Patents Represented by Attorney, Agent or Law Firm Charles M. Kinzig
  • Inhibitors of transcription factor-NF-&kgr;B
    Patent number: 6492425
    Abstract: The present invention provides pharmaceutical compositions of salicylanilide inhibitors of transcription factor NF-&kgr;B, and methods for treating diseases in which activation of NF-&kgr;B is implicated. More specifically, the present invention provides methods of treatment of a variety of diseases associated with NF-&kgr;B activation including inflammatory disorders; particularly rheumatoid arthritis, inflammatory bowel disease, and asthma; dermatosis, including psoriasis and atopic dermatitis; autoimmune diseases; tissue and organ rejection; Alzheimer's disease; stroke; atherosclerosis; restenosis; cancer, including Hodgkin's disease; certain viral infections, including AIDS; osteoarthritis; osteoporosis; and Ataxia Telangiestasia by administering to a patient in need thereof a compound of the present invention.
    Type: Grant
    Filed: December 19, 2000
    Date of Patent: December 10, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: James F. Callahan, Marie C. Chabot-Fletcher
  • Substituted isoquinoline derivatives and their use as anticonvulsivants
    Patent number: 6492378
    Abstract: This invention relates to novel substituted isoquinoline derivatives and their use as anticonvulsants.
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: December 10, 2002
    Assignee: SmithKline Beecham p.l.c.
    Inventors: John David Harling, Jag Paul Heer, Mervyn Thompson
  • Substituted imidazole compounds
    Patent number: 6489325
    Abstract: The present invention relates to novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 inhibitors.
    Type: Grant
    Filed: March 30, 2000
    Date of Patent: December 3, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Ralph F. Hall
  • C3A receptor ligands
    Patent number: 6489339
    Abstract: A compound according to Formula (I): wherein: A represents C1-4 alkylene, unsubstituted or optionally substituted by C1-4 alkyl or aryl; or A forms a 5-8 membered fused aliphatic ring with the adjacent phenyl ring; m is an integer from 1 to 3; each R1 is independently selected form the group consisting of halo, C1-4 alkyl, methanesulfonyl, alkoxy, nitrile, dimethylamine, methylenedioxy and CF3; and R2 is hydrogen or methyl is provided.
    Type: Grant
    Filed: February 7, 2001
    Date of Patent: December 3, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis Lee, William E. Bondinell, Anthony J. Jurewicz
  • FabZ from Staphylococcus aureus
    Patent number: 6489139
    Abstract: The invention provides fabZ polypeptides and polynucleotides encoding fabZ polypeptides and methods for producing such polypeptides by recombinant techniques. Also provided are methods for utilizing fabZ polypeptides to screen for antibacterial compounds.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: December 3, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Howard Kallender, John T. Lonsdale, Stephanie Van Horn, Patrick V. Warren
  • Hepatitis B vaccine
    Patent number: 6488934
    Abstract: A novel vaccine formulation is provided, comprising a hepatitis B component, particularly hepatitis B surface antigen, in combination with aluminum phosphate and 3 de-O-acylated monophosphoryl lipid A.
    Type: Grant
    Filed: December 6, 2000
    Date of Patent: December 3, 2002
    Assignee: SmithKline Beecham Biologicals S.A.
    Inventors: Pierre Hauser, Nathalie Marie-Josephe Claude Garcon, Pierre Desmons
  • Indole compounds
    Patent number: 6486211
    Abstract: Novel indole derivatives, pharmaceutical compositions containing these compounds and their use as inhibitors of the fatty acid synthase FabH are disclosed.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: November 26, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Robert A. Daines, William Dennis Kingsbury, Israil Pendrak
  • Indole compounds useful for treating bacterial infections
    Patent number: 6486192
    Abstract: This invention relates to the use of certain indole compounds, which are active as inhibitors of the fatty acid synthase FabH, for the treatment of bacterial infections.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: November 26, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Robert A. Daines, Pamela A. Chambers
  • Process for epoxidizing substituted cyclohexanones
    Patent number: 6482960
    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
  • Endothelin receptor antagonists
    Patent number: 6482956
    Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: November 19, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Juan Ignacio Luengo, John Duncan Elliott
  • Process of making 3-phenyl-1-methylenedioxyphenyl-indane-2-carboxylic acid derivatives
    Patent number: 6479659
    Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentano[b]pyridine derivatives. The most preferred compounds prepared by this inventino are (+)(1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S, 2R, 3S)-3-[(2-carboxymethoxy-4-methoxyphenyl)-1- (3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.
