Nitroxides, Oxyamines Or Hydroxylamines (i.e., N-o Or N-oh) Patents (Class 514/645)
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Patent number: 6747063Abstract: In the field of treatment of erectile dysfunction there is disclosed a novel therapy in which the actions of an agent or agents, produce a combination of effects to induce effective erection (and avoid priapism) while reducing or entirely avoiding pain. The method taught combines a first action of an agent which is to antagonize a drug-induced pain stimulus within nociceptive nerves of penile tissue with a second action of either the same agent or of a second agent, which enhances, synergistically, smooth muscle relaxation. The synergism allows for at least an equivalent effect of smooth muscle relaxation to be obtained at significantly lower doses of a smooth muscle relaxing agent such as PGE1 which in standard therapy is also in 40-45% of cases pain-inducing at doses which achieve effective erection.Type: GrantFiled: October 23, 1998Date of Patent: June 8, 2004Assignee: Cellegy Pharmaceuticals, Inc.Inventors: Michael A. Adams, Jeremy P. W. Heaton, Donald H. Maurice
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Patent number: 6723703Abstract: The present invention is directed to the treatment of cystic fibrosis that involves the administration of a nitrosylating agent, such as S-nitrosoglutathione or ethyl nitrite.Type: GrantFiled: March 24, 2003Date of Patent: April 20, 2004Assignees: Duke University, University of Virginia Patent FoundationInventors: Benjamin Gaston, Jonathan S. Stamler
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Patent number: 6717012Abstract: The invention provides novel adamantane compounds having one of the following formulas: wherein: R1 and R3 are H, OH, alkyl, cycloalkyl, amino or aryl, and can be the same or different; R2 is H, NH2, alkyl, OH, COOH, amino, amide, or carbamate; R4-R8 are H, OH, NH2, alkyl, OH, COOH, ester, amino, amide, or alkyloxy, and can be the same or different; R9-R14 are H, alkyl, or phenyl, and can be the same or different; and wherein when any of R1-R8 is amino, the compounds are the free bases and their acid addition salts. The present invention also relates to compositions and methods for treating and/or preventing neurological and inflammatory disorders in a patient by administering a therapeutically effective amount of the compounds of formula (I), (II) or (III) and a pharmaceutically acceptable carrier.Type: GrantFiled: April 2, 2002Date of Patent: April 6, 2004Assignee: NeuroMolecular, Inc.Inventors: Yuqiang Wang, James W. Larrick
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Patent number: 6716878Abstract: Compounds of formula (I) are antibacterial agents: wherein Z represents a radical of formula —N(OH)CH(═O) or of formula —C(═O)NH(OH), and R1-R4 are as defined in the specification. A method for the treatment of bacterial or protozoal infections in humans and non-human mammals, which comprises administering to a subject suffering such infection an antibacterially or antiprotozoally effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof.Type: GrantFiled: October 5, 2001Date of Patent: April 6, 2004Assignee: Vernalis (Oxford) LimitedInventors: Richard Simon Todd, Daniel Christopher Brookings, Helen Katherine Smith, Alison Jane Thompson, Raymond Paul Beckett
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Publication number: 20040063783Abstract: The present invention relates to a compound of formula (I) in which X, A, T, Y, G and R are as defined in Claim (1).Type: ApplicationFiled: April 3, 2003Publication date: April 1, 2004Inventors: Claude Lardy, Jean-Yves Nioche, Lidia Caputo, Jacques Decerprit, Jean-Yves Ortholand, Didier Festal, Daniel Guerrier
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Patent number: 6706761Abstract: The invention relates to insecticide-comprising polymer-based compositions which, in order to recognize the point in time when the insecticide is exhausted, comprise at least one dye which, after the insecticide has evaporated, turns a different colour.Type: GrantFiled: November 13, 2001Date of Patent: March 16, 2004Assignee: S. C. Johnson & Son, Inc.Inventors: Mike-Dirk Bublitz, Dietmar Kisters, Rainer Hamprecht
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Patent number: 6696472Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: February 24, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677379Abstract: The invention relates to substituted polycyclic aryl and heteroary tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted diamines.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6635677Abstract: This invention generally relates to novel compositions and methods for the treatment of certain cancers. Additionally, this invention relates to novel compositions and methods to screen drugs for the treatment of certain cancers. Specifically, the invention contemplates that temozolomide and methoxyamine, in combination or in sequence, shall be used as a treatment for certain tumors that are resistant to treatment by temozolomide alone. Additionally, methoxyamine is contemplated for methods of treatment of cancer, wherein methoxyamine is used, in combination or in sequence, with other anticancer drugs or agents.Type: GrantFiled: February 19, 2002Date of Patent: October 21, 2003Assignee: Case Western Reserve UniversityInventors: Stanton L. Gerson, Lili Liu
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Publication number: 20030191064Abstract: The present invention provides methods for preventing and treating loss of, or impairments to, the sense of balance. Specifically, the invention provides methods for preserving the sensory hair cells and neurons of the inner ear vestibular apparatus by preventing or reducing the damaging effects of oxidative stress by administering an effective amount of the following therapeutic agents: antioxidants; compounds utilized by inner ear cells for synthesis of glutathione; antioxidant enzyme inducers; trophic factors; mitochondrial biogenesis factors; and combinations thereof.Type: ApplicationFiled: March 31, 2003Publication date: October 9, 2003Inventor: Richard D. Kopke
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Publication number: 20030181527Abstract: Novel pharmaceutical formulations of &agr;-(2,4-disulfophenyl)-N-tert-butylnitrone and pharmaceutically acceptable salts thereof and the use of such formulations in the treatment of various diseases and conditions, especially stroke, are disclosed.Type: ApplicationFiled: November 18, 2002Publication date: September 25, 2003Inventors: Mats Andersson, Mattias Andersson, Patrik Eriksson
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Patent number: 6605447Abstract: Methods for identifying and monitoring increased or decreased levels of inducible nitric oxide synthase in biological samples are provided. A collection device for detecting inducible nitric oxide synthase in biological samples is also provided. Detection of inducible nitric oxide synthase is useful in the diagnosis of inflammatory responses such as infections mediated by bacteria, yeast or viruses, transplant rejection, rheumatoid arthritis, interstitial cystitis and cancer.Type: GrantFiled: September 14, 1998Date of Patent: August 12, 2003Assignee: Yale UniversityInventors: Robert M. Weiss, William C. Sessa, Marcia A. Wheeler, Shannon D. Smith
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Publication number: 20030149104Abstract: The present invention relates to certain tri-substituted phenyl derivatives and analogues of formula (I), to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: November 13, 2002Publication date: August 7, 2003Inventors: Maria Boije, Jonas Fagerhag, Eva-Lotte Lindstedt Alstermark, Bengt Ohlsson
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Patent number: 6589996Abstract: A method for the treatment of disorders relating to serotonergic system in humans, for example depression and anxiety, comprising orally administering deramciclane in a daily dosage of about 20 to about 60 mg.Type: GrantFiled: March 16, 2001Date of Patent: July 8, 2003Assignee: Orion CorporationInventors: Outi Mäki-Ikola, Harri Kanerva
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Patent number: 6589995Abstract: The present invention demonstrates a method for inhibiting O-linked protein glycosylation in a tissue or cell, comprising the step of contacting said tissue or cell with (Z)-1-[N-(3-Ammoniopropyl)-N-(n-propyl)amino] diazen-ium-1,2-diolate or a derivative thereof. The present invention is also directed to a method of treating or inhibiting the onset of diabetes mellitis in an individual in need of such treatment, comprising the step of admininstering to said individual a pharmacological dose of a compound which inhibiting O-linked protein glycosylation in a tissue or cell of said individual. Further, the present invention provides a pharmaceutical composition, comprising (Z)-1-[N-(3-Ammoniopropyl)-N-(n-propyl)amino] diazen-ium-1,2-diolate and a pharmaceutically acceptable carrier or a derivative thereof.Type: GrantFiled: March 21, 2001Date of Patent: July 8, 2003Assignee: UAB Research FoundationInventors: Robert Konrad, Jeffrey Kudlow
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Patent number: 6569895Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.Type: GrantFiled: September 8, 1999Date of Patent: May 27, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
