Abstract: Compounds having the general formula and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection.
Type:
Grant
Filed:
June 28, 2002
Date of Patent:
October 23, 2007
Assignee:
AstraZeneca AB
Inventors:
Gregory Basarab, Joseph Eyermann, Madhusudhan Gowravaram, Oluyinka Green, Lawrence MacPherson, Marshall Morningstar, Thanh Nguyen
Abstract: The invention provides novel yeast promoters useful for controlling the expression of homologous and heterologous nucleic acid molecules in yeast cells. The yeast promoters are induced by a fermentable carbon source, such as glucose, or a non-fermentable carbon source, such as ethanol, or both. Therefore, expression of nucleic acid molecules encoding a polypeptide under the control of the novel yeast promoters may be regulated by varying the level of a fermentable carbon source, or a non-fermentable carbon source, or both.
Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.
Type:
Grant
Filed:
April 18, 2005
Date of Patent:
October 23, 2007
Assignee:
AstraZeneca AB
Inventors:
Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
Abstract: Acetylcholine receptor ligands of formula I wherein D, E and G 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:
December 20, 2004
Publication date:
October 18, 2007
Applicant:
AstraZeneca AB
Inventors:
Glen Ernst, William Frietze, Robert Jacobs, Eifion Phillips
Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility in medicine in general and especially as P2Y12 inhibitors and as anti-thrombotic agents, etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3 and R4 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.
Type:
Application
Filed:
April 16, 2007
Publication date:
October 18, 2007
Applicant:
ASTRAZENECA AB
Inventors:
William Brown, Ziping Liu, Daniel Page, Zena Qadoumi, Sanjay Srivastava, Maxime Tremblay, Christopher Walpole, Zhong-yong Wei, Hua Yang
Abstract: The present invention concerns a process for preparing 4-(hydroxy)-[1,4?]bipiperidinyl-1?-carboxylic acid tert-butyl ester, comprising hydrogenating a mixture of 4-hydroxypiperidine and 1-tert-butoxycarbonyl-4-piperidone in a suitable solvent, in the presence of a suitable catalyst and at a suitable pressure.
Abstract: Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof, possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.
Type:
Grant
Filed:
August 8, 2006
Date of Patent:
October 2, 2007
Assignee:
AstraZeneca AB
Inventors:
Alan Martin Birch, Andrew David Morley, Andrew Stocker, Paul Robert Owen Whittamore
Abstract: The invention relates to a stable medicament for oral administration which comprises (a) a core which contains an active ingredient selected from Omeprazole, Lansoprazole and Pantoprazole, together with customary pharmaceutical adjuvants, (b) an intermediate layer applied onto the core, and (c) a gastric juice-resistant outer layer. The intermediate layer in (b) is formed as a reactive layer in which a gastric juice-resistant polymer layer material partially neutralized with alkali with cation exchange capacity is present. Further, a method for the production of the stable medicament is disclosed.
Type:
Grant
Filed:
August 11, 2006
Date of Patent:
October 2, 2007
Assignee:
AstraZeneca AB
Inventors:
Gerd-Ulfert Heese, Herbert Jünger, Arnim Laicher, Claudio Lorck, Thomas Profitlich, Gerd Weiss
Abstract: A compound of formula I wherein R1 represents chloro, fluoro or hydroxy as well as optical isomers and racemates thereof as well as pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, processes for preparing such compounds, their utility in treating clinical conditions associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 18, 2002
Date of Patent:
October 2, 2007
Assignee:
AstraZeneca AB
Inventors:
Eva-Lotte Alstermark Lindstedt, Anna Maria Persdotter Boije, Patrick Holm
Abstract: There are provided novel compounds of formula (I) wherein A, R1, R3, R4, R5, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory diseases, pain and CNS diseases.
Abstract: The present invention relates to a method for analysing the amount of free gas within a pharmaceutical sample. According to the invention the method comprises the following steps: providing a sample before an irradiating source; irradiating the sample with at least one beam of electromagnetic radiation; detecting radiation emitted through the sample and generating signals corresponding to the amount of free gas in the sample, and correlating the generated signals to at least one solid state parameter of the sample.
Type:
Grant
Filed:
March 12, 2003
Date of Patent:
October 2, 2007
Assignee:
AstraZeneca AB
Inventors:
Christoffer Abrahamson, Stefan Andersson-Engels, Staffan Folestad, Jonas Johansson, Mikael Sjöholm, Gabriel Somesfalean, Sune Svanberg
Abstract: A salt of the compound N-{2-tert-butyl-1-[(4,4-difluorocyclohexyl)methyl]-1H-benzimidazol-5-yl}ethanesulfonamide, which is an ethanesulphonic acid salt, a sulphuric acid salt, an ethane disulphonic acid salt, a hydrochloric acid salt, a hydrobromic acid salt, a phosphoric acid salt, an acetic acid salt, a fumaric acid salt, a maleic acid salt, a tartaric acid salt, a citric acid salt, a methanesulphonic acid salt, or a p-toluenesulphonic acid salt of said compound.
Abstract: There is provided pharmaceutically-acceptable acid addition salts of compounds of formula I, wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents C1-2 alkyl; and n represents 0, 1 or 2, which salts are useful as prodrugs of competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
Type:
Grant
Filed:
May 27, 2003
Date of Patent:
September 25, 2007
Assignee:
AstraZeneca AB
Inventors:
Matti Ahlqvist, Martin Bohlin, Tord Inghardt, Anita Lundblad, Carl-Gustaf Sigfridsson
Abstract: Provided herein are novel processes for the preparation of intermediates that may be useful in the preparation of 5-Ht1b receptor antagonist useful in the treatment of depression, anxiety and other related diseases. The present processes may offer improved yields, purity, ease of preparation and isolation of intermediates and final product and more industrially useful reaction conditions and workability.
Type:
Application
Filed:
March 22, 2005
Publication date:
September 20, 2007
Applicant:
AstraZeneca AB
Inventors:
Mouloud Dekhane, Alison Norton, Anne O'Kearney-McMullan, Graham Robinson
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 cycloalkyl; the process comprising either: a. hydrogenating a compound of formula (II): with a suitable transition metal catalyst in a C1-6 aliphatic alcohol, an ether, an ester or a hydrocarbon as solvent; or, b. 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; i. firstly at about 20° C. to form a compound of formula (IV): ii. 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: 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: An inhaler for delivery by inhalation of a medicament from the canister which is compressible to deliver a dose of medicament. The inhaler comprises a housing (1) for holding a canister (2) having a generally cylindrical body (3) with the cylindrical axis of the body (3) in predetermined direction and a loading mechanism for loading a resilient loading element (7) which is arranged, when loaded, to bias compression of the canister (2). The loading mechanism comprises a loading member (8) engaging the resilient loading element (7) and two contact members (9) movable relative to the housing (1) in a movement direction orthogonal to said predetermined direction and arranged to drive the loading member (8) to load the resilient loading element (7), through a cam arrangement between the contact member (8).
Abstract: The present invention is directed to assays that can be used to screen for compounds that act as agonists or antagonists or inverse agonists of bovine adrenal medulla docosapeptide (BAM-22P). The assays are based upon the binding of BAM-22P to the rat and human DRR receptors.
Type:
Grant
Filed:
October 16, 2001
Date of Patent:
September 18, 2007
Assignee:
AstraZeneca AB
Inventors:
Sultan Ahmad, Eric Grazzini, Thierry Groblewski, Paolo Lembo, Ralf Schmidt
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.