Aldimines Or Ketimines Which Contain A Benzene Ring (i.e., Rc=n Wherein R Is C Or H) Patents (Class 514/641)
  • Publication number: 20100278933
    Abstract: The invention relates to kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating disorders, especially cancer.
    Type: Application
    Filed: June 5, 2008
    Publication date: November 4, 2010
    Applicant: University of Florida Research Foundation, Inc
    Inventors: Peter P. Sayeski, György M. Keserü
  • Publication number: 20100280125
    Abstract: Medicine and pharmacology, in particular a medicinal agent exhibiting anti-tumoral and immunomodulatory actions and including a tri-p-amino-thiphenyl-chlormethan tetramethylated, pentamethylated or hexamethylated derivative, the mixtures thereof or the combination thereof with dextrin. The agent of this invention exhibits a high activity and a reduced side effect.
    Type: Application
    Filed: July 12, 2010
    Publication date: November 4, 2010
    Inventor: Mikhail Vladimirovich Kutushov
  • Patent number: 7754700
    Abstract: A composition for alleviating symptoms associated with neurotoxicity. The composition may comprise compounds for preventing glutamate mediated neurotoxicity. The composition may include one or more of the following elements: at least one glutamate antagonist, at least one cAMP stimulating agent, at least one antioxidant, vitamin B12, at least one transporter and at least one surfactant. The composition may be used in methods for alleviating tinnitus, Ménière's Disease and/or hearing loss.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: July 13, 2010
    Inventor: Seymour F. Trager
  • Patent number: 7732492
    Abstract: The present invention provides a small-sized preparation that is easy to take, containing 26% or more of nateglinide and 28% or more of at least one disintegrant selected from the group consisting of carmellose or salts thereof, sodium carboxymethyl starch, croscarmellose sodium, crospovidone, partly pregelatinized starch and low-substituted hydroxypropyl cellulose, based on the total mass of the preparation. The preparation of the present invention has high contents of nateglinide, which can be absorbed immediately to exhibit a hypoglycemic action.
    Type: Grant
    Filed: February 8, 2006
    Date of Patent: June 8, 2010
    Assignee: Ajinomoto Co., Inc.
    Inventors: Chisato Makino, Erika Motomura, Kunikazu Suzuki, Takahiko Andou, Nobutaka Ninomiya, Akira Yabuki
  • Patent number: 7718705
    Abstract: Methods for the prevention, treatment, or management of sexual dysfunction, such as premature ejaculation, by administering to a patient in need of therapy a therapeutically effective amount of a rapid-onset selective serotonin reuptake inhibitor on an as-needed basis shortly before sexual activity.
    Type: Grant
    Filed: August 22, 2000
    Date of Patent: May 18, 2010
    Assignee: Eli Lilly and Company
    Inventor: Karl Bruce Thor
  • Patent number: 7709533
    Abstract: The present invention provides a class of chemical compounds useful in the treatment of sickle cell disease, diseases characterized by unwanted or abnormal cell proliferation and for the treatment of ocular disorders such as glaucoma. The active compounds are tri-(aryl or heteroaryl) methane compounds or analogues thereof which further comprise an imine moiety and where the tertiary carbon atom can be replaced with a different atom such as Si, Ge, N or P. The compounds enhance resistance to degradation in a biological medium, inhibit potassium flux in a cell, reduce mammalian cell proliferation, reduce the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.
    Type: Grant
    Filed: February 1, 2006
    Date of Patent: May 4, 2010
    Assignee: Icagen, Inc.
    Inventors: Xiaodong Wang, Alan Bradley Fulp, Darrick Seconi
  • Publication number: 20100099742
    Abstract: The invention refers to the use of a cytokine antagonist which modulates the expression and/or the function of a cytokine, particularly a Th2 helper cell cytokine, in a cell and causes the down-regulation of anti-apoptotic proteins in said cell through the cytokine modulation for sensitizing cells for apoptosis. In particular, the cells that can be treated with the cytokine antagonists are drug-resistant cancer cells which fail to undergo apoptosis.
    Type: Application
    Filed: November 30, 2009
    Publication date: April 22, 2010
    Inventors: Giorgio Stassi, Matilde Todaro
  • Patent number: 7667077
    Abstract: A new class of fluorinated or polyhalogenated triazapentadienes are disclosed. The synthesized triazapentadienes are thermally stable, soluble in typical solvents and have several metal binding sites for complexation with metal ions. The compounds are prepared as colorless crystalline solids. Synthesis takes advantage of a reaction with triethylamine. Synthesized triazapentadienes (with and without complexed metals) inhibit bacterial growth of both Gram positive and Gram-negative bacteria.
    Type: Grant
    Filed: September 12, 2007
    Date of Patent: February 23, 2010
    Assignee: Board of Regents, The University of Texas
    Inventors: H. V. Rasika Dias, Lorraine G. Van Waasbergen, Jaime A. Flores
  • Publication number: 20100010084
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: July 15, 2009
    Publication date: January 14, 2010
    Inventor: Chongxi Yu
  • Publication number: 20090298905
    Abstract: This invention is related to new nitrogenated trans-stilbene analog compounds, more specifically, imine, pyrrol and Indole derivatives, with procedures for the preparation and use thereof as pharmaceutical compositions for the treatment and/or chemoprevention of those mammalian diseases such as cancer, fibrosclerosis and acute/chronic inflammation, graft-versus-host reaction, ischemic-reperfusion tissue injury in stroke and heart attack, neurodegeneration, and during organ transplantation, whose pathogenic and pathophysiological mechanisms depend on or are significantly contributed by undesirable oxidative stress, angiogenic and proliferative responses.
    Type: Application
    Filed: April 12, 2006
    Publication date: December 3, 2009
    Inventors: Fernando Pedro Cossio, Eneko Aldaba Arevalo, Yosu Ion Vara Salazar, Aizpea Zubia Olascoaga, Silvia Vivanco Amato, Miren Lorea Mendoza Arteche, Clarisa Salado Pogonza, Natalia Gallot Escobal, Fernando Vidal Vanaclocha
  • Publication number: 20090163545
    Abstract: A method for altering the lifespan of a eukaryotic organism. The method comprises the steps of providing a lifespan altering compound, and administering an effective amount of the compound to a eukaryotic organism, such that the lifespan of the organism is altered. In one embodiment, the compound is identified using the DeaD assay.
    Type: Application
    Filed: December 22, 2008
    Publication date: June 25, 2009
    Applicant: UNIVERSITY OF ROCHESTER
    Inventor: David Scott Goldfarb
  • Publication number: 20090137681
    Abstract: Provided herein are compositions and methods for treating or preventing cancer and autoimmune diseases. Compositions comprise a sirtuin inhibitory compound that decreases the activity of a sirtuin, such as SIRT1 or Sir2. Exemplary methods comprise contacting a cell or a molecule with a sirtuin inhibitory compound that decreases the activity of a sirtuin and thereby reduces the life span of a cell, kills the cell or renders it susceptible to certain cell stresses including radiation and chemotherapy. Other methods include treating pathogens expressing a sirtuin.
    Type: Application
    Filed: April 6, 2006
    Publication date: May 28, 2009
    Inventors: David A Sinclair, Antonello Mai
  • Publication number: 20090036462
    Abstract: Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of compound of formula I or a compound of formula IIa and at least about 50% by weight of at least one water soluble polymer selected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.
    Type: Application
    Filed: July 15, 2005
    Publication date: February 5, 2009
    Applicant: Onconova Therapeutics, Inc.
    Inventors: Stanley C. Bell, Albert Wong, Manoj Maniar
  • Publication number: 20080146674
    Abstract: A composition and method for treating a skin problem, particularly atopic dermatitis, the composition comprising an antiseptic dye, preferably gentian violet, in a vehicle effective for topical administration.
    Type: Application
    Filed: December 13, 2007
    Publication date: June 19, 2008
    Inventors: E. William Rosenberg, Robert B. Skinner
  • Publication number: 20080132568
    Abstract: Compounds having anti-androgenic activities are disclosed. Further disclosed are methods of using the compounds to prevent or treat androgen-dependent diseases or to provide nutraceutical benefits. Pharmaceutical and nutraceutical compositions containing the anti-androgenic compounds are also disclosed.
    Type: Application
    Filed: November 8, 2007
    Publication date: June 5, 2008
    Inventors: Todd A. Thompson, Debra A. MacKenzie
  • Patent number: 7354954
    Abstract: According to the subject invention, there is disclosed a method for treating a patient/subject having a spastic disorder, a convulsive disorder, pain or epilepsy which includes administering to the subject having any one of these conditions a therapeutically effective amount of the compound gamma-aminobutyramide, analogs, substituted forms, derivatives, the pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, or compounds which yield gamma-aminobutyramide as an intermediate, a metabolite, or a by-product.
    Type: Grant
    Filed: August 10, 2000
    Date of Patent: April 8, 2008
    Inventors: Jay M. Meythaler, Jean Peduzzi
  • Patent number: 7151196
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: December 19, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Robert R. Wilkening, Amy Fried
  • Patent number: 6914078
    Abstract: Disclosed are compounds having one of the following structures: wherein R and R? are hydrogen or substituted or unsubstituted C1 to C6 linear or branched alkyl, and at least one X is a halogen atom, pharmaceutical compositions containing the compounds as active ingredients, and methods for using the compounds in the photodynamic treatment of cancers.
    Type: Grant
    Filed: February 25, 2003
    Date of Patent: July 5, 2005
    Assignee: Wisconsin Alumni Research Foundation
    Inventor: Guilherme L. Indig
  • Patent number: 6878749
    Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide (1) stet or repaglinide and at least one other antidiabetic compound selected from the group consisting of thiazolidinedione derivatives (glitazones), sulfonyl urea derivatives and metformin for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of diseases, especially metabolic disorders and in particular type 2 diabetes and diseases and conditions associated with diabetes; to a composition, respectively, which comprises nateglinide and a pharmaceutically acceptable carrier and to a process of making such composition; the use of such combination or composition for the preparation of a medicament for the prevention, delay of progression or treatment of metabolic disorders; a method of prevention, delay of progression or treatment of diseases in warm-blooded animals; the use of such combination or composition for the cosme
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: April 12, 2005
    Assignee: Novartis AG
    Inventors: Marjorie Regan Gatlin, Michele Ann Ball, Richard Owen Mannion, Anees Abdulquadar Karnachi, Christiane Guitard, Malcolm Allison
  • Publication number: 20040175368
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: January 2, 2004
    Publication date: September 9, 2004
    Applicant: Wisconsin Alumni Research Foundation
    Inventor: Guilherme L. Indig
  • Publication number: 20040053890
    Abstract: The present invention relates to novel naphthalene derivatives of formula (I), wherein R1, R2, R3 and X are as defined in the description, and preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.
    Type: Application
    Filed: May 19, 2003
    Publication date: March 18, 2004
    Inventors: Christopher Thomas Brain, Andrew James Culshaw, Edward Karol Dziadulewicz, Ulrich Schopfer
  • Patent number: 6686345
    Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: February 3, 2004
    Assignee: Research Development Foundation
    Inventors: Sean Michael Kerwin, Wendi M. David
  • Patent number: 6656967
    Abstract: The invention provides fungicidal compounds of formula I and salts thereof: wherein the various radicals and substituents are as defined in the description, fungicidal compositions containing them and method for combating fungi which comprises applying these.
    Type: Grant
    Filed: August 6, 2001
    Date of Patent: December 2, 2003
    Assignee: Bayer Cropscience SA
    Inventors: Vincent Gerusz, Darren James Mansfield, Joseph Perez, Jean-Pierre Vors
  • Publication number: 20030199570
    Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1
    Type: Application
    Filed: January 10, 2003
    Publication date: October 23, 2003
    Inventors: Richard D. Coghlan, William F. Fobare, Heather A. Harris, James C. Keith, Leo M. Albert
  • Publication number: 20030187075
    Abstract: New antitumor compounds isolated from a sponge are of the a formulae (1), (2), (3) and (4).
    Type: Application
    Filed: January 31, 2003
    Publication date: October 2, 2003
    Inventors: Tanaka Keith Junichi, Higa Tatsuo
  • Patent number: 6596708
    Abstract: A composition for the treatment and prevention of endothelial dysfunction comprising a therapeutically effective amount of anti-inflammatory agents comprising; acetylsalicylic acid, an amino sugar and a zinc compound.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: July 22, 2003
    Assignee: Advanced Medical Instruments
    Inventor: Edward J. Petrus
  • Patent number: 6559188
    Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide (I) or repaglinide and at least one other antidiabetic compound selected from the group consisting of thiazolidinedione derivatives (glitazones), sulfonyl urea derivatives and metformin for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of diseases, especially metabolic disorders and in particular type 2 diabetes and diseases and conditions associated with diabetes; to a composition, respectively, which comprises nateglinide and a pharmaceutically acceptable carrier and to a process of making such composition; the use of such combination or composition for the preparation of a medicament for the prevention, delay of progression or treatment of metabolic disorders; a method of prevention, delay of progression or treatment of diseases in warm-blooded animals; the use of such combination or composition for
    Type: Grant
    Filed: September 15, 2000
    Date of Patent: May 6, 2003
    Assignee: Novartis AG
    Inventors: Marjorie Regan Gatlin, Michele Ann Ball, Richard Owen Mannion, Anees Abdulquadar Karnachi, Christiane Guitard, Malcolm Allison
  • Patent number: 6559185
    Abstract: The present invention relates to the compounds of formula: in which R1, R2, R3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: May 6, 2003
    Assignee: Merck Patent GmbH
    Inventors: Claude Lardy, Jaques Barbanton, Herve Dumas, Francois Collonges, Philippe Durbin
  • Patent number: 6541520
    Abstract: The present invention provides a highly efficient method for treating substance addiction and for changing addiction-related behavior of a mammal suffering from substance addiction. The method includes administering to a mammal an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof. The present invention also provides a method of treatment of cocaine, morphine, heroin, nicotine, amphetamine, methamphetamine, or ethanol addiction by treating a mammal with an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof. In one embodiment, the method of the present invention includes administering to the mammal an effective amount of a composition which increases central nervous system GABA levels wherein the effective amount is sufficient to diminish, inhibit or eliminate behavior associated with craving or use of drugs of abuse.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: April 1, 2003
    Assignee: Brookhaven Science Associates
    Inventors: Stephen L. Dewey, Jonathan D. Brodie, Charles R. Ashby, Jr.
  • Patent number: 6534546
    Abstract: Compounds represented by the general formula (1):   (where R1 is SR6 or NR7R8, where R6 is typically an alkyl group having 1-6 carbon atoms, R7 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2 and R3 are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3 and Y4 which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: March 18, 2003
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Toshio Honda, Toshihiko Makino, Toshiaki Nagafuji, Yasushi Kitoh, Nobuaki Kimura
  • Publication number: 20030027868
    Abstract: The invention concerns an aqueous solution capable of being injected by perinodular delivery or inhaled for use in the treatment of degenerative or autoimmune diseases or as immunomodulatory agent. Said solution is prepared by reacting camphor on ammonium hydroxide. The resulting product is then suspended in a saline solution. Said preparation having a basic pH is then neutralised with nitric acid. The resulting aqueous solution has pharmacological properties since it is an analogue of human cytokines, which makes it useful for treating degenerative or autoimmune diseases and/or as an immunomodulatory agent.
    Type: Application
    Filed: July 19, 2002
    Publication date: February 6, 2003
    Inventor: Gaston Naessens
  • Publication number: 20030013768
    Abstract: A pharmaceutical intermediate, N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine, which can be used in the production of sertraline hydrochloride, is conveniently prepared by reacting 4-(3,4-dichlorophenyl)-3,4-dihydro-1-(2H)-naphthalenone with monomethylamine in a solvent which is an amide solvent with a structure of general formula IV: 1
    Type: Application
    Filed: May 31, 2002
    Publication date: January 16, 2003
    Applicant: ORION COPRORATION FERMION
    Inventors: Ilpo Laitinen, Pekka Pietikaeinen
  • Publication number: 20020183281
    Abstract: Methods of making and using racemic and optically pure metabolites of sibutramine, and pharmaceutically acceptable salts, solvates, and clathrates thereof, are disclosed. Pharmaceutical compositions and dosage forms are also disclosed which comprise a dopamine reuptake inhibitor, such as a racemic or optically pure sibutramine metabolite, and optionally an additional pharmacologically active compound.
    Type: Application
    Filed: June 4, 2002
    Publication date: December 5, 2002
    Applicant: Sepracor Inc.
    Inventors: Chrisantha Hugh Senanayake, Qun Kevin Fang, Zhengxu Han, Dhileepkumar Krishnamurthy
  • Publication number: 20020132797
    Abstract: A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.
    Type: Application
    Filed: September 28, 2001
    Publication date: September 19, 2002
    Inventors: Sean Michael Kerwin, Wendi M. David
  • Patent number: 6399542
    Abstract: Alkoxyimino-substituted bicyclic derivatives or salts thereof having an excellent effect of controlling diseases and insect pests are disclosed.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: June 4, 2002
    Assignee: Agro-Kanesho Co., Ltd.
    Inventors: Shinya Henmi, Seiji Kakinuma, Satomi Katoh, Yuriko Shiihashi
  • Patent number: 6391869
    Abstract: Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O2−) scavengers, &bgr;-adrenergic agonists, cAMP-dependent protein kinase activators, &agr;1-adrenergic antagonists, L-type Ca2+ channel blockers, estrogens, ATP-sensitive K+ channel activators and smooth muscle relaxants are used.
    Type: Grant
    Filed: June 14, 2000
    Date of Patent: May 21, 2002
    Assignee: Cellergy Pharmaceuticals, Inc.
    Inventors: Thomas P. Parks, Vivien Mak, Jung-Chung Lee, Charles Lee
  • Patent number: 6258852
    Abstract: Disclosed are methods for treating or preventing inflammatory bowel disease (IBD) using aryl nitrone compounds. Pharmaceutical compositions containing aryl nitrone compounds which are useful for the treatment or prophylaxis of IBD are also disclosed.
    Type: Grant
    Filed: May 8, 2000
    Date of Patent: July 10, 2001
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: William D. Flitter, William A. Garland, Beverly Greenwood Van-Meerveld, Ian Irwin
  • Patent number: 6187808
    Abstract: This invention provides 6-amino-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one oximes and hydrazones which are useful in treating Parkinson's disease.
    Type: Grant
    Filed: September 27, 1999
    Date of Patent: February 13, 2001
    Assignee: Warner-Lambert Company
    Inventors: Stephen Joseph Johnson, Leonard Theodore Meltzer, Lawrence David Wise
  • Patent number: 6166032
    Abstract: A method for controlling tobacco use and alleviating withdrawal symptoms due to the cessation of tobacco use comprising administering to a human desiring to control tobacco use and/or suffering from withdrawal due to cessation of such use an effective amount of an acetylcholine esterase reactivator or prodrug derivative thereof optionally in association with an acetylcholine receptor antagonist.
    Type: Grant
    Filed: February 7, 1997
    Date of Patent: December 26, 2000
    Assignee: Synapse Pharmaceuticals International, Inc.
    Inventor: Norman Viner
  • Patent number: 6118017
    Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.
    Type: Grant
    Filed: April 8, 1999
    Date of Patent: September 12, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 6075044
    Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: June 13, 2000
    Assignee: The Regents of the University of California
    Inventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
  • Patent number: 6043286
    Abstract: Pesticidal as a pesticide against whitefly, Lepidoptera and certain fungi is provided of compound of general formula (I) ##STR1## or a salt thereof is provided, in which n represents an integer from 0 to 4; m represents an integer 0 or 1;each R independently represents a halogen atom or a nitro, cyano, hydroxyl, alkyl, alkenyl, haloalkyl, haloalkenyl, alkoxy, haloalkoxy, haloalkenoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, carboxyl, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, alkylamido, cycloalkyl, aryl or aralkyl group;R.sup.1 and R.sup.2 each independently represent an optionally substituted alkoxy group or together represent a group .dbd.O, .dbd.S or .dbd.N--OR.sup.9, where R.sup.9 represents a hydrogen atom or an optionally substituted alkyl group;R.sup.3 represents a hydroxyl group, or a group --OL where L is a leaving group, or a group which in vivo is transformed into a group --OL.sup.1 where L.sup.1 is a leaving group;R.sup.7 and R.sup.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: March 28, 2000
    Assignee: BTG International Limited
    Inventors: Bhupinder Pall Singh Khambay, Duncan Batty
  • Patent number: 6043281
    Abstract: The present invention relates to the compounds of formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: March 28, 2000
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Claude Lardy, Jaques Barbanton, Herve Dumas, Francois Collonges, Philippe Durbin
  • Patent number: 6020369
    Abstract: Respiratory viral infections may be effectively prevented or treated by administering an aerosol spray comprising a polyoxometalate to the lungs.
    Type: Grant
    Filed: July 7, 1998
    Date of Patent: February 1, 2000
    Inventors: Raymond F. Schinazi, Craig L. Hill
  • Patent number: 6020374
    Abstract: A pharmaceutical composition comprising, in admixture with a pharmaceutically acceptable carrier, a therapeutically effective amount of a polyaromatic ring-containing compound, capable of mimicking the physiological activity of insulin or insulin-like growth factor.
    Type: Grant
    Filed: May 14, 1998
    Date of Patent: February 1, 2000
    Assignee: Ramot University Authority for Applied Research & Industrial Development Ltd.
    Inventors: Avraham Geier, Hannah Kanety, Avraham Karasik
  • Patent number: 5990151
    Abstract: The present invention relates to an optically active, substituted phenylalkylamine derivative represented by Formula [1]: ##STR1## wherein A is a substituted or non-substituted phenyl or thienyl; X.sup.1 is hydrogen, halogen, hydroxyl or a substituted or non-substituted C.sub.1-5 alkoxy; R.sup.1 and R.sup.2 are equally or differently hydrogen, C.sub.1-7 alkyl, C.sub.3-7 alkenyl or C.sub.3-7 alkynyl; R.sup.3 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl or C.sub.2-10 alkynyl; n is an integer from 2 to 5; and m is an integer from 1 to 4,or a pharmaceutically acceptable salt thereof, and pharmaceutical use of such compound or salt. The compound of the invention is excellent in sigma 1 receptor antagonism and useful for treating schizophrenia, depression, anxiety, cerebrovascular diseases/senile troublesome behaviors, and cognitive dysfunctions and motor dysfunctions such as Alzheimer's disease, Parkinson's disease and Huntington's disease which are neurodegenerative diseases.
    Type: Grant
    Filed: May 15, 1998
    Date of Patent: November 23, 1999
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Atsuro Nakazato, Toshihito Kumagai, Tomoki Miyazawa, Koumei Ohta, Yutaka Kawashima, Katsuo Hatayama, deceased
  • Patent number: 5962463
    Abstract: Stimulating non-amyloidogenic processing by the activation of cell surface serotonin receptors linked to phospholipase and protein kinase C is described. Activation of the cell surface serotonin receptors is accomplished by contacting the cell with an agent which is a serotonin agonist or which increases the intrasynaptic concentration of serotonin. Also described is the activation of cell surface serotonin receptors by dexnorfenfluramine. Agents which cause the activation of cell surface serotonin receptors can be administered to an individual to stimulate non-amyloidogenic processing in the brain of the individual, thereby inhibiting the deposition of amyloid in the brain of the individual.
    Type: Grant
    Filed: January 27, 1997
    Date of Patent: October 5, 1999
    Assignee: Massachusetts Institute Of Technology
    Inventors: Roger M. Nitsch, Richard J. Wurtman
  • Patent number: 5939458
    Abstract: Mammalian hair growth is reduced by applying an inhibitor of aminoacyl-tRNA synthetase to the skin.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: August 17, 1999
    Inventors: James P. Henry, Gurpreet S. Ahluwalia
  • Patent number: RE37020
    Abstract: The present invention provides a method for providing nutrition to elderly patients. Pursuant to the present invention, the enteral composition includes a protein source, a lipid source, and a carbohydrate source. Preferably, the protein source includes at least 18% of the total calories. In an embodiment, the carbohydrate source includes a source of dietary fiber including a balance of soluble to insoluble fiber ratio of approximately 1:3. Still further, the composition of the present invention also includes increased levels of certain vitamins and minerals.
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: January 16, 2001
    Assignee: Nestec, Ltd.
    Inventors: Paul M. Lin, Shen-Youn Chang, Chris Kruzel
  • Patent number: RE36288
    Abstract: The present invention provides a method for providing nutrition to elderly patients. Pursuant to the present invention, the enteral composition includes a protein source, a lipid source, and a carbohydrate source. Preferably, the protein source includes at least 18% of the total calories. In an embodiment, the carbohydrate source includes a source of dietary fiber including a balance of soluble to insoluble fiber ratio of approximately 1:3. Still further, the composition of the present invention also includes increased levels of certain vitamins and minerals.
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: August 31, 1999
    Assignee: Nestec Ltd.
    Inventors: Paul M. Lin, Shen-Youn Chang, Chris Kruzel