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-4412075-A 优先权日:1981-01-16 标题 :Process for the preparation of quinolin-4-ones 发明人:BAUDOUIN MICHEL; DESBOIS MICHEL 权利人:RHONE POULENC SANTE 摘要:1,2,3,4-Tetrahydroquinolin-4-ones of the formula: ##STR1## wherein R represents a hydrogen or halogen atom, an alkyl radical (1 to 4 carbon atoms), an alkoxy radical (1 to 4 carbon atoms) or the trifluoromethyl radical, and R 1 represents a hydrogen atom, an alkyl radical (1 to 4 carbon atoms) or the trifluoromethyl radical, are prepared by cyclizing a 3-anilinopropionic acid of the formula: ##STR2## (wherein R and R 1 are as hereinbefore defined) in a mixture of hydrofluoric acid and boron trifluoride. n The quinolinone products are useful intermediates in the synthesis of therapeutically active substances.
专利号:AU-2022276509-A1 优先权日:2021-05-20 标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
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).
专利号:WO-2022246227-A1 优先权日:2021-05-20 标 题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
1: Alka K, Casey JR. Molecular phenotype of SLC4A11 missense mutants: Setting the stage for personalized medicine in corneal dystrophies. Hum Mutat. 2018 May;39(5):676-690. doi: 10.1002/humu.23401. Epub 2018 Feb 2. doi: 10.1124/jpet.117.241406. Epub 2017 Jun 19. doi: 10.1007/978-1-4939-3603-8_25. doi: 10.1016/j.jstrokecerebrovasdis.2016.03.045. Epub 2016 May 5. 5: Chiu AM, Mandziuk JJ, Loganathan SK, Alka K, Casey JR. High Throughput Assay Identifies Glafenine as a Corrector for the Folding Defect in Corneal Dystrophy-Causing Mutants of SLC4A11. Invest Ophthalmol Vis Sci. 2015 Dec;56(13):7739-53. doi: 10.1167/iovs.15-17802. doi: 10.1016/j.bcp.2014.11.006. Epub 2014 Nov 22. doi: 10.1242/dmm.009852. Epub 2012 Aug 23. 8: Wen B, Moore DJ. Bioactivation of glafenine by human liver microsomes and peroxidases: identification of electrophilic iminoquinone species and GSH conjugates. Drug Metab Dispos. 2011 Sep;39(9):1511-21. doi: 10.1124/dmd.111.039396. Epub 2011 May 31. doi: 10.1167/iovs.10-5897.