Patents Represented by Attorney Philip B. Polster
  • Patent number: 7012098
    Abstract: Agents and methods for chemoprevention and treatment of neoplasia are described, the agents including a selective inhibitor of inducible nitric oxide synthase and a combination of a selective inhibitor of inducible nitric oxide synthase and an inhibitor of cylcooxygenase-2 in a pharmaceutical composition. The agents and methods are used for chemoprevention and treatment of neoplasia including colorectal cancer and other cancers affecting epithelial cells throughout the body. The agents can also be used to treat the fibrosis that occurs with radiation therapy, as well as adenomatous polyps, including those with familial adenomatous polyposis (FAP).
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: March 14, 2006
    Assignee: Pharmacia Corporation
    Inventors: Pamela T. Manning, Jane R. Connor, Karen Seibert, Chinthalapally V. Rao, Bandaru S. Reddy
  • Patent number: 7005450
    Abstract: The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: April 7, 2004
    Date of Patent: February 28, 2006
    Assignee: Pharmacia Corporation
    Inventors: Richard C. Durley, James Sikorski, Donald W. Hansen, Jr., Michelle A. Promo, Ronald Keith Webber, Barnett S. Pitzele, Alok K. Awasthi, Alan Moormann
  • Patent number: 6998415
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
    Type: Grant
    Filed: January 12, 2004
    Date of Patent: February 14, 2006
    Assignee: Pharmacia Corporation
    Inventors: John J. Talley, James A. Sikorski, Balekudru Devadas, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Kathy L. Rogers, legal representative, Hwang-Fun Lu, David L. Brown, Roland S. Rogers, deceased
  • Patent number: 6998503
    Abstract: (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid is crystallized as an anhydrous, stoichiometric 1.5 HCl salt and a scaleable crystallization method is disclosed. The salt form was characterized and the absolute configuration of the chiral center was confirmed as ā€œSā€. (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid was high melting and appears acceptably non-hygroscopic for use in a pharmaceutical composition.
    Type: Grant
    Filed: August 22, 2003
    Date of Patent: February 14, 2006
    Assignee: Pharmacia Corporation
    Inventor: E. Ann Hallinan
  • Patent number: 6995281
    Abstract: Methods of selectively removing counterions from compounds are disclosed. Compounds derived from the methods, such as the compound S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine zwitterion with between zero and up to 2 molar equivalents of hydrochloride are also disclosed.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: February 7, 2006
    Assignee: Pfizer, Inc.
    Inventor: Christine Moore
  • Patent number: 6956131
    Abstract: The present invention is directed to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 is selected from the group consisting of H and methyl; and R2 is selected from the group consisting of H and methyl. The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: October 18, 2005
    Assignee: Pharmacia Corporation
    Inventors: Barnett S. Pitzele, James A. Sikorski, Ronald Keith Webber
  • Patent number: 6951889
    Abstract: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: September 15, 2001
    Date of Patent: October 4, 2005
    Assignee: Pharmacia Corporation
    Inventors: Donald W. Hansen, Jr., Ronald Keith Webber, Barnett S. Pitzele, James Sikorski, Mark A. Massa, Timothy J. Hagen, Margaret Grapperhaus, Lijuan Jane Wang, Arija A. Bergmanis, Steven W. Kramer, E. Ann Hallinan
  • Patent number: 6914158
    Abstract: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
    Type: Grant
    Filed: April 1, 2004
    Date of Patent: July 5, 2005
    Assignee: Pharmacia Corporation
    Inventors: Ronald Keith Webber, Richard C. Durley, Alok K. Awasthi, Arija A. Bergmanis, Kam F. Fok, Scott S. Ganser, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Brian S. Hickory, Pamela T. Manning, Michael Mao, Alan E. Moormann, Barnett S. Pitzele, Michelle A. Promo, Richard R. Schartman, Jeffrey A. Scholten, Jeffrey S. Snyder, Mihaly V. Toth, Mahima Trivedi, Sofya Tsymbalov, Foe Siong Tjoeng
  • Patent number: 6828456
    Abstract: The present invention relates to 2-amino-2-alkyl-3 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: September 15, 2001
    Date of Patent: December 7, 2004
    Assignee: Pharmacia Corporation
