1,2-diazoles (including Hydrogenated) Patents (Class 546/275.4)
Polycyclo ring system having the 1,2-diazole ring as one of the cyclos (Class 546/275.7)
Chalcogen attached directly to the 1,2-diazole ring by nonionic bonding (Class 546/276.1)
  • Anthranilamide Compounds and their use as Pesticides
    Publication number: 20140200134
    Abstract: The present invention relates to anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: July 17, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Prashant Deshmukh, Karsten Koerber, Wolfgang Von Deyn, Markus Kordes, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Carbamoylmethoxy- and carbamoylmethylthio- and carbamoylmethylamino benzamides for combating invertebrate pests
    Publication number: 20140200135
    Abstract: The present invention relates to substituted carbamoylmethoxy and carbamoylmethylthio benzamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the carbamoylmethoxy- and carbamoylmethylthio-benzamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 17, 2012
    Publication date: July 17, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Prashant Deshmukh, Karsten Köerber, Wolfgang Von Deyn, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Deborah L. Culbertson, Douglas D. Anspaugh
  • Trisubstituted pyrazoles as acetylcholine receptor modulators
    Patent number: 8779158
    Abstract: The present invention relates to 1-alkyl-3-aniline-5-aryl-pyrazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
    Type: Grant
    Filed: May 8, 2009
    Date of Patent: July 15, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Wei Zhuang
  • Pyridinonyl PDK1 inhibitors
    Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
  • Substituted heteroaryl inhibitors of B-RAF
    Patent number: 8778929
    Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: July 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
  • Pyrazolyl-Based Carboxamides I
    Publication number: 20140194443
    Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
  • PROCESS FOR PREPARING TETRAZOLE-SUBSTITUTED ANTHRANILIC ACID DIAMIDE DERIVATIVES BY REACTING BENZOXAZINONES WITH AMINES
    Publication number: 20140194623
    Abstract: The present invention relates to a process for preparing tetrazole-substituted anthranilic acid diamide derivatives of the formula (I) in which R1, R2, R3, R4, Q and Z have the meanings given in the description, by reacting benzoxazinones with amines.
    Type: Application
    Filed: August 24, 2012
    Publication date: July 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Sergii Pazenok, Werner Lindner, Hartmut Scheffel
  • Pyrazolyl-Based Carboxamides II
    Publication number: 20140194452
    Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
  • SUBSTITUTED 1-BENZYLINDOLIN-2-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF MUSCARINIC ACETYLCHOLINE M1 RECEPTORS
    Publication number: 20140194471
    Abstract: In one aspect, the invention relates to substituted 1-benzylindolin-2-one analog compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 6, 2013
    Publication date: July 10, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindlsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney
  • HETEROARYLMETHYL AMIDES
    Publication number: 20140194436
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Application
    Filed: February 24, 2014
    Publication date: July 10, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
  • N-Thio-anthranilamid compounds and their use as pesticides
    Patent number: 8772289
    Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is A1 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: July 8, 2014
    Assignee: BASF SE
    Inventors: Thomas Schmidt, Michael Puhl, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Toni Bucci, Henry Van Tuyl Cotter, David G. Kuhn, Hassan Oloumi-Sadeghi
  • Fungicide pyrazole carboxamides derivates
    Patent number: 8772266
    Abstract: The present invention relates to pyrazole carboxamides derivatives of formula (1) wherein Y represents CR5 or N, T represents S or O, X1 and X2 represent a chlorine or a fluorine atom, and Z1 represents a substituted or non-substituted cyclopropyl; Their process of preparation, their use as fungicide, and/or anti-mycotoxin active agents, and/or insecticide, and/or nematicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: July 8, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Guenter Bartels, Angela Becker, Jurgen Benting, Christoph-Andreas Braun, Peter Dahmen, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Ulrich Gorgens, Hiroyuki Hadano, Benoit Hartmann, Thomas Knobloch, Marc Kosten, Norbert Lui, Ruth Meissner, Sergiy Pazenok, Rachel Rama, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Inhibitors of hepatitis C virus polymerase
    Patent number: 8771665
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 8, 2014
    Assignee: Cocrystal Discovery, Inc.
    Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • N-THIO-ANTHRANILAMIDE COMPOUNDS AND THEIR USE AS PESTICIDES
    Publication number: 20140179519
    Abstract: The present invention relates to N-thio-anthranilamide compounds of the formula (I), the stereoisomers, the salts, the tautomers and the N-oxides thereof, wherein R1 is halogen, methyl or halomethyl, R2 is hydrogen, halogen or cyano; R3 is hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, C2-C6-alkenyl or the like; R4 is halogen; R5 and R6 independently of each other are optionally substituted C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl, or together represent an (hetero)aliphatic chain, or the like; and k is 0 or 1.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 26, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Karsten Körber, Prashant Deshmukh, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV
    Publication number: 20140179702
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.
    Type: Application
    Filed: October 15, 2013
    Publication date: June 26, 2014
    Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
  • Substituted bicyclic amines for the treatment of diabetes
    Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • PYRAZOLYL SUBSTITUTED CARBONIC ACID DERIVATIVES AS MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    Publication number: 20140171469
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: June 19, 2014
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
    Publication number: 20140163009
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Application
    Filed: January 23, 2012
    Publication date: June 12, 2014
    Applicant: CHDI Foundation
    Inventors: Christopher A Luckhurst, Alen F Haughan, Perla Breccia, Andrew J Stott, Roland W Burli, Samantha J Hughes, Ignacio Munoz-Sanjuan, Celia Dominguez
  • SUBSTITUTED PYRAZOLES AS N-TYPE CALCIUM CHANNEL BLOCKERS
    Publication number: 20140163031
    Abstract: The present invention relates to compounds of Formula (I), wherein X1, X2, X3, X4, R1, R2, R3, and Q are as defined herein, useful as N-type calcium channel blockers.
    Type: Application
    Filed: August 16, 2013
    Publication date: June 12, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark Wall, Nalin Subasinghe, Zhihua Sui
  • N-Thio-Anthranilamide Compounds and Their Use as Pesticides
    Publication number: 20140162875
    Abstract: The present invention relates to N-thio-anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the N-thio-anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 12, 2014
    Applicant: BASF SE
    Inventors: Prashant Deshmukh, Karsten Körber, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Markus Kordes, Florian Kaiser, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
    Publication number: 20140162874
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Maurice C. Yap, Ann M. Buysse, Daniel Knueppel, Yu Zhang, Negar Garizi, Noormohamed M. Niyaz, Christian T. Lowe, Ricky Hunter, Tony K. Trullinger, David A. Demeter, Dan Pernich, Carl DeAmicis, Ronald Ross, JR., Timothy C. Johnson
  • sGC stimulators
    Patent number: 8748442
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: June 10, 2014
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R Iyengar, Ara Mermerian, Angelika Fretzen
  • Microbicidal heterocycles
    Patent number: 8748431
    Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Syngenta Participations AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
  • Metalloenzyme inhibitor compounds
    Patent number: 8748461
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: June 10, 2014
    Assignee: 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
  • N-Thio-Anthranilamide Compounds and Their Use as Pesticides
    Publication number: 20140155264
    Abstract: The present invention relates to N-thio-anthranilamide compounds of the formula (I), the stereoisomers, the salts, the tautomers and the N-oxides thereof, wherein R1 is halogen or halomethyl; R2 is hydrogen, halogen or cyano; R3 is hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, C2-C6-alkenyl or the like; R4 is halogen; R5 and R6 independently of each other are optionally substituted C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl, or together represent an (hetero)aliphatic chain, or the like; k is 0 or 1.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 5, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Karsten Körber, Prashant Deshmukh, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK
    Publication number: 20140155410
    Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.
    Type: Application
    Filed: February 6, 2014
    Publication date: June 5, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Jerry Leroy Adams, Thomas H. Faitg, Neil W. Johnson, Jiri Kasparec, Hong Lin, Mark Mellinger, Xin Peng, Ren Xie
  • Pyruvate kinase M2 modulators, therapeutic compositions and related methods of use
    Patent number: 8742119
    Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: June 3, 2014
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Compounds
    Patent number: 8741892
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    Publication number: 20140148461
    Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: November 22, 2013
    Publication date: May 29, 2014
    Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS
  • FUNGICIDE PYRAZOLE CARBOXAMIDES DERIVATIVES
    Publication number: 20140148411
    Abstract: The present invention relates to pyrazole carboxamides derivatives of formula (1) wherein Y represents CR5 or N, T represents S or O, X1 and X2 represent a chlorine or a fluorine atom, and Z1 represents a substituted or non-substituted cyclopropyl; Their process of preparation, their use as fungicide, and/or anti-mycotoxin active agents, and/or insecticide, and/or nematicide, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: January 28, 2014
    Publication date: May 29, 2014
    Inventors: Guenter BARTELS, Angela BECKER, Juergen BENTING, Christoph-Andreas BRAUN, Peter DAHMEN, Philippe DESBORDES, Christophe DUBOST, Stephanie GARY, Ulrich GORGENS, Hiroyuki HADANO, Beniot HARTMANN, Thomas KNOBLOCH, Marc KOSTEN, Norbert LUI, Ruth MEISSNER, Sergiy PAZENOK, Rachel RAMA, Arnd VOERSTE, Ulrike WACHENDORFF-NEUMANN
  • Substituted Phenylureas and Phenylamides as Vanilloid Receptor Ligands
    Publication number: 20140142143
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: May 22, 2014
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Novel Heterocyclic Compounds as Pesticides
    Publication number: 20140135346
    Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to the use thereof for controlling animal pests, in particular arthropods and especially insects.
    Type: Application
    Filed: January 16, 2014
    Publication date: May 15, 2014
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Adeline KÖHLER, Reiner FISCHER, Martin FÜßLEIN, Peter JESCHKE, Joachim KLUTH, Friedrich August MÜHLTHAU, Arnd VOERSTE, Olga MALSAM, Ulrich GÖRGENS, Yoshitaka SATO
  • Mineralocorticoid receptor antagonists
    Patent number: 8722709
    Abstract: Mineralocorticoid receptor antagonists, of which the following is exemplary.
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: May 13, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Xin Guo, Stephen J. Boyer, Di Wu, Frank Wu
  • Sulfonylpyrazole and sulfonylpyrazoline carboxamidine derivatives as 5-HTantagonists
    Patent number: 8722887
    Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: May 13, 2014
    Assignee: Abbvie Bahamas, Ltd.
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • MICROBIOCIDAL HETEROCYCLES
    Publication number: 20140128406
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Application
    Filed: June 27, 2012
    Publication date: May 8, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
  • N-Link Hydroxamic Acid Derivatives Useful As Antibacterial Agents
    Publication number: 20140128363
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Pyrazole synthesis by coupling of carboxylic acid derivatives and enamines
    Patent number: 8716485
    Abstract: The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: May 6, 2014
    Assignee: Westfälishe Wilhelms-Universität Münster
    Inventors: Julia Neumann, Mamta Suri, Frank Glorius
  • Liquid formulations of carboxamide arthropodicides
    Patent number: 8709513
    Abstract: Disclosed are suspension concentrate compositions comprising by weight based on the total weight of the composition, (a) from about 0.1 to about 50% of one or more carboxamide arthropodicides that are solid at room temperature; ( b) from 0 to about 50% of one or more biologically active agents other than the carboxamide arthropodicides; (c) from about 20 to about 70% of water; (d) from about 10 to about 70% of one or more water-immiscible liquid compounds; and (e) from about 1 to about 55% of a surfactant component having a dispersing property. This invention also relates to a method for controlling an arthropod pest comprising diluting said suspension concentrate composition with water, optionally adding an adjuvant to form a diluted composition, and contacting the arthropod pest or its environment with an effective amount of said diluted composition.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: April 29, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Oliver Walter Gutsche, Isaac Billy Annan, Hector Eduardo Portillo
  • PYRIDYLAMINOACETIC ACID COMPOUND
    Publication number: 20140113907
    Abstract: The present invention provides a pyridylaminoacetic acid compound represented by the following formula (1): (wherein R1, R2, R3, Y and Z are as defined in the description and claims), or a pharmacologically acceptable salt thereof. Since the pyridylaminoacetic acid compound has EP2 agonistic action, it is useful as a therapeutic or prophylactic drug for respiratory diseases such as asthma or chronic obstructive pulmonary disease.
    Type: Application
    Filed: December 16, 2013
    Publication date: April 24, 2014
    Applicant: UBE INDUSTRIES, LTD.
    Inventors: Ryo IWAMURA, Masayuki TANAKA, Tetsushi KATSUBE, Manabu SHIGETOMI, Eiji OKANARI, Yasunori TOKUNAGA, Hiroshi FUJIWARA
  • SUBSTITUTED PICOLINAMIDE KINASE INHIBITORS
    Publication number: 20140113931
    Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 24, 2014
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • P38 MAP KINASE INHIBITORS
    Publication number: 20140114064
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
    Type: Application
    Filed: December 24, 2013
    Publication date: April 24, 2014
    Applicant: Respivert Ltd.
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
  • PYRAZOLE DERIVATIVES AS CANNABINOID RECEPTOR 1 ANTAGONISTS
    Publication number: 20140107157
    Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 17, 2014
    Applicant: Research Triangle Institute
    Inventors: Alan Bradley Fulp, Rangan Maitra, Yanan Zhang, Herbert H. Seltzman
  • ANTI-FIBROTIC PYRIDINONES
    Publication number: 20140107110
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 17, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Benzamides
    Publication number: 20140107340
    Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
  • PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK
    Publication number: 20140107131
    Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 17, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Jerry Leroy ADAMS, Thomas H. FAITG, Neil W. JOHNSON, Jiri KASPAREC, Hong LIN, Mark MELLINGER, Xin PENG, Ren XIE
  • Isoindolone M1 receptor positive allosteric modulators
    Patent number: 8697690
    Abstract: The present invention is directed to isoindolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: June 27, 2011
    Date of Patent: April 15, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Scott D. Kuduk, Youheng Shu, Zhi-Qiang Yang
  • PYRROLIDINONE DERIVATIVES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
    Publication number: 20140099333
    Abstract: The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 8, 2013
    Publication date: April 10, 2014
    Applicant: SANOFI
    Inventors: Lothar SCHWINK, Martin BOSSART, Heiner GLOMBIK, Matthias GOSSEL, Dieter KADEREIT, Thomas KLABUNDE, Thomas MAIER, Siegfried STENGELIN
  • ANTI-FIBROTIC PYRIDINONES
    Publication number: 20140094456
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 3, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Heterocyclic compounds as pesticides
    Patent number: 8685964
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: April 1, 2014
    Assignee: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Martin Füβlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
  • Thienylpyri(mi)dinylazole
    Patent number: 8685974
    Abstract: Thienylpyri(mi)dinylazole of the formula (I) in which R1 to R8 and X1 have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: April 1, 2014
    Assignee: Bayer CropScience AG
    Inventors: Alexander Sudau, Mazen Es-Sayed, Julia Neumann, Catherine Sirven, Jürgen Benting, Christoph Andreas Braun, Ruth Meissner, Anne-Sophie Rebstock, Samir Bennabi, Philippe Desbordes, Arounarith Tuch, Philippe Rinolfi, Stephane Brunet, Hiroyuki Hadano, Marie-Claire Grosjean-Cournoyer