Abstract: An aromatic sulfonyl alpha-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:
June 4, 1999
Date of Patent:
March 26, 2002
Assignee:
G. D. Searle & Company
Inventors:
John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
Abstract: The present invention provides compounds having the structure:
and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.
Type:
Grant
Filed:
May 14, 1999
Date of Patent:
July 24, 2001
Assignee:
G. D. Searle & Company
Inventors:
Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell, Julie Marion Miyashiro, James Malecha, Thomas Dale Penning
Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
Type:
Grant
Filed:
November 19, 1999
Date of Patent:
July 17, 2001
Assignee:
G.D. Searle and Company
Inventors:
Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
Abstract: The present invention relates to a class of compounds represented by Formula I
or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.
Type:
Grant
Filed:
April 8, 1999
Date of Patent:
June 26, 2001
Assignee:
G. D. Searle & Company
Inventors:
Barbara B. Chen, Helen Y. Chen, Glen J. Gesicki, Richard A. Haack, James W. Malecha, Thomas D. Penning, Joseph G. Rico, Thomas E. Rogers, Peter G. Ruminski, Mark A. Russell, Stella S. Yu
Abstract: Methods and compositions for preventing, reducing, or reversing multidrug resistance (MDR) during cancer chemotherapy in patients undergoing treatment with therapeutically effective amounts of chemotherapeutic agents are provided. The methods comprise administering an anti-MDR effective amount of an N-substituted-1,5-dideoxy-1,5-imino-D-glucitol or galactitol iminosugar to a patient.
Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
Type:
Grant
Filed:
March 11, 1998
Date of Patent:
March 27, 2001
Assignee:
G. D. 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: Monoclonal antibodies that recognize the &agr;v&bgr;3 integrin receptor complex, but do not significantly bind to &agr;IIb&bgr;IIIa, can be used in methods for treating &agr;v&bgr;3 integrin-mediated diseases, such as tunor metastasis.
Type:
Grant
Filed:
April 9, 1998
Date of Patent:
February 27, 2001
Assignees:
The Burnham Institute, G. D. Searle & Company
Inventors:
Christopher P. Carron, Debra M. Meyer, George A. Nickols, Jeffrey W. Smith
Abstract: The present invention provides a method for preventing or reducing a photosensitivity and/or phototoxicity reaction which may be caused by a once-per-day dose of a medication which causes a photosensitivity and/or phototoxicity reaction in a patient comprising administering the prescribed or suggested dose of the medication to the patient during the evening or early morning hours.
Type:
Grant
Filed:
September 24, 1997
Date of Patent:
January 9, 2001
Assignee:
G. D. Searle & Company
Inventors:
Paul Dale Klimstra, Barbara Roniker, Edward Allen Swabb
Abstract: A cDNA clone having a base sequence for human tissue factor inhibitor (TFI) has been developed and characterized and the amino acid sequence of the TFI has been determined. Antibodies having a binding region specific to human tissue factor inhibitor are disclosed.
Type:
Grant
Filed:
April 3, 1998
Date of Patent:
January 9, 2001
Assignee:
G. D. Searle and Company
Inventors:
Tze Chein Wun, Kuniko K. Kretzmer, George J. Broze, Jr.
Abstract: Monoclonal antibodies that recognize the &agr;v &bgr;3 integrin receptor complex, but do not significantly bind to &agr;IIb&bgr;IIIa, inhibit &agr;v&bgr;3 integrin-mediated diseases.
Type:
Grant
Filed:
April 9, 1998
Date of Patent:
January 9, 2001
Assignee:
G. D. Searle & Company
Inventors:
Christopher P. Carron, Debra M. Meyer, George A. Nickols
Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
October 4, 1999
Date of Patent:
January 2, 2001
Assignee:
G. D. Searle & Company
Inventors:
Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
Abstract: The present invention relates to human interleukin-3 (hIL-3) variant or mutant proteins (muteins) functionally co-administered with a other colony stimulating factors (CSF), cytokines, lymphokines, interleukins, hematopoietic growth factors or IL-3 variants.
Type:
Grant
Filed:
February 4, 1994
Date of Patent:
November 28, 2000
Assignee:
G. D. Searle & Company
Inventors:
S. Christopher Bauer, Mark Allen Abrams, Sarah Ruth Braford-Goldberg, Maire Helena Caparon, Alan M. Easton, Barbara Kure Klein, John P. McKearn, Peter O. Olins, Kumnan Paik, John W. Thomas
Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
Type:
Grant
Filed:
March 24, 1999
Date of Patent:
August 22, 2000
Assignee:
G.D. Searle and Company
Inventors:
Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
Abstract: Pharmaceutical compositions having a modified release profile for once daily dosing of metronidazole, methods for making the pharmaceutical compositions, and methods for treating a microbial infection with once daily dosing of the pharmaceutical compositions of the invention are provided. The compositions given once daily exhibit substantial bioequivalence to immediate release metronidazole given three times per day. The compositions of the invention comprise:(a) a first portion of metronidazole which is about 59 wt % to about 79 wt % metronidazole;(b) about 1.5 wt % to about 3.0 wt % of an aqueous insoluble poly(meth)acrylic acid ester copolymer which is aqueous permeable, aqueous expandable and pH-independent;(c) about 0.1 wt % to about 2.
Type:
Grant
Filed:
January 27, 1994
Date of Patent:
August 15, 2000
Assignee:
G. D. Searle & Company
Inventors:
Subhash Desai, Alan Mark Mancini, Steven Charles Schumann
Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein Q, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described in the specification.
Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
May 10, 1999
Date of Patent:
May 16, 2000
Assignee:
G.D. Searle & Company
Inventors:
Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
Abstract: The present invention relates to human interleukin-3 (hIL-3) variant or mutant proteins (muteins) fused with other colony stimulating factors (CSF), cytokines, lymphokines, interleukins, hematopoietic growth factors or IL-3 variants.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
February 29, 2000
Assignee:
G. D. Searle & Company
Inventors:
S. Christopher Bauer, Mark Allen Abrams, Sarah Ruth Braford-Goldberg, Maire Helena Caparon, Alan M. Easton, Barbara Kure Klein, John P. McKearn, Peter O. Olins, Kumnan Paik, John W. Thomas