Halogen Or Nitrogen Attached Directly To Diazine Ring Carbon By Nonionic Bonding Patents (Class 544/356)
  • Patent number: 9353094
    Abstract: Disclosed herein are compounds of formula (I) and methods of inhibiting IKK? and the NF-?B signaling and mTOR pathways.
    Type: Grant
    Filed: March 5, 2015
    Date of Patent: May 31, 2016
    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
  • Publication number: 20150099882
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, 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: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Applicant: Pfizer Inc.
    Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
  • 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
  • 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
  • Publication number: 20150005310
    Abstract: The present invention features tryptoline derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 1, 2015
    Applicant: X-Rx, Inc
    Inventors: Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
  • Patent number: 8916560
    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: Grant
    Filed: February 29, 2012
    Date of Patent: December 23, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, John McKearn, Donna L. Romero, Michael Clare
  • Patent number: 8916561
    Abstract: Disclosed herein are substituted quinoxaline 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 23, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero
  • Publication number: 20140364420
    Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
    Type: Application
    Filed: January 13, 2014
    Publication date: December 11, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
  • Publication number: 20140364408
    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: Application
    Filed: July 29, 2012
    Publication date: December 11, 2014
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 8895559
    Abstract: A variety of specific compounds within the scope of formula I which are useful as PI3K inhibitors and can be employed for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours, and pharmaceutical compositions and kits containing said specific compounds.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Markus Klein, Ulrich Emde, Hans-Peter Buchstaller, Christina Esdar, Oliver Poeschke
  • Patent number: 8889664
    Abstract: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: November 18, 2014
    Assignee: Exelixis, Inc.
    Inventors: William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20140291646
    Abstract: A pyrene-based compound and an organic light-emitting diode including the same, the pyrene-based compound being represented by Formula 1, below:
    Type: Application
    Filed: March 25, 2014
    Publication date: October 2, 2014
    Applicant: Samsung Display Co., Ltd.
    Inventors: Dong-Woo SHIN, O-Hyun KWON, Mie-Hwa PARK, Seul-Ong KIM, Byoung-Ki CHOI
  • Publication number: 20140275095
    Abstract: The present invention is directed to compounds of Formula I: wherein X is CR1 or N; Y is CR2 or N; Z is NH or O; R1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R2 is H, alkyl, or halo; R3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R4 is alkyl; R5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Curt A. Dvorak, Brock T. Shireman
  • Patent number: 8815412
    Abstract: An object is to provide a novel quinoxaline derivative, a light-emitting element with low driving voltage, and a light-emitting element which consumes low power. Another object is to provide a light-emitting device and an electronic appliance which consume low power by using the above light-emitting element. A quinoxaline derivative represented by a general formula (G11) is provided, in which at least one of carbon at a 2-position and carbon at a 3-position of quinoxaline, and carbon at a 2-position of a 1H-benzimidazole ring are bonded to each other via an arylene group.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: August 26, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Sachiko Kawakami, Satoko Shitagaki, Satoshi Seo
  • Publication number: 20140213572
    Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: April 1, 2014
    Publication date: July 31, 2014
    Applicant: AMGEN INC.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu Harrington, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
  • Publication number: 20140171430
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 19, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
  • Patent number: 8748430
    Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: June 10, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Publication number: 20140135338
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, 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: Application
    Filed: July 12, 2012
    Publication date: May 15, 2014
    Applicant: PFIZER INC.
    Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
  • Publication number: 20140128388
    Abstract: Drug candidates for inhibition of HIV-1 replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-1 viral replication in vitro.
    Type: Application
    Filed: July 31, 2013
    Publication date: May 8, 2014
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Lori Emert-Sedlak, Toshiaki Kodama, Billy W. Day, Weixiang Dai, Ronald P. Trible, Thomas E. Smithgall
  • Publication number: 20140128391
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Application
    Filed: November 1, 2013
    Publication date: May 8, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 8618102
    Abstract: The present invention is directed to bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, Georgia B. McGaughey, Anthony J. Roecker, John D. Schreier
  • Patent number: 8614215
    Abstract: The present invention is related to quinoxaline compounds of Formula (I) in particular for the treatment of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: February 21, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Serono SA
    Inventors: Pascale Gaillard, Vincent Pomel, Isabelle Jeanclaude-Etter, Jerome Dorbais, Jasna Klicic, Cyril Montagne
  • Patent number: 8614229
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Patent number: 8598173
    Abstract: The present invention relates to novel quioxaline-piperazine compounds, 1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives of formula (1): and their pharmaceutically acceptable salts, a process for their preparation thereof, and compositions containing such compounds. Therapeutic methods for the treatment of hyperproliferative disorders, including cancers, by administering quioxalin-piperazine compounds are also included.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: December 3, 2013
    Assignees: Korea Research Institute of Chemical Technology, Rexahn Pharmaceuticals, Inc.
