Patents Represented by Attorney Grace C. Hsu
  • Patent number: 8343986
    Abstract: The present invention relates to compounds of Formula (I): pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metalloproteinase enzymes (MMPs).
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: January 1, 2013
    Assignee: Glaxo Group Limited
    Inventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
  • Patent number: 8268839
    Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: September 18, 2012
    Assignee: Glaxosmithkline LLC
    Inventors: Ivan Leo Pinto, Shahzad Sharooq Rahman, Neville Hubert Nicholson
  • Patent number: 8263602
    Abstract: The present invention relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metallproteinase enzymes (MMPs).
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: September 11, 2012
    Assignee: Glaxo Group Limited
    Inventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
  • Patent number: 8143264
    Abstract: The present invention relates to a xanthine compound derivative which is 3-butyl-8-chloro-1-(3-{5-[(4-fluorophenyl)methyl]-2H-tetrazol-2-yl}propyl)-3,7-dihydro-1H-purine-2,6-dione: a pharmaceutically acceptable salt thereof, corresponding pharmaceutical formulations, combinations, preparation methods and methods or uses in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
    Type: Grant
    Filed: August 8, 2006
    Date of Patent: March 27, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Richard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
  • Patent number: 8076475
    Abstract: The present invention generally relates to a novel process for preparing vitronectin receptor antagonist compounds having a benzodiazepinyl core structure. This invention relates to the preparation of pharmaceutically active compounds which inhibit the vitronectin receptor and are useful for treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporosis. In particular, the present invention relates to a novel process for preparing (±)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid, (R)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid and (S)-3-oxo-8-{[3-(pyridin-2-ylamino)propyl]oxy}-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: December 13, 2011
    Assignee: GlaxoSmithKline LLC
    Inventor: Matthew Allen Zajac
  • Patent number: 7982053
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: July 19, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Michael Axten, Jesus R. Medina
  • Patent number: 7902378
    Abstract: The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.), and/or solvates thereof, compositions containing the aforementioned salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: March 8, 2011
    Assignee: SmithKline Beecham (Cork) Limited
    Inventors: Christopher S. Brook, Wei Chen, Philip C. Dell'Orco, Lee M. Katrincic, Ann Marie Louvet, Choon K. Oh, Paul G. Spoors, Christopher Werner
  • Patent number: 7893056
    Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined herein and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: February 22, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Donghui Qin, Beth Norton, Andrew Nicholas Knox, Siegfried B. Christensen, Kelly M. Aubart
  • Patent number: 7893100
    Abstract: The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.), and/or solvates thereof, compositions containing the aforementioned salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: February 22, 2011
    Assignee: SB Pharmco Puerto Rico Inc.
    Inventors: Christopher S. Brook, Wei Chen, Philip C. Dell'Orco, Lee M. Katrincic, Ann Marie Louvet, Choon K. Oh, Paul G. Spoors, Christopher Werner
  • Patent number: 7759384
    Abstract: The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.), and/or solvates thereof, compositions containing the aforementioned salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: July 20, 2010
    Assignee: SmithKline Beecham (Cork) Limited
    Inventors: Christopher S. Brook, Wei Chen, Philip C. Dell'orco, Lee M. Katrincic, Ann Marie Louvet, Choon K. Oh, Paul G. Spoors, Christopher Werner
  • Patent number: 7713982
    Abstract: The present invention relates to a therapeutically active xanthine derivative compound of formula (I): corresponding pharmaceutical formulations containing, manufacture processes for, methods or uses of such compounds in therapy, in particular for treatment of diseases where under-activation of the HM74A receptor contributes to such diseases or where activation of the HM74A receptor will be beneficial.
