Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/298)
  • Patent number: 8563557
    Abstract: The invention provides a compound according to formula (I): wherein: X is O or S; Y is O or S; each Ar and Ar? is independently a mono-, bi- or tricyclic aryl or heteroaryl group optionally substituted with one or more substituents selected from halo, alkyl, aryl, heteroaryl, hydroxyl, nitro, amino, alkoxy, alkylthio, cyano, thio, ester, acyl and amido; each R2 is independently hydrogen, halo, alkyl, aryl, heteroaryl, hydroxyl, nitro, amino, alkoxy, alkylthio, cyano and thio; and R1 is as defined herein, or a physiologically acceptable salt, solvate, ester, amide or other physiologically functional derivative thereof.
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: October 22, 2013
    Assignees: University Court of the University of Dundee, University Court of the University of St Andrews
    Inventors: Nicholas James Westwood, Sonia Lain, Federico Medda
  • Publication number: 20130271719
    Abstract: To provide a liquid crystal compound having a large positive value of dielectric anisotropy and a small viscosity. The compound is represented by formula (1): wherein, in formula (1), R1 is alkyl having 1 to 20 carbons or the like; ring A1 is 1,4-cyclohexylene or the like; ring A2 is 1,4-phenylene, 2-fluoro-1,4-phenylene, 2,6-difluoro-1,4-phenylene or the like; ring A3 is 1,4-cyclohexylene, 1,4-phenylene, 2-fluoro-1,4-phenylene, 2,6-difluoro-1,4-phenylene or the like; and X1 is halogen, alkyl having 1 to 10 carbons or the like, and in the alkyl, at least one of hydrogen may be replaced by halogen.
    Type: Application
    Filed: April 4, 2013
    Publication date: October 17, 2013
    Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATION
    Inventors: Takahiro KUBO, Yasuyuki GOTOH
  • Publication number: 20130267546
    Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
    Type: Application
    Filed: April 2, 2013
    Publication date: October 10, 2013
    Applicant: Arizona Board of Regents, a body corporate of the State of Arizona acting for and on behalf of Ari
    Inventors: Sidney HECHT, Omar KHDOUR, Jun LU, Pablo ARCE
  • Patent number: 8552002
    Abstract: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
    Type: Grant
    Filed: June 23, 2005
    Date of Patent: October 8, 2013
    Assignees: Novartis AG, IRM LLC
    Inventors: Qiang Ding, Nathanael Schiander Gray, Bing Li, Yi Liu, Taebo Sim, Tetsuo Uno, Guobao Zhang, Carole Pissot Soldermann, Werner Breitenstein, Guido Bold, Giorgio Caravatti, Pascal Furet, Vito Guagnano, Marc Lang, Paul William Manley, Joseph Schoepfer, Carsten Spanka
  • Publication number: 20130252981
    Abstract: A pyrimidine compound of the formula (1): wherein: R1 represents hydrogen, and the like; R2 represents hydrogen, and the like; R3 represents a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like; R4 and R5 are represent a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like; X represents nitrogen, and the like; Y represents nitrogen, and the like; and Z represents oxygen or —NR8— wherein R8 represents a C1-C6 chain hydrocarbon group optionally having one or more halogens, and the like. The compound has a superior activity of controlling pests.
    Type: Application
    Filed: November 30, 2011
    Publication date: September 26, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura
  • Publication number: 20130225617
    Abstract: Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.
    Type: Application
    Filed: January 31, 2013
    Publication date: August 29, 2013
    Applicant: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
    Inventor: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
  • Publication number: 20130225814
    Abstract: Substantially optically pure (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.
    Type: Application
    Filed: June 3, 2011
    Publication date: August 29, 2013
    Applicant: KOWA COMPANY, LTD.
    Inventors: Tadaaki Ohgiya, Takeshi Murakami, Katsutoshi Miyosawa, Kimiyuki Shibuya, Koichi Yamazaki, Taichi Kusakabe
  • Publication number: 20130216498
    Abstract: New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: December 23, 2010
    Publication date: August 22, 2013
    Inventors: Paul Robert Eastwood, Jacob Gonzales Rodriguez, Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Victor Giulio Matassa
  • Publication number: 20130217693
    Abstract: The invention relates to a compound of Formulae I and/or II: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N—OH, NH, NO2, CN, N—CN, N?O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.
    Type: Application
    Filed: April 1, 2011
    Publication date: August 22, 2013
    Inventors: Wayne Danter, Clinton Threlfall, Sylvain Guizzetti, Julien Marin
  • Patent number: 8512820
    Abstract: Ionic mesogenic compounds of formula (I) can be used to form liquid crystal displays, such as ferroelectric liquid crystal displays, having enhanced anti-image sticking properties. The mesogenic compounds may contain a cationic group such as an ammonium or phosphonium group bonded to an alkyl chain that is terminally bonded to a para-substituted pyrimidyl benzene moiety. The counterion can be an organic or inorganic anion. The compounds can be used either as dopants in art ferroelectric liquid crystal compositions to reduce image sticking, or can be used as the primary or predominant component of a liquid crystal display system. Additional compounds, devices, and methods are disclosed.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: August 20, 2013
    Assignee: Citizen Finetech Miyota Co., Ltd.
    Inventors: Yongqiang Zhang, Su Yang
  • Publication number: 20130210721
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
  • Patent number: 8507675
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: August 13, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rajinder Singh
  • Publication number: 20130203749
    Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.
    Type: Application
    Filed: March 10, 2013
    Publication date: August 8, 2013
    Applicants: ABBVIE INC., ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles Hutchins
  • Publication number: 20130202573
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: June 15, 2011
    Publication date: August 8, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
  • Publication number: 20130203727
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).
    Type: Application
    Filed: July 1, 2011
    Publication date: August 8, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
  • Publication number: 20130190320
    Abstract: The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 25, 2013
    Applicant: ACEA BIOSCIENCES, INC.
    Inventor: ACEA Biosciences, Inc.
  • Publication number: 20130190325
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilising or immobilisable derivative thereof; wherein: any one or two of X.
    Type: Application
    Filed: June 21, 2011
    Publication date: July 25, 2013
    Applicant: ITEK VENTURES PTY LTD
    Inventors: Shudong Wang, Osama Chahrour, Tiangong Lu, Anran Hu
  • Publication number: 20130184249
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: February 28, 2013
    Publication date: July 18, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130172316
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8475888
    Abstract: Provided is a liquid crystal compound having general physical properties necessary for a compound, stability to heat, light or the like, a wide liquid crystal phase temperature range, a high clearing point, an excellent compatibility with other liquid crystal compounds, a large refractive index anisotropy and a large dielectric anisotropy. Provided are a liquid crystal composition including the liquid crystal compound, and a liquid crystal display device containing the liquid crystal composition. The compound is represented by formula (1): wherein, for example, R1 is alkyl having 1 to 20 carbons; at least one of the rings A1 to A6 is pyrimidine-2,5-diyl or pyridine-2,5-diyl and the others are 1,4-cyclohexylene or 1,4-phenylene; Z1 to Z6 are a single bond; L1 to L4 is hydrogen or halogen; X1 is hydrogen, halogen, —C?N or alkyl having 1 to 10 carbons; and l, m, n, o, p and q are 0 or 1 and l+m+n+o+p+q=3.
    Type: Grant
    Filed: October 14, 2009
    Date of Patent: July 2, 2013
    Assignees: JNC Corporation, JNC Petrochemical Corporation
    Inventors: Hiroyuki Tanaka, Kouki Sagou
  • Publication number: 20130158004
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Application
    Filed: December 14, 2012
    Publication date: June 20, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Niklas HEINE, Gerald Juergen ROTH
  • Publication number: 20130143905
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Application
    Filed: December 13, 2010
    Publication date: June 6, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Kai Gerlach, Riccardo Giovannini, Christoph Hoenke, Marco Santagostino, Stefan Scheuerer, Thomas Trieselmann
  • Publication number: 20130137671
    Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
    Type: Application
    Filed: May 23, 2012
    Publication date: May 30, 2013
    Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
  • Patent number: 8450327
    Abstract: The present invention relates to novel CGRP antagonists of the general formula (I) in which U, V, X, Y, R1, R2, R3 are defined as described below, the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof, and the hydrates of the salts, particularly the physiologically compatible salts thereof having inorganic or organic acids or bases, pharmaceuticals comprising said compounds, the use thereof, and the method for the production thereof.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: May 28, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
  • Publication number: 20130123284
    Abstract: Provided herein are compounds useful for kinase inhibition.
    Type: Application
    Filed: March 24, 2011
    Publication date: May 16, 2013
    Applicant: AMITECH THERAPEUTIC SOLUTIONS INC
    Inventors: Lee Daniel Arnold, Eric A. Murphy
  • Patent number: 8431697
    Abstract: The present invention provides triallyl isocyanurate comprising a less amount of corrosive substances by identifying the corrosive substances among impurities included in the triallyl isocyanurate. Triallyl isocyanurate of the present invention comprises an organic chlorine compound represented by the following general formula (I) in an amount of not more than 100 ppm: wherein R1 and R2 are respectively a chlorine atom or an allyoxy group with the proviso that at least one of R1 and R2 is a chlorine atom.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: April 30, 2013
    Assignee: Nippon Kasei Chemical Company Limited
    Inventor: Mabuko Yamaura
  • Patent number: 8425990
    Abstract: A liquid crystalline compound shown by the following formula (I). wherein R1 to R13 represent a hydrogen atom, a fluorine atom, a methyl group, a trifluoromethoxy group, or a cyano group, X represents —O—, —O—CO—, or the like, n is 0 or 1, and R14 represents -A-CO—CH?CH2, wherein A is a linking group. The liquid crystalline compound has a higher liquid crystal phase upper limit temperature, is chemically stable, can be inexpensively produced, and exhibits a large selective reflection wavelength zone ?? (a large ?n). A liquid crystalline composition comprising the liquid crystalline compounds, an optical film having a liquid crystal layer formed using the liquid crystalline composition, and an optical laminate comprising a substrate, an alignment film formed on the substrate, a liquid crystal layer formed using the liquid crystalline composition on the alignment film are also disclosed.
    Type: Grant
    Filed: February 21, 2008
    Date of Patent: April 23, 2013
    Assignee: Zeon Corporation
    Inventors: Seiji Okada, Kentarou Tamura
  • Patent number: 8426426
    Abstract: The present invention relates to compounds which inhibit bacterial gyrase and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals. The present invention also relates to a method for preparing these compounds.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: April 23, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul Charifson, David Deininger, Joseph Drumm, Anne-Laure Grillot, Yusheng Liao, Patricia Oliver-Shaffer, Dean Stamos
  • Publication number: 20130096118
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.
    Type: Application
    Filed: June 16, 2011
    Publication date: April 18, 2013
    Inventors: Chunjian Liu, James Lin, George V. DeLucca, Batt G. Douglas, Qingjie Liu
  • Patent number: 8410122
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: April 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew Stamford, Hong Liu
  • Patent number: 8404685
    Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4 and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: March 26, 2013
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Patent number: 8399436
    Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: March 19, 2013
    Assignee: Glaxo Group Limited
    Inventors: David George Allen, Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Steven Leslie Sollis, Sadie Vile, Caroline Wilson
  • Publication number: 20130065906
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: March 13, 2012
    Publication date: March 14, 2013
    Applicants: NEUROCRINE BIOSCIENCES, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Bernd NOSSE, Andreas BLUM, Steffen BREITFELDER, Armin HECKEL, Frank HIMMELSBACH, Elke LANGKOPF, Bernd WELLENZOHN, Neil J. ASHWEEK, Nicole HARRIOTT
  • Publication number: 20130059871
    Abstract: The present invention provides (I) these compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes.
    Type: Application
    Filed: April 30, 2012
    Publication date: March 7, 2013
    Inventors: David Christopher HORWELL, David Ian Carter SCOPES
  • Publication number: 20130045955
    Abstract: The present invention provides compounds of formula (I) herein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: August 16, 2012
    Publication date: February 21, 2013
    Inventors: Nicholas J. Bennett, Thomas MCINALLY, Tobias MOCHEL, Stephen Thom, Anna-Karin Tidén
  • Patent number: 8372848
    Abstract: This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).
    Type: Grant
    Filed: March 23, 2005
    Date of Patent: February 12, 2013
    Assignees: Mixture Sciences, Inc., The Regents of the University of California
    Inventors: Richard A. Houghten, Colette Dooley, Adel Nefzi, Zhiwei Wang, Oliver Civelli, Hiroshi Nagasaki
  • Patent number: 8354535
    Abstract: The invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical composition for use, e.g., in treatment of airway disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: January 15, 2013
    Assignee: Nycomed GmbH
    Inventors: Ulrich Kautz, Matthias Webel, Christian Scheufler, Rolf-Peter Hummel
  • Publication number: 20130012390
    Abstract: The present invention relates to novel heterocyclic alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: Beyer Intellectual Property GmbH
    Inventors: Carl Friedrich NISING, Pierre CRISTAU, Hendrik HELMKE, Gorka PERIS, Tomoki TSUCHIYA, Pierre WASNAIRE
  • Publication number: 20130005752
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: June 19, 2012
    Publication date: January 3, 2013
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
  • Publication number: 20120329788
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: June 19, 2012
    Publication date: December 27, 2012
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
  • Publication number: 20120321563
    Abstract: The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.
    Type: Application
    Filed: May 9, 2012
    Publication date: December 20, 2012
    Inventors: Kevin Groves, Bagna Bao
  • Publication number: 20120322784
    Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: December 16, 2011
    Publication date: December 20, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
  • Publication number: 20120322785
    Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
    Type: Application
    Filed: December 14, 2011
    Publication date: December 20, 2012
    Applicant: Genentech, Inc.
    Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel Kintz, Hans Edward Purkey
  • Patent number: 8329390
    Abstract: The present invention relates generally to the detection and measurement of transmembrane potentials using an N,N,N?-trialkyl thiobarbituric acid-derived polymethine oxonol (shown below). In particular, the present invention is directed to compositions and optical methods for determining transmembrane potentials across the plasma membrane of biological cells using a slightly hydrophobic N,N,N?-trialkyl thiobarbituric acid-derived polymethine oxonols. The method comprises a slightly hydrophobic N,N,N?-trialkyl thiobarbituric acid-derived polymethine oxonol anion capable of redistributing from a first face of the membrane to a second face of the membrane in response to changes in the potential of the membrane. In one aspect the method is used to identify compounds which modulate membrane potentials in biological membranes.
    Type: Grant
    Filed: August 25, 2005
    Date of Patent: December 11, 2012
    Assignee: AnaSpec Incorporated
    Inventors: Zhenjun Diwu, Jianjun He, Yi Tang
  • Publication number: 20120287354
    Abstract: The present invention relates to an electro-optical light modulation element and to electro-optical displays and display systems, such as television screens and computer monitors, containing elements of this type. The light modulation elements according to the invention contain a mesogenic modulation medium which is in the isotropic phase during operation of the light modulation elements and are particularly distinguished by very short response times in addition to good contrast and low viewing-angle dependence. The mesogenic modulation media used in the electro-optical light modulation elements are likewise a subject-matter of the present invention.
    Type: Application
    Filed: June 7, 2012
    Publication date: November 15, 2012
    Applicant: MERCK Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Michael HECKMEIER, Achim Götz
  • Publication number: 20120288492
    Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
    Type: Application
    Filed: December 27, 2010
    Publication date: November 15, 2012
    Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Mann-Yan Kuo, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
  • Patent number: 8309556
    Abstract: The invention relates to the use of compounds derived from pyrimidinetrione of general formula (I) as acetyl cholinesterase (AChE) inhibitors. The invention also relates to the use of said compounds as insecticides, and to compositions containing the same.
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: November 13, 2012
    Assignees: Centre National de la Recherche Scientifique, Universite de Montpellier 2
    Inventors: Mylene Weill, Philippe Fort, Jean-Paul Leonetti
  • Patent number: 8304547
    Abstract: [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: November 6, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Nomura, Shunichiro Matsumoto, Takashi Shin, Hidenori Azami, Tomoaki Abe, Akira Suga, Ryushi Seo, Masayuki Tanahashi, Toru Watanabe
  • Patent number: 8293729
    Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.
    Type: Grant
    Filed: June 23, 2010
    Date of Patent: October 23, 2012
    Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences Inc.
    Inventors: Brian Dyck, Joe A. Tran, Junko Tamiya, Florence Jovic, Troy Vickers, Chen Chen, Nicole Harriott, Timothy Coon, Neil J. Ashweek
  • Publication number: 20120263659
    Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 18, 2012
    Applicants: BASF SE, SYMRISE AG
    Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel