Patents Represented by Attorney, Agent or Law Firm Mary E. McCarthy
  • Patent number: 6559172
    Abstract: Novel disubstituted imidazoles are disclosed which are useful in the treatment of bacterial infections, particularly through the inhibition of FAB I.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: May 6, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Dirk Heerding, Kenneth A. Newlander
  • Patent number: 6548504
    Abstract: The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof: in which the group D is selected from a group of formula (A), (B) or (C) below: in which P is a monocyclic, bicyclic or tricyclic alicyclic ring containing up to 20 carbon atoms in the ring(s); A is a single bond, a C1-6alkylene or a C2-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more fluorine atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, amino, alkylamino or dialkylamino, SR11 where R11 is hydrogen or C1-6alkyl or R1 is aryl, arylC1-6alkyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; n is 0, 1, 2 or 3; and R2 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl or C3-6cycloalkyl; or in which Ra is an alkyl group containing 1 to 20 carbon atoms o
    Type: Grant
    Filed: July 19, 2000
    Date of Patent: April 15, 2003
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Steven Mark Bromidge, Stephen Frederick Moss
  • Patent number: 6517871
    Abstract: This invention relates to bioenhanced formulations comprising eprosartan or eprosartan mesylate in the amorphous form, a process for its production, compositions containing the compound and methods of using the compound to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.
    Type: Grant
    Filed: May 23, 2001
    Date of Patent: February 11, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Gopadi M. Venkatesh, Manga R. Gudipati
  • Patent number: 6515010
    Abstract: This invention relates to carvedilol methanesulfonate, compositions containing this compound and methods of using carvedilol methanesulfonate to treat hypertension, congestive heart failure and angina.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: February 4, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Miriam Franchini, Gopadi M. Venkatesh
  • Patent number: 6514992
    Abstract: The present invention is to novel compounds of Formula (I), their pharmaceutical compositions, and to the novel inhibition of Caspases for use in the treatment of apoptosis, and disease states caused by excessive or inappropriate cell death.
    Type: Grant
    Filed: December 14, 2000
    Date of Patent: February 4, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis Lee, Scott A. Long
  • Patent number: 6506758
    Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein: A represents an optionally substituted aryl group or an optionally substituted heterocyclyl group; Ra represents —CO—NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heterocyclyl or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclyl group; R1 and R2 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R1 and R2 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R3 represents hydrogen, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carbox
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: January 14, 2003
    Assignees: SmithKline Beecham Laboratoires Pharmceutiques, SmithKline Beecham SpA
    Inventors: Stefania Gagliardi, Guy Marguerite Marie Gerard Nadler, Pietro A T Novella
  • Patent number: 6506774
    Abstract: The use of orexin receptor antagonists as neuroprotectants, and in the treatment of nausea and vomiting, irritable bowel syndrome and other conditions associated with visceral pain.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: January 14, 2003
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Elaine Alison Irving, Gareth John Sanger
  • Patent number: 6503903
    Abstract: Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment bacterial infections: wherein: R1 is H, C1-6alkyl or Ar—C0-6alkyl; R2 is H, C1-6alkyl, Ar—C0-6alkyl, HO—(CH2)n— or R′OC(O)—(CH2)n—; R3 is A—C0-4alkyl, A—C2-4alkenyl, A—C2-4alkynyl, A—C3-4oxoalkenyl, A—C3-4oxoalkynyl, A—C1-4aminoalkyl, A—C3-4aminoalkenyl, A—C3-4aminoalkynyl, optionally substituted by any accessible combination of one or more of R10 or R7; R5 is H, C1-6alkyl, Ar—C0-6alkyl or C3-6cycloalkyl-C0-6alkyl; A is H, C3-6cycloalkyl, Het or Ar; R7 is —COR8, —COCR′2R9, —C(S)R8, —S(O)kOR′, —S(O)kNR′R″, —PO(OR′), —PO(OR′)2, —B(OR′)2, —NO2, or tetrazolyl; R8 is —OR′, —NR′R″, —NR′SO2R′, —NR′OR′, or —OCR′
    Type: Grant
    Filed: October 18, 2001
    Date of Patent: January 7, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld
  • Patent number: 6500863
    Abstract: Novell IL-8 compounds and methods of using them are provided.
    Type: Grant
    Filed: June 13, 2001
    Date of Patent: December 31, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Qi Jin, Brent W. McCleland, Michael R. Palovich, Katherine L. Widdowson
  • Patent number: 6498187
    Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: December 24, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Robert A. Daines, Jack D. Leber, Israil Pendrak, Joseph Weinstock
  • Patent number: 6495560
    Abstract: A compound of the formula (I) is disclosed which is a vitronectin receptor antagonist and is useful in the treatment of osteoporosis: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: December 17, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: William H. Miller, Peter J. Manley
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • Patent number: 6458784
    Abstract: Pharmaceutically active benzodiazapine compounds of formula (I) are disclosed. These compounds inhibit the vitronectin receptor and are useful for treatment of osteoporosis.
    Type: Grant
    Filed: October 5, 2000
    Date of Patent: October 1, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Russell Donovan Cousins, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Irene Nijole Uzinskas
  • Patent number: 6458963
    Abstract: The present invention relates to a process for preparing eprosartan, an angiotensin II receptor antagonist useful in the treatment of hypertension, congestive heart failure, and renal failure. The process for preparing eprosartan consists of three stages. These stages are: (Stage†1) the regioselective protection of 2-n-butyl-4-formylimidazole; (Stage†2) the reaction between the product from Stage 1 and (2-thienylmethyl)-propanedioic acid, mono-C1-4alkyl ester; and (Stage†3) quaternary salt formation, followed by a basic work-up and an acidification. The efficiency of this synthetic sequence is particularly is particularly useful for the large-scale production of eprosartan.
    Type: Grant
    Filed: August 14, 2001
    Date of Patent: October 1, 2002
    Assignee: SMithKline Beecham Corporation
    Inventors: Richard T. Matsuoka, Peng Liu