1374263-53-2Relevant academic research and scientific papers
Substituted Benzo-Imidazo-Pyrido-Diazepine Compounds
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Page/Page column 132-133, (2012/05/07)
The present invention relates to substituted benzo-imidazo-pyrido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-imidazo-pyrido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: Part 2
Brumfield, Stephanie,Matasi, Julius J.,Tulshian, Deen,Czarniecki, Michael,Greenlee, William,Garlisi, Charles,Qiu, Hongchen,Devito, Kristine,Chen, Shu-Cheng,Sun, Yongliang,Bertorelli, Rosalia,Ansell, Justin,Geiss, William,Le, Van-Duc,Martin, Gregory S.,Vellekoop, Samuel A.,Haber, James,Allard, Melissa L.
, p. 7287 - 7290 (2012/02/04)
Novel P2X7 antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X7 receptor in human and rodent as well as efficacious in rodent pain models. Compound 15a was identified to have oral potency in several pain models in rodent similar to naproxen, gabapentin and pregabalin. Structure-activity relationship (SAR) development and results of pain models are presented.
