The Hetero Ring Is Six-membered Patents (Class 514/451)
  • Patent number: 11890263
    Abstract: Provided are compositions suitable for treating acne, disrupting a biofilm, and/or killing bacteria contained in a biofilm. Certain compositions comprise a. about 0.1 wt. % to about 7.5 wt. % glycolic acid; b. about 0.1 wt. % to about 5 wt. % gluconolactone; c. about 0.1 wt. % to about 5 wt. % mandelic acid d. a glycol; e. a salt-tolerant thickening polymer, wherein the total amount of glycolic acid, gluconolactone and mandelic acid is less than about 15 wt. % of the total composition.
    Type: Grant
    Filed: August 12, 2021
    Date of Patent: February 6, 2024
    Assignee: Johnson & Johnson Consumer Inc.
    Inventors: Aliaksandr Zhuk, Anthony Geonnotti, Dara Miller, Jennifer Li
  • Patent number: 11400156
    Abstract: A method of treating or preventing a disease associated with a secondary infection in a subject infected with a pathogen is provided. The method comprises administering to the subject a therapeutically effective amount of an anti-pathogenic agent directed towards the pathogen and a therapeutically effective amount of an agent which down-regulates at least one extracellular matrix-associated polypeptide.
    Type: Grant
    Filed: March 26, 2020
    Date of Patent: August 2, 2022
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Irit Sagi, Dalit Talmi-Frank, Inna Solomonov, Ido Amit
  • Patent number: 11325893
    Abstract: A compound is represented by the following general formula (I): (I) wherein each of Rf1 and Rf2 is, independently, F, CF3, C2F5, C3F7, or C4F9, with the proviso that if either of Rf1 and Rf2 is fluorine, then the other is not fluorine; Rf3 is F, CF3, C2F5, C3F7 or CF(CF3)2; Rf4 is F, CF3, C2F5, C3F7 or CF(CF3)2; and Rh is CH3 or C2H5.
    Type: Grant
    Filed: September 23, 2019
    Date of Patent: May 10, 2022
    Assignee: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Michael J. Bulinski, William M. Lamanna, Forrest A. Coughlin, Hui Ren, Nicholas A. Toso
  • Patent number: 11045447
    Abstract: A method for treating Alzheimer's disease (AD) by administering to an AD patient a PKC activator, such as a bryostatin-1, without administering a NMDA receptor antagonist, such as memantine.
    Type: Grant
    Filed: June 28, 2020
    Date of Patent: June 29, 2021
    Assignee: Synaptogenix, Inc.
    Inventor: Daniel L. Alkon
  • Patent number: 11007274
    Abstract: The present invention provides compounds for use in treating and/or preventing influenza. The compound comprises a first and second domain in which the first domain comprises at least one anchoring group which binds to the surface of influenza viruses and the second domain comprises at least one anionic group. The first and second domains are covalently linked. Also provided are pharmaceutically acceptable salts, solvates, prodrugs or stereoisomer of the compounds.
    Type: Grant
    Filed: May 18, 2018
    Date of Patent: May 18, 2021
    Assignee: Ausvir Therapeutics Pty LTD
    Inventors: Betty Jin, Ee-Ling Seah, Paul Arthur Jones, Peter James Jenkins, Henry Kenneth Windle, Wen Yang Wu
  • Patent number: 10493042
    Abstract: Provided are a pharmaceutical composition including geraniol or a pharmaceutically acceptable salt thereof as an active ingredient for use in preventing or treating diabetes mellitus, a method of preventing or treating diabetes mellitus or a complication due to diabetes mellitus of an individual, in which the method includes administering the individual with a pharmaceutical composition comprising geraniol or a pharmaceutically acceptable salt thereof as an active ingredient and inducing an olfactory stimulation to the individual using the pharmaceutical composition, and a screening method of an antidiabetic agent that may include contacting a cell expressing an olfactory receptor with a test material; measuring a level of expression of glucagon-like peptide-1 (GLP-1) secreted from the cell; and determining the test material, when the test material promotes expression of GLP-1, as a candidate material of an antidiabetic agent.
    Type: Grant
    Filed: August 1, 2014
    Date of Patent: December 3, 2019
    Assignee: UNIVERSITY-INDUSTRY COOPERATION GROUP OF KYUNG HEE UNIVERSITY
    Inventor: Hyeung Jin Jang
  • Patent number: 10494388
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: December 3, 2019
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Patent number: 10213375
    Abstract: The invention concerns topical compositions based on retinaldehyde, glycylglycine oleamide and, if necessary, delta-tocopheryl-glucopyranoside, and their use in cosmetology and dermatology to combat skin ageing and more particularly light-induced skin ageing.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: February 26, 2019
    Assignee: PIERRE FABRE DERMO-COSMETIQUE
    Inventors: Daniel Bacqueville, Patrick Bogdanowicz, Jean-Hilaire Saurat, Olivier Sorg
  • Patent number: 9724328
    Abstract: Treating subjects having a lipid storage disorder with a composition comprising a PKC activator, such as bryostatins, bryologs, and polyunsaturated fatty acids.
    Type: Grant
    Filed: April 14, 2015
    Date of Patent: August 8, 2017
    Assignees: Icahn School of Medicine at Mount Sinai, Neurotrope Bioscience
    Inventors: Yiannis A. Ioannou, Lawrence Altstiel, David R. Crockford, Sathapana Kongsamut
  • Patent number: 9592221
    Abstract: The invention provides compounds of formula Ia, Ib and Ic: and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula Ia-Ic, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.
    Type: Grant
    Filed: March 8, 2016
    Date of Patent: March 14, 2017
    Assignees: Rutgers, The State University of New Jersey, Provid Pharmaceuticals Inc.
    Inventors: Richard H. Ebright, Yon W. Ebright, Juan Shen, James Bacci, Anne-Cecile Hiebel, William Solvibile, Christopher Self, Gary Olson
  • Patent number: 9193715
    Abstract: The invention provides novel compounds of Formulas (I)-(IV), as described herein. Also provided are compositions of these compounds, method of making the compounds, and methods of using the compounds. The compounds can be used to regulate cholesterol homeostasis and to treat conditions and diseases associated with cholesterol homeostasis, including lysosomal lipid storage disorders such as Niemann-Pick Disease type C.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: November 24, 2015
    Assignee: University of Notre Dam du Lac
    Inventor: Richard Taylor
  • Patent number: 9066923
    Abstract: The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate ?-secretase activity; improve or enhance cognitive ability; and/or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: June 30, 2015
    Assignee: Blanchette Rockefeller Neurosciences Institute
    Inventor: Daniel Alkon
  • Publication number: 20150148408
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: February 2, 2015
    Publication date: May 28, 2015
    Inventors: Mohamed Naquib Attala, Philippe Diaz
  • Patent number: 9034921
    Abstract: A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: May 19, 2015
    Assignee: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon Kim, Dong Ho Hong, Misuk Kang
  • Publication number: 20150126549
    Abstract: The present invention relates to the general field of the treatment and prevention of diseases involving an inflammatory condition, namely sepsis or infectious or viral diseases as well as diseases requiring for the of treatment an immunosuppressive activity namely autoimmune diseases and graft rejection. In particular, the invention relates to an inhibitor of the activity or the formation of the PP1/GADD34 complex for the treatment of a condition requiring an immunosuppressive activity or an anti-inflammatory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 7, 2015
    Applicants: INSERM (Institut National de la Sante et de la Recherche Medicale), Universite d'Aix-Marseille
    Inventor: Philippe Pierre
  • Patent number: 8993618
    Abstract: New pharmaceutical compositions extracted from Ferula assa-foetida are confirmed to effectively treat influenza A (H1N1) virus. The extraction method of the new pharmaceutical compositions mainly includes steps of: (a) extracting F. assa-foetida with methanol to obtain a crude extract; (b) fractioning the crude extract with n-hexane-methanol to obtain a methanol extract; (c) fractioning the methanol extract with chloroform-water to obtain a chloroform extract; and (d) chromatographing the chloroform extract to obtain the pharmaceutical compositions, which can be further fractioned and chromatographed to obtain various sesquiterpene coumarins.
    Type: Grant
    Filed: July 21, 2014
    Date of Patent: March 31, 2015
    Assignee: Kaohsiung Medical University
    Inventors: Yang-Chang Wu, Fang-Rong Chang, Lien-Chai Chiang
  • Patent number: 8986683
    Abstract: The invention discloses a kit which comprises a formulation containing artemisinin or the derivatives thereof, a formulation containing ribonuclease, and a specification.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: March 24, 2015
    Assignees: Shanghai Biomodel Organism Science & Technology Co., Ltd., Shanghai Research Center for Model Organisms
    Inventors: Qingcheng Wang, Ruling Shen, Jun Li, Jian Fei, Zhugang Wang
  • Patent number: 8987323
    Abstract: Provided are crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2. The invention also provides pharmaceutical compositions, methods of preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition.
