Abstract: The use of N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide, or a pharmaceutically acceptable salt thereof, in the treatment of cancer and/or pain in a warm blooded animal such as man is described.
Type:
Application
Filed:
September 13, 2010
Publication date:
January 6, 2011
Applicant:
ASTRAZENECA AB
Inventors:
David Williams Tonge, Sian Tomiko Taylor, Francis Thomas Boyle, Andrew Mark Hughes, Donna Johnson, Marianne Bernice Ashford, Nigel Charles Barrass
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 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:
Grant
Filed:
August 3, 2007
Date of Patent:
January 4, 2011
Assignee:
AstraZeneca AB
Inventors:
Jean-Paul Dejonghe, Koen Peeters, Marc Renard
Abstract: Targeted binding agents, such antibodies directed to the antigen ?V?6 and uses of such agents are described. In particular, fully human monoclonal antibodies directed to the antigen ?V?6 are disclosed. Nucleotide sequences encoding, and amino acid sequences comprising, heavy and light chain immunoglobulin molecules, particularly sequences corresponding to contiguous heavy and light chain sequences spanning the framework regions and/or complementarity determining regions (CDR's), specifically from FR1 through FR4 or CDR1 through CDR3 are disclosed. Hybridomas or other cell lines expressing such immunoglobulin molecules and monoclonal antibodies are also disclosed.
Type:
Application
Filed:
May 18, 2010
Publication date:
December 30, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Julie RINKENBERGER, Ian FOLTZ, Avril ALFRED, Simon Thomas BARRY, Vahe BEDIAN
Abstract: The invention provides compounds of formula (I) wherein R1,R3,L1,L2,G1,G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
Type:
Application
Filed:
December 18, 2008
Publication date:
December 30, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Johan Bylund, Maria E. Ek, Ylva Gravenfors, Jorg Holenz, Alexander Minidis, Gunnar Nordvall, Daniel Sohn, Karl S.A. Vallin, Jenny Viklund, Stefan Von Berg
Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.
Type:
Application
Filed:
June 28, 2010
Publication date:
December 30, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Johan ANDERSSON, Helena GYBÄCK, Anh JOHANSSON, Christian Erik LINDE, Jonas MALMSTRÖM, Gunnar NORDVALL, Tatjana WEIGELT, Gitte TERP
Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.
Type:
Application
Filed:
September 10, 2010
Publication date:
December 30, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
Abstract: The present disclosure is directed to a method for treating a disease or disorder in a patient at risk of developing an NSAID-associated ulcer by administering to said patient in need thereof a pharmaceutical composition in unit dose form comprising naproxen, or pharmaceutically acceptable salt thereof, and esomeprazole, or pharmaceutically acceptable salt thereof to said at risk patient and thereby decreasing the patient's risk of developing an ulcer.
Type:
Application
Filed:
June 24, 2010
Publication date:
December 30, 2010
Applicants:
ASTRAZENECA AB, POZEN INC.
Inventors:
Brian Ault, Clara Hwang, Everardus Orlemans, John R. Plachetka, Mark Sostek
Abstract: This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl)cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1?,2?,3?(1S*,2R*),5?)]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.
Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.
Type:
Grant
Filed:
January 26, 2009
Date of Patent:
December 28, 2010
Assignee:
AstraZeneca AB
Inventors:
Bruce Thomas Dembofsky, Robert Jacobs, Cyrus Ohnmacht
Abstract: The present invention provides a process for the preparation of a compound of formula (I); wherein X is halogen; Y is ZR1; Z is oxygen or sulphur; and R1 is C1-6 alkyl, C1-6 haloalkyl or C3-7 cloalkyl; the process comprising either: hydrogenating a compound of formula (II); with a suitable transition metal catalyst in a C1-6 aliphatic alcohol, an ether, an hydrocarbon as solvent; or, conducting a one-pot hydrogenation of a compound of formula (III): wherein R2 is phenyl optionally substituted by chloro, C1-6 alkyl, C1-6 alkoxy or (C1-6 alkyl)2N; firstly at about 20° C. to form a compound of formula (IV): and then at about 40° C.; both steps (I) and (ii) being carried out in the presence of a suitable catalyst and in the presence of a suitable solvent.
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.
Type:
Application
Filed:
May 2, 2008
Publication date:
December 23, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Audrey Davies, Stephanos Ioannidis, Michelle Lamb, Mei Su, Tao Wang, Hai-Jun Zhang
Abstract: This invention relates to novel compounds having the structural formula I below: (I) 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: A process for isolating a compound of formula (I) or a salt thereof, where X and R1 are as defined in the specification, from a mixture containing it, and the corresponding diacid and dihydroxy derivative, said process comprising (i) adding to an organic solution containing said compounds, water and a one or more salts, all of which are bases selected from a carbonate or hydrogen carbonate base, (ii) separating the aqueous phase containing the compound of formula (II) from the organic phase containing the compounds of formula (I) and (III); then (iii) recovering the compound of formula (I) from remaining organic phase. The process provides for efficient isolation of the target compound, even on a large scale.
Type:
Application
Filed:
June 25, 2008
Publication date:
December 23, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Jeremy Stephen Parker, Evan William Snape
Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X2 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or —CONHSO2Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.
Type:
Application
Filed:
June 18, 2010
Publication date:
December 23, 2010
Applicant:
AstraZeneca AB
Inventors:
Alan Martin Birch, Roger John Butlin, Leonie Campbell, Clive Green, Andrew Leach, Michael James Waring, Paul Michael Murray, Per Olof Ryberg
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.
Inventors:
James Arnold, Phil Edwards, Mark Sylvester, Stefan Berg, Jörg Holenz, Annika Kers, Karin Kolmodin, Laszlo Rakos, Liselotte Öhberg, Rotticci Didier, Gianni Chessari, Miles Congreve, Christopher Murray, Sahil Patel
Abstract: The present invention relates to a novel method to determine the ratio of 5-methoxy and 6-methoxy isomers of omeprazole present in a mixture thereof. The method uses different Raman scattering efficiency values for the 5-methoxy and 6-methoxy isomers. This is of importance since the two isomers have different stability in the solid state in bulk form and in admixture with pharmaceutical excipients.
Abstract: Compounds of formula (I), and salts and pro-drugs thereof: wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.
Type:
Application
Filed:
August 3, 2010
Publication date:
December 16, 2010
Applicant:
AstraZeneca AB
Inventors:
Alan Martin BIRCH, Suzanne Saxon Bowker, Roger John Butlin, Craig Samuel Donald, William Mccoull, Thorsten Nowak, Alleyn Plowright
Abstract: Provided herein are 2,3-dihydro-1H-indene compounds, methods for making the compounds, pharmaceutical compositions containing the compounds. The described compounds inhibit IAP proteins and can be used to treat various cancers.
Type:
Application
Filed:
June 8, 2010
Publication date:
December 16, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Brian Aquila, Edward Hennessy, Alexander Hird, Vibha Oza, Jamal Carlos Saeh, Li Sha
Abstract: The present invention is directed to the use of (3-Amino-2-fluoropropyl)phosphinic acid or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, for the treatment or prevention of non-erosive reflux disease (NERD).
Type:
Application
Filed:
July 24, 2008
Publication date:
December 16, 2010
Applicant:
ASTRAZENECA AB
Inventors:
Goran Hasselgren, Anders Lehmann, Hans Rydholm