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 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:
Application
Filed:
September 16, 2016
Publication date:
March 23, 2017
Applicant:
AstraZeneca AB
Inventors:
Bernard Christophe Barlaam, Andrew John Eatherton, Thomas Anthony Hunt, Kurt Gordon Pike
Abstract: Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including oral administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including obesity and overweight, diabetes, dyslipidemia, hyperlipidemia, Alzheimer's disease, fatty liver disease, short bowel syndrome, Parkinson's disease, cardiovascular disease, and other and disorders of the central nervous system.
Inventors:
Mary Erickson, David C. Litzinger, Soumitra S. Ghosh, Zijian Guo, Swetha Neravetla, Chengzao Sun, Manoj P. Samant, Odile E. Levy, Abhinandini Sharma, Lala Mamedova, Christopher J. Soares
Abstract: The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
Type:
Application
Filed:
November 15, 2016
Publication date:
March 2, 2017
Applicant:
AstraZeneca AB
Inventors:
Paul David Johnson, Andrew Leach, Richard William, Arthur Luke, Zbigniew Stanley Matusiak, Jeffrey James Morris
Abstract: There are disclosed novel compounds of formula (I) wherein R1, R12, L, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardiovascular disorders and respiratory disorders.
Type:
Grant
Filed:
September 15, 2014
Date of Patent:
February 28, 2017
Assignee:
AstraZeneca AB
Inventors:
Anders Bogevig, Yvonne Lo-Alfredsson, Donald Pivonka, Anna-Karin Tiden
Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
Type:
Grant
Filed:
March 18, 2015
Date of Patent:
February 14, 2017
Assignee:
AstraZeneca AB
Inventors:
Nicola Murdoch Heron, Frederic Henri Jung, Andrew Mortlock, Georges Pasquet
Abstract: The present invention discloses certain new solid state forms of (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3 -d]pyrimidin-4-yl)piperidine-4-carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy.
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: 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 10 states associated with angiogenesis and/or increased vascular permeability.
Abstract: Provided are a series of novel pyridine or pyrimidine derivatives which inhibit CDK9 and may be useful for the treatment of hyperproliferative diseases. In particular the compounds are of use in the treatment of proliferative disease such as cancer including hematological malignancies such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, diffuse large B cell lymphoma, Burkitt's lymphoma, follicular lymphoma and solid tumors such as breast cancer, lung cancer, neuroblastoma and colon cancer.
Type:
Application
Filed:
June 27, 2016
Publication date:
December 29, 2016
Applicant:
AstraZeneca AB
Inventors:
Bernard Barlaam, Christopher De Savi, Janet Hawkins, Alexander Hird, Michelle Lamb, Kurt Pike, Melissa Vasbinder
Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; 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 ATM kinase mediated disease, including cancer, using such compounds and salts.
Type:
Application
Filed:
July 22, 2016
Publication date:
December 22, 2016
Applicant:
AstraZeneca AB
Inventors:
Bernard Christophe BARLAAM, Kurt Gordon PIKE
Abstract: The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
Type:
Grant
Filed:
January 21, 2015
Date of Patent:
December 20, 2016
Assignee:
AstraZeneca AB
Inventors:
Hans Roland Lonn, Stephen Connolly, Steven Swallow, Staffan PO Karlsson, Carl-Johan Aurell, John Fritiof Pontén, Kevin James Doyle, Amanda Jane Van de Poël, Graham Peter Jones, David Wyn Watson, Jaqueline Anne MacRitchie, Nicholas John Palmer
Abstract: A compound of formula Ia: The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
Inventors:
Markus Berger, Hartmut Rehwinkel, Jan Dahmen, Anders Eriksson, Thomas Hansson, Nafizal Hossain, Per Tomas Klingstedt, Matti Lepistö, Stinabritt Nilsson, Martin Hemmerling, Karl Edman
Abstract: The disclosure provides one-component, injectable, sustained release formulations which comprise microspheres containing active pharmaceutical ingredients (e.g., exenatide), wherein the microspheres are suspended in a non-aqueous carrier. The non-aqueous carrier can be an oil, a fractionated oil, triglycerides, diglycerides, monoglycerides, propylene glycol fatty acid diesters, and the like. The formulations offer distinct advantages of long shelf life for the stability and potency of the formulation and sustained release of active pharmaceutical ingredients to reduce the frequency of medication dosing and to increase patient compliance.
Abstract: The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of the compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
Abstract: The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
Type:
Grant
Filed:
February 19, 2015
Date of Patent:
November 15, 2016
Assignee:
AstraZeneca AB
Inventors:
Paul David Johnson, Andrew Leach, Richard William Arthur Luke, Zbigniew Stanley Matusiak, Jeffrey James Morris
Abstract: There is provided compounds of formula I, wherein E1, E2, E3, E4, L1, Y1, Y2, Y3, Ra and z have meanings provided in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of respiratory diseases and inflammation.
Type:
Application
Filed:
May 4, 2016
Publication date:
November 10, 2016
Applicant:
AstraZeneca AB
Inventors:
Robert Ronn, Carl Jonas Lindh, Erik Ringberg, Hanna Birgitta Ellinor Andersson, Peter Nilsson, Wesley Ralph Schaal, Magnus Munck af Rosenschöld, Antonios Nikitidis, Grigorios Nikitidis, Petra Johannesson, Christian Tyrchan
Abstract: The present invention relates to pharmaceutical compositions suitable for oral administration, and more particularly to pharmaceutical compositions, including pharmaceutical tablet compositions, containing N-(2-{2-dimethylaminoethyl-methyl-amino}-4-methoxy-5-[4-(1-methylindol-3-yppyrimidin-2-yl]amino phenyl)prop-2-enamide (“AZD9291”) or a pharmaceutically Cacceptable salt thereof, wherein such compositions comprise a certain amount of microcrystalline cellulose and at least one other pharmaceutical diluent.
Type:
Application
Filed:
January 2, 2015
Publication date:
November 10, 2016
Applicant:
AstraZeneca AB
Inventors:
Cindy FINNIE, Steven Anthony RAW, David WILSON
Abstract: The present invention discloses certain new solid state forms of (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy.
Abstract: The present invention relates to a combination comprising (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, or a pharmaceutically acceptable salt thereof, hereafter “Compound (I)”, and a taxane. Taxanes include established cancer drugs such as docetaxel (Taxotere™) and paclitaxel (Taxol™). Such combinations may be useful in the treatment or prophylaxis of cancer. The invention also relates to a pharmaceutical composition comprising such Compound (I) and a taxane. The invention further relates to a method of treatment comprising the simultaneous, sequential or separate administration of Compound (I) and a taxane, to warm-blooded animal, such as man. The invention also relates to a kit comprising Compound (I) and a taxane, optionally with instructions for use.
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