Abstract: A method and product for treating and preventing diarrhea and scours is provided. The method involves treating a subject who has diarrhea, or scours, or is at risk of getting diarrhea or scours with an aromatic compound of the invention. The products of the invention are a veterinary preparation of the aromatic compound of the invention and an anti-scours agent, and a pharmaceutical preparation of the aromatic compound of the invention and an anti-diarrheal agent.
Type:
Application
Filed:
November 8, 2002
Publication date:
June 26, 2003
Inventors:
Wayne I. Lencer, Carlo Brugnara, Seth Alper
Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
Type:
Application
Filed:
December 19, 2001
Publication date:
June 19, 2003
Inventors:
Mark E. Salvati, James Aaron Balog, Weifang Shan, Soren Giese
Abstract: This invention provides a method of treating pain in a mammal that includes administering to a mammal in need of such treatment a pain treating effective amount of a compound of the formula (I): 1
Type:
Application
Filed:
October 9, 2002
Publication date:
June 19, 2003
Applicant:
Wyeth
Inventors:
Michael Richard Brandt, Margaret Maria Zaleska, John Allen Moyer
Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
Type:
Application
Filed:
September 4, 2002
Publication date:
June 19, 2003
Inventors:
Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Harald Eschenhof, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
Abstract: Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.
Type:
Application
Filed:
April 18, 2002
Publication date:
June 12, 2003
Applicant:
Queen's University at Kingston
Inventors:
Robert Kisilevsky, Walter Szarek, Donald Weaver
Abstract: The invention provides compounds of formula
as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.
Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
Type:
Grant
Filed:
November 6, 2000
Date of Patent:
April 8, 2003
Assignee:
The Procter & Gamble Company
Inventors:
Biswanath De, Stanislaw Pikul, Menyan Cheng, Neil Gregory Almstead, Randall Stryker Matthews, Michael George Natchus, Yetunde Olabisi Taiwo
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
March 27, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: The invention relates to the use of compounds of formula (I), wherein n=0-3; R1, R2=H, alkyl, aryl, heteroaryl, acyl; R3=H, halogen, alkyl, aryl, heteroaryl, arylalkyl, acyl, CN, NO2, R4—X—; R4=H, alkyl, aryl, heteroaryl, aralkyl, acyl; X=NH, O, S, SO2, NHSO2, OSO2, and A, B, C=organic groups. The inventive compounds are used for the prophylaxis and the therapeutic treatment of infectious processes, especially of infectious processes caused by parasites. The invention further relates to medicaments that contain the inventive compounds.
Type:
Application
Filed:
August 23, 2002
Publication date:
February 20, 2003
Inventors:
Hassan Jomaa, Martin Schlitzer, Jochen Wiesner
Abstract: Maleimide and succinimide derivatives were found to be effective topoisomerase II catalytic inhibitors. Due to this property, the maleimide and succinimide derivatives were investigated for their use as cytostatic agents and thus in the treatment of cancer. The compounds of the invention can be used in combination treatments with other cytostatic agents, such as topoisomerase II poisons. The maleimide and succinimide derivatives, due to their effective topoisomerase II catalytic inhibitory activity, are also useful as extravasation agents, such as upon administration of a topoisomerase II poison.
Type:
Application
Filed:
March 29, 2002
Publication date:
February 13, 2003
Applicant:
Topo Target ApS
Inventors:
Peter Buhl Jensen, Birgitte Sokilde, Elisabeth Vang Carstensen, Seppo W. Langer, Andrew Creighton, Maxvell Sehested, Lars Hollund Jensen
Abstract: The present invention provides synthetic methods and compositions for treatment of autoimmune and anti-inflammatory disorders comprising administering an effective amount of a derivative of triptolide alone or in combination or alternation with other anti-autoimmune or anti-inflammatory compounds.
Type:
Application
Filed:
October 2, 2001
Publication date:
February 6, 2003
Inventors:
Susheng Wang, Dennis C. Liotta, James P. Snyder, Hariharan Venkatesan
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
February 6, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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:
Application
Filed:
August 23, 2002
Publication date:
February 6, 2003
Applicant:
Lahive & Cockfield, LLP
Inventors:
Walter A. Szarek, Xianqi Kong, Gregory R.J. Thatcher, Boris Gorine
Abstract: The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, and treating a wound.
Type:
Application
Filed:
March 19, 2001
Publication date:
February 6, 2003
Inventors:
Duane D. Miller, Gabor Tigyi, James T. Dalton, Vineet M. Sardar, Don B. Elrod, Huiping Xu, Daniel L. Baker, Dean Wang, Karoly Liliom, David J. Fischer, Tamas Virag, Nora Nusser
Abstract: An oxidizing species is described herein as a reaction product through an in situ preparation combining a protonizable phosphorus or sulfur compound, and a halide source at controlled proportions in an aqueous, non-aqueous, gel, aerosol, solid-phase or powdered media. The oxidizing species can be used to reduce microbial and viral populations on a surface or object or in a body or stream of water. The invention thus finds applications as a bleach, sanitizer, oxidant, or in any other application in which an oxidizing agent can be beneficially used alone or in a formulation.
Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.
Type:
Grant
Filed:
July 8, 1998
Date of Patent:
January 14, 2003
Assignee:
AnorMED, Inc.
Inventors:
Gary James Bridger, Eva Maria Boehringer, Zhongren Wang, Dominique Schols, Renato Tony Skerlj, David Earl Bogucki
Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as benzopyrone derivatives, including uses in the treatment of disease states mediated by chemokines. The relevant chemokine may for example be interleukin-8 (IL-8), and the relevant chemokine receptors may for example be corresponding chemokine receptors (CXCR-1 and/or CXCR-2). In other aspects, the invention provides corresponding pharamaceutical compositions and therapeutic methods. In one aspect, for example, the invention provides for the use of [7-[benzopyrone-5′(3′-amino)-thiazole]-phenylalanine-benyl ester in the treatment of disease.
Type:
Application
Filed:
November 13, 2001
Publication date:
January 2, 2003
Inventors:
Geeta Saxena, Christopher R. Tudan, N. Nick Cheng, Hassan Salari
Abstract: N-Heterocyclic derivatives of the formula (I): 1
Type:
Application
Filed:
April 12, 2002
Publication date:
January 2, 2003
Applicant:
Berlex Laboratories, Inc.
Inventors:
Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
Abstract: The present invention relates to peptide-like compounds, eg aminocarboxylic acid amide derivatives, and to methods of using same to stimulate cells of the immune system, bone marrow and other organs. The present compounds can be used to enhance vaccination, increase synthesis of and enhance function of blood cell components and enhance anti-neoplastic effects of various agents. The compounds of the invention can be used to produce a variety of further pharmacologic effects.
Type:
Grant
Filed:
October 7, 1999
Date of Patent:
December 24, 2002
Assignee:
Dovetail Technologies, Inc.
Inventors:
Floyd Taub, Thomas J. Perun, Christopher K. Murray, Randall J. Daughenbaugh, Daniel Lednicer
Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.
Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.
Type:
Application
Filed:
March 6, 2002
Publication date:
November 7, 2002
Inventors:
Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
Abstract: The present invention discloses highly packed polycationic ammonium, sulfonium and phosphonium lipid compounds useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Methods for their preparation and use as intracellular delivery agents are also disclosed.
Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.
Abstract: The present invention makes available methods and reagents for facilitating memory, e.g., to increase memory function such as long-term memory and recall ability. Memory is increased by increasing attention and long term consolidation.
Abstract: The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.
Type:
Application
Filed:
August 28, 2001
Publication date:
August 29, 2002
Inventors:
Carlo Brugnara, Jose Halperin, Emile M. Bellott, Mark Froimowitz, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Falguni M. Kher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
Abstract: Methods of synthesizing a phosphate ester of combretastat-in A-4 and trans-isomers thereof in which combretastatin A-4 is reacted with dibenzylphosphite in the presence of carbon tetrabromide, or with 2,2,2-trichloroethyl phosphorodichloridate, to form a phosphate ester of combretastatin A-4 with protecting groups thereon.
Type:
Application
Filed:
July 17, 2001
Publication date:
August 29, 2002
Inventors:
Faye Seyedi, Jonathan Gale, Reem Haider, John Hoare, Amy Baldwin
Abstract: Disclosed are methods and materials for visualizing or treating vasculature. The methods and materials in this invention relate to selective and non-invasive visualization, or treatment such as chemical occlusion, of vasculature in the mammalian eye. The methods utilize fluorescent dyes and tissue-reactive substances encapsulated within heat-sensitive liposomes which are subsequently heated to release the contents thereof at a pre-determined anatomical locus. The methods of this invention further utilize tissue-reactive agents which, when activated, are effective to cause localized tissue damage and occlusion of blood vessels and/or blood sinuses. The materials of this invention relate to diagnostic reagents and kits for visualizing or treating a mammalian blood vessel or sinus.
Abstract: The present invention provides compositions comprising improved beta-lactam antibiotics and methods for applying these compositions to inhibit the growth of microbial infections. The improved antibiotics are capable of inhibiting the growth of both antibiotic sensitive and antibiotic resistant microorganisms In addition, the invention provides methods for treating a subject infected with a microorganism by administering the compositions of the invention.
Type:
Application
Filed:
May 1, 2001
Publication date:
August 22, 2002
Inventors:
Ming Fai Chan, Rosario S. Castillo, Qing Li, Venkata Ramana Doppalapudi, Mark Stephen Hixon, Thomas J. Lobl
Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.
Type:
Application
Filed:
September 26, 2001
Publication date:
August 15, 2002
Inventors:
Hieu Trung Phan, Lan Mong Nguyen, Vinh Van Diep, Raymond Azoulay, Harald Eschenhof, Eric Joseph Niesor, Craig Leigh Bentzen, Robert John Ife
Abstract: The purposes of this invention are preparation of the non-mucin type synthetic compounds-carrier conjugated compounds which are stable against enzymes, and which have the ability of specific reactivity to induce immune response for cancer and HIV.
Abstract: The present invention relates to acetylenic aryl sulfonamide thiols which act as inhibitors of TNF-&agr; converting enzyme (TACE). The compounds of the present invention are useful in disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
Abstract: The present invention relates to bone-targeting compounds useful for treating a variety of disorders and conditions, e.g., of bone tissue.
Type:
Application
Filed:
December 18, 2000
Publication date:
August 1, 2002
Inventors:
Manfred Weigele, George P. Luke, Tomi K. Sawyer, Regine Bohacek, William C. Shakespeare, Rajeswari Sundaramoorthi, Yihan Wang, David C. Dalgarno, Chester A. Metcalf, Chi B. Vu, Noriyuki H. Kawahata
Abstract: The present invention makes available methods and reagents for facilitating memory, e.g., to increase memory function such as long-term memory and recall ability.
Abstract: The invention related to novel 3, 5, and/or 6 swainsonine analogues, processes for their preparation and their use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.
Type:
Application
Filed:
October 29, 2001
Publication date:
July 25, 2002
Applicant:
GlycoDesign Inc.
Inventors:
Rajan Shah, Jeremy Carver, Jose Marino-Albernas, Igor Tvaroska, Francois Daniel Tropper, James Dennis
Abstract: The present invention relates to oral compositions and methods for inhibiting bone resoprtion in a mammal while counteracting the occurrence of potentially adverse gastrointestinal effects. The compositions useful herein comprise the combination of a pharmaceutically effective amount of a nitrogen-containing bisphosphonate or a pharmaceutically-acceptable salt thereof and a pharmaceutically effective amount of an isoprenoid compound.