1,4-diazines Patents (Class 544/336)
  • Patent number: 10519121
    Abstract: Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is disclosed. A novel crystalline form of vortioxetine hydrobromide propylene glycol solvate, designated form AC1, is disclosed along with a method for making same. Form AC1 may be characterized by an x-ray powder diffraction pattern with peaks at about 19.64, 22.85, 25.51, 29.57, 30.18±0.2 degrees 2-theta.
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: December 31, 2019
    Assignee: Apicore US LLC
    Inventors: Ravishanker Kovi, Jayaraman Rao Kannapan, Ananda Babu Thirunavakarasu, Veerabhadra Rao Bobbili, Gaurav Yadav
  • Patent number: 10512637
    Abstract: The invention surprisingly found that agents that inhibit system xc? provide the therapeutic intervention in substance-related and addictive disorders and the treatment and/or prevention in substance-mediated brain damage and confirms that system xc? is a promising therapeutic target for substance-induced addiction and brain damage.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: December 24, 2019
    Assignee: CHINA MEDICAL UNIVERSITY
    Inventor: Chia-Hung Hsieh
  • Patent number: 10040771
    Abstract: The present invention relates to preparation methods of a prostacyclin receptor agonist of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide and its intermediates. These methods are simple and convenient to operate, environment-friendly and suitable for industrial production to obtain the product with good yield and high purity.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: August 7, 2018
    Assignee: SEASONS BIOTECHNOLOGY (TAIZHOU) CO., LTD.
    Inventors: Fanghui Tang, Chi Ma, Qiang Jia
  • Patent number: 10022371
    Abstract: The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: July 17, 2018
    Assignee: The Board of Trustees of the University of Illinois
    Inventor: Paul J. Hergenrother
  • Patent number: 9504683
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: November 29, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • Patent number: 9458115
    Abstract: A method for synthesizing a pyrazine-containing material according to one embodiment includes contacting an iminodiacetonitrile derivative with a base and a reagent selected from a group consisting of hydroxylamine, a hydroxylamine salt, an aliphatic primary amine, a secondary amine, an aryl-substituted alkylamine a heteroaryl-substituted alkyl amine, an alcohol, an alkanolamine and an aryl alcoholamine. Additional methods and several reaction products are presented.
    Type: Grant
    Filed: April 20, 2009
    Date of Patent: October 4, 2016
    Assignee: Lawrence Livermore National Security, LLC
    Inventors: Philip F. Pagoria, Mao Xi Zhang
  • Patent number: 9371521
    Abstract: Substituted dithiol pyrazine compounds useful as reducing agents in biologically relevant media having formula: where variables are defined herein and corresponding oxidized pyrazine dithianes. Reducing agents useful to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins, and other biological molecules. Reducing agents useful to regulate protein function in proteins in which a sulfhydryl group is associated with biological activity. Reducing agents useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. S-acylated dithiol pyrazine compounds, where R3 is an acyl group, are selectively activated as reducing agents by removal of the S-acyl groups enzymatically or chemically. Dithiol pyrazine reducing agents and corresponding S-acylated dithiol pyrazines, immobilized on surfaces or conjugated to other chemical species, are provided.
    Type: Grant
    Filed: June 30, 2014
    Date of Patent: June 21, 2016
    Assignee: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Ronald Thaddeus Raines, John C. Lukesh, III
  • Patent number: 9346767
    Abstract: Described include (1) a substituted pyrazine compound of general formula (VIII): and (2) a process for producing the substituted pyrazine compound of general formula (VIII), where R1 is hydrogen, a halogen, a substituted or unsubstituted hydrocarbon group, or a substituted or unsubstituted heterocyclic group, and R4 is a protecting group. The process comprises (1) the step of reacting 2-amino-3,5-dibromo-6-chloropyrazine with R1MgX and ZnCl2 in the presence of a palladium catalyst to produce a compound of general formula (V); (2) the step of reacting the compound of general formula (V) with a compound of general formula (VI) to produce a compound of general formula (VII); and (3) the step of reacting the compound of formula (VII) with tributyl(vinyl)tin in the presence or a palladium catalyst to given the compound of general formula (VIII).
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: May 24, 2016
    Assignees: JNC CORPORATION, NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY
    Inventors: Satoshi Inouye, Yuiko Miura, Suguru Yoshida, Takamitsu Hosoya
  • Patent number: 9075058
    Abstract: Coelenterazine analogs with different luminescence properties from conventional ones and coelenteramide analogs with different fluorescence properties from conventional ones have been desired. The invention provides coelenterazine analogs modified at the 8-position of coelenterazine and coelenteramide analogs modified at the 2- or 3-position of coelenteramide.
