Bicyclo Ring System Patents (Class 514/657)
  • Publication number: 20030220382
    Abstract: The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: R1 and R2 include alkyl and phenylalkyl; R3 is hydrogen or alkyl; and R4 and R5 include alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using compounds of Formula (I).
    Type: Application
    Filed: November 4, 2002
    Publication date: November 27, 2003
    Inventors: Nancy Sue Barta, Christopher Franklin Bigge
  • Patent number: 6649614
    Abstract: The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or anti-anxiety agent.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: November 18, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Emma Joanne Carlson, Nadia Melanie Rupniak
  • Publication number: 20030212145
    Abstract: The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an effective illness, a neurodegenerative disease, a neurotoxic injury, stroke, brain ischemia, a head trauma injury, a spinal trauma injury, neurotrauma, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan.
    Type: Application
    Filed: November 27, 2002
    Publication date: November 13, 2003
    Applicants: Teva Pharmaceutical Industries, Ltd., Technion Research Development Foundation, Ltd.
    Inventors: Moussa B.H. Youdim, John P.M. Finberg, Ruth Levy, Jeffrey Sterling, David Lerner, Haim Yellin, Alex Veinberg
  • Publication number: 20030199578
    Abstract: The present invention relates to compounds and their ability to act as potassium channel openers.
    Type: Application
    Filed: April 19, 2002
    Publication date: October 23, 2003
    Inventors: Sean C. Turner, Neil A. Castle, William A. Carroll, Tammie K. White
  • Patent number: 6630514
    Abstract: The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, stroke, brain ischemia, a head trauma injury, a spinal trauma injury, neurotrauma, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan, or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: October 7, 2003
    Assignees: Teva Pharmaceutical Industries, Ltd., Technion Research and Development Foundation, Ltd.
    Inventors: Moussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Jeffrey Sterling
  • Patent number: 6624201
    Abstract: The invention relates to high purity (1R,2S,4R)-(−)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof containing not more than 0.2% of (1R,3S,4R)-3-[(2′-{N,N-dimethylamino}-ethyl)]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane-2-one and/or of a pharmaceutically acceptable acid addition salt thereof. Furthermore the invention is concerned with a process for the preparation of these compounds. Moreover the invention relates to medicaments containing 1 or more of these compounds and their use.
    Type: Grant
    Filed: October 30, 2001
    Date of Patent: September 23, 2003
    Assignee: Orion Corporation
    Inventors: Gyula Lukács, Gyula Simig, Tibor Mezei, Zoltán Budai, Márta Porcs-Makkay, György Krasznai, Kálmán Nagy, Györgyi Donáth Vereczkey, Tibor Szabó, Norbert Németh, János Szulágyi
  • Patent number: 6613313
    Abstract: A hair dye composition containing at least one of the following compounds: or analogues thereof; and a method for dyeing hair which comprises a step of applying to the hair the hair dye composition is used. The dye composition of the invention exhibits excellent spreadability, applicability, level-dyeing property and shampoo resistance.
    Type: Grant
    Filed: November 27, 1998
    Date of Patent: September 2, 2003
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Keizo Kimura
  • Publication number: 20030158266
    Abstract: 2-Aminotetralines, a process for their preparation, and pharmaceutical compositions, for the prevention and therapeutic treatment of inflammatory pathologies (particularly septic shock) and/or autoimmune pathologies in which the aetiopathogenic role of inflammatory cytokines has been ascertained.
    Type: Application
    Filed: March 26, 2001
    Publication date: August 21, 2003
    Applicant: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Nicola Fanto, Gian Piero Moretti, Piero Foresta
  • Patent number: 6589996
    Abstract: A method for the treatment of disorders relating to serotonergic system in humans, for example depression and anxiety, comprising orally administering deramciclane in a daily dosage of about 20 to about 60 mg.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: July 8, 2003
    Assignee: Orion Corporation
    Inventors: Outi Mäki-Ikola, Harri Kanerva
  • Publication number: 20030109500
    Abstract: Treatment of warm-blooded animals having a tumor or non-malignant hypervascularation, by administering a sufficient amount of a cytotoxic agent formulated into a phosphate prodrug form having substrate specificity for microvessel phosphatases, so that microvessels are destroyed preferentially over other normal tissues, because the less cytotoxic prodrug form is converted to the highly cytotoxic dephosphorylated form.
