Quinoxalines (including Hydrogenated) Patents (Class 544/353)
Chalcogen bonded directly to diazine ring carbon (Class 544/354)
Having -c(=x)-, wherein x is chalcogen, bonded directly to diazine ring carbon (Class 544/355)
Halogen or nitrogen attached directly to diazine ring carbon by nonionic bonding (Class 544/356)
  • Quinoxaline compounds and uses thereof
    Patent number: 11661411
    Abstract: Provided herein are compounds having a structure of formula (I) and methods of using the disclosed compounds to inhibit IKK? activity.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: May 30, 2023
    Assignee: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
    Inventor: Amarnath Natarajan
  • Methods of treating anxiety by administering a substituted quinolone
    Patent number: 11273168
    Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
    Type: Grant
    Filed: March 16, 2020
    Date of Patent: March 15, 2022
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
  • Optically active substituted 2,3-bisphosphinoquinoxalines and processes for producing the same
    Patent number: 11053265
    Abstract: An optically active 2,3-bisphosphinopyrazine derivative represented by the following general formula (1): wherein R1 represents a group selected from a branched alkyl group having 3 or more carbon atoms, an adamantyl group, an optionally substituted cycloalkyl group, and an optionally substituted aryl group; R2 represents a group selected from a branched alkyl group having 3 or more carbon atoms, an adamantyl group, and an optionally substituted cycloalkyl group, provided that when R1 is a tert-butyl group, R1 and R2 are not the same; R3 represents a monovalent substituent; n represents an integer of 0 to 4; and * represents an asymmetric center on a phosphorus atom.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: July 6, 2021
    Assignees: NIPPON CHEMICAL INDUSTRIAL CO., LTD., NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY
    Inventors: Hajime Ito, Hiroaki Iwamoto, Tsuneo Imamoto, Ken Tamura
  • Method of treating disorders caused by reduced neurotransmission of serotonin, norephnephrine or dopamine
    Patent number: 10603331
    Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: March 31, 2020
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
  • Organic electroluminescent compound and an organic electroluminescent device comprising the same
    Patent number: 10186669
    Abstract: The present invention relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. By using the organic electroluminescent compound according to the present invention, it is possible to produce an organic electroluminescent device having low driving voltage, excellent current and power efficiencies, and noticeably improved driving lifespan.
    Type: Grant
    Filed: April 16, 2018
    Date of Patent: January 22, 2019
    Assignee: ROHM AND HAAS ELECTRONIC MATERIALS KOREA LTD
    Inventors: Hee-Ryong Kang, Hyun-Ju Kang, Jin-Ri Hong, Doo-Hyeon Moon, Young-Mook Lim, Bit-Na-Ri Kim, Nam-Kyun Kim, Mi-Ja Lee
  • Method for treating depression and/or depression status with substituted quinoxaline compounds
    Patent number: 10064879
    Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
    Type: Grant
    Filed: April 24, 2017
    Date of Patent: September 4, 2018
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
  • Preparation of polymers comprising at least one benzo[c][1,2,5]thiadiazol-5,6-dicarbonitrile-unit
    Patent number: 10059797
    Abstract: A polymer containing at least one unit of formula is prepared by treating a compound of formula wherein Y2 is I, Br, Cl or O—S(O)2CF3, with an S-donor agent, in order to obtain the compound of formula wherein Y2 is as defined for the compound of formula (5).
    Type: Grant
    Filed: November 23, 2015
    Date of Patent: August 28, 2018
    Assignees: BASF SE, Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.
    Inventors: Thomas Gessner, Helmut Reichelt, Jakob Jacek Wudarczyk, Felix Peter Hinkel, Tomasz Marszalek, Martin Baumgarten, Klaus Muellen
  • Substituted quinoxalines for inhibiting kinase activity
    Patent number: 10047059
    Abstract: Described herein are kinase inhibitors represented by Formula I: pharmaceutical compositions thereof, and uses thereof including but not limited to uses in treatment of cancer.
    Type: Grant
    Filed: June 8, 2017
    Date of Patent: August 14, 2018
    Assignee: NeuPharma, Inc.
    Inventors: Xiangping Qian, Yong-liang Zhu
  • Substituted quinoxalines as FGFR kinase inhibitors
    Patent number: 9856236
    Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: January 2, 2018
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Steven John Woodhead, Yannick Aime Eddy Ligny, Patrick René Angibaud
  • Antimicrobial agents
    Patent number: 9822108
    Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: November 21, 2017
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Malvika Kaul
  • Substituted quinoxalines as positive allosteric modulators of mGluR4
    Patent number: 9763938
    Abstract: The present invention relates to the use of novel quinoxaline derivatives of formula (I) as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.
    Type: Grant
    Filed: July 14, 2016
    Date of Patent: September 19, 2017
    Assignee: MERCK PATENT GMBH
    Inventor: Thomas E. Richardson
  • Methods and intermediates for preparing macrolactams
    Patent number: 9073825
    Abstract: A first aspect of the present invention describes a compound selected from group consisting of: wherein R is either H, C(O)RA, or C(O)NHCH(X)COOH; provided that X is a C2-C6 alkyl, or a C3-C8 cycloalkyl and RA is a C1-6 alkyl or aryl; These compounds are used to make Compound A
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: July 7, 2015
    Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.
    Inventors: Nobuyoshi Yasuda, Jeffrey T. Kuethe, Guy Humphrey, Gregory L. Beutner, Yong-Li Zhong, Edward Cleator, Carl Baxter
  • TRIAZOLO COMPOUNDS AS PDE10 INHIBITORS
    Publication number: 20150148332
    Abstract: The present invention provides compounds of formula (Ia) and (Ib) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Bernd Kuhn, Christian Lerner, Markus Rudolph, Herve Schaffhauser
  • NON-SYSTEMIC TGR5 AGONISTS
    Publication number: 20150148311
    Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.
    Type: Application
    Filed: June 20, 2014
    Publication date: May 28, 2015
    Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
  • PESTICIDALLY ACTIVE PYRIDYL- AND PYRIMIDYL- SUBSTITUTED THIAZOLE DERIVATIVES
    Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands
    Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Diarylacetylene hydrazide containing tyrosine kinase inhibitors
    Patent number: 9024021
    Abstract: The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animals.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: May 5, 2015
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Prabal Sengupta, Hemant Ashvinbhai Chokshi, Chetan Surjitsingh Puri, Sabbirhusen Yusufbhai Chimanwala, Varun Anilkumar Mehta, Dipali Manubhai Desai, Trinadha Rao Chitturi, Rajamannar Thennati
  • Anti-malarial agents
    Patent number: 9024033
    Abstract: The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical foimulation for the inhibition of malaria parasite proliferation.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: May 5, 2015
    Assignee: MMV Medicines for Malaria Venture
    Inventors: Michael John Witty, David Hardick
  • PYRAZOLYL QUINOXALINE KINASE INHIBITORS
    Publication number: 20150105368
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 2, 2014
    Publication date: April 16, 2015
    Applicant: ASTEX THERAPEUTICS LTD
    Inventors: Gordon SAXTY, Christopher William MURRAY, Valerio BERDINI, Gilbert Ebai BESONG, Christopher Charles Frederick HAMLETT, Christopher Norbert JOHNSON, Steven John WOODHEAD, Michael READER, David Charles REES, Laurence Anne MEVELLEC, Patrick René ANGIBAUD, Eddy Jean Edgard FREYNE, Tom Cornelis Hortense GOVAERTS, Johan Erwin Edmond WEERTS, Timothy Pietro Suren PERERA, Ronaldus Arnodus Hendrika Joseph GILISSEN, Berthold WROBLOWSKI, Jean Fernand Armand LACRAMPE, Alexandra PAPANIKOS, Oliver Alexis Georges QUEROLLE, Elisabeth Thérèse Jeanne PASQUIER, Isabelle Noëlle Constance PILATTE, Pascal Ghislain André BONNET, Werner Constant Johan EMBRECHTS, Rhalid AKKARI, Lieven MEERPOEL
  • METHOD FOR PREVENTING OR TREATING SKIN TUMOR
    Publication number: 20150098917
    Abstract: Methods, compositions and products for preventing skin tumor formation or inhibiting the development of an existing skin tumor in a subject are described. The methods involve administering to the subject a composition containing an ?2 adrenergic receptor agonist, such as brimonidine.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Guy BOUVIER, Matthew James LEONI, Michael GRAEBER
  • NOVEL DIAMINE COMPOUND AND METAL COMPLEXES, AND METHOD FOR PRODUCING OPTICALLY ACTIVE COMPOUNDS
    Publication number: 20150094468
    Abstract: The present invention relates to a novel diamine compound represented by the general formula (1), a ruthenium-diamine complex, an iridium-diamine complex, and a rhodium-diamine complex having the diamine compound as a ligand. Furthermore, the present invention relates to methods for selectively producing optically active compounds by using any of these complexes as a catalyst. wherein R1, R2, R3, X, Y, and Z are as defined in claim 1.
