Abstract: Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
Type:
Grant
Filed:
March 6, 2003
Date of Patent:
October 28, 2008
Assignee:
AstraZeneca AB
Inventors:
Nicholas John Newcombe, Andrew Peter Thomas
Abstract: The invention concerns amide derivatives of Formula (Ia) wherein X is —NHCO— or —CONH—; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino and carboxy; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino and N-(1-6C)alkyl-arylamino; 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 cytokines.
Abstract: Process for the preparation of an ester of formula (1), wherein R1 represents a leaving group, CN, OH or a COOR5 group, R3 and R4 each independently represent a 1-3 C alkyl group, and R2 and R5 each independently represent an ester residue, wherein the corresponding salt with formula (2), wherein M represents H or an alkali (earth) metal in an inert solvent is contacted with an acid chloride forming agent to form the corresponding acid chloride, and the acid chloride is contacted with an alcohol with formula R2OH in the presence of N-methyl-morpholine. Preferably M represents an alkali metal, and R2 represents an alkyl group, particularly a t.-butyl group.
Type:
Grant
Filed:
June 12, 2003
Date of Patent:
October 28, 2008
Assignee:
AstraZeneca UK Limited
Inventors:
Hermanus Carolus Catherina Karel Bakel Van, Dominique Monique Charles Callant, Jacob Hermanus Mattheus Hero Kooistra, Peter Johannes Dominicus Maas
Abstract: Compounds of Formula: wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Type:
Application
Filed:
January 5, 2005
Publication date:
October 23, 2008
Applicant:
ASTRAZENECA AB
Inventors:
William Brown, Andrew Griffin, Christopher Walpole
Abstract: Certain 4,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, methods for their therapeutic use and pharmaceutical compositions containing them are described.
Abstract: Compounds of formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Type:
Application
Filed:
February 24, 2006
Publication date:
October 23, 2008
Applicant:
ASTRAZENECA AB
Inventors:
William Brown, Andrew Griffin, Andrea Penwell
Abstract: The present invention relates crystals of LigA and computer-assisted methods for screening, identifying, and designing inhibitors and allosteric modulators of LigA.
Abstract: The present invention relates to novel imidazole compounds having a positive allosteric GABAB receptor (CUR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).
Type:
Application
Filed:
April 17, 2008
Publication date:
October 23, 2008
Applicant:
ASTRAZENECA AB
Inventors:
Udo Bauer, Wayne Brailsford, Leifeng Cheng, Maria Jonforsen, Florian Raubacher, Peter Schell, Tor Svensson
Abstract: Methods and systems for providing and correlating clinical and business performance measures and benchmarks for medical practitioners are provided. Clinical and business data is collected from a plurality of medical practitioners. The clinical data may pertain to one or more clinical metrics that relate to treatment offered to patients by medical practitioners. The business data may pertain to one or more business metrics that relate to commercial performance of the medical practitioners. Several benchmarking reports are prepared based on this data and provided to different medical practitioners showing them where they stand in comparison to other practitioners within their practice, specific or general discipline or industry.
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 chemokine (such as CCR3) or H1 mediated disease state.
Type:
Application
Filed:
April 5, 2005
Publication date:
October 23, 2008
Applicant:
ASTRAZENECA AB
Inventors:
Tobias Mochel, Matthew Perry, Brian Springthorpe
Abstract: The present invention arises from the identification of an association between the gene encoding glucosyltransferase-like protein (GT) and osteoarthritis (OA). It therefore relates to diagnostic techniques for determining a patient's susceptibility to develop OA by detecting all or part of the GT gene, its precursors or products (mRNA, cDNA, genomic DNA, or protein). In particular, the invention relates to methods and materials for analysing allelic variation in the GT gene, and to the use of GT polymorphisms in the identification of an individuals' risk to develop OA. The invention is also directed to methods for identifying modulators of OA, which modulate the GT gene or its encoded protein.
Abstract: A method for attenuating a microorganism which comprises inhibiting in the microorganism a metabolic pathway essential for viability, by promoting use of the substrate of the pathway in a different metabolic pathway which is non-essential to the microorganism whereby the substrate is unavailable to the essential pathway and the micro organism is attenuated.
Abstract: The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR2 wherein R2 is H or C1-C6 alkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5, wherein R4 and R5 are as defined in the specification; and R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined in the specification. The invention further relates to a process for the preparation of the intermediates.
Type:
Grant
Filed:
October 3, 2006
Date of Patent:
October 21, 2008
Assignee:
AstraZeneca AB
Inventors:
Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
Abstract: There is provided a process for the preparation of a compound of formula I, (I), or a pharmaceutically acceptable derivative thereof, wherein A, B, G, R1, R2, R3, R4 and R41 to R46 have meanings given in the description, which process comprises the dehydrative cyclisaton of a compound of formula II. (II).
Abstract: The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.
Type:
Grant
Filed:
June 23, 2003
Date of Patent:
October 21, 2008
Assignee:
AstraZeneca AB
Inventors:
Andrew Bailey, Garry Pairaudeau, Anil Patel, Stephen Thom
Abstract: Compounds of formula I wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation and new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
Type:
Application
Filed:
October 2, 2006
Publication date:
October 16, 2008
Applicant:
AstraZeneca AB
Inventors:
Per I. Arvidsson, Erwan Arzel, Jeremy Burrows, Helena Gyback, Tobias Rein, Didier Rotticci, Peter Soderman
Abstract: The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to a5b1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins.
Type:
Application
Filed:
April 11, 2008
Publication date:
October 16, 2008
Applicant:
ASTRAZENECA AB
Inventors:
Jean-Claude ARNOULD, Benedicte DELOUVRIE, Craig Steven HARRIS
Abstract: The invention relates to substituted aryl acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
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 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.
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:
Application
Filed:
January 9, 2006
Publication date:
October 16, 2008
Applicant:
ASTRAZENECA AB
Inventors:
Jonas Bostrom, Kay Brickmann, Anders Broo, Robert Judkins, Lanna Li, Pernilla Sandberg, Marianne Swanson, Christer Westerlund, Patrik Holm