Nitroxides, Oxyamines Or Hydroxylamines (i.e., N-o Or N-oh) Patents (Class 514/645)
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Patent number: 6114392Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.Type: GrantFiled: April 16, 1996Date of Patent: September 5, 2000Inventors: Gad M. Gilad, Varda H. Gilad
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Patent number: 6083988Abstract: 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: September 4, 1997Date of Patent: July 4, 2000Inventor: David Alan Becker
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Patent number: 6071970Abstract: Method and compositions for treating a patient having 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, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).Type: GrantFiled: June 7, 1995Date of Patent: June 6, 2000Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Manuel F. Balandrin, Bradford C. VanWagenen, Eric G. DelMar, Scott T. Moe, Linda D. Artman, Robert M. Barmore
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Patent number: 6056966Abstract: Pharmaceutical compositions in topical or parenteral form containing specific organic mono- or dinitrates, some of them novel compounds, are effective in treating male impotence and erectile dysfunction through topical or intracavernosal administration to the penis. Methods of treatment utilizing the mono- or dinitrate-containing compositions are also disclosed.Type: GrantFiled: May 18, 1998Date of Patent: May 2, 2000Assignee: Baker Norton Pharmaceuticals, Inc.Inventors: Sami Selim, Robert Testman, Ho-Leung Fung, John A. Bauer
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Patent number: 6045827Abstract: 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: August 19, 1997Date of Patent: April 4, 2000Assignee: Meri Charmyne RussellInventor: Meri Charmyne Russell
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Patent number: 6046232Abstract: Disclosed are novel .alpha.-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: October 15, 1998Date of Patent: April 4, 2000Assignee: 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: 6028106Abstract: The invention provides a method for the treatment and prevention of urinary incontinence in mammals, e.g., human males and females, especially nonpregnant female mammals, by administering a nitric oxide synthase substrate and/or nitric oxide donor, alone or in combination with an estrogenic agent and/or a progestational substance, with or without supplementation with an alpha-adrenergic agonist, beta-adrenergic receptor blocking agent, cholinergic-receptor blocking compound or a cholinergic-receptor-stimulating drug, as well as pharmaceutical compositions useful in practicing the methods of this invention.Type: GrantFiled: October 29, 1997Date of Patent: February 22, 2000Assignees: Schering Aktiengesellschaft, Board of Regents, The Univ. of TX SystemInventors: Robert E. Garfield, Kristof Chwalisz
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Patent number: 6025384Abstract: 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: February 13, 1998Date of Patent: February 15, 2000Assignee: LeukoSite, Inc.Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
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Patent number: 5973011Abstract: The present invention describes the use of nitric-oxide-liberating or transferring compounds, stimulators of endogenous NO formation, as well as stimulators of guanylate cyclase, for prevention, treatment and elimination of endothelial dysfunctions and the diseases accompanying these dysfunctions or caused by them, as well as the use of said compounds to produce pharmaceutical products for the cited areas of application.Type: GrantFiled: September 27, 1996Date of Patent: October 26, 1999Assignee: ISIS PHARMA GmbHInventors: Eike Albrecht Noack, Georg Kojda
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Patent number: 5932538Abstract: Disclosed are nitrosated and nitrosylated .alpha.-adrenergic receptor antagonists, compositions of an .alpha.-adrenergic receptor antagonist (.alpha.-antagonist), which can optionally be substituted with at least one NO or NO.sub.2 moiety, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.circle-solid.); and uses for each of them in treating human male impotence or erectile dysfunction.Type: GrantFiled: February 2, 1996Date of Patent: August 3, 1999Assignee: NitroMed, Inc.Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
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Patent number: 5895783Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.Type: GrantFiled: July 16, 1993Date of Patent: April 20, 1999Assignees: Schering Aktiengesellschaft, The University of TexasInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampal Li
