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-9765042-B2 优先权日:2013-10-07 标题 :Methods of chemical synthesis of diaminophenothiazinium compounds including methylthioninium chloride (MTC) 发明人:SINCLAIR JAMES PETER; NICOLL SARAH LOUISE; STOREY JOHN MERVYN DAVID 权利人:WISTA LAB LTD 摘要:Methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compoundsâ€?) including Methythioninium Chloride (MTC) (also known as Methylene Blue) are provided.
专利号:US-2006287257-A1 优先权日:2005-06-20 标 题 :Pharmaceutical compositions to treat diseases caused by mycobacterium 发明人:STOCKEL RICHARD F 权利人:STOCKEL RICHARD F 摘要:The invention teaches the synthesis of pharmaceutical composition and methods of synthesis to treat people and animals infected with a pathogenic mycobacterium. In particular the compositions of this invention are suitable for the treatment of tuberculosis, malaria, and other infections diseases caused by mycobacterium.
专利号:US-7790881-B2 优先权日:2004-09-23 标 题:Methods of chemical synthesis and purification of diaminophenothiazinium compounds including methylthioninium chloride (MTC) 发明人:STOREY JOHN MERVYN DAVID; SINCLAIR JAMES PETER; MARSHALL COLIN; TAN HAN WAN 权利人:WISTA LAB LTD 摘要:This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compoundsâ€?) including Methylthioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). The present invention also pertains to the resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment and diagnosis, etc., for example, for tauopathies, Alzheimer's disease (AD), skin cancer, melanoma, viral diseases, bacterial diseases, or protozoal diseases. Wherein: each of R 1 and R 9 is independently selected from: —H; C 1-4 alkenyl; and halogenated C 1-4 alkyl; each of R 3NA and R 3NB is independently selected from: C 1-4 alkyl; C 2-4 alkenyl; and halogenated C 4-1 alkyl; each of R 7NA and R 7NB is independently selected from: C 1-4 alkyl; C 2-4 alkenyl; and halogenated C 1-4 alkyl; and X is one or more anionic counter ions to achieve electrical neutrality.
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).
1: Kuemmerle A, Gossen D, Marx MW, Lorch U, Szramowska M, Kumar A, Singh D, Singh S, Ramachandruni H, Thankachen B, Kore S, Gaaloul ME, Borghini-Fuhrer I, Chalon S. A randomized, open-label two-period crossover pilot study to evaluate the relative bioavailability in the fed state of atovaquone-proguanil (Atoguanil™) versus atovaquone-proguanil hydrochloride (Malarone®) in healthy adult participants. Naunyn Schmiedebergs Arch Pharmacol. 2024 Jun 25. doi: 10.1007/s00210-024-03245-x. Epub ahead of print. 225:106179. doi: 10.1016/j.actatropica.2021.106179. Epub 2021 Oct 8. 45(6):376-383. doi: 10.1080/01913123.2021.1984349. Epub 2021 Oct 1. 12(1):10.24926/iip.v12i1.3555. doi: 10.24926/iip.v12i1.3555. 5: Lee SH, Kwak D, Kim KT. The first clinical cases of Haemoproteus infection in a snowy owl (Bubo scandiacus) and a goshawk (Accipiter gentilis) at a zoo in the Republic of Korea. J Vet Med Sci. 2018 Aug 10;80(8):1255-1258. doi: 10.1292/jvms.18-0072. Epub 2018 Jun 22.
合成参考文献
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