693774-26-4Relevant academic research and scientific papers
SMALL MOLECULE MODULATORS OF IL-17
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Page/Page column 83, (2020/09/30)
The present invention relates to a compound according to formula I and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to, to said compounds for use in therapy, to pharmaceutical compositions comprising said
AMINO-ACID ANILIDES AS SMALL MOLECULE MODULATORS OF IL-17
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Page/Page column 90-91, (2020/07/14)
The present invention relates to a compound according to formula I (I) and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
Silylium-Ion-Promoted (5+1) Cycloaddition of Aryl-Substituted Vinylcyclopropanes and Hydrosilanes Involving Aryl Migration
Bonetti, Vittorio,He, Tao,Klare, Hendrik F. T.,Oestreich, Martin,Wang, Guoqiang
supporting information, p. 12186 - 12191 (2020/05/22)
A transition-metal-free (5+1) cycloaddition of aryl-substituted vinylcyclopropanes (VCPs) and hydrosilanes to afford silacyclohexanes is reported. Catalytic amounts of the trityl cation initiate the reaction by hydride abstraction from the hydrosilane, and further progress of the reaction is maintained by self-regeneration of the silylium ions. The new reaction involves a [1,2] migration of an aryl group, eventually furnishing 4- rather than 3-aryl-substituted silacyclohexane derivatives as major products. Various control experiments and quantum-chemical calculations support a mechanistic picture where a silylium ion intramolecularly stabilized by a cyclopropane ring can either undergo a kinetically favored concerted [1,2] aryl migration/ring expansion or engage in a cyclopropane-to-cyclopropane rearrangement.
Palladium-Catalyzed Carbonylative Cross-Coupling Reaction between Aryl(Heteroaryl) Iodides and Tricyclopropylbismuth: Expedient Access to Aryl Cyclopropylketones
Benoit, Emeline,Dansereau, Julien,Gagnon, Alexandre
supporting information, p. 2833 - 2838 (2017/10/06)
The carbonylative cross-coupling reaction between aryl and heteroaryl iodides and tricyclopropylbismuth is reported. The reaction is catalyzed by (SIPr)Pd(allyl)Cl, a NHC-palladium(II) catalyst, operates under 1 atm of carbon monoxide and tolerates a wide range of functional groups. The use of lithium chloride was found to provide higher yields of the desired aryl cyclopropylketones. The conditions were also applied to the carbonylative cross-coupling of an iodoalkene to afford the corresponding alkenyl cyclopropylketone.
Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor
Cumming, Jared N.,Smith, Elizabeth M.,Wang, Lingyan,Misiaszek, Jeffrey,Durkin, James,Pan, Jianping,Iserloh, Ulrich,Wu, Yusheng,Zhu, Zhaoning,Strickland, Corey,Voigt, Johannes,Chen, Xia,Kennedy, Matthew E.,Kuvelkar, Reshma,Hyde, Lynn A.,Cox, Kathleen,Favreau, Leonard,Czarniecki, Michael F.,Greenlee, William J.,McKittrick, Brian A.,Parker, Eric M.,Stamford, Andrew W.
scheme or table, p. 2444 - 2449 (2012/05/19)
From an initial lead 1, a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers CNS-derived Aβ following oral administration to rats. Herein we report SAR development in the S3 and F′ subsites of BACE1 for this series, the synthetic approaches employed in this effort, and in vivo data for the optimized compound.
