Abstract: Compound of formula (I) or a pharmaceutically-acceptable salt thereof, formula (I) wherein Ar is optionally substituted phenyl; R1 is selected from: formula a) or b) (wherein is a single or double bond); R5, R6, R7 and R8 are for or alkyl; R4 is selected from hydrogen, (3-4C)cycloalkyl and optionally substituted (1-4C)alkyl; R10 is for example selected from hydrogen, (1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, hydroxy(1-4C)alkyl, (1-4C)alkoxy, aryl(1-4C)alkyl; Y is carbon and Ring A is optionally substituted phenylene; or each Y may independently be carbon or nitrogen and Ring A is optionally substituted 5- or 6-membered, heteroarylene ring; R11 is selected from hydrogen and optionally substituted phenyl; p is independently at each occurrence 0, 1 or 2; are described. Processes for making such compounds and their use as DPP-IV inhibitors in the treatment of diabetes are also described.
Type:
Application
Filed:
June 14, 2005
Publication date:
January 10, 2008
Applicant:
ASTRAZENECA AB
Inventors:
Alan Birch, Paul Kemmitt, Nathaniel Martin, Richard Ward
Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I), wherein: R1, R2, R4, R5, R6, R6a, R7, R8, A and B are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.
Abstract: An oral solid pharmaceutical dosage form comprising an acid sensitive proton pump inhibitor (PPI) as single active drug, releasing the PPI in two separate pulses, one immediate and one delayed. The PPI is formulated into a core material in the form of tablets, which are coated i.a. with a combination of a delay release modifying layer and a lag time controlling layer that together achieves beneficial release properties. The tablets are further provided with an enteric coating layer. The application also relates to processes for preparing the dosage forms as well as their use in the treatment of gastrointestinal diseases.
Type:
Application
Filed:
November 2, 2005
Publication date:
January 3, 2008
Applicant:
ASTRAZENECA AB
Inventors:
Niclas Clemmensen, Jan-Erik Lofroth, Henrik Sahlen, Katrin Walter, Peter Wang, Martin Wikberg
Abstract: The present invention relates to an isolated nucleic acid molecule comprising a nucleotide sequence that encodes an acetyl CoA carboxylase 2 (ACC2) splice variant. It also relates the corresponding polypeptide encoded by said nucleic acid and to methods of identifying a compound potentially useful for treating diseases or disorders associated with impaired ability to oxidise fatty acids, which comprises assaying the compound for its ability to modulate the activity or amount of a ACC2 splice variant complex or a complex thereof.
Type:
Application
Filed:
July 6, 2005
Publication date:
January 3, 2008
Applicant:
ASTRAZENECA AB
Inventors:
John Clapham, Brit Corneliussen, Stefan Hallen
Abstract: The invention provides compounds of formula (I): wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
Type:
Application
Filed:
July 4, 2005
Publication date:
January 3, 2008
Applicant:
AstraZeneca AB
Inventors:
Balint Gabos, Lena Ripa, Kristian Stenvall
Abstract: The invention provides medicaments comprising combinations of bronchodilators, glucocorticosteroids and HMG-CoA reductase inhibitors in the treatment of respiratory disorders such as chronic obstructive pulmonary disease (COPD).
Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: Formula (I) wherein R1, R2, R3 and R8 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: 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.
Abstract: Compounds of Formula I, wherein R2 represents C1-6 alkyl (optionally substituted by one or more substituents selected from —OH, halo, cyano, nitro and aryl) or aryl, wherein each aryl and aryloxy group, unless otherwise specified, is optionally substituted, and methods of preparation thereof are disclosed
Abstract: A process for preparing a dibenzothiazepine derivative such as dibenzo[b,f][1,4]thiazepin-11-one employable as a starting material for the preparation of 11-[4-(2-(2-hydroxyethoxy)ethyl)]-1-piperadinyldibenzothiazepine derivative which is known to be effective as an antipsychotic pharmaceutical, has the steps of reacting a nitrobenzene derivative with a thiosalicylic acid derivative, reducing the obtained 2-nitro-2?-carboxy-diphenylsulfide derivative, and subjecting the obtained 2-amino-2?-carboxy-diphenylsulfide derivative to dehydration-condensation reaction.
Abstract: The present invention provides methods for screening for compounds that modulate, e.g. inhibit, the activity of topoisomerases such as DNA gyrase, comprising providing cells expressing topoisomerase and containing a promoter sensitive to changes in DNA topology having a reporter gene operatively linked thereto, and measuring the expression of said reporter gene in the presence and in the absence of a test compound. Compounds that modulate the activity of topoisomerase can be identified by virtue of an alteration in reporter gene expression.
Type:
Application
Filed:
March 30, 2004
Publication date:
December 27, 2007
Applicant:
AstraZeneca AB
Inventors:
Beth Andrews, Scott Mills, Maria Uria-Nickelsen, Wei Yang, Peter Barth
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: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
Type:
Grant
Filed:
December 9, 2003
Date of Patent:
December 25, 2007
Assignee:
AstraZeneca Canada Inc.
Inventors:
Daniel Delorme, Edward Roberts, Zhongyong Wei
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.
Abstract: The invention provides new forms of a chemical compound of formula (I). The invention relates to forms fo a chemical compound (I), in particular to crystalline and amorphous forms, more particularly four crystalline forms and an amorphous form. The invention further relates to processes for the preparation of such forms, to pharmaceutical compositions comprising the compound in crystalline and/or amorphous form and to therapeutic use of such forms.
Type:
Application
Filed:
August 24, 2007
Publication date:
December 20, 2007
Applicant:
AstraZeneca AB
Inventors:
Martin Bohlin, Steve Cosgrove, Bo Lassen
Abstract: The present invention relates to new compounds of formula I, to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
Type:
Application
Filed:
August 18, 2007
Publication date:
December 20, 2007
Applicants:
AstraZeneca AB, NPS PHARMACEUTICALS INC.
Inventors:
Louise Edwards, Methvin Isaac, Martin Johansson, Annika Kers, Johan Malmberg, Donald McLeod, Alexander Mindis, Karin Staaf, Abdelmalik Slassi, Tomislav Stefanac, Thomas Stormann, David Wensbo, Tao Xin, Jalaj Arora
Abstract: A compound of formula (I) wherein T represents O, S or NR and wherein R represents a H, a C1-6alkyl group or a phenyl C1-6alkyl group and pharmaceutically acceptable salts thereof, processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and and pharmaceutical compositions containing them