    Type: Grant
    Filed: January 30, 2015
    Date of Patent: July 7, 2015
    Assignees: JNC CORPORATION, NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY
    Inventors: Satoshi Inouye, Yuiko Sahara, Takamitsu Hosoya
  • Patent number: 9056840
    Abstract: Coelenterazine analogs with different luminescence properties from conventional ones and coelenteramide analogs with different fluorescence properties from conventional ones have been desired. The invention provides coelenterazine analogs modified at the 8-position of coelenterazine and coelenteramide analogs modified at the 2- or 3-position of coelenteramide.
    Type: Grant
    Filed: July 7, 2014
    Date of Patent: June 16, 2015
    Assignees: JNC CORPORATION, NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY
    Inventors: Satoshi Inouye, Yuiko Sahara, Takamitsu Hosoya
  • Publication number: 20150141427
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150126490
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
  • Publication number: 20150119575
    Abstract: A simple process for producing ?-coelenterazine compounds has been desired. The invention provides a process for producing a ?-coelenterazine compound represented by general formula (II) which comprises (1) the step of reacting a compound represented by general formula (VIII) with a methyltriphenylphosphonium salt in the presence of a base to give a compound represented by general formula (IX), (2) the step of performing a ring-closing metathesis reaction on any one selected from the group consisting of the compound represented by general formula (IX) and a compound represented by general formula (X) which is the compound represented by general formula (IX) wherein the amino is protected with R5, and then deprotecting R4 and, if any, R5 to give a ?-coelenteramine compound represented by general formula (XIV), and (3) the step of reacting the compound represented by general formula (XIV) with a compound represented by general formula (XV) to give the compound represented by general formula (II).
    Type: Application
    Filed: January 8, 2015
    Publication date: April 30, 2015
    Inventors: SATOSHI INOUYE, YUIKO MIURA, SUGURU YOSHIDA, TAKAMITSU HOSOYA
  • Publication number: 20150112065
    Abstract: It is an object to provide a novel material having a bipolar property, a light emitting element provided with the novel material, and a display device that includes the light emitting element. It is an object to provide a pyrazine derivative represented by the following general formula (g-1).
    Type: Application
    Filed: December 29, 2014
    Publication date: April 23, 2015
    Inventors: Hiroko Murata, Masakazu EGAWA, Harue NAKASHIMA, Sachiko KAWAKAMI, Nobuharu OHSAWA, Satoshi SEO
  • Patent number: 9012637
    Abstract: Disclosed herein are substituted pyrazinyl acrylic acids of Formula (IV): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: April 28, 2014
    Date of Patent: April 21, 2015
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Patent number: 9006269
    Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: April 14, 2015
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
  • Publication number: 20150080408
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 19, 2015
    Applicant: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Patent number: 8969553
    Abstract: Process for the selective N-sulfonylation of oxindoles, in particular process for the N-sulfonylation of 3-triazinyloxindoles, and also N-sulfonyl-substituted 3-triazinyloxindoles and the use of N-sulfonyl-substituted oxindoles and of N-sulfonyl-substituted 3-triazinyloxindoles as intermediates for the synthesis of fine chemicals and of active ingredients in the field of pharmacy and agriculture, and also the use of these compounds as active ingredients in the field of agriculture.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: March 3, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Gunter Karig, Mark James Ford, Konrad Siegel, Stefan Schnatterer
  • Patent number: 8969356
    Abstract: The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: March 3, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Joanne Pinder, Stephen Young, Philip Michael Reaper
  • Patent number: 8969351
    Abstract: A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively.
    Type: Grant
    Filed: November 17, 2011
    Date of Patent: March 3, 2015
    Assignee: Novartis AG
    Inventors: Joerg Berghausen, Haixia Ren
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150057278
    Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.
    Type: Application
    Filed: September 10, 2012
    Publication date: February 26, 2015
    Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
  • Patent number: 8952010
    Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R represents a hydrogen atom, a hydroxy group, or a halogen atom Ar1 represents a bicyclic heterocyclic group represented by the following formula: ?and Ar2 represents a bicyclic heterocyclic group represented by the following formulae:
    Type: Grant
    Filed: February 6, 2012
    Date of Patent: February 10, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hiroaki Inagaki, Tetsunori Fujisawa, Masao Itoh, Aki Yokomizo, Toshifumi Tsuda, Saito Higuchi, Biswajit Das, Rita Katoch, Dilip J. Upadhyay
  • Patent number: 8946413
    Abstract: There is provided a compound of Formula I(a) or I(b): or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 3, 2015
    Assignee: Pfizer Inc.
    Inventors: Robert O. Hughes, Rajesh V. Devraj, Donald J. Rogier, John I. Trujillo, Steve R. Turner, Wei Huang
  • Patent number: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • Publication number: 20150031682
    Abstract: The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 29, 2015
    Inventors: Yassir Younis, Kelly Chibale, Michael John Witty, David Waterson
  • Publication number: 20150031627
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Jeremy Travins, Zhenwei Cai, Dawei Cui, Ding Zhou
  • Patent number: 8921373
    Abstract: The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: December 30, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventor: Noriyuki Kurose
  • Patent number: 8916705
    Abstract: The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: December 23, 2014
    Assignee: The Board of Trustees of the University of Illilnois
    Inventor: Paul J. Hergenrother
  • Publication number: 20140371073
    Abstract: The present invention relates to novel non-steroidal brassinosteroid mimetic derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.
    Type: Application
    Filed: September 11, 2012
    Publication date: December 18, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph Marcel Jung, Joerg Leipner, Mathilde Denise Lachia, Alain De Mesmaeker
  • Publication number: 20140356430
    Abstract: Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.
    Type: Application
    Filed: May 28, 2014
    Publication date: December 4, 2014
    Applicant: Signal Pharmaceuticals, LLC
    Inventors: Marie Georges BEAUCHAMPS, Antonio Christian FERRETTI, Juan Antonio GAMBOA, Kevin KLOPFER, William Edward KONNECKE, Matthew Michael KREILEIN, Anil MENON, Amanda Nicole MIKLOS, John Fitzgerald TRAVERSE
  • Patent number: 8901119
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: December 2, 2014
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • Publication number: 20140350030
    Abstract: The present invention provides compounds of formula (I): where R1, R2, X, Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.
    Type: Application
    Filed: September 17, 2012
    Publication date: November 27, 2014
    Inventors: Dario Doller, Guiying Li
  • Patent number: 8883432
    Abstract: Coelenterazine analogs with different luminescence properties from conventional ones and coelenteramide analogs with different fluorescence properties from conventional ones have been desired. The invention provides coelenterazine analogs modified at the 8-position of coelenterazine and coelenteramide analogs modified at the 2- or 3-position of coelenteramide.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: November 11, 2014
    Assignees: JNC Corporation, National University Corporation Tokyo Medical and Dental University
    Inventors: Satoshi Inouye, Yuiko Sahara, Takamitsu Hosoya
  • Patent number: 8883786
    Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch
  • Publication number: 20140323484
    Abstract: The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer. The compounds have the general formula (1): and salts, N-oxides and tautomers thereof, wherein m is 2, 3 or 4; n is 0 or 1; Q1 is selected from a bond; C(?O); S(O); SO2; and an alkylene chain of 1 to 4 carbon atoms in length between the moiety R4 and the nitrogen atom.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 30, 2014
    Inventors: Robert George Boyle, Richard Justin Boyce
  • Patent number: 8871931
    Abstract: A process for producing coelenteramide or its analog in a high yield has been desired. The invention provides a process for producing di-O-methylcoelenteramide or its analog of formula (3) which comprises reacting O-methylcoelenteramine or its analog with 4-methoxyphenylacetyl halide or its analog. The invention also provides a process for producing coelenteramide or its analog, which comprises demethylation of di-O-methylcoelenteramide or its analog.
    Type: Grant
    Filed: May 29, 2013
    Date of Patent: October 28, 2014
    Assignee: JNC Corporation
    Inventor: Satoshi Inouye
  • Publication number: 20140316137
    Abstract: Coelenterazine analogs with different luminescence properties from conventional ones and coelenteramide analogs with different fluorescence properties from conventional ones have been desired. The invention provides coelenterazine analogs modified at the 8-position of coelenterazine and coelenteramide analogs modified at the 2- or 3-position of coelenteramide.
    Type: Application
    Filed: July 7, 2014
    Publication date: October 23, 2014
    Inventors: Satoshi Inouye, Yuiko Sahara, Takamitsu Hosoya
  • Publication number: 20140315898
    Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
    Type: Application
    Filed: December 12, 2012
    Publication date: October 23, 2014
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo
  • Patent number: 8865732
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: October 21, 2014
    Assignee: Novartis AG
    Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • Publication number: 20140309237
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Patent number: 8859558
    Abstract: This present disclosure is related to the field of pyrazine carboxamides and their derivatives and the use of these compounds as fungicides.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: October 14, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Kristy Bryan, George E. Davis, Paul R. Graupner, Beth Lorsbach, W. John Owen, Francis E. Tisdell
  • Patent number: 8859591
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: October 14, 2014
    Assignee: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8859814
    Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
  • Patent number: 8846917
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 30, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, David Matthew Shaw
  • Patent number: 8846918
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 30, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay
  • Patent number: 8846687
    Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: September 30, 2014
    Assignee: Novartis AG
    Inventors: Ian Bruce, Emma Budd, Lee Edwards, Catherine Howsham
  • Patent number: 8841449
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Knegtel
  • Patent number: 8841337
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Pierre-Henri Storck, Joanne Pinder, John R. Studley
  • Patent number: 8841450
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell, Simon Robert Everitt