Neuartige basische Liganden für die homogenkatalytische Methanolcarbonylierung X. Synthese, eigenschaften und komplexchemie mehrzähniger alkoxyethylphosphane und ihr verhalten als steuerliganden bei der methanolhydrocarbonylierung
从2-氨基-4,5-二氢萘并[2,1- b ]噻吩-1开始,制备了几种含有二氢萘,萘[ 2,1- b ]噻吩和噻吩并[2,3- d ]嘧啶环系统的衍生物。腈(1)。还进行了thioxo衍生物7的结构表征,并研究了其与某些氯和溴代烷基试剂的反应。此外,通过确定EC 50和LD 50来测试制备的产物对H5N1病毒的抗病毒活性[A /鸡/埃及/ 1/2006(H5N1)],并通过在MDCK细胞上的噬斑减少试验来证实。化合物5,7和8 与其他测试化合物相比,显示出最高的效果。
[EN] 5-O-SUBSTITUTED 3-N-PHENYL-1,3,4-OXADIAZOLONES FOR MEDICAL USE<br/>[FR] 3-N-PHÉNYL-1,3,4-OXADIAZOLONES 5-O-SUBSTITUÉES POUR UNE UTILISATION MÉDICALE
申请人:BIAL PORTELA & COMPANHIA S A
公开号:WO2009084970A1
公开(公告)日:2009-07-09
The present invention relates to compounds having a 5-O-substituted 3-N-phenyl-1,3,4-oxadiazolone structural unit which have unexpectedly high level of inhibition of FAAH (fatty acid amide hydrolase). (I)
[EN] KCNT1 INHIBITORS AND METHODS OF USE<br/>[FR] INHIBITEURS DE KCNT1 ET PROCÉDÉS D'UTILISATION
申请人:PRAXIS PREC MEDICINES INC
公开号:WO2020227097A1
公开(公告)日:2020-11-12
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
Novel Solid-Phase Parallel Synthesis of <i>N</i>-Substituted-2-aminobenzo [<i>d</i>]thiazole Derivatives via Cyclization Reactions of 2-Iodophenyl Thiourea Intermediate Resin
作者:Seul-Gi Kim、Se-Lin Jung、Gee-Hyung Lee、Young-Dae Gong
DOI:10.1021/co300112b
日期:2013.1.14
N-sulfonyl-2-aminobenzo[d]thiazole derivatives. The key step in this procedure involves the preparation of polymer-bound 2-aminobenzo[d]thiazole resins 5 by cyclization reaction of 2-iodophenyl thiourea resin 3. The resin-bound 2-iodophenyl thiourea 3 is produced by addition of 2-iodophenyl isothiocyanate 2 to the amine-terminated linker amide resin 1. These core skeleton 2-aminobenzo[d]thiazole resins 5 undergo
已经开发了用于合成N-烷基,N-酰基和N-磺酰基-2-氨基苯并[ d ]噻唑衍生物的新型固相方法。该过程中的关键步骤涉及通过2-碘苯基硫脲树脂3的环化反应制备与聚合物结合的2-氨基苯并[ d ]噻唑树脂5。通过将2-碘苯基异硫氰酸酯2添加到胺封端的连接酰胺树脂1中来生产树脂结合的2-碘苯基硫脲3。这些核心骨架的2-氨基苯并[ d ]噻唑树脂5经历与各种亲电子,如烷基卤,酰基氯,和磺酰氯官能化反应以产生Ñ -烷基,Ñ -酰基,和Ñ磺酰基-2-氨基苯并[ d ]噻唑树脂6,7,和8,分别。最后,Ñ -烷基,Ñ -酰基,和Ñ磺酰基-2-氨基苯并[ d ]噻唑衍生物9,10,和11,然后在良好的产率和纯度通过各树脂的切割产生6,7,和8 在二氯甲烷(DCM)中使用三氟乙酸(TFA)。
Mixing divalent ionic liquids: effects of charge and side-chains
作者:Eduards Bakis、Adriaan van den Bruinhorst、Laure Pison、Ivan Palazzo、Thomas Chang、Marianne Kjellberg、Cameron C. Weber、Margarida Costa Gomes、Tom Welton
DOI:10.1039/d1cp00208b
日期:——
We have prepared novel divalent ionic liquids (ILs) based on the bis(trifluoromethylsulfonyl)imide anion where two charged imidazolium groups in the cations are either directly bound to each other or linked by a single atom. We assessed the influence of the side-chain functionality and divalency on their physical properties and on the thermodynamics of mixing. The results indicate that shortening the
[EN] SUBSTITUTED PIPERAZINES, (1,4) DIASZEPINES, AND 2,5-DIAZABICYCLO (2.2.1) HEPTANES AS HISTAMINE H1 AND/OR H3 ANTAGONISTS OR HISTAMINE H3 REVERSE ANTAGONISTS<br/>[FR] PIPERAZINES, (1,4) DIAZEPINES, ET 2,5-DIAZABICYCLO (2.2.1) HEPTANES SUBSTITUES EN TANT QU'ANTAGONISTES DE L'HISTAMINE H1 ET/OU H3 OU ANTAGONISTES INVERSES DE L'HISTAMINE H3
申请人:GLAXO GROUP LTD
公开号:WO2004035556A1
公开(公告)日:2004-04-29
The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.