934584-88-0Relevant articles and documents
Synthesis of Vixotrigine, a Use-Dependent Sodium Channel Blocker. Part 1: Development of Bulk Supply Routes to Enable Proof of Concept
Giblin, Gerard,Heseltine, Adrian,Kiesman, William,Macpherson, David,Ramsden, James,Vadali, Ravi,Williams, Michael,Witty, David
, p. 2802 - 2813 (2020/12/22)
Two syntheses of vixotrigine are reported. Route 1, adapted from the medicinal chemistry route, enabled rapid delivery of drug substance for clinical development. Route 2, which was developed to address many of the limitations of Route 1, was used to manu
Synthesis of Vixotrigine, a Voltage- And Use-Dependent Sodium Channel Blocker. Part 2: Development of a Late-Stage Process
Cerea, Paolangelo,Chen, Robbie,Couming, Vincent,Grohmann, Markus,Gu, Chaozhan,Guzowski, John,Haefner, Benjamin,Irdam, Erwin,Kiesman, William F.,Kuhn, Roman,Kwok, Daw-Iong Albert,Liang, Wenli,Lotz, Joerg,Mack, Tamera,Matzinger, Hanspeter,Nonnenmacher, Michael,O'Brien, Erin M.,Opalka, Suzanne M.,Osei-Yeboah, Frederick,Patience, Daniel,Sahli, Stefan,St?ckli, Markus,Stucki, Thiemo,Thut, Michael,Walker, Donald G.,Zhang, Xin
, p. 2814 - 2829 (2020/12/22)
As vixotrigine (1) entered a later clinical phase for trigeminal neuralgia (Zakrzewska, J. M.; et al. Lancet Neurol. 2017, 16, 291-300), the development of a sustainable late-stage process was required to meet the supply needs for formulation optimization
PROCESS FOR PREPARING ALPHA-CARBOXAMIDE PYROLIDINE DERIVATIVES
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Page/Page column 61-62, (2019/04/27)
The invention relates to a novel process for preparing a-carboxamide pyrrolidine derivatives, in particular (2S, 5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide, and to novel intermediates for use in said process along with processes for pr
PROCESS FOR PREPARING ALPHA-CARBOXAMIDE PYRROLIDINE DERIVATIVES
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, (2016/07/27)
The invention relates to a novel process for preparing a-carboxamide pyrrolidine derivatives, in particular (2S, 5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide, and to novel intermediates for use in said process along with processes for pr
PHARMACEUTICAL COMPOSITIONS COMPRISING 2-METHOXY-5- (5-TRIFLUOROMETHYL-TETRAZOL-I-YL-BENZYL) - (2S-PHENYL-PIPERIDIN-3S-YL-)
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Page/Page column 38, (2008/12/07)
The present invention relates to pharmaceutical compositions comprising the NK1 receptor antagonist [2-Methoxy-5-(5-trifuoromethyl-tetrazol-1-yl)-benzyl]-(2S-phenyl- piperidin-3S-yl)-amine, or a pharmaceutically acceptable salt or solvate thereof, and a sodium channel blocker, as a combined preparation for simultaneous or sequential administration and to the use of such compositions in the treatment of certain disorders, including epilepsy, mood disorders and pain.
QUATERNARY ALPHA-AMINOCARBOXAMIDE DERIVATIVE AS MODULATORS OF VOLTAGE-GATED SODIUM CHANNELS
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Page/Page column 80-81, (2010/11/27)
The invention relates to quaternary E-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.