    Type: Application
    Filed: August 14, 2002
    Publication date: June 12, 2003
    Inventors: Ronald W. Pero, David Sherris, Kevin G. Pinney, Vani P. Mocharla, Zhi Chen
  • Patent number: 6576671
    Abstract: The invention relates to a method of treatment of left ventricular dysfunction, by administering to a subject suffering from left ventricular remodeling a therapeutically effective amount of 5,6-dihydroxy-2-methylaminotetralin or 5,6-diisobutyroyl-oxy-2-methyl-aminotetralin, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: June 10, 2003
    Assignee: Chiese Farmaceutici S.p.A.
    Inventors: Stefano Bongrani, Roberta Razzetti, Maurizio Civelli, Alberto Umile, Paolo Chiesi
  • Patent number: 6552014
    Abstract: The present invention pertains to methods for reducing the platelet activation state in an individual comprising administering a selective serotonin reuptake inhibitor (SSRI). The platelet activation state is reduced upon administering a SSRI, as measured by one or more platelet activation markers. The invention also relates to methods for treating or preventing an individual at risk for a vascular event, disease or disorder by administering a SSRI.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: April 22, 2003
    Assignee: HeartDrug Research, L.L.C.
    Inventors: Victor L. Serebruany, Paul A. Gurbel, Christopher M. O'Connor
  • Publication number: 20030065038
    Abstract: The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, stroke, brain ischemia, a head trauma injury, a spinal trauma injury, neurotrauma, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargy-1-aminoindan, or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject.
    Type: Application
    Filed: October 26, 2001
    Publication date: April 3, 2003
    Applicant: Teva Pharmaceutical Industries, Ltd.
    Inventors: Moussa B.H. Youdim, John P.M. Finberg, Ruth Levy, Jeffrey Sterling
  • Patent number: 6541478
    Abstract: Nicotine dependency is treated by administration of an opioid antagonist. In some embodiments, rapid or ultra rapid detoxification techniques include using a combination of an effective amount of an opioid antagonist such as nalmefene, naloxone or naltrexone or a mixture of any one of these, and either clonidine or related compounds either while awake, or while under sedation or anesthesia, followed by continued administration of an effective amount of an opioid antagonist with or without agents that enhance nicotine dependency treatment.
    Type: Grant
    Filed: September 16, 1999
    Date of Patent: April 1, 2003
    Assignee: Yale University
    Inventors: Stephanie O'Malley, Boris Meandzija, Suchitra Krishnan-Sarin
  • Publication number: 20030055112
    Abstract: The present invention is directed to forms II, III, V, VI, VII, VIII, IX and X of sertraline hydrochloride and novel methods for their preparation. According to the present invention, sertraline hydrochloride polymorph II may be produced by slurrying sertraline hydrochloride polymorph VI in aprotic organic solvent. Sertraline hydrochloride polymorphic form III may be produced by heating sertraline hydrochloride polymorphs V and VI. Sertraline hydrochloride forms V and VI may be produced from either sertraline hydrochloride or sertraline base by crystallization. Sertraline hydrochloride Form VII may be produced by suspending sertraline chloride polymorph V in water, followed by filtration. Sertraline hydrochloride Forms VIII and IX may be produced by suspending sertraline base in water followed by acidification and filtration. Sertraline hydrochloride Form X may be produced by suspending sertraline hydrochloride in benzyl alcohol with heating, followed by filtration.
    Type: Application
    Filed: August 13, 2002
    Publication date: March 20, 2003
    Inventors: Eduard Schwartz, Tamar Nidam, Anita Liberman, Marioara Mendelovici, Judith Aronhime, Claude Singer, Evgeni Valdman
  • Patent number: 6528685
    Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: March 4, 2003
    Assignees: Teva Pharmaceutical Industries, Ltd., Technion Research and Development Foundation, Ltd.
    Inventors: Sasson Cohen, Yaacov Herzig, Ruth Levy, Mitchell Shirvan, Jeff Sterling, Alex Veinberg, Moussa B. H. Youdim, John P. M. Finberg
  • Patent number: 6518291
    Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: September 14, 1999
    Date of Patent: February 11, 2003
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
  • Patent number: 6500849
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: January 26, 1999
    Date of Patent: December 31, 2002
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: John Joseph Tegeler, Barbara Seavey Rauckman, Russell Richard Lee Hamer, Brian Scott Freed, Gregory Harold Merriman
  • Publication number: 20020173511
    Abstract: A method of treating Mild Cognitive Impairment has been discovered. The treatment method comprises administering an effective amount of a serotonergic agent, including, but not limited to dexnorfenfluramine. The agent can be any serotonergic agonist, partial agonist, serotonin reuptake inhibitor, or combinations of these agents. The treatment method also encompasses combinations of serotonergic agents and non-steroidal anti-inflammatory agents. The treatment method may also delay the onset of Mild Cognitive Impairment, dementia, or both.
    Type: Application
    Filed: November 8, 2001
    Publication date: November 21, 2002
    Inventors: Richard J. Wurtman, Robert K. K. Lee
  • Patent number: 6462056
    Abstract: The invention relates to novel oxazolidine derivatives of the formula in which R1, R2 and R3 have the meanings stated in claim 1, their salts and processes for preparing the compounds according to the invention. The compounds of the formula I act as 5-HT2A antagonists with a 5-HT reuptake-inhibiting, antidepressant or anxiolytic effect and can be used to produce pharmaceuticals.
    Type: Grant
    Filed: August 25, 1999
    Date of Patent: October 8, 2002
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Henning Böttcher, Helmut Prücher, Hartmut Greiner, Gerd Bartoszyk, Christoph Seyfried
  • Patent number: 6452054
    Abstract: The present invention is directed to novel polymorphic Forms XI, XII, XIII, XIV, XV and XVI of sertraline hydrochloride, to processes for preparing them, methods of using them to treat disease, methods of using them to make other sertraline hydrochloride forms, and to pharmaceutical dosages containing the novel forms.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: September 17, 2002
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Judith Aronhime, Marioara Mendelovici, Tamar Nidam, Claude Singer
  • Patent number: 6448295
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 10, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6441049
    Abstract: The invention is directed to a method of treating a neurodegenerative disorder in a subject in need thereof which comprises administering to the subject an amount of a compound effective to inhibit the interaction of amyloid-beta with alpha-7 nicotinic acetylcholine receptors.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: August 27, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Allen B. Reitz, David A. Demeter, Daniel H. S. Lee, Hoau-Yan Wang, Robert H. Chen, Tina Morgan Ross, Malcolm K. Scott, Carlos R. Plata-Salaman
  • Publication number: 20020115715
    Abstract: Amine and amide derivatives of the formula: 1
    Type: Application
    Filed: February 7, 2002
    Publication date: August 22, 2002
    Inventors: Scott L. Dax, James McNally, Mark Youngman
  • Patent number: 6436973
    Abstract: The invention concerns LTA4 hydrolase inhibiting compositions of formula (1) as set forth below. It also concerns their therapeutic, in particular anti-inflammatory, applications.
    Type: Grant
    Filed: June 11, 2001
    Date of Patent: August 20, 2002
    Assignees: Bioprojet, Institut National de la Sante et de la Recherche Medicale (Inserm)
    Inventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte
  • Patent number: 6413987
    Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: July 2, 2002
    Assignee: Bridge Pharma, Inc.
    Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
  • Patent number: 6387956
    Abstract: A method of treating an obsessive-compulsive spectrum disorder comprises the step of administering an effective amount of tramadol to an individual.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: May 14, 2002
    Assignee: University of Cincinnati
    Inventors: Nathan A. Shapira, Toby D. Goldsmith, Paul E. Keck, Jr.
  • Patent number: 6380236
    Abstract: A method of treating onychomycosis is described which includes administration to an infected area around a nail of a patient a tissue softening composition containing urea and an antifungal composition in one or separate compositions, concurrently or non-concurrently. Also described is a kit which contains the unit dosage forms, a protective gel and appropriate dressings for ready application.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: April 30, 2002
    Assignee: Bradley Pharmaceuticals, Inc.
    Inventor: Daniel Glassman
  • Patent number: 6376545
    Abstract: The present invention relates to a dispersible pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester, a therapeutically effective amount of a decarboxylase inhibitor, a filler, a disintegrant, and a lubricant. The present invention also provides a method of preparing the pharmaceutical composition described herein.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: April 23, 2002
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventor: Galit Levin
  • Patent number: 6369051
    Abstract: This invention comprises methods of depression, anxiety, generalized anxiety disorder (GAD), hot flush, post partum depression, premenstrual syndrome, obesity, obsessive compulsive disorder, post-traumatic stress disorder, social phobia, disruptive behavior disorders, impulse control disorders, borderline personality disorder, chronic fatigue disorder, premature ejaculation, pain, attention deficit disorders, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa, or Shy Drager Syndrome comprising administration of a selective serotonin reuptake inhibitor and compound of the formulae I or II: wherein Z is a moiety selected from the group of: wherein: R1 is selected from H, OH or the C1-C12 esters or C1-C12 alkyl ethers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated e
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: April 9, 2002
    Assignee: American Home Products Corporation
    Inventor: Simon Nicholas Jenkins
  • Publication number: 20020035105
    Abstract: The neuropathic pain alleviating effectiveness of an antidepressant is significantly potentiated by administering the antidepressant prior to, with or following the administration of a nontoxic NMDA receptor antagonist.
    Type: Application
    Filed: September 28, 2001
    Publication date: March 21, 2002
    Inventor: Frank S. Caruso
  • Publication number: 20020013374
    Abstract: The invention is directed to a method of treating a neurodegenerative disorder in a subject in need thereof which comprises administering to the subject an amount of a compound effective to inhibit the interaction of amyloid-beta with alpha-7 nicotinic acetylcholine receptors.
    Type: Application
    Filed: May 27, 1999
    Publication date: January 31, 2002
    Inventors: ALLEN B. REITZ, DAVID A. DEMETER, DANIEL H.S. LEE, HOAU-YAN WANG, ROBERT H. CHEN, TINA MORGAN ROSS, MALCOLM K. SCOTT, CARLOS R. PLATA-SALAMAN
  • Patent number: 6329399
    Abstract: Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. [in the formula (1, R1 represents a C1-5 alkyl group which may be halogenated, R2 represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3 represents oxygen atom or a methylene group which may be substituted by a C1-4 alkyl group; and R4 represents 1-or 2 naphthyl group or a phenyl group which may be substituted.
    Type: Grant
    Filed: May 18, 2000
    Date of Patent: December 11, 2001
    Assignee: Pola Chemical Industries, Inc.
    Inventors: Takao Itoh, Takuji Nakashima, Akira Nozawa, Kouji Yokoyama, Hiroyuki Takimoto, Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima
  • Publication number: 20010044474
    Abstract: A controlled release dosage form for sertraline has a core comprising a sertraline-containing composition and a water-swellable composition wherein the water-swellable composition is in a separate region within the core. A coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. In one embodiment, the dosage form releases sertraline to the use environment at an average rate of 6 to 10 wt % per hour from the second to the twenth hour after introduction to a use environment and less than about 25 wt % for the first two hours and at least 70 wt % by the twelfth hour, where the percentages correspond to the mass of drug released from the tablet divided by the total mass of drug originally present in the tablet.
    Type: Application
    Filed: December 20, 2000
    Publication date: November 22, 2001
    Inventors: William J. Curatolo, Kenneth C. Waterman, Avinash G. Thombre, Michael B. Fergione, Michael C. Roy, Leah E. Appel, Danni Supplee, Dwayne T. Friesen, Mark B. Chidlaw, Ronald A. Beyerinck
  • Patent number: 6316504
    Abstract: The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing the same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, stroke, brain ischemia, a head trauma injury, a spinal trauma injury, neurotrauma, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject.
    Type: Grant
    Filed: November 16, 1998
    Date of Patent: November 13, 2001
    Assignees: Technion Research and Development Foundation, Ltd., Teva Pharmaceuticals Industries, Ltd.
    Inventors: Moussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Jeffrey Sterling, David Lerner, Haim Yellin, Alex Veinberg
  • Patent number: 6316469
    Abstract: Selective serotonin reuptake inhibitors useful in the treatment of non-cardiac chest pain or the treatment of symptoms of gastro-esophageal reflux disease.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: November 13, 2001
    Assignee: Duke University
    Inventors: Krishnaswamy Ranga Krishnan, Christopher O'Connor, Indira Varia
  • Patent number: 6281248
    Abstract: A method of treating asthma that includes the step of controlling the asthma by ingesting a composition which includes a selective serotonin reuptake inhibitor that is sertraline hydrochloride. Chronic administration of the sertraline thereof downregulates brain norepinephrine receptors. The increased output of the brain norepinephrine receptors increases the dilation of the bronchi. Sertraline has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors. Antagonism of such receptors has been hypothesized to be associated with various adverse anticholinergic, sedative, and cardiovascular effects.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: August 28, 2001
    Inventor: Magda Abdel Fattah Ahmed
  • Patent number: 6268361
    Abstract: The present invention is related to methods for treating pathological conditions resulting from an estrogen deficiency, such as cardiovascular disease and osteoporosis, and is further related to methods for treating estrogen-dependent cancer, such as breast and uterine cancer, employing compounds of formula I
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 31, 2001
    Inventor: Alan D. Palkowitz
  • Publication number: 20010005760
    Abstract: The naphthyloxyacetic acid derivatives of the formula (I) 1
    Type: Application
    Filed: January 22, 2001
    Publication date: June 28, 2001
    Inventors: Yuuki Nagao, Kazuhiko Torisu, Nobuyuki Hamanaka
  • Patent number: 6251943
    Abstract: The present invention provides a method for treating or preventing septic shock. Specifically, the present invention provides a method of treating or preventing septic shock by administering to a patient a MEK inhibitor.
    Type: Grant
    Filed: August 2, 1999
    Date of Patent: June 26, 2001
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
  • Patent number: 6245774
    Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D):  wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: June 12, 2001
    Assignee: Celltech Therapeutics Limited
    Inventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
  • Patent number: 6242497
    Abstract: 6,7-substituted 2-aminotetralines are used to treat inflammatory and/or autoimmune conditions induced by inflammatory cytokines.
    Type: Grant
    Filed: March 22, 2000
    Date of Patent: June 5, 2001
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p. A.
    Inventors: Piero Foresta, Vito Ruggiero
  • Patent number: 6225501
    Abstract: S(−)-amino-6-fluoro-7-methoxytetraline, a process for its preparation and pharmaceutical compositions containing same, active in preventing and treating septic shock, are disclosed.
    Type: Grant
    Filed: July 16, 1999
    Date of Patent: May 1, 2001
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Gian Piero Moretti, Piero Foresta
  • Patent number: 6201025
    Abstract: &bgr;-Aminotetralin derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a &bgr;-aminotetralin derivative as the active ingredient are described. The 62 -aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
    Type: Grant
    Filed: October 6, 1999
    Date of Patent: March 13, 2001
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Scott L. Dax, Timothy W. Lovenberg, Ellen W. Baxter, John R. Carson, Donald W. Ludovici, Mark A. Youngman
  • Patent number: 6191133
    Abstract: It has been found that the treatment of depression using known serotonin reuptake inhibitors (SRIs) and noradrenaline reuptake inhibitors (NRIs) may be improved by the administration therewith of folic acid or a precursor which produces folate in the patient. The daily dose of NRI or SRI is as prescribed for treatment of depression in the usual way. The daily dose of the folic acid or precursor should be such as to provide a folate dosage of 300-5000 micrograms/day.
    Type: Grant
    Filed: June 24, 1998
    Date of Patent: February 20, 2001
    Assignee: Scarista Limited
    Inventor: Alec James Coppen
  • Patent number: 6169111
    Abstract: Conformationally rigid aryl prostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic pharmaceutical compositions comprising said prostaglandins.
    Type: Grant
    Filed: May 12, 1999
    Date of Patent: January 2, 2001
    Assignee: Alcon Laboratories, Inc.
    Inventors: Paul W. Zinke, John E. Bishop, Thomas R. Dean, Mark R. Hellberg
  • Patent number: 6169116
    Abstract: Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined in the description, are useful as pharmaceuticals.
    Type: Grant
    Filed: June 28, 1999
    Date of Patent: January 2, 2001
    Assignee: Novartis AG
    Inventor: Robert Swoboda
  • Patent number: 6162815
    Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders are provided. In particular, based on their RXR-agonist activity, these compounds may be used to treat noninsulin-dependent diabetes mellitus (NIDDM) and obesity.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: December 19, 2000
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 6162805
    Abstract: The present invention relates to the use of an NK-1 receptor antagonist and a selective serotonin reuptake inhibitor for the treatment or prevention of obesity.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: December 19, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Franz Fridolin Hefti
  • Patent number: RE37087
    Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: March 6, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles