Nitrogen Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/467)
  • Patent number: 10583112
    Abstract: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: March 10, 2020
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Stephen John Atkinson, Emmanuel Hubert Demont, Lee Andrew Harrison, Alexander G. Preston, Jonathan Thomas Seal, Ian David Wall, Robert J. Watson, James Michael Woolven
  • Patent number: 10287240
    Abstract: Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxy-methyl benzonitrile as an enantiomer thereof, comprising the following steps: a salt of (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl benzonitrile with a resolving agent D-(+)di-p-toluoyl tartaric acid was crystallized in a resolving solvent; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: May 14, 2019
    Assignee: Zhejiang Hushai Pharmaceuticals Co., Ltd.
    Inventors: Zunjun Liang, Siqi Hu, Caihua Peng, Wenfeng Huang, Qifeng Lu, Guoliang Tu
  • Patent number: 9987293
    Abstract: The present disclosure provides methods for treating chronic lymphocytic leukemia (CLL) with medicaments useful for same. The medicaments can be pharmaceutical compositions or kits comprising compounds of formula (I) or a salt, solvate or prodrug thereof. Specific compounds of the invention include 2-methyl-7-hydroxy-3-(3,4,5-trimethoxybenzoyl)-6-methoxybenzofuran which is also known as BNC105 and disodium 6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzofuran-7-yl phosphate which is also known as BNC 105P.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: June 5, 2018
    Assignee: BIONOMICS LIMITED
    Inventors: Alan R. Eastman, Darcy Bates
  • Patent number: 9115108
    Abstract: Abexinostat tosylate of formula (II): and its crystalline form I characterized by its X-Ray powder diffraction diagram, its Raman spectrum and its solid-state 13C CP/MAS NMR spectrum. Medicinal products containing the same which are useful in the treatment of cancer.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: August 25, 2015
    Assignee: PHARMACYCLICS, INC.
    Inventors: Anne Pimont-Garro, Philippe Letellier
  • Patent number: 9040553
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: May 26, 2015
    Assignee: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Publication number: 20150119418
    Abstract: Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein A represents a C1-C3 linear alkylene group, in which one methylene group is optionally substituted with O or S; n represents an integer of from 3 to 5; X1 and X2 each independently represent CH or N; W1 and W2 each independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group, in which one methylene group is optionally substituted with O or S; and R represents a substituted phenyl group, for example.
    Type: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Applicant: TOA EIYO LTD.
    Inventors: Kazuhiro Uemoto, Yoshimichi Sato, Naoki Okada, Emiko Iimori, Masayuki Kageyama
  • Patent number: 8962865
    Abstract: A process is disclosed for the preparation of a compound of formula and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: February 24, 2015
    Assignee: Lonza AG
    Inventors: Dominique Michel, Rudolf Fuchs
  • Publication number: 20150051270
    Abstract: A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein either Q1, CR6a and optionally R6b together form a cyclic moiety wherein: Q1 is selected from C1-2 alkylene, C1-2 alkenylene, OC1 alkylene and OC1 alkenylene moieties optionally substituted by oxo; R6a is a single bond and R6b is H; or R6a and R6b together form a double bond; and Q2 and Q3 are independently selected from H, R1 and R2; or Q2 and Q3 together form a cyclic moiety in which one of Q2 and Q3 is a cyclic moiety selected from OC1 alkylene and OC1 alkenylene moieties optionally substituted by oxo or a group R5 as here in below defined for R2 and the other of Q2 and Q3 is a cyclic moiety selected from C1-2 alkylene, C1-2 alkenylene and OC1 alkylene optionally substituted by oxo; R6a and R6b are each H or a cyclic moiety as defined above; and Q1 is selected from H, R1 and R2 and a cyclic moiety as defined above; and R1-4 are H or substituen
    Type: Application
    Filed: February 15, 2013
    Publication date: February 19, 2015
    Inventors: Shailesh Mistry, Etíenne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
  • Patent number: 8952056
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Grant
    Filed: February 23, 2009
    Date of Patent: February 10, 2015
    Assignee: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael Eissenstat, Dehui Duan, Sergi Gulnik, John W. Erickson
  • Publication number: 20150038507
    Abstract: The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.
    Type: Application
    Filed: August 4, 2013
    Publication date: February 5, 2015
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Publication number: 20150031892
    Abstract: Sphingolipid metabolite mimetics and methods of synthesizing them are provided. The sphingolipid metabolite mimetics are shown to be effective at inducing apoptosis in various types of tumor cells. Further, the sphingolipid metabolite mimetics are shown to be effective at sensitizing multiple types of tumor cells to TRAIL-induced apoptosis. Formulations containing one or more sphingolipid metabolite mimetics and, optionally, one or more cell death receptor agonists are provided. Methods of treating cancer in a subject in need thereof are provided using one or more sphingolipid metabolite mimetics.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Feiyan Liu, Kebin Liu, Zhizhen Huang, Ping Wu
  • Publication number: 20150031901
    Abstract: The invention relates to a method for preparing 5-amino-benzoyl-benzofuran derivatives having the general formula in which R1 is hydrogen or an alkyl or aryl group and R2 is hydrogen, an alkyl, alkoxy or dialkylaminoalkoxy group. According to the invention, the compounds having formula I are prepared by hydrogenating a 5-nitro-benzofuran derivative having the general formula in which R1 and R2 have the same meaning as above in the presence of palladised charcoal as a catalyst and in an ether or a mixture of ether as a solvent, thus forming the desired compounds.
    Type: Application
    Filed: November 28, 2012
    Publication date: January 29, 2015
    Applicant: SANOFI
    Inventors: Xavier Bon, Jean-Louis Delepine, Laure Jourdin, Denis Largeau, Philippe Vayron
  • Publication number: 20150011512
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 8, 2015
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Publication number: 20140350045
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Application
    Filed: July 11, 2013
    Publication date: November 27, 2014
    Inventors: IRAJ LALEZARI, JILL FABRICANT
  • Patent number: 8895759
    Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: November 25, 2014
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski, Tracy L. Hutchison, Brian Bray, Xiaoming Shen
  • Patent number: 8877804
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Grant
    Filed: April 29, 2013
    Date of Patent: November 4, 2014
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, John E. Donello, Xiaoxia Liu, Veena Viswanath
  • Patent number: 8871955
    Abstract: The present invention is concerned with a process in connection with the purification of a pharmaceutically acceptable salt of escitalopram or citalopram.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: October 28, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Hans Petersen, Martin Markvard Knudsen
  • Patent number: 8865914
    Abstract: The invention provides fluorescent sensors for the selective detection of a metal such as copper. The sensors may be considered to be derivatives of cyanine, fluorescein, rhodamine, rhodol, Tokyo green, or BODIPY. The sensors find particular use in detecting copper in cells and living animals.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: October 21, 2014
    Assignee: The Regents of the University of California
    Inventors: Christopher J. Chang, Genevieve C. Van De Bittner, Tasuku Hirayama, Jefferson Chan
  • Publication number: 20140288317
    Abstract: The present invention provides a novel radiolabelled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: GE HEALTHCARE LIMITED
    Inventors: HARRY JOHN WADSWORTH, DENNIS O'SHEA
  • Publication number: 20140275172
    Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Nalin Subasinghe
  • Publication number: 20140275043
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20140249215
    Abstract: Abexinostat tosylate of formula (II): and its crystalline form I characterised by its X-ray powder diffraction diagram, its Raman spectrum and its solid-state 13C CP/MAS NMR spectrum. Medicinal products containing the same which are useful in the treatment of cancer.
    Type: Application
    Filed: March 3, 2014
    Publication date: September 4, 2014
    Applicants: PHARMACYCLICS, LES LABORATOIRES SERVIER
    Inventors: Anne PIMONT-GARRO, Philippe LETELLIER
  • Patent number: 8822530
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: September 2, 2014
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20140192305
    Abstract: The present invention relates to photoreactive compounds that are particularly useful in materials for the alignment of liquid crystals.
    Type: Application
    Filed: August 7, 2012
    Publication date: July 10, 2014
    Applicant: ROLIC AG
    Inventors: Frederic Lincker, Izabela Bury S. Pires, Sabrina Chappellet, Patricia Scandiucci De Freitas, Mohammed Ibn-Elhaj, Qian Tang, Satish Palika, Masato Hoshino, Jean-Francois Eckert
  • Publication number: 20140171642
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.
    Type: Application
    Filed: February 19, 2014
    Publication date: June 19, 2014
    Applicant: BIONOMICS LIMITED
    Inventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
  • Patent number: 8728708
    Abstract: Disclosed is a photosensitive resin composition comprising: (Component A) an oxime sulfonate compound represented by Formula (1); (Component B) a resin comprising a constituent unit having an acid-decomposable group that is decomposed by an acid to form a carboxyl group or a phenolic hydroxy group; and (Component C) a solvent wherein in Formula (1) R1 denotes an alkyl group, an aryl group, or a heteroaryl group, each R2 independently denotes a hydrogen atom, an alkyl group, an aryl group, or a halogen atom, Ar1 denotes an o-arylene group or an o-heteroarylene group, X denotes O or S, and n denotes 1 or 2, provided that of two or more R2s present in the compound, at least one denotes an alkyl group, an aryl group, or a halogen atom.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: May 20, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Kyouhei Sakita, Wataru Kikuchi, Masatoshi Yumoto, Masanori Hikita
  • Publication number: 20140113897
    Abstract: The present invention embraces compounds that modulate the activity of Epstein-Barr Nuclear Antigen 1 (BBNA1) protein and use thereof in methods for treating latent Epstein-Barr virus infection. R7 is a substituted or unsubstituted phenyl, pyridyl, or pyrimidinyl group. A pharmaceutical composition comprising a compound of the invention in admixture with a pharmaceutically acceptable carrier is also provide as are methods for modulating the activity of Epstein-Barr Nuclear Antigen 1 (EBNA1) protein and treating a latent EpsteinBarr virus infection with a composition of the present invention.
    Type: Application
    Filed: May 22, 2012
    Publication date: April 24, 2014
    Applicant: THE WISTAR INSTITUTE
    Inventors: Paul M. Lieberman, Troy Messick
  • Patent number: 8680135
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: March 25, 2014
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
  • Patent number: 8674121
    Abstract: A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: March 18, 2014
    Assignee: SANOFI
    Inventors: Gerhard Kretzschmar, Volker Kraft, Thomas Olpp, Kai Rossen
  • Publication number: 20140057978
    Abstract: Provided herein are compounds for use in the treatment of central nervous system (CNS)-trauma related disorders like spinal cord injuries. Pharmaceutical compositions, single unit dosage forms, and kit suitable for use for the treatment of (CNS)-trauma related disorders are also disclosed.
    Type: Application
    Filed: March 9, 2012
    Publication date: February 27, 2014
    Applicant: ALGIAX PHARMACEUTICALS GMBH
    Inventors: Guido Koopmans, Birgit Hasse
  • Patent number: 8658808
    Abstract: A process for the production of Dronedarone intermediates of the formula (I), by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-(4-methoxyphenyl)-ethanone, subsequent treatment of the ester with bases and a zeolite (alumosilicate) catalyst and optional subsequent demethylation. This process can be used for the production of Dronedarone.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: February 25, 2014
    Assignee: Sanofi
    Inventors: Gerhard Kretzschmar, Volker Kraft, Kai Rossen, Joachim Graeser
  • Patent number: 8653286
    Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: February 18, 2014
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski, Tracy L. Hutchison, Brian Bray, Xiaoming Shen
  • Publication number: 20140031290
    Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 30, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
  • Patent number: 8614247
    Abstract: The invention relates to a method for preventing, attenuating or treating pulmonary hypertension in an individual in need thereof, comprising administering at least one 5-HTT inhibitor to said individual.
    Type: Grant
    Filed: October 11, 2005
    Date of Patent: December 24, 2013
    Assignees: Institut National de la Sante et de la Recherche Medicale, Assistance Publique-Hopitaux de Paris
    Inventors: Serge Adnot, Saadla Eddahibi
  • Publication number: 20130338116
    Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 19, 2013
    Inventor: Irving Sucholeiki
  • Patent number: 8586743
    Abstract: The present disclosure is directed to a reactive ester agent capable of conjugating a reporter molecule to a carrier molecule or solid support. The reactive ester agent has the general formula: wherein the variables are described throughout the application.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: November 19, 2013
    Assignee: Life Technologies Corporation
    Inventors: Kyle Gee, Aleksey Rukavishnikov, Diane M. Witczak
  • Publication number: 20130287727
    Abstract: The present specification discloses psyllid attractants, compositions comprising such attractants, lures, traps and other devices using such attractants, methods and uses to attract, capture and/or kill psyllids using such attractants, compositions and/or lures, traps and/or other devices, and methods and uses for monitoring a psyllid population using such attractants, compositions and/or lures, traps and/or other devices.
    Type: Application
    Filed: April 25, 2013
    Publication date: October 31, 2013
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos
  • Patent number: 8552032
    Abstract: The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: October 8, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Edward C. Lawson, Dennis J. Hlasta, Shyamali Ghosh, Renee L. DesJarlais, Carsten Schubert
  • Patent number: 8536350
    Abstract: The invention relates to a new process for the preparation of dronedarone and its salts, in particular a synthesis process which allows said compound and its salts to be obtained with good yields, high purity and in an industrially expedient manner; the invention also concerns a new synthesis intermediate.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: September 17, 2013
    Assignee: Laboratorio Chimico Internazionale S.p.A.
    Inventors: Mara Sada, Antonio Nardi, Stefano Maiorana
  • Publication number: 20130225674
    Abstract: The invention relates to a pharmaceutical product comprising a dibenzofuranone derivative as the active ingredient. The invention further relates to the use of dibenzofuranone derivatives to inhibit kinases, in particular serine/threonine kinases, to the use of dibenzofuranone derivatives for producing drugs and/or medicinal products for treatment, and to the use of dibenzofuranone derivatives as a diagnostic product for analyzing the role of protein kinases, in particular serine/threonine kinases, in particular protein kinase CK2 in cellular processes, the pathogenesis of diseases, ontogenesis and/or other developmental biological phenomena or relationships.
    Type: Application
    Filed: June 22, 2011
    Publication date: August 29, 2013
    Inventors: Joachim Jose, Claudia Götz, Andreas Gratz, Uwe Kuckländer
  • 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
  • Patent number: 8519165
    Abstract: There is provided a process for the preparation of a compound of formula (I), wherein R1, R2, R3, R4, X and Y are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone. Intermediate steps of the process comprise formulae according to (II) and (III).
    Type: Grant
    Filed: October 2, 2008
    Date of Patent: August 27, 2013
    Assignee: Cambrex Karlskoga AB
    Inventor: Lars Eklund
  • Publication number: 20130211107
    Abstract: The present invention is concerned with a process in connection with the purification of a pharmaceutically acceptable salt of escitalopram or citalopram.
    Type: Application
    Filed: July 12, 2011
    Publication date: August 15, 2013
    Applicant: H. Lundbeck A/S
    Inventors: Hans Petersen, Martin Markvard Knudsen
  • Patent number: 8501804
    Abstract: The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: October 26, 2009
    Date of Patent: August 6, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Makoto Kamata, Tohru Yamashita, Asato Kina, Michiko Amano
  • Patent number: 8486996
    Abstract: The invention relates to novel substituted 2-(phenyl-, pyridyl- or pyrimidyl-carbonyl)-furanes and -thiophenes and related phenoxy/phenylthio-acetophenones and corresponding heterocyclic compounds, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune diseases, and a method for the treatment of such a diseases.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: July 16, 2013
    Assignee: Basilea Pharmaceutica AG
    Inventors: Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Goutam Saha, Subir Kumar Sadhukhan, Rohit Saxena, Sudhir Srivastava
  • Publication number: 20130171415
    Abstract: Disclosed is a photosensitive resin composition comprising: (Component A) an oxime sulfonate compound represented by Formula (1); (Component B) a resin comprising a constituent unit having an acid-decomposable group that is decomposed by an acid to form a carboxyl group or a phenolic hydroxy group; and (Component C) a solvent wherein in Formula (1) R1 denotes an alkyl group, an aryl group, or a heteroaryl group, each R2 independently denotes a hydrogen atom, an alkyl group, an aryl group, or a halogen atom, Ar1 denotes an o-arylene group or an o-heteroarylene group, X denotes O or S, and n denotes 1 or 2, provided that of two or more R2s present in the compound, at least one denotes an alkyl group, an aryl group, or a halogen atom.
    Type: Application
    Filed: February 27, 2013
    Publication date: July 4, 2013
    Applicant: FUJIFILM Corporation
    Inventor: FUJIFILM Corporation
  • Publication number: 20130143960
    Abstract: Serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.
    Type: Application
    Filed: February 4, 2013
    Publication date: June 6, 2013
    Applicant: Ramot at Tel-Aviv University Ltd.
    Inventor: Ramot at Tel-Aviv University Ltd.
  • Patent number: 8450367
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Grant
    Filed: December 9, 2011
    Date of Patent: May 28, 2013
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20130116275
    Abstract: Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided.
    Type: Application
    Filed: April 20, 2011
    Publication date: May 9, 2013
    Applicants: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, EMORY UNIVERSITY
    Inventors: Erwin G. Van Meir, Binghe Wang
  • Patent number: 8436043
    Abstract: Provision of a prophylactic or therapeutic agent for diabetes, which has superior efficacy. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 7, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh