Abstract: Compounds of formula (I): with a variety of therapeutic uses, more particularly novel prodrugs that are particularly useful for delivering a parent compound for selective estrogen receptor modulation.
Type:
Grant
Filed:
October 4, 2004
Date of Patent:
October 28, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
John Fred Eaddy, III, Dennis Heyer, Amarjit Sab Randhawa, Vicente Samano, John Albert Ray, Subba Reddy Katamreddy, Michael Tolar Martin, Michael Scott McClure
Abstract: There is provided novel diazepines that function as agonists at the melanocortin 4 receptor and as agonists at the melanocortin 1 receptor, pharmaceutical compositions containing them, methods for their use in treatment, and processes for their preparation.
Type:
Grant
Filed:
May 27, 2005
Date of Patent:
October 28, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Jerzy Ryszard Szewczyk, Jason Daniel Speake, Douglas McCord Sammond, Ronald George Sherrill
Abstract: The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1 is phenyl optionally substituted by 1, 2 or 3 halogen atoms which halogen atoms may be the same or different; R2 is C1-6alkyl, C3-6cycloalkyl or acetyl; X is oxygen or sulphur; a is 1, 2 or 3; b is 0 or 1; c is 0, 1 or 2; R3 is hydrogen or C1-6alkyl; R4 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxyC1-6alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-6alkyl; R5 is hydrogen; or R5 and R3, together with the interconnecting atoms, form a 4, 5 or 6 membered ring; R6 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; and z is 0, 1 or 2; wherein when z is 1 or 2, Z is a halogen atom, and wherein when z is 2 the halogen atoms may be the same or different.
Abstract: The present invention provides combinations of compounds of formula (I) and other therapeutic agents for the treatment of PPAR related diseases.
Type:
Grant
Filed:
August 17, 2006
Date of Patent:
October 21, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Rodolfo Cadilla, Romain Luc Marie Gosmini, Millard Hurst Lambert, III, Michael Lawrence Sierra
Abstract: Polypeptides capable of binding human IL-13 and/or of binding human IL-4 in the presence of IL-4 R? can be used in medicine, in diagnosis and in screening for agonists/antagonist of IL-13/IL-4. One such polypeptide is shown in FIG. 1.
Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
Type:
Application
Filed:
October 13, 2005
Publication date:
October 16, 2008
Applicant:
Smithkline Beecham Corporation
Inventors:
Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Stewart
Abstract: Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
Type:
Application
Filed:
July 28, 2004
Publication date:
October 16, 2008
Applicant:
SMITHKLINE BEECHAM CORPORATION
Inventors:
Dirk A. Heerding, Tammy J. Clark, David Harold Drewry, Jack Dale Leber, Igor Safonov, Dennis S. Yamashita
Abstract: The present invention relates to 4?-[(1R)-1-[[(6,7-dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin- 4-yl)acetyl](methyl)amino]-2-(4-morpholinyl)ethyl]-4-biphenylcarboxylic acid and its pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
Type:
Grant
Filed:
July 20, 2007
Date of Patent:
October 7, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Krista B. Goodman, Michael J. Neeb, Clark A. Sehon, Andrew Q. Viet, Gren Z. Wang
Abstract: There is provided a method of loading a container with a defined quantity of product which comprises the steps of a) closing off a perforation in a perforated plate; b) directing powder into said closed-off perforation by the action of a first leveller blade moveable in a sweeping path relative to the perforated plate; and c) transferring the contents of the perforation to said container, and an apparatus for achieving such method.
Type:
Grant
Filed:
May 18, 2000
Date of Patent:
September 23, 2008
Assignee:
Smithkline Beecham Corporation
Inventors:
Alan Anthony Wilson, Phillip William Farr, Marcus Edward Pike
Abstract: The present invention relates to novel members of the Tumor Necrosis Factor family of receptors. The invention provides isolated nucleic acid molecules encoding a human TR2 receptor and two splice variants thereof. TR2 polypeptides are also provided as are vectors, host cells and recombinant methods for producing the same. The invention further relates to screening methods for identifying agonists and antagonists of TR2 receptor activity. Also provided are diagnostic methods for detecting disease states related to the aberrant expression of TR2 receptors. Further provided are therapeutic methods for treating disease states related to aberrant proliferation and differentiation of cells which express the TR2 receptors.
Type:
Grant
Filed:
October 30, 1996
Date of Patent:
September 23, 2008
Assignees:
Human Genome Sciences, Inc., SmithKline Beecham Corporation
Inventors:
Jian Ni, Craig A. Rosen, Reiner L. Gentz
Abstract: Furo- and thienopyrimidine derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such furo- and thienopyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
Type:
Grant
Filed:
September 10, 2002
Date of Patent:
September 23, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Jerry Leroy Adams, Deborah Lynne Bryan, Yanhong Feng, Shinichiro Matsunaga, Yutaka Maeda, Yasushi Miyazaki, Masato Nakano, Jean-Philippe Rocher, Hideyuki Sato, Marcus Semones, Domingos J. Silva, Jun Tang
Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.
Type:
Grant
Filed:
April 29, 2003
Date of Patent:
September 16, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Richard Martyn Angell, Paul Bamborough, Ian Robert Baldwin, Anne-Marie Li-Kwai-Cheung, Timothy Longstaff, Suzanne Joy Merrick, Kathryn Jane Smith, Stephen Swanson, Ann Louise Walker
Abstract: An improved process for preparing arylethanoldiamines is described. Compounds of this type are known to be useful as agonists at a typical beta-adrenoceptors (also known as beta-3-adrenoceptors).
Type:
Grant
Filed:
December 17, 2001
Date of Patent:
September 16, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Jason William Beames Cooke, Bobby Neal Glover, Ronnie Maxwell Lawrence, Matthew Jude Sharp, Maria Fumiko Tymoschenko
Abstract: Disclosed is a water-dispersible solid composition of a sparingly water-soluble compound in a particulatable lipidic carrier, methods for the preparation and use of the same. The compositions of this intention provide improved solubility and dissolution characteristics and enhanced bioavailability of the sparingly soluble compound.
Abstract: The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.
Type:
Grant
Filed:
June 7, 2004
Date of Patent:
September 2, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
Sharon Davis Boggs, Kristjan S Gudmundsson
Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. 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 hydroxy-1-azobenzene derivative.
Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates 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 novel compounds of formula (I) with a variety of therapeutic uses, more particularly novel substituted quinoline compounds particularly useful for selective estrogen receptor modulation.
Type:
Grant
Filed:
February 22, 2005
Date of Patent:
July 29, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
William Joel Hoekstra, Aaron Bayne Miller, William John Zuercher, Harikrishna Suryakant Patel
Abstract: Genes associated with schizophrenia are identified. Methods of screening small molecule compounds for use in treating schizophrenia are described.
Type:
Application
Filed:
January 8, 2008
Publication date:
July 24, 2008
Applicant:
SMITHKLINE BEECHAM CORPORATION
Inventors:
Stephanie Chissoe, Margaret G. Ehm, Pamela St. Jean