    Inventors: Young-Dae Gong, Moon-Kook Jeon, Dong-Su Kim, Jae Y. Kong, Gun-Do Kim, Chang Ho Ahn, Young Bok Lee
  • Publication number: 20130317223
    Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.
    Type: Application
    Filed: November 6, 2012
    Publication date: November 28, 2013
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, David M. Knapp, Eric P. Gillis
  • Patent number: 8586739
    Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: November 19, 2013
    Assignee: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20130253183
    Abstract: Provided are: an aromatic amine derivative in which a terminal substituent such as a dibenzofuran ring or a dibenzothiophene ring is bonded to a nitrogen atom directly or through an arylene group or the like; an organic electroluminescence device including an organic thin film layer formed of one or more layers including a light emitting layer and interposed between a cathode and an anode in which a layer of the organic thin film layer contains the aromatic amine derivative by itself or as a component of a mixture, and the device has a long lifetime and high luminous efficiency; and an aromatic amine derivative for realizing the device.
    Type: Application
    Filed: May 24, 2013
    Publication date: September 26, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Yumiko MIZUKI, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
  • Patent number: 8541415
    Abstract: Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: September 24, 2013
    Assignee: University of Pittsburgh—of the Commonwealth System of Higher Education
    Inventors: Lori Emert-Sedlak, Toshiaki Kodama, Billy W. Day, Weixiang Dai, Ronald P. Trible, Thomas E. Smithgall
  • Publication number: 20130225552
    Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.
    Type: Application
    Filed: February 28, 2013
    Publication date: August 29, 2013
    Applicant: AMGEN INC.
    Inventor: Amgen Inc.
  • Patent number: 8518560
    Abstract: Provided are: an aromatic amine derivative in which a terminal substituent such as a dibenzofuran ring or a dibenzothiophene ring is bonded to a nitrogen atom directly or through an arylene group or the like; an organic electroluminescence device including an organic thin film layer formed of one or more layers including a light emitting layer and interposed between a cathode and an anode in which a layer of the organic thin film layer contains the aromatic amine derivative by itself or as a component of a mixture, and the device has a long lifetime and high luminous efficiency; and an aromatic amine derivative for realizing the device.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: August 27, 2013
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Yumiko Mizuki, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
  • Publication number: 20130217670
    Abstract: Compounds of the formula I in which R, R1 and R2 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.
    Type: Application
    Filed: September 22, 2011
    Publication date: August 22, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Markus Klein, Ulrich Emde, Hans-Peter Buchstaller, Christina Esdar, Oliver Poeschke
  • Publication number: 20130211076
    Abstract: The present invention provides a new synthesis for preparing N-(3-amino-quinoxalin-2-yl)-sulfonamides of general formulae (I) or (I?) and intermediates sulfonamides of formula (II) or (II?):
    Type: Application
    Filed: October 18, 2011
    Publication date: August 15, 2013
    Applicant: MERCK SERONO S.A. GENEVA
    Inventors: Danig Pohin, Dominique Swinnen
  • Publication number: 20130190296
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Application
    Filed: November 20, 2012
    Publication date: July 25, 2013
    Applicant: Dendreon Corporation
    Inventor: Dendreon Corporation
  • Publication number: 20130158004
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Application
    Filed: December 14, 2012
    Publication date: June 20, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Niklas HEINE, Gerald Juergen ROTH
  • Publication number: 20130140544
    Abstract: This invention relates to deuterated indolocarbazole compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.
