Abstract: This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
Abstract: This invention relates to the compound of Formula I and pharmaceutically acceptable salts thereof: (R)-N*6*-ethyl-6,7-dihydro-5H-indeno[5,6-d]thiazole-2,6-diamine This invention also relates to methods of making, methods of using, and pharmaceutical compositions comprising the compound of Formula I and salts thereof.
Type:
Application
Filed:
February 19, 2009
Publication date:
August 27, 2009
Applicant:
ASTRAZENECA AB
Inventors:
William C. Blackwell, III, James Hulsizer, JianWei Liu, Gary Steelman, Rebecca Urbanek, Dan Widzowski, Ye Wu
Abstract: The invention provides quinazoline derivatives of formula (I): in the preparation of a medicament for use in the inhibition of Aurora kinase and also novel quinazoline derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
May 28, 2008
Publication date:
August 27, 2009
Applicant:
AstraZeneca AB
Inventors:
Frederic Henri Jung, Georges Rene Pasquet
Abstract: A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.
Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof 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:
May 12, 2004
Date of Patent:
August 25, 2009
Assignee:
Astrazeneca AB
Inventors:
David William Heaton, Andrew Peter Thomas
Abstract: The invention provides pteridine compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. Formula (I) in which A is a group of formula (a) or (b).
Type:
Grant
Filed:
July 15, 2004
Date of Patent:
August 25, 2009
Assignee:
AstraZeneca
Inventors:
Roger Bonnert, Stewart Gardiner, Fraser Hunt, Iain Walters
Abstract: The present invention relates crystals of UMP kinase and computer-assisted methods for screening, identifying, and designing inhibitors and allosteric modulators of UMP kinase.
Type:
Application
Filed:
August 15, 2005
Publication date:
August 20, 2009
Applicant:
ASTRAZENECA AB
Inventors:
Jason Breed, Peter Doig, Charles J. Eyermann, Richard Pauptit, Julie Tucker
Abstract: The present invention provides compounds of formula (1) wherein R1, R2, R3 and R4 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:
November 20, 2008
Publication date:
August 20, 2009
Applicant:
AstraZeneca AB
Inventors:
Nicholas J. BENNETT, Thomas MCINALLY, Tobias MOCHEL, Stephen THOM, Anna-Karin TIDEN
Abstract: The present invention is directed to compounds of formula I: wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, R1, R2, R3, R4, and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
Type:
Grant
Filed:
February 18, 2005
Date of Patent:
August 18, 2009
Assignee:
Astrazeneca AB
Inventors:
David Wensbo, Martin Johansson, Alexander Minidis, Karin Staaf, Annika Kers, Louise Edwards, Methvin Isaac, Tom Stefanac, Abdelmalik Slassi, Don McLeod, Tao Xin
Abstract: The present invention relates to 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula IA and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Abstract: The present invention relates to a new use of a compound of the formula (I) wherein R1 is NH2, piperazin-1-yl, 4-methylpiperazin-1-yl,4-methyl-1,4-diazepan-1-yl or 4-ethylpiperazin-1-yl; R2 is hydrogen, fluoro, CH3, CH2CH3, OCH3, CF3 or OCF3; R3 is hydrogen, CH3 or fluoro; as a free base or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the prevention and/or treatment of bone-related disorders, osteoporosis and increasing bone formation, bone mineral density. The present invention further relates to a method of prevention and/or treatment of these disorders.
Abstract: The present invention relates to compounds that inhibit 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 compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.
Type:
Application
Filed:
February 7, 2007
Publication date:
August 13, 2009
Applicant:
AstraZeneca AB
Inventors:
Jean Claude Arnould, Benedicte Delouvrie, Jason Grant Kettle
Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4?, R5?, R6, R7, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
August 28, 2006
Publication date:
August 13, 2009
Applicant:
AstraZeneca AB
Inventors:
Andrew Bailey, Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
Abstract: Binding members, especially antibody molecules, for interleukin (IL)-4 receptor alpha (IL-4R?), and their therapeutic use e.g. in treating or preventing disorders associated with IL-4R?, IL-4 and/or IL-13, examples of which are asthma and COPD.
Type:
Application
Filed:
December 18, 2008
Publication date:
August 13, 2009
Applicant:
AstraZeneca AB
Inventors:
Per-Olof Fredrik Eriksson, Karin Von Wachenfeldt, Suzanne Cohen, Claire Louise Dobson, Deborah Louise Lane
Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.
Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.
Type:
Grant
Filed:
January 24, 2008
Date of Patent:
August 11, 2009
Assignee:
AstraZeneca AB
Inventors:
Alan D. Robertson, Shaun Jackson, Vijaya Kenche, Cindy Yaip, Hishani Parbaharan, Phil Thompson
Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 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:
January 13, 2004
Date of Patent:
August 11, 2009
Assignee:
AstraZeneca AB
Inventors:
Alan Wellington Faull, Craig Johnstone, Andrew David Morley, Jeffrey Philip Poyser
Abstract: The invention concerns quinazoline derivatives of the Formula (I); wherein each of R1, R2, W, X1, X2, Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula (I) are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.
Type:
Grant
Filed:
September 13, 2004
Date of Patent:
August 4, 2009
Assignee:
Astrazeneca AB
Inventors:
Laurent Francois Andre Hennequin, Christopher Thomas Halsall
Abstract: The invention relates to substituted phenylacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
Type:
Application
Filed:
October 5, 2006
Publication date:
July 30, 2009
Applicant:
ASTRAZENECA AB
Inventors:
Timothy Jon Luker, Rukhsana Tanseem Mohammed, Stephen Thom, Anil Patel
Abstract: There is provided the use of a low molecular weight thrombin inhibitor for the manufacture of a medicament for the treatment by dialysis, particularly haemodialysis, of a patient in need of such treatment, in which the thrombin inhibitor is provided in the dialysing solution, as well as dialysing solutions and concentrates including low molecular weight thrombin inhibitors, such as melagatran.