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Assignee: G. D. Searle & Co


Location: Skokie, IL
No. of patents: 277

1              
NumberTitleIssue Date
7141594Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
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 particula...
11/28/2006
7135489Crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl] benzenesulfonamide
A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical character...
11/14/2006
6887991Processes for preparation of 9, 11-epoxy steroids and intermediates useful therein
Processes for the preparation of 4,5-dihydro-5,7-lactone steroid compounds are provided. ...
05/03/2005
6875790Cyclic sulfone containing retroviral protease inhibitors
The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease. ...
04/05/2005
6863902Immediate release eplerenone compositions
The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials. ...
03/08/2005
6852740Pyrazole derivatives as p38 kinase inhibitors
A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein Q, R1, R2, R3 and R
02/08/2005
6689787Method of using an integrin antagonist and radiation therapy as combination therapy in the treatment of neoplasia
The present invention provides methods to treat neoplasia disorders in a mammal using a combination of radiation and an integrin antagonist....
02/10/2004
6682727Site specific ligation of proteins to synthetic particles
The present invention relates to site-specific conjugation of synthetic particles to proteins....
01/27/2004
6653098Method of producing mouse and human endostatin
Methods for producing mouse and human endostatin are disclosed. Methods for refolding and purifying endostatin from inclusion bodies expressed in bacteria and nucleic acids encoding full-length and truncated forms of endostatin are also disclosed....
11/25/2003
6632921Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myristoyl transferase as anti-infective agents
Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the...
10/14/2003
6630587Processes for preparation of 9,11-epoxy steroids and intermediates useful therein
Novel 9଱-hydroxy steroid compounds, including compounds of Formula IX ##STR1## wherein --A--A--, --B--B--, R1, R3, R8 and R9 are as defined in the specification....
10/07/2003
6617324Substituted pyrazoles as p38 kinase inhibitors
A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA ##STR1## wherein R1, R2, R3 and R4 are as described in the ...
09/09/2003
6558707Immediate release eplerenone compositions
The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials....
05/06/2003
6525059Substituted pyrazoles as p38 kinase inhibitors
A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA ##STR1## wherein R1, R 2, R3 and R4 are as described in ...
02/25/2003
6500832଱- and ଲ-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
଱- and ଲ-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease....
12/31/2002
6423713Substituted pyrazoles as p38 kinase inhibitors
A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA ##STR1## wherein R1, R2, R3 and R4 are as described in t...
07/23/2002
6410054Immediate release eplerenone compositions
The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials....
06/25/2002
6362183Aromatic sulfonyl alpha-hydroxy hydroxamic acid compounds
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 comp...
03/26/2002
6342510Treatment of inflammation and inflammation-related disorders with a combination of a cyclooxygenase-2 inhibitors and a leukotriene B4 receptor antagonist
Combinations of a cyclooxygenase-2 inhibitor and a leukotriene B4 receptor antagonist are described for treatment of inflammation and inflammation-related disorders....
01/29/2002
6323326Method of solubilizing, purifying, and refolding protein
A method of modifying protein solubility employs polyionic polymers. These facilitate the solubilization, formulation, purification and refolding of proteins especially incorrectly folded proteins and aggregated proteins. Compositions are described that a...
11/27/2001
6316496Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
Selected bis-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, ...
11/13/2001
6268392Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors
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...
07/31/2001
6265433LTA4 hydrolase inhibitors
The present invention provides compounds having the structure: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as pso...
07/24/2001
6258946Keto-Substituted Steroid Compounds
Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other compounds of Formula I ##STR1## wherein the variables are as defined by the specification....
07/10/2001
6193968Methods for using anti-଱v댣 integrin antibody
Monoclonal antibodies that recognize the ଱vଲ.sub.3 integrin receptor complex, but do not significantly bind to ଱IIbଲ.sub.IIIa, can be used in methods for treating ଱vଲ.sub.3 integrin-medi...
02/27/2001
6171588Anti-଱v댣 integrin antibody antagonists
Monoclonal antibodies that recognize the ଱v 댣 integrin receptor complex, but do not significantly bind to ଱IIbଲ.sub.IIIa, inhibit ଱vଲ.sub.3 integrin-mediated diseases....
01/09/2001
6156731Polypeptide composition for oral administration
There is disclosed a composition containing a biologically active polypeptide selected from LHRH, an LHRH analog, somatostatin and a somatostatin analog, in a therapeutically effective amount, a membrane permeability enhancing agent, and a protease enzyme...
12/05/2000
6156781Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation
A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R2 is selected from hydrido, a...
12/05/2000
6087381Pyrazole derivatives as p38 kinase inhibitors
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, R1, R2, R3 and R4 are as describ...
07/11/2000
5952210Nucleic acids and expression vectors encoding human leukotiene C4 synthase
DNAs which encode human LTC4 synthase and expression vectors comprising such DNAs are provided. DNAs encoding human LTC4 synthase may be used in assay methods of the invention for detecting LTC4 synthase inhibitors. Nuclei...
09/14/1999
5932598Prodrugs of benzenesulfonamide-containing COX-2 inhibitors
Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders....
08/03/1999
59169052,3-substituted pyridines for the treatment of inflammation
A class of substituted pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II wherein R1 is selected from hydrido, halo, alkoxy, haloalkoxy,...
06/29/1999
59088521,3,5 trisubstituted pyrazole compounds for treatment of inflammation
A class of 1,3,5-substituted pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I ##STR1## wherein R1, R2, R
06/01/1999
5892053Process for preparing 3-haloalkyl-1H-pyrazoles
An efficient synthesis of 3-haloalkyl-1H-pyrazoles, suitable for adoption in a safe, large-scale process, has been developed....
04/06/1999
5861403Purinylalkyl benzamide derivatives
The present invention relates to compounds of the formula ##STR1## wherein HET is ##STR2## m is an integer from 1 to 4; R1 and R2 are independently selected from the group consisting of linear or branched alkyl of 1 to 6 ...
01/19/1999
5859257Isoxazole compounds as cyclooxygenase inhibitors
A class of substituted isoxazolyl compounds is described for use in treating cyclooxygenase-2 related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R1, R2, and R3, are described...
01/12/1999
5831117Method of preparing retroviral protease inhibitor intermediates
Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective meth...
11/03/1998
5830917L-N6 -(1-iminoethyl) lysine derivatives useful as nitric oxide synthase inhibitors
There is disclosed a novel amino alcohol amine derivatives of L-N6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors....
11/03/1998
57565303,4-substituted pyrazoles for the treatment of inflammation
A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R1 is selected from hydrido, alkyl, alkenyl, aral...
05/26/1998
5719290Fatty acid analogs and prodrugs
Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcoho...
02/17/1998
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