Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/219)
  • Patent number: 7071186
    Abstract: The present invention is directed to methods of treating addictive behavior and sleep disorders by administering compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including addictive behavior and sleep disorders.
    Type: Grant
    Filed: February 26, 2004
    Date of Patent: July 4, 2006
    Assignee: Bristol-Myers Squibb Pharma Co.
    Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael G. Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emilie J. Calvello, David M. Zawrotny
  • Patent number: 7071185
    Abstract: Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
    Type: Grant
    Filed: April 24, 2003
    Date of Patent: July 4, 2006
    Assignee: Wyeth
    Inventors: P. Sivaramakrishnan Ramamoorthy, Robert E. McDevitt
  • Patent number: 7026311
    Abstract: The invention relates to compounds of the formula I and their tautomeric forms, possible enantiomeric and diastereomeric forms and their prodrugs, and to their preparation and use, where A, B, R1 and X1 have the meanings given in the description.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: April 11, 2006
    Assignee: Abbott GmbH & Co., KG
    Inventors: Wilfried Lubisch, Roland Grandel, Wilfried Braje, Thomas Subkowski, Reinhold Mueller, Wolfgang Wernet, Karla Drescher
  • Patent number: 7022697
    Abstract: The invention relates to compounds of the Formula I, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment or prevention of disorders linked to a dysfunction of the nicotinic receptors.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: April 4, 2006
    Assignee: Sanofi-aventis
    Inventors: Frédéric Galli, Odile Leclerc, Alistair Lochead
  • Patent number: 7015213
    Abstract: The invention concerns the use of pyrido-thieno-triazolo-diazepins for preparing a medicine for treating pathological conditions or diseases involving one of the growth hormone release inhibiting factor receptors. The invention also concerns novel pyrido-thieno-triazolo-diazepins and therapeutic compositions containing them.
    Type: Grant
    Filed: June 15, 1999
    Date of Patent: March 21, 2006
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Dennis Bigg, Anne-Marie Liberatore, Jacques Pommier, John Taylor
  • Patent number: 7001902
    Abstract: Compound corresponding to the general formula (I) in which R1, R2, R3, R4 and R5 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoroalkoxy, cyano, hydroxyl, (C1–C6)alkyl or (C1–C6)alkoxy group and R6 represents a (C1–C6)alkyl group. Therapeutic application.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: February 21, 2006
    Assignee: sanotl-aventis
    Inventors: Thierry Gallet, Frédéric Galli, Odile Leclerc, Alistair Lochead
  • Patent number: 6998399
    Abstract: The invention relates to compounds of the Formula I, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotinic receptors.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: February 14, 2006
    Assignee: sanofi-aventis
    Inventors: Frédéric Galli, Odile Leclerc, Alistair Lochead
  • Patent number: 6987106
    Abstract: Compounds of general formula in which X represents an oxygen atom or a group of formula NZ in which Z represents a hydrogen atom or an alkyl group, n represents a number 0, 1 or 2, and R1, R2, R3, R4 and R5 each represent a hydrogen or halogen atom or a trifluoromethyl, trifluoromethoxy, cyano, hydroxyl, alkyl, alkoxy, phenoxy or phenyl group optionally substituted with a halogen atom or a trifluoromethyl, cyano, hydroxyl, alkyl or alkoxy group, or alternatively R2 and R3 together form a group of formula —OCH2O— or —CH2CH2CH2CH2—. Application in therapy.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: January 17, 2006
    Assignee: Sanofi-Aventis
    Inventors: Thierry Gallet, Samir Jegham, Patrick Lardenois, Alistair Lochead, Alain Nedelec
  • Patent number: 6979682
    Abstract: A novel use of platelet-activating factor antagonists that bind to intracellular PAF binding sites such as BN-50730 (tetrahedra-4,7,8,10 methyl-1 (chloro-1 phenyl)-6 (methoxy-4 phenyl-carbamoyl)-9 pyrido [4?,3?-4,5] thieno [3,2-f] triazolo-1,2,4 [4,3-a] diazepine-1,4) has been discovered. These intracellular-binding platelet-activating factor antagonists were found to inhibit both in vivo and in vitro tumor growth and angiogenesis where the angiogenesis is stimulated by basic fibroblast growth factor.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: December 27, 2005
    Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: Jay D. Hunt, Haydee E. Bazan, Victor L. Marcheselli, Julio Alvarez Builla Gomez, Nicholas G. Bazan
  • Patent number: 6936604
    Abstract: The invention is directed to bridged bicyclic amino acid-derived [1,4]benzodiazepine compounds, intermediates and pharmaceutical compositions thereof useful as vasopressin receptor antagonists and methods for treating vasopressin mediated disorders.
