Chalcogen Or Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/470)
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Patent number: 6610652Abstract: Methods for treating vascular conditions associated with localized imbalance in vascular tone, which are hypothesized to be largely due to elevated endothelin (ET) are provided. The methods involve administration of nitric oxide (NO), agents which are able to provide NO, such as NO donors, agents which activate guanyl cyclase, such as YC-1, or agents which prolong the actions of endogenous NO or cyclic guanosine monophosphate (cGMP; a 2nd messenger molecule), such as phosphodiesterase (PDE) inhibitors. According to the invention, such agents are administered in minimal doses or microdoses by any route known in the art, so as to provide dosages which are about one half to about one twentieth (½ to {fraction (1/20)}) of those known to induce vasodilation in “normal” circulations.Type: GrantFiled: March 8, 2002Date of Patent: August 26, 2003Assignee: Queen's University at KingstonInventors: Michael A. Adams, Jeremy P. W. Heaton, James D. Banting
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Patent number: 6610687Abstract: The invention relates to benzofuranylsulfonates of the general formula (I), their preparation and their use for the treatment of inflammation.Type: GrantFiled: February 25, 2002Date of Patent: August 26, 2003Assignee: Bayer AktiengesellschaftInventors: Gabriele Bräunlich, Mazen Es-Sayed, Rüdiger Fischer, Burkhard Fugmann, Rolf Henning, Stephan Schneider, Michael Sperzel, Karl-Heinz Schlemmer, Graham Sturton, Mary F. Fitzgerald, Barbara Briggs, Arnel Concepcion, William Bullock
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Publication number: 20030158253Abstract: This invention provides O-&agr;-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I): 1Type: ApplicationFiled: December 10, 2002Publication date: August 21, 2003Applicant: WyethInventors: John P. Yardley, Magid A. Abou-Gharbia, John W. Ullrich
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Publication number: 20030147960Abstract: This invention relates to an ionic antimicrobial coating. Such a coating may contain (1) a water-insoluble polymer having a first ionized group and (2) an antimicrobial agent having a second ionized group with a charge opposite to that of the first ionized group, in which the antimicrobial agent is attached to the water-insoluble polymer via an ionic bond between the first ionized group and the second ionized group.Type: ApplicationFiled: February 21, 2003Publication date: August 7, 2003Inventors: Tung-Liang Lin, Min-Shyan Sheu
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Publication number: 20030139434Abstract: The invention relates to a combination which comprises a DPP-IV inhibitor and at least one further antidiabetic compound, preferably selected from the group consisting of insulin signalling pathway modulators, like inhibitors of protein tyrosine phosphatases (PTPases), non-small molecule mimetic compounds and inhibitors of glutamine-fructose-6-phosphate amidotransferase (GFAT), compounds influencing a dysregulated hepatic glucose production, like inhibitors of glucose-6-phosphatase (G6Pase), inhibitors of fructose-1,6-bisphosphatase (F-1,6-BPase), inhibitors of glycogen phosphorylase (GP), glucagon receptor antagonists and inhibitors of phosphoenolpyruvate carboxykinase (PEPCK), pyruvate dehydrogenase kinase (PDHK) inhibitors, insulin sensitivity enhancers, insulin secretion enhancers, &agr;-glucosidase inhibitors, inhibitors of gastric emptying, insulin, and &agr;2-adrenergic antagonists, for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of conditions mediatedType: ApplicationFiled: October 10, 2002Publication date: July 24, 2003Inventors: Bork Balkan, Thomas Edward Hughes, David Grenville Holmes, Edwin Bernard Villhauer
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Patent number: 6589970Abstract: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: Wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, hydroxy, phenyl-(CH2)0-6—, phenyl-(CH2)0-6O—, C3-C6 cycloalkyl, —(CH2)—C3-C6 cycloalkyl, halogen, C1-C3 perflouroalkyl and C1-C3 perfluoroalkoxy where phenyl can be substituted with from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl or trifluoromethoxy; R1 is hydrogen, C1-C6 alkyl or phenyl-(CH2)1-6— where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R2 and R3 are H, C1-C6 alkyl, phenyl-(CH2)0-3—, halo and C1-C3 perfluType: GrantFiled: June 13, 2002Date of Patent: July 8, 2003Assignee: WyethInventors: Thomas Joseph Commons, Susan Christman Croce, Richard Page Woodworth, Eugene John Trybulski, Hassan Mahmoud Elokdah, David LeRoy Crandall
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Patent number: 6586604Abstract: The present invention relates to a compound having a tricyclic amine substituent which may have various substituents, the compound being represented by formula (I), a salt or hydrate thereof, and a hydrate of the salt and a drug containing them as an active ingredient. They exhibit excellent antimicrobial activity against Gram negative bacteria and Gram positive bacteria with a satisfactory fate and safety and are useful in the treatment of infectious diseases.Type: GrantFiled: June 8, 2001Date of Patent: July 1, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Kenichi Kimura, Rie Miyauchi, Hitoshi Ohki, Katsuhiro Kawakami
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Publication number: 20030119899Abstract: Disclosed herein is a method for making compounds that are useful as caspase inhibitor prodrugs of formula I: 1Type: ApplicationFiled: August 28, 2002Publication date: June 26, 2003Inventors: Marion W. Wannamaker, Cornelia Forster
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Publication number: 20030109578Abstract: N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.Type: ApplicationFiled: May 24, 2002Publication date: June 12, 2003Inventors: Gabriele Braunlich, Rudiger Fischer, Mazen Es-Sayed, Rolf Henning, Michael Sperzel, Karl-Heinz Schlemmer, Ulrich Nielsch, Stephen Tudhope, Graham Sturton, Trevor S. Abram, Mary F. Fitzgerald
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Patent number: 6573295Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.Type: GrantFiled: November 21, 2001Date of Patent: June 3, 2003Assignee: Ariad Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Michael G. Yang, Rajeswari Sundaramoorthi, Regine Bohacek, Charles Joseph Eyermann, Tomi K. Sawyer
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Patent number: 6548086Abstract: Pharmaceutical composition and a method useful for treating immunodeficiency in animals or human beings, said composition comprising effective amount of the extract obtained from any part of plant Cryptolepis buchanani, either as such or its individual constituents singly or in composition with each other, optionally associated with pharmaceutically acceptable additives.Type: GrantFiled: December 18, 2001Date of Patent: April 15, 2003Assignee: Council of Scientific and Industrial ResearchInventors: Rakesh Maurya, Anpurna Kaul, Sarang Bani, Usha Zutshi, Anamika Khajuria, Ajit Kumar Saxena, Lila Ram Manahas, Ashwani Kumar, Bal Krishnan Kapahi, Om Parkash Suri, Gulam Nabi Qazi
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Publication number: 20030068302Abstract: The present invention relates to optimal compositions useful in treating HCV infections in humans.Type: ApplicationFiled: August 28, 2001Publication date: April 10, 2003Inventors: Pravin Chaturvedi, Ene Ette
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Publication number: 20030055104Abstract: A composition for removal of lice ova or nits from the hair of human subjects comprises about 1-50% by weight of dimethylisosorbide (DMI) in an aqueous vehicle having a neutral to acidic pH. The composition is preferably in the form of a gel or a liquid shampoo, the shampoo preferably including an active pediculicidal or ovicidal agent. A method of removing lice ova from human hair comprises the application of the novel composition to the hair and subsequent removal thereof, e.g., by rinsing with water. Any unremoved ova can be physically dislodged by combing. The composition can also be included with a fine tooth nit comb in a kit for removal of lice ova from human hair.Type: ApplicationFiled: July 29, 2002Publication date: March 20, 2003Inventors: Serap Ozelkan, Zegong Zhang, Vyacheslav Malayev
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Publication number: 20030046718Abstract: Transgenic animals that do not express functional SR-BI and ApoE develop severe atherosclerosis, by age four weeks in transgenic mice. Moreover, these animals exhibit progressive heart dysfunction by as early as age four weeks, and die by age nine weeks. This animal model has now been demonstrated to be useful as a screen for compounds which alleviate the symptoms of atherosclerosis and heart disease. Animals (Apo E−/− SR-BI +/−) were fed PROBUCOL beginning at the time of mating. Offspring are weaned at three weeks and fed PROBUCOL. In contrast to animals (Apo E−/− SR-BI −/−) not fed PROBUCOL, 50% of whom are dead at six weeks, all animals (Apo E−/− SR-BI −/−) on PROBUCOL have a normal phenotype (MRI of heart function, ECG, echocardiogram, histology) at six weeks. At seven to eight months, there is evidence of atherosclerosis and some myocardial infarction. This demonstrates that the compound has a preventative action.Type: ApplicationFiled: May 16, 2002Publication date: March 6, 2003Applicant: Massachusetts Institute of TechnologyInventors: Monty Krieger, Anne Braun, Helena E. Miettinen
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Patent number: 6524623Abstract: A therapeutic composition and a method of using the composition are provided. The composition includes an osmotic agent and an active agent. The osmotic agent improves the delivery of the active agent to the targeted tissue site.Type: GrantFiled: August 7, 2000Date of Patent: February 25, 2003Inventor: Milton Hodosh
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Patent number: 6524604Abstract: A composition for removal of lice ova or nits from the hair of human subjects comprises about 1-50% by weight of dimethylisosorbide (DMI) in an aqueous vehicle having a neutral to acidic pH. The composition is preferably in the form of a gel or a liquid shampoo, the shampoo preferably including an active pediculicidal or ovicidal agent. A method of removing lice ova from human hair comprises the application of the novel composition to the hair and subsequent removal thereof, e.g., by rinsing with water. Any unremoved ova can be physically dislodged by combing. The composition can also be included with a fine tooth nit comb in a kit for removal of lice ova from human hair.Type: GrantFiled: July 21, 2000Date of Patent: February 25, 2003Assignee: Del Laboratories, Inc.Inventors: Serap Ozelkan, Zegong Zhang, Vyacheslav Malayev
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Patent number: 6518291Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: September 14, 1999Date of Patent: February 11, 2003Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
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Publication number: 20030027846Abstract: 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; 1Type: ApplicationFiled: August 26, 2002Publication date: February 6, 2003Applicant: Allergan Sales, Inc.Inventors: David W. Old, Robert M. Burk
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Patent number: 6515020Abstract: A pharmaceutical product which comprises admixed or separately packaged (A) L-Carnitine or an alkanoyl L-canitine and (B) a trihydroxy- or tetrahydroxystilbene such as resveratrol is useful for the prevention and treatment of pathological neuronal or cerebral disorders.Type: GrantFiled: March 30, 2001Date of Patent: February 4, 2003Assignee: Sigma-Tau HealthScience S.p.A.Inventor: Claudio Cavazza
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Patent number: 6514979Abstract: Synergistic combinations of guanosine nucleoside analog reverse transcriptase inhibitors such as abacavir with inosine monophosphate dehydrogenase inhibitors such as mycophenolates, pharmaceutical compositions comprising such combinations, and therapeutic methods comprising administering the synergistic combinations to subjects in need thereof, for treating a viral infection, such as an HIV-1 infection.Type: GrantFiled: March 3, 1999Date of Patent: February 4, 2003Assignee: University of Maryland Biotechnology InstituteInventors: David Margolis, Alonso Heredia, David Oldach, Robert Redfield
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Publication number: 20030017190Abstract: The present invention provides improved devices and methods for minimizing and/or inhibiting restenosis and hyperplasia after intravascular intervention. In particular, the present invention provides luminal prostheses which allow for programmed and controlled mycophenolic acid delivery with increased efficacy to selected locations within a patient's vasculature to inhibit restenosis. An intraluminal delivery prosthesis may comprise an expansible structure and means on or within the structure for releasing mycophenolic acid at a rate selected to inhibit smooth muscle cell proliferation.Type: ApplicationFiled: September 11, 2002Publication date: January 23, 2003Applicant: Avantec Vascular CorporationInventors: Motasim Sirhan, John Yan
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Publication number: 20030013758Abstract: This invention describes the novel use of alkyl, alkoxyl, halogenyl, or hydroxy substituted dicinnamoylquinides as therapeutic agents for enhancing adenosine levels in the brain and peripheral organs. These agents are particularly useful in treating human diseases or conditions that benefit from acute or chronic elevated levels of adenosine, such as reperfusion injury, coronary or cerebral ischemia, coronary vasoconstriction, paroxysmal supraventricular tachycardia, hypertension, wound healing, diabetes, inflammation, or sleep disturbances. They can also be used to protect normal cells from chemotoxicity in patients undergoing cancer therapy, and reverse the behavioral effects of caffeine intake.Type: ApplicationFiled: May 10, 2002Publication date: January 16, 2003Inventors: Tomas de Paulis, David M. Lovinger, Peter R. Martin
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Publication number: 20030013717Abstract: The invention provides a COX-2 inhibitor or a pharmaceutically acceptable derivative thereof for use in the treatment of constipation.Type: ApplicationFiled: July 25, 2002Publication date: January 16, 2003Inventors: Allen Wyane Mangel, Alan Naylor
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Publication number: 20030008898Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: 1Type: ApplicationFiled: May 3, 2002Publication date: January 9, 2003Inventors: Siavosh Mahboobi, Sabine Kuhr, Herwig Pongratz, Alfred Popp, Harald Hufsky, Frank-D Bohmer, Steffen Teller, Andrea Uecker, Thomas Beckers
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Patent number: 6503942Abstract: This invention provides O-&agr;-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I): wherein: the configuration at the steriogenic center (*) may be R, S, or RS (the racemate); R1 is selected from C1-C6 alkyl, C1-C6 alkoxy, C3-C6 cycloalkyl, or the moiety: R2 is selected from H, or C1-C6 alkyl; or, R1 and R2 may be concatenated such that form a moiety having formula (b): R3 is selected from H or C1-C6 alkyl; and R4 and R5 are independently selected from H, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 thioalkoxy, —CN, —OH, —CF3, —OCF3, halogen, —NH2, —NO2, or mono or dialkylamino wherein each alkyl group has 1 to 6 carbon atoms, or pharmaceutically acceptable salts or hydrates thereof, R, S, or RS forms thereof; as well as pharmaceutical compositions and methods treating central nervous system disoType: GrantFiled: November 21, 2001Date of Patent: January 7, 2003Assignee: WyethInventors: John P. Yardley, Magid A. Abou-Gharbia, John W. Ullrich
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Patent number: 6492374Abstract: The present invention relates to benzofuran derivatives having general Formula (I) wherein A is selected from (1), (2), (3), (4) wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C26-alkynyl, C1-6-alkyl-aryl, or C1-6-alkyl-O-aryl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; its enantiomers, and pharmaceutically acceptable acid addition salt thereof. The compounds are potently binding to the 5-HT1A receptor.Type: GrantFiled: June 4, 2001Date of Patent: December 10, 2002Assignee: H. Lundbeck A/SInventors: Kim Andersen, Mario Rottländer, Klaus Peter Bøgesø, Henrik Pedersen, Thomas Ruhland, Robert Dancer
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Patent number: 6489365Abstract: Compounds of the formula which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.Type: GrantFiled: January 18, 2000Date of Patent: December 3, 2002Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Frank Himmelsbach, Franz Birke, Armin Fugner
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Patent number: 6489357Abstract: The subject invention relates the use of cembranoids to inhibit nicotine addiction at the behavioral level. The subject host is sensitized to nicotine. Cembranoids are then administered to reduce such sensitization.Type: GrantFiled: October 21, 2000Date of Patent: December 3, 2002Assignees: University of Puerto Rico, Universidad Central del Caribe BayamònInventors: Vesna A. Eterovic, Pedro A. Ferchmin, Richard M. Hann, One R. Pagan, Abimael D. Rodriguez, Osvaldo Rosario
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Patent number: 6472406Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 5, 2000Date of Patent: October 29, 2002Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 6469054Abstract: 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: GrantFiled: February 16, 2001Date of Patent: October 22, 2002Assignee: Bayer AktiengesellshaftInventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Frank Mauler, Jean-Marie-Victor de Vry, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schumacher, Michael-Harold Rock, Ervin Horvàth, Arno Friedl, Klaus-Helmut Mohrs, Siegfried Raddatz, Reinhard Jork
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Patent number: 6465508Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: February 23, 2001Date of Patent: October 15, 2002Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
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Patent number: 6465463Abstract: The present invention provides methods or treating and preventing mortality associated with heart failure in an African American patient with hypertension and improving oxygen consumption, quality of life and exercise tolerance by administering a therapeutically effective amount of at least one hydralazine compound and at least one of isosorbide dinitrate and isosorbide mononitrate, and, optionally, one or more compounds, such as, for example, a digitalis, a diuretic compound, or a compound used to treat cardiovascular diseases. In the present invention, the hydralazine compound is preferably hydralazine or a pharmaceutically acceptable salt thereof. Preferred methods of the invention comprise administering hydralazine or a pharmaceutically acceptable salt thereof and isosorbide dinitrate.Type: GrantFiled: September 8, 2000Date of Patent: October 15, 2002Assignee: NitroMed, Inc.Inventors: Jay N. Cohn, Peter Carson
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Patent number: 6462074Abstract: The present invention relates to novel substituted (&agr;,&bgr;-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.Type: GrantFiled: July 14, 2000Date of Patent: October 8, 2002Assignee: Bayer AktiengesellschaftInventors: Andreas Stolle, Horst-Peter Antonicek, Stephen Lensky, Arnd Voerste, Thomas Müller, Jörg Baumgarten, Karsten von dem Bruch, Gerhard Müller, Udo Stropp, Ervin Horváth, Jean-Marie-Viktor de Vry, Rudy Schreiber
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Patent number: 6462055Abstract: Compounds having the formula: wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W-Y-(CH2)n-Z provided that at least one of R1-R5 is not hydrogen; or R1 and R2 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 memberedType: GrantFiled: April 30, 2001Date of Patent: October 8, 2002Assignee: WyethInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 6458825Abstract: Compounds related to lactacystin and lactacystin lactone, pharmaceutical compositions containing the compounds, and methods of use.Type: GrantFiled: August 15, 2000Date of Patent: October 1, 2002Assignee: President and Fellows of Harvard CollegeInventors: Gabriel Fenteany, Timothy F. Jamison, Stuart L. Schreiber, Robert F. Standaert
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Publication number: 20020132764Abstract: A pharmaceutical composition useful in the treatment or prevention of transgenic xenograft rejection comprising immunosuppressant compounds selected from the group consisting of an IL-2 transcription inhibitor and immunosuppressant compounds that immunosuppress for B-cell-mediated or antibody-mediated rejection of xenografts, and pharmaceutically acceptable diluents or carriers, and a method of preventing hyperacute rejection, reducing early graft damage, improving early xenograft function and promoting long term survival of said transgenic xenografts comprising the steps of i) contacting the body fluid removed from a human recipient with a xenoantigenic material which is bound to a biocompatible solid support, ii) reintroducing the treated body fluid into the recipient, and iii) treating the recipient with said pharmaceutical composition.Type: ApplicationFiled: November 7, 2001Publication date: September 19, 2002Inventors: Hendrik J. Schuurman, Emanuele Luigi Cozzi, Francoise Richard, Guy Taccard, David James Graham White, Peter John Friend, John Wallwork, Paolo Brenner
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Patent number: 6451844Abstract: The use of menthyl 2-pyrrolidone-5-carboxylate as an insect repellent, usually by application to a substrate or into an air space. The menthyl 2-pyrrolidone-5-arboxylate can be used as a composition, which may be perfumed. A useful composition comprises a mixture of menthyl 2-pyrrolidone-5-arboxylate and a known insect repellent or a compound shown to be an effective insect repellent on a test described herein.Type: GrantFiled: March 16, 2001Date of Patent: September 17, 2002Assignee: Quest International BVInventors: Stephen D Watkins, Maxine J Hills, Richard A Birch
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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Publication number: 20020128205Abstract: Patients needing NO donor therapy or inhibition of pathologically proliferating cells or increased NO bioactivity are treated with a therapeutically effective amount of an inhibitor of glutathione-dependent formaldehyde dehydrogenase.Type: ApplicationFiled: January 11, 2001Publication date: September 12, 2002Applicant: DUKE UNIVERSITY Office of Science and TechnologyInventors: Jonathan S. Stamler, Limin Liu, Alfred Hausladen, Raphael Nudelman
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Patent number: 6444682Abstract: Nucleotide or base analogues having structure (3) or (4) wherein X═O or NH or S and each R6 is independently H or alkyl or alkenyl or alkoxy or aryl or a reporter moiety.Type: GrantFiled: April 18, 2000Date of Patent: September 3, 2002Assignee: Nycomed Amersham PLCInventors: Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
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Publication number: 20020114823Abstract: The present invention provides improved devices and methods for minimizing and/or inhibiting restenosis and hyperplasia after intravascular intervention. In particular, the present invention provides luminal prostheses which allow for programmed and controlled mycophenolic acid delivery with increased efficacy to selected locations within a patient's vasculature to inhibit restenosis. An intraluminal delivery prosthesis may comprise an expansible structure and means on or within the structure for releasing mycophenolic acid at a rate selected to inhibit smooth muscle cell proliferation.Type: ApplicationFiled: February 13, 2001Publication date: August 22, 2002Inventors: Motasim Sirhan, John Yan