    Type: Grant
    Filed: February 10, 2005
    Date of Patent: May 11, 2010
    Assignee: Smithkline Beecham Corporation
    Inventor: Ivan Leo Pinto
  • Patent number: 7649010
    Abstract: The present invention relates to a salt of carvedilol, corresponding compositions containing such a carvedilol salt or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease states in mammals, in particular man. The present invention further relates to a novel crystalline form of carvedilol hydrobromide, which is the hydrobromide salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol, and/or other carvedilol solvates thereof, compositions containing salts or solvates of carvedilol hydrobromide, and methods of using the aforementioned compound(s) to treat hypertension, congestive heart failure, and angina, etc.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: January 19, 2010
    Assignee: SmithKline Beechman Cork Limited
    Inventors: Pingyun Y. Chen, Qunying Dai, Philip C. Dell'Orco, Claire Hisler, David H. Igo, Lee M. Katrincic, Clifford S. Labaw, Li-Jen J. Ping
  • Patent number: 7626041
    Abstract: The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.), and/or solvates thereof, compositions containing the aforementioned salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: December 1, 2009
    Assignee: SmithKline Beecham (Cork) Ltd
    Inventors: Christopher S. Brook, Wei Chen, Philip C. Dell'orco, Lee M. Katrincic, Ann Marie Louvet, Choon K. Oh, Paul G. Spoors, Christopher Werner
  • Patent number: 7601729
    Abstract: Compounds of Formula (I): wherein: A represents bond, C1-6alkyl or CH?CH—C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1? each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl;
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: October 13, 2009
    Assignee: Glaxo Group Limited
    Inventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
  • Patent number: 7476759
    Abstract: Compounds of Formula (I): wherein: R1 is optionally substituted —C4-12 alkyl, —C2-10alkylcycloalkyl, —C2-6alkylheterocycloalkyl, —C2-6alkylaryl, optionally substituted 5- or 6-membered aryl or heteroaryl with the proviso that R2 in not pyridinyl; Z is a bond, CH2, O, S, SO, SO2, NR4, OCR4R5 or CR4R5O; or Z, R1 and Q together form an optionally substituted fused tricyclic group; Q is an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X is COR3; R2 is CONH2, CO2H, CO2R7, SO2R7 or SO2NR8R9, with the proviso that R2 is not CO2R7, when X is CONH2; R3 is OR6 or NR8R9; R4 and R5 each independently is H, C1-6 alkyl or C1-4 alkylaryl; R6 is H or C1-6 alkyl; R7 is C1-6 alkyl; and R8 and R9 each independently is H or C1-6 alkyl; or R8 and R9 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; or physiologically functional derivatives thereof, with the proviso that formula (I) c
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: January 13, 2009
    Assignee: Glaxo Group Limited
    Inventors: Ian Holmes, Stephen Paul Watson
  • Patent number: 7452906
    Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: November 18, 2008
    Assignee: SmithKline Beecham P.L.C.
    Inventors: Mark James Bamford, David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson
  • Patent number: 7446106
    Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: November 4, 2008
    Assignee: SmithKline Beecham plc
    Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
  • Patent number: 7375248
    Abstract: Compounds of formula (I): wherein R1 represents optionally substituted C4-12 alkyl, optionally substituted C2-6alkylaryl, or optionally substituted 5- or 6-membered aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR4, OCR4R5, CR4R5O, or Z, R1 and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents COR3 or N(OR8)COR9; R2 represents SO2R10 or SO2NR10R11; R3 represents OR6, NR6R7 or NR6OH; R4 and R5 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R6 and R7 each independently represents H, C1-6 alkyl, or C1-6 alkyl substituted with one or more heteroaryl groups, or R6 and R7 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; R8 and R9 each independently represents H or C1-6 alkyl; R10 and R11 each independently represents H or C1-6 alkyl; and and physiolo
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: May 20, 2008
    Assignee: Glaxo Group Limited
    Inventors: Ian Holmes, Stephen Paul Watson
  • Patent number: 7375105
    Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: May 20, 2008
    Assignee: SmithKline Beecham p.l.c.
    Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
  • Patent number: 7297694
    Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: November 20, 2007
    Assignee: SmithKline Beechum P.L.C.
    Inventors: David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson