1152550-37-2Relevant academic research and scientific papers
Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition
Ellard, John M.,Madin, Andrew,Philps, Oliver,Hopkin, Mark,Henderson, Scott,Birch, Louise,O'Connor, Desmond,Arai, Tohru,Takase, Kazuma,Morgan, Louise,Reynolds, David,Talma, Sonia,Howley, Eimear,Powney, Ben,Payne, Andrew H.,Hall, Adrian,Gartlon, Jane E.,Dawson, Lee A.,Castro, Luis,Atkinson, Peter J.
, p. 5792 - 5796 (2015)
Herein we describe a series of tetrahydrobenzotriazoles as novel, potent metabotropic glutamate receptor subtype 5 (mGlu5) positive allosteric modulators (PAMs). Exploration of the SAR surrounding the tetrahydrobenzotriazole core ultimately led to the ide
Enantioselective synthesis of a highly substituted tetrahydrofluorene derivative as a potent and selective estrogen receptor beta agonist
Maddess, Matthew L.,Scott, Jeremy P.,Alorati, Anthony,Baxter, Carl,Bremeyer, Nadine,Brewer, Sarah,Campos, Kevin,Cleator, Ed,Dieguez-Vazquez, Alejandro,Gibb, Andrew,Gibson, Andrew,Howard, Melissa,Keen, Stephen,Klapars, Artis,Lee, Jaemoon,Li, Jing,Lynch, Joseph,Mullens, Peter,Wallace, Debra,Wilson, Robert
, p. 528 - 538 (2014/05/06)
The development and execution of a practical asymmetric synthesis of the estrogen receptor beta selective agonist (8R,10aS)-6-(trifluoromethyl)-8,9,10, 11-tetrahydro-8,10a-methanocyclohepta[1,2]indeno[4,5-d][1,2,3]triazol-7(3H)-one is described. The optimized route features a key chiral auxiliary-mediated dialkylation approach to set the all-carbon quaternary center with exceptional stereocontrol. Overall, the chemistry has been used to prepare >30 kg of drug candidate in 21% overall yield through 13 longest linear steps and with >99% ee.
BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
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Page/Page column 44, (2012/05/19)
The present invention relates to compounds of formula IA and IB and pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds,
BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
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Page/Page column 57, (2011/06/25)
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salt thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, method