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: August 30, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Alexey B. Dyatkin, William J. Hoekstra, Bruce E. Maryanoff
  • Patent number: 6927238
    Abstract: Novel inhibitors of polyisoprenyl phosphate signaling regulates phopholipase D activity.
    Type: Grant
    Filed: October 19, 2001
    Date of Patent: August 9, 2005
    Assignee: The Brigham & Women's Hospital, Inc.
    Inventor: Charles N. Serhan
  • Patent number: 6864288
    Abstract: Novel inhibitors of polyisoprenyl phosphate signaling regulates phopholipase D activity.
    Type: Grant
    Filed: October 19, 2001
    Date of Patent: March 8, 2005
    Assignee: Brigham & Women's Hospital, Inc.
    Inventor: Charles N. Serhan
  • Patent number: 6864251
    Abstract: Compounds according to formula I: wherein R1, R2, R3, R4, R5 and n are as defined herein, are administered for the treatment of inflammatory disorders mediated by LTB4.
    Type: Grant
    Filed: December 3, 2002
    Date of Patent: March 8, 2005
    Assignee: Vela Pharmaceuticals, Inc.
    Inventors: Robert F. Kucharik, Herbert W. Harris
  • Patent number: 6858604
    Abstract: This invention provides compounds of the formula: wherein R1 and R2 are each, independently, H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or phenoyl or thiophenoyl; R3 and R4 are each, independently, H, alkyl or cycloalkyl; R5 is H or alkyl; R6 is H or; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions and methods utilizing these compounds for the treatment or prevention of disorders including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: February 22, 2005
    Assignee: Wyeth
    Inventors: Annmarie Louise Sabb, Robert Lewis Vogel
  • Publication number: 20040248877
    Abstract: Compounds of Formula 8 are provided: 1
    Type: Application
    Filed: April 30, 2004
    Publication date: December 9, 2004
    Inventors: Sandeep Gupta, David Michael Carrig, Raghavan Rajagopalan, Prabhavathi Fernandes
  • Publication number: 20040229865
    Abstract: This invention provides compounds of formula I having the structure 1
    Type: Application
    Filed: June 18, 2004
    Publication date: November 18, 2004
    Applicant: Wyeth
    Inventors: Annmarie Louise Sabb, Robert Lewis Vogel
  • Publication number: 20040186094
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) 1
    Type: Application
    Filed: February 20, 2004
    Publication date: September 23, 2004
    Inventors: Albert J. Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
  • Patent number: 6784172
    Abstract: This invention provides processes for synthesizing compounds of formula I: wherein R is H or alkyl; R1, R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, alkyl sulfonamide, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or aroyl; R3 and R4 are H, alkyl or cycloalkyl; the dashed line indicates an optional double bond; as well as intermediates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: August 31, 2004
    Assignee: Wyeth
    Inventors: Annmarie Louise Sabb, Robert Lewis Vogel, Madelene Miyoko Antane, Panolil Raveendranath, Sreenivasulu Megati, Michael David Smith, James Albert Nelson
  • Patent number: 6784194
    Abstract: A method of inhibiting effects of exogenous neurotoxic or neurotoxinic products in warm-blooded animals comprising administering to warm-blooded animals before exposure to said products an inhibitorily effective amount of reversible cholinesterase inhibitor selected from the group consisting of pyridostigmine and physostigmine followed by administration of an inhibitorily effective amount of 2-methyl-1-(1-piperidinyl)-1-(2-thienyl)-cyclohexane in substantially pure racemic, diastereoisomeric or enantiomeric form.
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: August 31, 2004
    Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Guy Lallement, Pierre D'Arbigny, Jean-Marc Kamenka
  • Patent number: 6777407
    Abstract: This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceut
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: August 17, 2004
    Assignee: Wyeth
    Inventors: Annmarie Louise Sabb, Robert Lewis Vogel, James Albert Nelson, Sharon Joy Rosenzweig-Lipson, Gregory Scott Welmaker, Joan Eileen Sabalski
  • Publication number: 20040157831
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: February 3, 2004
    Publication date: August 12, 2004
    Applicant: Pharmacia & Upjohn Company
    Inventor: William W. McWhorter
  • Publication number: 20040157832
    Abstract: Fluorenecarboxylic acid esters of general formula 1 1
    Type: Application
    Filed: February 5, 2004
    Publication date: August 12, 2004
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhauser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Publication number: 20040132723
    Abstract: Compounds represented by formula 1: 1
    Type: Application
    Filed: September 15, 2003
    Publication date: July 8, 2004
    Applicant: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Christiane Yoakim, Jeffrey O'Meara, Bruno Simoneau, William Ogilvie, Robert Deziel
  • Patent number: 6759405
    Abstract: This invention provides compounds of formula I having the structure wherein: R1 and R2 are H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated, acyl, or aroyl; R3, R4 are H, alkyl, cycloalkyl or —CH2-cycloalkyl; R5 is H or alkyl; R6 is H or alkyl; and wherein the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods for using these compounds to treat central nervous system disorders, including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: July 6, 2004
    Assignee: Wyeth
    Inventors: Annmarie Louise Sabb, Robert Lewis Vogel
  • Publication number: 20040116409
    Abstract: Methods for the treatment of a subject suffering from ERM formation or retinal detachment due to ERM formation comprising administering to a subject suffering from ERM formation or retinal detachment due to ERM formation an effective amount of a staurosporine derivative to treat ERM formation or retinal detachment in the eye of the subject, or a salt thereof, are provided.
    Type: Application
    Filed: November 6, 2003
    Publication date: June 17, 2004
    Inventor: Peter A. Campochiaro
  • Patent number: 6743789
    Abstract: The present invention is a compound of formula The compound and derivatives or pharmaceutically acceptable salts thereof of the invention have a good affinity and selectivity to the GABA A &agr;5 receptor and are useful for the treatment of diseases related to this receptor.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: June 1, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Raffaello Masciadri, Andrew William Thomas, Juergen Wichmann
  • Patent number: 6743785
    Abstract: The present invention provides selective kinase inhibitors of formula (I).
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: June 1, 2004
    Assignee: Eli Lilly and Company
    Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, Jianping Huang, Sajan Joseph, James Edward Ray, Philip Parker Waid
  • Publication number: 20040092502
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) 1
    Type: Application
    Filed: December 19, 2001
    Publication date: May 13, 2004
    Inventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
  • Patent number: 6720354
    Abstract: Aspirin (ASA) triggers a switch in the biosynthesis of lipid mediators, inhibiting prostanoid production and initiating 15-epi-lipoxin generation, through the acetylation of cyclooxygenase II.
    Type: Grant
    Filed: June 20, 2002
    Date of Patent: April 13, 2004
    Assignee: The Brigham and Women's Hospital
    Inventor: Charles N. Serhan
  • Patent number: 6699492
    Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.
    Type: Grant
    Filed: April 22, 2002
    Date of Patent: March 2, 2004
    Assignees: InSite Vision Incorporated, SSP Co., Ltd.
    Inventors: Samir Roy, Santosh Kumar Chandrasekaran, Katsumi Imamori, Takemitsu Asaoka, Akihiro Shibata, Masami Takahashi, Lyle M. Bowman
  • Patent number: 6699849
    Abstract: Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: March 2, 2004
    Assignee: Cyclops, ehf.
    Inventors: Thorsteinn Loftsson, Mar Masson, Einar Stefansson
  • Publication number: 20040034015
    Abstract: The present invention is directed to methods of treating addictive behavior and sleep disorders by administering compounds represented by structural Formula (I) 1
    Type: Application
    Filed: February 20, 2003
    Publication date: February 19, 2004
    Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. MC Clung, Emilie J.B. Calvello, David M. Zawrotny
  • Patent number: 6685958
    Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: February 3, 2004
    Assignees: InSite Vision Incorporated, SSP Co., Ltd.
    Inventors: Samir Roy, Santosh Kumar Chandrasekaran, Katsumi Imamori, Takemitsu Asaoka, Akihiro Shibata, Masami Takahashi, Lyle M. Bowman
  • Publication number: 20030229078
    Abstract: A new method to synthesize the platelet-activating factor antagonist which is a derivative of thienotriazolodiazepene, tetrahydro-4,7,8,10 methyl-1(chloro-2 phenyl)-6 (methosy-4 phenyl carbamoyl)-9 pyrido[4,3-:4,5] thieno[3,2-f] triazolo-1,2,4 [4,3-&agr;] diazepine-1,4] (1) is disclosed. The compound synethesized by this new method has been designated “LAU-8080” which has the same structure as the compound currently named in the literature as “BN-50730.” LAU-8080 was shown to prevent photoreceptor cell death, inhibit pathological neovascularization in the retina, and minimize the loss of neurons due to ischemic-reperfusion damage due to stroke. Thus LAU-8080 can be used to treat the retinal diseases of age-related macular degeneration, retinitis pigmentosa, and diabetic retinopathy. It can also be used to minimize the neuronal damage due to stroke.
    Type: Application
    Filed: March 10, 2003
    Publication date: December 11, 2003
    Inventors: Nicholas G Bazan, Julio Alvarez Builla Gomez
  • Patent number: 6649607
    Abstract: The present invention relates to compositions comprising S-tofisopam substantially free of R-tofisopam, and methods for treating or preventing convulsions and/or seizures comprising administration of the composition to subjects in need of treatment therefor. Also provided are compositions and methods for treating or preventing convulsions and/or seizures comprising administering S-tofisopam substantially free of R-tofisopam with another anti-convulsant.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: November 18, 2003
    Assignee: Vela Pharmaceuticals, Inc.
    Inventors: Steven M. Leventer, Robert Kucharik
  • Publication number: 20030191109
    Abstract: There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, the &bgr;-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The &bgr;-sheet mimetics have utility as inhibitors of one or more of proteases, kinases, CAAX, peptides binding to SH2 domains and MHC-I and/or MHC-II presentation of peptides to T cell receptors in warm-blooded animals.
    Type: Application
    Filed: October 25, 2001
    Publication date: October 9, 2003
    Inventor: Michael Kahn
  • Patent number: 6630461
    Abstract: A method for treating neurodegenerative diseases in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula wherein A selected from the group consisting of hydrogen and wherein the substituents are defined as set forth in the specification.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: October 7, 2003
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Publication number: 20030176420
    Abstract: Retinoids with retinoid receptor antagonistic activity, pharmaceutically acceptable salts and pharmaceutically acceptable hydrolyzable esters thereof, have been found efficacious in treating T-helper cell type 2 (Th2)-mediated immune diseases, such as immunoglobulin E (IgE)-mediated allergic diseases.
    Type: Application
    Filed: January 29, 2003
    Publication date: September 18, 2003
    Inventors: Werner Bollag, Michael Klaus, Paola Panina-Bordignon, Francesco Sinigaglia
  • Patent number: 6617321
    Abstract: The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation or olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.
