Abstract: This invention relates to a method for the prophylaxis of or for treating COPD by administering a PDE4 inhibitor which has a defined therapeutic ratio.
Type:
Grant
Filed:
August 31, 2001
Date of Patent:
December 30, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Mary S. Barnette, Theodore J. Torphy
Abstract: Herein is provided a process for preparing substituted cyclohexanoic acids of formula (I), where Ra is a carbon-containing group optionally linked by oxygen, sulfur or nitrogen to the phenyl ring and j is 1-5; and one of R and R* is hydrogen and the other is C(O)OH.
Abstract: Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis,
in which:
R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH;
R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system;
R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system;
W is SO2 or a bond;
X is O or S; and
Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).
Type:
Grant
Filed:
February 21, 2001
Date of Patent:
May 6, 2003
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Colin Andrew Leach, Stephen Allan Smith
Abstract: This invention relates to treating pulmonary diseases such as chronic obstructive pulmonary disease or asthma by administering a phosphodiesterase 4 inhibitor in combination with beta adrenergic bronchodilator.
Type:
Grant
Filed:
August 20, 2001
Date of Patent:
April 29, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Richard Nieman, Anthony S Rebuck, Theodore J Torphy
Abstract: A combined laboratory condenser and vessel connector having a conduit with an inlet/outlet adjacent its upper end with a condenser jacket around the lower part of the conduit, an upper part of the jacket formed into or provided with a connector to enable the apparatus to be mated with a vessel with at least part of the jacket extending into the vessel. The device is useful in chemical laboratory operations.
Type:
Grant
Filed:
April 24, 2000
Date of Patent:
February 18, 2003
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Brian Henry Furlong, Clive Adrian Smith
Abstract: A laboratory vessel comprising two substantially cylindrical chambers with parallel longitudinal axes between their bottom and mouth openings and lower and upper conduits linking the chambers so that he contents of the vessel can flow between the first and second chambers via the upper and lower conduits. The vessel is particularly suited for use with automated reactor systems.
Type:
Grant
Filed:
March 7, 2000
Date of Patent:
December 10, 2002
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Gillian Elizabeth Smith, Kenneth Thomas Veal
Abstract: This invention relates to a method for preparing 1-oxaspiro[2,5]-carbonitriles from ketones using spinning disc reactor technology.
Type:
Grant
Filed:
February 22, 2002
Date of Patent:
November 19, 2002
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Clemens Michael Helmut Brechtelsbauer, Paul Oxley
Abstract: This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carboxyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and water.
Type:
Grant
Filed:
November 8, 2001
Date of Patent:
September 17, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Kevin Webb, Wilford Mendelson, Jianhao Chen
Abstract: This invention relates to a method for the prophylaxis of or reducing the severity of post-viral bacterial infection by administering a PDE 4-specific inhibitor prior to or during the course of a viral infection or thereafter during the course of the bacterial infection.
Type:
Grant
Filed:
February 8, 2001
Date of Patent:
August 20, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Peter L. DeMarsh, Susan B. Dillon, Gary Woodnutt
Abstract: The invention relates to compounds which are ligands for 5HT1, of formula (I)
Wherein L, Q, Ra, Rb and Ry are as defined in the specification, processes for their preparation and their pharmaceutical composition as well as their use in the treatment of anxiety and depression.
Type:
Grant
Filed:
January 26, 2000
Date of Patent:
May 21, 2002
Assignee:
SmithKline Beecham plc
Inventors:
Laramie Mary Gaster, Paul Adrian Wyman, Sean Thomas Flynn
Abstract: A method for treating COPD is disclosed comprising administering compounds of Formula (I)
wherein the terms R1, R3, X, X2 and Z are herein defined.
Type:
Grant
Filed:
June 28, 2000
Date of Patent:
April 9, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Theodore Torphy
Abstract: This invention relates to a method of preparing a compound of the following type
by treating a compound of formula (II)
with lithium bromide, magnesium bromide and the like.
Type:
Grant
Filed:
March 22, 2000
Date of Patent:
January 8, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Andrew Allen, Ann Marie Diederich, Li Liu, Wilford Mendelson, Kevin Webb
Abstract: Novel 3-cyano-3-(3,4-disubstituted)phenylcyclohexyl-1-carboxylates or derivatives thereof and their corresponding cyclohexenyl analogs are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. These compounds are also useful mediating or inhibiting the enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in treating diseases in need of mediation or inhibition thereof.
Type:
Grant
Filed:
January 30, 1996
Date of Patent:
October 9, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Siegfried B. Christensen, IV, Cornelia Jutta Forster