Abstract: There is provided a process for the preparation of a sulfonic acid salt of formula I, or a solvate thereof, which process comprises hydrogenating a sulfonic acid salt of formula II, or a solvate thereof; in the presence of a solvent system consisting essentially of water, a C3-5 secondary alkyl alcohol and no more than 15% v/v of another organic solvent, wherein the sulfonic acid salt of formula I is optionally, without isolation, converted to a compound of formula IX, or a pharmaceutically-acceptable derivative thereof, wherein R1, R2, R3, R6, R7, R8, A, B and D have meanings given in the description.
Abstract: The invention concerns a compound of the Formula I wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl or (1-6C)alkyl; R3 is hydrogen, halogeno or (1-6C)alkyl; and R4 is (3-6C)cycloalkyl;or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
Type:
Grant
Filed:
December 22, 2005
Date of Patent:
August 31, 2010
Assignee:
AstraZeneca AB
Inventors:
Ian Alun Nash, Kenneth Mark Page, Paul Allen Bethel
Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
Abstract: Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.
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 a platinum anti-tumour agent; to a pharmaceutical composition comprising ZD6474 and a platinum anti-tumour agent; to a combination product comprising ZD6474 and a platinum anti-tumour agent for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and a platinum anti-tumour agent; to the use of ZD6474 and a platinum anti-tumour agent in the manufacture of a medicament for use in the production of all antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.
Type:
Application
Filed:
November 24, 2009
Publication date:
August 26, 2010
Applicant:
AstraZeneca AB
Inventors:
Stephen Robert Wedge, Anderson Joseph Ryan
Abstract: The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, 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.
Type:
Application
Filed:
August 15, 2007
Publication date:
August 26, 2010
Applicant:
ASTRAZENECA
Inventors:
Brian Aquila, Donald J. Cook, Craig Johnstone, Stephen Lee, Paul Lyne, David Alan Rudge, Melissa Vasbinder, Haixia Wang
Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
Type:
Grant
Filed:
October 8, 2009
Date of Patent:
August 24, 2010
Assignee:
AstraZeneca AB
Inventors:
Joseph Cacciola, James Empfield, James Folmer, Angela M Hunter, Scott Throner
Abstract: A process for the preparation of a dispersion of crystalline nanoparticles in an aqueous medium is disclosed. Specifically, a first solution comprising a substantially water-insoluble substance in a water-miscible organic solvent is rapid mixed with an aqueous phase comprising water, and optionally a stabilizer, to form a dispersion of amorphous particles. The dispersion of amorphous particles is then sonicated for a sufficient period to form crystalline nanoparticles of the substantially water-insoluble substance. The process provides nanocrystals with a mean hydrodynamic diameter of less than 1 micron, particularly less than 300 nm, and is particularly useful for the preparation of nanocrystalline dispersions of pharmaceutical substances.
Type:
Grant
Filed:
July 14, 2003
Date of Patent:
August 24, 2010
Assignee:
AstraZeneca AB
Inventors:
Tommy Urban Skantze, Per Lennart Lindfors, Sara Forssen
Abstract: A powder inhaler for administering powder by inhalation, comprising: a flow path defined by a plurality of surfaces through which a stream of air is in use drawn on inhalation by a user; and dosing means (18) for providing a dose of powder to the flow path for entrainment in the stream of air; characterized in that the inhaler further comprises dislodging means for dislodging powder accumulated on a surface of the flow path downstream of the dosing means (18).
Type:
Grant
Filed:
November 15, 2007
Date of Patent:
August 24, 2010
Assignee:
AstraZeneca AB
Inventors:
Jan Andersson, Allan Dagsland, Hans Strid, Jan Trofast, Stefan Friess, Harald Heckenmueller, Uwe Rollwage, Volker Tiedemann, John Conway
Abstract: A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents hydrogen, hydroxy, methoxy or ethoxy, and n represents 0, 1 or 2; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable diluent or carrier; provided that the formulation may only contain iota-carageenan and a neutral gelling polymer when the compound of formula (I) is in the form of a salt; such formulations being of use for the treatment of a cardiovascular disorder.
Abstract: A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defined in the specification, is described. Novel intermediates are also described and claimed.
Type:
Application
Filed:
February 15, 2010
Publication date:
August 19, 2010
Applicant:
AstraZeneca AB
Inventors:
Michael Butters, Jeffrey Crabb, Philip Hopes, Bharti Patel
Abstract: A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described.
Type:
Application
Filed:
February 15, 2010
Publication date:
August 19, 2010
Applicant:
AstraZeneca AB
Inventors:
Sharon Ann BOWDEN, David Peter HOILE, Karin LÖVQVIST
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.
Abstract: A process is provided for the preparation of a compound of formula (1) wherein R and R? represent optionally substituted hydrocarbyl groups and X represents a hydrocarbyl linking group. The process comprises either the stereoselective reduction of the keto group in a dihydroxy keto precursor followed by selective esterification of a primary hydroxy, or selective esterification of a primary hydroxy of a dihydroxy keto precursor followed by stereoselective reduction of the keto group.
Type:
Application
Filed:
April 27, 2010
Publication date:
August 19, 2010
Applicant:
AstraZeneca UK Limited
Inventors:
Andrew John BLACKER, Christopher David REEVE, Robert Anthony HOLT
Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
Abstract: Methods for producing and using protein/peptide fingerprints, derived from elastin degraded by the enzyme human Neutrophil Elastase (HNE), allowing identification and investigation of disease-associated proteins/peptides that can be linked to specific drug targets, or to specific drug target combinations. The methods are particularly useful for studies relating to Chronic Obstructive Pulmonary Disease (COPD).
Type:
Application
Filed:
March 20, 2006
Publication date:
August 12, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Per Broberg, Thomas Fehniger, Claes Lindberg, Gyorgy Marko-Varga, Stephan Uebel
Abstract: The present invention relates to compounds of Formula (I) and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.
Abstract: A novel process for the preparation of hydantoin sulfonyl chlorides of general formula (I) wherein R and n are as specified in the description, and certain novel intermediates thereto, are disclosed.
Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno-(1-6C)alkyl, hydroxyl-(1-6C)alkyl, di-[(1-6C)akly]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6C)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cyt
Type:
Grant
Filed:
September 23, 2004
Date of Patent:
August 10, 2010
Assignee:
AstraZeneca AB
Inventors:
Dearg Sutherland Brown, George Robert Brown