Abstract: Inhibitors of phosphoserine- or posphothreonine-specific peptidyl prolyl isomerases are described. Such inhibitors include molecules that mimic the structure and conformation of the pSer/pThr-Pro peptide moiety of the isomerase substrate when the substrate is bound into the active site of the isomerase. For example, a protein, peptide or peptide mimetic including xSer/ThrY where x is a negatively charged tetra or pentavalent moiety and Y is a Pro or a Pro analog. Methods of inhibiting cell growth and methods of identifying phosphoserine- or phosphothreonine-proline specific peptidyl-prolyl isomerase inhibitors are also included in the invention.
Type:
Grant
Filed:
December 11, 1997
Date of Patent:
October 8, 2002
Assignees:
Max-Planck-Gesellschaft zur Forderung der, Beth Israel Deaconess Medical Center
Inventors:
Kun Ping Lu, Lewis Cantley, Michael Yaffe, Gunter Fischer
Abstract: Aryl alkenamides derivatives of Formula I or a pharmaceutically acceptable salt thereof are novel MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection
where
V═O,S, NH or a bond;
Ar can be unsubstituted or substituted benzimidazole, phenyl, biphenyl, pyridyl, naphthyl, quinoline or isoquinoline. The other meanings for the terms are recited in the specification below.
Type:
Grant
Filed:
August 12, 1997
Date of Patent:
October 1, 2002
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Richard John Booth, Kenneth Gordon Carson, David Thomas Connor, Roberta Ellen Glynn, Bruce David Roth, Charles F. Schwender, Bharat Kalidas Trivedi, Paul Charles Unangst
Abstract: A method of cleaning or protecting surfaces by treatment with compositions comprising N-(3-oxododecanoyl)-L-homoserine lactone (OdDHL) blocking compounds and/or N-butyryl-L-homoserine lactone (BHL) analogs, either in combination or separately.
Abstract: The invention relates to methods and compositions for manipulating bacterial resistance to non-antibiotic antibacterial compositions, disinfectants and organic solvents. The invention provides methods for rendering bacterial cells susceptible to non-antibiotic antibacterial compositions. Also provided are methods to reduce the selection of bacterial mutants having an multiple antibiotic resistance phenotype by non-antibiotic antibacterial compositions. The invention also provides methods for testing the ability of non-antibiotic antibacterial compositions to select for or induce a multiple antibiotic resistance phenotype in bacteria. Also provided are methods for increasing or decreasing bacterial tolerance to organic solvents by increasing or decreasing the activity of bacterial organic solvent efflux pumps. Compositions useful in the foregoing methods are also provided.
Abstract: Therapeutic compounds and methods for modulating amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is modulated by the administration to a subject of an effective amount of a therapeutic compound comprising a phosphonate group and a carboxylate group, a congener thereof, or a pharmaceutically acceptable salt or ester thereof. In preferred embodiments, an interaction between an amyloidogenic protein and a basement membrane constituent is modulated.
Type:
Grant
Filed:
May 17, 2001
Date of Patent:
August 27, 2002
Assignee:
Queen's University at Kingston
Inventors:
Walter A. Szarek, Xianqi Kong, Gregory R. J. Thatcher, Boris Gorine
Abstract: Methods for increasing Schwann cell survival are disclosed. The methods of the invention are useful for the treatment of conditions such as peripheral neuropathies, including diabetic neuropathies.
Abstract: The invention relates to novel oxazinones designed to bind to the penicillin receptor, methods of synthesizing the compounds, and the use of the compounds as antibacterial agents. The compounds have the general formula (I)
Preferably the compounds have a carboxyethyl or a substituted carboxymethyl substituent at the 2-position and a hydroxyl group at the 5-position and have a molecular shape suitable for binding to and reacting with the active site of a pencillin-recognizing enzyme. The compounds are synthesized by condensing a carboxyl-protected N-hydroxy amino acid with a 3-hydroxyprotected-4-bromobutanoic acid to form a a doubly protected N-hydroxy N-acylamino acid, which is cyclized with an organic base to yield a doubly protected 1,2-oxazin-3-one. The protecting groups are then removed to provide an antibacterial agent.
Type:
Grant
Filed:
June 22, 1998
Date of Patent:
June 4, 2002
Assignee:
Simon Fraser University
Inventors:
Saul Wolfe, Christiana Akuche, Stephen Ro
Abstract: An isolated and cloned region of a bacterial chromosome containing a multiple antibiotic resistance operon is disclosed. A description of the structure and function of the operon is provided as are assorted recombinant DNA constructs involving the operon or fragments thereof. The diagnostic, therapeutic and experimental uses of these constructs are also disclosed. Methods of evaluating the antibiotic effectiveness of compositions are disclosed and methods of treatment employing effective compositions are provided.
Abstract: A polymethacrylate or other bone cement composition having analgesic properties is described. Bone cements containing up to 5% by weight of a local anaesthetic agent, such as lidocaine, have been demonstrated to elute sufficient lidocaine to provide an analgesic effect in vivo.
Abstract: Benzimidazole derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders
wherein A is N or CH;
where W, X, Y, and Z can be independently C—R2, C—R3, C—R4, C—R5, or N;
no more than two of W, X, Y, and Z can be N in any one structure,
R2, R3, R4, and R5 are as define in the specification.
Type:
Grant
Filed:
October 27, 2000
Date of Patent:
February 19, 2002
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
David Thomas Connor, Shelly Ann Glase, Terri Stoeber Purchase, Bruce David Roth, Bharat Kalidas Trivedi
Abstract: The instant methods and compositions represent an advance in controlling drug resistance in microbes. AcrAB-like efflux pumps have been found to control resistance to drugs, even in highly resistant microbes. Accordingly, methods of treating infection, methods of screening for inhibitors of AcrAB-like efflux pumps, and methods of enhancing antimicrobial activity of drugs are provided. Pharmaceutical composition comprising an inhibitor of an AcrAB-like efflux pump and an antimicrobial agent are also provided.
Abstract: Autoinducer compounds which enhance gene expression in a wide variety of microorganisms, therapeutic compositions and therapeutic methods wherein gene expression within microorganisms is regulated are disclosed.
Type:
Grant
Filed:
June 18, 1998
Date of Patent:
January 8, 2002
Assignee:
The Research & Development Institute, Inc.
Abstract: Therapeutic compounds and methods for modulating amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is modulated by the administration to a subject of an effective amount of a therapeutic compound comprising a phosphonate group and a carboxylate group, a congener thereof, or a pharmaceutically acceptable salt or ester thereof. In preferred embodiments, an interaction between an amyloidogenic protein and a basement membrane constituent is modulated.
Type:
Grant
Filed:
April 8, 1999
Date of Patent:
December 11, 2001
Assignees:
Neurochem, Inc., Queen's University At Kingston
Abstract: The instant invention is a series of compounds which are MCP-1 receptor antagonists of Formula I
Also included in the invention are intermediates and processes for the preparation of the compounds as well as methods of using the compounds as agents for the treatment of atherosclerosis, chronic and acute inflammatory disease, chronic and acute immune disorders and transplant rejection as well as for preventing infection by HIV, treating infection by HIV, delaying the onset of AIDS, or treating AIDS.
Type:
Grant
Filed:
April 25, 2000
Date of Patent:
November 13, 2001
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Larry Don Bratton, Steven Robert Miller, Bruce David Roth, Bharat Kalidas Trivedi, Paul Charles Unangst
Abstract: Therapeutic compounds and methods for inhibiting a glycosaminoglycan (GAG)-associated molecular interaction in a subject, whatever its clinical setting, are described.
Type:
Grant
Filed:
July 27, 1999
Date of Patent:
October 30, 2001
Assignees:
Queen's University at Kingston, Neurochem, Inc.
Inventors:
Robert Kisilevsky, Allan M. Green, Francine Gervais
Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and epileptogenesis. Methods for preparing the compounds of the invention are also described.
Type:
Grant
Filed:
March 11, 1998
Date of Patent:
October 23, 2001
Assignee:
Queen's University at Kingston
Inventors:
Donald E. Weaver, Paul H. Milne, Christopher Y. K. Tan, John R. Carran
Abstract: The present invention provides for the use of aminoguanidines for prophylactic and/or therapeutic treatments of undesirable cell growth, e.g. tumors. The present invention provides methods of using aminoguanidines, optionally in combination with a hyperplastic inhibitory agent, to inhibit the growth of undesirable cells in a subject. The present invention is based, at least in part, on the discovery that aminoguanidines inhibit cell growth. The present invention further pertains to compositions for inhibiting undesirable cell growth in a subject. The compositions of the present invention include an effective amount of the aminoguanidine in a pharmaceutically acceptable carrier. Other aspects of the invention include a packaged aminoguanidine. The packaged compound includes instructions for using the aminoguanidine compound for inhibiting undesirable cell growth in a patient or instructions for using the compound in selected quantities, in a pharmaceutically acceptable carrier.
Abstract: Methods for controlling growth of gram negative bacteria, such as Helicobacter pylori, which are agents associated with disorders of the gastrointestinal tract of a mammal are described. They include administering a therapeutically effective amount of a polyether ionophore antibiotic to a mammal, such that growth of gram negative bacteria which are agents associated with disorders of the gastrointestinal tract of a mammal is controlled. Packaged pharmaceutical compositions for controlling gram negative bacteria are also described.
Type:
Grant
Filed:
November 30, 1999
Date of Patent:
August 7, 2001
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Barry Berkowitz, George Sachs, Chris Blackburn
Abstract: An entomopathogenic fungus virulent against insects of the grasshopper family is described. The entomopathogenic fungus is a strain Beauveria bassiana. Also, formulations that include the entomopathogenic fungus are described. These formulations can be delivered to grasshopper-infested areas by land or by air. In addition, methods of killing an insect of the grasshopper family using the aforementioned formulation and baits and traps for killing an insect of the grasshopper family containing the formulation are described.
Type:
Grant
Filed:
April 15, 1999
Date of Patent:
July 17, 2001
Assignee:
Mycotech Corporation
Inventors:
Clifford A. Bradley, Pauline P. Wood, James Britton