Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
Type:
Grant
Filed:
June 29, 1999
Date of Patent:
August 1, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Juan Ignacio Luengo, John Duncan Elliott
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:
September 14, 1998
Date of Patent:
August 1, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Timothy F. Gallagher, Susan M. Thompson
Abstract: The present invention relates to a new method of treatment using compounds which are dual non-selective beta-adrenoceptor and alpha-1-adrenoceptor antagonists, in particularly the carbazolyl-(4)-oxypropanolainine compounds of Formula 1, as defined herein, for inhibiting the expression of Fas, a cell surface protein.
Abstract: A process for preparing 2-amino-6-chloropurine or a 2-acylated derivative thereof, comprising reacting guanine or 2,9-diacylguanine with a chlorinating agent, in the presence of methyltriethylammonium chloride as phase transfer catalyst, and thereafter when necessary, removing the 9-acyl group by hydrolysis.
Abstract: Novel herpes viral protease crystalline structures are identified which have an active site formed by the three amino acids Ser, His and His. Also disclosed are methods of identifying inhibitors of these proteases and/or active sites.
Type:
Grant
Filed:
May 9, 1997
Date of Patent:
July 4, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Sherin Salaheldin Abdel-Meguid, Xiayang Qiu, Ward Whitlock Smith, Jr., Cheryl Ann Janson, Susan S. Hoog, Jeffrey Culp, Christine Marie Debouck
Abstract: The present invention provides method of increasing the biological activity of KC, gro-.alpha., gro-.beta., and gro-.gamma. proteins, truncated and modified proteins characterized by having biological activity at least 1 log better than the full-length protein, and pharmaceutical compositions containing same.
Type:
Grant
Filed:
March 5, 1996
Date of Patent:
June 27, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Louis Martin Pelus, Pradip Kumar Bhatnagar, Andrew Garrison King, Joanna Maria Balcarek
Abstract: The present invention is directed to a synthetic route for preparing endothelium receptor antagonists of formulae (7B) and (7A) and to the chiral intermediates ##STR1##
Type:
Grant
Filed:
May 8, 1998
Date of Patent:
June 27, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Robert John Mills, Conrad John Kowalski, Li-Jeng Ping, Kerry Joseph Gombatz
Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
Abstract: Novel compounds of the general formula (I) which have hemoregulatory activities and can be used to stimulate haematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases ##STR1##
Type:
Grant
Filed:
December 14, 1998
Date of Patent:
June 20, 2000
Assignees:
SmithKline Beecham Corporation, Nycomed Austria GmbH
Inventors:
Pradip Kumar Bhatnagar, Dirk Andries Heerding, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
Abstract: Novel compounds of the general formula (I) which have hemoregulatory activities and can be used to stimulate haematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
Type:
Grant
Filed:
December 4, 1998
Date of Patent:
June 20, 2000
Assignees:
SmithKline Beecham Corporation, Nycomed Austria GmbH
Inventors:
Pradip Kumar Bhatnagar, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
Abstract: A pharmaceutical formulation comprising an amoxycillin hydrate and an effervescent couple, for example citric acid plus sodium bicarbonate or sodium glycine carbonate, or tartaric acid or malic acid plus sodium carbonate. Potassium equivalents of these sodium salts may be used. The formulations may be free flowing powders or granules, or tablets.
Type:
Grant
Filed:
August 19, 1998
Date of Patent:
June 20, 2000
Assignee:
Beecham Group plc
Inventors:
David Roy Merrifield, Paul Laurence Carter, David George Doughty
Abstract: The present invention is to novel photochemically cleavable aryl sulfonamides of the formulaP--A.sub.3 --A.sub.2 --A.sub.1 --S(O).sub.2 NR.sub.1 R.sub.2whereinR.sub.1 and R.sub.2 are independently selected from optionally substituted alkyl, arylalkyl or heteroarylalkyl;A.sub.1 is an aryl or heteroaryl moiety;A.sub.2 is a linking agent is an aryl, heteroaryl, arylalkyl, heteroaryl alkyl, or an alkyl, wherein the alkyl moiety in the arylalkyl, heteroaryl alkyl, or alkyl group is optionally interrupted one or more times independently by oxygen, NR.sub.3, sulfur or an amide group;R.sub.3 is alkyl;A.sub.3 is an electron rich aryl or heteroaryl moiety having an E.sub.1/2 potential of 0.5 to 2.0 and which moiety is capable of forming an exciplex;P is a solid support.Another aspect of the present invention is to the novel use of these photolytically cleavable aryl sulfonamides in combinatorial chemistry synthesis, for use in non-sequential encoding, as a tagging agent.
Type:
Grant
Filed:
March 31, 1995
Date of Patent:
June 13, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Ravi Shunker Garigipati, Jerry Leroy Adams
Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
Type:
Grant
Filed:
January 11, 1996
Date of Patent:
May 30, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Fadia El-Fehail Ali, William Edward Bondinell, Raul Rolando Calvo, Thomas Wen-Fu Ku, William Henry Miller, James Samanen, Joseph Walter Venslavsky, Tobias Oregon Yellin
Abstract: DNA sequences obtained from S. clavuligerus ATCC 27064, recombinant vectors incorporating such sequences and hosts transformed with such vectors are disclosed. The DNA comprises one or more genes coding for one or more enzymes involved in the biosynthesis of penicillin and cephalosporin .beta.-lactams and such enzymes are expressed by hosts into which the recombinant vectors are transformed. The DNA and the enzymes encoded thereby have utility in the preparation of penicillins and cephalosporins, both known and novel, possessing pharmacological, especially antimicrobial, activity.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
May 23, 2000
Assignee:
Beecham Group plc
Inventors:
Martin Karl Russel Burnham, Ian David Normansell, John Edward Hodgson
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 use of a compound of formula (A) or a bioprecursor, or a pharmaceutically acceptable salt, phosphate ester and/or acyl derivative of either of the foregoing in the manufacture of a medicament for use in the treatment (including prophylaxis) of HHV-6 infection.
Type:
Grant
Filed:
July 29, 1997
Date of Patent:
May 2, 2000
Assignee:
SmithKline Beecham plc
Inventors:
Richard Anthony Vere Hodge, Malcolm Richard Boyd
Abstract: The present invention relates to novel compounds of the Formula I which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral fungal and bacterial infectious diseases.