344462-84-6Relevant articles and documents
N-PHENYLALKOXY-7-OXO-6-SULFOOXY-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS
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Page/Page column 17, (2018/01/20)
Compounds of Formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, their preparation, pharmaceutical compositions comprising such compounds and their use in treating and/or preventing bacterial infections are disclosed.
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome
Zhou, Yu,Ma, Jing,Lin, Xingyu,Huang, Xi-Ping,Wu, Kaichun,Huang, Niu
, p. 707 - 720 (2016/02/09)
Here we employed structure-based ligand discovery techniques to explore a recently determined crystal structure of the 5-hydroxytryptamine 2B (5-HT2B) receptor. Ten compounds containing a novel chemical scaffold were identified; among them, seven molecules were active in cellular function assays with the most potent one exhibiting an IC50 value of 27.3 nM. We then systematically probed the binding characteristics of this scaffold by designing, synthesizing, and testing a series of structural modifications. The structure-activity relationship studies strongly support our predicted binding model. The binding profiling across a panel of 11 5-HT receptors indicated that these compounds are highly selective for the 5-HT2B receptor. Oral administration of compound 15 (30 mg/kg) produced significant attenuation of visceral hypersensitivity in a rat model of irritable bowel syndrome (IBS). We expect this novel scaffold will serve as the foundation for the development of 5-HT2B antagonists for the treatment of IBS.
Amination of aryl iodides using a fluorous-tagged ammonia equivalent
Nielsen, Simon Dalsgaard,Smith, Garrick,Begtrup, Mikael,Kristensen, Jesper L.
experimental part, p. 3704 - 3710 (2010/09/05)
A fluorous-tagged ammonia equivalent for the Cu-catalyzed amination of aryl iodides is described in which N-Boc-protected anilines are produced in high overall yield and purity. All purification steps are performed using Fluorous SolidPhase Extraction (F-SPE) greatly simplifying and speeding up the isolation of the desired products.
Macrocyclic Compounds Useful as Bace Inhibitors
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Page/Page column 27, (2008/12/05)
The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
NEW COMPOUNDS
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Page 137-138, (2010/02/06)
The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
Seleno compounds containing nitrone moiety, their preparation and their therapeutic uses
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, (2008/06/13)
The present invention provides novel seleno compounds containing nitrone moiety, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactiv
Cyclopentyl sulfonamide derivatives
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Page/Page column 36, (2010/01/31)
The present invention provides certain cyclopentyl sulfonamide derivatives of formula (I): useful for potentiating glutamate receptor function in a mammal. It also relates to novel cyclopentyl sulfonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