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Patent number: 5891472Abstract: 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: November 19, 1996Date of Patent: April 6, 1999Assignee: Meri Charmyne RussellInventor: Meri Charmyne Russell
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Patent number: 5840759Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.Type: GrantFiled: March 11, 1997Date of Patent: November 24, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
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Patent number: 5837736Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.Type: GrantFiled: March 11, 1997Date of Patent: November 17, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
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Patent number: 5817697Abstract: The pharmaceutical use of nitroglycerin, which is also designated as glycerol trinitrate or, chemically, as 1,2,3-propanetriol trinitrate, in a transdermal application form prevents undesired labour in pregnant mammals. The pharmaceutical use prevents premature labour.Type: GrantFiled: July 1, 1997Date of Patent: October 6, 1998Assignee: Schwarz Pharma AGInventors: Hans-Michael Wolff, Dietrich Schacht, Martin Feelisch, Bruce Ramsay, John Francis Martin, Christoph Christopher Lees, Adam Julian De Belder
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Patent number: 5814667Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.Type: GrantFiled: March 11, 1997Date of Patent: September 29, 1998Assignee: United States of America as represented by the Department of Health and Human ServicesInventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
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Patent number: 5811463Abstract: Compositions and methods for relaxing smooth muscle in a warm-blooded animal are provided, comprising the step of administering to the animal a transition-metal nitrosyl complex. In one aspect, the transition-metal nitrosyl complex is represented by the formula L.sub.3 M(NO).sub.y X.sub.3-y where L is a two-electron Lewis base or L.sub.3 is a six-electron Lewis base, M is a Group 6 or 8 transition-metal, and when y is 1, X is carbon monoxide, and when y is 2, X is a halide or pseudohalide. In another aspect, the transition-metal nitrosyl complex is represented by the formula ?M(NO).sub.2 X.sub.y !.sub.2 where X is a halide or pseudohalide, and when M is a Group 6 transition-metal, y is 2, and when M is a Group 8 transition-metal, y is 1. Methods are also described for treating hypertension, angina pectoris, congestive heart disease, and impotence utilizing pharmaceutical compositions comprising the above-described transition-metal nitrosyl complexes.Type: GrantFiled: December 20, 1996Date of Patent: September 22, 1998Assignee: University of British ColumbiaInventors: Peter Legzdins, Catherine C. Y. Pang, Michael J. Shaw
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Patent number: 5795915Abstract: The invention relates to the use of a compound selected from:?.alpha.-(tert-butylaminomethyl)-3,4-dichlorobenzyl!thioacetamide and its laevorotatory isomer,?.alpha.-(tert-amylaminomethyl)-3,4-dichlorobenzyl!thioacetamide and its isomers,?.alpha.-(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 17, 1996Date of Patent: August 18, 1998Assignee: Laboratoire L. LafonInventor: Philippe Laurent
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Patent number: 5789442Abstract: The invention provides a method for the treatment and prevention of urinary incontinence in mammals, e.g., human males and females, especially nonpregnant female mammals, by administering a nitric oxide synthase substrate and/or nitric oxide donor, alone or in combination with an estrogenic agent and/or a progestational substance, with or without supplementation with an alpha-adrenergic agonist, beta-adrenergic receptor blocking agent, cholinergic-receptor blocking compound or a cholinergic-receptor-stimulating drug, as well as pharmaceutical compositions useful in practicing the methods of this invention.Type: GrantFiled: January 18, 1996Date of Patent: August 4, 1998Assignee: Schering AktiengesellschaftInventors: Robert E. Garfield, Kristof Chwalisz
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Patent number: 5750565Abstract: 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: May 31, 1995Date of Patent: May 12, 1998Assignee: Cytomed, Inc.Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
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Patent number: 5728714Abstract: A method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth is disclosed. The method comprises administering substituted or unsubstituted 2,2,6,6-tetramethyl-1-piperdinyloxyl (TEMPO) to the affected tissue.Type: GrantFiled: June 5, 1995Date of Patent: March 17, 1998Inventor: Peter H. Proctor
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Patent number: 5725839Abstract: Compositions and processes to alleviate free radical toxicity are disclosed based on the use of nitroxides in association with physiologically compatible macromolecules. In particular, hemoglobin-based red cell substitutes are described featuring stable nitroxide free radicals for use in cell-free hemoglobin solutions, encapsulated hemoglobin solutions, stabilized hemoglobin solutions, polymerized hemoglobin solutions, conjugated hemoglobin solutions, nitroxide-labelled albumin, and nitroxide-labelled immunoglobulin. Formulations are described herein that interact with free radicals, acting as antioxidant enzymemimics, which preserve nitroxides in their active form in vivo. Applications are described including blood substitutes, radioprotective agents, imaging agents, agents to protect against ischemia and reperfusion injury, and in vivo enzyme mimics among others.Type: GrantFiled: June 7, 1995Date of Patent: March 10, 1998Inventor: Jen-Chang Hsia
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Patent number: 5719150Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: November 14, 1996Date of Patent: February 17, 1998Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
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Patent number: 5658954Abstract: A specially formulated environmental insecticide is provided which effectively controls whiteflies and other insects but is safe to humans, farm animals, pets, crops, and fish. The cost-effective non-polluting insecticide can be in the form of a 100% concentrate or an aqueous solution. The sprayable easy-to-use insecticide can comprise a synergistic blend of cottonseed oil amides, coconut oil amides, tall oil amides and a nonionic surfactant, as well as a chelating agent, a viscosity control agent and free amine.Type: GrantFiled: January 29, 1996Date of Patent: August 19, 1997Inventor: Eugene F. Targosz
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Patent number: 5652270Abstract: The invention refers to a pharmaceutical composition, a process for the preparation thereof and a novel medical use of bicycloheptane derivatives. The pharmaceutical compositions of the invention comprise a bicycloheptane derivative of the formula I ##STR1## wherein said derivative is as defined in the specification herein. The pharmaceutical compositions of the invention are suitable for the treatment of diseases and disorders that are connected with the influence on the cholecystokinin system, especially for preventing the spastic contraction of the gallbladder.Type: GrantFiled: June 17, 1996Date of Patent: July 29, 1997Assignee: Egis Gyogyszergyar RTInventors: Zoltan Budai, Istvan Gacsalyi, Gabor Szenasi, Tibor Mezei, Aniko Kovacs, Gabor Blasko, Katalin Szemeredi, Gyula Simig, Lujza Petocz, Klara Reiter nee Esses
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Patent number: 5650442Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.Type: GrantFiled: October 7, 1994Date of Patent: July 22, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
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Patent number: 5648393Abstract: Methods of relaxing corpus cavernosum smooth muscle, treating disease states responsive to prevention or relaxation of undesirable contractions of corpus cavernosum smooth muscle and of treating male impotence by administering an S-nitrosothiol such as a low molecular weight S-nitrosothiol, S-nitroso-ACE-inhibitor or S-nitroso-protein.Type: GrantFiled: August 29, 1994Date of Patent: July 15, 1997Assignee: Brigham & Women's HospitalInventors: Jonathan Stamler, Joseph Loscalzo, Adam Slivka, Daniel Simon, Robert Brown, Jeffrey Drazen
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Patent number: 5646181Abstract: Pharmaceutical compositions in topical or parenteral form containing organic nitrites are effective in treating male impotence and erectile dysfunction through topical or intracavernosal administration to the penis. Methods of treatment utilizing the nitrite-containing compositions are also disclosed, as are certain novel organic nitrite compounds.Type: GrantFiled: May 2, 1995Date of Patent: July 8, 1997Assignee: Research Foundation of State University of New YorkInventors: Ho-Leung Fung, John Anthony Bauer
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Patent number: 5631284Abstract: Compositions and methods for relaxing smooth muscle in a warm-blooded animal are provided, comprising the step of administering to the animal a transition-metal nitrosyl complex. In one aspect, the transition-metal nitrosyl complex is represented by the formula L.sub.3 M(NO).sub.y X.sub.3-y where L is a two-electron Lewis base or L.sub.3 is a six-electron Lewis base, M is a Group 6 or 8 transition-metal, and when y is 1, X is carbon monoxide, and when y is 2, X is a halide or pseudohalide. In another aspect, the transition-metal nitrosyl complex is represented by the formula [M(NO).sub.2 X.sub.y ].sub.2 where X is a halide or pseudohalide, and when M is a Group 6 transition-metal, y is 2, and when M is a Group 8 transition-metal, y is 1. Methods are also described for treating hypertension, angina pectoris, congestive heart disease, and impotence utilizing pharmaceutical compositions comprising the above-described transition-metal nitrosyl complexes.Type: GrantFiled: October 6, 1993Date of Patent: May 20, 1997Assignee: University of British ColumbiaInventors: Peter Legzdins, Catherine C. Y. Pang, Michael J. Shaw