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Patent number: 6436447Abstract: Disclosed is an evacuant possessing a sufficient evacuating effect in a small dose substantially without accompanying any irritation to bowel, irrespective of whether its preparations are in the form of tablets, liquids or elixirs, and having a suppressing action to odor of feces. This evacuant is characterized by containing an active magnesium oxide which has a BET value (surface area in terms of m2/g) of at least 21, preferably 21-50, more preferably 30-40 and is excellent in acid reactivity, and may preferably be incorporated with lactic acid bacteria, a mixture of sporolactobacteria and yeast extracts and/or oligosaccharides. The preparations are preferably in the form of liquids, granules, tablets and capsules.Type: GrantFiled: November 23, 1999Date of Patent: August 20, 2002Assignee: Fujix, Inc.Inventors: Ranko Inoue, Takeshi Inoue, Seiichi Yamagiwa
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Patent number: 6433004Abstract: The present invention relates to novel substituted &bgr;,&ggr;-fused lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.Type: GrantFiled: July 14, 2000Date of Patent: August 13, 2002Assignee: Bayer AktiengesellschaftInventors: Andreas Stolle, Horst-Peter Antonicek, Stephen Lensky, Arnd Voerste, Thomas Müller, Jörg Baumgarten, Karsten von dem Bruch, Gerhard Müller, Udo Stropp, Ervin Horváth, Jean-Marie-Viktor de Vry, Rudy Schreiber
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Patent number: 6433005Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —C(O)—, —O—, —S—, —S(O)—, or —S(O)2— and the other substituents are as defined in the specification; or prodrugs, individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: December 3, 2001Date of Patent: August 13, 2002Assignee: Syntex (U.S.A.) LLCInventors: Kevin L. McLaren, David Bernard Smith, Jahari Laurant Tracy
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Publication number: 20020107280Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: 1Type: ApplicationFiled: December 3, 2001Publication date: August 8, 2002Inventors: Kevin L. McLaren, David Bernard Smith, Jahari Laurant Tracy
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Patent number: 6423683Abstract: Methods for treating vascular conditions associated with localized imbalance in vascular tone, which are hypothesized to be largely due to elevated endothelin (ET) are provided. The methods involve administration of nitric oxide (NO), agents which are able to provide NO, such as NO donors, agents which activate guanyl cyclase, such as YC-1, or agents which prolong the actions of endogenous NO or cyclic guanosine monophosphate (cGMP; a 2nd messenger molecule), such as phosphodiesterase (PDE) inhibitors. According to the invention, such agents are administered in minimal doses or microdoses by any route known in the art, so as to provide dosages which are about one half to about one twentieth (½ to {fraction (1/20)}) of those known to induce vasodilation in “normal” circulations.Type: GrantFiled: July 11, 2000Date of Patent: July 23, 2002Assignee: Queens University at KingstonInventors: Jeremy P. W. Heaton, Michael A. Adams, James D. Banting
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Patent number: 6420427Abstract: An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.Type: GrantFiled: April 7, 2000Date of Patent: July 16, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kanji Takahashi, Tsuneyuki Sugiura
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Patent number: 6420418Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: August 14, 2000Date of Patent: July 16, 2002Assignee: Merck & Co., Inc.Inventors: William K. Hagmann, Stephen E. Delaszlo, George Doherty, Linda L. Chang, Ginger X. Yang
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Publication number: 20020090604Abstract: Truncated thyroid hormone receptors &Dgr;TR&agr;1 and &Dgr;TR&agr;2 have been discovered to play a role in actin-based endocytosis, e.g., in the nervous system. The invention relates to methods of discovering ligands effective in modulating endocytosis and transgenic mice with altered expression of &Dgr;TR&agr;1 and &Dgr;TR&agr;2. The invention is useful for the discovery and testing of compounds for treating disorders of the nervous system such as depression.Type: ApplicationFiled: June 28, 2001Publication date: July 11, 2002Inventors: Jack L. Leonard, Alan P. Farwell
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Publication number: 20020086895Abstract: A method for treating a fungal infection is disclosed. The method includes contacting a fungus with a substituted aurone derivative.Type: ApplicationFiled: September 20, 2001Publication date: July 4, 2002Inventors: Wai-Lam Alex Chu, Flemming R. Jensen, Thomas B. Jensen, James B. McAlpine, Brigitte Sokilde, Alexandra M. SantAna-Sorensen, Sunil Ratnayake, Jack B. Jiang, Catharine Noble, Angela M. Stafford