    Type: Application
    Filed: September 26, 2014
    Publication date: April 2, 2015
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventor: Taichiro TOUGE
  • Substituted quinoxalines and uses thereof
    Patent number: 8993758
    Abstract: Disclosed herein are compounds of formula (I) and methods of inhibiting IKK? and the NF-?B signaling and mTOR pathways.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: March 31, 2015
    Assignees: Board of Regents of the University of Nebraska, The Board of Regents, University of Texas System
    Inventors: Amarnath Natarajan, Qianyi Chen, Vashti C. Bryant, Rajkumar Rajule
  • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    Publication number: 20150080372
    Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line.
    Type: Application
    Filed: October 14, 2014
    Publication date: March 19, 2015
    Inventors: Prabha N. Ibrahim, Guoxian Wu, Jack Lin, Wayne Spevak, Hanna Cho, Todd Ewing, Chao Zhang
  • NEUROFIBROMATOSES THERAPEUTIC AGENTS AND SCREENING FOR SAME
    Publication number: 20150065554
    Abstract: Disclosed herein are methods of treating a patient at risk of developing or having a neurofibromatosis or a sporadic schwannoma. In exemplary embodiments, the method involves administering to a subject in need an effective amount of a modulator of a target related to neurofibromatosis. Also disclosed are screening assays involving the implementation of Merlin-null Schwann cells, and to compounds identified using same.
    Type: Application
    Filed: March 13, 2013
    Publication date: March 5, 2015
    Applicant: University of Central Florida Research Foundation, Inc.
    Inventor: Cristina Fernandez-Valle
  • Cadherin-11 Inhibitors and Methods of Use Thereof
    Publication number: 20150064168
    Abstract: Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.
    Type: Application
    Filed: July 3, 2014
    Publication date: March 5, 2015
    Inventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Jaime M. Guidry Auvil, Milton L. Brown
  • BIARYL ACETAMIDE COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20150065468
    Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
  • Substituted quinoxalines and quinoxalinones as PDE-10 inhibitors
    Patent number: 8969349
    Abstract: Provided herein are compounds of formula A-L-B, and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is R1 and R2 together with the carbon atoms to which they are attached form a 1,2-phenylene ring optionally substituted with one or more R11; L is —C(R6)2—C(R6)2—; B is a heteroaromatic group defined herein; and -A1-A2- , A3, R11 and R6 are defined herein. Also disclosed are methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: March 3, 2015
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: John Emmerson Campbell, Michael Charles Hewitt, Philip Jones, Linghong Xie
  • DIHYDROBENZOXAZINE AND TETRAHYDROQUINOXALINE SODIUM CHANNEL INHIBITORS
    Publication number: 20150057271
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: February 12, 2013
    Publication date: February 26, 2015
    Inventors: Christiane Boezio, Alessandro Boezio, Howard Bregman, Nagasree Chakka, James R. Coats, Katrina Woodin Copeland, Erin F. Dimauro, Thomas Dineen, Hua Gao, Daniel La, Isaac E. Marx, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss
  • CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
    Publication number: 20150057277
    Abstract: Chemical entities that are quinoxaline kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: January 25, 2013
    Publication date: February 26, 2015
    Inventors: Yong-liang Zhu, Xiangping Qian
  • CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
    Publication number: 20150057276
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: September 20, 2012
    Publication date: February 26, 2015
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • NEW BIS-AMIDO PYRIDINES
    Publication number: 20150057286
    Abstract: This invention relates to bis-amido pyridines of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Ulrich REISER
  • INHIBITORS OF HCV NS5A
    Publication number: 20150057218
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 26, 2015
    Inventors: Min ZHONG, Leping LI
  • Herbicidal 5H-quinoxaline-6-one derivatives detailed description
    Patent number: 8962628
    Abstract: The present invention provides a compound of formula (I) wherein R4 is of sub-formula (a) or (b) and wherein the other substituents are as defined in the specification. The compounds of formula (I) are potentially useful as herbicides.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: February 24, 2015
    Assignee: Syngenta Limited
    Inventors: Alaric James Avery, Alain De Mesmaeker, Nicholas Phillip Mulholland, Nigel James Willetts, Paul Anthony Worthington
  • COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC LIGHT EMITTING DIODE INCLUDING THE SAME AND DISPLAY INCLUDING THE ORGANIC LIGHT EMITTING DIODE
    Publication number: 20150034938
    Abstract: A compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode are disclosed and the compound for an organic optoelectronic device represented by the following Chemical Formula 1 or 2 provides an organic light emitting diode having life-span characteristics due to excellent electrochemical and thermal stability, and high luminous efficiency at a low driving voltage.