    Type: Grant
    Filed: June 13, 2011
    Date of Patent: March 24, 2015
    Assignee: Theracos, Inc.
    Inventors: Mengzhuang Cai, Qian Liu, Ge Xu, Binhua Lv, Brian Seed, Jacques Y. Roberge
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Patent number: 8962679
    Abstract: Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: February 24, 2015
    Assignees: The Administrators of the Tulane Educational Fund, Xavier University of Louisiana
    Inventors: Guangdi Wang, Matthew E. Burow, Stephen M. Boue, Thomas E. Wiese, Quan Jiang
  • Publication number: 20150038566
    Abstract: The invention provides novel compounds of Formulas (I)-(IV), as described herein. Also provided are compositions of these compounds, method of making the compounds, and methods of using the compounds. The compounds can be used to regulate cholesterol homeostasis and to treat conditions and diseases associated with cholesterol homeostasis, including lysosomal lipid storage disorders such as Niemann-Pick Disease type C.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventor: Richard Taylor
  • Patent number: 8940301
    Abstract: The present invention provides methods of treating cancer by administering an IL8-CXCR1 pathway inhibitor (e.g., an anti-CXCR1 antibody or Repertaxin) alone or in combination with an additional chemotherapeutic agent such that non-tumorigenic and tumorigenic cancer cells in a subject are killed. The present invention also provides compositions and methods for detecting the presence of and isolating solid tumor stem cells in a patient (e.g., based on the presence of CXCR1 or FBXO21).
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: January 27, 2015
    Assignee: The Regents of The University of Michigan
    Inventors: Max S. Wicha, Christophe Ginestier
  • Publication number: 20150025054
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: January 22, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
  • Patent number: 8937097
    Abstract: Methods for making trans-(?)-?9-tetrahydrocannabinol and trans-(+)-?9-tetrahydrocannabinol are disclosed herein. In one embodiment, a trans-(?)-?9-tetrahydrocannabinol composition is prepared by allowing a composition comprising (±)-?9)-tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(?)-?9-tetrahydrocannabinol composition comprising at least about 99% by weight of trans-(?)-?9-tetrahydrocannabinol based on the total amount of trans-(?)-?9-tetrahydrocannabinol and trans-(+)-?9-tetrahydrocannabinol. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of a trans-(?)-?9-tetrahydrocannabinol having a purity of at least about 98% based on the total weight of cannabinoids.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: January 20, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Arie L. Gutman, Marina Etinger, Irina Fedotev, Ram Khanolkar, Gennady A. Nisnevich, Boris Pertsikov, Igor Rukhman, Boris Tishin
  • Patent number: 8933116
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: January 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
  • Patent number: 8927597
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: January 6, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Publication number: 20150005319
    Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 1, 2015
    Inventors: Michael Taylor, Nicholas K. Terrett, William H. Connors, Cheri Snedeker, Kelley C. Shortsleeves, Benjamin A. Seigal, Stephen P. Hale, Timothy F. Briggs, Frank G. Favaloro, Jr., Tyler J. Cipriani, Dingxue Yan, Sethu L. Alexander, Atli Thorarensen, Li Xing
  • Publication number: 20140357707
    Abstract: Provided are an insect pest-targeting gel composition causing neither leakage nor reaction of a volatile substance and capable of releasing the volatile substance at a constant rate; and a sustained release preparation including the insect pest-targeting gel composition. More specifically, provided is an insect pest-targeting gel composition including one or more volatile substances and an oil gelling agent, wherein the volatile substance is included in an amount of from 70.0 to 99.0% by weight by the insect pest-targeting gel composition.
    Type: Application
    Filed: December 6, 2012
    Publication date: December 4, 2014
    Inventors: Naoki Ishibashi, Ryuichi Saguchi, Tatsuya Hojo, Takehiko Fukumoto
  • Patent number: 8877715
    Abstract: There is provided a series of novel neuropeptide Y-cytotoxic conjugates, compositions comprising the same, and methods relating to their therapeutic use for the treatment of disease or condition states associated with aberrant or undesirable proliferation of cells that express NPY-Y1 receptors.
    Type: Grant
    Filed: August 18, 2011
    Date of Patent: November 4, 2014
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Zheng Xin Dong, Kevin Zhou, Daniel B. Deoliveira
  • Publication number: 20140315894
    Abstract: The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same.
    Type: Application
    Filed: December 21, 2012
    Publication date: October 23, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE
    Inventors: Dan Theodorescu, Michael Fitzpatrick Wempe, David Ross, Samy Meroueh, Martin A. Schwartz, Phillip Reigan
  • Patent number: 8865761
    Abstract: The invention provides novel compounds of Formulas (I)-(IV), as described herein. Also provided are compositions of these compounds, method of making the compounds, and methods of using the compounds. The compounds can be used to regulate cholesterol homeostasis and to treat conditions and diseases associated with cholesterol homeostasis, including lysosomal lipid storage disorders such as Niemann-Pick Disease type C.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: October 21, 2014
    Assignee: The University of Notre Dame du Lac
    Inventor: Richard Taylor
  • Patent number: 8858991
    Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: October 14, 2014
    Assignee: Pathologica LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 8841264
    Abstract: Compositions containing a combination of hydroxytyrosol and resveratrol or liqustilide or (?)-epigallocatechin gallate or honokiol or genistein or Magnolia bark extract or a combination of oleuropein and resveratrol or ligustilide are used to treat inflammatory disorders.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: September 23, 2014
    Assignee: DSM IP Assets B.V.
    Inventors: Daniel Raederstorff, Nathalie Richard, Joseph Schwager, Karin Wertz
  • Patent number: 8841290
    Abstract: Disclosed is a tetrahydronapthalene compound having Formula I the variables of which are as described herein, methods of preparing same and their use.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: September 23, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
  • Patent number: 8829034
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: September 9, 2014
    Assignee: Boehringer Ingerlheim International GmbH
    Inventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Parke, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
  • Patent number: 8815941
    Abstract: Compounds of structural formula (I) useful for the treatment or prophylaxis of viral infection, particularly viral influenza are provided Pharmaceutical preparations thereof and methods for their preparation are also described. The therapeutic effect is achieved via inhibition of viral neuraminidases, also known as viral sialidases. These neuraminidases are classified under the GH34 family of viral enzymes.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: August 26, 2014
    Assignee: The University of British Columbia
    Inventors: Stephen Withers, Andrew Graham Watts, Jin Hyo Kim, Tom Wennekes
  • Publication number: 20140221330
    Abstract: An objective of the present invention is to provide a novel NDM (New Delhi metallo-?-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of ?-lactam antibiotics that have been inactivated as a result of decomposition by NDM.
    Type: Application
    Filed: July 26, 2012
    Publication date: August 7, 2014
    Inventors: Akihiro Morinaka, Kazunori Maebashi, Takashi Ida, Muneo Hikida, Mototsugu Yamada, Takao Abe
  • Patent number: 8796327
    Abstract: A method for inhibiting the production of cytokines of T helper cell type II (Th2 cell) and/or inhibiting the production of chemokines in a mammal is provided, wherein the method comprises administrating to the mammal an effective amount of an active component selected from a group consisting of a compound of formula (I), pharmaceutically acceptable salts and esters of the compound, and combinations thereof:
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: August 5, 2014
    Assignee: China Medical University
    Inventors: Chen-Chen Lee, Chien-Neng Wang
  • Patent number: 8778988
    Abstract: A method of making an endoperoxide from a diene and oxygen in the presence of a photocatalyst having an excited state lifetime of at least 100 nanoseconds, the endoperoxide being represented by the formula: where R1 is an aryl substituted with at least one group selected from the group consisting of alkoxy, hydroxyl, halogen, carbamate, sulfonamide, silyloxy, amide, and combinations thereof or a substituted or unsubstituted heteroaryl, R2 is hydrogen, alkyl, alkynyl, or aryl, R3 is hydrogen, alkyl, alkynyl, or aryl, R4 is alkynyl or aryl, R5 is hydrogen or a substituent, R6 is hydrogen or a substituent, and A1, A2, and A3 are the same or different atoms and form a divalent group that combines with the two carbon atoms of the endoperoxide ring to form a saturated or unsaturated, substituted or unsubstituted ring system of a size of from five to six atoms.
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: July 15, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Tehshik P. Yoon, Jonathan D. Parrish, Michael A. Ischay
  • Patent number: 8765949
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Kai Gerlach, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Marco Santagostino, Stefan Scheuerer, Christofer Tautermann, Thomas Trieselmann
  • Patent number: 8748484
    Abstract: An anti-cancer ruthenium complex containing organometallic triruthenium with two maltol ligands is claimed.
    Type: Grant
    Filed: April 9, 2012
    Date of Patent: June 10, 2014
    Assignee: Research Foundation of The City University of New York
    Inventor: Varattur Dayal Reddy
  • Patent number: 8653304
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 18, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Patent number: 8633182
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
  • Patent number: 8633026
    Abstract: Methods and compositions for treating cells with cytokines are provided herein.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: January 21, 2014
    Inventor: Robert Sackstein
  • Publication number: 20140018414
    Abstract: The present invention provides methods for determining the selectivity of an anesthetic for an anesthetic-sensitive receptor by determining the molar water solubility of the anesthetic. The invention further provides methods for modulating the selectivity of an anesthetic for an anesthetic-sensitive receptor by altering or modifying the anesthetic to have higher or lower water solubility. The invention further provides methods of inducing anesthesia in a subject by administering via the respiratory pathways (e.g., via inhalational or pulmonary delivery) an effective amount of an anesthetic compound identified according to the present methods.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 16, 2014
    Inventor: Robert J. Brosnan
  • Publication number: 20140011845
    Abstract: Disclosed are cyclic dione derivatives represented by formula (I), wherein the substituents are as defined in the description. The preparation method, intermediate and use thereof are also provided.
    Type: Application
    Filed: December 30, 2011
    Publication date: January 9, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Stephane Andre Marie Jeanmart, Long Lu, Yaming Wu, Lisheng Mao, Michel Muehlbeach
  • Patent number: 8623912
    Abstract: Novel Fostriecin (or FST) derivatives represented by formula (I), the pharmaceutical compositions and preparation methods thereof. The pharmaceutical uses of these compounds, especially the use for the preparation of pharmaceutical compositions for treating tumor, inhibiting cell over growth, or lowering myocardial infarction and the injury to cells.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: January 7, 2014
    Assignees: Beijing Biostar Technologies, Ltd., Dalian University of Technology
    Inventors: Li Tang, Rongguo Qiu
  • Patent number: 8580846
    Abstract: The invention is directed to a method of preventing or ameliorating a neuropsychiatric or neurodegenerative disease or disorder in a subject. The method includes administering a composition comprising equol in an amount sufficient to prevent or ameliorate the neuropsychiatric or neurodegenerative disease or disorder. The equol may be a racemic mixture of R-equol and S-equol. The equol may be enantiomerically enriched with R-equol or enantiomerically enriched with S-equol.
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: November 12, 2013
    Assignees: Brigham Young University, Children's Hospital Medical Center, Colorado State University Research Foundation
    Inventors: Edwin Douglas Lephart, Trent D. Lund, Kenneth David Reginald Setchell, Robert J. Handa
  • Publication number: 20130296414
    Abstract: Metabolites of [2-(3-methoxyphenyl)-cyclohexylmethyl]dimethylamine as free bases and/or in the form of physiologically acceptable salts, corresponding medicaments, the use of [2-(3-methoxyphenyl)-cyclohexylmethyl]-dimethylamine and the metabolites thereof for producing a medicament used for treating depression, and related methods of treating depression, pain and urinary incontinence.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Elmar FRIDERICHS, Wolfgang STRASSBURGER, Ulrich JAHNEL, Helmut BUSCHMANN, Joerg HOLENZ, Oswald ZIMMER, Derek SAUNDERS, Werner ENGLBERGER, Hagen-Heinrich HENNIES
  • Patent number: 8569362
    Abstract: The present invention relates to a polyketide molecule of the following formula (I): or a pharmaceutically acceptable salt thereof, where R1 is a hydrogen atom or a (C1-C7) alkyl group, as well as the method of preparation and use thereof, in particular as an anticancer agent.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: October 29, 2013
    Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique (CNRS), Institut de Recherche pour le Development (IRD)
    Inventors: Isabelle Carletti, Georges Massiot, Cécile Debitus