Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The 1,4-diazine Ring Patents (Class 514/255.06)
  • Patent number: 10188648
    Abstract: The present disclosure relates to solid state forms of Selexipag, in particular selexipag forms IV and V, and processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: January 29, 2019
    Assignee: TEVA PHARMACEUTICALS INTERNATIONAL GMBH
    Inventors: Nidia Villalva, Ivon Cante, Martin Aybar, Angel Rodriguez, Alejandro Guillen Torres, Hana Kantor, Ales Gavenda, Hugo Herrera, Alexander Jegorov, Nydia Lopez
  • Patent number: 10167266
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutical compositions thereof. Compounds of Formula (I) are epithelial sodium channel (ENaC) blockers useful in the hydration of mucosal surfaces, enhancement of mucociliary clearance, or restoration of mucosal defense in a subject. The compounds and compositions can therefore be used to treat diseases which rely on the hydration of mucosal surfaces.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: January 1, 2019
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 9890110
    Abstract: An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: February 13, 2018
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Youji Aoki, Yumi Kobayashi, Hidenori Daido, Hiroyuki Katsuta, Hidetaka Tsukada, Atsushi Hirabayashi, Yusuke Takahashi, Michikazu Nomura, Atsuko Kawahara
  • Patent number: 9878988
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: January 5, 2016
    Date of Patent: January 30, 2018
    Assignee: PARION SCIENCES, INC.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Patent number: 9861593
    Abstract: Method for the treatment or prophylaxis of dry eye disorders by the administration of alkylamino-polyhydroxyalkanes and compositions thereof.
    Type: Grant
    Filed: November 7, 2016
    Date of Patent: January 9, 2018
    Assignee: Dynamis Pharmaceuticals, Inc.
    Inventors: Alice Marcy, Annette Tobia
  • Patent number: 9849129
    Abstract: Provided are methods of treating a variety of disorders of the skin with inhibitors of the epithelial sodium channel (ENaC). The inhibitors are represented by formula (I)-(IV): where R is defined herein.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: December 26, 2017
    Assignee: PARION SCIENCES, INC.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Patent number: 9738651
    Abstract: Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula (II) wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 22, 2017
    Assignee: EPIZYME, INC.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Patent number: 9714226
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: July 25, 2017
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 9688639
    Abstract: Disclosed are solid forms of 4-(2-bromo-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are compositions for protecting a plant or plant seed from diseases caused by fungal pathogens comprising a biologically effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other nematocide, insecticide and/or fungicide are also disclosed. Also disclosed are methods for protecting a plant or plant seed from diseases caused by fungal pathogens comprising applying to a plant or seed, or to the environment of the plant or seed, a biologically effective amount of a solid form of Compound 1.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: June 27, 2017
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: Matthew Richard Oberholzer
  • Patent number: 9586911
    Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: March 7, 2017
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 9550777
    Abstract: The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.
    Type: Grant
    Filed: July 16, 2015
    Date of Patent: January 24, 2017
    Assignee: Genentech, Inc.
    Inventors: Anthony Estrada, Wen Liu, Snahel Patel, Michael Siu
  • Patent number: 9493427
    Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. Those compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: November 15, 2016
    Assignee: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
  • Patent number: 9491941
    Abstract: The present invention relates to new compounds of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: November 15, 2016
    Assignee: NOVARTIS TIERGESUNDHEIT AG
    Inventors: Emilie Dupont, Noelle Gauvry, Steve Nanchen, Chikako Ogawa, Chouaib Tahtaoui
  • Patent number: 9458106
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, A and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: October 4, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hui Hu, Min Jiang, Taiguang Jin, Rui Niu, Jianhua Wang, Min Wang, Song Yang, Taichang Yuan, Chengang Zhou, Zheng Zhou
  • Patent number: 9394240
    Abstract: An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: July 19, 2016
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Youji Aoki, Yumi Kobayashi, Hidenori Daido, Hiroyuki Katsuta, Hidetaka Tsukada, Atsushi Hirabayashi, Yusuke Takahashi, Michikazu Nomura, Atsuko Kawahara
  • Patent number: 9365557
    Abstract: The present invention relates to pyrazine 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. Certain compounds of this invention have formula IA: wherein the variables are as defined herein.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: June 14, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Patent number: 9260398
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: February 16, 2016
    Assignee: PARION SCIENCES, INC.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Patent number: 9139560
    Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerization and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: September 22, 2015
    Assignee: YM Biosciences Australia Pty Ltd.
    Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
  • Patent number: 9116161
    Abstract: Provided is a preparation method of a free fatty acid particle dispersion solution, the preparation method including: a) dissolving fatty acid in a solvent to prepare a fatty acid solution; and b) injecting the fatty acid solution in a non-solvent having miscibility with the solvent to prepare a free fatty acid particle dispersion solution.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: August 25, 2015
    Assignee: KOREA RESEARCH INSTITUTE OF STANDARDS AND SCIENCE
    Inventors: Se Hwa Kim, Eun-Soo Lee
  • Patent number: 9102633
    Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: August 11, 2015
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 9096548
    Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: August 4, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dieter Wiedenmayer, Armin Heckel, Dieter Hamprecht
  • Patent number: 9090570
    Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: July 23, 2013
    Date of Patent: July 28, 2015
    Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
  • 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: 20150141387
    Abstract: The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclopropyl-3-fluoro-4-methyl-5-[3-[[1-[2-[2-(methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-benzamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a ?2 adrenoceptor agonist; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DPI antagonist; an Histone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a MABA compound; an MPO inhibitor; a muscarinic antagonist; a PDE4 inhibitor; a PPAR? agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 21, 2015
    Inventors: Anne Elizabeth COOPER, Timothy Jon LUKER, Jerzy Andrzej SCHMIDT
  • Publication number: 20150133414
    Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.