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Patent number: 5622994Abstract: Spin trapping compositions in general have now been discovered to be effective in treating a variety of disorders, including disorders such as those arising from ischemia, infection, inflammation, exposure to radiation or cytotoxic compounds, not just of the central and peripheral nervous systems but of peripheral organ disease having a wide variety of etiologies. In the preferred embodiment, the compositions for treating tissue damage from ischemia contain PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for intravenous, oral, topical, or nasal/pulmonary administration. Many different disorders can be treated using these compounds, including diseases or disorders of the central and peripheral nervous systems, and disorders arising from ischemia, infection, inflammation, oxidation from exposure to radiation or cytotoxic compounds, as well as due to naturally occurring processes such as aging.Type: GrantFiled: March 15, 1994Date of Patent: April 22, 1997Assignees: Oklahoma Medical Research Foundation, University of Kentucky Research FoundationInventors: John M. Carney, Robert A. Floyd
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Patent number: 5612381Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: June 7, 1995Date of Patent: March 18, 1997Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
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Patent number: 5610195Abstract: Compounds of formula (I) in which (a) four of the radicals R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen and the others independently of one another are in each case C.sub.1 -C.sub.2 alkyl, these groups being bonded to the same carbon atom or to two different carbon atoms, or (b) five of the radicals R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydrogen and the other radical is C.sub.1 -C.sub.2 alkyl or hydroxymethyl, or salts thereof, are described. The compounds of formula (I) and their salts are ornithine decarboxylase inhibitors.Type: GrantFiled: December 12, 1994Date of Patent: March 11, 1997Assignee: Ciba-Geigy CorporationInventors: J org Frei, Jaroslav Stanek
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Patent number: 5594032Abstract: Treatment of erectile dysfunction comprising administering to a patient, inducible Nitric Oxide Synthase (iNOS) agents, including penile iNOS, inducers of penile iNOS, iNOS cDNA, or penile smooth muscle cells transformed with iNOS cDNA. Typical in vivo treatment involves delivery of these agents to the penile tissue of a patient by constant or intermittent implanted or external infusion pump, by implantation of time-release microcapsules or introduction of the genetically-engineered cells as by injection. Also disclosed are methods of treatment involving in vitro induction of iNOS in cultured smooth muscle cells and thereafter delivery of purified or recombinant iNOS enzyme, production of iNOS cDNA and genetic transformation with iNOS cDNA, followed by delivery thereof to the penis of a patient.Type: GrantFiled: November 10, 1994Date of Patent: January 14, 1997Inventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
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Patent number: 5583101Abstract: A method for inhibiting or relaxing skeletal muscle contractions which comprises contacting said skeletal muscle with a skeletal muscle relaxing amount, and a method for the treatment of disease states resulting from or exacerbated by undesirable contractions of skeletal muscle, which comprises administering a skeletal muscle relaxing amount to an individual in need thereof of a compound selected from the group consisting of nitroxyl ion (NO.sup.-), nitrosonium ion (NO.sup.+), nitric oxide and nitric oxide adducts or providers. This invention also is directed to stimulating the contraction of muscles in a mammal by administering an effective amount of a nitric oxide synthase inhibitor.Type: GrantFiled: July 15, 1994Date of Patent: December 10, 1996Assignees: Harvard College, Duke UniversityInventors: Jonathan Stamler, Lester Kobzik
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Patent number: 5567411Abstract: Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject.Type: GrantFiled: September 29, 1994Date of Patent: October 22, 1996Assignee: State of Oregon Acting by and Through the State Board of Higher Education on Behalf of the University of OregonInventors: John F. W. Keana, Vladimir Martin, William H. Ralston
