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
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 āSā. (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.
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.
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
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
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
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
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
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
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
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
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
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
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
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
Abstract: Pyrrolo[2,1-c][1,2,4]thiadiazole or pyrollo[2,1-c][1,2,4]oxadiazoles having the formula:
or pharmaceutically acceptable salts thereof, useful as nitric oxide synthase inhibitors wherein each substituent is defined herein.
Type:
Grant
Filed:
March 26, 2001
Date of Patent:
April 22, 2003
Assignee:
Monsanto/G.D. Searle
Inventors:
Donald W. Hansen, Jr., R. Keith Webber, E. Ann Hallinan, Mihaly V. Toth, Barnett S. Pitzele, Alok K. Awasthi, Alan E. Moormann, Suzanne Metz, Jeffery S. Snyder, William M. Moore, Jeffrey A. Scholten