886-46-4Relevant academic research and scientific papers
HEPATITIS B ANTIVIRAL AGENTS
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Page/Page column 200, (2013/07/05)
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
Synthesis and characterization of enantiomerically pure cis- and trans-3-fluoro-2,4-dioxa-8-aza-3-phosphadecalin 3-oxides as γ- homoacetylcholine mimetics and inhibitors of acetylcholinesterase
Clerc, Christian,Rueedi, Peter
scheme or table, p. 17 - 33 (2012/03/07)
The title compounds, the P(3)-axially and P(3)-equatorially substituted cis- and trans-configured 8-benzyl-3-fluoro-2,4-dioxa-8-aza-3-phosphadecalin 3-oxides (=8-benzyl-3-fluoro-2,4-dioxa-8-aza-3-phosphabicyclo[4.4.0]decane 3-oxides=2-fluorohexahydro-6-(phenylmethyl)-4H-1,3,2-dioxaphosphorino[5,4-c] pyridine 2-oxides) were prepared (ee>98%) and fully characterized (Schemes2 and 3). The absolute configurations were established from that of their precursors, the enantiomerically pure cis- and trans-1-benzyl-4- hydroxypiperidine-3-methanols which were unambiguously assigned. Being configuratively fixed and conformationally constrained phosphorus analogues of acetyl γ-homocholine (=3-(acetyloxy)-N,N,N-trimethylpropan-1-aminium), they are suitable probes for the investigation of molecular interactions with acetylcholinesterase. As determined by kinetic methods, all of the compounds are weak inhibitors of the enzyme. Copyright
5-Quinoline derivatives having an anti-bacterial activity
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Page/Page column 25, (2010/12/31)
The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.
QUINOLONE ANTIBACTERIAL AGENTS
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Page/Page column 84; 107, (2010/02/11)
Compounds of formula (I, II, III, IV, V, and VI) and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula (I) as well as pharmaceutically acceptable compositions comprising compounds of formula (I). Compounds of formula (I) as disclosed herein can be used in a variety of applications including use as antibacterial agents.
2,4-Dioxa-7-aza-, 2,4-dioxa-8-aza-, and 2,4-dioxa-9-aza-3-phosphadecalins as rigid acetylcholine mimetics: Syntheses and characterization
Furegati, Stefan,Ganci, Walter,Gorla, Fabrizio,Ringeisen, Urs,Rueedi, Peter
, p. 2629 - 2661 (2007/10/03)
Phosphorylation of suitable piperidine precursors yielded a series of novel decalin-type O,N,P-heterocycles. The title compounds, P(3)-axially and P(3)-equatorially X-substituted, cis- and trans-configurated 2,4-dioxa-7-aza-, 2,4-dioxa-8-aza-, and 2,4-dioxa-9-aza-3-phosphabicyclo[4.4.0]decane 3-oxides (X = Cl, F, 4-nitrophenoxy, and 2,4-dinitrophenoxy), are configuratively fixed and conformationally constrained P-analogues of acetylcholine and as such represent acetylcholine (7-aza and 9-aza isomers) or γ-homo-acetylcholine mimetics (8-aza isomers). Being irreversible inhibitors of acetylcholinesterase (AChE), the compounds are considered to be suitable probes for the investigation of the stereochemical course of the inhibition reaction by 31P-NMR spectroscopy. Moreover, the design of these mimetics will enable studies of molecular interactions with AChE, in particular, the recognition conformation of acetylcholine.
INHIBITORS OF BACE
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, (2008/06/13)
The present invention relates to inhibitors of aspartic proteinases, particularly, BACE. The present invention also relates to compositions thereof and methods therewith for inhibiting BACE activity in a mammal, and for treating Alzheimer's Disease and other BACE-mediated diseases.
Piperidine-renin inhibitors compounds with improved physicochemical properties
Gueller, Rolf,Binggeli, Alfred,Breu, Volker,Bur, Daniel,Fischli, Walter,Hirth, Georges,Jenny, Christian,Kansy, Manfred,Montavon, Francois,Mueller, Marcel,Oefner, Christian,Stadler, Heinz,Vieira, Eric,Wilhelm, Maurice,Wostl, Wolfgang,Maerki, Hans Peter
, p. 1403 - 1408 (2007/10/03)
Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D((pH 7.4)) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets.