    Type: Application
    Filed: September 12, 2014
    Publication date: February 5, 2015
    Inventors: Dong-Min KANG, Hyun-Jung KIM, Chang-Ju SHIN, Jong-Woo WON, Nam-Heon LEE, Soo-Young JEONG, Ho-Kuk JUNG, Mi-Young CHAE
  • ANTICANCER BENZOPYRAZINES VIA THE INHIBITION OF FGFR KINASES
    Publication number: 20150031669
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: January 29, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Steven John Woodhead, Christopher William Murray, Valerio Berdini, Gordon Saxty, Gilbert Ebai Besong, Lieven Meerpoel, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
  • HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
    Publication number: 20150031679
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: September 29, 2014
    Publication date: January 29, 2015
    Inventors: John M. McCall, Donna L. Romero, John McKearn, Michael Clare
  • Metalloenzyme inhibitor compounds
    Patent number: 8940735
    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 20, 2012
    Date of Patent: January 27, 2015
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
  • Pyrazine derivative, and light emitting element, display device, electronic device using the pyrazine derivative
    Patent number: 8920941
    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: Grant
    Filed: December 22, 2006
    Date of Patent: December 30, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Murata, Masakazu Egawa, Harue Nakashima, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Allosteric protein kinase modulators
    Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Substituted quinoxaline carboxylic acids for the inhibition of PASK
    Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): 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: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • NOVEL OXIDATION DYE PRECURSORS
    Publication number: 20140359951
    Abstract: An agent for oxidative coloring of keratin-containing fibers, in particular human hair, includes as oxidation dye precursor of the developer type at least one compound of formula (I).
    Type: Application
    Filed: August 22, 2014
    Publication date: December 11, 2014
    Inventors: Antje Gebert, Annika Koenen
  • BENZOPIPERAZINE DERIVATIVES AS CETP INHIBITORS
    Publication number: 20140357632
    Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: August 13, 2012
    Publication date: December 4, 2014
    Inventors: Rajan Anand, Vincent J. Colandrea, Maud Reiter, Petr Vachal, Aaron Zwicker, Jonathan E. Wilson, Fengqi Zhang, Kake Zhao
  • Arylpiperazine-containing pyrrole 3-carboxamide derivatives for treating depressive disorders
    Patent number: 8895558
    Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: November 25, 2014
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
  • CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
    Publication number: 20140343068
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. Specifically quinoxaline derivatives of Formula I and their use in modulating the activity of Braf and/or mutant Braf kinase to regulate and modulate abnormal or inappropriate cell proliferation, differentiation, or metabolism are disclosed. Also disclosed are methods of treating cancer associated with Braf and/or mutant Braf kinase activity in a subject, comprising administering the compounds of Formula I.
    Type: Application
    Filed: September 28, 2012
    Publication date: November 20, 2014
    Inventors: Xiangping Qian, Yong Zhu
  • Glucocorticoid receptor antagonists
    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
  • PRMT5 INHIBITORS AND USES THEREOF
    Publication number: 20140329794
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 6, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • COMPOUNDS AND METHODS
    Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Aminooxazole inhibitors of cyclin dependent kinases
    Patent number: 8865709
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: October 21, 2014
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • ORGANIC ELECTROLUMINESCENCE DEVICE AND ANTHRACENE DERIVATIVE
    Publication number: 20140291653
    Abstract: An organic electroluminescence device which comprises a cathode, an anode and an organic thin film layer comprising at least one layer comprising a light emitting layer and disposed between the cathode and the anode, wherein at least one layer in the organic thin film layer comprises an anthracene derivative having a specific structure singly or as a component of a mixture, and an anthracene derivative having a specific asymmetric structure and providing an organic electroluminescence device exhibiting a great efficiency of light emission and having a long life, are provided.
    Type: Application
    Filed: June 11, 2014
    Publication date: October 2, 2014
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Hidetsugu IKEDA, Motohisa IDO, Masakazu FUNAHASHI
  • THERAPEUTIC COMPOUNDS AND COMPOSITIONS
    Publication number: 20140288081
    Abstract: Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye