Nitroxides, Oxyamines Or Hydroxylamines (i.e., N-o Or N-oh) Patents (Class 514/645)
  • Patent number: 6114392
    Abstract: 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: Grant
    Filed: April 16, 1996
    Date of Patent: September 5, 2000
    Inventors: Gad M. Gilad, Varda H. Gilad
  • Patent number: 6083988
    Abstract: 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: Grant
    Filed: September 4, 1997
    Date of Patent: July 4, 2000
    Inventor: David Alan Becker
  • Patent number: 6071970
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: June 6, 2000
    Assignee: 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
  • Patent number: 6056966
    Abstract: 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: Grant
    Filed: May 18, 1998
    Date of Patent: May 2, 2000
    Assignee: Baker Norton Pharmaceuticals, Inc.
    Inventors: Sami Selim, Robert Testman, Ho-Leung Fung, John A. Bauer
  • Patent number: 6045827
    Abstract: 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: Grant
    Filed: August 19, 1997
    Date of Patent: April 4, 2000
    Assignee: Meri Charmyne Russell
    Inventor: Meri Charmyne Russell
  • Patent number: 6046232
    Abstract: 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: Grant
    Filed: October 15, 1998
    Date of Patent: April 4, 2000
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: Judith A. Kelleher, Kirk R. Maples, Alina Dykman, Yong-Kang Zhang, Allan L. Wilcox, Julian Levell
  • Patent number: 6028106
    Abstract: 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: Grant
    Filed: October 29, 1997
    Date of Patent: February 22, 2000
    Assignees: Schering Aktiengesellschaft, Board of Regents, The Univ. of TX System
    Inventors: Robert E. Garfield, Kristof Chwalisz
  • Patent number: 6025384
    Abstract: 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: Grant
    Filed: February 13, 1998
    Date of Patent: February 15, 2000
    Assignee: LeukoSite, Inc.
    Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
  • Patent number: 5973011
    Abstract: 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: Grant
    Filed: September 27, 1996
    Date of Patent: October 26, 1999
    Assignee: ISIS PHARMA GmbH
    Inventors: Eike Albrecht Noack, Georg Kojda
  • Patent number: 5932538
    Abstract: 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: Grant
    Filed: February 2, 1996
    Date of Patent: August 3, 1999
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
  • Patent number: 5895783
    Abstract: 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: Grant
    Filed: July 16, 1993
    Date of Patent: April 20, 1999
    Assignees: Schering Aktiengesellschaft, The University of Texas
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampal Li
  • Patent number: 5891472
    Abstract: 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: Grant
    Filed: November 19, 1996
    Date of Patent: April 6, 1999
    Assignee: Meri Charmyne Russell
    Inventor: Meri Charmyne Russell
  • Patent number: 5840759
    Abstract: 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: Grant
    Filed: March 11, 1997
    Date of Patent: November 24, 1998
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
  • Patent number: 5837736
    Abstract: 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: Grant
    Filed: March 11, 1997
    Date of Patent: November 17, 1998
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
  • Patent number: 5817697
    Abstract: 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: Grant
    Filed: July 1, 1997
    Date of Patent: October 6, 1998
    Assignee: Schwarz Pharma AG
    Inventors: Hans-Michael Wolff, Dietrich Schacht, Martin Feelisch, Bruce Ramsay, John Francis Martin, Christoph Christopher Lees, Adam Julian De Belder
  • Patent number: 5814667
    Abstract: 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: Grant
    Filed: March 11, 1997
    Date of Patent: September 29, 1998
    Assignee: United States of America as represented by the Department of Health and Human Services
    Inventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
  • Patent number: 5811463
    Abstract: 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: Grant
    Filed: December 20, 1996
    Date of Patent: September 22, 1998
    Assignee: University of British Columbia
    Inventors: Peter Legzdins, Catherine C. Y. Pang, Michael J. Shaw
  • Patent number: 5795915
    Abstract: 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: Grant
    Filed: May 17, 1996
    Date of Patent: August 18, 1998
    Assignee: Laboratoire L. Lafon
    Inventor: Philippe Laurent
  • Patent number: 5789442
    Abstract: 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: Grant
    Filed: January 18, 1996
    Date of Patent: August 4, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Robert E. Garfield, Kristof Chwalisz
  • Patent number: 5750565
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: May 12, 1998
    Assignee: Cytomed, Inc.
    Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
  • Patent number: 5728714
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: March 17, 1998
    Inventor: Peter H. Proctor
  • Patent number: 5725839
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: March 10, 1998
    Inventor: Jen-Chang Hsia
  • Patent number: 5719150
    Abstract: 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: Grant
    Filed: November 14, 1996
    Date of Patent: February 17, 1998
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5658954
    Abstract: 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: Grant
    Filed: January 29, 1996
    Date of Patent: August 19, 1997
    Inventor: Eugene F. Targosz
  • Patent number: 5652270
    Abstract: 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: Grant
    Filed: June 17, 1996
    Date of Patent: July 29, 1997
    Assignee: Egis Gyogyszergyar RT
    Inventors: Zoltan Budai, Istvan Gacsalyi, Gabor Szenasi, Tibor Mezei, Aniko Kovacs, Gabor Blasko, Katalin Szemeredi, Gyula Simig, Lujza Petocz, Klara Reiter nee Esses
  • Patent number: 5650442
    Abstract: 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: Grant
    Filed: October 7, 1994
    Date of Patent: July 22, 1997
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
  • Patent number: 5648393
    Abstract: 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: Grant
    Filed: August 29, 1994
    Date of Patent: July 15, 1997
    Assignee: Brigham & Women's Hospital
    Inventors: Jonathan Stamler, Joseph Loscalzo, Adam Slivka, Daniel Simon, Robert Brown, Jeffrey Drazen
  • Patent number: 5646181
    Abstract: 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: Grant
    Filed: May 2, 1995
    Date of Patent: July 8, 1997
    Assignee: Research Foundation of State University of New York
    Inventors: Ho-Leung Fung, John Anthony Bauer
  • Patent number: 5631284
    Abstract: 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: Grant
    Filed: October 6, 1993
    Date of Patent: May 20, 1997
    Assignee: University of British Columbia
    Inventors: Peter Legzdins, Catherine C. Y. Pang, Michael J. Shaw
  • Patent number: 5622994
    Abstract: 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: Grant
    Filed: March 15, 1994
    Date of Patent: April 22, 1997
    Assignees: Oklahoma Medical Research Foundation, University of Kentucky Research Foundation
    Inventors: John M. Carney, Robert A. Floyd
  • Patent number: 5612381
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: March 18, 1997
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5610195
    Abstract: 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: Grant
    Filed: December 12, 1994
    Date of Patent: March 11, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: J org Frei, Jaroslav Stanek
  • Patent number: 5594032
    Abstract: 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: Grant
    Filed: November 10, 1994
    Date of Patent: January 14, 1997
    Inventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
  • Patent number: 5583101
    Abstract: 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: Grant
    Filed: July 15, 1994
    Date of Patent: December 10, 1996
    Assignees: Harvard College, Duke University
    Inventors: Jonathan Stamler, Lester Kobzik
  • Patent number: 5567411
    Abstract: 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: Grant
    Filed: September 29, 1994
    Date of Patent: October 22, 1996
    Assignee: State of Oregon Acting by and Through the State Board of Higher Education on Behalf of the University of Oregon
    Inventors: John F. W. Keana, Vladimir Martin, William H. Ralston
  • Patent number: 5552439
    Abstract: Provided is a method for treating inflammatory bowel disease in mammals utilizing certain phenol and benzamide compounds.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: September 3, 1996
    Assignee: Eli Lilly and Company
    Inventor: Jill A. Panetta
  • Patent number: 5532277
    Abstract: 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: Grant
    Filed: April 10, 1995
    Date of Patent: July 2, 1996
    Assignee: Oklahoma Medical Research Foundation
    Inventors: Edward G. Janzen, Allan L. Wilcox, Randall D. Hinton
  • Patent number: 5532219
    Abstract: 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: Grant
    Filed: April 5, 1993
    Date of Patent: July 2, 1996
    Assignee: The University of British Columbia
    Inventors: Patrick L. McGeer, Nobua Harada, Horoshi Kimura, Edith G. McGeer, Michael Schulzer
  • Patent number: 5527828
    Abstract: 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: Grant
    Filed: April 10, 1995
    Date of Patent: June 18, 1996
    Assignee: Oklahoma Medical Research Foundation
    Inventors: Edward G. Janzen, Allan L. Wilcox, Randall D. Hinton
  • Patent number: 5523322
    Abstract: 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: Grant
    Filed: June 30, 1994
    Date of Patent: June 4, 1996
    Assignee: Roussel UCLAF
    Inventors: Denis Blache, Christian Bloy, Bernard Hercelin
  • Patent number: 5516806
    Abstract: 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: Grant
    Filed: December 12, 1994
    Date of Patent: May 14, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Jorg Frei, Jaroslav Stanek
  • Patent number: 5496857
    Abstract: 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: Grant
    Filed: March 17, 1994
    Date of Patent: March 5, 1996
    Inventor: Eugene F. Targosz
  • Patent number: 5489610
    Abstract: 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: Grant
    Filed: March 1, 1994
    Date of Patent: February 6, 1996
    Assignee: Research Foundation of the State University of New York
    Inventors: Ho-Leung Fung, John A. Bauer
  • Patent number: 5472984
    Abstract: 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: Grant
    Filed: December 29, 1993
    Date of Patent: December 5, 1995
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5455272
    Abstract: 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: Grant
    Filed: October 22, 1993
    Date of Patent: October 3, 1995
    Assignee: Oklahoma Medical Research Foundation
    Inventors: Edward G. Janzen, Allan L. Wilcox
  • Patent number: 5444093
    Abstract: Wood preservatives contain a copper salt, a polyamine and a fatty amine and are used for preserving wood from fungi and termites.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: August 22, 1995
    Assignee: Dr. Wolman GmbH
    Inventors: Reimer Goettsche, Hans-Volker Borck
  • Patent number: 5411990
    Abstract: 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: Grant
    Filed: May 17, 1993
    Date of Patent: May 2, 1995
    Assignees: Yoshitomi Pharmaceutical Industries Ltd., Katayama Chemical Inc.
    Inventors: Katsuji Tsuji, Hidenori Hirashima
  • Patent number: 5362749
    Abstract: 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: Grant
    Filed: September 15, 1992
    Date of Patent: November 8, 1994
    Assignee: British Technology Group Limited
    Inventors: Ian F. Henderson, Joseph I. Bullock, Geoffrey G. Briggs, Leslie F. Larkworthy
  • Patent number: 5278192
    Abstract: 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: Grant
    Filed: July 2, 1992
    Date of Patent: January 11, 1994
    Assignee: The Research Foundation of State University of New York
    Inventors: Ho-Leung Fung, John A. Bauer
  • Patent number: RE36594
    Abstract: 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: Grant
    Filed: October 2, 1997
    Date of Patent: February 29, 2000
    Assignee: Oklahoma Medical Research Foundation
    Inventors: Edward G. Janzen, Allan L. Wilcox