Synthesis and anti-Influenza virus activity of 7-O-Alkylated derivatives related to zanamivir
摘要:
A series of 7-alkyl ether derivatives related to zanamivir were synthesized using direct alkylation of the C-7 alcohol of sialic acid. Alkyl ether moiety of less than 12 carbons in length showed low nanomolar inhibitory activity against influenza A virus sialidase. Furthermore, their moiety improved influenza A virus plaque reduction activity compared to zanamivir. However, removal of the 8,9-diol of the 7-O-alkyl derivatives resulted in loss of antiviral potency. This result suggests that 8,9-diol must play an important role in binding with both influenza A and B virus sialidases. (C) 2002 Elsevier Science Ltd. All rights reserved.
[EN] MULTICOMPONENT CRYSTALLINE SYSTEM OF EZETIMIBE AND PROLINE<br/>[FR] SYSTÈME CRISTALLIN À PLUSIEURS COMPOSANTS CONSTITUÉ D'ÉZÉTIMIBE ET DE PROLINE
申请人:BASF SE
公开号:WO2013014604A1
公开(公告)日:2013-01-31
Provided is a crystalline composition comprising a mixture of a compound of formula 1 (Ezetimibe) and proline or proline derivatives, or a hydrate/solvate thereof, as well as a process for obtaining the same. And a process for the purification of Ezetimibe is also disclosed.
Method of synthesis and isolation of solid N-desmethylclozapine and crystalline forms thereof
申请人:Tolf Bo-Ragnar
公开号:US20050282800A1
公开(公告)日:2005-12-22
Disclosed herein are crystalline Forms A, B, C, D, and E of N-desmethylclozapine, methods of preparing the same, pharmaceutical compositions comprising the same, and methods of therapeutic treatment involving N-desmethylclozapine polymorphic forms.
Salt of dimethylaminomethyl-phenyl-cyclohexane and crystalline forms thereof
申请人:Gruss Michael
公开号:US20070032551A1
公开(公告)日:2007-02-08
Novel 3-[2-(dimethylamino)methyl-(cyclohex-1-yl)]-phenol fumarate compounds corresponding to formula I:
and processes for preparing these compounds are provided. Pharmaceutical compositions including these compounds and methods of treating or alleviating pain with these compounds are also provided.
Provided is a mirabegron-containing pharmaceutical composition in which the leakage of mirabegron can be inhibited when the pharmaceutical composition is dispersed in a liquid, and in which the change in pharmacokinetics caused by the presence or absence of food intake is decreased. The pharmaceutical composition comprises an acid addition salt of alkyl sulfuric acid and mirabegron, and a base for modified release.
Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
申请人:Rogers D. Robin
公开号:US20070093462A1
公开(公告)日:2007-04-26
Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.