    Inventors: Donald W. Hansen, Jr., Ronald Keith Webber
  • Patent number: 6787668
    Abstract: The present invention is directed to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from the group consisting of H and methyl; and R2 is selected from the group consisting of H and methyl. The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: September 7, 2004
    Assignee: Pharmacia Corporation
    Inventors: Barnett S. Pitzele, James A. Sikorski, Ronald Keith Webber
  • Patent number: 6774126
    Abstract: Pyrrolo[1,2-b][1,2,4]oxadiazine-2,3(6H)-diones having the formula: or pharmaceutically acceptable salts thereof, useful as nitric oxide synthase inhibitors wherein each substituent is defined herein.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: August 10, 2004
    Assignee: Pharmacia Corporation
    Inventors: Donald W. Hansen, Jr., E. Ann Hallinan, Alok K. Awasthi, Suzanne Metz, Jeffrey A. Scholten, Jeffery S. Snyder, Mihaly V. Toth, Ronald Keith Webber
  • Patent number: 6716844
    Abstract: An aromatic sulfonyl aipha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: December 3, 2001
    Date of Patent: April 6, 2004
    Assignee: Pharmacia Corporation
    Inventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
  • Patent number: 6716829
    Abstract: Combinations of aldosterone blockers and Cyclooxygenase-2 inhibitors useful in the treatment of inflammation are disclosed.
    Type: Grant
    Filed: July 26, 2001
    Date of Patent: April 6, 2004
    Assignee: Pharmacia Corporation
    Inventors: Ricardo Rocha, Marc Zack, Ellen McMahon, Eileen R. Blasi
  • Patent number: 6656954
    Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: November 29, 2001
    Date of Patent: December 2, 2003
    Assignee: Pharmacia Corporation
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
  • Patent number: 6653350
    Abstract: Methods of treating osteoarthritis by administering an therapeutically effective amount of NOS inhibitor are provided.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: November 25, 2003
    Assignees: G.D. Searle & Co., Pharmacia Corporation
    Inventors: Pamela T. Manning, Jane R. Connor, Mark G. Currie, Jean Pierre Pelletier, Johanne Martel Pelletier
  • Patent number: 6638758
    Abstract: A method of separating enantiomeric lactam esters. The lactam esters are contacted with a biocatalyst, such as an enzyme or a microorganism, in a solution wherein only one enantiomer is selectively hydrolyzed to give the optically active isomer of the corresponding acid. The hydrolysis product is then separated from the unreacted lactam esters. The enzyme is then recycled for reuse in the next enzymatic resolution. The undesired isomer is also racemized and reused in the next enzymatic resolution.
    Type: Grant
    Filed: June 6, 2001
    Date of Patent: October 28, 2003
    Assignee: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Mahima Trivedi, Rolando E. Gapud, John S. Ng, Alok K. Awasthi, Ping T. Wang
  • Patent number: 6638952
    Abstract: An aromatic sulfonyl alpha-cycloamino hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-cycloamino hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: December 23, 1999
    Date of Patent: October 28, 2003
    Assignee: Pharmacia Corporation
    Inventors: Hui Li, Daniel P. Becker, Clara I. Villamil, Terri L. Boehm, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo
  • Patent number: 6586474
    Abstract: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: July 1, 2003
    Assignee: Pharmacia Corporation
    Inventors: Ronald Keith Webber, Richard C. Durley, Alok K. Awasthi, Arija A. Bergmanis, Kam F. Fok, Scott S. Ganser, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Brian S. Hickory, Pamela T. Manning, Michael Mao, Alan E. Moormann, Barnett S. Pitzele, Michelle A. Promo, Richard R. Schartman, Jeffrey A. Scholten, Jeffrey S. Snyder, Mihaly V. Toth, Mahima Trivedi, Sofya Tsymbalov, Foe Siong Tjoeng
  • Patent number: 6586471
    Abstract: The present invention contains halogenated 2-amino-3,4 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: July 1, 2003
    Assignee: G. D. Searle
    Inventors: Donald W. Hansen, Jr., Barnett S. Pitzele, Ronald Keith Webber, Mihaly V. Toth, Pamela T. Manning, Alok K. Awasthi, Mahima Trivedi
  • Patent number: 6576780
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: June 10, 2003
    Assignee: GD Searle & Company
    Inventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth