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-10947203-B2 优先权日:2016-03-25 标题 :1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor 发明人:CHEN TAOSHENG; LIN WENWEI; WANG YUEMING 权利人:ST JUDE CHILDRENS RES HOSPITAL; ST JUDE CHILDRENS RSEARCH HOSPITAL 摘要:In an aspect, the invention relates to 1,4,5-substituted 1,2,3-triazole and 1,2,4,5-substituted imidazoles having a structure represented by a formula: n nwhich are modulators the pregnane X receptor (“PXRâ€?); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of modulating an adverse drug reaction in a mammal using the compounds and pharmaceutical compositions; methods of treatment of a disorder of uncontrolled cellular proliferation, such as a cancer, using the compounds and pharmaceutical compositions; methods of modulating pregnane X receptor activity in a mammal using the compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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:US-10363247-B2 优先权日:2015-08-18 标 题:(S,E)-3-(6-aminopyridin-3-yl)-N-((5-(4-(3-fluoro-3-methylpyrrolidine-1-carbonyl)phenyl-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide for the treatment of cancer 发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to substituted benzofuranyl compounds and, more particularly, to a compound represented by Structural Formula 1a: (I) or a pharmaceutically acceptable salt thereof. The invention also includes the synthesis and use of the compound of Structural Formula 1a, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of diseases or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disease) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
专利号:CA-3219525-A1 优先权日:2021-05-20 标 题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
参考文献:10.1186/s12941-017-0228-7 摘要:Rahman L, Shinwari ZK, Iqrar I, Rahman L, Tanveer F. An assessment on the role of endophytic microbes in the therapeutic potential of Fagonia indica. Annals of Clinical Microbiology and Antimicrobials. 2017 Aug 01;16(1):53. doi: 10.1186/s12941-017-0228-7.