Plural Ring Chalcogens In The Hetero Ring Patents (Class 514/360)
  • Patent number: 9988395
    Abstract: The present disclosure relates generally to systems, methods, and compounds for therapeutic use against parasitic infections. More particularly, the disclosure relates to anti-parasitic compounds, and methods for making and for using the anti-parasitic compounds, where the anti-parasitic compounds have the general formula: where X, R1, R2, R3, R4, R5, and R6 are defined more fully below.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: June 5, 2018
    Assignee: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Rachid Skouta, Rosa A. Maldonado
  • Patent number: 9943506
    Abstract: The invention provides compositions and methods for blocking the BCL6 BTB domain with small molecule, non-peptide compounds as disclosed and claimed herein. BCL6 is a transcriptional repressor of the BTB-POZ (brie a brae, tramtrack, broad complex/pox virus zincfinger) family of proteins. It is required for normal development of germinal center (GC) B-cells and is also the most commonly involvedoncogene in diffuse large B-celllymphomas (DLBCLs), and constitutive expression of BCL6 in GC B-cells causes DLBCL in mice.
    Type: Grant
    Filed: June 16, 2014
    Date of Patent: April 17, 2018
    Assignees: Cornell University, University of Maryland, Baltimore
    Inventors: Ari Melnick, Leandro Carlos A. Cerchietti, Mariano G. Cardenas, Fengtian Xue, Alexander D. MacKerell
  • Patent number: 8962617
    Abstract: The present invention relates to the use of substituted dihydroimidazolones, particularly [1-(4-Chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazol-2-one] (AWD 131-138) or a physiologically acceptable salt thereof for the treatment of epilepsy in dogs.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Chris Rundfeldt, Rita Dost, Wolfgang Loscher, Andrea Tipold, Klaus Unverferth, Hans-Joachim Lankau
  • Publication number: 20150030539
    Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
    Type: Application
    Filed: July 21, 2014
    Publication date: January 29, 2015
    Applicant: PIRAMAL IMAGING SA
    Inventors: Lutz LEHMANN, Andrea THIELE, Tobias HEINRICH, Thomas BRUMBY, Christer HALLDIN, Balazs GULYAS, Sangram NAG
  • Publication number: 20140378415
    Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20140364461
    Abstract: A method of treating a dermatological disorder in a subject includes the step of administering a therapeutically effective amount of at least one PPAR? agonist or derivative thereof to the subject.
    Type: Application
    Filed: August 4, 2014
    Publication date: December 11, 2014
    Inventor: Pratima Karnik
  • Patent number: 8859540
    Abstract: The present invention relates to the use of substituted dihydroimidazolones, particularly [1-(4-Chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazol-2-one] (AWD 131-138) or a physiologically acceptable salt thereof for the treatment of epilepsy in dogs.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Chris Rundfeldt, Rita Dost, Wolfgang Loscher, Andrea Tipold, Klaus Unverferth, Hans-Joachim Lankau
  • Publication number: 20140296269
    Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II) and pyribencarb: shows an excellent controlling efficacy on plant diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Atsushi Iwata, Makoto Kurahashi
  • Publication number: 20140296254
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Patent number: 8846726
    Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: September 30, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue
  • Patent number: 8841335
    Abstract: Provided is a pharmaceutical composition for inhibiting apoptosis of neurons or neurodegeneration. The pharmaceutical composition effectively prevents or treats diseases related to apoptosis of neurons or neurodegeneration.
    Type: Grant
    Filed: May 3, 2011
    Date of Patent: September 23, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol Hyoung Park, Hye Kyung Min, In Suk Park, Mi Jung Lim, Ji Won Lee, Jin Yong Chung, Yeo Jin Yoon, Joo Young Park
  • Patent number: 8835469
    Abstract: The present invention relates to substituted benzamide derivatives of the Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: September 16, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Rajendra Kharul, Mukul R. Jain, Pankaj R. Patel
  • Patent number: 8785483
    Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for treating COPD.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: July 22, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Satish K. Srivastava, Kota V. Ramana, Umesh Yadav
  • Patent number: 8778979
    Abstract: Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.
    Type: Grant
    Filed: April 5, 2006
    Date of Patent: July 15, 2014
    Assignee: Yale University
    Inventors: Vladimir Coric, John H. Krystal, Gerard Sanacora
  • Patent number: 8735362
    Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: May 27, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Publication number: 20140113884
    Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.
    Type: Application
    Filed: April 4, 2012
    Publication date: April 24, 2014
    Inventors: John David Imig, William B. Campell, John Russell Falck
  • Patent number: 8658650
    Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: February 25, 2014
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
  • Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Patent number: 8618134
    Abstract: A method and composition for treating serotonin receptor-mediated conditions.
    Type: Grant
    Filed: December 13, 2008
    Date of Patent: December 31, 2013
    Assignee: Vanda Pharmaceuticals Inc.
    Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt Wolfgang
  • Patent number: 8618086
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: December 31, 2013
    Assignee: Duke University
    Inventors: Mitchell Anthony deLong, John McMillan McIver, Robert Scott Youngquist
  • Patent number: 8614168
    Abstract: The invention relates to the use of at least one compound, selected from the group consisting of tebuconazole, epoxiconazole, metconazole, cyproconazole, prothioconazole and any mixtures thereof, for increasing the resistance of plants to abiotic stress factors.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: December 24, 2013
    Assignee: Monheim
    Inventors: Jan Dittgen, Isolde Häuser-Hahn, Heinz Kehne, Stefan Lehr, Jörg Tiebes, Marco Busch
  • Patent number: 8592420
    Abstract: Anxiety disorders, such as panic disorder, agoraphobia, obsessive-compulsive disorder, social phobia, post-traumatic stress disorder, generalized anxiety disorder, specific phobia, or the like, are treated by administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof, optionally in combination with an anxiolytic(s) other than the adenosine A2A receptor antagonist.
    Type: Grant
    Filed: April 16, 2012
    Date of Patent: November 26, 2013
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Hiroshi Kase, Naoki Seno, Shizuo Shiozaki, Minoru Kobayashi, Junya Kase
  • Publication number: 20130303525
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: July 19, 2011
    Publication date: November 14, 2013
    Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.
    Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
  • Patent number: 8569346
    Abstract: Compositions and methods for inhibiting BoNT protease activity are presented. In most preferred aspects, inhibitors comprise a thiol reactive group, a zinc binding group, a redox active group, an alkylating group, and/or an electrophilic Michael addition acceptor group. Particularly preferred inhibitors include an isothiazolone ring, a thiadiazolidine dione ring, a (hydro)quinone ring, an iminophenol group, and/or a hydrazonophenol group, and inhibit BoNT/A at ?M and sub-?M concentrations.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: October 29, 2013
    Assignee: Biomadison, Inc.
    Inventors: Füsûn N. Zeytin, Ward Tucker
  • Patent number: 8541466
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: September 24, 2013
    Assignee: Duke University
    Inventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
  • Patent number: 8518978
    Abstract: There is provided a pharmaceutical composition for prevention and treatment of restenosis comprising isoxazole derivatives. The pharmaceutical composition includes a therapeutic effective amount of isoxazole derivatives represented by Formula 1 or pharmaceutically available salts thereof. The pharmaceutical composition may be useful to prevent and treat vascular restenosis since the pharmaceutical composition shows an anti-restenosis activity and accelerates the re-endothelization.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: August 27, 2013
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Sun Gwan Hwang, Sang Rak Choi, Jeong Woo Cho, Sung Jin Bae, Tae Sung Koo, So Young Lee, Kyung Chul Cho, Hyeon Cheol Gwon
  • Publication number: 20130165485
    Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, X, R7, R8, R9, R10 and R11 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: Syngenta Crop Protection LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Godfrey, Thomas Pitterna, Pierre Joseph Jung, Jagadish Pabba
  • Patent number: 8466166
    Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, A and E are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zolli?ger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.
    Type: Grant
    Filed: September 17, 2007
    Date of Patent: June 18, 2013
    Assignee: Raqualia Pharma Inc.
    Inventors: Hiroki Koike, Mikio Morita
  • Patent number: 8399495
    Abstract: Novel metabolites of talarazole of formula (I) have been isolated and characterized, wherein R?H, OH, OSO3H or O-gly; R1, ?H, OH, OSO3H, O-gly or =0; and gly=a glucuronate, or a pharmaceutically acceptable salt thereof. These compounds are targeted for the treatment of various skin-, hair- and nail-associated disorders.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: March 19, 2013
    Assignee: Stiefel Laboratories, Inc.
    Inventor: Debra Barrett
  • Patent number: 8383579
    Abstract: Generally the method involves identifying the concentration of each of two or more active therapeutics tailored to treat a particular patient's unique metabolism and one or more diseases, communicating that information to a producer who has multiple fixed or variable concentrations of each active available, where the producer then combines the individual concentrations of each active into single units such as a tablets or pills, and distributes those indirectly or directly to the patient.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: February 26, 2013
    Assignee: Glaxosmithkline, LLC
    Inventors: Richard L. Kirsh, Steven D. Finkelmeier, Robert Glinecke, Luigi Martini
  • Patent number: 8372870
    Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Grant
    Filed: August 29, 2011
    Date of Patent: February 12, 2013
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue
  • Patent number: 8367645
    Abstract: The invention relates to a composition that includes a first agent selected including an agent that possesses anti-inflammatory activity or acetaminophen, phenacetin, tramadol and the like; a second agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5-monophosphate-activated Protein kinase (AMPK) activator; a third agent that possesses or maintains serotonin activity.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: February 5, 2013
    Inventor: Chien-Hung Chen
  • Patent number: 8338464
    Abstract: Provided are methods of inhibiting BCL6 repression in a mammalian cell. Also provided are methods of treating cancer in a mammal.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: December 25, 2012
    Assignees: Albert Einstein College of Medicine of Yeshiva University, University Health Network, University of Maryland, Baltimore
    Inventors: Ari Matthew Melnick, Alexander D. MacKerell, Jr., Gilbert Gerard Privé
  • Patent number: 8287631
    Abstract: The invention relates to compounds from the groups of (A) electrophiles, (B) nucleophiles, (C) alkylating agents, (D) antioxidants and (E) oxidizing agents as odor preventatives for reducing so-called ghost odor which is induced by 2-methyl-4-isothiazolin-3-one and/or octyl-4-isothiazolin-3-one. The invention further relates to biocide compositions which comprise 2-methyl-4-isothiazolin-3-one and/or octyl-4-isothiazolin-3-one and also one or more odor preventatives, and to the use of odor preventatives for preventing ghost odor.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: October 16, 2012
    Assignee: THOR GmbH
    Inventors: Rudiger Baum, Hans-Jurgen Schmidt, Thomas Wunder, Christos Savides
  • Publication number: 20120238517
    Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: December 1, 2010
    Publication date: September 20, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Publication number: 20120232104
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
  • Patent number: 8247398
    Abstract: The present invention relates to the use of zinc complexes of natural amino acids, especially L-arginine, L-lysine, L-ornithine, and other natural amino acids, in a molar ratio of about 1:2 (metal:amino acid), and formulations thereof. These pharmaceutical compositions offer better tolerated and faster acting regimens than common zinc salts (i.e., acetate, sulfate, etc.) for long term maintenance therapy of diseases caused by abnormal elevated copper levels, such as in Wilson's disease, inflammatory and fibrotic diseases and Alzheimer's disease.
    Type: Grant
    Filed: February 17, 2007
    Date of Patent: August 21, 2012
    Assignee: SSV Therapeutics, Inc.
