[EN] SUBSTITUTE 1, 6-NAPHTHYRIDINES FOR USE AS SCD INHIBITORS<br/>[FR] 1,6-NAPHTYRIDINES SUBSTITUÉES EN VUE D'UNE UTILISATION EN TANT QU'INHIBITEURS DE SCD
申请人:SMITHKLINE BEECHAM CORP
公开号:WO2009056556A1
公开(公告)日:2009-05-07
The present invention relates to substituted tetrahydronaphthyridine (THN) compounds of the formula (I) and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity.
Fluorine-containing 2,3-diaryl quinolines as potent inhibitors of methicillin and vancomycin-resistant Staphylococcus aureus: Synthesis, antibacterial activity and molecular docking studies
affect a large section of global population. Antibacterial drug discovery has stagnated owing to multiple factors including unattractive returns for major pharmaceutical companies. Thus, discovery of effective antibacterial drugs against drug-resistant bacteria is an urgent unmet need affecting healthcare systems globally. In this study, fluorine-containing 2,3-diarylquinolines (4a-l) and non-fluorinated
耐药细菌是一个主要的健康问题,并影响到全球大部分人口。由于主要制药公司的回报不具吸引力等多种因素,抗菌药物的发现停滞不前。因此,发现针对耐药细菌的有效抗菌药物是影响全球医疗保健系统的紧迫未满足需求。在这项研究中,利用芳烃重氮盐和芳炔的环境友好化学合成了含氟2,3-二芳基喹啉 ( 4a - l ) 和非氟化类似物4m,用于在 C-2 和 C-3 位置区域选择性安装芳基,分别。体外针对各种革兰氏阴性和革兰氏阳性细菌的抗菌评估显示,这些化合物中的大多数对革兰氏阳性金黄色葡萄球菌ATCC 29213 具有抑制活性。化合物4e、4i、4j和4l是最有效的抑制剂,MIC 值为 10.95-24.0 µM . 没有一种化合物能抑制革兰氏阴性菌。4e、4i和4l还显示出对 Vero 细胞的低水平细胞毒性,因此提供了高安全性。重要的是,4e、4i和4l表现出对甲氧西林和耐万古霉素的金黄色葡萄球菌的同等抑制作
Nitrogen bridgehead compounds. Part 18. New antiallergic 4H-pyrido[1,2-a]pyrimidin-4-ones. Part I
A new type of antiallergic agent, 9-hydrazono-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-ones, was synthesized and evaluated for inhibitory effects in the rat reagenic passive cutaneous anaphylaxis (PCA) screen. Several racemic 6-methyl derivatives were found to be more potent than disodium chromoglycate intravenously and some were also active orally. Structure-activity relationships are discussed
合成了一种新型的抗过敏药9-肼基-6,7,8,9-四氢-4H-吡啶并[1,2-a]嘧啶-4-酮,并评估了其对大鼠自发性被动皮肤的抑制作用。过敏反应(PCA)屏幕。已发现几种消旋的6-甲基衍生物在静脉内比色甘氨酸二钠更有效,有些还具有口服活性。讨论了构效关系。在具有6S和6R绝对构型的对映异构体之间的6-甲基系列中观察到高立体特异性,前者更具活性。化合物17,(+)-6(S)-甲基-9-(苯肼基)-4-氧代-4H-吡啶并[1,2-a]嘧啶-3-羧酸[Chinoin-1045; [UCB L140],ED50值为1.0 mumol / kg po,目前正在临床研究中。
[EN] N-THIAZOLYL-1, 2, 3, 4-TETRAHYDRO-6-ISOQUINOLINECARBOXAMIDE DERIVATIVES AS INHIBITORS OF STEAROYL COENZYME A DESATURASE<br/>[FR] DÉRIVÉS DE N-THIAZOLYL-1, 2, 3, 4-TÉTRAHYDRO-6-ISOQUINOLINE CARBOXAMIDE COMME INHIBITEURS DE LA STÉAROYLE COA DÉSATURASE
申请人:SMITHKLINE BEECHAM CORP
公开号:WO2009150196A1
公开(公告)日:2009-12-17
The present invention relates to substituted thiazole compounds of the formula (I) wherein Z represents (A), (B), (C) and (D) where * represents the point of attachment and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity.
Flow synthesis of ethyl isocyanoacetate enabling the telescoped synthesis of 1,2,4-triazoles and pyrrolo-[1,2-c]pyrimidines
作者:Marcus Baumann、Antonio M. Rodriguez Garcia、Ian R. Baxendale
DOI:10.1039/c5ob00245a
日期:——
The efficient flow synthesis of important heterocyclic building blocks based on the 1,2,4-triazole and pyrrolo[1,2-c]pyrimidine scaffold has been achieved.