Abstract: The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.
Type:
Application
Filed:
September 18, 2017
Publication date:
May 17, 2018
Applicant:
AstraZeneca UK Limited
Inventors:
Michael Karl Bechtold, Julie Kay Cahill, Katja Maren Fastnacht, Kieran James Lennon, Bernd Harald Liepold, Claudia Bettina Packhaeuser, Benedikt Steitz
Abstract: The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.
Type:
Application
Filed:
March 3, 2017
Publication date:
June 22, 2017
Applicant:
AstraZeneca UK Limited
Inventors:
Michael Karl Bechtold, Julie Kay Cahill, Katja Maren Fastnacht, Kieran James Lennon, Bernd Harald Liepold, Claudia Bettina Packhaeuser, Benedikt Steitz
Abstract: The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.
Type:
Grant
Filed:
May 7, 2015
Date of Patent:
April 11, 2017
Assignees:
AstraZeneca AB, AstraZeneca UK Limited
Inventors:
Admassu Abebe, Kyle Martin, Jatin M. Patel, Divyakant Desai, Peter Timmins
Abstract: A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7) wherein A is an acetal or ketal protecting group and R is alkyl, via isolated crystalline compounds of the formula (8) or of formula (10) is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.
Type:
Grant
Filed:
July 19, 2011
Date of Patent:
June 21, 2016
Assignees:
AstraZeneca UK Limited, Shionogi & Company Limited
Inventors:
Tetsuo Okada, John Horbury, David Dermot Patrick Laffan
Abstract: The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.
Type:
Application
Filed:
April 16, 2015
Publication date:
January 14, 2016
Applicant:
ASTRAZENECA UK LIMITED
Inventors:
Michael Karl Bechtold, Julie Kay Cahill, Katja Maren Fastnacht, Kieran James Lennon, Bernd Harald Liepold, Claudia Bettina Packhaeuser, Benedikt Steitz
Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
Type:
Application
Filed:
June 20, 2014
Publication date:
June 4, 2015
Applicant:
AstraZeneca UK Limited
Inventors:
David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
Type:
Application
Filed:
October 31, 2013
Publication date:
October 2, 2014
Applicant:
AstraZeneca UK Limited
Inventors:
David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
Abstract: The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is acetyl salicylic acid, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a such a co-crystal.
Type:
Application
Filed:
May 31, 2012
Publication date:
May 29, 2014
Applicant:
AstraZeneca UK Limited
Inventors:
Stephen David Cosgrove, David Thomas Jonaitis, Jonathan Charles Derrick Sutch
Abstract: The present invention relates to solid, semisolid, or liquid formulations comprising water soluble antioxidants that prevent or reduce formic acid and/or formyl species generation in the dosage form during the manufacturing process and/or during shelf-life storage. The formulations of the present invention prevent or reduce formation of N-formyl impurities (and gelatin crosslinking) during the manufacturing process and/or during shelf-life storage.
Type:
Application
Filed:
January 31, 2012
Publication date:
March 20, 2014
Applicants:
AstraZeneca UK Limited, Bristol-Myers Squibb Company
Inventors:
Ajit Narang, Venkatramana M. Rao, Divyakant S. Desai
Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
Abstract: The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.
Type:
Application
Filed:
August 13, 2013
Publication date:
December 12, 2013
Applicants:
AstraZeneca UK Limited, Bristol-Myers Squibb Company
Inventors:
Admassu Abebe, Kyle Martin, Jatin M. Patel, Divyakant Desai, Peter Timmins
Abstract: The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.
Type:
Grant
Filed:
November 12, 2010
Date of Patent:
September 17, 2013
Assignees:
Bristol-Myers Squibb Company, AstraZeneca UK Limited
Inventors:
Admassu Abebe, Kyle Martin, Jatin M. Patel, Divyakant Desai, Peter Timmins
Abstract: Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.
Abstract: Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.
Type:
Grant
Filed:
March 1, 2011
Date of Patent:
May 7, 2013
Assignee:
AstraZeneca UK Limited
Inventors:
Rebecca Jane Booth, Peter Anthony Cittern, Jeffrey Norman Crabb, John Horbury, David Wyn Calvert Jones
Abstract: The present invention provides an immediate release pharmaceutical formulation which includes a tablet or capsule formulation comprising metformin and the sodium dependent glucose transporter (SGLT2) inhibitor dapagliflozin or its propylene glycol hydrate. The present invention also provides methods of preparing the formulations and methods of treating diseases or disorders associated with SGLT2 activity employing these formulations.
Type:
Application
Filed:
November 12, 2010
Publication date:
February 7, 2013
Applicants:
ASTRAZENECA UK LIMITED, BRISTOL-MYERS SQUIBB COMPANY
Inventors:
Agneta Hallgren, Ralf Magnus Werner Swenson
Abstract: Triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation. The compounds of the invention have the formula (I) as follows: wherein R, X and R1 through R3 are as defined in the specification.
Type:
Grant
Filed:
December 21, 2015
Date of Patent:
January 17, 2017
Assignee:
AstraZeneca UK Limited
Inventors:
David Hardem, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile