Abstract: The present invention relates to an Breath actuated inhaler (BAI) actuator, comprising: a loading element capable of being loaded with an actuation force, a breath actuated trigger mechanism arranged to counteract the actuation force of the loading element, and to fire the actuator by releasing the actuation force of the loading element in response to an inhalation breath, and actuation locking means moveable between a locked position wherein it relieves the actuation force from the trigger mechanism setting the trigger mechanism in a neutral position, and an armed position wherein the trigger mechanism is set in an armed position.
Type:
Grant
Filed:
December 21, 2007
Date of Patent:
July 24, 2012
Assignee:
AstraZeneca AB
Inventors:
Nicholas Bowman, Jörgen Fruensgaard, Jörgen Funder Rasmussen, Henrik Hougaard Vilstrup, Keld Sloth Christensen
Abstract: The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound (I): X is ?O, ?N—OH or ?N—OC(O)Me; Y is hydrogen, PhS- or p-chlorophenylsulfanyl; Z is hydrogen or —CH2COOR1 wherein R1 is selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.
Type:
Grant
Filed:
July 6, 2010
Date of Patent:
July 24, 2012
Assignee:
AstraZeneca AB
Inventors:
Debra Ainge, Eric Merifield, Colin Thomson, Michael Butters, Ravi Ramakrishnan, Ravi Naidu Rayapati, Parhalad Ray Sharma
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: The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
March 12, 2012
Publication date:
July 12, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Håkan Bladh, Frank Burkamp, Balint Gabos, Peter Hansen, Svetlana Ivanova, Karolina Lawitz
Abstract: A pharmaceutical composition which comprises N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide with mannitol and/or microcrystalline cellulose is described.
Type:
Application
Filed:
March 21, 2012
Publication date:
July 12, 2012
Applicant:
ASTRAZENECA AB
Inventors:
John David Blyth, Andrew John Day, Kieran James Lennon
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
Type:
Grant
Filed:
May 19, 2009
Date of Patent:
July 3, 2012
Assignees:
AstraZeneca AB, Bayer Schering Pharma AG
Inventors:
Markus Berger, Hartmut Rehwinkel, Jan Dahmén, Anders Eriksson, Thomas Hansson, Nafizal Hossain, Per Tomas Klingstedt, Matti Lepistö, Stinabritt Nilsson, Martin Hemmerling, Karl Edman
Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
Type:
Application
Filed:
July 21, 2011
Publication date:
June 28, 2012
Applicant:
AstraZeneca AB
Inventors:
David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
Abstract: The invention concerns quinazoline derivatives of Formula I or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r 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 or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
Type:
Application
Filed:
December 20, 2011
Publication date:
June 28, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Gabor Csjernyik, Sofia Karlström, Annika Kers, Karin Kolmodin, Martin Nylöf, Liselotte Öhberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Söderman, Britt-Marie Swahn, Stefan Von Berg
Abstract: The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
Type:
Application
Filed:
December 20, 2011
Publication date:
June 28, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Karin Kolmodin, Britt-Marie Swahn, Jacob Kihlström, Johan Lindström, Sofia Karlström, Marie Sundström, Stefan Von Berg
Abstract: The invention provides compounds of formula (I) wherein R4 is a group of formula (II) or (IIIa) or (IIIb) and R1, R2, R3, R5, a, b and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation (I), (II), (IIIa), (IIIb).
Type:
Grant
Filed:
November 13, 2007
Date of Patent:
June 26, 2012
Assignee:
Astrazeneca AB
Inventors:
Rhonan Ford, Andrew Mather, Antonio Mete
Abstract: The invention concerns benzamide compounds 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 tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).
Type:
Grant
Filed:
October 17, 2006
Date of Patent:
June 26, 2012
Assignee:
Astrazeneca AB
Inventors:
David Michael Andrews, Elaine Sophie Elizabeth Stokes, Andrew Turner, Michael James Waring
Abstract: A processing method and apparatus are disclosed for processing an inhaler component of a dry powder inhaler so as to remove any electrostatic charge and improve inhaler performance in drug delivery to the respiratory tract. The method includes exposing the inhaler component, while it contains an amount of medicament, to a gas in a chamber at a first predetermined pressure; exposing the inhaler component, in the chamber, to gas at a second pressure greater than the first pressure; and repeating the exposure of the inhaler component to gas at a pressure no greater than the first predetermined pressure.
Abstract: A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation.
Type:
Application
Filed:
February 21, 2012
Publication date:
June 14, 2012
Applicant:
AstraZeneca AB
Inventors:
Nicola Frances Bateman, Philip Alexander Macfaul, Ian Alun Nash
Abstract: A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation.
Type:
Application
Filed:
February 21, 2012
Publication date:
June 14, 2012
Applicant:
AstraZeneca AB
Inventors:
Nicola Frances BATEMAN, Philip Alexander MACFAUL, Ian Alun NASH
Abstract: There is provided a process for the preparation of a compound of Formula 1, the use of said process in the preparation of a compound of Formula 5 or a phosphate, sulphate, hydrogensulphate, malate, citrate, tartrate or fumarate salt thereof, and the use of the fumarate salt in a composition for use in therapy.
Type:
Grant
Filed:
June 18, 2009
Date of Patent:
June 12, 2012
Assignee:
AstraZeneca AB
Inventors:
Helen Blade, Gwydion Huw Churchill, Angela Charlotte Currie, Benjamin Charles Dobson, Martin Neal Kenworthy, Lyn Powell, Steven Anthony Raw, Peter Samuel Hynes
Abstract: The invention concerns pyrazine derivatives of the Formula I or pharmaceutically-acceptable salts thereof; wherein each of n, m and R 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 bone-related disorders or conditions.
Type:
Grant
Filed:
January 18, 2011
Date of Patent:
June 12, 2012
Assignee:
Astrazeneca AB
Inventors:
Tao Feng, Hitesh Jayantilal Sanganee, Hiroki Wada
Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.
Type:
Application
Filed:
November 29, 2011
Publication date:
June 7, 2012
Applicant:
ASTRAZENECA AB
Inventors:
Jonas Bostrõm, Hans Emtenäs, Kenneth Granberg, Mickael Mogemark, Antonio Llinas
Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
May 6, 2010
Date of Patent:
June 5, 2012
Assignee:
AstraZeneca AB
Inventors:
Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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:
Grant
Filed:
August 20, 2009
Date of Patent:
June 5, 2012
Assignee:
AstraZeneca AB
Inventors:
Seth Björk, Peter Johnström, Nils Anders Nilsson, Katinka Ruda, Per Magnus Schou, Britt-Marie Swahn, Vern Delisser