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.
Abstract: Dihydropyridopyrimidine compounds of formula (Ia) and therapeutically acceptable salts thereof, wherein R1, R2 and Z are as defined in the specification; processes for making them and methods for using them in the treatment of A?-related pathologies.
Type:
Grant
Filed:
November 6, 2009
Date of Patent:
May 29, 2012
Assignee:
AstraZeneca AB
Inventors:
Rickard Forsblom, Kim Paulsen, Didier Rotticci, Ellen Santangelo, Magnus Waldman
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 wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X2 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or —CONHSO2Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.
Type:
Grant
Filed:
June 18, 2010
Date of Patent:
May 29, 2012
Assignee:
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 invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.
Type:
Application
Filed:
January 30, 2012
Publication date:
May 24, 2012
Applicant:
AstraZeneca AB
Inventors:
Adrian Clark, Elfyn Jones, Ulf Larsson, Anna Minidis
Abstract: One aspect of the invention features a method of analyzing dose metered devices by: spraying an aerosol from a metered dose device directly into a spray chamber of a mass spectrometer detector by firing a dose from a metered dose device, for example a pMDI, by depressing the pMDI in its actuator, which spraying step is optionally preceded by a step of priming the drug container of the metered dose device; ionizing the aerosol; and identifying and quantifying the content of the dose using the detector.
Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X1, X2, X5, R1, R2 and R4 are as defined herein. Compounds of Formula Ia-2 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
Type:
Grant
Filed:
June 21, 2006
Date of Patent:
May 22, 2012
Assignees:
Array BioPharma Inc., AstraZeneca AB
Inventors:
John DeMattei, Sagar Shakya, Paul J. Nichols, Bradley R. Barnett, Bruno P. Hache, Matthew Charles Evans, James Gair Ford, John Leonard
Abstract: The invention provides compounds of formula (I): wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds are useful as MMP inhibitors.
Type:
Grant
Filed:
November 28, 2007
Date of Patent:
May 22, 2012
Assignee:
AstraZeneca AB
Inventors:
David Chapman, Balint Gabos, Magnus Munck af Rosenschöld
Abstract: The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.
Type:
Grant
Filed:
February 8, 2011
Date of Patent:
May 22, 2012
Assignee:
AstraZeneca AB
Inventors:
Adrian Clark, Elfyn Jones, Ulf Larsson, Anna Minidis
Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
Type:
Application
Filed:
January 25, 2012
Publication date:
May 17, 2012
Applicant:
AstraZeneca AB
Inventors:
Michelle Lamb, Tao Wang, Dingwei Yu, Peter Mohr, Bin Wang
Abstract: The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of A?-related diseases.
Type:
Application
Filed:
November 9, 2011
Publication date:
May 17, 2012
Applicant:
ASTRAZENECA AB
Inventors:
István MACSÁRI, Kim PAULSEN, Laszlo RAKOS, Britt-Marie SWAHN, Magnus WALDMAN, Didier ROTTICCI, Stefan VON BERG
Abstract: Compounds of formula (IA) 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:
Application
Filed:
May 28, 2010
Publication date:
May 17, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Neil Bifulco, Allison Laura Choy, Olga Quiroga, Brian Alan Sherer
Abstract: Imidazole substituted pyrimidines and pharmaceutically acceptable salts thereof; pharmaceutical formulations containing such pyrimidines; the use of such compounds in therapy; the use of such compounds for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as methods of treatment of such disorders comprising administering to subjects in need of such treatment therapeutically effective amounts of such compounds.
Type:
Grant
Filed:
April 14, 2010
Date of Patent:
May 15, 2012
Assignee:
AstraZeneca AB
Inventors:
Per I Arvidsson, Jeremy Nicholas Burrows, Ulrika Yngve, Erica Tjerneld
Abstract: The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.
Type:
Application
Filed:
November 10, 2011
Publication date:
May 10, 2012
Applicants:
ARRAY BIOPHARMA, INC, ASTRAZENECA AB
Inventors:
Nicola Frances Bateman, Paul Richard Gellert, Kathryn Jane Hill
Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.
Type:
Application
Filed:
January 6, 2012
Publication date:
May 3, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Peter Hansen, Marianne Ivarsson, Karolina Lawitz, Hans Lonn, Antonios Nikitidis, Asim Ray
Abstract: Processes for the preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline, salts thereof, and the intermediates used in the process are described.
Type:
Application
Filed:
April 22, 2010
Publication date:
May 3, 2012
Applicant:
AstraZeneca AB
Inventors:
Kay Alison Boardman, Oliver Robert Cunningham, William Robert Fraser Goundry, David Dermot Patrick Laffan
Abstract: DGAT-1 inhibitor compounds of formula (1), 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 wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ?0; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.
Type:
Application
Filed:
May 5, 2011
Publication date:
May 3, 2012
Applicant:
AstraZeneca AB
Inventors:
Udo Andreas BAUER, Jonas Gunnar BARLIND, Petra JOHANNESSON, Jan Magnus JOHANSSON, Alexander Tobias NOESKE, Annika Ulrika PETERSSON, Alan Martin BIRCH, Roger John BUTLIN, Clive GREEN, Andrew LEACH, Ragnar HOVLAND
Abstract: The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
Type:
Application
Filed:
January 11, 2012
Publication date:
May 3, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Gloria Breault, Charles Joseph Eyermann, Bolin Geng, Marshall Morningstar, Folkert Reck
Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
Type:
Grant
Filed:
October 14, 2009
Date of Patent:
May 1, 2012
Assignee:
AstraZeneca AB
Inventors:
Yevgeni Besidski, Martin Nylof, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin