- BACE1 INHIBITORS
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The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
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Page/Page column 51; 52
(2017/03/08)
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- Rhodium(I)-catalyzed borylation of nitriles through the cleavage of carbon-cyano bonds
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The reaction of aryl cyanides with diboron in the presence of a rhodium/Xantphos catalyst and DABCO affords arylboronic esters via carbon-cyano bond cleavage. This unprecedented mode of reactivity for a borylrhodium species allows the regioselective intro
- Tobisu, Mamoru,Kinuta, Hirotaka,Kita, Yusuke,Remond, Emmanuelle,Chatani, Naoto
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supporting information; experimental part
p. 115 - 118
(2012/03/07)
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- NOVEL OXADIAZOLE COMPOUNDS
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Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation o
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Page/Page column 124
(2011/06/26)
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- Subtlety of the Structure-Affinity and Structure-Efficacy Relationships around a Nonpeptide Oxytocin Receptor Agonist
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Very few nonpeptide oxytocin agonists have currently been reported, and none of them seem suitable for the in vivo investigation of the oxytocin mediated functions. In an attempt to rationalize the design of better tools, we have systematically studied the structural determinants of the affinity and efficacy of representative ligands of the V1a, V2, and OT receptor subtypes. Despite apparently obvious similarity between the ligand structures on one hand, and between the receptor subtypes on the other hand, the binding affinity and the functional activity profiles of truncated and hybrid ligands highlight the subtlety of ligand-receptor interactions for obtaining nonpeptide OT receptor agonists.
- Frantz, Marie-Céline,Rodrigo, Jordi,Boudier, Laure,Durroux, Thierry,Mouillac, Bernard,Hibert, Marcel
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experimental part
p. 1546 - 1562
(2010/08/05)
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- NOVEL OXADIAZOLE COMPOUNDS
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Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation o
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Page/Page column 97
(2008/12/06)
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- Vasopressin agonist formulation and process
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This invention provides novel formulations for vasopressin agonist compounds, or a pharmaceutically acceptable salt thereof, having the general structure: and processes for making them, the formulations comprising from about 1% to about 20% of active ingredient, from about 1% to about 18% of a surfactant component, from about 50% to about 80% of a component of one or more polyethylene glycols, from about 1% to about 20% of a component of one or more sucrose fatty acid esters and/or polyvinylpyrrolidone and, optionally, one or more preservatives or antioxidants.
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Page/Page column 58
(2010/02/09)
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