Abstract: A process for the preparation of a compound of Formula (1) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(?NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidizing the dihydropyrimidine to form the compound of Formula (I). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, an aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ?O.
Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.
Type:
Grant
Filed:
May 26, 2009
Date of Patent:
September 25, 2012
Assignee:
AstraZeneca AB
Inventors:
Glen Andrews, Rhona Jane Cox, Christopher De Savi, Premji Meghani, Hitesh Jayantilal Sanganee, Daniel Jon Warner
Abstract: The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.
Type:
Grant
Filed:
March 24, 2011
Date of Patent:
September 25, 2012
Assignee:
AstraZeneca AB
Inventors:
Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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:
April 28, 2009
Date of Patent:
September 18, 2012
Assignee:
Astrazeneca AB
Inventors:
Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet
Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
Type:
Grant
Filed:
November 17, 2010
Date of Patent:
September 18, 2012
Assignee:
AstraZeneca AB
Inventors:
David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
Abstract: The invention concerns benzamide compounds of formula (I): compound of formula (I): wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).
Type:
Application
Filed:
May 15, 2012
Publication date:
September 6, 2012
Applicant:
AstraZeneca AB
Inventors:
David Michael Andrews, Elaine Sophie Elizabeth Stokes, Andrew Turner, Michael James Waring
Abstract: The invention concerns bicyclic compounds of Formula I wherein , R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.
Type:
Grant
Filed:
February 9, 2010
Date of Patent:
September 4, 2012
Assignee:
Astrazeneca AB
Inventors:
Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
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 relates to a container for solids or liquid and a method of opening a container. The container comprises a hollow body which holds the contents and a closure which cooperates with the body to close the container. The closure comprises an opening member which is movable from a retracted position to an opening position in which the closure can be opened. The container further comprises a locking member for securing the opening member, the locking member being movable between a locking position in which the opening member is kept secured in the retracted position and an unlocked position in which the opening member is movable into the opening position.
Type:
Grant
Filed:
January 18, 2007
Date of Patent:
August 28, 2012
Assignee:
AstraZeneca AB
Inventors:
Lars Arvidsson, Lena Axelson-Larsson, Maria Benktzon, Thomas Nilsson, Ulrika Vejbrink
Abstract: There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
June 9, 2011
Date of Patent:
August 28, 2012
Assignee:
Astrazeneca AB
Inventors:
Kevin Michael Foote, Johannes Wilhelmus Maria Nissink, Paul Turner
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:
Application
Filed:
March 6, 2012
Publication date:
August 23, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by histone deacetylase.
Type:
Grant
Filed:
September 10, 2010
Date of Patent:
August 21, 2012
Assignee:
Astrazeneca AB
Inventors:
Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
Type:
Application
Filed:
April 23, 2012
Publication date:
August 16, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Ylva Gravenfors, Catrin Jonasson, Jonas Malmström, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Ström, David Wensbo
Abstract: Aromatic or heteroaromatic nitro compounds are catalytically hydrogenated to the corresponding amines in the presence of a platinum catalyst comprising elemental platinum on a support; the platinum catalyst is modified with a molybdenum compound and a phosphorus compound wherein the phosphorus has an oxidation state of less than +5, e.g. hypophosphorous acid; the catalyst is particularly useful in the hydrogenation of nitro compounds with halogen and/or sulfur-containing substituents.
Type:
Grant
Filed:
September 22, 2010
Date of Patent:
August 14, 2012
Assignee:
AstraZeneca AB
Inventors:
Wilhelm Quittman, Thomas Peter Belser, Rhony Niklaus Aufdenblatten
Abstract: There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of the enzyme myeloperoxidase (MPO) is beneficial. Certain novel compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof are disclosed, together with processes for their preparation. The compounds of formulae (Ia) and (Ib) are MPO inhibitors and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders.
Type:
Grant
Filed:
August 4, 2008
Date of Patent:
August 7, 2012
Assignee:
AstraZeneca AB
Inventors:
Sverker Hanson, Gunnar Nordvall, Anna-Karin Tiden
Abstract: Rotary metering valve (200) with a valve inlet (260), a valve outlet (270) and a rotary valve member (280) for transferring a metered dose of aerosol formulation from the inlet to the outlet, wherein the rotary valve member is provided with an inlet port (290) and an outlet port (300), both in communication with a metering conduit (310) in the rotary valve member, the rotary valve member in sequence being rotatable between at least three positions: inlet position where the inlet port is in communication with the valve inlet and aerosol formulation enters the metering conduit, metering position where both ports are closed preserving a metered volume of aerosol formulation in the metering conduit, outlet position where the outlet port is in communication with the valve outlet and the metered dose of aerosol formulation is dispensed from the valve.
Abstract: A package for a dispensing device, comprising a protection pouch arranged to enclose the dispensing device. The protection pouch comprises a base section that is arranged to support the dispensing device in the general vertical direction, and the package comprises a support member arranged to essentially elevate the base section of the pouch from a support surface.
Type:
Grant
Filed:
October 1, 2008
Date of Patent:
August 7, 2012
Assignee:
Astrazeneca AB
Inventors:
Simon Berry, Eric Connolly, Dave Salmon
Abstract: 6-Methyl-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:
Grant
Filed:
February 16, 2010
Date of Patent:
July 31, 2012
Assignee:
Astrazeneca AB
Inventors:
Lars-Erik Briggner, Per Tomas Klingstedt, Hans Roland Lönn, Robert Zuban, Marie-Lyne Alcaraz, Robert Anthony Nixon, Andrew James Watts
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:
December 13, 2011
Publication date:
July 26, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Paul David Johnson, Andrew Leach, Richard William Arthur Luke, Zbigniew Stanley Matusiak, Jeffrey James Morris