Carboxamides (i.e., R-c(=o)-n, Wherein R Is A Radical Having Carbon Bonded Directly To The C(=o)-n Or Is Hydrogen And Wherein Any Substituent Attached To Nitrogen Will Be Referred To As E) Patents (Class 514/613)
Abstract: A polypeptide is identified as being functionally included in a signal transduction pathway having a biological effect. Contemplated polypeptides are different from a retinoic acid receptor, a retinoid X receptor, or a cellular retinoic acid binding protein; however, binding of the retinoid or retinoid metabolite leads to a modulation of the biological effect. In particularly contemplated methods, a retinoid or retinoid metabolite is administered to a cell or mammal in a concentration effective to modulate the biological effect.
Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
Type:
Grant
Filed:
July 28, 2000
Date of Patent:
November 25, 2003
Assignee:
Telik, Inc.
Inventors:
Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
Abstract: The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.
Type:
Application
Filed:
April 22, 2003
Publication date:
November 13, 2003
Inventors:
Meir Bialer, Ofer Spigelstein, Boris Yagen
Abstract: The present invention relates to insect repellant compositions containing, based upon the total weight of the composition, from about 6 to about 30 percent by weight of insect repellant active material having functionality selected from ester, amide, urethane or combinations thereof; from about 5 to about 30 percent by weight of alcohol, and from about 1 to about 10 percent by weight of nonionic surfactant. The compositions of the invention exhibit reduced rates of degradation of the active material in solution and are less drying and irritating to sensitive skin.
Type:
Grant
Filed:
June 3, 1998
Date of Patent:
November 11, 2003
Assignee:
Johnson & Johnson Consumer Companies, Inc.
Inventors:
Danilo L. Lambino, Kennie U. Dee, Susan M. Niemiec
Abstract: The present invention relates to novel aromatic amines of general formula (I) and to the use of these amines for the treatment of obesity, anorexia, inflammation, mental disorders an other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.
Type:
Application
Filed:
November 20, 2002
Publication date:
October 16, 2003
Inventors:
Torbjorn Lundstedt, Anna Skottner, Elisabeth Seifert, Igor Starchenkov, Peteris Trapencieris, Valerjans Kauss, Ivars Kalvins, Arne Boman
Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.
Type:
Grant
Filed:
September 26, 2002
Date of Patent:
September 16, 2003
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Inventors:
Dennis Bigg, Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jeremiah Harnett, Gérard Ulibarri
Abstract: The invention relates to a method of treating non inflammatory cartilage damage by administering a GABA analog of Formula:
and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
September 14, 2001
Date of Patent:
September 16, 2003
Assignee:
Warner-Lambert Company
Inventors:
Denis Schrier, Howard Glenn Welgus, David Juergen Wustrow
Abstract: Suspensions, emulsions or dispersions of therapeutically active agents which are water insoluble or water intolerant such as nutritional supplements, herbal products, drugs, bacteria, yeast, vitamins and minerals are prepared as suspensions in edible vegetable oils such as orange, lemon, soybean, cotton seed, peanut, canola corn oil, sunflower, safflower, palm kernel, palm and coconut. The active therapeutic agent may be in crystalline or amorphous form, it may be a liquid as for example an oil such as vitamin B or beta carotene, or a preparation of a comminuted plant structure such as flower, parts, leaf; stern, root or tree bark, or an extract of a dried plant structure or a freeze dried preparation of a vital bacteria or yeast. The suspension is formed by active mixing of the active agent and oil.
Abstract: A composition for prophylaxis and therapy of dermal aging which comprises a substance having human leukocyte elastase inhibitory activity as an active ingredient.
Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z), 14(Z)-dienoic acid and 20-, 21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z), 15(Z)-dienoic acid.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
August 12, 2003
Assignee:
MCW Research Foundation
Inventors:
Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1
Type:
Application
Filed:
January 16, 2003
Publication date:
July 31, 2003
Applicant:
Allergan Sales, Inc.
Inventors:
Robert M. Burk, Mark Holoboski, Mari F. Posner
Abstract: There are described new active compound combinations of a compound of the formula (I) 1
Type:
Application
Filed:
November 6, 2002
Publication date:
July 24, 2003
Inventors:
Klaus Stenzel, Wilhelm Brandes, Stefan Dutzmann, Bernd-Wieland Kruger, Karl-Heinz Kuck, Rolf Pontzen, Thomas Seitz, Atsumi Kamochi, Ikuya Saitoh
Abstract: The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.
Type:
Grant
Filed:
August 25, 2000
Date of Patent:
July 22, 2003
Assignee:
Sugen, Inc.
Inventors:
Ping Huang, Chung Chen Wei, Peng Cho Tang, Chris Liang, John Ramphal, Bahija Jallal, John Biltz, Sharon Li, Matt Mattson, Gerald McMahon, Marcel Koenig
Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),4(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
July 22, 2003
Assignee:
MCW Research Foundation
Inventors:
Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives.
Type:
Application
Filed:
October 29, 2002
Publication date:
July 10, 2003
Applicant:
Allergan, Inc.
Inventors:
Robert M. Burk, Mark Holoboski, Mari F. Posner
Abstract: Disclosed is a novel use of a prostaglandin compound as a chloride channel opener. According to the instant invention, chloride channels in a mammalian subject can be opened by a prostaglandin compound to facilitate chloride ion transportation.
Abstract: Bipolar lipids are described which are able to form complexes with polyanions. The lipids comprise a cationic head linked to a hydrophobic backbone and a hydrophilic tail and are capable of self assembly to form stable complexes in aqueous solutions. The lipids are of particular use for the delivery of bioactive substances such as nucleic acids to cells in vitro and especially in vivo.
Type:
Grant
Filed:
November 20, 2000
Date of Patent:
June 24, 2003
Assignee:
Celltech R & D Limited
Inventors:
Michael Anthony William Eaton, Timothy John Norman, David Parker, Terence Seward Baker, Andrew Neil Charles Weir, Catherine Fiona Catterall
Abstract: Pharmaceutical conjugates comprising a therapeutic component and an efficacy enhancing component that enhances the pharmacokinetic disposition of the therapeutic component is disclosed. In one embodiment, therapeutic component is joined to an efficacy enhancing component by a linker. In one embodiment, the therapeutic component and the efficacy enhancing component disassociate under physiolocal conditions, preferably near the site where the therapeutic component may exert a therapeutic effect.
Abstract: A hydrogel formed by adding an anion having a molecular weight of 90 or more to an aqueous dispersion of a cationic amphiphile comprising a linear or branched alkyl group having 10 or less carbon atoms in a hydrophobic moiety. The hydrogel has a network having a bilayer-membrane, nano-fiber structure and undergoes a reversible gel-sol transformation.
Abstract: A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.
Type:
Application
Filed:
July 8, 2002
Publication date:
June 5, 2003
Inventors:
Robert W. Curley,, Serena M. Mershon, Derek W. Barnett, Margaret Clagett-Dame, Jason S. Chapman
Abstract: A compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)-cyclohexane, has a renal interstitial fibrosis inhibitory action in renal interstitial fibrosis model mice and various other actions, and therefore, is useful as an agent for the prophylaxis or treatment of renal diseases.
Abstract:
Compounds I-III wherein U is CH, O, or S; Z is mono- or di-substituted carbon; R is (CH2)nCO2H, (CH2)nSO3H, (CH2)nPO3H2, (CH2)nNO2, CH(SCH3)3, esters; R1 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl; RR1 is O; n is 0-4; R2, R3 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkyl; R4 is (CH2)nOH, (CH2)nNH2, substituted alkyl were prepd. as neuraminidase inhibitors. Thus, (1R,3R,4R,1′S)-(−)-(1′-acetylamino-2 ′-ethyl)butyl-4-(aminoimino)methylaminocyclopentan-1-carboxylic acid was prepd. and tested in vitro as neuraminidase inhibitor (IC50<1.mu.M).
Type:
Grant
Filed:
May 25, 2000
Date of Patent:
May 13, 2003
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Yarlagadda S. Babu, Pooran Chand, John A. Montgomery
Abstract: The present invention relates to compounds of the formula I
in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention relates to the use of compounds of the formula I for the therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, novel compounds of the formula I, pharmaceutical preparations comprising them and processes for their preparation.
Type:
Grant
Filed:
March 8, 2001
Date of Patent:
April 15, 2003
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Type:
Grant
Filed:
May 24, 2000
Date of Patent:
April 8, 2003
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Bing-Yan Zhu, Ting Su, Zhaozhong Jon Jia, Robert M. Scarborough, Yonghong Song
Abstract: The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension. A preferred class of compounds for practicing the invention have the structure shown by Formula I
wherein Z is oxygen or sulfur, W is carbon phosphorous or sulfur, X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1-R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 is each independently C1-C20 substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, or heterocyclic.
Type:
Grant
Filed:
November 21, 2000
Date of Patent:
March 11, 2003
Assignee:
Regents of the University of California
Inventors:
Deanna L. Kroetz, Darryl C. Zeldin, Bruce D. Hammock, Christophe Morisseau
Abstract: The present invention provides compounds of Formula I shown below.
The present invention also provides methods of treating or preventing 3 inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of Formula I.
Type:
Grant
Filed:
May 15, 2001
Date of Patent:
March 4, 2003
Assignee:
Warner-Lambert Company
Inventors:
David Thomas Connor, William Howard Roark, Karen Elaine Sexton, Roderick Joseph Sorenson
Abstract: A composition formulated from a primary anionic surfactant; optionally a secondary surfactant and/or a resin; and a nitrogen-containing compound of the structural formula:
wherein R is a saturated, linear, branched or cyclic alkyl or aryl group containing 12 to 22 carbon atoms, with the proviso that R contains at least 80% of a single chain length and R is not lanolin, wheat germ or other natural broad-based chain distribution oil, R1 is a saturated or unsaturated, linear, branched or cyclic alkyl or aryl group containing 1 to 6 carbon atoms and may contain one or more hydroxyl groups, R2 is selected from the group consisting of hydrogen, methyl, ethyl and benzyl; and A− is a monovalent anion.
Type:
Grant
Filed:
October 19, 2001
Date of Patent:
February 25, 2003
Assignee:
Goldschmidt Chemical Corporation
Inventors:
Damon M. Dalrymple, Mona Manning, Frank Merz
Abstract: A purpose of the present invention is to provide TNF-&agr; production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis.
Abstract: The present invention relates to compounds and pharmaceutical compositions useful for treating pain. The invention also relates to methods of treating or alleviating pain in mammals, comprising administering to a mammal suffering from pain, a pain-alleviating amount of a compound of the general formula (I) or (II).
Type:
Grant
Filed:
June 25, 2001
Date of Patent:
February 11, 2003
Assignee:
D-Pharm Ltd.
Inventors:
Alexander Kozak, Revital Duvdevani, Firas M. Younis
Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula:
wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
Type:
Grant
Filed:
March 16, 2001
Date of Patent:
February 11, 2003
Assignee:
3-Dimensional Pharmaceuticals, Inc.
Inventors:
Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.
Type:
Grant
Filed:
June 29, 1999
Date of Patent:
February 4, 2003
Assignee:
Euro-Celtique, S.A.
Inventors:
Mark Chasin, Richard Sackler, Ronald M. Burch, Paul Goldenheim, Joseph Tigner
Abstract: Compounds of the formula:
are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.
Type:
Grant
Filed:
March 15, 2000
Date of Patent:
January 14, 2003
Assignee:
Axys Pharmaceuticals, Inc.
Inventors:
Ann M. Buysse, Rohan V. Mendonca, James T. Palmer, Zong-Qiang Tian, Shankar Venkatraman
Abstract: Disclosed is a novel class of compounds of formula (I)
wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
Type:
Grant
Filed:
May 16, 2000
Date of Patent:
January 7, 2003
Assignee:
Noro Nordisk A/S
Inventors:
Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Josef Vagner, Inge Thøger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thøgersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Shenghua Shi
Abstract: There are described a flowable composition for controlling harmful insects and representatives of the order Acarina, comprising at least one pesticidally active compound, one or more signal substances selected from the group consisting of pheromones, kairomones and attractants, a UV absorber or a UV absorber mixture and, if appropriate, one or more additives selected from the group consisting of viscosity-regulating thickeners, fillers, solvents and other formulation auxiliaries,
which composition comprises 40 to 98% by weight of the UV absorber or the UV absorber mixture,
0.01 to 30% by weight of one or more signal substance(s) and
0.1 to 20% by weight of one or more pesticidally active compound(s) of the formulae (I) to (V) as specified, and a method of controlling harmful insects and representatives of the order Acarina using this composition.
Type:
Grant
Filed:
February 22, 2001
Date of Patent:
December 31, 2002
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Dieter Hofer, Max Angst, Pierre-Joseph Charmillot
Abstract: There are described new active compound combinations of a compound of the formula (I)
with known fungicidal active compounds, and their use for combating phytopathogenic fungi.
Type:
Grant
Filed:
June 17, 2002
Date of Patent:
December 31, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Klaus Stenzel, Wilhelm Brandes, Stefan Dutzmann, Bernd-Wieland Krüger, Karl-Heinz Kuck, Rolf Pontzen, Thomas Seitz, Atsumi Kamochi, Ikuya Saitoh
Abstract: The present invention provides non-peptide organic compounds that have a structure analogous to or reminiscent of the TMOF structure and have pesticidal activity. Thus the present invention concerns pesticidal compounds that inhibit digestion in pests by terminating or otherwise blocking synthesis of digestive enzymes by activating a TMOF receptor (collectively referred to herein as “pesticidal compounds”). The pesticidal compounds and other compounds of the present invention are usefully employed in the control of pests, particularly insect pests such as mosquitoes, which ingest blood.
Type:
Application
Filed:
June 7, 2001
Publication date:
December 19, 2002
Inventors:
Russell J. Linderman, R. Michael Roe, Deborah M. Thompson, Matthew Vanderherehen
Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives.
Type:
Application
Filed:
May 24, 2002
Publication date:
December 12, 2002
Inventors:
Robert M. Burk, Mark Holoboski, Mari F. Posner
Abstract: The subject invention provides a method of treating mania in bipolar disorder in a subject comprising administering to the subject a therapeutically effective amount of derivatives of 1-aminoindan or their racemic mixtures, enantiomers, or salts, of the general formula:
wherein n is 0 or 1;
each of R1 and R2 are hydrogen, C1-C4 alkyl, halogen;
R3 is hydrogen, C1-C4 alkyl, hydroxy, C1-C4 alkoxy;
R4 is hydrogen, C1-C4 alkyl;
R6 is hydrogen, substituted or unsubstituted C1-C12 alkyl, C6-C12 aryl, C7-C12 aralkyl or A—N—R9R10, provided that R6 is not methyl when R1, R2, R3 and R4 are hydrogen atoms,
wherein A is substituted or unsubstituted C1-C12 alkyl, substituted or unsubstituted C6-C12 aryl, substituted or unsubstituted C7-C12 aralkyl, and each of R9 and R10 are independently hydrogen, C1-C12 alkyl, C6-C12 aryl, C7-C12 aralkyl, COOtBu, or indanyl;
and racemic mixtures, enantiomers, and salts thereof.
Abstract: The present invention involves the identification and use of compositions for treating myeloma bone disease. The compositions inhibit proteasomal activity and decrease the activity of the transcription factor NF-&kgr;B. Assessment of a candidate compound for its ability to inhibit production or activity of proteasomal enzymes or NF-&kgr;B provides a useful means to identify agents to treat myeloma bone disease.
Abstract: A pharmaceutical composition for parenteral delivery, comprising a retinide such as fenretinide in combination with a solvent capable of dispersing or solubilizing the retinide. The solvent comprises an alcohol, such as ethanol, in combination with an alkoxylated castor oil, such as CREMOPHOR® EL, or comprising a retinide, such as fenretinide, in an emulsion composed of a lipoid dispersed in an aqueous phase, a stabilizing amount of a non-ionic surfactant, optionally a solvent, and optionally an isotonic agent. In addition, a method of use in the treatment of hyperproliferative disorders, such as cancers is described.
Type:
Application
Filed:
December 5, 2001
Publication date:
December 5, 2002
Inventors:
Shanker Gupta, Barry J. Maurer, C. Patrick Reynolds, B. Rao Vishnuvajjala
Abstract: Disclosed is a method of selecting analgesic agents based on their selective ability to block tetrodotoxin-insensitive sodium channels, particularly in comparison to blocking tetrodotoxin-sensitive sodium channels. Also disclosed is a novel class of compounds that is selective for blocking tetrodotoxin-insensitive sodium channels.
Type:
Grant
Filed:
December 6, 1999
Date of Patent:
December 3, 2002
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
James L. Miller, George P. Miljanich, Stephen S. Bowersox, Laszlo Nadasdi
Abstract: A novel method of treating and preventing diseases is provided. In particular, compositions and methods of blocking diseases associated with aberrant levels of nitric oxide and facilitated by a serine proteolytic (SP) activity are disclosed, which consist of administering to a subject a therapeutically effective amount of a compound having a serine protease inhibitory activity. Among effective compounds are &agr;1-antitrypsin and synthetic drugs mimicking some or all of the actions of &agr;1-antitrypsin.
Type:
Grant
Filed:
March 3, 2000
Date of Patent:
December 3, 2002
Assignee:
Trustees of University of Technology Corporation
Abstract: The present invention is directed to certain novel compounds represented by structural formula I:
or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.
Type:
Grant
Filed:
September 21, 2001
Date of Patent:
November 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
Abstract: The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.
Type:
Grant
Filed:
August 20, 2001
Date of Patent:
November 5, 2002
Assignees:
Pacific Corporation, Digital Biotech Co., Ltd.
Inventors:
Jeewoo Lee, Uhtaek Oh, Young-Ho Park, Young-Ger Suh, Hyeung-Geun Park, Hee-Doo Kim