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Patent number: 5552439Abstract: Provided is a method for treating inflammatory bowel disease in mammals utilizing certain phenol and benzamide compounds.Type: GrantFiled: September 29, 1993Date of Patent: September 3, 1996Assignee: Eli Lilly and CompanyInventor: Jill A. Panetta
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Patent number: 5532277Abstract: The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: ##STR1## Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R.sub.3 is an alkyl; and R.sub.4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl) nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl) nitronyl phenol (DMONP); N-tert -octylC-phenyl nitrone (OPN).Type: GrantFiled: April 10, 1995Date of Patent: July 2, 1996Assignee: Oklahoma Medical Research FoundationInventors: Edward G. Janzen, Allan L. Wilcox, Randall D. Hinton
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Patent number: 5532219Abstract: This invention pertains to the novel use of 4,4'-diaminodiphenylsulfone and its didextrose sulfonate derivative and other closely related sulfones in the prevention and treatment of dementia (Alzheimer's disease). A method of preventing and treating dementia in a human being suffering from dementia which comprises administering to the human being a therapeutic amount of a substance selected from the group consisting of 4,4'-diaminodiphenylsulfone, its didextrose sulfonate derivative, and sulfoxone, sulfetrone and thiazolsulfone, and therapeutically acceptable salts thereof.Type: GrantFiled: April 5, 1993Date of Patent: July 2, 1996Assignee: The University of British ColumbiaInventors: Patrick L. McGeer, Nobua Harada, Horoshi Kimura, Edith G. McGeer, Michael Schulzer
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Patent number: 5527828Abstract: The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: ##STR1## Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R.sub.3 is an alkyl; and R.sub.4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl) nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl) nitronyl phenol (DMONP); N-tert-octylC-phenyl nitrone (OPN).Type: GrantFiled: April 10, 1995Date of Patent: June 18, 1996Assignee: Oklahoma Medical Research FoundationInventors: Edward G. Janzen, Allan L. Wilcox, Randall D. Hinton
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Patent number: 5523322Abstract: A method of inhibiting blood-platelet aggregation in warm-blooded animals comprising administering to warm-blooded animals a blood-platelet aggregation inhibiting effective amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of --NH--CO--NH.sub.2, --NH--CO--CH.sub.3, --OH and their non-toxic, pharmaceutically acceptable acid addition salts.Type: GrantFiled: June 30, 1994Date of Patent: June 4, 1996Assignee: Roussel UCLAFInventors: Denis Blache, Christian Bloy, Bernard Hercelin
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Patent number: 5516806Abstract: Compounds of formula (I): H.sub.2 N--(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --O--NH.sub.2 and salts thereof are described in which the radical A is C.sub.3 -C.sub.6 cycloalkylene; n is 0 or 1 and, independently thereof, m is 0 or 1; with the provisos that a) the distance between the aminooxy radical H.sub.2 N--O-- and the amino group --NH.sub.2 is at least 3 and not more than 4 carbon atoms and that b) the two radicals H.sub.2 N--(CH.sub.2).sub.n -- and --(CH.sub.2).sub.m --O--NH.sub.2 are not bonded to the same ring carbon of A. The compounds of formula (I) and their salts are ornithine decarboxylase inhibitors.Type: GrantFiled: December 12, 1994Date of Patent: May 14, 1996Assignee: Ciba-Geigy CorporationInventors: Jorg Frei, Jaroslav Stanek
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Patent number: 5496857Abstract: A specially formulated environmental insecticide is provided which effectively controls whiteflies and other insects but is safe to humans, farm animals, pets, crops, and fish. The cost-effective non-polluting insecticide can be in the form of a 100% concentrate or an aqueous solution. The sprayable easy-to-use insecticide can comprise a synergistic blend of cottonseed oil amides, coconut oil amides, tall oil amides and a nonionic surfactant, as well as a chelating agent, a viscosity control agent and free amine.Type: GrantFiled: March 17, 1994Date of Patent: March 5, 1996Inventor: Eugene F. Targosz
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Patent number: 5489610Abstract: A method of treating a patient suffering from a condition requiring vasodilator therapy, comprising long term, continuous adminstration of an organic nitrite to the patient in a dosage form capable of delivering a sufficient therapeutic amount of nitrite to the bloodstream of the patient thereby providing effective vasodilator therapy for at least 24 hours without the development of tolerance in the patient. The method of the invention is useful in treating conditions such as angina, particularly chronic, stable angina pectoris, ischemic diseases and congestive heart failure, and for controlling hypertension and/or impotence in male patients.Type: GrantFiled: March 1, 1994Date of Patent: February 6, 1996Assignee: Research Foundation of the State University of New YorkInventors: Ho-Leung Fung, John A. Bauer
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5472984Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: December 29, 1993Date of Patent: December 5, 1995Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5455272Abstract: The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: ##STR1## Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R.sub.3 is an alkyl; and R.sub.4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl)nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl)nitronyl phenol (DMONP); N-tert-octyl-C-phenyl nitrone (OPN).Type: GrantFiled: October 22, 1993Date of Patent: October 3, 1995Assignee: Oklahoma Medical Research FoundationInventors: Edward G. Janzen, Allan L. Wilcox
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Patent number: 5444093Abstract: Wood preservatives contain a copper salt, a polyamine and a fatty amine and are used for preserving wood from fungi and termites.Type: GrantFiled: November 3, 1993Date of Patent: August 22, 1995Assignee: Dr. Wolman GmbHInventors: Reimer Goettsche, Hans-Volker Borck
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Patent number: 5411990Abstract: An industrial microbicide which comprises at least one haloglyoxime derivative of the formula (I): ##STR1## wherein X is a halogen atom; Y is a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; and Z is a hydrogen atom or an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms; and a known industrial microbicidal ingredient selected from the group consisting of an organonitrogen-sulfur compound, an organohalogen compound, an organonitrogen compound and an organosulfur compound; and optionally a carrier or diluent.Type: GrantFiled: May 17, 1993Date of Patent: May 2, 1995Assignees: Yoshitomi Pharmaceutical Industries Ltd., Katayama Chemical Inc.Inventors: Katsuji Tsuji, Hidenori Hirashima
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Patent number: 5362749Abstract: The use as a molluscicide of a chelate of aluminium (III) with a ligand of formula I or of iron (III) with a ligand of formula II[R.sup.1 COCHCOR.sup.2 ].sup.- I[R.sup.3 NO.N=O].sup.- IIwherein formulae II: R.sup.3 represents:C.sub.1 -C.sub.6 alkyl, provided that when the alkyl group contains more than four carbon atoms the group is a branched chain alkyl group.Type: GrantFiled: September 15, 1992Date of Patent: November 8, 1994Assignee: British Technology Group LimitedInventors: Ian F. Henderson, Joseph I. Bullock, Geoffrey G. Briggs, Leslie F. Larkworthy
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Patent number: 5278192Abstract: The present invention provides a novel method of vasodilator therapy for treating a patient suffering from a condition, comprising long term, continuous administration of an organic nitrite to a patient suffering from the condition in a dosage form capable of delivering a sufficient therapeutic amount of nitrite to the blood stream of the patent thereby providing effective vasodilator therapy for at least 24 hours without development of tolerance in the patient. The method of the invention is useful in treating conditions such as, for example, angina, particularly chronic, stable angina pectoris, ischemic diseases, congestive heart failure, for controlling hypertension and/or impotence in male patients.Any conventional drug delivery system can be employed in carrying out the method of the invention. The drug delivery system can take virtually as many different forms as there are dosage forms available for delivery of nitrite to a patient.Type: GrantFiled: July 2, 1992Date of Patent: January 11, 1994Assignee: The Research Foundation of State University of New YorkInventors: Ho-Leung Fung, John A. Bauer
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Patent number: RE36594Abstract: The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: ##STR1## Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R.sub.3 is an alkyl; and R.sub.4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl)nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl)nitronyl phenol (DMONP); N-tert-octyl-C-phenyl nitrone (OPN).Type: GrantFiled: October 2, 1997Date of Patent: February 29, 2000Assignee: Oklahoma Medical Research FoundationInventors: Edward G. Janzen, Allan L. Wilcox