Abstract: This invention concerns the use of the compounds of formula 1
Type:
Application
Filed:
June 28, 2002
Publication date:
May 1, 2003
Inventors:
Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
Abstract: Disclosed is both a method and composition for controlling deleterious organisms, such as insects, nematodes and weeds while maintaining beneficial soil organisms, by applying a compound comprised of a liquid medium and comprising an azide and an amino acid polymer. The azide can be selected from the group consisting of sodium azide and potassium azide or a combination of the two. The composition provides an effective pesticide, without causing significant harm to the environment. The composition may be applied to soil to control a population of a deleterious organism.
Abstract: Disclosed is both a method and composition for controlling deleterious organisms, such as insects, nematodes and weeds by applying a compound comprised of a liquid medium comprising azide and amine. The azide can be selected from the group consisting of sodium azide and potassium azide or a combination of the two. The composition provides an effective pesticide, without causing significant harm to the environment. The composition may be applied to soil to control a population of a deleterious organism.
Abstract: Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
February 22, 2002
Publication date:
May 1, 2003
Applicant:
Virtual Drug Development, Inc.
Inventors:
Wayne J. Brouillette, Lawrence DeLucas, Christie Brouillette, Sadanandan E. Velu, Yong-Chul Kim, Liyuan Mou, R. Stephen Porter
Abstract: A broad class of pharmaceutical agents which react directly with electron carriers or with reactive species produced by electron transport to release a pharmacologically active molecule to effect a therapeutic functional change in the organism by a receptor or nonrecepter mediated action.
Abstract: The present invention relates to novel arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.
Type:
Application
Filed:
August 21, 2002
Publication date:
April 17, 2003
Inventors:
Joachim Mittendorf, Jurgen Dressel, Michael Matzke, Jorg Keldenich, Frank Mauler, Jean-Marie-Victor de Vry, Jurgen Franz, Peter Spreyer, Verena Vohringer, Joachim Schumacher, Michael-Harold Rock, Ervin Horvath, Arno Friedl, Klaus-Helmut Mohrs, Siegfried Raddatz, Reinhard Jork
Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
Type:
Application
Filed:
September 5, 2001
Publication date:
April 17, 2003
Inventors:
J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Siquan Sun, Kevin L. Tays, Robin L. Thumond, Jianmei Wei
Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
Type:
Application
Filed:
February 13, 2002
Publication date:
April 10, 2003
Inventors:
J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Siquan Sun, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei
Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.
Type:
Application
Filed:
October 30, 2001
Publication date:
April 3, 2003
Applicant:
Merck Frosst Canada & Co.
Inventors:
Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
Type:
Application
Filed:
September 12, 2002
Publication date:
April 3, 2003
Applicant:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: The present invention provides compositions, therapeutic combinations and methods including: (a) at least one bile acid sequestrant; and (b) at least one substituted azetidinone or substituted &bgr;-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.
Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
Type:
Application
Filed:
September 12, 2002
Publication date:
March 6, 2003
Applicant:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: Methods are provided for treatment of eye disorders and injury, including methods for treatment of reduced flow of blood or other nutrients to retinal tissue and/or optic nerve, methods for treatment of retinal ischemia and trauma and methods for treatment for optic nerve injury/damage.
Abstract: The present invention is a method of inhibiting islet cell transplant rejection particular, to treat diabetes, such as type-1 and type-2 diabetes, by administering to a subject an effective amount of a soluble CTLA4 mutant molecule. One example of soluble CTLA4 mutant molecule is L104EA29YIg.
Type:
Application
Filed:
May 23, 2002
Publication date:
January 30, 2003
Inventors:
Christian P. Larsen, Thomas C. Pearson, Andrew B. Adams
Abstract: The present invention discloses dye-azide derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and nitrene at the lesion of interest.
Type:
Application
Filed:
July 3, 2001
Publication date:
January 23, 2003
Applicant:
MALLINCKRODT INC.
Inventors:
Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
Abstract: The present invention relates to novel compounds, compositions and methods for inhibiting the growth, elaboration and/or replication of HIV in human patients and to the prevention and treatment of human acquired immunodeficiency syndrome (AIDS) and other diseases caused by retroviral infection. More particularly, in preferred aspects, the present invention provides a method for the use of novel prodrug forms of 9-(2,3-Dideoxy-&bgr;-D-glycero-pent-2-enofuranosyl)guanine (d4G) for the prevention and treatment of both wild type and drug-resistant Human Immunodeficiency Virus (HIV), the causative pathogen of AIDS.
Type:
Application
Filed:
February 5, 2002
Publication date:
January 23, 2003
Inventors:
Karen S. Anderson, Adrian Staffin Ray, Chung K. Chu, Yang Zhenjun
Abstract: The present invention discloses novel photoactive compounds that may be crosslinked to target substrates. Methods for the preparation and use of the compounds, as well as compositions comprising them, are also disclosed.