    Type: Grant
    Filed: September 10, 2001
    Date of Patent: November 12, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Yemane Woldeselassie Andemichael, Neil Howard Baine, William Morrow Clark, Conrad John Kowalski, Michael Anthony McGuire, Robert John Mills
  • Process for the preparation of anti-malarial drugs
    Patent number: 6479660
    Abstract: The invention relates to novel intermediates and processes for the preparation of quinoline compounds useful as anti-malarial drugs and novel intermediates useful in the process. A process for the preparation of a compound of formula (I) in which R1 is C1-6 alkyl; R2 and R3 are independently hydrogen, halogen, trifluoromethyl or C1-6 alkoxy; R4 is C1-6 alkyl; R5 is hydrogen or C1-6 alkyl; and R6 or amino which comprises reacting a compound of formula (II) in which R1, R4 and R5 are as defined in formula (I) and X is a leading group with a compound of formula (III).
    Type: Grant
    Filed: December 14, 2001
    Date of Patent: November 12, 2002
    Assignees: SmithKline Beecham p.l.c., SmithKline Beecham Corporation
    Inventors: Cletus Onwuzurike Ugwuegbulam, James Edward Foy
  • Process for manufacturing bite-dispersion tablets
    Patent number: 6475510
    Abstract: This invention relates to a method for the manufacture of Bite-dispersion tablets which disperse easily and quickly in the oral cavity, after a gentle bite, without the aid of water, and if necessary includes masking the bitter taste of medicaments. The process comprises preparing a dry granulation of one or more of medicaments blended with suitable excipients, flavors and a combination of a waxy material and phospholipid (BMI-60) or an intense sweetener derived from fruit flavonoids (Neohesperidine) for taste-masking and compressing into tablets which can be packaged in bottles or blisters using conventional equipment.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: November 5, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Gopadi M. Venkatesh, Nageswara R. Palepu
  • Compounds and methods
    Patent number: 6476028
    Abstract: A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: November 5, 2002
    Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.
    Inventors: William E. Bondinell, James Chan, Roderick A. Porter, Joseph W. Venslavsky, Steven Dabbs, David T. Davies
  • Pharmaceutical formulations
    Patent number: 6472383
    Abstract: A pharmaceutical formulation comprises, in combination with a penem of formula (I): in which: R1 is hydrogen or an organic substituent group; R2 is a fused bicyclic heterocyclic ring system of general formula:  wherein R4 and R5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is zero, 1 or 2; and R3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol ═/═ indicates that the double bond may be in either the E or Z configuration; and a pharmaceutically acceptable carrier; a &bgr;-lactam antibiotic selected from the group consisting of ceftazidime, cefotaxime, amoxycillin, and piperacillin, and pharmaceutically acceptable derivatives thereof.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: October 29, 2002
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Kenneth Coleman, Jane Elizabeth Neale
  • Controlled release dosage form of [R-(Z)]-&agr;-(methoxyimino)-&agr;-(1-azabicyclo[2.2.2]oct-3yl) acetonitrile monohydrochloride
    Patent number: 6468560
    Abstract: A controlled release formulation of an acetonitrile compound and its use in the treatment and/or prophylaxis of certain disorders.
    Type: Grant
    Filed: September 19, 2001
    Date of Patent: October 22, 2002
    Assignees: SmithKline Beecham p.l.c., SmithKline Beecham Corporation
    Inventors: Joseph Peter Sauer, Susan Marie Milosovich, William Thomas Muldoon, James Albert Napper, Laurence Rousseau
  • Procedure for producing formylimidazoles
    Patent number: 6469178
    Abstract: A new process for the catalytic conversion of hydroxymethyl imidazoles to formylimidazoles is described. The reaction takes place in the presence of a peroxide. Formylimidazoles are important intermediate products for pharmaceutical substances.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: October 22, 2002
    Assignee: Lonza AG
    Inventors: Yves Bessard, Josef Heveling
  • Indole compounds useful for treating bacterial infections
    Patent number: 6469046
    Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH useful in treating bacterial infections.
    Type: Grant
    Filed: November 28, 2001
    Date of Patent: October 22, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Robert A. Daines, Kelvin C. Sham
  • Tetrahydroisoquinoline derivatives as modulators of dopamine D3 receptors
    Patent number: 6465485
    Abstract: Compounds of formula (I): and their salts having affinity for dopamine receptors, in particular the D3 receptor, and thus potential in the treatment of conditions wherein modulation of the D3 receptor is beneficial, e.g., as antipsychotic agents.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: October 15, 2002
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Clive Leslie Branch, Christopher Norbert Johnson, Geoffrey Stemp
  • Injection moulding process and apparatus for making articles from two components
    Patent number: 6464920
    Abstract: A process for making a molded article of two components e.g., plastic material and elastomer, in which internal cores are used to form a hollow toothbrush body, and elastomer is injected to form surface features. The toothbrush body can be made bulky in shape but light by virtue of being hollow.
    Type: Grant
    Filed: August 12, 1999
    Date of Patent: October 15, 2002
    Assignee: SmithKline Beecham Consumer Healthcare GmbH
    Inventor: Hans Krämer