N6-(5,6-epoxynorbornyl)adenosine analogs as A1 adenosine agonists
摘要:
A range of related adenosines and 5'-N-ethylcarboxamidoadenosines bearing oxygenated substituents in the N-6 position have been synthesised and evaluated as A(1)-adenosine receptor ligands. Compound 9 emerged with potent affinity (EC50 = 1.1 nM). (C) 1998 Elsevier Science Ltd. All rights reserved.
Alkyl and aryl isothiocyanates as masked primary amines
摘要:
Primary and secondary (but not tertiary) alkyl as well as aryl isothiocyanates react rapidly with 4-methyl-1,2-benzenedithiol (1) in methanol at room temperature, releasing the corresponding amines in good yields. This mild and simple procedure for unmasking amines proceeds chemospecifically with isothiocyanates even in the presence of such normally electrophilic and reactive functionalities as carboxylate ester and N-alkylphthalimide.
[EN] 2,6-QUINOLINYL AND 2,6-NAPHTHYL DERIVATIVES, PROCESSES FOR PREPARING THEM AND THEIR USES AS VLA-4 INHIBITORS<br/>[FR] DERIVES DE 2,6-QUINOLINYLE ET DE 2,6-NAPHTYLE, LEURS PROCEDES DE PREPARATION ET LEUR UTILISATION COMME INHIBITEURS DE VLA-4
申请人:UCB SA
公开号:WO2003093237A1
公开(公告)日:2003-11-13
The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals for the treatment of VLA-4 dependent inflammatory diseases such as for example asthma, allergic rhinitis, sinusitis, conjunctivitis, food allergy, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and atherosclerosis. Formula (I): wherein X is N or CH.
The flash vacuum thermolysis and/or gasâsolid phase multistep sequences allow the synthesis of vinylideneamine and a safe, preparative-scale synthesis of Î1-azirine.
通过闪蒸真空热解和/或气固相多步顺序,可以合成亚乙烯基胺,并安全地制备出δ1-氮丙啶。
Substituted Oxadiazoles for Combating Phytopathogenic Fungi
申请人:BASF SE
公开号:US20200045974A1
公开(公告)日:2020-02-13
The present invention relates to novel trifluoromethyloxadiazoles of the formula I, or the N-oxides, or the agriculturally useful salts thereof; and to their use for controlling phytopathogenic fungi; and to a method for combating phytopathogenic harmful fungi, which process comprises treating the fungi, the plants, the soil or seeds to be protected against fungal attack, with an effective amount of at least one compound of the formula I, or an N-oxide, or an agriculturally acceptable salt thereof; and to agrochemical compositions comprising at least one compound of the formula I; and to agrochemical compositions further comprising seeds.
[EN] DEGRADABLE POLYMERIC TISSUE SCAFFOLD<br/>[FR] ÉCHAFAUDAGE DE TISSU POLYMÈRE DÉGRADABLE
申请人:MOSAIC BIOSCIENCES INC
公开号:WO2020232270A1
公开(公告)日:2020-11-19
The present disclosure relates generally to degradable polymeric scaffolds, methods of making them, and their use in the biomedical field.
本公开涉及可降解聚合物支架,其制备方法以及在生物医学领域中的应用。
[EN] NOVEL A1 ADENOSINE RECEPTOR AGONISTS AND ANTIAGONISTS<br/>[FR] NOUVEAUX AGONISTES ET ANTAGONISTES DE RECEPTEURS DE L'ADENOSINE A1
申请人:UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
公开号:WO1995011904A1
公开(公告)日:1995-05-04
(EN) Adenosine and xanthine derivatives, and compositions comprising those compounds, are potent selective agonists and antagonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias.(FR) On décrit des dérivés d'adénosines et de xanthines, qui sont de puissants agonistes et antagonistes sélectifs de récepteurs d'une adénosine, ainsi que des compositions contenant ces composés. On utilise ces dérivés et compositions pour traiter des pathologies telles que certaines arythmies cardiaques.