Abstract: A compound of formula (I): namely (2S)-2-amino-4-{[2-(ethanimidoylamino)ethyl]thio}butanoic acid, compound with phosphoric acid, or a solvate or physiologically functional derivative thereof, is useful as a relatively non-hygroscopic selective inhibitor of inducible nitric oxide synthase.
Type:
Grant
Filed:
December 17, 2001
Date of Patent:
January 8, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
David Box, David Colclough, Iain Gillies, Michael Simon Loft, Rebecca Moore
Abstract: An improved process for preparing N6 -substituted aminopurine ribofuranose nucleosides. Compounds of this type are known to be usefull in the prepartation of compounds having activitity at adenosine receptors, e.g. Adenosine A1 receptor. The process comprises the step of reacting a 6-halopurine ribofuranose nucleoside with an amine in the presence of CaCO3 , wherein acid is added to the reaction mixture.
Type:
Grant
Filed:
March 19, 2002
Date of Patent:
November 20, 2007
Assignee:
Glaxo Group Limited
Inventors:
Malcolm Berry, John C. Roberts, Shiping Xie
Abstract: A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are provided
Type:
Grant
Filed:
October 15, 2002
Date of Patent:
October 23, 2007
Assignee:
SmithKline Beecham P.L.C.
Inventors:
Andrew J Carpenter, Joel P Cooper, Anthony L Handlon, Donald L Hertzog, Clifton E Hyman, Yu C Guo, Jason D Speake, David Richard Witty
Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
Type:
Grant
Filed:
December 12, 2003
Date of Patent:
September 18, 2007
Assignee:
SmithKline Beecham Corporation
Inventors:
Hanbiao Yang, Wieslaw Mieczyslaw Kazmierski, Christopher Joseph Aquino
Abstract: The present invention relates to novel hydroxyethylamine compounds having Asp2 (?-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
Type:
Grant
Filed:
December 3, 2003
Date of Patent:
August 7, 2007
Assignee:
Glaxo Group Limited
Inventors:
Emmanuel H Demont, Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Alan Naylor, Sally Redshaw, Steven James Stanway, David R Vesey, Daryl S Walter
Abstract: The present invention provides a compound of formula I comprising: a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof.
Type:
Grant
Filed:
June 30, 2005
Date of Patent:
January 30, 2007
Assignee:
SmithKline Beecham Corporation
Inventors:
Jerzy Ryszard Szewczyk, Kelly H. Donaldson
Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (?-secretase. BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
Type:
Grant
Filed:
November 29, 2002
Date of Patent:
January 9, 2007
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Andrew Faller, Peter Henry Milner, John Gerard Ward
Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation and use; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.
Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (?-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
Type:
Grant
Filed:
November 29, 2002
Date of Patent:
January 31, 2006
Assignee:
SmithKline Beecham P.L.C.
Inventors:
Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Steven James Stanway, Leontine Saskia Trouw
Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, methods for preparing them, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.
Type:
Grant
Filed:
May 17, 2002
Date of Patent:
February 15, 2005
Assignee:
SmithKline Beecham Corporation
Inventors:
Toby Broom, Monica Delpogetto, Richard Atkins, Alan Negus, Paul William Oxley
Abstract: The present invention relates to a process for the preparation of both the phenyl pyrazine derivative 2,6-diamino-3-(2,3,5-trichlorophenyl)pyrazine and an intermediate in the synthesis of 2,6-diamino-3-(2,3,5-trichlorophenyl)pyrazine, 2-{[Cyano-(2,3,5-trichlorophenyl)-methyl]-amino}-acetamidine or a salt thereof.
Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, addiction to cocaine or nicotine-containing (especially tobacco) products, or addiction to alcohol using such compound, salts, solvates or compositions.
Abstract:
A process for the preparation of the compound (I) or an acid addition salt thereof which comprises reacting a compound of formula (II), wherein R is an optionally substituted benzyl group under concomitant reduction and hydrogenolysis conditions, followed, if required, by isolation of the compound as an acid addition salt thereof.
Abstract: The invention relates to therapeutic benzamide compounds of formula (I)
wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present invention also provides pharmaceutical compositions, processes for the preparation of compounds of formula (I) and their use in the treatment of conditions mediated by ApoB-100 regulation.
Abstract: Methods of treatment and prevention of malarial infection caused by Plasmodium vivax, in which combinations of atovaquone, proguanil and primaquine are administered to a patient.
Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.
Type:
Grant
Filed:
June 22, 2001
Date of Patent:
May 21, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Phillip Frederick Morgan, David Lee Musso, John Joseph Partridge
Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholino and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.
Type:
Grant
Filed:
January 20, 1999
Date of Patent:
August 14, 2001
Assignee:
Glaxo Wellcome Inc.
Inventors:
Phillip Frederick Morgan, David Lee Musso, John Joseph Partridge
Abstract: A process for preparing an oil-in-water emulsion is provided, which process comprises mixing and heating a water-insoluble organomodified polysiloxane oil, an organomodified silicone emulsifier, water and an alkaline metal salt above the cloud point of the emulsifier under agitated conditions and cooling the resulting mixture below the cloud point.
Type:
Grant
Filed:
December 2, 1991
Date of Patent:
August 10, 1993
Assignee:
Union Carbide Chemicals & Plastics Technology Corporation
Inventors:
William C. Breneman, William C. Crane, Michael J. Walsh, Eric A. Warren
Abstract: Compositions are provided containing epoxysilanes and diphenylamine in an amount at least sufficient to inhibit degradation. Methods for producing such compositions are also provided.
Type:
Grant
Filed:
December 24, 1991
Date of Patent:
October 13, 1992
Assignee:
Union Carbide Chemicals & Plastics Technology Corporation