专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-11466046-B2 优先权日:2014-10-08 标题 :14-membered ketolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.
专利号:US-9790531-B2 优先权日:2012-08-14 标 题 :Enzymes and polymerases for the synthesis of RNA 发明人:WANG YUXUN; RAMAKRISHNAN DIVAKAR; DE FOUGEROLLES ANTONIN; WHORISKEY SUSAN 权利人:MODERNATX INC 摘要:The invention relates to compositions and methods for the design, evolution, preparation, and/or manufacture of enzymes for use with polynucleotides, primary transcripts and mmRNA molecules.
专利号:US-9273084-B2 优先权日:2012-04-06 标 题 :Moenomycin analogs, methods of synthesis, and uses thereof 发明人:KAHNE DANIEL EVAN; KAHNE SUZANNE WALKER; TSUKAMOTO HIROKAZU 权利人:HARVARD COLLEGE 摘要:The present invention provides compounds of Formula (I); or a pharmaceutically acceptable form thereof; wherein R 1 ,R 2 ,R 3 ,R 6 ,R 7 ,R 12 ,R a , and R b are as defined herein, and G is a group of Formula (a), (b), or (c): Formula (II), wherein X 1 ; X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , Y, R C , R d , R z , a, d, e, x, n, and m are as defined herein. The present invention further provides pharmaceutical compositions comprising a compound of Formula (I), kits comprising such compositions, methods of use and treatment, and preparative methods.
专利号:EP-4339199-A2 优先权日:2017-10-04 标题:Synthesis of cantharidin
专利号:US-9321713-B2 优先权日:2011-06-03 标 题:Hyperforin analogs, methods of synthesis, and uses thereof 发明人:SHAIR MATTHEW D; SPARLING BRIAN A; MOEBIUS DAVID 权利人:SHAIR MATTHEW D; SPARLING BRIAN A; MOEBIUS DAVID; HARVARD COLLEGE 摘要:The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisioned useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.
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