873693-14-2Relevant articles and documents
Chemical development of NBI-75043. Use of a flow reactor to circumvent a batch-limited metal#halogen exchange reaction
Gross, Timothy D.,Chou, Shine,Bonneville, Daniel,Gross, Raymond S.,Wang, Peng,Campopiano, Onorato,Ouellette, Michael A.,Zook, Scott E.,Reddy, Jayachandra P.,Moree, Wilna J.,Jovic, Florence,Chopade, Shubham
, p. 929 - 939 (2008)
The discovery route and subsequent scale-up routes for NBI-75043 are presented. When traditional batch chemistry was found to limit the scale of a key reaction, a flow reactor was designed and optimized to provide an alternate method of production.
Novel benzothiophene H1-antihistamines for the treatment of insomnia
Moree, Wilna J.,Jovic, Florence,Coon, Timothy,Yu, Jinghua,Li, Bin-Feng,Tucci, Fabio C.,Marinkovic, Dragan,Gross, Raymond S.,Malany, Siobhan,Bradbury, Margaret J.,Hernandez, Lisa M.,O'Brien, Zhihong,Wen, Jianyun,Wang, Hua,Hoare, Samuel R.J.,Petroski, Robert E.,Sacaan, Aida,Madan, Ajay,Crowe, Paul D.,Beaton, Graham
scheme or table, p. 2316 - 2320 (2010/09/05)
SAR of lead benzothiophene H1-antihistamine 2 was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H1-antihistamines with a range of projected half-li
Sleep inducing compounds and methods relating thereto
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Page/Page column 21, (2010/02/15)
Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