Type:
Application
Filed:
March 27, 2002
Publication date:
January 16, 2003
Inventors:
Angela M. Desjardins, David H. Dolphin, Ethan D. Sternberg
Abstract: Methods of use and pharmaceutical compositions for a genus of low molecular weight compounds comprising optionally substituted isoxazoline ring systems that act as inhibitors of MIF (macrophage migration inhibitory factor) are disclosed. Specifically, the compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases (including rheumatiod arthritis, insulin-dependent diabetes, multiple sclerosis, graft versus host disease, lupus syndromes), asthma, arthritis, ARDS, psoriasis, interleukin-2 toxicity, proliferative vascular disease, and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization (angiogenesis).
Abstract: The invention relates to methods of treating disease based upon pharmaceutical compositions, and processes for the preparation thereof, comprising zidovudine, or a derivative thereof and lamivudine, or a derivative thereof. The pharmaceutical composition is made by a wet granulation process whereby a binder is added to the zidovudine, or a derivative thereof. and lamivudine, or a derivative thereof, during the wet granulation process.
Type:
Application
Filed:
May 24, 2001
Publication date:
January 2, 2003
Inventors:
Malcolm Ross, David Caron, Tamar Gordon-Sommer
Abstract: Activated carbon, as well as compositions and kits comprising the same, are effective for preventing pregnancy and sexually transmitted diseases including HIV.
Type:
Application
Filed:
August 8, 2002
Publication date:
January 2, 2003
Applicant:
The Procter & Gamble Company
Inventors:
Richard Joseph Sunberg, Sheri Anne Hunt
Abstract: The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels and thus improve the effectiveness of treatment regimens involving these drugs. Further agents such as methotrexate and AZT can also be used in cancer and HIV-positive patients employing camptothecin drugs.
Abstract: A pharmacological composition comprises a reverse transcriptase inhibitor in a quantity sufficient to reduce a viral serum titer of a virus in an amount of at least 20% over a period of at least 6 hours, wherein preferred reverse transcriptase inhibitor comprise a plant extract.
Abstract: The invention provides a method of inhibiting tumor growth by contacting the tumor with a composition containing a taurine compound. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death.
Type:
Application
Filed:
March 15, 2002
Publication date:
December 5, 2002
Applicant:
Rhode Island Hospital
Inventors:
Paul Calabresi, Bai-Chuan Pan, James Darnowski
Abstract: The present invention relates to pharmaceutically acceptable salts of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
Abstract: The present invention discloses novel aromatic azide derivatives and their bioconjugates for phototherapy of tumors and other lesions. The organic azides of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of nitrene, the reactive intermediate produced upon photoexcitation of the aromatic azide, with the tissue of interest. The compounds of the present invention are administered to a patient, allowed to accumulate at the site of the tumor or other lesion, and are exposed to light in order to perform a phototherapeutic procedure.
Type:
Application
Filed:
January 19, 2001
Publication date:
November 14, 2002
Applicant:
Mallinckrodt Inc.
Inventors:
Raghavan Rajagopalan, Gary Cantrell, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.
Type:
Application
Filed:
June 7, 2001
Publication date:
September 19, 2002
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.
Abstract: This invention provides methods for screening a modulating agent which when combined with antitumor therapeutic agent increases apoptosis in tumor cells. This invention also provides methods for screening antitumor therapeutic agents suitable for combination therapy with a protein kinase C inhibitors capable of potentiating apoptosis in tumor cells. This invention further provides different combination therapies comprising the specific protein kinase C inhibitors and the antitumor therapeutic agents.
Type:
Grant
Filed:
August 20, 1998
Date of Patent:
September 3, 2002
Assignee:
Sloan-Kettering Institute for Cancer Research
Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
Type:
Grant
Filed:
December 22, 2000
Date of Patent:
August 20, 2002
Assignee:
Kinetek Pharmaceuticals, Inc.
Inventors:
Zaihui Zhang, Timothy Scott Daynard, Shisen Wang, Mikhail Chafeev
Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: 1
Type:
Application
Filed:
August 24, 2001
Publication date:
June 27, 2002
Inventors:
Gregory E. Agoston, Jamshed H. Shah, Kimberly A. Hunsucker, Victor S. Pribluda, Theresa M. LaVallee, Shawn J. Green, Christopher J. Herbstritt, Xiaoguo H. Zhan, Anthony M. Treston
Abstract: The invention concerns a method for inhibiting cytokine production by cells, in particular animal or human cells, and their secretion, which consists in applying on said cells at least an azo compound derivatives corresponding to formula (I), in which A represents a carboxyl or a group (a); B represents a carboxyl or a group (b); R1, R2, R3 and R4=H, Hal, OH or a hydrocarbon radical, R1 and R2 as well as R3 and R4 capable of being a heterocyclic ring; X1 and X2=O or NR5, where R5=H, Hal, a hydrocarbon radical or a nitro group.
Type:
Grant
Filed:
October 13, 2000
Date of Patent:
June 18, 2002
Assignee:
Previsan AG
Inventors:
Michel Goldman, Hélène Margery, Patrick Adelin Oscar Robberecht, Jean Pierre Robert Tassignon, Michel Vandevelde