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Patent number: 6569902Abstract: PBN (&agr;-phenyl-tert-butylnitrone), and its derivatives nitrone-based free radical traps, significantly reduce preneoplastic nodule development as well as inhibit hepatocellular carcinoma (HCC) formation at very low levels. The involvement of reactive oxygen species (ROS) in cancer development has been strongly implicated for many years. The involvement of ROS has been strongly implicated in cancer development is a model system where feeding a choline deficiency (CD) diet to rats leads to hepatocellular carcinoma (HCC) development. Administering PBN in the drinking water inhibits HCC formation. Preneoplastic nodule growth in the liver is significantly suppressed by administering PBN, or some of its natural metabolites, in the diet. The effectiveness of PBN in preventing HCC development in the CD liver model is considered due to its prevention of tumor development after the target cells have already been initiated, i.e. genetically changed into tumor cells.Type: GrantFiled: March 28, 2001Date of Patent: May 27, 2003Assignee: Oklahoma Medical Research FoundationInventors: Robert A. Floyd, Yashige Kotake, Kenneth L. Hensley, Dai Nakae
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Publication number: 20030078241Abstract: A method of treatment is disclosed whereby a nitroxide compound is administered to a patient in a therapeutically effective amount. The nitroxide compound is comprised of a first portion which comprises a nitrogen atom and an oxygen atom bound directly together and an unpaired electron (.NO), and a second portion which provides a negative charge. The first and second portions are connected directly or indirectly by a linking group positioned between and bound to the first portion and the second portion in a manner such that the negative charge of the second portion stabilizes the .NO of the first portion when the nitroxide is present in the patient. By stabilizing the .NO portion of the molecule the nitroxide is allowed to interact with reactive oxygen species in the patient for a longer period of time and modulate adverse effects of those reactive oxygen species.Type: ApplicationFiled: September 6, 2002Publication date: April 24, 2003Inventors: Jen-Chang Hsia, Li Ma
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Publication number: 20030073712Abstract: Cytoprotective compounds, many of which are phenolic derivatives characterized by a substituted phenol having certain conjugated bonds, are useful in the treatment of certain ischemic or inflammatory conditions, including but not limited to stroke, myocardial infarction, congestive heart failure, and skin disorders characterized by inflammation or oxidative damage. They are also useful in the manufacture of pharmaceutical and cosmetic formulations for the treatment of such conditions.Type: ApplicationFiled: July 23, 2002Publication date: April 17, 2003Inventors: Bing Wang, Yong-Kang Zhang, Jian Chen, Wei Zhang, Jiangao Song, Ughetta Del Balzo, Lesley Brown, Sekhar Boddupalli, Steven Bobzin, Sylvain Gilat, Guy Miller
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Patent number: 6538033Abstract: Nitric oxide donor compounds of the formula: are provided. In the formula, R is (CH2)n, wherein n ranges from 1 to 8 and wherein each hydrogen atom on the alkylene group and on the phenyl groups can optionally be replaced by a substituent selected from the group consisting of alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, and hydroxy groups. A particularly preferred compound is 1,3-(nitrooxymethyl)phenyl 2-hydroxybenzoate. The compounds are useful for treating and preventing various conditions, including coronary artery disease.Type: GrantFiled: August 29, 2001Date of Patent: March 25, 2003Assignee: Huntington Medical Research InstitutesInventor: Richard J. Bing
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Publication number: 20030050345Abstract: The invention refers to pharmaceutical compositions which have an enhanced antitumor activity or reduced side effect(s) comprising a known active substance having antitumor effect or a pharmaceutically acceptable salt thereof and a hydroximic acid derivative of formula (I) or a therapeutically useful acid addition salt thereof.Type: ApplicationFiled: February 28, 2002Publication date: March 13, 2003Applicant: N-Gene Research Laboratories, Inc.Inventor: Balazs Sumegi
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Patent number: 6521607Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Subsbitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-phenoxy N-phenyl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: February 18, 2003Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20020198264Abstract: This invention generally relates to novel compositions and methods for the treatment of certain cancers. Additionally, this invention relates to novel compositions and methods to screen drugs for the treatment of certain cancers. Specifically, the invention contemplates that temozolomide and methoxyamine, in combination or in sequence, shall be used as a treatment for certain tumors that are resistant to treatment by temozolomide alone. Additionally, methoxyamine is contemplated for methods of treatment of cancer, wherein methoxyamine is used, in combination or in sequence, with other anticancer drugs or agents.Type: ApplicationFiled: February 19, 2002Publication date: December 26, 2002Applicant: Case Western Reserve UniversityInventors: Stanton L. Gerson, Lili Liu
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Publication number: 20020169214Abstract: The present invention relates to methods and processes of inactivating a viral contaminants in a biological source material or process intermediate by contacting the biological source material (e.g., a host cell, cell supernatant, cell lysate, blood plasma, tissue homogenate, or other biological materials) with a solution containing one or more alkylamine compounds. In a particular embodiment, the active ingredients are amphipathic, charged amines or amine oxides coupled to saturated hydrocarbon chains of varying lengths.Type: ApplicationFiled: May 14, 2001Publication date: November 14, 2002Inventor: Scot R. Shepard
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Patent number: 6479552Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted diamines.Type: GrantFiled: November 14, 2001Date of Patent: November 12, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6465448Abstract: This invention generally relates to novel compositions and methods for the treatment of certain cancers. Additionally, this invention relates to novel compositions and methods to screen drugs for the treatment of certain cancers. Specifically, the invention contemplates that temozolomide and methoxyamine, in combination or in sequence, shall be used as a treatment for certain tumors that are resistant to treatment by temozolomide alone.Type: GrantFiled: August 13, 1999Date of Patent: October 15, 2002Assignee: Case Western Reserve UniversityInventors: Stanton L. Gerson, Lili Liu
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Patent number: 6455589Abstract: The invention provides pharmaceutical compositions comprising primary N-hydroxylamines and related therapeutic, prophylactic, diagnostic and screening methods. The pharmaceutical compositions generally comprise a pharmaceutical composition comprising an orally administrable effective unit solid dosage of a primary N-hydroxylamine or a pharmaceutically acceptable salt thereof and substantially free of a nitrone corresponding to the hydroxylamine.Type: GrantFiled: October 28, 1999Date of Patent: September 24, 2002Assignee: The Regents of the University of CaliforniaInventors: Bruce N. Ames, Hani Atamna
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Patent number: 6441032Abstract: Disclosed are novel &agr;-aryl-N-alkylnitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals and as analytical reagents for detecting free radicals.Type: GrantFiled: August 9, 2000Date of Patent: August 27, 2002Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Alina Dykman, Yong-Kang Zhang, Allan L. Wilcox, Julian Levell
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Patent number: 6423690Abstract: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises administering to a subject suffering such infection an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-CType: GrantFiled: January 7, 2000Date of Patent: July 23, 2002Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Patent number: 6417162Abstract: The present invention is directed to nitrosated or nitrosylated &agr;-adrenergic receptor antagonists, compositions comprising &agr;-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females.Type: GrantFiled: May 7, 1999Date of Patent: July 9, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
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Patent number: 6380258Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 24, 1999Date of Patent: April 30, 2002Assignee: G. D. Searle, L.L.C.Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
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Patent number: 6376508Abstract: The invention features a method of modulating SMN exon 7 expression in a subject by administering a histone deacetylase inhibitor.Type: GrantFiled: December 13, 2000Date of Patent: April 23, 2002Assignee: Academia SinicaInventors: Hung Li, Hsiu-Mei Hsieh-Li, Jan-Gowth Chang
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Patent number: 6358536Abstract: The invention relates to compositions, methods, apparatus, and kits for alleviating or preventing vasoconstriction or vasospasm in a mammal. The compositions, methods, apparatus, and kits are also useful for alleviating or preventing ischemic tissue damage resulting from ischemia associated with cerebral vasoconstriction which follows aneurysmal subarachnoid hemorrhage, with embolic stroke, with coronary artery obstruction, and with other conditions. These compositions, methods, apparatus, and kits generally relate to adventitial (i.e. extra-luminal) administration of a nitric oxide donor compound to a blood vessel in a mammal.Type: GrantFiled: October 2, 1998Date of Patent: March 19, 2002Assignee: Thomas Jefferson UniversityInventor: Jeffrey E. Thomas
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Patent number: 6348504Abstract: This invention relates generally to oxime ethers which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: March 30, 1999Date of Patent: February 19, 2002Inventors: Richard E. Olson, William E. Frietze
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Patent number: 6342523Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have the formula: where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.Type: GrantFiled: December 1, 1999Date of Patent: January 29, 2002Assignee: Centaur Pharmaceuticals, Inc.Inventors: L. David Waterbury, Allan L. Wilcox, John M. Carney, Farah Mavandadi, Albert Danielzadeh
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Publication number: 20010053555Abstract: A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteases).Type: ApplicationFiled: October 27, 1997Publication date: December 20, 2001Inventors: DINESH V. PATEL, KHEHYONG NGU
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Publication number: 20010039257Abstract: In the field of treatment of erectile dysfunction there is disclosed a novel therapy in which the actions of an agent or agents, produce a combination of effects to induce effective erection (and avoid priapism) while reducing or entirely avoiding pain. The method taught combines a first action of an agent which is to antagonize a drug-induced pain stimulus within nociceptive nerves of penile tissue with a second action of either the same agent or of a second agent, which enhances, synergistically, smooth muscle relaxation. The synergism allows for at least an equivalent effect of smooth muscle relaxation to be obtained at significantly lower doses of a smooth muscle relaxing agent such as PGE1 which in standard therapy is also in 40-45% of cases pain-inducing at doses which achieve effective erection.Type: ApplicationFiled: October 23, 1998Publication date: November 8, 2001Inventors: MICHAEL A. ADAMS, JEREMY P. W. HEATON, DONALD H. MAURICE
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Patent number: 6306912Abstract: Method for identifying a compound useful for the therapeutic treatment of a neurological disease or disorder such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease or Parkinson's Disease, or useful as a muscle relaxant, analgesic, or adjuvant to general anesthetics. The compound is active on a receptor-operated calcium channel, including, but not limited to, that present as part of an NMDA receptor-ionophore complex, a calcium-permeable AMPA receptor, or a nicotinic cholinergic receptor, as a noncompetitive antagonist. The method includes identifying a compound which binds to the receptor-operated calcium channel at the site bound by the arylalkylamines Compound 1, Compound 2 or Compound 3.Type: GrantFiled: June 7, 1995Date of Patent: October 23, 2001Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Bradford C. VanWagenen, Eric G. DelMar, Manuel F. Balandrin, Scott T. Moe, Linda D. Artman
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Patent number: 6297278Abstract: There is provided methods for inhibiting the activity of enveloped viruses, treatment of viral infections and method inactivating sperm. There is provided articles for use in these methods.Type: GrantFiled: April 4, 1994Date of Patent: October 2, 2001Assignee: Biosyn Inc. (a Pennsylvania Corporation)Inventors: Edwin B. Michaels, Daniel Malamud
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Patent number: 6287601Abstract: Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID mixed in a lipid-based carrier are described. The application of such combinations to the affected areas, e.g., the hoofs and surrounding tissues, of an equine afflicted with laminitis provides relief from the debilitating effects of this painful, often life-threatening condition.Type: GrantFiled: June 16, 1999Date of Patent: September 11, 2001Inventor: Meri Charmyne Russell
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Patent number: 6284790Abstract: A method for potentiating an organic nitrate having vasodilating activity by administering to a subject an effective amount of the organic nitrate with a potentiating amount of a thromboxane receptor antagonist and a reducing agent. Formulations and synergistic compositions are also described.Type: GrantFiled: June 15, 2000Date of Patent: September 4, 2001Inventor: Sachin Gupte