    Type: Application
    Filed: April 22, 2013
    Publication date: May 14, 2015
    Applicant: University of Virginia Patent Foundation
    Inventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
  • Patent number: 9029382
    Abstract: The present invention relates compounds of the formula: or pharmaceutically acceptable salts thereof, useful as sodium channel blockers, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including cystic fibrosis, chronic obstructive pulmonary disease, asthma, bronchiectasis, acute and chronic bronchitis, emphysema, and pneumonia.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: May 12, 2015
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • 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: 20150126527
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 7, 2015
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou
  • Publication number: 20150110871
    Abstract: The present invention relates to a gastric retentive tablet composition comprising: (1) coated particles essentially consisting of a drug and an amino methacrylate copolymer, (2) a methacrylic acid copolymer and (3) an excipient, wherein items 1, 2, and 3 are blended together, and then compressed into a gastric retentive tablet. Thus, the coated particles (item 1), a methacrylic acid copolymer and the excipient are evenly distributed in the tablet. The excipient is selected from a group consisting of a retarding agent, a binder, a filler, a chelating agent, a diluent, a disintegrant, a lubricant, a colorant, a solubilizing agent, or a mixture thereof. The coated particles (item 1) do not contain methacrylic acid polymer.
    Type: Application
    Filed: January 3, 2015
    Publication date: April 23, 2015
    Inventor: David Wong
  • Patent number: 9005581
    Abstract: Provided herein are compounds, preparations and formulations comprising pyrazine derivatives having multiple poly(ethylene glycol) containing substituents. Many of the compounds disclosed herein are excretable by the renal system of a subject or patient and are useful for visualizing the renal system of a subject or patient. Upon excitation by electromagnetic radiation, a number of the compounds disclosed herein exhibit luminescence and are externally detectable when present in the body fluid of a patient or subject. Also provided herein are methods for visualizing the renal system of a subject or patient.
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: April 14, 2015
    Assignee: MediBeacon, LLC
    Inventors: Amruta Poreddy, William L. Neumann
  • Publication number: 20150099764
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Applicant: PARION SCIENCES, INC.
    Inventors: Michael Ross JOHNSON, William Robert Thelin, Richard C. Boucher
  • Patent number: 8999996
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: April 7, 2015
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Publication number: 20150087656
    Abstract: Prolongation compositions for prolonging the presence of drugs in blood.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Inventors: Aida Salatinjants, Robert Salatinjants
  • Patent number: 8980898
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: May 29, 2013
    Date of Patent: March 17, 2015
    Assignee: Parion Sciences, Inc.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Publication number: 20150065431
    Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 5, 2015
    Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
  • 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
  • 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: 20150056305
    Abstract: Provided are dithiol mucolytic agents. These agents increase the liquefaction of mucus in a patient with excessive mucus or mucus with increased viscoelastic, cohesive, or adhesive properties. Also provided are a variety of methods of treatment using these inventive mucolytic agents.
    Type: Application
    Filed: August 13, 2014
    Publication date: February 26, 2015
    Applicant: PARION SCIENCES, INC.
    Inventors: Michael R. Johnson, William R. Thelin, Ronald A. Aungst, JR.
  • Publication number: 20150057289
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Application
    Filed: November 4, 2014
    Publication date: February 26, 2015
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Patent number: 8962631
    Abstract: The present invention relates to pyrazine 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 II: wherein the variables are as defined herein.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: February 24, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Michael O'Donnell, Philip Michael Reaper
  • Patent number: 8962623
    Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has an Itk inhibitory activity, and is useful as a method for preventing and/or treating atopic dermatitis, and the like.
    Type: Grant
    Filed: February 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Locus Pharmaceuticals, Inc.
    Inventors: Rupa S. Shetty, Martha J. Kelly, Bin Liu, Jinming Zou, Kristofer K. Moffett, Younghee Lee, Dora Do-York Wong
  • Publication number: 20150051199
    Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.
    Type: Application
    Filed: October 31, 2012
    Publication date: February 19, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
  • Publication number: 20150051187
    Abstract: The present invention relates to pyrazine 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: Application
    Filed: August 25, 2014
    Publication date: February 19, 2015
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Publication number: 20150045312
    Abstract: Methods of treating autism, autistic spectrum disorders or Fragile X syndrome comprised of administering molecules that engage the cystine-glutamate exchange (System xc?) and/or elevate the extracellular levels of glutathione in the CNS. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.
    Type: Application
    Filed: August 11, 2014
    Publication date: February 12, 2015
    Inventors: Michael Neary, Chad Beyer
  • Publication number: 20150045326
    Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 7, 2014
    Publication date: February 12, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter WIEDENMAYER, Armin HECKEL, Dieter HAMPRECHT
  • 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: 20150031661
    Abstract: The present invention relates to pyrazine 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: Application
    Filed: March 24, 2014
    Publication date: January 29, 2015
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Patent number: 8937072
    Abstract: Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: January 20, 2015
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Changling Liu, Guang Huang, Jie Lan, Shulin Hao, Zhinian Li, Huichao Li, Aiying Guan, Airu Jiang, Ying Xu
  • Publication number: 20150018374
    Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1 is F, Cl or Br; R2 is H or F; and R3 is Cl or Br; and (b) at least one fungicidal compound selected from (b1) through (b13) as disclosed herein. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed are process intermediate compounds useful for preparing compounds of Formula 1.
    Type: Application
    Filed: January 30, 2013
    Publication date: January 15, 2015
    Inventors: Andrew Edmund Taggi, Jeffrey Keith Long, James Francis Bereznak
  • Publication number: 20150011470
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Application
    Filed: September 19, 2014
    Publication date: January 8, 2015
    Applicant: PFIZER INC.
    Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith