Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, where R1, R4, R5, R6, R7, Linker, X, Y, A, G, D and E have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts and prodrugs thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
December 31, 2019
Assignee:
AstraZeneca AB
Inventors:
Bin Yang, Jason Grant Kettle, Thomas George Christopher Hayhow, Timothy Gordon Rasmusson, Johannes Wilhelmus Maria Nissink, Charlene Fallan, Gillian McGregor Lamont
Abstract: The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
Type:
Application
Filed:
June 19, 2019
Publication date:
December 26, 2019
Applicant:
AstraZeneca AB
Inventors:
Sam Butterworth, Maurice Raymond Verschoyle Finlay, Richard Andrew Ward, Heather Marie Redfearn, Vasantha Krishna KADAMBAR, Chandrasekhara Reddy CHINTAKUNTLA, Andiappan MURUGAN, Claudio Edmundo CHUAQUI
Abstract: The invention relates to an inhalation device for powdered drugs to be received by a patient by an inhalation-caused air stream, comprising at least one powder reservoir, metering means for repeatedly metering a powder dose from the reservoir, a transportation mechanism for moving said metering means from a filling position for receiving a powder dose into an emptying position for releasing said powder dose into a powder channel, at least one activating device for manual operation by the patient, said activating device being operatively connected to said transportation mechanism such that upon operation a single powder dose is being metered, said activating device comprising a dosage key (5) acting on said transportation mechanism when pressed by the patient. The inhalation device further comprises an advancing mechanism for advancing a counter means each time the inhalation device has been activated by the patient so that a powder dose has been released into the powder channel.
Type:
Grant
Filed:
January 17, 2013
Date of Patent:
December 24, 2019
Assignee:
ASTRAZENECA AB
Inventors:
Martin Herder, Gerhard Ludanek, Ingo Mett, Joachim Schmidt
Abstract: The present application relates to novel compounds of formula (I) to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.
Type:
Grant
Filed:
November 20, 2018
Date of Patent:
December 17, 2019
Assignee:
ASTRAZENECA AB
Inventors:
Johan Olof Broddefalk, Hans Fredrik Emtenâs, Kenneth Lars Granberg, Malin Anita Lemurell, Daniel Tor Pettersen, Alleyn Thomas Plowright, Lars Johan Andreas Ulander
Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.
Abstract: Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1-R8 have any of the meanings defined herein. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I) and methods of using the same.
Type:
Application
Filed:
January 16, 2018
Publication date:
December 5, 2019
Applicant:
AstraZeneca AB
Inventors:
Karl Magnus NILSSON, Annika Birgitta Margareta ASTRAND, Anna Ingrid Kristina BERGGREN, Johan R. JOHANSSON, Matti Juhani LEPISTO, Sameer Pralhad KAWATKAR, Qibin SU, Jason Grant KETTLE
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:
December 18, 2018
Publication date:
December 5, 2019
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 specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of compounds of Formula (I) and salts thereof to treat or prevent ATM mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising to substituted imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; and intermediates useful in such manufacture.
Type:
Grant
Filed:
November 27, 2017
Date of Patent:
October 29, 2019
Assignee:
AstraZeneca AB
Inventors:
Bernard Christophe Barlaam, Kurt Gordon Pike, Andrew John Eatherton, Thomas Anthony Hunt
Abstract: The invention relates to an inhalation device for powdered drugs to be received by a patient by an inhalation-caused air stream, comprising at least one powder reservoir, metering means for repeatedly metering a powder dose from the reservoir, a transportation mechanism for moving said metering means from a filling position for receiving a powder dose into an emptying position for releasing said powder dose into a powder channel, at least one activating device for manual operation by the patient, said activating device being operatively connected to said transportation mechanism such that upon operation a single powder dose is being metered, said activating device comprising a dosage key (5) acting on said transportation mechanism when pressed by the patient.
Type:
Grant
Filed:
January 17, 2013
Date of Patent:
October 8, 2019
Assignee:
ASTRAZENECA AB
Inventors:
Martin Herder, Gerhard Ludanek, Ingo Mett, Joachim Schmidt
Abstract: There are provided pharmaceutical compositions comprising a compound of Formula (I) as defined herein and an amount of an alkaline effervescent agent that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.
Abstract: The invention relates to an inhalation device for powdered drugs to be received by a patient by an inhalation-caused air stream, comprising at least one powder reservoir, metering means for repeatedly metering a powder dose from the reservoir, a transportation mechanism for moving said metering means from a filling position for receiving a powder dose into an emptying position for releasing said powder dose into a powder channel, at least one activating device for manual operation by the patient, said activating device being operatively connected to said transportation mechanism such that upon operation a single powder dose is being metered, said activating device comprising a dosage key (5) acting on said transportation mechanism when pressed by the patient. The inhalation device further comprises an advancing mechanism for advancing a counter means each time the inhalation device has been activated by the patient so that a powder dose has been released into the powder channel.
