Abstract: A process for preparing 3-[(S)-7-bromo-2-((2-oxo propyl)amino)-5-pyridin-2-yl-3H-1,4,-benzodiazepin-3-yl]propionic acid methyl ester (compound (FK)), at a high conversion rate with good reproducibility by oxidizing 3-[(S)-7-bromo-2-(2-hydroxypropylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3yl]propionic acid methyl ester (compound (EM)), in the presence of an oxidation catalyst is provided by defining the ammonium ion content of the oxidation reaction mixture.
Abstract: The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 20 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.
Type:
Application
Filed:
October 24, 2017
Publication date:
February 15, 2018
Applicant:
Paion UK Limited
Inventors:
Karin WILHELM-OGUNBIYI, Keith BORKETT, Gary Stuart TILBROOK, Hugh WILTSHIRE
Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
Type:
Application
Filed:
September 13, 2017
Publication date:
January 4, 2018
Applicant:
Paion UK Limited
Inventors:
Gary Stuart TILBROOK, Louisa Jane Quegan
Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
Type:
Grant
Filed:
July 10, 2007
Date of Patent:
November 24, 2015
Assignee:
PAION UK Limited
Inventors:
Gary Stuart Tilbrook, Louisa Jane Cubitt
Abstract: The invention relates to esylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
Type:
Grant
Filed:
July 10, 2007
Date of Patent:
February 4, 2014
Assignee:
PAION UK Limited
Inventors:
Gary Stuart Tilbrook, Louisa Jane Cubitt
Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.
Type:
Application
Filed:
September 15, 2010
Publication date:
December 27, 2012
Applicant:
PAION UK Limited
Inventors:
Gary Stuart Tilbrook, Andreas Schumacher, René Emmengger
Abstract: Administration scheme of an analgesically active polar metabolite of an opioid or the salt thereof for the manufacture of a medicament for the treatment of pain after medical operation, whereas the medicament is administered at least once before the end of the medical operation.
Abstract: The invention relates to besylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
Type:
Application
Filed:
July 10, 2007
Publication date:
April 1, 2010
Applicant:
PAION UK Limited
Inventors:
Gary Stuart Tilbrook, Louisa Jane Cubitt