Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Type:
Grant
Filed:
March 17, 2010
Date of Patent:
June 14, 2011
Assignee:
AstraZeneca AB
Inventors:
Anders Broo, Robert Judkins, Lanna Li, Eva-Lotte Lindstedt-Alstermark, Pernilla Sandberg, Marianne Swanson, Lars Weidolf, Kay Brickmann, Patrik Holm
Abstract: There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.
Type:
Grant
Filed:
September 27, 2007
Date of Patent:
June 14, 2011
Assignee:
AstraZeneca AB
Inventors:
Rolf Johansson, Sofia Karlström, Annika Kers, Gunnar Nordvall, Tobias Rein, Can Slivo
Abstract: A method of treating at least one symptom or condition associated with but not limited to: Anxiety Disorders including but not limited to Panic Disorder Without Agoraphobia, Panic Disorder With Agoraphobia, Agoraphobia Without History of Panic Disorder, Specific Phobia, Social Phobia, Obsessive-Compulsive Disorder, Postaumatic Stress Disorder, Acute Stress Disorder, Generalized Anxiety Disorder and Generalized Anxiety Disorder Due to a General Medical Condition comprising administering an effective amount of Formula I or its pharmaceutically acceptable salt. In another aspect of the invention a pharmaceutical composition is provided comprising an effective amount of Formula I or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier or diluent.
Type:
Application
Filed:
November 8, 2010
Publication date:
June 9, 2011
Applicant:
AstraZeneca AB
Inventors:
Patricia C. Davis, Jeffrey M. Goldstein, Scott W. Grimm, Helen R. Winter, Raymond F. Suckow
Abstract: The present invention provides compounds of formula (I): wherein Ra, Rb, Rc, R1, R2, R3, X1, Y1, Z1, A, n and m 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.
Type:
Application
Filed:
December 2, 2010
Publication date:
June 9, 2011
Applicants:
Dainippon Sumitomo Pharma Co. Ltd., AstraZeneca AB
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:
Application
Filed:
November 5, 2010
Publication date:
June 9, 2011
Applicant:
AstraZeneca AB
Inventors:
Hui-Fang Chang, Christopher Holmquist, Eifion Phillips, Timothy Piser, Thomas Simpson, Rebecca Urbanek, James Woods, Hui Xiong
Abstract: The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure trans-cyclopropane carboxylic acid derivatives, processes for preparing the carboxylic acid derivatives and their use in preparing pharmaceuticals.
Type:
Application
Filed:
November 30, 2010
Publication date:
June 9, 2011
Applicant:
ASTRAZENECA AB
Inventors:
Jean-Paul Dejonghe, Koen Peeters, Marc Renard
Abstract: Compounds of formula (I) Q-L-W—C(?X)—Z—P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C—C chemokine mediated conditions.
Type:
Application
Filed:
February 1, 2011
Publication date:
June 9, 2011
Applicant:
ASTRAZENECA AB
Inventors:
Justin Fairfield Bower, Jeffrey Philip Poyser, Paul Turner, David Waterson, Jon Winter
Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
September 6, 2006
Date of Patent:
June 7, 2011
Assignee:
AstraZeneca AB
Inventors:
Alan Faull, Craig Johnstone, Andrew Morley, Jeffrey Philip Poyser
Abstract: Compounds of Formulae I, or pharmaceutically acceptable salts thereof: wherein A1, A2, G1, G2 G3, R1, R2, X, Y, Z, m, n and p 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.
Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.
Type:
Application
Filed:
June 22, 2009
Publication date:
June 2, 2011
Applicant:
ASTRAZENECA AB
Inventors:
Jonas Branalt, David Gustafsson, Ingemar Nilsson, Magnus Polla
Abstract: The present invention relates to sublingual compositions comprising (2S)-(4E)-N-methyl-5-(3-(5-iso-propoxypyridin)yl)-4-penten-2-amine or pharmaceutically acceptable salts thereof, to the preparation of said compositions and the use of thereof in therapy.
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
Type:
Application
Filed:
October 26, 2005
Publication date:
June 2, 2011
Applicant:
ASTRAZENECA AB
Inventors:
Håkan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepistö
Abstract: The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.
Type:
Grant
Filed:
March 12, 2007
Date of Patent:
May 31, 2011
Assignee:
AstraZeneca AB
Inventors:
Lilian Alcaraz, Andrew Lister, Garry Pairaudeau
Abstract: New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.
Type:
Grant
Filed:
February 3, 2009
Date of Patent:
May 31, 2011
Assignee:
AstraZeneca AB
Inventors:
Gary Peter Tomkinson, Martin John Packer, James Stewart Scott, Paul Robert Owen Whittamore, Andrew Stocker
Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).
Type:
Grant
Filed:
February 2, 2009
Date of Patent:
May 31, 2011
Assignee:
AstraZeneca AB
Inventors:
Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Clifford David Jones, Darren McKerrecher, Michael Howard Block, Craig Johnstone
Abstract: Compounds of formula I: and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy.
Type:
Application
Filed:
October 27, 2010
Publication date:
May 26, 2011
Applicant:
AstraZeneca AB
Inventors:
Hui-Fang Chang, Yan Li, Eifion Phillips
Abstract: The invention concerns compounds of the formula (I) wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man.
Type:
Grant
Filed:
December 12, 2005
Date of Patent:
May 24, 2011
Assignee:
AstraZeneca AB
Inventors:
Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
Abstract: A process for preparing an intermediate compound of formula (II) where X is as defined in the specification, R1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl; R2, R3, R4 and R5 are organic groups as defined in the specification, which process comprises aromatisation of a compound of formula (III) where R1, R2, R3, n, X and R5 are as defined in relation to formula (II) and R4? is a group R4 or a precursor group thereof, and thereafter if necessary or desired, carrying out one or more of the following steps: (i) removing any hydroxy-protecting groups R; (ii) converting a precursor group R4? to a group R4, or where R4? is a group R4, converting it to a different such group. Compounds obtained are useful intermediates for example in the preparation of fulvestrant. Novel intermediates are also claimed.
Type:
Grant
Filed:
October 9, 2001
Date of Patent:
May 24, 2011
Assignee:
AstraZeneca AB
Inventors:
Robert Stevenson, Fraser Witton Kerr, Anthony Raymond Lane, Eve Joanne Brazier, Phillip John Hogan, David Dermot Patrick Laffan