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-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 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 substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-2018312463-A1 优先权日:2015-10-22 标题:Synthesis of Cyclohexane Carboxamide Derivatives Useful as Sensates in Consumer Products 发明人:YELM KENNETH EDWARD; WOS JOHN AUGUST; BUNKE GREGORY MARK; FREDERICK HEATH; HAUGHT JOHN CHRISTIAN; HOKE STEVEN HAMILTON; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Synthesis methods to produce a series of carboxamides built off of an (S)-2-amino acid backbone or an (R)-2-amino acid backbone, depending upon the desired diastereomer of the end product.
专利号:US-6710185-B2 优先权日:2000-09-20 标 题 :Process for the preparation of cell proliferation inhibitors 发明人:GUPTA ASHOK K; KING STEVEN A; LEE ELAINE C; MORTON HOWARD E; PLATA DANIEL J; PU YU-MING; SHARMA PADAM N 权利人:ABBOTT LAB 摘要:The instant invention discloses a process for the synthesis of substituted indole cell proliferation inhibitors.
专利号:US-2010047841-A1 优先权日:2007-02-27 标 题 :Synthesis of desacetoxytubulysin h and analogs thereof 发明人:WIPF PETER; WANG ZHIYONG 权利人:UNIV PITTSBURGH 摘要:Compounds of formula I, XVI and XXI possess potent cell growth inhibitory activity. These compounds are described have therapeutic utility, particularly in the treatment of cancer as well as conditions and disorders related to uncontrolled cell growth: n n n n n n n n n n wherein the variables R 1 , R 2 , R 3 , R 4 , R 5 , X, Y and Z are described herein.
专利号:WO-2010126607-A2 优先权日:2009-04-30 标 题:Synthesis of tetracyclines and intermediates thereto