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-7279572-B2 优先权日:2003-05-22 标题:Process for the 2-stage synthesis of hexanitrohexaazaisowurtzitane starting from a primary amine 发明人:CAGNON GUY; ECK GENEVIEVE; HERVE GREGOIRE; JACOB GUY 权利人:SNPE MATERIAUX ENERGETIQUES 摘要:A subject-matter of the present invention is a novel process for the synthesis of hexanitrohexaazaisowurtzitane (HNIW), a compound of use as energetic filler in powders, propellants and explosives. n This process comprises a first stage of reaction of an α,β-dicarbonyl derivative with a primary amine which makes it possible to form a hexasubstituted hexaazaisowurtzitane derivative. n The HNIW is subsequently obtained directly, in a single reaction stage, by nitration of the hexasubstituted hexaazaisowurtzitane derivative. n This process, in only 2 stages starting from a primary amine, is particularly simple and inexpensive.
专利号:US-5948693-A 优先权日:1994-09-01 标题:Solid phase synthesis of immunosuppressive agents 发明人:RICH DANIEL H; RAMAN PRAKASH; ANGELL YVONNE M 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention relates generally to cyclosporin analogs, and more paritcularly to methods for the solid-phase synthesis and on-resin cyclization of cyclosporin analogs. Methods are described for the on-resin cyclization of sterically hindered compounds synthesized through solid phase synthesis techniques. The methods utilize solvent, temperature, and washing conditions that allow the efficient on-resin cyclization of compounds like analogs of cyclosporin A.
专利号:US-7157477-B2 优先权日:2000-10-25 标题 :Aliphatic amino-substituted demethoxylated hypocrellins and their synthesis 发明人:ZHANG MANHUA; XU SHANGJIE; WU TAO; CHEN SHEN; SHEN TAO 权利人:INST OF PHOTOGRAPHIC CHEMISTRY 摘要:The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.