Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 514/379)
  • Patent number: 7713959
    Abstract: Disclosed are pharmaceutical compositions comprising mirtazapine and an anticonvulsant drug. Also disclosed are methods of preventing weight gain associated with the administration of mirtazapine comprising identifying a patient to whom mirtazapine is to be administered and administering to said patient a pharmaceutical composition comprising mirtazapine and an anticonvulsant drug. Further disclosed are methods of increasing the efficacy of mirtazapine comprising identifying a patient to whom mirtazapine is to be administered and administering to said patient a pharmaceutical composition comprising mirtazapine and an anticonvulsant drug.
    Type: Grant
    Filed: August 31, 2005
    Date of Patent: May 11, 2010
    Assignee: Duke University
    Inventors: K. Ranga R. Krishnan, Kishore M. Gadde
  • Publication number: 20100113423
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Application
    Filed: October 19, 2009
    Publication date: May 6, 2010
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Publication number: 20100093733
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.
    Type: Application
    Filed: February 15, 2008
    Publication date: April 15, 2010
    Applicant: PROSIDION LIMITED
    Inventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
  • Publication number: 20100093788
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.
    Type: Application
    Filed: October 9, 2009
    Publication date: April 15, 2010
    Inventors: Mark R. Player, Daniel J. Parks, William Parsons, Senath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
  • Patent number: 7696238
    Abstract: Substituted benzo[d]isoxazol-3-yl amine compounds corresponding to formula I which exhibit an strong affinity to the KCNQ2/3 K+ channel, and which are suitable for treating or inhibiting pain and/or disorders or disease states that are at least partly mediated by the KCNQ2/3 K+ channel.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: April 13, 2010
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Robert Frank, Gregor Bahrenberg, Wolfgang Schroeder, Saskia Zemolka
  • Publication number: 20100069451
    Abstract: The present invention relates to oxalate salt of the compound of formula (I) in all its stereochemical configurations, a process for its preparation and its use in treating mood disorders, disorders of anxiety, depression and convulsive conditions, in the improvement of learning ability, in the reversal of amnesia, in resolving the abstinence syndrome from drugs and drugs of abuse. Preferably, the invention concerns oxalate salt of rel-(3R,3aS,7aS)-3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one.
    Type: Application
    Filed: October 31, 2007
    Publication date: March 18, 2010
    Applicant: ABIOGEN PHARMA S.P.A
    Inventors: Fabio Neggiani, Laura Dini
  • Publication number: 20100069433
    Abstract: The present invention provides a therapeutic agent for hyperlipidemia having an excellent effect of lowering the cholesterol and triglyceride level in blood plasma.
    Type: Application
    Filed: March 28, 2008
    Publication date: March 18, 2010
    Applicant: KOWA COMPANY, LTD.
    Inventors: Toshiaki Takizawa, Noriyuki Inoue, Katsutoshi Miyosawa
  • Publication number: 20100069450
    Abstract: The present invention relates to fumarate salt of the compound of formula (I) in all its stereochemical configurations, a process for its preparation and its use in treating mood disorders, disorders of anxiety, depression and convulsive conditions, in the improvement of learning ability, in the reversal of amnesia, in resolving the abstinence syndrome from drugs and drugs of abuse. Preferably, the invention concerns fumarate salt of rel-(3R,3aS,7aS)-3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one.
    Type: Application
    Filed: October 31, 2007
    Publication date: March 18, 2010
    Applicant: ABIOGEN PHARMA S.P.A
    Inventors: Fabio Neggiani, Laura Dini
  • Patent number: 7655681
    Abstract: A method of treating or preventing Obstructive Sleep Apnea (OSA) comprises the administration of a pharmacologically effective amount of zonisamide to a patient in need thereof, with the proviso that OSA caused by external mechanical obstruction of the airways, such as by mucus, is excluded. Also disclosed is the use of zonisamide for the manufacture of a medicament useful in the treatment; a protective patch comprising zonisamide and a pharmaceutically acceptable carrier for transdermal or transmucosal administration to a person suffering from OSA; and the use of zonisamide for the manufacture of a diagnostic device, kit or composition for the diagnosis of sleep disordered breathing.
    Type: Grant
    Filed: February 15, 2005
    Date of Patent: February 2, 2010
    Inventors: Ludger Grote, Kaj Stenlof, Jan Hedner
  • Patent number: 7655700
    Abstract: The present invention describes a transgenic mouse susceptible to neuromuscular disease. The present invention also includes methods for treatment of neuromuscular diseases by interfering with activity between androgen and androgen receptors exclusively in the muscle fibers.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: February 2, 2010
    Assignee: Michigan State University
    Inventors: Cynthia Jordan, Douglas A. Monks, Marc Breedlove
  • Publication number: 20100022530
    Abstract: Compounds of the formula (I) in which A1, A2, R1, X1, X2, X3, Y, R2, Cy and n have meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: November 22, 2007
    Publication date: January 28, 2010
    Applicant: MERCK PATENT GMBH
    Inventors: Kai Schiemann, Dirk Finsinger, Frank Zenke
  • Publication number: 20100016299
    Abstract: The present application relates to novel substituted benzoxepinoisoxazole derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis, restenosis and ischemias.
    Type: Application
    Filed: June 28, 2007
    Publication date: January 21, 2010
    Applicant: BAYER HEALTHCARE AG
    Inventors: Nils Griebenow, Anja Buchmüller, Peter Kolkhof, Hilmar Bischoff
  • Patent number: 7645885
    Abstract: The invention provides non-steroidal ligands for the androgen receptor, methods for making non-steroidal ligands of the androgen receptor, compositions of non-steroidal ligands of the androgen receptor and methods of using non-steroidal ligands and compositions of non-steroidal ligands of the androgen receptor for treating or preventing diseases (e.g., prostate cancer) associated with androgen binding to the androgen receptor.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: January 12, 2010
    Assignee: The Regents of the University of California
    Inventors: Thomas S. Scanlan, Dmitry V. Kadnikov
  • Patent number: 7642276
    Abstract: Compounds of formula (I): wherein A is a 5-membered heteroaryl ring are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38, such as rheumatoid arthritis.
    Type: Grant
    Filed: July 30, 2003
    Date of Patent: January 5, 2010
    Assignee: SmithKline Beecham Corporation
    Inventors: Richard Martyn Angell, Ian Robert Baldwin, Paul Bamborough, Nigel Marc Deboeck, Timothy Longstaff, Stephen Swanson
  • Publication number: 20090306051
    Abstract: The present invention relates to methods and compositions for treating CNS-related disorders.
    Type: Application
    Filed: December 11, 2008
    Publication date: December 10, 2009
    Inventors: Laurence R. Meyerson, Gregory T. Went, Timothy J. Fultz
  • Patent number: 7629372
    Abstract: A class of compounds having Formula I and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of developing conditions and sequelae that are associated with these diseases, such as atherosclerosis.
    Type: Grant
    Filed: September 12, 2005
    Date of Patent: December 8, 2009
    Assignee: Merck & Co., Inc.
    Inventors: James F. Dropinski, Guo Q. Shi, Yong Zhang
  • Publication number: 20090298854
    Abstract: This invention is directed to indole acetic acid derivatives and their use in pharmaceutical compositions for the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic disease. The invention is also directed to intermediates useful in preparation of indole acetic derivatives and to methods of preparation.
    Type: Application
    Filed: July 23, 2009
    Publication date: December 3, 2009
    Inventors: Xin Ma, Louis-David Cantin, Soongyu Choi, Roger Clark, Martin Hentemann, Joachim Rudolph, Rico Lavoie, Zhonghua Zhang
  • Publication number: 20090275628
    Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.
    Type: Application
    Filed: May 17, 2006
    Publication date: November 5, 2009
    Applicant: Gruenenthal GmbH
    Inventors: Robert Frank, Ruth Jostock, Melanie Reich, Gregor Bahrenberg, Hans Schick, Helmut Sonnenschein
  • Patent number: 7598283
    Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: October 6, 2009
    Assignee: Abbott Laboratories, Inc.
    Inventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
  • Publication number: 20090221488
    Abstract: Disclosed inter alia is the use of certain chromenone derivatives, which are modulators of a mitotic kinesin such as KSP, in the treatment of cellular proliferative diseases. The chromenones derivatives are administered with another chemotherapeutic agent selected from neutropenia treatment agents, alkylating agents, antimetabolites, platinating agents, topoisomerase inhibitors, tubulin agents and signalling inhibitors (e.g., kinase inhibitors). Pharmaceutical compositions comprising one or both types of active agents are also disclosed.
    Type: Application
    Filed: December 7, 2006
    Publication date: September 3, 2009
    Inventors: Kenneth W. Wood, Lisa Belmont
  • Publication number: 20090197884
    Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.
    Type: Application
    Filed: October 26, 2006
    Publication date: August 6, 2009
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
  • Publication number: 20090163563
    Abstract: Novel macrolactone compounds, their methods of preparation, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the macrolactone compounds may be useful, inter alia, for treating various cancers, inducing apoptosis in malignant cells, or inhibiting cancer cell division.
    Type: Application
    Filed: December 1, 2008
    Publication date: June 25, 2009
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: Thomas M. Razler, Amos B. Smith, III, Jeffrey P. Ciavarri, Tomoyasu Hirose, Tomoyasu Ishikawa
  • Publication number: 20090156592
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: July 27, 2007
    Publication date: June 18, 2009
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Robert James Pasteris, Mary Ann Hanagan, Rafael Shapiro
  • Patent number: 7544667
    Abstract: The present invention relates to novel hypocholesterolemic compounds of formula (I) useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alone or in combination with other active agents.
    Type: Grant
    Filed: September 15, 2004
    Date of Patent: June 9, 2009
    Assignee: Lipideon Biotechnology AG
    Inventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder
  • Publication number: 20090143422
    Abstract: This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.
    Type: Application
    Filed: February 2, 2009
    Publication date: June 4, 2009
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Mark Munson, David A. Mareska, Youngboo Kim, Robert D. Groneberg, James Rizzi, Martha Rodriguez, Ganghyeok Kim, Guy Vigers, Chang Rao, Devan Balachari, Darren Harvey
  • Publication number: 20090111820
    Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
    Type: Application
    Filed: October 24, 2008
    Publication date: April 30, 2009
    Inventors: Kenneth GRANBERG, Bjorn HOLM
  • Publication number: 20090105245
    Abstract: The present invention provides methods for inhibiting increased vascular permeability and/or pathologic ocular angiogenesis via administration of a combination of one or more molecules that potently inhibit select receptor tyrosine kinases (RTKs) or vascular endothelial growth factor (VEGF) and one or more anti-inflammatory agents.
    Type: Application
    Filed: December 21, 2007
    Publication date: April 23, 2009
    Inventor: David P. Bingaman
  • Publication number: 20090054430
    Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
    Type: Application
    Filed: July 16, 2008
    Publication date: February 26, 2009
    Applicant: Abbott Laboratories
    Inventors: Yujia Dai, Ji Zhiqin, Michael R. Michaelides
  • Patent number: 7495020
    Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
    Type: Grant
    Filed: January 18, 2006
    Date of Patent: February 24, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, A. Brian Jones, Joel P. Berger, James F. Dropinski, Alexander Elbrecht, Kun Liu, Karen Lamb MacNaul, Guo-Qiang Shi, Derek J. Von Langen, Gaochao Zhou
  • Publication number: 20090048247
    Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.
    Type: Application
    Filed: February 13, 2006
    Publication date: February 19, 2009
    Inventors: Venkata P. Palle, Sarala Balachandran, Nidhi Gupta, Nagarajan Muthukamal, Mandadapu Raghu Ramaiah, Manoj Kumar Khera, Lailt Kumar Baregama, Vinayak Vasantrao Khairnar, Abhijit Ray, Sunanda G. Dastidar
  • Publication number: 20090042866
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Application
    Filed: November 23, 2005
    Publication date: February 12, 2009
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Publication number: 20090042945
    Abstract: The present invention relates to substituted benzo[d]isoxazol-3-yl-amine compounds, methods for their production, medicaments containing these compounds and the use of these compounds to produce medicaments.
    Type: Application
    Filed: May 18, 2006
    Publication date: February 12, 2009
    Applicant: Gruenenthal GmbH
    Inventors: Robert Frank, Beatrix Merla, Melanie Reich, Ruth Jostock
  • Publication number: 20090036426
    Abstract: The present invention relates to methods of treating obesity, anorexia nervosa, or bulimia nervosa comprising administering a compound of the invention conjointly with zonisamide, naltrexone, or a pharmaceutically acceptable salt thereof. The present invention further relates to the treatment of metabolic syndrome comprising administering a compound of the invention conjointly with zonisamide, naltrexone, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: July 30, 2008
    Publication date: February 5, 2009
    Applicant: AMPLA Pharmaceuticals Inc.
    Inventor: James R. Hauske
  • Publication number: 20090023779
    Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.
    Type: Application
    Filed: October 14, 2005
    Publication date: January 22, 2009
    Applicant: Laboratoire Theramex
    Inventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos
  • Publication number: 20090012074
    Abstract: The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH?N—, —CH?CH— or —N?CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts
    Type: Application
    Filed: October 14, 2005
    Publication date: January 8, 2009
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry
  • Publication number: 20090005323
    Abstract: This invention relates to the treatment of obesity, the treatment of obesity related disorders, prevention of weight gam, prevention of weight regain or for weight maintenance by the use of a cathepsin K inhibitor as active ingredient, alone or in conjunction with other anti-obesity agents The invention also relates to the pharmaceutical compositions comprising cathepsin K inhibitor as active ingredient, pharmaceutically acceptable carriers or excipients, and optionally one or more anti-obesity agents.
    Type: Application
    Filed: January 17, 2006
    Publication date: January 1, 2009
    Inventor: Michael David Percival
  • Publication number: 20080319036
    Abstract: The present invention relates, in general, to obesity, and, in particular, to a method of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight-loss promoting anticonvulsant either alone or in combination with bupropion or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.
    Type: Application
    Filed: September 5, 2008
    Publication date: December 25, 2008
    Applicant: Duke University
    Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
  • Publication number: 20080312163
    Abstract: This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.
    Type: Application
    Filed: June 13, 2007
    Publication date: December 18, 2008
    Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
  • Publication number: 20080312301
    Abstract: The invention relates to substituted N-benzo[d]isoxazol-3-yl-amine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are defined as in patent claim 1. The invention also relates to the use of said compounds for producing medicaments.
    Type: Application
    Filed: June 6, 2006
    Publication date: December 18, 2008
    Applicant: Gruenenthal GmbH
    Inventors: Beatrix Merla, Matthias Gerlach, Corinna Sundermann, Utz-Peter Jagusch, Hagen-Heinrich Hennies, Stefan Oberborsch, Michael Haurand, Ruth Jostock, Melanie Reich
  • Patent number: 7462636
    Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(?O)—, —C(?S)—, —S(?O)2—, C1-6alkanediyl-C(?O)—, C1-6alkanediyl-C(?S)— or C1-6alkanediyl-S(?O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-
    Type: Grant
    Filed: May 16, 2003
    Date of Patent: December 9, 2008
    Assignee: Tibotec Pharmaceuticals Ltd
    Inventors: Dominique Louis Nestor Ghislain Surleraux, Bernhard Joanna Bernard Vergouwen, Herman Augustinus De Kock
  • Patent number: 7459564
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: December 2, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. Pinto
  • Patent number: 7449487
    Abstract: The invention relates to the use of at least one unsaponifiable component of vegetable oil, in particular of avocado, soya bean and/or lupin oils, for the preparation of a medicament intended to stimulate the expression of TGF-? or the expression of the plasminogen activator inhibitor PAI-1. The invention also relates to a method of cosmetic treatment comprising the application of at least one unsaponifiable component of vegetable oil as well as the use of the latter as additive in a food for human beings and/or for animals.
    Type: Grant
    Filed: July 15, 2003
    Date of Patent: November 11, 2008
    Assignee: Laboratoires Expanscience
    Inventors: Karim Boumediene, Jean-Pierre Pujol, Georges Bernard Guillou, Philippe Msika, Chafik Ghayor
  • Publication number: 20080269271
    Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.
    Type: Application
    Filed: May 17, 2006
    Publication date: October 30, 2008
    Applicant: Gruenenthal GmbH
    Inventors: Robert Frank, Melanie Reich, Ruth Jostock, Gregor Bahrenberg, Hans Schick, Birgitta Henkel, Helmut Sonnenschein
  • Publication number: 20080262055
    Abstract: There is provided a series of heterocyclic-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: April 8, 2008
    Publication date: October 23, 2008
    Inventors: Shuhao Shi, Samuel Gerritz, Shirong Zhu
  • Publication number: 20080255133
    Abstract: This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: January 18, 2008
    Publication date: October 16, 2008
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Jean-Michel Vernier, Andreas Maderna, Yung-hyo Koh, Zhi Hong
  • Patent number: 7429580
    Abstract: Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is a psychotherapeutic agent and the second compound is a anticonvulsant. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual with a psychotherapeutic agent and an anticonvulsant.
    Type: Grant
    Filed: January 11, 2005
    Date of Patent: September 30, 2008
    Assignees: Orexigen Therapeutics, Inc., Duke University
    Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
  • Patent number: 7425571
    Abstract: The present invention relates, in general, to obesity, and, in particular, to a method of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight-loss promoting anticonvulsant either alone or in combination with bupropion or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.
    Type: Grant
    Filed: April 23, 2004
    Date of Patent: September 16, 2008
    Assignee: Orexigen Therapeutics, Inc.
    Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
  • Publication number: 20080194586
    Abstract: Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dylipidermia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
    Type: Application
    Filed: March 3, 2006
    Publication date: August 14, 2008
    Inventors: Harold B. Wood, Peter T. Meinke, Guo Q. Shi, Yong Zhang
  • Publication number: 20080188476
    Abstract: The present invention relates, in general, to obesity, and, in particular, to a method of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight-loss promoting anticonvulsant either alone or in combination with bupropion or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.
    Type: Application
    Filed: May 5, 2006
    Publication date: August 7, 2008
    Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
  • Publication number: 20080188510
    Abstract: The present invention relates to usefulness of zonisamide as a pharmaceutical composition for treating dementia or cognitive impairment.
    Type: Application
    Filed: May 23, 2006
    Publication date: August 7, 2008
    Applicant: Eisai R & D Management Co., Ltd.
    Inventor: Hiroshi Yoshino