Abstract: The present invention relates to a method for synthesizing imidazole derivatives having 4-aryl, 5-pyrimidine heterocyclic rings using a cycloaddition reaction.
Abstract: Stable aqueous compositions of biologically active oils for the preparation of optically clear products for use in human or animal healthcare, for example beverages, are prepared.
Type:
Grant
Filed:
August 7, 1998
Date of Patent:
June 26, 2001
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Maarten Van Den Braak, Andrew Symonds, Michael Anthony Ford
Abstract: A process for preparing an enzyme from Penicillium chrysogenum having Phenylacetate-Coenzyme A activity. DNA encoding for the enzyme is also provided and its use in the production of modified strains.
Type:
Grant
Filed:
February 11, 1998
Date of Patent:
June 12, 2001
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Linden Gledhill, Philip Andrew Greaves, John Patrick Griffin
Abstract: A high speed agitation granulator method of preparing a substantially spherical granule for pharmaceutical use comprising a medicament for pharmaceutical use, wherein the medicament has an aqueous solubility of 0.01 to 0.30 g/ml, which method comprises introducing a mixture of medicament and excipients comprising at least 5% crystalline cellulose into the granulator and spraying on water or a mixture of ethanol and water as binder solution; a substantially spherical granule for pharmaceutical use comprising famciclovir and 5% or more crystalline cellulose, together with an optional coating; and a sachet containing a unit dose of famciclovir in the form of such granules.
Type:
Grant
Filed:
July 7, 1998
Date of Patent:
June 5, 2001
Assignee:
SmithKline Beecham Seiyaku K.K.
Inventors:
Hidero Akiyama, Zene Matsumoto, Takashi Ueno
Abstract: This invention relates to substituted bis-acridines and related compounds which are ligands, in particular, antagonists of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders, rheumatoid arthritis, atherosclerosis, psoriasis, auto immune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted bis-acridines and related compounds which are CCR5 receptor antagonists. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.
Type:
Grant
Filed:
July 2, 1999
Date of Patent:
June 5, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
William E. Bondinell, Valerie A. Reader, Thomas Wen Fu Ku
Abstract: The present invention relates to a novel method for synthesizing imidazole derivatives having 4-aryl, 5-pyrimidine heterocyclic rings using a novel cycloaddition reaction.
Abstract: A compound of formula (I) or a salt thereof:
wherein:
P1 is pyridiyl;
P2 is phenyl;
A is a bond or a chain of 1 to 5 atoms optionally substituted by C1-6 alkyl;
R1 and R2 groups are each independently hydrogen, C1-6alkyl optionally substituted by NR12R13, C2-6alkenyl, C2-6alkynyl, cyano, halogen, CF3, NR12R13, CHO, OCF3, COR14, CH2OR14 or OR14 where R12, R13 and R14 are independently hydrogen or C1-6alkyl;
n and m are independently 0, 1 or 2;
R3 is hydrogen or C1-6 alkyl;
R4 is a group of formula (i):
in which:
R6 and R7 are independently hydrogen, C1-6 alkyl optionally substituted by one or more fluorine atoms, C1-6alkylthio, C1-6alkoxy or halogen.
Type:
Grant
Filed:
July 23, 1999
Date of Patent:
May 22, 2001
Assignee:
SmithKline Beecham p.l.c.
Inventors:
Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies, David Malcolm Duckworth, Ian Thomson Forbes, Graham Elgin Jones
Abstract: The present invention is directed to the use of 2,4,5-trisubstituted imidazole compounds and compositions in the treatment of CNS injuries to the brain.
Abstract: Improved methods for the preparation of clavams by fermentation of a clavam-producing organism in a suitable medium wherein the ammonium levels are kept low so as to avoid repression of enzymes, particularly urease, are disclosed.
Type:
Grant
Filed:
September 29, 1999
Date of Patent:
May 22, 2001
Assignee:
SmithKline Beecham, p.l.c.
Inventors:
Brian Peter Valentine, Paul Alan Jeffkins, William Henry Holms, David Michael Mousdale
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 and 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:
June 11, 1999
Date of Patent:
May 15, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Thomas Joseph Carr, Renee Louise Desjarlais, Timothy Francis Gallagher, Stacie Marie Halbert, Hye-Ja Oh, Scott Kevin Thompson, Daniel Frank Veber, Dennis Shinji Yamashita, Jack Hwekwo Yen
Abstract: The compositions of the present invention are useful for the topical delivery of a wide variety of active ingredients. These compositions are particularly useful for treating conditions such as acne and its attendant skin lesions, blemishes, and other imperfections. These compositions are nonirritating to the skin and also provide skin feel benefits. These compositions can be in the form of leave-on products and products that are rinsed or wiped from the skin after use.
Abstract: Solid phase combinatorial synthesis is carried out in a multi-reactor synthesizer comprising an array of separate reactor cells (1-9) containing a solid reaction support medium (26). Subsets of the reactor cells (1-9) are interconnected with one another in a desired pattern, and, in a first reaction step, reagents (A, B, C) are circulated through the subsets. After the first reaction step is completed, the reactor cells (1-9) are rearranged into a new configuration of the subsets, and the same, or other, reagents (A, B, C) are circulated through the new subsets. The process can be repeated to produce large numbers of compounds differing from one another.
Type:
Grant
Filed:
November 20, 1998
Date of Patent:
May 1, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Michael Lee Moore, Dennis Shinji Yamashita
Abstract: This invention relates to methods for treating diseases or disorders mediated by lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which method comprises administration to a mammal in need thereof of an effective Coenzyme A independent transacylase (CoA-IT) inhibiting amount of a triphenylmethylazetidinone. This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a triphenylmethylazetidinone.
Type:
Grant
Filed:
November 8, 1999
Date of Patent:
April 24, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
William E. Bondinell, James David Winkler
Abstract: A method for promoting smoking cessation, which method comprises administrating an effective, non-toxic amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof to a human in need thereof. Said ropinirole is preferably administered orally or transdermally. Also provided is a medicament for use in smoking cessation that comprises ropinirole. Said medicament may be a tablet for oral use or a transdermal patch containing ropinirole.
Abstract: Infections potentially caused by DRSP may be treated by a method, which comprises administering to an adult or older child patient a pharmaceutical formulation comprising from 800 to 1100 mg amoxycillin and from 100 to 150 mg clavulanate in a weight ratio between 6:1 and 10:1 inclusive, in combination with a pharmaceutically acceptable carrier or excipient, three times a day (tid).