On August 25, 2011, Simoneau, Bruno; Deroy, Patrick; Fader, Lee; Faucher, Anne-Marie; Gagnon, Alexandre; Grand-Maitre, Chantal; Kawai, Steven; Landry, Serge; Mercier, Jean-Francois; Rancourt, Jean published a patent.Electric Literature of 38939-88-7 The title of the patent was 1-Phenyl-1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione derivatives as HIV replication inhibitors and their preparation and use for the treatment of HIV infection. And the patent contained the following:
The invention relates to benzodiazepinedione derivatives of formula I, which are HIV replication inhibitors and which are useful in the treatment of HIV infection. Compounds of formula I wherein X is C=O; Y is substituted CHPh, substituted benzo-fused spirocycle, substituted NPh, etc.; XY taken together to form (un)substituted 5-membered heteroaryl; each R1 is independently C1-6 alkyl, C1-6 haloalkyl, halo and C3-7 cycloalkyl; R2 is H, C1-6 alkyl, C1-6 alkyl-C3-7 cycloalkyl and C3-7 cycloalkyl; R3 is (un)substituted Ph and thiophene; m is 1 to 3; are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their HIV replication inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values in the range 0.38 – 047 μM and an EC50 value of 2.6 μM. The experimental process involved the reaction of 2-Chloro-4-methyl-1-nitrobenzene(cas: 38939-88-7).Electric Literature of 38939-88-7
The Article related to benzodiazepinedione preparation replication inhibitor treatment hiv infection, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Electric Literature of 38939-88-7
Referemce:
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