Abstract: The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation, allergy and/or autoimmune conditions.
Type:
Grant
Filed:
June 11, 2007
Date of Patent:
August 21, 2012
Assignee:
Glaxo Group Limited
Inventors:
Heather Anne Barnett, Ian Baxter Campbell, Diane Mary Coe, Anthony William James Cooper, Graham George Adam Inglis, Haydn Terence Jones, Steven Philip Keeling, Simon John Fawcett MacDonald, Iain McFarlane McLay, Philip Alan Skone, Gordon Gad Weingarten, James Michael Woolven
Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament, particularly for the treatment of inflammation and/or allergic conditions.
Type:
Grant
Filed:
April 18, 2007
Date of Patent:
May 15, 2012
Assignee:
Glaxo Group Limited
Inventors:
Keith Biggadike, Anthony William James Cooper, David House, Iain McFarlane McLay, Grahame Robert Woollam
Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Type:
Grant
Filed:
March 20, 2008
Date of Patent:
December 6, 2011
Assignee:
GlaxoSmithKline LLC
Inventors:
Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Type:
Grant
Filed:
October 31, 2007
Date of Patent:
November 22, 2011
Assignee:
GlaxoSmithKline, LLC
Inventors:
Jeffrey K. Kerns, Qi Jin, Michael Lindenmuth, Sonia M Thomas, Katherine L. Widdowson
Abstract: The invention provides N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo [3,4-b]pyridin-5-yl]methyl}-4-({8-[(2-hydroxyethyl) (methyl)amino]octanoyl}amino)benzamide, whose formula is or a salt thereof, such as the monohydrochloride salt thereof. The invention also provides the use of the compound or salt as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, or rhinitis (e.g. allergic and/or non-allergic rhinitis).
Type:
Grant
Filed:
July 31, 2007
Date of Patent:
August 23, 2011
Assignee:
Glaxo Group Limited
Inventors:
David George Allen, Rodger Phillip Barnett, Reshma Manesh Chudasama, Caroline Jane Day, Christopher David Edlin, Leanda Jane Kindon
Abstract: Compounds of formula (I) or a salt thereof are disclosed: wherein R1 is pyrazolyl substituted by two or three substituents independently selected from halogen, C1-4alkyl and haloC1-4alkyl; R2 is hydrogen or methyl; and R3 is quinolinyl, oxazolyl or phenyl, each of which is optionally substituted by one or two halogen, C1-4alkyl or haloC1-4alkyl. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.