    Inventor: Om P. Goel
  • Patent number: 8231721
    Abstract: The invention relates to stable antifungal liquid formulations for protecting material, containing 3-iodopropynyl butyl carbamate (IPBC) and n-octylisothiazolinone (n-OIT).
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: July 31, 2012
    Assignee: LANXESS Deutschland GmbH
    Inventors: Hermann Uhr, Tanja Gerharz, Frank Sauer
  • Patent number: 8217063
    Abstract: The present application relates to novel lactam-substituted dicarboxylic acid 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, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 15, 2008
    Date of Patent: July 10, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
  • Patent number: 8193228
    Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: June 5, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Michael M. C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
  • Patent number: 8188124
    Abstract: Novel metabolites of talarazole of formula (I) have been isolated and characterized, wherein R?H, OH, OSO3H or O-gly; R1, ?H, OH, OSO3H, O-gly or =0; and gly=a glucuronate, or a pharmaceutically acceptable salt thereof. These compounds are targeted for the treatment of various skin-, hair- and nail-associated disorders.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: May 29, 2012
    Assignee: Stiefel Laboratories, Inc.
    Inventor: Debra Barrett
  • Patent number: 8183275
    Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: May 22, 2012
    Assignees: Merck Sharp & Dohme Corp., Albany Molecular Research, Inc.
    Inventors: Peter H. Dobbelaar, Christopher L. Franklin, Allan Goodman, Cheng Guo, Peter R. Guzzo, Mark Hadden, Shuwen He, Alan J. Henderson, Tianying Jian, Linus S. Lin, Jian Liu, Ravi P. Nargund, Megan Ruenz, Bruce J. Sargent, Iyassu K. Sebhat, Larry Yet
  • Publication number: 20120115912
    Abstract: A method of treating a PPAR? and/or RXR related disease or disorder in a subject includes adminstering to the subject an RXR agonist alone or in combination with a PPAR? agonist.
    Type: Application
    Filed: July 12, 2010
    Publication date: May 10, 2012
    Inventors: Gary E. Landreth, Paige E. Cramer
  • Patent number: 8153667
    Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: April 10, 2012
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Rabindranath Tripathy
  • Patent number: 8153682
    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 A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: April 10, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Patent number: 8110589
    Abstract: An ectoparasiticide composition for animals including etoxazole as an active ingredient, a UV absorber and a phenol antioxidant, and a method for exterminating ectoparasites using the composition. The preferable blending ratio between etoxazole, a UV absorber and a phenol antioxidant in terms of mass ratio is 1: from 0.05 to 5: from 0.05 to 5.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: February 7, 2012
    Assignee: Kyoyu Agri Co., Ltd.
    Inventors: Yosuke Hashimoto, Yoshiko Tamura, Mamoru Takiuchi, Hidenobu Yanase
  • Publication number: 20110319429
    Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds.
    Type: Application
    Filed: January 28, 2010
    Publication date: December 29, 2011
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Rocco D. Gogliotti, Darren W. Engers
  • Publication number: 20110294780
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Application
    Filed: May 24, 2011
    Publication date: December 1, 2011
    Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
  • Publication number: 20110288136
    Abstract: Disclosed herein are compounds, compositions and methods for treating or ameliorating flavivirus infections. This is particularly important because the present disclosure provides methods for treating flavivirus infections for which there is no effective vaccine.
    Type: Application
    Filed: July 18, 2011
    Publication date: November 24, 2011
    Inventor: Eric Barklis
  • Patent number: 8022032
    Abstract: The method set out herein involves identifying the concentration of each of two or more active therapeutics tailored to treat a particular patient's unique metabolism and one or more diseases, communicating that information to a producer who has multiple fixed or variable concentrations of each active available, where the producer then combines the individual concentrations of each active into single units such as a tablets or pills, and distributes those indirectly or directly to the patient.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: September 20, 2011
    Assignee: SmithKline Beecham Corporation
    Inventors: Richard L. Kirsh, Steven D. Finkelmeier, Robert Glinecke, Luigi Martini