Abstract: The present invention relates to compounds of Formula (I): pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metalloproteinase enzymes (MMPs).
Type:
Grant
Filed:
September 1, 2009
Date of Patent:
January 1, 2013
Assignee:
Glaxo Group Limited
Inventors:
Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
Abstract: Compounds of formula (I) and salts thereof are provided: wherein R4, R5, R6, Q, A, and Y are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
Type:
Grant
Filed:
September 18, 2008
Date of Patent:
January 1, 2013
Assignee:
Glaxo Group Limited
Inventors:
David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Paul Adrian Wyman
Abstract: A dry powder pharmaceutical composition comprising (i) a medicament particle fraction comprising medicament particles with an aerodynamic diameter no greater than 10 ?m; and (ii) at least 50% of a non-respirable excipient fraction comprising low density excipient particles with an aerodynamic diameter greater than 10 ?m and a geometric diameter greater than 30 ?m. In additional embodiments of the invention, the pharmaceutical composition includes a respirable excipient fraction comprising excipient particles with an aerodynamic diameter no greater than 10 ?m. In a preferred embodiment of the invention, the non-respirable excipient particles include pores adapted to receive a portion of the respirable excipient fraction and/or the medicament fraction.
Type:
Grant
Filed:
September 16, 2002
Date of Patent:
December 25, 2012
Assignee:
Glaxo Group Limited
Inventors:
Andrew Bruce Brown, Michael Mary Van Oort
Abstract: A fault indicator for a strip advancement mechanism comprising a base that defines a fault sensing portion of a path for at least a component of a strip, an element for bearing against a strip, or a component of the strip, while it passes through the fault sensing portion of the path, wherein the element is adapted to move from that bearing or non-fault position, to a fault indicating position in the event of the strip or the component of the strip ceasing to pass through the fault sensing portion of the path.
Type:
Grant
Filed:
May 12, 2006
Date of Patent:
December 25, 2012
Assignee:
Glaxo Group Limited
Inventors:
Gregor John McLennan Anderson, Stephen James Harvey, Andrew Roderick Taylor, Daniel Thomas De Sausmarez Lintell, Mark Digby Teucher, James Anthony West
Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
Type:
Grant
Filed:
April 29, 2009
Date of Patent:
December 11, 2012
Assignee:
Glaxo Group Limited
Inventors:
Thomas Daniel Heightman, John Skidmore, Hailong Wang, Colin David Eldred, Jag Paul Heer
Abstract: The present invention provides compounds of formula (I) or salts thereof: having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated by S1P1 receptors.
Type:
Grant
Filed:
April 17, 2008
Date of Patent:
December 4, 2012
Assignee:
Glaxo Group Limited
Inventors:
Mahmood Ahmed, Gerard Martin Paul Giblin, James Myatt, David Norton, Dean Andrew Rivers
Abstract: Compounds of Formula (I), wherein substituents R1, R2 and R5 are as defined, and Ar represents substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, furanyl, imidazolyl and thiophenyl substituted by a hydroxyalkyl substituent and an optional other substituent; compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
Type:
Grant
Filed:
January 15, 2010
Date of Patent:
November 27, 2012
Assignee:
Glaxo Group Limited
Inventors:
Carlos Alemparte-Gallardo, David Barros-Aguirre, Monica Cacho-Izquierdo, Jose Maria Fiandor Roman, Jose Luis Lavandera Diaz, Modesto Jesús Remuiñan-Blanco
Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, R4, R5, m, n and X are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
Type:
Grant
Filed:
December 12, 2007
Date of Patent:
November 20, 2012
Assignee:
Glaxo Group Limited
Inventors:
Alessandra Gaiba, Mark Patrick Healy, Christopher Norbert Johnson, Susan Roomans, Steven James Stanway, Martin Edward Swarbrick
Abstract: The present invention relates to an oral dosage form comprising N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine) or a pharmaceutically acceptable salt or solvate thereof, to a process for preparing such a dosage form and to the use of such a dosage form in medicine.
Abstract: The invention relates to anhydrous crystalline orvepitant maleate (Form 1), pharmaceutical formulations comprising the same, its use in therapy and processes for preparing the same, wherein orvepitant is as shown in formula (I).
Type:
Grant
Filed:
April 9, 2009
Date of Patent:
November 13, 2012
Assignee:
Glaxo Group Limited
Inventors:
Stefania Beato, Franco Sartor, Ian Philip Steeples
Abstract: A novel process for preparing a compound of formula (I) which comprises converting a compound of formula (II) to a compound of formula (I) via a compound of formula (III), or a salt thereof, without isolating any intermediates.
Type:
Grant
Filed:
June 13, 2007
Date of Patent:
November 13, 2012
Assignee:
Glaxo Group Limited
Inventors:
Malcolm Brian Berry, Mark Jason Hughes, David Parry-Jones, Stephen John Skittrall
Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.
Type:
Grant
Filed:
February 24, 2010
Date of Patent:
November 6, 2012
Assignee:
Glaxo Group Limited
Inventors:
Simon Teanby Hodgson, Yannick Maurice Lacroix, Pauayiotis Alexandron Procopiou
Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
Type:
Grant
Filed:
September 18, 2008
Date of Patent:
October 30, 2012
Assignee:
Glaxo Group Limited
Inventors:
David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
Abstract: A compound of formula (I) or salts thereof, wherein R1, R2, R3, R4, n and X are as defined in the specification; a process for preparing such compounds, a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
Type:
Grant
Filed:
October 30, 2008
Date of Patent:
October 23, 2012
Assignee:
Glaxo Group Limited
Inventors:
Alessandra Gaiba, Susan Roomans, Martin Edward Swarbrick
Abstract: Compounds of formula (I) and salts are provided: wherein R6 is selected from hydrogen, halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano, and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
October 16, 2012
Assignee:
Glaxo Group Limited
Inventors:
Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
Abstract: Compounds of formula (I) and salts are provided: wherein R5 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; R6 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
October 16, 2012
Assignee:
Glaxo Group Limited
Inventors:
Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
Abstract: The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}piperazine or a pharmaceutically acceptable salt thereof, in particular the hydrochloride salt thereof and crystalline forms of the hydrochloride salt; to processes for the preparation of the compound or its salt; to compositions containing it; and to its use in the treatment or prophylaxis of neurological or psychiatric diseases, such as cognitive impairment, fatigue or a sleep disorder, for example in a mammal such as a human. The compound or a salt thereof has affinity for and is an antagonist and/or inverse agonist of the histamine H3 receptor.
Type:
Grant
Filed:
September 4, 2008
Date of Patent:
October 16, 2012
Assignee:
Glaxo Group Limited
Inventors:
Desmond John Best, Sing Yeung Mak, Barry Sidney Orlek, Geracimos Rassias, Pamela Joan Theobald