Abstract: The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same.
Type:
Grant
Filed:
November 13, 2002
Date of Patent:
February 20, 2007
Assignee:
Glaxo Group Limited
Inventors:
Alan David Borthwick, Matthew Campbell, Chuen Chan, Henry Anderson Kelly, Nigel Paul King, Savvas Kleanthous, Andrew McMurtrie Mason, Stefan Senger, Paul William Smith, Nigel Stephen Watson, Robert John Young
Abstract: The present invention includes novel retinoid compounds that have selectivity as RXR agonists on one or more isoforms of RXR, currently, RXR?, RXR?, or RXR?. The present compounds, and pharmaceutical compositions incorporating these compounds, therefore, are effective in treating conditions mediated by RXRs. Among other physiological responses, the compounds of the present invention reduce blood glucose and maintain body weight, and, thus, are useful for the treatment of diabetes (NIDDIM) and obesity.
Abstract: The present invention includes a method for preparing cyclic alcohols. The method includes a reduction, deprotection, and rearrangement scheme. The present invention further provides a method of preparation of an intermediate useful in the synthesis of compounds that function as inhibitors of the aspartyl protease enzyme of human immunodeficiency virus (HIV).
Type:
Grant
Filed:
September 16, 2002
Date of Patent:
December 5, 2006
Assignee:
SmithKline Beecham Corporation
Inventors:
Brian Daniel Doan, Roman D Davis, Thomas Claiborne Lovelace
Abstract: The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility.
Type:
Grant
Filed:
June 26, 2002
Date of Patent:
November 7, 2006
Assignee:
SmithKlineBeecham Corporation
Inventors:
Curt Dale Haffner, Darryl Lynn McDougald, Amarjit Sab Randhawa, Steven Michael Reister, James Martin Lenhard
Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
Type:
Grant
Filed:
June 6, 2002
Date of Patent:
August 1, 2006
Assignee:
SmithKline Beecham Corporation
Inventors:
Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
Abstract: Disclosed is a method for the treatment of diabetes mellitus, especially Type 2 diabetes and conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a dipeptidyl peptidase IV inhibitor and another antidiabetic agent, to a mammal in need thereof.
Type:
Grant
Filed:
June 19, 2001
Date of Patent:
July 18, 2006
Assignee:
SmithKline Beecham Corporation
Inventors:
Jonathan Robert Sanders Arch, James Martin Lenhard
Abstract: The present invention disclosed compounds of Formula I. The present invention also discloses beta-3 agonists of formula I and methods for treating beta-3 mediated diseases and condition using the compounds of formula I, in particular methods for treating diabetes or obesity.
Type:
Grant
Filed:
December 17, 2001
Date of Patent:
April 25, 2006
Assignee:
SmithKline Beecham Corporation
Inventors:
David N. Deaton, Barry George Shearer, David Edward Uehling
Abstract: The present invention relates to certain novel pyrimidine intermediates and their salts, processes for their preparation and processes for their conversion to 9-substituted-2-aminopurines which are useful in medical therapy.
Type:
Grant
Filed:
June 27, 2002
Date of Patent:
March 22, 2005
Assignee:
SmithKline Beecham Corporation
Inventors:
Susan Mary Daluge, Michelle Joanne Fugett, Michael Tolar Martin
Abstract: An improved process for preparing steriods, such as 3-oxo-4-azasteroids, is described. Compounds of this type are known to be useful in the preparation of compounds having 5a-reductase inhibitor activity. The process comprises the hydrogenation of the corresponding steroid alkene in the presence of ammonium acetate, ammonium formate, and/or ammonium propionate and an appropriate catalyst.
Type:
Grant
Filed:
May 5, 2003
Date of Patent:
September 21, 2004
Assignee:
SmithKline Beecham Corporation
Inventors:
Roman Davis, Alan Millar, Jeffrey Thomas Sterbenz
Abstract: A method for the treatment of conditions associated with a need for inhibition of GSK-3, such as diabetes, dementias such as Alzheimer's disease and manic depression which method comprises the administration of a pharmaceutically effective, non-toxic amount of a compound of formula (I):
or a pharmaceutically acceptable derivative thereof, wherein:
R is hydrogen, alkyl, aryl, or aralkyl;
R1 is hydrogen, alkyl, aralkyl, hydroxyalkyl or alkoxyalkyl;
R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl;
R3 is hydrogen, substituted or unsubstituted alkyl, cycloalkyl, alkoxyalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl or aralkyl wherein the aryl moiety is substituted or unsubstituted; or,
R1 and R3 together with the nitrogen to which they are attached form a single or fused, optionally substituted, saturated or unsaturated heterocylic ring;
to a human or non-human mammal in need thereof, and compounds of formula I.
Type:
Grant
Filed:
May 28, 2003
Date of Patent:
April 13, 2004
Assignee:
SmithKline Beecham Corporation
Inventors:
Matthew Paul Coghlan, Ashley Edward Fenwick, David Haigh, Julie Caroline Holder, Robert John Ife, Alastair David Reith, David Glynn Smith, Robert William Ward
Abstract: The present invention relates to a process for the preparation of a carbocyclic purine nucleoside analogue of formula (I), its salts and pharmaceutically acceptable derivatives thereof which comprises hydrolysing a compound of formula (IV) wherein P is a protecting group, in the presence of an acid, condensing the product of formula (V) formed in situ in the presence of a base with a compound of formula (VI) followed by in situ ring closure of the resulting intermediate.
Type:
Grant
Filed:
April 25, 2000
Date of Patent:
November 11, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Martin Francis Jones, Christopher John Wallis
Abstract: The present invention relates to pharmaceutical compostions of (1S,4R)-cis-4-[2-amino-6-cyclopropylamino}-9H-purin-9-yl]-2-cyclopentene-1-methanol (1592U89).
Abstract: The present invention is a process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof:
that includes preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof:
Abstract: A compound of formula (VI)
A process for the preparation of a compound of formula (VI):
comprising:
reacting a compound of formula (III):
with an amine of formula R3NH2.
Type:
Grant
Filed:
July 31, 1996
Date of Patent:
September 10, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Susan Mary Daluge, Michael Tolar Martin
Abstract: The present invention relates to a process for the preparation of enantiomerically enriched N-derivatized (1R,4S)-2-azabicyclo[2.2.1]hept-5-en-3-ones by use of an enzyme.
Type:
Grant
Filed:
February 14, 2000
Date of Patent:
January 22, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Michael John Dawson, Mahmoud Mahmoudian, Christopher John Wallis
Abstract: The hemisulfate salt of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol or a solvate of it is used in the treatment of viral infections.
Type:
Grant
Filed:
December 1, 1999
Date of Patent:
September 25, 2001
Assignee:
Glaxo Wellcome Inc.
Inventors:
Alastair Couper Brodie, Martin Francis Jones, John Frederick Seager, Christopher John Wallis