专利号:US-6025502-A 优先权日:1999-03-19 标题:Enantopselective synthesis of methyl phenidate 发明人:WINKLER JEFFREY DAVID; AXTEN JEFFREY M; KRIM LORI 权利人:UNIV PENNSYLVANIA 摘要:The invention relates to an enantioselective method of making methylphenidate and derivatives thereof. The method involves use of a rhodium catalyst, and selectively produces the D-enantiomer of the methylphenidate derivative in excess of the L-enantiomer thereof. Furthermore, the method selectively produces the threo-diastereomer in excess of the erythro-diastereomer. The method is thus suitable for synthesis of D-threo-methylphenidate (the biologically active form of this compound) and derivatives thereof.
专利号:WO-2024172286-A1 优先权日:2023-02-14 标题 :Synthesis of photodegradable iron nitrosyl complex and development of pharmaceutical composition for prevention or treatment of vascular diseases, using same 发明人:CHO JAEHEUNG; LEE JUNYEOP; CHOE JISU 权利人:ULSAN NATIONAL INSTITUTE OF SCIENCE AND TECH; ASAN FOUND; UNIV ULSAN FOUND IND COOP 摘要:The present invention relates to a compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof, a compound represented by chemical Formula 2 or a pharmaceutically acceptable salt thereof, a preparation method thereof, and uses of the compound represented by chemical formula 2 or a pharmaceutically acceptable salt thereof. The compound represented by chemical formula 2 or a pharmaceutically acceptable salt thereof exhibits the effect of releasing nitric oxide in vivo upon light stimulation, thereby dilating blood vessels.
专利号:US-11155562-B2 优先权日:2014-06-30 标 题 :Synthesis of halichondrin analogs and uses thereof 发明人:KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE 权利人:HARVARD COLLEGE 摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
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-2014378538-A1 优先权日:2011-12-14 标 题:Methods of responding to a biothreat 发明人:BANCEL STEPHANE 权利人:MODERMA THERAPEUTICS INC 摘要:The present disclosure provides for devices, in particular mobile devices, which may be used in the synthesis of modified nucleic acid molecules, in particular modified mRNA molecules. The device for making the modified nucleosides, modified nucleotides and modified nucleic acids (e.g., mRNA) disclosed herein may be mobile devices comprising at least one sample block for insertion of one or more sample vessels, a device base with electronic control units for the sample block, a voltage supply, and one or more reagent(s) for the synthesis of at least one nucleic acid.
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.