Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/299)
  • Publication number: 20100035915
    Abstract: Novel compounds of the formula (I), in which X, Y, R, R1, R1, R1?, R2, R2?, R3, R4, R4?, R5 and n have the meanings indicated in patent claim 1, are suitable as antidiabetics.
    Type: Application
    Filed: November 17, 2007
    Publication date: February 11, 2010
    Applicant: Merck Patent Gesellschaft
    Inventors: Werner Mederski, Norbert Beier, Lars Thore Burgdorf, Rolf Gericke, Markus Klein, Christos Tsaklakidis
  • Publication number: 20100034745
    Abstract: The subject invention concerns the reduction of protein aggregation in the neurons of a mammal through the use of a ketogenic treatment such as a ketogenic diet, a physical training regimen and/or administration of agents to increase fatty acid oxidation. Such ketogenic treatment can be useful in the reduction of certain aggregates including amyloid ? peptide, polyglutamine containing huntintin protein, polyglutamine containing androgen receptor, polyglutamine containing atrophin-1, polyglutamine containing ataxins, ?-synclein, prion protein, tau and superoxide dismutase 1 (SOD1).
    Type: Application
    Filed: July 8, 2009
    Publication date: February 11, 2010
    Applicant: NEUERA PHARMACEUTICALS, INC.
    Inventor: Samuel T. Henderson
  • Publication number: 20100035916
    Abstract: The invention relates to compounds of the general formula (I): Wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.
    Type: Application
    Filed: August 4, 2009
    Publication date: February 11, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Omar BEN AYAD, Odile LECLERC, Alistair LOCHEAD, Mourad SAADY, Franck SLOWINSKI, Julien VACHE
  • Publication number: 20100035914
    Abstract: The present invention relates to novel compounds of formula (I)?, and pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R1 is hydrogen or C1-4 alkyl; R2 is a group A, K or W wherein A is K is an ? or ? naphthyl group, optionally substituted by 1 or 2 groups R18, each of them being the same or different; and W is and wherein G is a 5,6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; wherein G may be substituted by (R15)p, which can be the same or different; p is an integer from 0 to 5; R3 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to a group X or X1; R4 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to a group X or X1; R5 is hydrogen or C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; or is a group X, X1, X2 or X3; wherein X is X1 is X2 is and X3 is R6 is hydrogen or C1-4 alkyl; or is a group X or X1; R9 is C1-4a
    Type: Application
    Filed: September 7, 2007
    Publication date: February 11, 2010
    Inventors: Barbara Bertani, Romano Di Fabio, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20100029624
    Abstract: A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.
    Type: Application
    Filed: July 16, 2009
    Publication date: February 4, 2010
    Applicant: King's College London
    Inventors: Nnaemeka Ikechukwu AMOBI, Ian Christopher SMITH
  • Publication number: 20100021420
    Abstract: A combination comprising (a) a compound of formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NR9(C?O) or 0(C?O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1 to 3 carbon atoms; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or an optionally substituted C1-8 hydrocarbyl group wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; and (b) a compound of formul
    Type: Application
    Filed: July 13, 2007
    Publication date: January 28, 2010
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: John Francis Lyons, Matthew Simon Squires, Neil Thomas Thompson, Neil James Gallagher
  • Publication number: 20100016349
    Abstract: Disclosed herein are pseudoazulenyl nitrone compounds and methods of using these compounds to trap free radicals and to treat, prevent, or ameliorate various diseases associated with free radicals.
    Type: Application
    Filed: June 27, 2007
    Publication date: January 21, 2010
    Applicant: THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES
    Inventors: David A. Becker, Amolkumar Kolhe
  • Publication number: 20100009960
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure formula (I) enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.
    Type: Application
    Filed: July 2, 2007
    Publication date: January 14, 2010
    Inventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
  • Publication number: 20100009983
    Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, in combination with one or more other neurogenic agents, or anti-astrogenic agent, to stimulate or activate the formation of new nerve cells.
    Type: Application
    Filed: June 25, 2009
    Publication date: January 14, 2010
    Applicant: BrainCells, Inc.
    Inventors: Carrolee Barlow, Todd A. Carter, Andrew Morse, Kai Treuner, Kym I. Lorrain
  • Publication number: 20100010034
    Abstract: The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: [3-(2,4-dichlorophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(2-fluoro-4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methanesulfonyl-2-trifluoromethylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, (R)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, [3-(4-ethanesulfonylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, (S)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, ethanesulfonylaminobenzenesulfonyl)-6-fluoro-2-methyiindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(2-chloro-4-methanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(4-methanesulfonylbenzyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-chlorobenzyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-
    Type: Application
    Filed: December 21, 2006
    Publication date: January 14, 2010
    Inventors: George Hynd, Nicholas Charles Ray, Harry Finch, David Middlemiss, Michael Colin Cramp, Paul Matthew Blaney, Karen Williams, Yann Griffon, Trevor Keith Harrison, Peter Crackett
  • Patent number: 7645765
    Abstract: The invention relates to a drug containing an aqueous formulation of Moxaverin and at least one water-miscible solubilizer.
    Type: Grant
    Filed: September 2, 2002
    Date of Patent: January 12, 2010
    Assignee: Molecular and Clinical Drug Research
    Inventor: Ralph E. Eckert
  • Publication number: 20100003353
    Abstract: In a method for treating an affected skin region of a patient having a skin disorder, a vasodilation composition is applied to an affected skin region of a patient, the affected skin region exhibiting a skin disorder characterized by at least one abnormal blood vessel, and the affected skin region is then treated so as to non-invasively disrupt tissue architecture, e.g., by inducing ischemia, of the at least one abnormal blood vessel. A vasoconstriction composition can then be applied to the skin region to cause vasoconstriction of the at least one blood vessel in order to promote healing.
    Type: Application
    Filed: June 11, 2009
    Publication date: January 7, 2010
    Applicant: BIOCHEMICS, INC.
    Inventors: Laura Stephens, John J. Masiz, Stephen G. Carter, Zhen Zhu, Kanu Patel
  • Publication number: 20090325999
    Abstract: This invention relates to personalized pharmaceutical kits, packaging, compositions, and methods for treatment of a mammal, comprising at least one antihistamine for treating an allergic disease or condition in a mammal, in combination with at least one wakefulness promoting agent for preventing sedative effects during day time use, while promoting the antihistamine and sedating effect during evening use.
    Type: Application
    Filed: June 27, 2008
    Publication date: December 31, 2009
    Inventor: Jie Du
  • Publication number: 20090326000
    Abstract: A method is provided for preventing or treating obesity and for reducing the percentage body fat content of an individual. The method involves administration, preferably topical administration, of an active agent selected from the group consisting of resveratrol, pharmacologically acceptable salts, esters, amides, and analogs thereof, and combinations of any of the foregoing. Topical formulations for use in conjunction with the method for reducing the percentage body fat content of an individual are provided as well.
    Type: Application
    Filed: June 27, 2008
    Publication date: December 31, 2009
    Inventors: Christopher Hull, Jeffrey Feliciano
  • Publication number: 20090325949
    Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.
    Type: Application
    Filed: June 25, 2009
    Publication date: December 31, 2009
    Applicant: BrainCells, Inc.
    Inventors: Carrolee Barlow, Todd Carter, Andrew Morse, Kai Treuner, Kym I. Lorrain
  • Patent number: 7638488
    Abstract: The present invention provides methods for treating a flavivirus infection, including hepatitis C virus (HCV) infection, in an individual suffering from a flavivirus infection. In some embodiments, the methods involve administering to an individual in need thereof an effective amount of an agent that inhibits enzymatic activity of a membrane-bound ?-glucosidase inhibitor. In other embodiments, the methods involve administering to an individual in need thereof effective amounts of an ?-glucosidase inhibitor and at least one additional therapeutic agent.
    Type: Grant
    Filed: March 7, 2006
    Date of Patent: December 29, 2009
    Assignee: Intermune, Inc.
    Inventors: Lawrence M. Blatt, Hua Tan, Scott Seiwert
  • Patent number: 7638533
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating RXR mediated disorders. More particularly, the compounds of the present invention are RXR agonists useful for treating RXR mediated disorders.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: December 29, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Bharat Lagu, Rimma Lebedev, Barbara Pio
  • Patent number: 7635702
    Abstract: Novel imidazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)- signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: December 22, 2009
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Michael J. Munchhof, Laura C. Blumberg
  • Publication number: 20090312364
    Abstract: This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: December 18, 2007
    Publication date: December 17, 2009
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, John Paul Redrobe, Gunnar M. Olson, Elsebet Ostergaard Nielsen
  • Publication number: 20090312362
    Abstract: Compounds that are inhibitors of the unfolded protein response and endonuclease IRE1 are provided, together with compositions comprising such compounds, and methods for their use in the treatment of various disorders, such as cancer, autoimmune disorders, and diabetes. Also provided are packaged pharmaceuticals comprising these compositions. The compositions may be administered in combination with another therapeutic agent.
    Type: Application
    Filed: February 27, 2007
    Publication date: December 17, 2009
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Albert C. Koong, Douglas E. Feldman
  • Publication number: 20090312295
    Abstract: The instant invention relates to methods using satraplatin, packaged-pharmaceutical-products that include satraplatin and uses of satraplatin to prepare pharmaceutical compositions for the 2nd line treatment of metastatic hormone refractory prostate cancer.
    Type: Application
    Filed: September 24, 2007
    Publication date: December 17, 2009
    Inventors: Thomas J. McKearn, Marcel Rozencweig
  • Patent number: 7629337
    Abstract: Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.
    Type: Grant
    Filed: July 27, 2006
    Date of Patent: December 8, 2009
    Assignee: Genzyme Corporation
    Inventors: Gary J. Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols
  • Publication number: 20090286777
    Abstract: The present invention is directed to certain 5,6-fused pyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Application
    Filed: May 11, 2007
    Publication date: November 19, 2009
    Inventors: Jianming Bao, Robert J. DeVita, Sander G. Mills, Gregori J. Morriello
  • Patent number: 7619110
    Abstract: The present invention provides a prodrug of propofol and crystalline forms thereof, methods of making the propofol prodrug and crystalline forms thereof, pharmaceutical compositions of the propofol prodrug and crystalline forms thereof, methods of using the propofol prodrug and crystalline forms thereof and pharmaceutical compositions thereof to treat diseases or disorders such as headache pain, post-chemotherapy or post-operative surgery nausea and vomiting, neurodegenerative disorders, and mood disorders.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: November 17, 2009
    Assignee: XenoPort, Inc.
    Inventors: Feng Xu, Mark A. Gallop, Vivek Sasikumar, Usha Dilip
  • Publication number: 20090281135
    Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof: wherein G is selected from the group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, and a 8- to 11-membered heteroaryl bicyclic group; wherein G may be substituted by (R2)p, which can be the same or different; R1 is hydrogen or C1-4 alkyl; R2 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to R8; R5 is hydrogen or C1-4 alkyl; R6 is hydrogen or C1-4 alkyl; R7 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to X, X1, X2 or X3; wherein X corresponds to: X1 corresponds to: X2 corresponds to: X3 corresponds to: R3 is hydrogen or C1-4 alkyl; or corresponds to X or X1; R4 is hydrogen or C1-4 alkyl; or corresponds to X or X1; R8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents select
    Type: Application
    Filed: September 7, 2007
    Publication date: November 12, 2009
    Inventors: Romano Di Fabio, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20090275606
    Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable salts. These compounds can act as potential MEK inhibitors in the treatment of hyperproliferative diseases, like cancer and inflammation. The present invention also reveals methods of preparation thereof.
    Type: Application
    Filed: April 21, 2009
    Publication date: November 5, 2009
    Inventors: Dinesh Chikkanna, Clive McCarthy, Henrik Moebitz, Chetan Pandit, Ramesh Sistla, Hosahalli Subramanya
  • Publication number: 20090274677
    Abstract: The invention provides the use a 2,2-dimethyl chroman as a SOD mimetic in a cosmetic preparation. Cosmetic preparations comprising a 2,2-dimethyl chroman as a SOD mimetic are described, as well as methods for treating or preventing free radical damage to skin cells and treating or preventing hair loss which comprise topical administration of a 2,2-dimethyl chroman as a SOD mimetic.
    Type: Application
    Filed: May 1, 2009
    Publication date: November 5, 2009
    Inventors: Elliot James Isaacs, Emma Gregory
  • Patent number: 7612084
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: November 3, 2009
    Assignee: Pfizer Inc
    Inventors: Kim James, Lyn Howard Jones, David Anthony Price
  • Patent number: 7612087
    Abstract: This invention discloses and claims methods for inhibiting bacterial ?-lactamases and treating bacterial infections by inhibiting bacterial ?-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a ?-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a ?-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.
    Type: Grant
    Filed: July 26, 2004
    Date of Patent: November 3, 2009
    Assignee: Novexel
    Inventors: Jozsef Aszodi, Claude Fromentin, Maxime Lampilas, David Alan Rowlands
  • Patent number: 7612085
    Abstract: A series of N-substituted 9-azabicyclo[3.3.1]nonan-3?-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (?1 and ?2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3?-yl)-N?-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3?-yl)-N?-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for ?2 versus ?1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the ?2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: November 3, 2009
    Assignee: Washington University
    Inventors: Robert H. Mach, Zhude Tu, Wenhua Chu, Suwanna Vangveravong, Richard Hotchkiss, William Hawkins, Rebecca Aft
  • Patent number: 7608626
    Abstract: Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
    Type: Grant
    Filed: October 27, 2005
    Date of Patent: October 27, 2009
    Assignee: Wyeth
    Inventors: Annmarie Louise Sabb, Robert Lewis Vogel
  • Publication number: 20090263322
    Abstract: The invention features substituted fused bicyclic compounds, pharmaceutical compositions containing them, and methods of using them to treat or prevent histamine-mediated diseases and conditions.
    Type: Application
    Filed: June 30, 2009
    Publication date: October 22, 2009
    Inventors: Richard Apodaca, Nicholas I. Carruthers, John R. Carson, Wenying Chai, Annette K. Kwok, Xiaobing Li, Timothy W. Lovenberg, Dale A. Rudolph, Chandravadan R. Shah
  • Publication number: 20090258858
    Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
    Type: Application
    Filed: October 28, 2005
    Publication date: October 15, 2009
    Inventors: Jakob Busch-Petersen, Jeffrey Charles Boehm, Huijie Li, John J. Taggart, Hong Xing Yan
  • Publication number: 20090258896
    Abstract: Novel compositions comprising a combination of at least one higher primary aliphatic alcohol preferably selected from those having 18 to 40 carbon atoms or mixtures thereof, at least one source of 5-hydroxytryptophan (5-HTP) optionally additionally comprising a source of caffeine and/or catechin-polyphenol and/or epigallocatechin gallate as active agents, either alone or in combination with other active agent(s), optionally with one or more excipient(s) are provided. Particularly, the invention relates to compositions and process for preparation of such compositions and method of use thereof for the management of obesity and associated disorders.
    Type: Application
    Filed: May 9, 2007
    Publication date: October 15, 2009
    Applicant: PANACEA BIOTEC LTD.
    Inventors: Rajesh Jain, Kour Chand Jindal
  • Publication number: 20090258872
    Abstract: The invention relates to therapeutic use of aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description.
    Type: Application
    Filed: June 23, 2009
    Publication date: October 15, 2009
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Petra LENNIG
  • Patent number: 7601735
    Abstract: Use of certain castanospermine esters in the treatment of diseases caused by flaviviruses, in particular in the treatment of disease caused by the hepatitis C virus (HCV) and compositions containing said esters in combination with adjunctive therapeutic agents.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: October 13, 2009
    Assignee: Virogen Ltd.
    Inventors: Albert Stanley Tyms, Debra Lynn Taylor
  • Publication number: 20090253705
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: April 2, 2009
    Publication date: October 8, 2009
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
  • Patent number: 7598233
    Abstract: This invention relates to a method for treating thrombosis by combined administration of a pitavastatin with aspirin.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: October 6, 2009
    Assignees: Kowa Co., Ltd., Nissan Chemical Industries, Ltd.
    Inventors: Toru Yokoyama, Taro Aoki
  • Publication number: 20090247570
    Abstract: The present invention relates to the use of a CCR5 antagonist in an HIV infected patient to enhance their immune reconstitution and so treat to HIV related opportunistic conditions resulting from the immunocompromised state of the HIV patient. The invention also allows treatment with a CCR5 antagonist of patients having a CXCR4 using viral population since such patients will also benefit from an increase in their CD4 and/or CD8 cell count.
    Type: Application
    Filed: May 30, 2007
    Publication date: October 1, 2009
    Inventor: Howard Bernard Mayer
  • Publication number: 20090247568
    Abstract: This application discloses aminopiperidinyl compounds of generic Formulae I-II: or pharmaceutically acceptable salts thereof, wherein m, r, Q1, Q2, Q3, R, Ra, R1, R2a, R2b, and R3 are defined as described herein, useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Application
    Filed: March 25, 2009
    Publication date: October 1, 2009
    Inventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
  • Patent number: 7592337
    Abstract: Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: September 22, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, Dehua Huang, Steve F. Poon, Thomas S. Reger, Jeffrey R. Roppe, Nicholas D. Smith
  • Publication number: 20090232898
    Abstract: There is provided pharmaceutical compositions for the treatment of migraine comprising a pharmacologically-effective amount of a triptan or an ergot, or a pharmaceutically-acceptable salt thereof; a pharmacologically-effective amount of an antiemetic compound, or a pharmaceutically-acceptable salt thereof; a bioadhesion and/or a mucoadhesion promoting agent; and carrier particles, wherein the active ingredients are presented in particulate form upon the surfaces of the carrier particles, which carrier particles are larger in size than the particles of the active ingredients; and the bioadhesion and/or mucoadhesion promoting agent is, at least in part, presented on the surfaces of the carrier particles.
    Type: Application
    Filed: March 28, 2006
    Publication date: September 17, 2009
    Inventors: Anders Pettersson, Thomas Lundqvist
  • Publication number: 20090227620
    Abstract: The use of a steroid sulfatase inhibitor in the preparation of a medicament for the treatment of inflammatory diseases.
    Type: Application
    Filed: March 15, 2006
    Publication date: September 10, 2009
    Inventor: Josef Gottfried Meingassner
  • Patent number: 7585874
    Abstract: The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I: wherein R1 to R5 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A ?5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: September 8, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Bo Han, Henner Knust, Andrew Thomas
  • Publication number: 20090221569
    Abstract: The invention relates to methods of treatment or prophylaxis of physiological and/or pathological conditions with at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonistsuch that the at least one LHRH antagonist is administered in a dose, which does not cause chemical (hormonal) castration.
    Type: Application
    Filed: February 27, 2009
    Publication date: September 3, 2009
    Applicant: AETERNA ZENTARIS GmbH
    Inventor: Juergen ENGEL
  • Patent number: 7582650
    Abstract: The invention is directed to compounds of Formula (I) useful as delta and mu opioid receptor modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
    Type: Grant
    Filed: June 15, 2006
    Date of Patent: September 1, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Bart DeCorte, Li Liu, Mark McDonnell, Jim McNally
  • Patent number: 7572798
    Abstract: The present invention relates to a series of new chemical agents that demonstrate anti-tumor activity. More particularly, the present invention relates to molecules, referred to as “combi-molecules”, that combine two major mechanisms of anti-tumor action. A combi-molecule is capable of degrading to a ligand involved in cell signaling pathways and to an agent capable of damaging DNA. More specifically, the present invention relates to molecules capable of blocking epidermal growth factor receptor (EGFR) mediated signal transduction and capable of damaging DNA. The present invention also relates to a general method of synthesis of these combi-molecules.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: August 11, 2009
    Assignee: McGill University
    Inventors: Bertrand J. Jean-Claude, Fabienne Dudouit, Stephanie Matheson
  • Publication number: 20090197822
    Abstract: The present disclosure provides compositions and methods for the treatment and elimination of chronic intracellular infections in cells or organisms. The compositions may include one or more acidic substances and one or more antimicrobial substances, administered in combination or separately. The methods may include administering an amount of one or more such compositions to an infected cell or organism for a period of time ranging from days to years, until the infection is substantially eliminated.
    Type: Application
    Filed: January 31, 2009
    Publication date: August 6, 2009
    Inventor: Paul Griffin
  • Publication number: 20090186916
    Abstract: Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3-dihydrdo-1-benzofuran, 2,3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.
    Type: Application
    Filed: July 17, 2007
    Publication date: July 23, 2009
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Satoshi Hayashibe, Shingo Yamasaki, Kazushi Watanabe, Nobuyuki Shiraishi, Daisuke Suzuki, Hiroaki Hoshii, Junya Ohmori, Takatoshi Kanayama
  • Patent number: 7563774
    Abstract: A combination therapy of at least one FBPase inhibitor and at least one other antidiabetic agent is disclosed.
    Type: Grant
    Filed: July 5, 2001
    Date of Patent: July 21, 2009
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Paul D. van Poelje, Mark D. Erion, Toshihiko Fujiwara