82104-06-1Relevant articles and documents
INHIBITORS OF FATTY ACID AMIDE HYDROLASE
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Paragraph 1253; 1256, (2016/01/15)
The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof.
Bioactive cyclometalated phthalimides: Design, synthesis and kinase inhibition
Blanck, Sebastian,Geisselbrecht, Yann,Kr?ling, Katja,Middel, Stephen,Mietke, Thomas,Harms, Klaus,Essen, Lars-Oliver,Meggers, Eric
supporting information; experimental part, p. 9337 - 9348 (2012/09/08)
The regioselective cyclometalation of 4-(pyridin-2-yl)phthalimide was exploited for the economical design of organometallic protein kinase inhibitors. 4-(Pyridin-2-yl)phthalimide can be prepared from inexpensive 4-bromophthalimide in just three steps including one Pd-catalyzed Stille cross-coupling. The versatility of this new ligand was demonstrated with the synthesis of ruthenium(ii) half-sandwich as well as octahedral ruthenium(ii) and iridium(iii) complexes. The regioselectivity of the C-H activation in the course of the cyclometalation can be influenced by the reaction conditions and the steric demand of the introduced metal complex fragment. The biological activity of this new class of metalated phthalimides was evaluated by profiling two representative members against a large panel of human protein kinases. A cocrystal structure of one metallo-phthalimide with the protein kinase Pim1 confirmed an ATP-competitive binding with the intended hydrogen bonding between the phthalimide moiety and the hinge region of the ATP-binding site.
Application of a spin-labeled spin-trap to the detection of Nitric Oxide (NO)
Marx, Lucien,Rassat, Andre
, p. 4494 - 4496 (2007/10/03)
Sensitive detection of reaction products is a potential use of diradicals as spin-labeled spin-traps. When diradical 1 reacts with NO, the EPR spectrum not only changes from a single broad line to a three-line spectrum, but the apparent intensity of the monoradical products, such as 2, is more than 500 times greater than that of the original diradical.