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 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.
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.
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