Abstract: This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvent thereof, which is an inhibitor of cysteine proteases, particularly cathespin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor
Type:
Grant
Filed:
May 6, 2002
Date of Patent:
June 24, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Robert Wells Marquis, Jr., Daniel Frank Veber
Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
Abstract: The present invention relates to adjuvant compositions which are suitable to be used in vaccines. In particular, the adjuvant compositions of the present invention comprises a saponin and an immunostimulatory oligonucleotide, preferably the saponins used in said adjuvant combinations are haemolytic. Also provided by the present invention are vaccines comprising the adjuvants of the present invention and an antigen. Further provided are methods of manufacture of the adjuvants and vaccines of the present invention and their use as medicaments.
Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected azo-pyrazole derivative.
Type:
Grant
Filed:
March 22, 2002
Date of Patent:
April 22, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Kevin J. Duffy, Nannan Liu, Juan I. Luengo
Abstract: The present invention is related to novel 2-alkyl substituted imidazoles of formula (I) useful for the treatment of CSBP kinase mediated diseases.
Type:
Grant
Filed:
March 3, 2001
Date of Patent:
April 15, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Jerry L. Adams, Susan B. Dillon, Sandra D. Griego, Dennis Lee
Abstract: The present invention is directed to novel pyridin-4-yl or pyrimidin-4-yl substituted pyrazine compounds and compositions for use in therapy.
Type:
Grant
Filed:
April 5, 2001
Date of Patent:
April 15, 2003
Assignee:
Smithkline Beecham Corporation
Inventors:
Jerry L. Adams, Ralph F. Hall, Jeffrey C. Boehm
Abstract: The present invention relates to adjuvant compositions which are suitable to be used in vaccines. In particular, the adjuvant compositions of the present invention comprises a saponin and an immunostimulatory oligonucleotide, optionally with a carrier. Also provided by the present invention are vaccines comprising the adjuvants of the present invention and an antigen. Further provided are methods of manufacture of the adjuvants and vaccines of the present invention and their use as medicaments. Methods of treating an individual susceptible to or suffering from a disease by the administration of the vaccines of the present invention are also provided.
Type:
Grant
Filed:
October 18, 2000
Date of Patent:
April 8, 2003
Assignee:
SmithKline Beecham Biologicals s.a.
Inventors:
Martin Friede, Nathalie Garcon, Catherine Marie Ghislaine Gerard, Philippe Hermand
Abstract: The present invention relates to pyrrolyl and pyridyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of urotensin II.
Type:
Grant
Filed:
June 13, 2002
Date of Patent:
April 8, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Dashyant Dhanak, Steven David Knight, Jian Jin, Richard McCulloch Keenan
Abstract: Syrup formulations comprising water and compacted granulates which are mixture of amoxycillin and clavulanic acid, together with an intra-granular disintegrant.
Type:
Grant
Filed:
November 19, 2001
Date of Patent:
April 8, 2003
Assignee:
Labratorios Beecham SA
Inventors:
Luis Carvajal Martin, Juan Dedios Romero
Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists as described.
Type:
Grant
Filed:
October 30, 2000
Date of Patent:
April 8, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Juan Ignacio Luengo, John Duncan Elliott, Jia-Ning Xiang
Abstract: This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.
Type:
Grant
Filed:
May 6, 2002
Date of Patent:
March 18, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Robert W. Marquis, Jr., Yu Ru, Daniel Frank Veber
Abstract: A method for the treatment of cerebrovascular disorders and/or disorders associated with cerebral senility and/or other disorders which method comprises the administration of an effective, non-toxic amount of a compound of formula (I):
or if appropriate a pharmaceutically acceptable salt thereof, wherein R1 and R2 each independently represent alkyl or a moiety of formula (a):
—(CH2)m−A (a)
wherein m represents zero or an integer 1, 2 or 3; A represents a substituted or unsubstituted cyclic hydrocarbon radical; and R3 represents a halogen atom, a nitro group, or a group −NR4R5 wherein R4 and R5 each independently represents hydrogen, alkyl or alkylcarbonyl or R4 and R5 together with the nitrogen to which they are attached forming an optionally substituted, heterocyclic group; certain novel compounds falling within formula (I) and compositions comprising such compounds.
Type:
Grant
Filed:
November 8, 2000
Date of Patent:
March 11, 2003
Assignee:
Beecham Group p.l.c.
Inventors:
Barbara Ann Spicer, Harry Smith, Harald Maschler
Abstract: This invention relates to the novel amino substituted pyrimidine compounds of Formulas (I), (II) and (III), and pharmaceutical compositions comprising a compound of these Formulas and a pharmaceutically acceptable diluent or carrier.
This invention also relates to a method of inhibiting CSBP kinase and cytokines mediated by this kinase, for the treatment of cytokine mediated diseases, in mammals, by administration of a compound of Formula (I), (II) or (III).
Type:
Grant
Filed:
June 26, 2000
Date of Patent:
March 4, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Timothy F. Gallagher, Susan M. Thompson
Abstract: Compounds of formula (I) wherein R1, R2, A, q are as defined herein, and salts thereof, have affinity for dopamine receptors, in particular the D3 receptor, and thus have potential in the treatment of conditions wherein modulation of the D3 receptor is beneficial, e.g. as antipsychotic agents.
Type:
Grant
Filed:
June 8, 2001
Date of Patent:
February 18, 2003
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Christopher Norbert Johnson, Geoffrey Stemp
Abstract: The present invention provides bis-aminomethyl carbonyl protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
Type:
Grant
Filed:
November 21, 2000
Date of Patent:
February 11, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
William Edward Bondinell, Renee Louise DesJarlais, Daniel Frank Veber, Dennis Shinji Yamashita
Abstract: The present invention is directed to a novel pharmaceutical composition of polymorph B which has been found to be stable and palatable for long term commercial usage.