479234-83-8Relevant articles and documents
SALTS AND CRYSTALS
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Page/Page column 28-30, (2022/03/22)
This invention relates to solid forms of 1-methyl-1,4,5,10-tetrahydropyrazolo[3,4-b][1,5]benzodiazepine freebase possessing desirable pharmacokinetic properties, such as low hygroscopicity and improved thermal stability. These solid forms include a crystalline form of 1-methyl-1,4,5,10-tetrahydropyrazolo[3,4-b][1,5]benzodiazepine 5 freebase and phosphate and L-tartrate salts of 1-methyl-1,4,5,10-tetrahydropyrazolo[3,4-b][1,5]benzodiazepine freebase. Pharmaceutical compositions, medicaments and kits comprising these solid forms are also described. Also provided are methods of using these forms to treat various diseases, conditions and disorders.
Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors
Jorgensen, William T.,Gulliver, Damien W.,Katte, Timothy A.,Werry, Eryn L.,Reekie, Tristan A.,Connor, Mark,Kassiou, Michael
, p. 1644 - 1656 (2017/11/13)
WAY-267,464 (1) and twelve conformationally rigid analogues (3a-f–4a-f) were synthesised, characterised and evaluated in cellular assays with the aim of systematically exploring interactions with the oxytocin receptor (OTR). Each analogue was evaluated in
The Formation of Seven-Membered Heterocycles under Mild Pictet-Spengler Conditions: A Route to Pyrazolo[3,4]benzodiazepines
Katte, Timothy A.,Reekie, Tristan A.,Jorgensen, William T.,Kassiou, Michael
, p. 4883 - 4889 (2016/07/06)
Reported is a method for the synthesis of seven-membered heterocycles via a Pictet-Spengler condensation reaction under very mild conditions. High substrate scope allows for use of aldehydes using catalytic amounts of acetic acid yielding 39-90% and keton