Type:
Grant
Filed:
January 17, 2013
Date of Patent:
September 17, 2019
Assignee:
ASTRAZENECA AB
Inventors:
Martin Herder, Gerhard Ludanek, Ingo Mett, Joachim Schmidt
Abstract: A crystalline form of (1R,2R)-2-[4-(3-Methyl-1H-pyrazol-5-yl)benzoyl]-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl)cyclohexanecarboxamide, pharmaceutical compositions containing it and its use in therapy.
Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.
Type:
Grant
Filed:
December 19, 2017
Date of Patent:
September 10, 2019
Assignees:
AstraZeneca AB, Cancer Research Technology Limited
Inventors:
Maurice Raymond Verschoyle Finlay, Frederick Woolf Goldberg, Attilla Kuan Tsuei Ting
Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.
Type:
Grant
Filed:
April 11, 2018
Date of Patent:
September 10, 2019
Assignee:
AstraZeneca AB
Inventors:
Robert Hugh Bradbury, Alfred Arthur Rabow, Michael James Waring, James Francis McCabe, Steven Christopher Glossop, Arshed Mahmood, Zoe Ann Cotter
Abstract: A crystalline form of 2,2-difluoro-N-[(1R,2S)-3-methyl-1-{[1-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1H-indazol-5-yl]oxy}-1-phenylbutan-2-yl]propanamide (form C), pharmaceutical compositions containing it and its use in therapy.
Abstract: The present disclosure relates to methods of treating, ameliorating or preventing a disorder comprising administering a therapeutically effective amount of a composition comprising a protein which inhibits the ligand of Uniprot #P05112 and/or the ligand of Uniprot #P35225 from binding to their respective receptors to a subject in need thereof. In some embodiments, the disorder is preferably associated with an increase of the Th2 immune response. In some embodiments, administration is preferably locally to the lung in order to treat, ameliorate or prevent allergic asthma, rhinitis, conjunctivitis, lung fibrosis, cystic fibrosis, chronic obstructive pulmonary disease, pulmonary alveolar proteinosis or adult respiratory distress syndrome.
Type:
Grant
Filed:
June 7, 2018
Date of Patent:
September 3, 2019
Assignees:
Pieris Pharmaceuticals GmbH, Astrazeneca AB
Inventors:
Andreas Hohlbaum, Laurent Audoly, Beverly Koller
Abstract: The invention relates to a formulation comprising formoterol and budesonide for use in the treatment of respiratory diseases. The composition further contains HFA 227, PVP and PEG, preferably PVP K25 and PEG 1000.
Abstract: The present invention provides a compound of a formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an ENaC mediated disease state (such as asthma, CF or COPD).
Type:
Grant
Filed:
December 13, 2017
Date of Patent:
July 2, 2019
Assignee:
AstraZeneca AB
Inventors:
Susanne Elisabeth Berglund, Stephen Connolly, Martin Hemmerling, Nafizal Hossain, Anna Kristoffersson, Johan Rune Michael Lundkvist, Grigorios Nikitidis, Lena Elisabeth Ripa, Igor Shamovsky
Abstract: Systems and methods are provided for over the counter statin delivery to a subject. Survey results from the subject are run against a first plurality of filters. When a filter in the first plurality of filters is fired, the subject is deemed not qualified. The survey results are also run against a second plurality of filters. When a respective filter in the second plurality is fired, the subject is provided with a corresponding warning. The method proceeds to a fulfillment process when no filter in the first plurality fires and the subject has acknowledged each warning associated with each fired filter in the second plurality. The fulfillment stores the composition order, communicates a drug facts label for the statin to the subject, and authorizes, upon subject confirmation that the label has been read, provision of the statin to the subject, the authorization including a destination associated with the subject.
Type:
Grant
Filed:
January 22, 2018
Date of Patent:
June 18, 2019
Assignee:
AstraZeneca UK Ltd.
Inventors:
James Blasetto, Judy Firor, David Guiga, William Mongan, Robert Prybolsky, Richard L. Skelly
Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
Type:
Grant
Filed:
November 29, 2016
Date of Patent:
June 18, 2019
Assignees:
AstraZeneca AB, Cancer Research Technology Limited
Inventors:
Johannes Wilhelmus Maria Nissink, Maurice Raymond Verschoyle Finlay, Mark David Charles