The Diazine Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/116)
  • Patent number: 10351538
    Abstract: The present invention provides methods respectively for producing a 2,4,6-tris(2-hydroxy-3-methyl-4-alkoxyphenyl)-1,3,5-triazine compound and 2,4,6-tris(2,4-dihydroxy-3-methylphenyl)-1,3,5-triazine, both of which are improved in yield and quality. The methods according to the present invention are characterized in that a reaction of 2,4,6-tris(2,4-dihydroxy-3-methylphenyl)-1,3,5-triazine with an alkylating agent is carried out using a base in the presence of an alcohol or water, and are also characterized in that an ester compound is used as an additive in a reaction of cyanuric chloride with 2-methylresorcinol.
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: July 16, 2019
    Assignee: KANEKA CORPORATION
    Inventors: Koji Machida, Akira Nishiyama
  • Patent number: 9745272
    Abstract: This invention relates to novel Quinazoline-2,4(1H,3H)-dione derivatives of Formula (I): and their use as TRPC5 modulators, pharmaceutical compositions containing the same, and methods of using the same as agents for the treatment of TRPC5 receptor mediated disorders or conditions. R1, R2, R3 and R4 have meanings given in the description.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: August 29, 2017
    Assignee: Hydra Biosciences, Inc.
    Inventors: Bertrand L. Chenard, Randall J. Gallaschun
  • Patent number: 9656996
    Abstract: Disclosed are a fused heterocyclic compound, a preparation method therefor, a pharmaceutical composition, and uses thereof. The preparation method of the fused heterocyclic compound and/or the pharmaceutically acceptable salt thereof in the present invention comprises three synthesizing routes. The present invention also provides a pharmaceutical composition, containing one or more of the fused heterocyclic compound, the pharmaceutically acceptable salt, hydrates, solvent compounds, polymorphs and prodrugs thereof, and a pharmaceutically acceptable carrier. The present invention also relates to an application of the fused heterocyclic compound and/or the pharmaceutical composition in preparing kinase inhibitors and in preparing drugs for preventing and treating diseases related to kinase.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: May 23, 2017
    Assignee: SHANGHAI YINGLI PHARMACEUTICAL CO., LTD.
    Inventors: Zusheng Xu, Yangtong Lou
  • Patent number: 9543521
    Abstract: An organic semiconductor device selected from organic diodes, organic field effect transistors, and devices comprising an organic diode and/or organic field effect transistor and a method of producing such a device are provided. The organic semiconductor device comprises at least one semiconducting layer based on a diketopyrrolopyrrole (DPP) polymer. The semiconducting layer may effectively be protected against degradation by radiation and/or oxidation by adding at least one stabilizing agent selected from hydroxybenzophenones, hydroxyphenyl benzotriazoles, oxalic acid anilides, hydroxyphenyl triazines, hindered phenols and/or merocyanines to the DPP polymer layer. The stabilization is effective both during production and during usage of the device, while the device's electronic properties are retained. The stabilizing agent is preferably a UV absorbing agent or an antioxidant or anti-radical agent known from the field of organic polymer technology.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: January 10, 2017
    Assignee: BASF SE
    Inventors: Nikolai Kaihovirta, Tero Mustonen, Subramanian Vaidyanathan, Jean-Luc Budry
  • Patent number: 9487533
    Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: November 8, 2016
    Assignees: Genentech, Inc., F. Hoffmann-La Roche AG
    Inventors: Georgette Castanedo, Jennafer Dotson, Richard Goldsmith, Janet Gunzner, Tim Heffron, Simon Mathieu, Alan Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Steven Staben, Vickie Tsui, Tracy Bayliss, Irina Chuckowree, Adrian Folkes, Nan Chi Wan
  • 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
  • Publication number: 20150141411
    Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Frederik Jan Rita Rombouts, Andres Avelino Trabanco-Suarez, Henricus Jacobus Maria Gijsen, Gregor James Macdonald, Francois Paul Bischoff, Sergio-Alvar Alonso-de-Diego, Adriana Ingrid Velter, Yves Emiel Maria Van Roosbroeck
  • Publication number: 20150141400
    Abstract: The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 21, 2015
    Inventors: Takeshi Murata, Hatsuo Kawada, Satoshi Niizuma, Sousuke Hara, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Toshiyuki Mio
  • Publication number: 20150141643
    Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
    Type: Application
    Filed: July 14, 2014
    Publication date: May 21, 2015
    Inventors: Kouki FUCHINO, R. Richard GOEHRING, Akira MATSUMURA, Bin SHAO, Yoshiyuki TAODA, Naoki TSUNO, John William Frank WHITEHEAD, Jiangchao YAO
  • Publication number: 20150087644
    Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, 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 26, 2014
    Publication date: March 26, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
  • Publication number: 20150031672
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • 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: 20150025071
    Abstract: Compounds of the formula I in which U, V and W have the meanings indicated in claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Application
    Filed: January 14, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Hans-Peter Buchstaller, Christina Esdar, Birgitta Leuthner
  • Publication number: 20150011544
    Abstract: The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Inventors: Ke Ding, Chiwai Wong, Lijie Peng, Zhanfang Kang, Xi Zhou
  • Publication number: 20150005289
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 1, 2015
    Inventors: Hongyan Qi, Soongyu Choi, Amal Dakka, Gary Mitchell Karp, Jana Narasimhan, Nikolai Naryshkin, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Luke Green, Emmanuel Pinard, Hasane Ratni
  • 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
  • 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: 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
  • Publication number: 20140349996
    Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: August 11, 2014
    Publication date: November 27, 2014
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlacter, Anna L. Banka, Jun Liang, Brian Safina, Jun Li, Christine Chabot
  • Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140349997
    Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlacter, Anna L. Banka, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
  • 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
  • Publication number: 20140309215
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 16, 2014
    Inventors: Michael H. RABINOWITZ, Mark D. ROSEN, Kyle T. TARANTINO, Hariharan VENKATESAN
  • Publication number: 20140296206
    Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Lucian V. DiPietro, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Steven Mark Wenglowsky, Douglas Wilson, Yulian Zhang
  • Publication number: 20140275024
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Publication number: 20140275059
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Patent number: 8835634
    Abstract: The present invention relates to methods for the treatment of a pathology associated with hyperglycaemia, particularly diabetes, by administering quinoxalinone compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the claims. The compounds have activity as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone compounds for modulating insulin secretion in insulin-1 cells by contacting the cells with the compounds.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: September 16, 2014
    Assignee: Merck Patent GmbH
    Inventors: Gerard Botton, Eric Valeur, Micheline Kergoat, Christine Charon, Samer Elbawab
  • Publication number: 20140228352
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Patent number: 8802670
    Abstract: Compounds of Formulae Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: August 12, 2014
    Assignees: F. Hoffmann-La Roche AG, Genentech, Inc.
    Inventors: Adrian Folkes, Stephen Shuttleworth, Irina Chuckowree, Sally Oxenford, Nan Chi Wan, Georgette Castanedo, Richard Goldsmith, Janet Gunzner, Tim Heffron, Simon Mathieu, Alan Olivero, Daniel P. Sutherlin, Bing-Yan Zhu
  • Patent number: 8796263
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: August 5, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Patent number: 8791113
    Abstract: The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • Patent number: 8791119
    Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Sanofi
    Inventors: Sylvain Cote Des Combes, Jacques Froissant, Jean-Francois Gibert, Frank Marguet, Christophe Pacaud, Frédéric Puech, Antoine Ravet
  • Publication number: 20140206687
    Abstract: Disclosed are as represented by Formula (I) a quinazoline derivative and a pharmaceutical acceptable salt thereof, or, an enantiomer, a non-enantiomer, a tautomer, a racemate, a solvate, a metabolic precursor, or a prodrug of both. Also disclosed are a preparation method therefor, an intermediate, a pharmaceutical composition having the quinazoline derivative, and an application thereof. The quinazoline derivative of the present invention is provided with improved anti-tumor activity.
    Type: Application
    Filed: July 27, 2012
    Publication date: July 24, 2014
    Applicants: ZHEJIANG UNIVERSITY, SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Jingkang Shen, Yongping Yu, Wenteng Chen, Chunchun Zhang, Yu Hao, Jing Zhang, Bojun Li, Xuejun Liu
  • Patent number: 8759344
    Abstract: The invention relates to compounds corresponding to formula (I): in which R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached. Preparation process and therapeutic use.
    Type: Grant
    Filed: July 4, 2011
    Date of Patent: June 24, 2014
    Assignee: Sanofi
    Inventors: Chantal Alcouffe, Reinhard Kirsch, Corentin Herbert, Gilbert Lassalle
  • Publication number: 20140171431
    Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.
    Type: Application
    Filed: May 15, 2012
    Publication date: June 19, 2014
    Inventors: Jianhua Shen, Yiping Wang, Kai Wang
  • Patent number: 8741491
    Abstract: Embodiments are related to ionic liquids and more specifically to ionic liquids used in electrochemical metal-air cells in which the ionic liquid includes sulfonate ions as the anion.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: June 3, 2014
    Assignee: Fluidic, Inc.
    Inventors: Derek Wolfe, Cody A. Friesen, Paul Bryan Johnson
  • Publication number: 20140140956
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 22, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: David John Fairfax, Gregory Scott Martin, John Frederick Quinn, Bryan Cordell Duffy, Gregory Steven Wagner, Peter Ronald Young
  • Publication number: 20140142102
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 22, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: David John Fairfax, Bryan Cordell Duffy, Gregory Scott Martin, John Frederick Quinn, Shuang Liu, Gregory Steven Wagner, Peter Ronald Young
  • Publication number: 20140128392
    Abstract: Disclosed herein are new heterocyclic compounds of Formula IIa: and compositions thereof, 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 19, 2010
    Publication date: May 8, 2014
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero
  • Publication number: 20140107073
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Application
    Filed: October 4, 2013
    Publication date: April 17, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • Patent number: 8697693
    Abstract: Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase, in particular the p110 delta subtype, such as immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: April 15, 2014
    Assignee: F. Hoffmann LaRoche AG
    Inventors: Stewart James Baker, Paul John Goldsmith, Timothy Colin Hancox, Neil Anthony Pegg, Stephen Price, Stephen Joseph Shuttleworth, Sukhjit Sohai
  • Patent number: 8685968
    Abstract: Provided herein is a pharmaceutical composition that comprises a pharmaceutically acceptable carrier or diluent and, as an active ingredient, the compound 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: April 1, 2014
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Irina Chuckowree, Adrian Folkes, Tim Hancox, Stephen Shuttleworth
  • Publication number: 20140080829
    Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: November 21, 2013
    Publication date: March 20, 2014
    Applicants: Genentech, Inc., Array BioPharma Inc.
    Inventors: Josef Bencsik, James F. Blake, James M. Graham, Martin F. Hentemann, Nicholas C. Kallan, Ian S. Mitchell, Stephen T. Schlachter, Keith L. Spencer, Dengming Xiao, Rui Xu, Mike Welch, Jun Liang, Brian S. Safina
  • Patent number: 8664221
    Abstract: The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye).
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: March 4, 2014
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Masatomo Kato, Miwa Takai, Takahiro Matsuyama, Tatsuji Kurose, Yumi Hagiwara, Kenji Oki, Mamoru Matsuda, Toshiyuki Mori
  • Patent number: 8653077
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: February 18, 2014
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Kennith O. Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Publication number: 20140018363
    Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R7, R8, R2?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br, methoxyl group, NH2 group or NMe2 group; X represents NH, O or S; and R6 is selected from the group consisting of: pyrrolidinyl group, piperidinyl group, morpholino group, methoxyl group, and dimethylamine group. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.
    Type: Application
    Filed: July 30, 2013
    Publication date: January 16, 2014
    Applicant: China Medical University
    Inventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
  • 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
  • Publication number: 20130303537
    Abstract: A 1,2,3,4-tetrahydroquinoxaline compound represented by the following formula: In the formula (1), R1 represents substituents such as a halogen, an alkyl, a cycloalkyl, an aryl or a heterocyclic group; p represents 0 to 5; R2 represents substituents such as a halogen, an alkyl, a hydroxyl or an alkoxy group; q represents 0 to 2; R3 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkylcarbonyl or an arylcarbonyl group; R4 and R5 independently represent substituents such as hydrogen, a halogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; R6 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; R8 and R9 independently represent substituents such as hydrogen, an alkyl or an alkenyl; and X represents O or S.
    Type: Application
    Filed: July 9, 2013
    Publication date: November 14, 2013
    Inventors: Mamoru MATSUDA, Toshiyuki MORI, Kenji KAWASHIMA, Minoru YAMAMOTO, Masatomo KATO, Miwa TAKAI, Masato NAGATSUKA, Sachiko KOBAYASHI
  • Patent number: 8536175
    Abstract: The invention relates to compounds of formula (I) wherein the substituens are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: September 17, 2013
    Assignee: Novartis AG
    Inventors: Pascal Furet, Diana Graus Porta, Vito Guagnano
  • Publication number: 20130203756
    Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 24, 2011
    Publication date: August 8, 2013
    Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen