Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
Type:
Grant
Filed:
December 5, 2008
Date of Patent:
December 14, 2010
Assignee:
AstraZeneca AB (PUBL)
Inventors:
Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-[(4-fluoro-2-methy-1-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline starting from a compound of Formula IX: wherein R4 is a protecting group; or an intermediate there between, using process steps, reagents and conditions as described.
Type:
Grant
Filed:
October 31, 2007
Date of Patent:
December 14, 2010
Assignee:
AstraZeneca AB
Inventors:
Euan Alexander Arnott, John Crosby, Matthew Charles Evans, James Gair Ford, Martin Francis Jones, Kevin William Leslie, Ian Michael McFarlane, George Joseph Sependa
Abstract: The invention relates to melanocortin receptor-specific cyclic peptides of Formula (I) or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4a, R4b, R4c, R5, x and y are as defined in the specification. These compounds are particularly useful in the treatments of energy homeostasis and metabolism related (e.g. diabetes), food intake related and/or energy balance and body weight related diseases, disorders and/or conditions, including obesity, overweight and diseases, disorders and/or conditions associated with obesity and/or overweight, such as type 2 diabetes and metabolic syndrome.
Abstract: Compounds of formula (I) or salts thereof, wherein A, and R1 to R5 are as defined in the specification, are DGAT-1 inhibitors and are thereby useful in the treatment of, for example, obesity. Processes to make compounds of formula (I) are also described.
Abstract: The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z).
Type:
Application
Filed:
August 29, 2008
Publication date:
December 9, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Leslie Dakin, Benjamin Fauber, Alexander Hird, James Janetka, Daniel John Russell, Qibin Su, Bin Yang, Xiaolan Zheng
Abstract: The invention provides [2-(4-chloro-benzyloxy)-ethyl]-[2-((R)-cyclohexyl-hydroxy-phenyl-methyl)-oxazol-5-yl-methyl]-dimethyl-ammonium napadisylate, pharmaceutical compositions containing it, and its use in therapy.
Type:
Grant
Filed:
February 6, 2008
Date of Patent:
December 7, 2010
Assignees:
AstraZeneca AB, Argenta Discovery Ltd.
Inventors:
Barbara Giuseppina Avitabile, David O'Sullivan, Richard James Bull
Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein X, A, R1, R2, R3 and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Type:
Application
Filed:
June 11, 2007
Publication date:
December 2, 2010
Applicant:
AstraZeneca AB
Inventors:
William Brown, Daniel Page, Sanjay Srivastava, Christopher Walpole, Zhong-Yong Wei, Hua Yang
Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
Type:
Grant
Filed:
September 3, 2008
Date of Patent:
November 30, 2010
Assignee:
AstraZeneca AB
Inventors:
Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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:
September 29, 2003
Date of Patent:
November 30, 2010
Assignee:
AstraZeneca AB
Inventors:
Jan Andersson, Allan Dagsland, Hans Strid, Jan Trofast, Stefan Friess, Harald Heckenmueller, Uwe Rollwage, Volker Tiedemann, John Conway
Abstract: Nicotinic acetylcholine receptor ligands of Formula I wherein X, n, R1 and R2 are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing, and methods for using the same.
Type:
Grant
Filed:
May 17, 2007
Date of Patent:
November 30, 2010
Assignee:
AstraZeneca AB
Inventors:
Hui-Fang Chang, Christopher Holmquist, Eifion Phillips, Timothy Piser, Thomas Simpson, Rebecca Urbanek, James Woods, Hui Xiong
Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.
Abstract: The present invention relates to methods and tools for producing large quantities of gamma-carboxylated protein comprising: (i) culturing a cell adapted to express a protein which requires gamma-carboxylation and ?-glutamyl carboxylase in a ratio of at least 10:1, under conditions suitable for expression of both proteins, and (ii) isolating gamma-carboxylated protein.
Type:
Grant
Filed:
October 14, 2004
Date of Patent:
November 30, 2010
Assignee:
AstraZeneca AB
Inventors:
Christel Fenge, Ann Lövgren, Anders Thelin
Abstract: The present invention provides 2-azetidinone derivatives, or pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof, comprising formula (I): wherein the substituents are as herein defined. The compounds possess cholesterol absorption inhibitory activity and are accordingly of value in the treatment of disease states associated with hyperlipidaemic conditions.
Abstract: There is provided compounds of formula I, wherein R1 to R7 have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
Type:
Application
Filed:
July 12, 2007
Publication date:
November 25, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Annika Bjore, Jonas Bostrom, Ojvind Davidsson, Hans Emtenas, Ulrik Gran, Tommy Iliefski, Johan Kajanus, Roine Olsson, Lars Sandberg, Gert Strandlund, Johan Sundell, Zhong-Qing Yuan
Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
Abstract: The invention provides triazolo [4,5-d]pyrimidine compounds, acting as P2T(P2Y12)receptor antagonists. The compounds are useful for the treatment or prevention of abdominal aortic aneurysms.
Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.
Abstract: The invention provides salts of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate, pharmaceutical compositions containing them and their use in therapy.
Abstract: A compound of formula (1), 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:
August 23, 2005
Date of Patent:
November 23, 2010
Assignee:
AstraZeneca AB
Inventors:
David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Jeffrey Paul Stonehouse