Vasoconstrictor (nondecongestant) Patents (Class 514/930)
  • Patent number: 7923455
    Abstract: The present invention relates to a method for the prevention or the treatment of heart failure comprising administration of a therapeutically effective amount of an anticholinergic 1, medicaments for the prevention or treatment of heart failure comprising one or more, preferably one anticholinergic 1, and methods for the preparation of these medicaments.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: April 12, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Steven Kesten, Klaus Viel
  • Patent number: 7666914
    Abstract: Disclosed herein is a preparation for topically delivering and localizing therapeutic agents, comprising: a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; and a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Further disclosed is an associated method of topically delivering and localizing therapeutic agents, comprising the steps of: using a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; in combination with using a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Also disclosed are various courses of treatment which comprise applying the various disclosed combinations of agents to the patient's skin.
    Type: Grant
    Filed: June 3, 2004
    Date of Patent: February 23, 2010
    Inventors: David M. Richlin, George R. Doherty
  • Patent number: 7291592
    Abstract: Methods for treating a mammal suffering from massive blood loss comprising administering to the mammal a polymerized hemoglobin solution.
    Type: Grant
    Filed: October 3, 2003
    Date of Patent: November 6, 2007
    Assignee: Northfield Laboratories, Inc.
    Inventors: Steven Gould, Richard DeWoskin, Marc Doubleday, George Hides
  • Patent number: 7265087
    Abstract: A composition for the treatment of impaired glucose tolerance (IGT) including a compound which binds to a receptor for glucagon-like peptide-1, and a pharmaceutical carrier. The amount of the compound present is an effective amount to improve pancreatic ?-cell sensitivity to blood glucose levels in a human with IGT. Also, a method for improving the pattern of insulin secretory responses in a human with IGT by administering to the human a composition comprising a compound which binds to a receptor for glucagon-like peptide-1 and a pharmaceutical carrier.
    Type: Grant
    Filed: May 7, 1999
    Date of Patent: September 4, 2007
    Assignee: Amylin Pharmaceuticals, Inc.
    Inventors: Burkhard Göke, Maria Byrne, Thomas R. Coolidge
  • Patent number: 7122655
    Abstract: The present invention relates to screening methods that make use of Myosin Phosphatase-Rho interacting Protein (M-RIP) for the identification of novel therapeutics for hypertension and hypertensive conditions. Also disclosed are methods for treating or preventing hypertension or hypertensive conditions by administering to a mammal a therapeutically effective amount of an agent that reduces the level or activity of M-RIP. According to this invention, the agent decreases contractile and increases relaxant effects of smooth muscle cells, ultimately decreasing the systemic blood pressure of a mammal. For example, the agent may reduce binding of M-RIP to myosin phosphatase, RhoA, or both.
    Type: Grant
    Filed: November 17, 2003
    Date of Patent: October 17, 2006
    Assignee: New England Medical Center Hospital, Inc.
    Inventors: Michael E. Mendelsohn, Howard K. Surks
  • Patent number: 7115588
    Abstract: The present invention relates to compositions comprising semi-crystalline ?-1-4-N-acetylglucosamine polymers (p-GlcNac) and methods utilizing such polymers modulation of vascular structure and/or function. The compositions and methods disclosed are useful for stimulating, in a p-GlcNac concentration-dependent manner, endothelin-1 release, vasoconstriction, and/or reduction in blood flow out of a breached vessel, as well as for contributing to or effecting cessation of bleeding. The methods of the present invention comprise topical administration of materials comprising semi-crystalline p-GlcNac polymers that are free of proteins, and substantially free of single amino acids as well as other organic and inorganic contaminants, and whose constituent monosaccharide sugars are attached in a ?-1-4 conformation.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: October 3, 2006
    Assignee: Marine Polymer Technologies Inc.
    Inventors: John N. Vournakis, Sergio Finkielsztein
  • Patent number: 7094431
    Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: August 22, 2006
    Inventor: Mickey L. Peshoff
  • Patent number: 7041657
    Abstract: The present invention relates to compositions comprising semi-crystalline ?-1-4-N-acetylglucosamine polymers (p-GlcNac) and methods utilizing such polymers modulation of vascular structure and/or function. The compositions and methods disclosed are useful for stimulating, in a p-GlcNac concentration-dependent manner, endothelin-1 release, vasoconstriction, and/or reduction in blood flow out of a breached vessel, as well as for contributing to or effecting cessation of bleeding. The methods of the present invention comprise topical administration of materials comprising semi-crystalline p-GlcNac polymers that are free of proteins, and substantially free of single amino acids as well as other organic and inorganic contaminants, and whose constituent monosaccharide sugars are attached in a ?-1-4 conformation.
    Type: Grant
    Filed: February 12, 2001
    Date of Patent: May 9, 2006
    Assignee: Marine Polymer Technologies Inc.
    Inventors: John N Vournakis, Sergio Finkielsztein
  • Patent number: 6605447
    Abstract: 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: Grant
    Filed: September 14, 1998
    Date of Patent: August 12, 2003
    Assignee: Yale University
    Inventors: Robert M. Weiss, William C. Sessa, Marcia A. Wheeler, Shannon D. Smith
  • Patent number: 6333057
    Abstract: This invention relates to the topical and oral treatment of hair loss, especially androgenic alopecia, by providing formulations that include anti-androgens, especially extracts of the saw palmetto plant, co-enzyme Q, and acetyl carnitine, and optionally stimulators of adenylate cyclase to stimulate hair growth, to increase the luster of hair, and to decrease hair graying.
    Type: Grant
    Filed: July 16, 1998
    Date of Patent: December 25, 2001
    Inventor: Wilson T. Crandall
  • Patent number: 6184254
    Abstract: Methods of identifying compounds that relax or stimulate arterial tension through their action on perivascular sensory nerve calcium receptors are described. Compounds identified through such methods are useful for the treatment of hypertension, hypotension and other diseases and conditions that alter normal physiological blood pressure.
    Type: Grant
    Filed: November 13, 1998
    Date of Patent: February 6, 2001
    Assignee: Board of Regents, The University of Texas System
    Inventors: Richard D. Bukoski, Ka Bian
  • Patent number: 6037366
    Abstract: A composition including 2-hexyl cyanoacrylate and gold is useful in treating arteriovenous malformations (AVMs) and other body lumens to be blocked.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: March 14, 2000
    Assignee: Prohold Medical Technologies, Inc.
    Inventors: Robert E. Krall, Charles W. Kerber, Kimberly Knox
  • Patent number: 6020308
    Abstract: The present invention is directed to the use of an inhibitor of NO activity, such as a nitric oxide scavenger or an NO synthase inhibitor, as as an adjunct to treatment of inappropriate tissue vascularization disorders.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: February 1, 2000
    Assignees: Duke University, North Carolina State University, Apex Bioscience, Inc.
    Inventors: Mark W. Dewhirst, Robert E. Meyer, Joseph Bonaventura, Joseph DeAngelo
  • Patent number: 5965155
    Abstract: The invention relates to a pharmaceutic product as well as to a process for its production for a transdermal application in the prophylaxis and treatment of vasodilations, said pharmaceutic product comprising at least one skin-compatible auxiliary agent and portions of an active substance, characterized in that said pharmaceutic product contains as active substance pentetrazole.
    Type: Grant
    Filed: June 8, 1998
    Date of Patent: October 12, 1999
    Assignee: LTS Lohmann Therapie-Systeme GmbH & Co.
    Inventors: Fritz Herrmann, Thomas Hille
  • Patent number: 5962008
    Abstract: A medicament for use in the treatment of anorectal inflammation in hemorrhoids and the like contains a petroleum base, water, phenylephrine hydrochloride, squalene, and 8-hydroxyquinoline.
    Type: Grant
    Filed: May 22, 1998
    Date of Patent: October 5, 1999
    Inventor: MaryAnn Carroll
  • Patent number: 5942241
    Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.
    Type: Grant
    Filed: June 16, 1997
    Date of Patent: August 24, 1999
    Assignee: Euro-Celtique, S.A.
    Inventors: Mark Chasin, Richard Sackler, Ronald M. Burch, Paul Goldenheim, Joseph Tigner
  • Patent number: 5880101
    Abstract: The present invention relates to the use of at least one polyene macrolide for the preparation of pharmaceutical compositions for the treatment of diseases that are associated with an impaired energy turnover. Particularly, the present inventions allows to specifically stimulate the energy conversion in human cell, i.e. to stimulate the cell metabolism, and thus to treat or prevent a series of diseases.
    Type: Grant
    Filed: February 27, 1997
    Date of Patent: March 9, 1999
    Assignee: Dr. Zerle GmbH
    Inventor: Georgi Stankov
  • Patent number: 5776979
    Abstract: The present invention involves a method for prophylaxis or treatment of an animal for systemic hypotension induced by endotoxin and/or a biological response modifier such as the cytokines, IFN, TNF, IL-1 or IL-2 and the like. The method involves administering, preferably intravascularly, a therapeutically effective amount of dobutamine and an inhibitor of nitric oxide formation from arginine.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: July 7, 1998
    Assignees: Board of Regents, The University Of Texus System, Cornell Research Foundation, Inc.
    Inventors: Robert G. Kilbourn, Steven S. Gross, Owen W. Griffith
  • Patent number: 5770623
    Abstract: A method for prophylaxis or treatment of an animal for systemic hypotension induced by internal nitrogen oxide production. The method involves administering a therapeutically effective amount of certain arginine derivatives to inhibit nitrogen oxide formation from arginine. Preferably N.sup.G -substituted arginine or an N.sup.G,N.sup.G -disubstituted arginine (having at least one hydrogen on a terminal guanidino amino group replaced by another atomic species) is administered to an animal possibly developing or already having such induced systemic hypotension. The arginine derivatives are preferably of the L configuration and include pharmaceutically acceptable addition salts. Prophylaxis or treatment of systemic hypotension in a patient which has been induced by chemotherapeutic treatment with biologic response modifiers such as tumor necrosis factor or interleukin-2 may be accomplished. Treatment of an animal for systemic hypotension induced by endotoxin, i.e.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: June 23, 1998
    Assignees: Board of Regents, The University of Texas System, Cornell Research Foundation, Inc.
    Inventors: Robert G. Kilbourn, Steven S. Gross, Roberto Levi, Owen W. Griffith
  • Patent number: 5593664
    Abstract: The present invention relates to the use of certain anionic polyamide and polyurea oligomers for inhibiting angiogenesis, and for their use in treating diseases associated with angiogenesis. These oligomers have a number average molecular weight (M.sub.n) less than 10,000, comprise recurring units coupled by carbonyl linking moieties and have predominantly linear geometry such that regular spacing between anionic groups exists in an aqueous medium. The oligomers also have a preferably linear backbone and be be in their salt form, preferably wherein the salt is pharmaceutically acceptable.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: January 14, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Paul S. Wright, Alan J. Bitonti
  • Patent number: 5545625
    Abstract: Administration of argininosuccinate synthetase activity reducing agents, e.g., argininosuccinate synthetase induction blocking agents (e.g., antibiotics that bind to DNA sequences present in the upstream regulatory region of the argininosuccinate synthetase gene, such as mithramycin) and argininosuccinate synthetase inhibitors (e.g., L-citrulline antagonists such as methyl citrulline and L-aspartate antagonists such as D-aspartate) is useful to prevent or treat sepsis or cytokine-induced systemic hypotension, is useful in the treatment of sepsis or cytokine-induced systemic hypotension to restore vascular sensitivity to the effects of .alpha..sub.1 -adrenergic agonists, and is useful to suppress an immune response, e.g., in treating inflammation. In one embodiment, certain argininosuccinate synthetase activity reducing agents are used together with arginine antagonists to treat sepsis or cytokine induced hypotension.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: August 13, 1996
    Assignee: The Medical College of Wisconsin Research Foundation, Inc.
    Inventors: Steven S. Gross, Owen W. Griffith
  • Patent number: 5510331
    Abstract: Peptides of the formulaR.sub.1 --HX.sub.1 DX.sub.2 IX.sub.3 Iwherein R.sub.1, X.sub.1, X.sub.2 and X.sub.3 are defined as in the specification having antihypertensive activity without vascoconstricting activity.
    Type: Grant
    Filed: October 13, 1994
    Date of Patent: April 23, 1996
    Assignee: Roussel UCLAF
    Inventors: Gilles Hamon, Eve Mahe, Dung Le-Nguyen
  • Patent number: 5385935
    Abstract: This invention provides a method for treating patients to inhibit restenosis associated with coronary intervention. A 600 mg dosage of Tranilast for a treatment period of three consecutive months after coronary intervention lowers the incidence of restenosis, and reduces the degree of stenosis in patients.
    Type: Grant
    Filed: September 7, 1993
    Date of Patent: January 31, 1995
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideo Tamai, Kinzo Ueda, Yung-sheng Hsu
  • Patent number: 5373010
    Abstract: A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## , pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms.
    Type: Grant
    Filed: February 10, 1994
    Date of Patent: December 13, 1994
    Assignee: Allergan, Inc.
    Inventors: Charles Gluchowski, Michael E. Garst, James A. Burke, Larry A. Wheeler
  • Patent number: 5340587
    Abstract: A method and system for treating bronchial constriction. The system includes a liposome composition containing a .beta..sub.2 -adrenoreceptor agonist in a liposome-entrapped form, and a device for aerosolizing a metered quantity of the composition. The drug in liposome aerosol form is substantially more effective in bronchodilation, over a substantially longer time, than the same amount of drug in free-drug aerosol form.
    Type: Grant
    Filed: June 13, 1989
    Date of Patent: August 23, 1994
    Assignee: Liposome Technology, Inc.
    Inventors: Paul J. Mihalko, Robert M. Abra, Ramachandran Radhakrishnan
  • Patent number: 5312835
    Abstract: The present invention involves a method for prophylaxis or treatment of an animal for systemic hypotension induced by endotoxin and/or a biological response modifier such as the cytokines, IFN, TNF, IL-1 or IL-2 and the like. Said method involves administering, preferably intravascularly, a therapeutically effective amount of dobutamine and an inhibitor of nitric oxide formation from arginine. Although preferable administration is intravascular, it is contemplated that other parenteral administration routes such as intraperitoneal, intramuscular or subdermal injection, for example, may prove useful. Enteral or topical administration of arginine analogs may also prove beneficial under certain clinical conditions.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: May 17, 1994
    Assignees: Board of Regents, the University of Texas System, Cornell Research Foundation, Inc.
    Inventors: Robert G. Kilbourn, Steven S. Gross, Owen W. Griffith
  • Patent number: 5216025
    Abstract: A method for treatment of an animal for systemic hypotension induced by internal nitric oxide production caused by endotoxin or cytokines. The method involves administering an .alpha..sub.1 adrenergic agonist and an amount of an inhibitor of nitric oxide formation from argiResearch relating to the development of this invention was supported by the United States Public Health Service grants which gives the United States government certain rights to use of the present invention.
    Type: Grant
    Filed: July 1, 1991
    Date of Patent: June 1, 1993
    Assignees: Board of Regents, The University of Texas System, Cornell Research Foundation, Inc.
    Inventors: Steven S. Gross, Robert G. Kilbourn, Roberto Levi
  • Patent number: 5194448
    Abstract: Composition containing nervonic acid (cis-tetracos-15-enoic acid) in a physiologically acceptable form are useful in the treatment of demyelinating disease, such as multiple sclerosis. Additional long chain fatty acids of chain length C16 to C26, especially erucic acid, or their esters, may be included in such compositions.
    Type: Grant
    Filed: August 6, 1991
    Date of Patent: March 16, 1993
    Assignee: Croda International PLC
    Inventors: Keith Coupland, Nigel A. Langley
  • Patent number: 5116878
    Abstract: This medicinal composition for the treatment and prevention of the symptoms of heart failure contains, by way of active principle, at least one compound chosen from 2-amino-1-(2,5-dimethoxyphenyl)-1-propanol (methoxamine) and its pharmaceutically acceptable salts, and it is presented in a form which can be administered by inhalation (aerosol or nebulizate).It was demonstrated, in particular, that the administration of methoxamine-HCl by inhalation, at a unit dosage of 10 mg, in the form of a 2% (w/v) solution in physiological saline, decreases airways resistance in subjects suffering from decompensated left ventricular failure, and increases the exertion tolerance of patients suffering from compensated left vetricular failure, whether the latter is of ischemic origin or otherwise.
    Type: Grant
    Filed: June 14, 1989
    Date of Patent: May 26, 1992
    Assignee: Universite de Paris V
    Inventors: Laure Cabanes, Alain Lockhart, Simon Weber
  • Patent number: 5091194
    Abstract: The invention relates to cosmetic compositions for the treatment of phlebectasiae, particularly haemorrhoids and phlebectasiae mainly occurring on the lower limbs optionally accompanied with phlebitis, as well as for relieving the phlebalgia thereby induced, with comprises potassium aluminum sulfate and/or one or more hydrates thereof in admixture with one or more cosemtically acceptable carriers, auxiliary and optionally odorizing materials commonly used in the preparation of cosmetics.The compositions according to the invention preferably contain potassium aluminum sulfate dodecahydrate in an amount of 10 to 90% by weight, most preferably 40 to 70% by weight and are preferably formulated to ointments, creams, lotions or pastes.
    Type: Grant
    Filed: December 14, 1988
    Date of Patent: February 25, 1992
    Inventor: Laszlo Hanko
  • Patent number: 5041284
    Abstract: A method for preventing frostbite of body portions is disclosed. The method includes applying an antiperspirant composition to the body portion and covering the body portion with a thermally insulating material.
    Type: Grant
    Filed: September 8, 1989
    Date of Patent: August 20, 1991
    Inventor: Alphonso L. Mack
  • Patent number: 5036107
    Abstract: 1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C.sub.1 to C.sub.7 alkyl, C.sub.3 to C.sub.6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one.The compounds are highly specific M.sub.1 -AChR antagonists with relatively prolonged duration of activity.
    Type: Grant
    Filed: November 16, 1989
    Date of Patent: July 30, 1991
    Assignee: Marion Merrell Dow Inc.
    Inventors: Waclaw J. Rzeszotarski, Maria E. Guzewska, Daniel W. McPherson, Ciro J. Spagnuolo, Kenneth J. Natalie, Jr.
  • Patent number: 5028627
    Abstract: A method for prophylaxis of treatment of an animal for systemic hypotension induced by internal nitrogen oxide production. The method involves administering a therapeutically effective amount of certain arginine derivatives to inhibit nitrogen oxide formation from arginine. Preferaby N.sup.G -substituted arginine or an N.sup.G,N.sup.G -disubstituted arginine (having at least one hydrogen on a terminal guanidino amino group replaced by another atomic species) is administered to an animal possibly developing or already having induced systemic hypotension. The arginine derivatives are preferably of the L configuration and include pharmaceutically acceptable addition salts. Prophylaxis or treatment or systemic hypotension in a patient which has been induced by chemotherapeutic treatment with biologic response modifiers such as tumor necrosis factor or interleukin-2 may be accomplished. Treatment of an animal for systemic hypotension induced by endotoxin, i.e.
    Type: Grant
    Filed: September 13, 1989
    Date of Patent: July 2, 1991
    Assignees: Cornell Research Foundation, Inc., Board of Regents, The University of Texas System
    Inventors: Robert G. Kilbourn, Steven Gross, Roberto Levi, Owen W. Griffith
  • Patent number: 5010096
    Abstract: The use of a compound of formula (I) or a physiologically acceptable salt or hydrate thereof in the treatment, relief or prevention of the effects of cerebral ischaemia ##STR1## Compounds of formula (I) are described in UK Published Patent Application No. 2157691A.The compounds of formula (I) have been found to protect mammals, including man, against neuronal damage resulting from cerebral ischaemia.The preferred compound for use in this indication is (.+-.)-trans-5-fluoro-2,3,3a,9a-tetrahydro-1H-[1,4]-benzodioxino[2,3-c]- pyrrole (formula (I), R=H, R.sup.1 =F, R.sup.2 =H), especially in the form of its hydrochloride salt.
    Type: Grant
    Filed: November 30, 1989
    Date of Patent: April 23, 1991
    Assignee: Glaxo Group Limited
    Inventors: Ann G. Hayes, Phillip J. Birch
  • Patent number: 5002767
    Abstract: The invention relates to a therapeutic composition containing, as the active principle, .alpha.-linolenic acid and an alcohol of vegetable origin, such as a tocopherol or sitosterol. Preferably, the composition contains other fatty acids and is an organic extract of plants, especially of the Resedaceae family.The invention also relates to the plant extracts as novel products.The therapeutic composition is especially useful as an antiinflammatory.
    Type: Grant
    Filed: August 24, 1988
    Date of Patent: March 26, 1991
    Assignee: Laboratories Natura Medica
    Inventor: Jean-Pierre Masse
  • Patent number: 4994483
    Abstract: Indole derivatives are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sub.2 is a hydrogen, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, phenyl, phen(C.sub.1-4)alkyl or C.sub.5-7 cycloalkyl; R.sub.3 and R.sub.4 are hydrogen, C.sub.1-3 alkyl or propenyl groups or together form an aralkylidene group; Alk is C.sub.2 -C.sub.3 alkylene chain and A is C.sub.2 -C.sub.5 alkylene chainand its physiologically acceptable salts and solvates.The compounds may be prepared, for example, by cyclization of a compound of general formula (II): ##STR2## where Q is the group NR.sub.3 R.sub.4 or a protected derivative thereof or a leaving group and R.sub.1 l, R.sub.2, R.sub.3, R.sub.4, A and Alk are as defined for formula (I).The compounds have a selective vosoconstrictor action and are useful in treating pain such as migraine. The compounds may be formulated as pharmaceutical compositions in conventional manner, preferably for oral administration.
    Type: Grant
    Filed: November 30, 1989
    Date of Patent: February 19, 1991
    Assignee: Glaxo Group Limited
    Inventors: Alexander W. Oxford, Brian Evans, Michael D. Dowle, Ian H. Coates
  • Patent number: 4978332
    Abstract: A pharmaceutical composition and method of treating cellular disorders involving abnormal solid cellular growths which comprises administering a pharmaceutical composition containing cytotoxic agents in combination with a vasoconstrictive drug. Enhanced effectiveness of the composition is observed, with reduced cytotoxic effects on cells distant from the site of introduction. Agents may be included to enhance therapeutic gain and reduce adverse affects to normal tissue.
    Type: Grant
    Filed: September 28, 1987
    Date of Patent: December 18, 1990
    Assignee: Matrix Pharmaceutical, Inc.
    Inventors: Edward E. Luck, Dennis M. Brown
  • Patent number: 4970301
    Abstract: Compound of general formula I: ##STR1## in which: A is a single or double bond,R.sub.1 and R.sub.3, which may be identical or different, are each a hydrogen atom, an alkoxycarbonylmethylene radical of formula --CH.sub.2 CO.sub.2 R.sub.4 (in which R.sub.4 denotes an alkyl radical having 1 to 5 carbon atoms) or a radical of formula W: ##STR2## (in which n is equal to 0 or 1 and R.sub.5, R.sub.6 and R.sub.7, which may be identical or different, are each a hydrogen or halogen atom, a hydroxyl radical, a trifluoromethyl radical, a lower alkyl radical containing 1 to 5 carbon atoms or an alkoxy radical containing 1 to 5 carbon atoms),R.sub.2 is a hydrogen atom, an alkoxycarbonylmethylene radical of formula --CH.sub.2 CO.sub.2 R.sub.4, a radical of formula W, or a .beta.-glucose or rutinose molecule linked to the oxygen to which it is attached with a glycoside bond,on condition, however, that at least either R.sub.1 or R.sub.2 or R.sub.
    Type: Grant
    Filed: November 29, 1988
    Date of Patent: November 13, 1990
    Assignee: Adir et Cie
    Inventors: Yves Rolland, Jacques DuHault
  • Patent number: 4853216
    Abstract: Processes and Compositions for effecting a pilomotor effect on a hair-bearing skin area by the application of an alpha.sub.1 adrenergic agonist having essentially only alpha.sub.1 adrenergic agonist activity.
    Type: Grant
    Filed: April 2, 1987
    Date of Patent: August 1, 1989
    Assignee: Bristol-Myers Company
    Inventors: Randy J. Koslo, Alison B. Lukacsko
  • Patent number: 4851450
    Abstract: The present invention is a group of biologically active agents, di-hydroxy alkyl glycerols with vicinal hydroxyl groups and their acetyl-derivatives having the general formula: ##STR1## where R is selected from the group of H and CH.sub.3 CO-- and x+y is between 9 and 21; and methods for their synthesis. The compounds of the present invention are synthesized starting with an unsaturated 1-O-alkyl-glycerol of the formula: ##STR2## where R is an unsaturated alkyl group with a chain length of 12 to 24 carbon atoms and introducing a vicinal hydroxyl into the alkyl carbon chain using either osmium tetroxide or performic acid, produced by mixing formic acid with hydrogen peroxide.The new glycerol ether derivatives exert platelet activating factor (PAF)-like action in vitro in low concentrations, and, surprisingly, in higher doses act as selective antagonists of PAF, or 1-O-alkyl-2-O-acetyl-sn-glyceryl-3-phosphorylcholine (AGEPC), activities.
    Type: Grant
    Filed: October 26, 1987
    Date of Patent: July 25, 1989
    Inventor: Constantine A. Demopoulos
  • Patent number: 4795756
    Abstract: Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, phenyl optionally substituted by C.sub.1-3 alkoxy or phen(C.sub.1-4) alkyl in which the phenyl ring is optionally substituted by C.sub.1-3 alkoxy;R.sub.2 is H or C.sub.1-6 alkyl;R.sub.3 is H or C.sub.1-3 alkyl;R.sub.4 and R.sub.5 independently represents H, C.sub.1-3 alkyl or 2-propenyl; andn represents zero or 1;and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. The compounds may be formulated as pharmaceutical compositions with physiologically acceptable carrier or excipients for administration by any convenient route. Various methods for the preparation of the compounds (I) are disclosed.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: January 3, 1989
    Assignee: Glaxo Group Limited
    Inventors: Alexander W. Oxford, Michael D. Dowle
  • Patent number: 4785014
    Abstract: Disclosed is a method of treating cognitive decline in a normal aged primate by administering thereto a therapeutically effective amount of 2-[(2,6-dichlorophenyl)-amino]-2-imidazoline or a nontoxic, pharmaceutically acceptable salt thereof. Administration is preferably in amounts of at least about 0.001 mg/day.
    Type: Grant
    Filed: November 6, 1986
    Date of Patent: November 15, 1988
    Assignee: Yale University
    Inventors: Patricia S. Goldman-Rakic, Amy F. T. Arnsten
  • Patent number: RE39150
    Abstract: A composition including 2-hexyl cyanoacrylate and goal is useful in treating arteriovenous malformations (AVMs) and other body lumens to be blocked.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: June 27, 2006
    Assignee: Prohold Technologies, Inc.
    Inventors: Robert E. Krall, Charles W. Kerber, Kimberly Knox
  • Patent number: RE42377
    Abstract: A composition including 2-hexyl cyanoacrylate and gold is useful in treating arteriovenous malformations (AVMs) and other body lumens to be blocked.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: May 17, 2011
    Assignees: Stryker Corporation, Stryker NV Operations Limited
    Inventors: Robert E. Krall, Charles W. Kerber, Kimberly Knox