CAS: 85482-13-9; 2-(Bromomethyl)-1,4-Dichlorobenzene

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CAS号34145-05-6 2,5-二氯苯甲醇 | CAS号19398-61-9 2,5-二氯甲苯 | CAS号3218-50-6 2,5-二氯苯乙腈 | CAS号10541-69-2 2,5-二氯苄胺

2,5-二氯苯甲酸置于三溴化磷,Diborane(6)体系中,用 四氢呋喃,二氯甲烷 作为反应溶剂,化学反应 4.0H,反应生成 2,5-二氯苄基溴
参考文献:Discovery,Synthesis And Anti-Atherosclerotic Activities Of A Novel Selective Sphingomyelin Synthase 2 Inhibitor
标题:Discovery,Synthesis And Anti-Atherosclerotic Activities Of A Novel Selective Sphingomyelin Synthase 2 Inhibitor
摘要:The Sphingomyelin Synthase 2 (Sms2) Is A Potential Target For Pharmacological Intervention In Atherosclerosis. However,So Far,Few Selective Sms2 Inhibitors And Their Pharmacological Activities Were Reported. In This Study,A Class Of 2-Benzyloxybenzamides Were Discovered As Novel Sms2 Inhibitors Through Scaffold Hopping And Structural Optimization. Among Them,Ly93 As One Of The Most Potent Inhibitors Exhibited Ic50 Values Of 91 Nm And 133.9 Mu M Against Purified Sms2 And Sms1 Respectively. The Selectivity Ratio Of Ly93 Was More Than 1400-Fold For Purified Sms2 Over Sms1. The In Vitro Studies Indicated That Ly93 Not Only Dose-Dependently Diminished Apob Secretion From Huh7 Cells,But Also Significantly Reduced The Sms Activity And Increased Cholesterol Efflux From Macrophages. Meanwhile,Ly93 Inhibited The Secretion Of Lps-Mediated Pro-Inflammatory Cytokine And Chemokine In Macrophages. The Pharmacokinetic Profiles Of Ly93 Performed On C57Bl/6J Mice Demonstrated That Ly93 Was Orally Efficacious. As A Potent Selective Sms2 Inhibitor,Ly93 Significantly Decreased The Plasma Sm Levels Of C57Bl/6J Mice. Furthermore,Ly93 Was Capable Of Dose-Dependently Attenuating The Atherosclerotic Lesions In The Root And The Entire Aorta As Well As Macrophage Content In Lesions,In Apolipoprotein E Gene Knockout Mice Treated With Ly93. In Conclusion,We Discovered A Novel Selective Sms2 Inhibitor Ly93 And Demonstrated Its Anti-Atherosclerotic Activities In Vivo. The Preliminary Molecular Mechanism-Of-Action Studies Revealed Its Function In Lipid Homeostasis And Inflammation Process,Which Indicated That The Selective Inhibition Of Sms2 Would Be A Promising Treatment For Atherosclerosis. (C) 2018 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2018.12.028

专利信息

专利号:US-2013274466-A1
优先权日:2010-09-27
标 题:Process for the preparation of tetracyclic derivatives and intermediate products used in the process
发明人：GORIN BORIS; DIXON CRAIG EDWARD; QU YANG
权利人:GORIN BORIS; DIXON CRAIG EDWARD; QU YANG; ALPHORA RES INC
摘要:A process for preparation of a compound of formula I or a pharmaceutically acceptable salt thereof, is disclosed. The process involves subjecting a compound of formula II to Ullmann-type conditions to effect an intra-molecular ring closure reaction to form the compound of formula I. The different substituents are as described in the specification. Further, the process can provide an alternate route for the synthesis of asenapine from starting materials that can be readily available.

专利号:US-7250410-B2
优先权日:2001-06-07
标题:Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof
发明人：BOURGUIGNON JEAN-JACQUES; LAGOUGE YAN; LUGNIER CLAIRE; KLOTZ EVELINE; MACHER JEAN-PAUL; RABOISSON PIERRE; SCHULTZ DOMINIQUE
权利人:VIA PHARMACEUTICALS INC
摘要:The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates. The inventive compounds more particularly correspond to general formula (I):

专利号:US-7825149-B2
优先权日:2006-01-19
标 题 :Substituted imidazoles
发明人：CHUBB NATHAN ANTHONY LOGAN; COX MARK ROGER; DAUVERGNE JEROME SEBASTIEN; EWIN RICHARD ANDREW; LAURET CHRISTELLE
权利人:PFIZER LTD
摘要:This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.