Abstract: The present invention relates to compounds of formula (I) The compounds act via antagonism of the CCR2b receptor and may be used to treat inflammatory disease and/or neuropathic pain.
Type:
Application
Filed:
July 25, 2012
Publication date:
November 15, 2012
Applicant:
ASTRAZENECA AB
Inventors:
John Cumming, Alan Wellington Faull, David Waterson
Abstract: This invention generally relates to substituted benzoimidazole compounds, particularly methyl 2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-5-methyl-1H-benzo[d]imidazol-1-yl)methyl)morpholine-4-carboxylate and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.
Type:
Application
Filed:
May 16, 2012
Publication date:
November 15, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Louis-David Cantin, Xuehong Luo, Miroslaw Jerzy Tomaszewski
Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity
Type:
Application
Filed:
April 25, 2012
Publication date:
November 15, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Alan Martin Birch, Roger John Butlin, Leonie Campbell, Clive Green, Andrew Leach, Michael James Waring, Paul Michael Murray, Per Olof Ryberg
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:
November 12, 2010
Publication date:
November 8, 2012
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 chemical processes useful in the manufacture of the compound 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline (the active entity within AZD0530), to intermediates useful in the manufacture of that compound and to processes for the manufacture of those intermediates. The invention also relates to particular crystalline forms of that compound such as a difumarate salt and a trihydrate and to pharmaceutical compositions containing such crystalline forms.
Type:
Grant
Filed:
December 14, 2005
Date of Patent:
November 6, 2012
Assignee:
AstraZeneca AB
Inventors:
James Gair Ford, James Francis McCabe, Anne O'Kearney-McMullan, Simon Mark Pointon, Lyn Powell, Philip O'Keefe, Mark Purdie, Jane Withnall
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: (S)-2-methyl-1-phenyl-2-(pyridin-2-yl)propan-1-amine, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, uses of said compound or salt for therapy of depression and other conditions, and methods of treating depression and other conditions by administering said compound or salt.
Type:
Application
Filed:
March 27, 2012
Publication date:
November 1, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Michael Balestra, Peter Bernstein, Glen E. Ernst, William Frietze, John P. McCauley, Lihong Shen, David Nugiel
Abstract: Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
May 17, 2006
Date of Patent:
October 30, 2012
Assignees:
Array Biopharma Inc., Astrazeneca AB
Inventors:
Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, Jim Blake, Richard Anthony Storey, Rebecca Jane Booth, John David Pittam, John Leonard, Mark Richard Fielding
Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
March 6, 2012
Date of Patent:
October 30, 2012
Assignee:
AstraZeneca AB
Inventors:
Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
Abstract: 6-M ethyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form.
Type:
Application
Filed:
June 27, 2012
Publication date:
October 25, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Lars-Erik BRIGGNER, Per Thomas KLINGSTEDT, Hans Roland LÖNN, Robert ZUBAN, Marie-Lyne ALCARAZ, Robert Anthony NIXON, Andrew James WATTS
Abstract: The invention relates to compounds of the formula (I) wherein ring C, Z, m, n, R1 and R2 are defined herein and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals; processes for the preparation of such compounds; intermediates used in such processes; processes for making such intermediates; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof.
Abstract: Compounds of formula (I) Q-L-W—C(?X)—Z—P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C—C chemokine mediated conditions.
Type:
Application
Filed:
June 7, 2012
Publication date:
October 18, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Justin Fairfield Bower, Jeffrey Philip Poyser, Paul Turner, David Waterson, Jon Winter
Abstract: The invention concerns chromenone compounds of Formula I; or pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, n and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
Type:
Application
Filed:
April 11, 2012
Publication date:
October 18, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Bernard Christophe BARLAAM, Sebastien Louis DEGORCE, Christine Marie Paul LAMBERT-VAN DER BREMPT, Jean-Jacques Marcel LOHMANN, Patrick PLE
Abstract: The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.
Type:
Application
Filed:
June 4, 2012
Publication date:
October 18, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Seth Björk, Vern Delisser, Peter Johnström, Nils Anders Nilsson, Katinka Ruda, Per Magnus Schou, Britt-Marie Swahn
Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
Type:
Grant
Filed:
June 3, 2009
Date of Patent:
October 9, 2012
Assignee:
AstraZeneca AB
Inventors:
Allison Laura Choy, Pamela Hill, John Irvin Manchester, Brian Sherer
Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human, which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises: the administration of ZD6474 in combination with 5-FU; ZD6474 in combination with CPT-11; or ZD6474 in combination with 5-FU and CPT-11.
Type:
Application
Filed:
October 27, 2011
Publication date:
October 4, 2012
Applicant:
AstraZeneca AB
Inventors:
Stephen Robert Wedge, Anderson Joseph Ryan
Abstract: This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl) cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1?,2?,3?(1S*,2R*),5?]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.