    Type: Grant
    Filed: May 1, 2002
    Date of Patent: September 9, 2003
    Assignee: Eli Lilly and Company
    Inventors: Douglas J. Allen, Kurt D. Dekemper, Thomas H. Ferguson, Stuart J. Garvin, Linda C. Murray, Norman D. Brooks, Charles A. Bunnell, Snehlata S. Mascarenhas, Sharon L. Shinkle, Barry A. Hendriksen, David E. Tupper, Manuel V. Sanchez-Felix
  • Patent number: 6610271
    Abstract: A therapeutic composition of lorazepam and its pharmaceutically acceptable derivatives are provided for intranasal administration of at least one predetermined volumetric unit dose in the form of a spray by means that delivers one or more therapeutically prescribed unit doses that are highly accurate as to the volume discharged and which leave no significant quantity of the composition in the delivery means.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: August 26, 2003
    Assignee: University of Kentucky Research Foundation
    Inventor: Daniel P. Wermeling
  • Publication number: 20030144268
    Abstract: The invention relates to novel tetracyclic pyrroloquinolone derivatives of the formula (I) or (II): 1
    Type: Application
    Filed: November 12, 2002
    Publication date: July 31, 2003
    Inventors: Weiqin Jiang, Zhihua Sui
  • Publication number: 20030139394
    Abstract: The invention relates to compounds of the formula I 1
    Type: Application
    Filed: January 10, 2002
    Publication date: July 24, 2003
    Inventors: Wilfried Lubisch, Roland Grandel, Wilfried Braje, Thomas Subkowski, Reinhold Mueller, Wolfgang Wernet, Karla Drescher
  • Patent number: 6569851
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: May 27, 2003
    Assignees: Elan Pharmaceutials, Inc., Eli Lilly & Company
    Inventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. VanMeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Patent number: 6562806
    Abstract: A compound with formula (I) where R10 is a therapeutically removable nitrogen protecting group; R2 and R3 are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R, CH2—CO2H, CH2—SO2R, O—SO2—R, CO2R, COR and CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, nitro, Me3Sn; X is S, O or NH; R11 is either H or R; and where there is optionally a double bond between C1 and C2 or C2 and C3; and R8 is selected from H, R, OH, OR, halo, amino, nitro, Me3Sn, or R7 and R8 together form a group —O—(CH2)p—O—, where p is 1 or 2. Such compounds may be used in methods of ADEPT, GDEPT, NPEPT or PDT.
    Type: Grant
    Filed: February 26, 2001
    Date of Patent: May 13, 2003
    Assignee: Spirogen Limited
    Inventors: David Edwin Thurston, Philip Wilson Howard
  • Patent number: 6552017
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: April 22, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. Mc Clung, Emilie J. B. Calvello, David M. Zawrotny
  • Publication number: 20030064979
    Abstract: This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al, Proc Natl Acad Sci USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1 1
    Type: Application
    Filed: June 27, 2002
    Publication date: April 3, 2003
    Inventors: Thomas Kruse Hansen, Ole Hvilsted Olsen, Anders Klarskov Petersen, Jesper Lau, Henrik Sune Andersen, Niels Peter Hundahl Moller
  • Patent number: 6541468
    Abstract: Novel indolocarbazole derivatives potentially useful for the treatment of dementias characterized by tau hyperphosphorylation [Alzheimer's disease (AD), frontal lobe degeneration (FLD), argyrophilic grains disease, subacute sclerotising panencephalitis (SSPE) as a late complication of viral infections in the CNS], and cancer.
    Type: Grant
    Filed: August 25, 1999
    Date of Patent: April 1, 2003
    Assignee: Bayer Corporation
    Inventors: Hanno Roder, Timothy B. Lowinger, David R. Brittelli, Michael C. VanZandt
  • Publication number: 20030060462
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: August 3, 2002
    Publication date: March 27, 2003
    Inventors: Robert L. Hoffman, Michael D. Ennis
  • Publication number: 20030050300
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: August 2, 2002
    Publication date: March 13, 2003
    Inventor: William W. McWhorter
  • Patent number: 6521266
    Abstract: A method for enhancing growth hormone production and release, for appetite suppression, or both, in a subject in need thereof. The method comprises administering to the subject an effective amount of a first composition, wherein the first composition increases cholinergic tone and growth hormone synthesis, and the second composition inhibits somatostatin. The first composition may be a combination of an acetylcholinesterase inhibitor and Vitamin E D-&agr;-succinate, whereas the second composition may be a salt of cysteamine and an alkali buffer, or may be pantothenic acid and an alkali metal salt. A two-part composition comprising the first and second compositions as also disclosed.
    Type: Grant
    Filed: September 23, 2000
    Date of Patent: February 18, 2003
    Inventor: Morris A. Mann