroxy-7,8,9,10-tetrahydro-5,12-naphthacenedione. 4-Demethoxydaunomycinone may be converted to 4-demethoxydaunorubicin which is an anthracycline derivative known to have antitumor activity.
专利号:US-2016317682-A1 优先权日:2015-04-30 标题:PREPARATION OF Ag18F AND ITS USE IN THE SYNTHESIS OF PET RADIOTRACERS 发明人:SCOTT PETER J H; BROOKS ALLEN F; ICHIISHI NAOKO; SANFORD MELANIE S 权利人:UNIV MICHIGAN REGENTS; THE REGENTS OFTHE UNIV OF MICHIGAN 摘要:Copper-catalyzed radiofluorination of aryl iodides using Ag 18 F, methods of preparing Ag 18 F, and compounds obtained by copper-catalyzed radiofluorination of aryl iodides using Ag 18 F are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.