Dl-赖氨酸,阿司匹林 以 水,丙酮 作为反应溶剂,化学反应 1.0H,以92.4%的收率获得产物赖氨匹林 参考文献:Method For Preparing A Salt Of Acetylsalicylic Acid And A Basic Amino Acid 标题:Method For Preparing A Salt Of Acetylsalicylic Acid And A Basic Amino Acid 摘要:一种制备乙酰水杨酸和基本氨基酸盐的方法.在常压下,将乙酰水杨酸溶液和所述基本氨基酸溶液在温度低于或等于30oc的条件下混合在反应器中.通过同时逐渐将乙酰水杨酸和基本氨基酸以等摩尔量引入反应器中,形成混合物.
专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-9051302-B2 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents 发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN 权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG 摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:US-10882811-B2 优先权日:2016-12-23 标题 :Synthesis of lysine acetylsalicylate glycine particles 发明人:NOCKER KARLHEINZ; ZUHSE RALF; OSTROVSKYI DMYTRO 权利人:ASPIAIR GMBH 摘要:The invention relates to a method for the production of acetylsalicylic acid lysinate, optionally lysine acetylsalicylate.glycine, comprising the following steps: a) providing a solution of acetylsalicylic acid in ethanol; b) providing an aqueous solution of lysine; c) combining the solutions of step a) and b) to form a mixture; d) optionally stirring the mixture; e) adding acetone to the mixture; f) incubating the mixture, to allow the formation of a acetylsalicylic acid lysinate product; g) isolating the acetylsalicylic acid lysinate product; wherein acetylsalicylic acid is used in excess compared to lysine and wherein no seed crystals are added to the mixture; and optionally the following further steps: h) providing a recrystallized glycine; wherein the glycine has been recrystallized with the following steps: h1) dissolving glycine in water; h2) adding acetone to the glycine solution; h3) stirring the mixture until a precipitate is obtained; i) combining the recrystallized glycine of step h) with the acetylsalicylic acid lysinate product of step g) to obtain lysine acetylsalicylate.glycine (LASAG) particles.
专利号:US-2025073250-A1 优先权日:2022-01-05 标题:Improved synthesis of lysine acetylsalicylate - Glycine particles 发明人:NOCKER KARLHEINZ; ZUHSE RALF; VON SCHRADER THOMAS; BRAUNE CHRISTIAN 权利人:ASPIAIR GMBH 摘要:The invention provides an improved method for preparing lysine acetylsalicylateâ‹…glycine (LASAG) that allows for high yields without the need for an addition of seed crystal, as well as yielding controlled, small particle sizes (median particles size preferably <40 μm) and high stability of the LASAG. Advantageously, the method can be performed at room temperature without negatively impacting yield or particle properties. The invention also provides the LASAG obtained from said method, and its uses as a medicine.
专利号:US-9994558-B2 优先权日:2013-09-20 标题 :Multicyclic compounds and methods of using same 发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).
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合成参考文献
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