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Patent number: 6274570Abstract: A liquid pesticidal composition, which is substantially free of water, comprising a hydrophobic pesticide or mixture of pesticides dissolved in an organic solvent and comprising as surfactants (a) a castor oil ethoxylate having 30-50 mol ethoxylate, (b) a branched C8-C18 alcohol ethoxylate having 5-10 mol ethoxylate, and (c) a tristyrenephenol-ethoxylate having 8-30 mol ethoxylate, or its phosphate or salt thereof. The compositions also include gels having a viscosity of 500 to 20,000 mPas and comprising additionally a gelling agent.Type: GrantFiled: December 22, 1998Date of Patent: August 14, 2001Assignee: Syngenta Crop Protection, Inc.Inventors: Manfred Vogt, William Baettig
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Patent number: 6268397Abstract: The invention relates to the use of a compound selected from: [&agr;-(tert-butylaminomethyl)-3,4-dichlorobenzyl]thioacetamide and its laevorotatory isomer, [&agr;-(tert-amylaminomethyl)-3,4-dichlorobenzyl]thioacetamide and its isomers, [&agr;-(1-adamantylaminomethyl)3,4-dichlorobenzyl]thioacetamide and its isomers, as well as the addition salts of these compounds with pharmaceutically acceptable acids, for inhibiting dopamine reuptake.Type: GrantFiled: May 1, 1998Date of Patent: July 31, 2001Assignee: Laboratoire. L. LafonInventor: Philippe Laurent
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Patent number: 6255353Abstract: Certain simple chemical agents, referred to herein as nitrone related therapeutics or “NRTs”, when administered to a patient susceptible to neovascularization (angiogenesis), can intervene and inhibit the disease's progress. Methods for therapeutically and prophylactically inhibiting angiogenesis by administering one or more NRTs are disclosed as are pharmaceutical compositions for use in such methods of treating. NRTs useful in these compositions and therapeutic methods are also disclosed.Type: GrantFiled: March 12, 1999Date of Patent: July 3, 2001Assignee: Centaur Pharmaceuticals, Inc.Inventors: Lowell D. Waterbury, Kenneth W. Narducy, Allan L. Wilcox
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Patent number: 6228858Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions.Type: GrantFiled: November 17, 1997Date of Patent: May 8, 2001Assignee: University of Kansas Medical CenterInventors: Billy G. Hudson, Parvin Todd, Raja Gabriel Khalifah, Aaron Ashley Booth
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Patent number: 6197825Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.Type: GrantFiled: May 28, 1998Date of Patent: March 6, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Patent number: 6197826Abstract: Disclosed are novel &agr;-(2-hydroxyphenyl) nitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.Type: GrantFiled: July 16, 1999Date of Patent: March 6, 2001Assignee: Centaur Pharmaceuticals, Inc.Inventors: L. David Waterbury, John M. Carney, Allan L. Wilcox
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Patent number: 6194461Abstract: A compound represented by the figure (1) or a pharmaceutically acceptable salt thereof is useful as medicament for treating retinal degenerative disorders: wherein Ar is optionally substitued phenyl or optionally substituted heteroaryl;. n is 0, 1 or 2; W is —CH2NH— or —CH═N(O)—; R1, R2 and R3 are independently optionally substituted alkyl, carboxyl or alkoxycarbonyl; any two groups of R1, R2 and R3 may be taken together with the carbon atom to form optionally substituted cycloalkane; all of R1, R2 and R3 may be taken together with the adjusent carbon atom to form optionally substituted bicycloalkane or optionally substituted tricycloalkane; R4 and R5 are independently hydrogen atom or optionally substituted alkyl.Type: GrantFiled: March 15, 1999Date of Patent: February 27, 2001Assignee: Sumitomo Pharmaceuticals Co., Ltd.Inventors: Kazuhito Ikeda, Tohru Tatsuno, Hiroki Ogo, Shuji Masumoto, Tatsuya Fujibayashi, Ryu Nagata
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Patent number: 6160021Abstract: A method of treating a subject for an unwanted epidermal or dermal condition comprising administering to the subject, a treatment which modulates the level of nitric oxide (NO) in the skin.Type: GrantFiled: February 3, 1998Date of Patent: December 12, 2000Assignee: The General Hospital CorporationInventors: Ethan A. Lerner, Abrar A. Qureshi, Lisa H. Lerner
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Patent number: 6147068Abstract: A pharmaceutical composition of matter for delivering nitric oxide. The composition is an amine that was reacted with nitric oxide. The composition of matter is lipophilic and insoluble and therefore delivers nitric oxide to the specific area of the body where it is introduced. Also, a method of synthesizing an amine and reacting it with nitric oxide to form the pharmaceutical composition of matter. Finally, a method of using the pharmaceutical composition of matter to deliver nitric oxide to the body.Type: GrantFiled: September 21, 1998Date of Patent: November 14, 2000Assignee: The University of AkronInventors: Daniel J. Smith, Dominick Roselle