    Type: Application
    Filed: January 24, 2013
    Publication date: June 6, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: E I DU PONT DE NEMOURS AND COMPANY
  • Publication number: 20130137672
    Abstract: Certain disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo[3.2.0]heptane are described, which are useful as orexin inhibitors. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: October 21, 2010
    Publication date: May 30, 2013
    Inventors: Bryan James Branstetter, Michael A. Letavic, Kiev S. Ly, Dale A. Rudolph, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman
  • Patent number: 8445678
    Abstract: Disclosed are 2-quinoxalinol salen compounds and in particular 2-quinoxalinol salen Schiff-base ligands. The disclosed 2-quinoxalinol salen compounds may be utilized as ligands for forming complexes with cations, and further, the formed complexes may be utilized as catalysts for oxidation reactions. The disclosed 2-quinoxalinol salen compounds also may be conjugated to solid supports and utilized in methods for selective solid-phase extraction or detection of cations.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: May 21, 2013
    Assignee: Auburn University
    Inventors: Anne E. V. Gorden, Xianghong Wu
  • Publication number: 20130065902
    Abstract: The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Application
    Filed: March 21, 2011
    Publication date: March 14, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Heinz Fretz, Julien Hazemann, Sylvia Richard-Bildstein, Romain Siegrist
  • Patent number: 8394801
    Abstract: The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: March 12, 2013
    Assignee: Aeterna Zentaris GmbH
    Inventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Tilmann Schuster, Emmanuel Polymeropoulos, Michael Czech, Eckhard Claus
  • Publication number: 20130059852
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
    Type: Application
    Filed: April 8, 2011
    Publication date: March 7, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
  • Publication number: 20130053384
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.
    Type: Application
    Filed: August 24, 2012
    Publication date: February 28, 2013
    Applicant: NeuPharma, Inc.
    Inventors: Yong-Liang Zhu, Xiangping Qian
  • Publication number: 20130018052
    Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 17, 2013
    Applicant: SK CHEMICALS CO., LTD.
    Inventors: Ju Young LEE, Keun-Ho RYU, Jae-Sun KIM, Yong-Hyuk KIM, Dong Chul SHIN, Bong-yong LEE, Sang-hwan KANG, Hyun-Jung LEE, Hoechul JUNG, Young Ah SHIN, Euisun PARK, Jaeseung AHN
  • Publication number: 20120316380
    Abstract: The present invention is related to pyrazolo piperidine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: GENKYOTEX SA
    Inventors: Patrick Page, Benoît Laleu, Francesca Gaggini, Mike Orchard
  • Publication number: 20120299473
    Abstract: There are provided an aminoanthracene derivative having an end substituent, such as a dibenzofuran ring, that is bonded at a position other than the 2-position in the formula (1) to anthracene through a nitrogen atom, and an organic electroluminescent device containing a cathode and an anode, and therebetween one or plural organic thin film layers containing at least a light emitting layer, at least one layer of the organic thin film layers containing the aminoanthracene derivative. The organic electroluminescent device has a long lifetime and a high luminous efficiency. (In the formula, R1, m and Ar1 to Ar4 have the meanings described in claim 1.
    Type: Application
    Filed: February 4, 2011
    Publication date: November 29, 2012
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Sayaka Mizutani, Takayasu Sado
  • Publication number: 20120283265
    Abstract: The present invention relates to compound Formula (I) wherein: Formula (II) means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a NO2 group, a NR1R2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n is 1 or 2, R is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group, a hydroxyl group, a COOR1 group, a NO2 group, a NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating AIDS. Some of said compounds are new and also form part of the invention.
    Type: Application
    Filed: June 14, 2010
    Publication date: November 8, 2012
    Applicants: SOCIETE SPLICOS, UNIVERSITE DE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jamal Tazi, Florence Mahuteau, Romain Najman, Didier Scherrer, Noelie Campos, Aude Garcel
  • Publication number: 20120277230
    Abstract: The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a NO2 group, a NR1R2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n is 1 or 2, R is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group, a hydroxyl group, a COOR1 group, a NO2 group, a NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating cancer. Some of said compounds are new and also form part of the invention.
    Type: Application
    Filed: June 14, 2010
    Publication date: November 1, 2012
    Applicants: SOCIETE SPLICOS, UNIVERSITE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Pierre Roux, Florence Mahuteau, Romain Najman, Jamal Tazi, Gilles Gadea, Didier Scherrer, Carsten Brock, Nathalie Cahuzac
  • Publication number: 20120263708
    Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: August 24, 2010
    Publication date: October 18, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
  • Publication number: 20120264704
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Application
    Filed: October 26, 2007
    Publication date: October 18, 2012
    Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
  • Publication number: 20120232056
    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: March 2, 2012
    Publication date: September 13, 2012
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly