Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 514/379)
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Patent number: 7713959Abstract: 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: GrantFiled: August 31, 2005Date of Patent: May 11, 2010Assignee: Duke UniversityInventors: K. Ranga R. Krishnan, Kishore M. Gadde
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Publication number: 20100113423Abstract: 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: ApplicationFiled: October 19, 2009Publication date: May 6, 2010Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Publication number: 20100093788Abstract: 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: ApplicationFiled: October 9, 2009Publication date: April 15, 2010Inventors: Mark R. Player, Daniel J. Parks, William Parsons, Senath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
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Publication number: 20100093733Abstract: 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: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Patent number: 7696238Abstract: 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: GrantFiled: November 16, 2007Date of Patent: April 13, 2010Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Robert Frank, Gregor Bahrenberg, Wolfgang Schroeder, Saskia Zemolka
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Publication number: 20100069433Abstract: The present invention provides a therapeutic agent for hyperlipidemia having an excellent effect of lowering the cholesterol and triglyceride level in blood plasma.Type: ApplicationFiled: March 28, 2008Publication date: March 18, 2010Applicant: KOWA COMPANY, LTD.Inventors: Toshiaki Takizawa, Noriyuki Inoue, Katsutoshi Miyosawa
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Publication number: 20100069450Abstract: 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: ApplicationFiled: October 31, 2007Publication date: March 18, 2010Applicant: ABIOGEN PHARMA S.P.AInventors: Fabio Neggiani, Laura Dini
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Publication number: 20100069451Abstract: 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: ApplicationFiled: October 31, 2007Publication date: March 18, 2010Applicant: ABIOGEN PHARMA S.P.AInventors: Fabio Neggiani, Laura Dini
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Patent number: 7655681Abstract: 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: GrantFiled: February 15, 2005Date of Patent: February 2, 2010Inventors: Ludger Grote, Kaj Stenlof, Jan Hedner
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Patent number: 7655700Abstract: 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: GrantFiled: August 24, 2006Date of Patent: February 2, 2010Assignee: Michigan State UniversityInventors: Cynthia Jordan, Douglas A. Monks, Marc Breedlove
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Publication number: 20100022530Abstract: 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: ApplicationFiled: November 22, 2007Publication date: January 28, 2010Applicant: MERCK PATENT GMBHInventors: Kai Schiemann, Dirk Finsinger, Frank Zenke
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Publication number: 20100016299Abstract: 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: ApplicationFiled: June 28, 2007Publication date: January 21, 2010Applicant: BAYER HEALTHCARE AGInventors: Nils Griebenow, Anja Buchmüller, Peter Kolkhof, Hilmar Bischoff
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Patent number: 7645885Abstract: 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: GrantFiled: August 28, 2006Date of Patent: January 12, 2010Assignee: The Regents of the University of CaliforniaInventors: Thomas S. Scanlan, Dmitry V. Kadnikov
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Patent number: 7642276Abstract: 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: GrantFiled: July 30, 2003Date of Patent: January 5, 2010Assignee: SmithKline Beecham CorporationInventors: Richard Martyn Angell, Ian Robert Baldwin, Paul Bamborough, Nigel Marc Deboeck, Timothy Longstaff, Stephen Swanson
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Publication number: 20090306051Abstract: The present invention relates to methods and compositions for treating CNS-related disorders.Type: ApplicationFiled: December 11, 2008Publication date: December 10, 2009Inventors: Laurence R. Meyerson, Gregory T. Went, Timothy J. Fultz
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Patent number: 7629372Abstract: 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: GrantFiled: September 12, 2005Date of Patent: December 8, 2009Assignee: Merck & Co., Inc.Inventors: James F. Dropinski, Guo Q. Shi, Yong Zhang
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Publication number: 20090298854Abstract: 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: ApplicationFiled: July 23, 2009Publication date: December 3, 2009Inventors: Xin Ma, Louis-David Cantin, Soongyu Choi, Roger Clark, Martin Hentemann, Joachim Rudolph, Rico Lavoie, Zhonghua Zhang
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Publication number: 20090275628Abstract: 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: ApplicationFiled: May 17, 2006Publication date: November 5, 2009Applicant: Gruenenthal GmbHInventors: Robert Frank, Ruth Jostock, Melanie Reich, Gregor Bahrenberg, Hans Schick, Helmut Sonnenschein
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Patent number: 7598283Abstract: 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: GrantFiled: October 5, 2007Date of Patent: October 6, 2009Assignee: Abbott Laboratories, Inc.Inventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Publication number: 20090221488Abstract: 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: ApplicationFiled: December 7, 2006Publication date: September 3, 2009Inventors: Kenneth W. Wood, Lisa Belmont
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Publication number: 20090197884Abstract: 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: ApplicationFiled: October 26, 2006Publication date: August 6, 2009Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20090163563Abstract: 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: ApplicationFiled: December 1, 2008Publication date: June 25, 2009Applicant: The Trustees of the University of PennsylvaniaInventors: Thomas M. Razler, Amos B. Smith, III, Jeffrey P. Ciavarri, Tomoyasu Hirose, Tomoyasu Ishikawa
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Publication number: 20090156592Abstract: 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: ApplicationFiled: July 27, 2007Publication date: June 18, 2009Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Robert James Pasteris, Mary Ann Hanagan, Rafael Shapiro
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Patent number: 7544667Abstract: 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: GrantFiled: September 15, 2004Date of Patent: June 9, 2009Assignee: Lipideon Biotechnology AGInventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder
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Publication number: 20090143422Abstract: 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: ApplicationFiled: February 2, 2009Publication date: June 4, 2009Applicant: 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
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Publication number: 20090111820Abstract: 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: ApplicationFiled: October 24, 2008Publication date: April 30, 2009Inventors: Kenneth GRANBERG, Bjorn HOLM
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Publication number: 20090105245Abstract: 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: ApplicationFiled: December 21, 2007Publication date: April 23, 2009Inventor: David P. Bingaman
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Publication number: 20090054430Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: ApplicationFiled: July 16, 2008Publication date: February 26, 2009Applicant: Abbott LaboratoriesInventors: Yujia Dai, Ji Zhiqin, Michael R. Michaelides
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Patent number: 7495020Abstract: 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: GrantFiled: January 18, 2006Date of Patent: February 24, 2009Assignee: 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
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Publication number: 20090048247Abstract: 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: ApplicationFiled: February 13, 2006Publication date: February 19, 2009Inventors: 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
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Publication number: 20090042866Abstract: 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: ApplicationFiled: November 23, 2005Publication date: February 12, 2009Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
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Publication number: 20090042945Abstract: 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: ApplicationFiled: May 18, 2006Publication date: February 12, 2009Applicant: Gruenenthal GmbHInventors: Robert Frank, Beatrix Merla, Melanie Reich, Ruth Jostock
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Publication number: 20090036426Abstract: 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: ApplicationFiled: July 30, 2008Publication date: February 5, 2009Applicant: AMPLA Pharmaceuticals Inc.Inventor: James R. Hauske
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Publication number: 20090023779Abstract: 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: ApplicationFiled: October 14, 2005Publication date: January 22, 2009Applicant: Laboratoire TheramexInventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos
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Publication number: 20090012074Abstract: 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 saltsType: ApplicationFiled: October 14, 2005Publication date: January 8, 2009Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry
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Publication number: 20090005323Abstract: 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: ApplicationFiled: January 17, 2006Publication date: January 1, 2009Inventor: Michael David Percival
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Publication number: 20080319036Abstract: 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: ApplicationFiled: September 5, 2008Publication date: December 25, 2008Applicant: Duke UniversityInventors: Kishore M. Gadde, K. Ranga R. Krishnan
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Publication number: 20080312163Abstract: 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: ApplicationFiled: June 13, 2007Publication date: December 18, 2008Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
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Publication number: 20080312301Abstract: 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: ApplicationFiled: June 6, 2006Publication date: December 18, 2008Applicant: Gruenenthal GmbHInventors: Beatrix Merla, Matthias Gerlach, Corinna Sundermann, Utz-Peter Jagusch, Hagen-Heinrich Hennies, Stefan Oberborsch, Michael Haurand, Ruth Jostock, Melanie Reich
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Patent number: 7462636Abstract: 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: GrantFiled: May 16, 2003Date of Patent: December 9, 2008Assignee: Tibotec Pharmaceuticals LtdInventors: Dominique Louis Nestor Ghislain Surleraux, Bernhard Joanna Bernard Vergouwen, Herman Augustinus De Kock
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Patent number: 7459564Abstract: 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: GrantFiled: January 12, 2006Date of Patent: December 2, 2008Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. Pinto
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Patent number: 7449487Abstract: 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: GrantFiled: July 15, 2003Date of Patent: November 11, 2008Assignee: Laboratoires ExpanscienceInventors: Karim Boumediene, Jean-Pierre Pujol, Georges Bernard Guillou, Philippe Msika, Chafik Ghayor
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Publication number: 20080269271Abstract: 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: ApplicationFiled: May 17, 2006Publication date: October 30, 2008Applicant: Gruenenthal GmbHInventors: Robert Frank, Melanie Reich, Ruth Jostock, Gregor Bahrenberg, Hans Schick, Birgitta Henkel, Helmut Sonnenschein
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Publication number: 20080262055Abstract: 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: ApplicationFiled: April 8, 2008Publication date: October 23, 2008Inventors: Shuhao Shi, Samuel Gerritz, Shirong Zhu
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Publication number: 20080255133Abstract: 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: ApplicationFiled: January 18, 2008Publication date: October 16, 2008Applicant: ARDEA BIOSCIENCES, INC.Inventors: Jean-Michel Vernier, Andreas Maderna, Yung-hyo Koh, Zhi Hong
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Patent number: 7429580Abstract: 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: GrantFiled: January 11, 2005Date of Patent: September 30, 2008Assignees: Orexigen Therapeutics, Inc., Duke UniversityInventors: Kishore M. Gadde, K. Ranga R. Krishnan
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Patent number: 7425571Abstract: 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: GrantFiled: April 23, 2004Date of Patent: September 16, 2008Assignee: Orexigen Therapeutics, Inc.Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
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Publication number: 20080194586Abstract: 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: ApplicationFiled: March 3, 2006Publication date: August 14, 2008Inventors: Harold B. Wood, Peter T. Meinke, Guo Q. Shi, Yong Zhang
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Publication number: 20080188476Abstract: 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: ApplicationFiled: May 5, 2006Publication date: August 7, 2008Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
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Publication number: 20080188510Abstract: The present invention relates to usefulness of zonisamide as a pharmaceutical composition for treating dementia or cognitive impairment.Type: ApplicationFiled: May 23, 2006Publication date: August 7, 2008Applicant: Eisai R & D Management Co., Ltd.Inventor: Hiroshi Yoshino