Patents by Inventor Gary Stuart Tilbrook

Gary Stuart Tilbrook has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Dosing regimen for sedation with CNS 7056 (Remimazolam)
    Patent number: 9737547
    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: Grant
    Filed: January 6, 2017
    Date of Patent: August 22, 2017
    Assignee: PAION UK LIMITED
    Inventors: Karin Wilhelm-Ogunbiyi, Keith Borkett, Gary Stuart Tilbrook, Hugh Wiltshire
  • DOSING REGIMEN FOR SEDATION WITH CNS 7056 (REMIMAZOLAM)
    Publication number: 20170112852
    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: January 6, 2017
    Publication date: April 27, 2017
    Inventors: Karin WILHELM-OGUNBIYI, Keith BORKETT, Gary Stuart TILBROOK, Hugh WILTSHIRE
  • 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 THE BENZENE SULFONATE SALT THEREOF, AND COMPOUNDS USEFUL IN THAT PROCESS
    Publication number: 20170044135
    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 materials or as intermediates for performing that process.
    Type: Application
    Filed: October 27, 2016
    Publication date: February 16, 2017
    Inventors: Gary Stuart TILBROOK, Andreas SCHUMACHER, Rene EMMENEGGER
  • Dosing regimen for sedation with CNS 7056 (Remimazolam)
    Patent number: 9561236
    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: Grant
    Filed: November 7, 2011
    Date of Patent: February 7, 2017
    Assignee: PAION UK LTD.
    Inventors: Karin Wilhelm-Ogunbiyi, Keith Borkett, Gary Stuart Tilbrook, Hugh Wiltshire
  • Process for preparing 3-[(45)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-A][1,4]benzodiazepine-4-yl]propionic acid methyl ester or the benzene sulfonate salt thereof, and compounds useful in that process
    Patent number: 9512078
    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: Grant
    Filed: September 1, 2015
    Date of Patent: December 6, 2016
    Assignee: PAION UK LIMITED
    Inventors: Gary Stuart Tilbrook, Andreas Schumacher, Rene Emmenegger
  • SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS
    Publication number: 20160176881
    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: November 23, 2015
    Publication date: June 23, 2016
    Inventors: Gary Stuart TILBROOK, Louisa Jane QUEGAN
  • 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 THE BENZENE SULFONATE SALT THEREOF, AND COMPOUNDS USEFUL IN THAT PROCESS
    Publication number: 20150368199
    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 1, 2015
    Publication date: December 24, 2015
    Applicant: PAION UK LIMITED
    Inventors: Gary Stuart Tilbrook, Andreas Schumacher, Rene Emmenegger
  • Short-acting benzodiazepine salts and their polymorphic forms
    Patent number: 9193730
    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
  • 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 the benzene sulfonate salt thereof, and compounds useful in that process
    Patent number: 9156842
    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: Grant
    Filed: September 15, 2010
    Date of Patent: October 13, 2015
    Assignee: PAION UK LIMITED
    Inventors: Gary Stuart Tilbrook, Andreas Schumacher, René Emmenegger
  • DOSING REGIMEN FOR SEDATION WITH CNS 7056 (REMIMAZOLAM)
    Publication number: 20140080815
    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 10 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.
    Type: Application
    Filed: November 7, 2011
    Publication date: March 20, 2014
    Applicant: PAION UK LTD.
    Inventors: Karin Wilhelm-Ogunbiyi, Keith Borkett, Gary Stuart Tilbrook, Hugh Wiltshire
  • Short-acting benzodiazepine salts and their polymorphic forms
    Patent number: 8642588
    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
  • 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 THE BENZENE SULFONATE SALT THEREOF, AND COMPOUNDS USEFUL IN THAT PROCESS
    Publication number: 20120330007
    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
  • SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS
    Publication number: 20100081647
    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
  • SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS
    Publication number: 20100075955
    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: Application
    Filed: July 10, 2007
    Publication date: March 25, 2010
    Inventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
  • Pyrano [3,2-d]-1,3-dioxin-8 ones
    Patent number: 6506911
    Abstract: A novel 3-hydroxypyridin-4-one compound of formula I is provided wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, R3 is selected from hydrogen and C1-6 alkyl; and R4 is selected from hydrogen, C1-6 alkyl and a group as described for R2; characterised in that R2 is selected from groups (i) —CONH—R5 (ii) —CH2NHCO—R5 (iii) —SO2NH—R5 (iv) —CH2NHSO2—R5 (v) —CR6R6OR7 (viii) —CONHCOR5  wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-3 alkyl, aryl and C7-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl, and R7 is selected from hydrogen, C1-13 alkyl, aryl and C7
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: January 14, 2003
    Assignee: BTG International Limited
    Inventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
  • Orally active iron (III) chelators
    Patent number: 6448273
    Abstract: A compound of formula I wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, and R3 is selected from hydrogen and C1-6 alkyl; characterized in that R2 is selected from groups (i) —CONH—R5 (ii)—CR6R6OR7 (iii) —CONHCOR5 and (iv) —CON(CnH2n+1)2 R4 is selected from hydrogen, C1-6 alkyl and a group as described for R2; R5 is selected from hydrogen and optionally hydroxy, alkoxy, aryloxy or aralkoxy substituted C1-13 alkyl, aryl and C7-13 alkyl R6 is independently selected from hydrogen and C1-13 alkyl, R7 is selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl or a pharmaceutically acceptable salt of any such compound and CnH2n+1 is C1-6alkyl with the proviso that the compound
    Type: Grant
    Filed: November 30, 1999
    Date of Patent: September 10, 2002
    Assignee: BTG International Limited
    Inventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
  • Novel orally active iron (III) chelators
    Publication number: 20020068758
    Abstract: A novel 3-hydroxypyridinone compound of formula I is provided 1
    Type: Application
    Filed: September 4, 2001
    Publication date: June 6, 2002
    Applicant: BTG International Limited.
    Inventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
  • Orally active iron (III) chelators
    Patent number: 6335353
    Abstract: A novel 3-hydroxypyridin-4-one compound of formula I is provided wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, R3 is selected from hydrogen and C1-6alkyl; and R4 is selected from hydrogen, C1-6alkyl and a group as described for R2; characterised in that R2 is selected from groups —CONH—R5  (i) —CH2NHCO—R5  (ii) —SO2NH—R5  (iii) —CH2NHSO2—R5  (iv) —CR6R6OR7  (v) —CONHCOR5  (viii)  wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-13 alkyl, aryl and C71-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl,
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: January 1, 2002
    Assignee: BTG International Limited
    Inventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu