Substituent Nitrogen Bonded Directly To Carbon Of The Triazine Ring Patents (Class 544/194)
  • Patent number: 10131650
    Abstract: The alpha-helix mimetic containing a triazine-piperazine scaffold is provided. The alpha-helix mimetic compound can mimic efficiently the alpha-helix structure of protein secondary structure and act as an inhibitor for the protein interaction being specific to various diseases mediated by alpha-helix. Therefore, the compound can be used as a biological probe and have a high potential of drug treating diseases.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: November 20, 2018
    Assignees: POSCO, POSTECH ACADEMY-INDUSTRY FOUNDATION
    Inventors: Hyun-Suk Lim, Misook Oh, Quyen Q. Hoang, Wei Wang
  • Patent number: 10111878
    Abstract: Provided are compounds of formula (I), Wherein: ring A and ring B are each independently an optionally substituted 5-6 membered monocyclic aryl or heteroaryl. The compounds are inhibitors of isocitrate dehydrogenase 2 (IDH2) mutants useful for treating cancer.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: October 30, 2018
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Jeremy Travins, Luke Utley
  • Patent number: 10030024
    Abstract: The present invention relates to compounds useful as inhibitors of the PAR-2 signaling pathway. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of GPCRs in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such GPCRs; and the comparative evaluation of new inhibitors of the PAR-2 signaling pathway. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: July 24, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Luc J. Farmer, Pierre-Andre Fournier, Stephanie Lessard, Bingcan Liu, Miguel St-Onge, Claudio Sturino, Janek Szychowski, Constantin Yannopoulos, Frederic Vallee, Jean-Eric Lacoste, Julien Martel, Monica Bubenik, Yeeman Ramtohul, Camil Elie Sayegh
  • Patent number: 10000497
    Abstract: A series of fused bicyclic heteroaromatic derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase III? (PI4KIII?) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: June 19, 2018
    Assignees: UCB BIOPHARMA SPRL, KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D
    Inventors: Helen Tracey Horsley, Qiuya Huang, Judi Charlotte Neuss, James Thomas Reuberson, Bart Vanderhoydonck
  • Patent number: 9724350
    Abstract: Provided are compounds of formula (I), Wherein: ring A and ring B are each independently an optionally substituted 5-6 membered monocyclic aryl or heteroaryl. The compounds are inhibitors of isocitrate dehydrogenase 2 (IDH2) mutants useful for treating cancer.
    Type: Grant
    Filed: July 10, 2014
    Date of Patent: August 8, 2017
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Jeremy Travins, Luke Utley
  • Patent number: 9700562
    Abstract: Disclosed herein are triazine compounds and methods of making and using thereof to treat malaria, provide chemoprophylaxis, and/or treat or inhibit infection by one or more Plasmodium spp.
    Type: Grant
    Filed: April 5, 2016
    Date of Patent: July 11, 2017
    Assignee: The United States of America, as represented by the Secretary of the Army, on behalf of the Walter Reed Army Institute of Research
    Inventors: Richard J. Sciotti, Gregory A. Reichard, Kristina M. Pannone, Victor E. Zottig
  • Patent number: 9618654
    Abstract: This film-forming composition includes, for example, a polymer, crosslinking agent and light-diffusing agent that contain a triazine ring-containing repeating unit structure such as that represented formula (17), and is able to provide cured films with good light diffusing properties. Furthermore, this film-forming composition, which includes the same polymer, crosslinking agent and fine inorganic particles having a cross-linkable functional group, is able to provide cured films with good high temperature and high humidity resistance.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: April 11, 2017
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Naoya Nishimura, Takahiro Kaseyama, Yasufumi Shikauchi, Natsumi Murakami, Masashi Abe, Shigeru Mitsui, Masaaki Ozawa
  • Patent number: 9579325
    Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.
    Type: Grant
    Filed: November 25, 2014
    Date of Patent: February 28, 2017
    Assignee: Genzyme Corporation
    Inventors: Scott F. Sneddon, John L. Kane, Bradford H. Hirth, Frederic Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
  • Patent number: 9465255
    Abstract: A rubbing cloth, a roller, a method of forming an LC alignment angle and a method of cleaning debris are provided. The rubbing cloth is dyed by using a solution dissolved with a dye containing at least one of hydroxyl group and cyano-group. An outer surface of the roller is provided with the rubbing cloth. The method of forming the LC alignment angle forms the LC alignment angle by using a roller with an outer surface wrapped by the rubbing cloth of the present invention. The method of cleaning debris cleans debris by using the rubbing cloth or the roller under illumination condition. They present advantages of excellent cleaning effect, simple implementation and low cost.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: October 11, 2016
    Assignees: BOE TECHNOLOGY GROUP CO., LTD., BEIJING BOE DISPLAY TECHNOLOGY CO., LTD.
    Inventors: Yupeng Wang, Chao Tian
  • Patent number: 9309270
    Abstract: The present invention relates to a method for silylating 2-amino-1,3,5-triazines of the general formula (I) in which R1 and R2 are each independently hydrogen, hydroxyl, NH2, NHR3, NR32, NO2, NHCOR3, C1- to C2-alkyl, C1- to C20-hydroxyalkyl, C2- to C20-alkenyl, C1- to C20-alkoxy, aryl or aryloxy optionally substituted with C1- to C8-alkyl and R3 is C1- to C20-alkyl, C3- to C12-cycloalkyl, C4 to C30-alkylcycloalkyl, aryl optionally substituted with C1- to C8-alkyl, with silanes, by reacting silanes of the general formula (II) X—SiH(R4R5)??(II), in which X is fluorine, chlorine, bromine or iodine R4 and R5 are each independently C1- to C20-alkyl, C1- to C20-hydroxyalkyl, C1- to C20-haloalkyl, C2- to C20-alkenyl, C1- to C20-alkoxy, aryl or aryloxy optionally substituted with C1- to C8-alkyl, in the presence of a base.
    Type: Grant
    Filed: April 1, 2014
    Date of Patent: April 12, 2016
    Assignee: BASF SE
    Inventors: Alexander König, Rebekka Von Benten, Jens Aβmann, Edwin Kroke, Sandra Jähnigen, Anke Schwarzer
  • Patent number: 9221799
    Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.
    Type: Grant
    Filed: August 6, 2014
    Date of Patent: December 29, 2015
    Assignee: The Walter and Eliza Hall Institute of Medical Research
    Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard, Guillaume Lessene
  • Patent number: 9153788
    Abstract: An organic light-emitting device containing a compound represented by the following general formula in a light light-emitting layer has a high light-emission efficiency. The ring containing Y1, Y2 and Y3 represent a triazine ring or a pyrimidine ring; Z1, Z2 and R1 to R8 represent a hydrogen atom or a substituent; and at least one of R1 to R8 represents a diarylamino group or a carbazolyl group. The compound represented by the general formula (1) contains at least two carbazole structures in the molecule thereof.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: October 6, 2015
    Assignee: KYUSHU UNIVERSITY NATIONAL UNIVERSITY CORPORATION
    Inventors: Chihaya Adachi, Takuma Yasuda, Saeyoun Lee, Hiroko Nomura, Tetsuya Nakagawa
  • Patent number: 9150525
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: September 8, 2014
    Date of Patent: October 6, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Stepan Vyskocil, Gabriel S. Weatherhead
  • Publication number: 20150011752
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Application
    Filed: September 4, 2014
    Publication date: January 8, 2015
    Inventors: Aranapakam Mudumbai VENKATESAN, Zecheng CHEN, Christoph Martin DEHNHARDT, Osvaldo DOS SANTOS, Efren Guillermo DELOS SANTOS, Arie ZASK, Jeroen Cunera VERHEIJEN, Joshua Aaron KAPLAN, David James RICHARD, Semiramis AYRAL-KALOUSTIAN, Tarek Suhayl MANSOUR, Ariamala GOPALSAMY, Kevin Joseph CURRAN, Mengxiao SHI
  • Patent number: 8921547
    Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: December 30, 2014
    Assignee: Genzyme Corporation
    Inventors: Scott F. Sneddon, John L. Kane, Bradford H. Hirth, Frederic Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
  • Patent number: 8906475
    Abstract: Provide is a cellulose acylate film, of which the environmental humidity-dependent retardation change is small and which, when stuck to a polarizer and used in high-temperature and high-humidity environments, is effective for preventing the polarizing element from being deteriorated. A cellulose acylate film, which contains a hydrogen-bonding compound satisfying the following requirements (A) to (C), and at least one hydrophobizing agent selected from a polyalcohol ester-base hydrophobizing agent, a polycondensate ester-base hydrophobizing agent and a carbohydrate derivative-base hydrophobizing agent: (A) the compound has both a hydrogen-bonding donor part and a hydrogen-bonding acceptor part in one molecule, (B) the value computed by dividing the molecular weight of the compound by the total number of the hydrogen-bonding donor number and the hydrogen-bonding acceptor number in the compound is from 30 to 65, and (C) the total number of the aromatic ring structures in the compound is from 1 to 3.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: December 9, 2014
    Assignee: Fujifilm Corporation
    Inventors: Nobutaka Fukagawa, Masato Nagura, Takayasu Yasuda, Takahiro Ohno, Satoshi Tanaka, Aiko Yamamoto, Aiko Yoshida, Shinya Watanabe
  • Patent number: 8906920
    Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: December 9, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney
  • Patent number: 8894815
    Abstract: The instant invention relates to storage stable solutions of optical brighteners based on certain salt forms of anilino-substituted bistriazinyl derivatives of 4,4?-diaminostilbene-2,2?-disulphonic acid and of organic acids which do not need extra solubilizing additives.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: November 25, 2014
    Assignee: Clariant Finance (BVI) Limited
    Inventors: John Martin Farrar, Andrew Clive Jackson, Margaret Mahon, Martin Oberholzer
  • Patent number: 8895747
    Abstract: Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: November 25, 2014
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Dieter Heindl, Heribert Maerz, Axel Schmidt
  • Patent number: 8859679
    Abstract: The instant invention relates to storage stable aqueous solutions of stilbene optical brighteners with polyvinyl alcohols which can be directly used by the papermaker in that they may be diluted with water and/or be metered directly into a coating composition, to provide coated papers of a particularly high whiteness.
    Type: Grant
    Filed: April 5, 2006
    Date of Patent: October 14, 2014
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Andrew Clive Jackson, Alec Stewart Tindal, Mariela Gauto
  • Patent number: 8835629
    Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: September 16, 2014
    Assignee: The Walter and Eliza Hall Institute of Medical Research
    Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard
  • Publication number: 20140249128
    Abstract: The present disclosure provides substituted triazine carboxamides of Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein A1, X, A2, E, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Application
    Filed: February 26, 2014
    Publication date: September 4, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Dawit Tadesse, Jianming Yu
  • Patent number: 8822464
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: September 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
  • Publication number: 20140221650
    Abstract: The present invention relates to novel 1,4,2-diazaphospholidine derivatives, to a process for preparation thereof and to use as catalysts.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: Bayer MaterialScience AG
    Inventor: Frank Richter
  • Publication number: 20140212980
    Abstract: The present invention provides a probe that further promotes ionization in proteomic analysis using mass spectrometry, and a high-sensitive mass spectrometry method for a protein using such a probe. Further, the present invention provides an ionization-enhancing probe that can be used even for a protein that has a high degree of hydrophobicity and quickly turns over, and a high-sensitive mass spectrometry method for a protein using such a probe. A thiol probe for a protein, which is represented by the following formula (I): [Chemical Formula 1] wherein R1 represents a linker group, and R2 represents a substituted ammonium group or a substituted amino group. A mass spectrometry method for a protein, comprising the steps of: obtaining a modified protein by reacting the thiol probe with a protein to be subjected to mass spectrometry; and subjecting the modified protein to mass spectrometry.
    Type: Application
    Filed: August 17, 2012
    Publication date: July 31, 2014
    Inventors: Takashi Shimada, Taka-Aki Sato, Koichi Tanaka
  • Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • Patent number: 8785628
    Abstract: A series of substituted [1,3,5]triazin-2-yl derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: July 22, 2014
    Assignee: UCB Pharma, S.A.
    Inventors: Daniel Rees Allen, Roland Bürli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, David John Nash, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
  • Patent number: 8784612
    Abstract: The instant invention relates to storage stable solutions of optical brighteners based on certain salt forms of anilino-substituted bistriazinyl derivatives of 4,4?-diaminostilbene-2,2?-disulphonic acid and of organic acids which do not need extra solubilizing additives.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: July 22, 2014
    Assignee: Clariant Finance (BVI) Limited
    Inventors: John Martin Farrar, Andrew Clive Jackson, Margaret Mahon, Martin Oberholzer
  • Publication number: 20140194429
    Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 10, 2014
    Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
  • Patent number: 8772480
    Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: July 8, 2014
    Assignee: Amgen Inc.
    Inventors: Kristin L. Andrews, Yunxin Y. Bo, Shon Booker, Victor J. Cee, Noel D'Angelo, Bradley J. Herberich, Fang-Tsao Hong, Claire L. M. Jackson, Brian Alan Lanman, Hongyu Liao, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Liping H. Pettus, Anthony B. Reed, Adrian Leonard Smith, Seifu Tadesse, Nuria A. Tamayo, Bin Wu, Ryan Wurz, Kevin C. Yang
  • Patent number: 8747999
    Abstract: The present invention related to (micro-or nano-) capsules that have two different functional groups on the outer shell of the particles that allow deposition onto the textile surfaces (i.e. exhibit substantivity) and subsequent covalent bonding of the particles onto the textile (i.e. are reactive towards the fiber).
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: June 10, 2014
    Assignee: BASF SE
    Inventors: Bryan David Grey, Kishor Kumar Mistry, Chun-tian Zhao
  • Patent number: 8618101
    Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 31, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney
  • Patent number: 8557986
    Abstract: A polysaccharide derivative having a high solubility in an aqueous solvent is produced. The production method of the present invention uses a compound shown by the general formula (1) as a condensing agent and allows a polysaccharide having a carboxyl group to react with an an organic compound having a functional group capable of condensing with the carboxyl group to prepare the polysaccharide derivative: R1 and R2 independently represent a substituent selected among alkyl groups of 1 to 4 carbon atoms and aryl groups of 6 to 8 carbon atoms; Z?represents a counter anion; and E+represents an organic group shown as: R3, R4, and R5 independently represent an organic group having at least one carbon atom directly bound to a quaternary nitrogen atom and any two or all of R3, R4, and R5 may link together to form a cyclic structure.
    Type: Grant
    Filed: April 27, 2007
    Date of Patent: October 15, 2013
    Assignee: Seikagaku Corporation
    Inventor: Yousuke Yasuda
  • Publication number: 20130219634
    Abstract: Tanned leather, skin or pelt is produced by non-metal tanning, comprising the step of tanning a bated hide, skin or pelt with a tanning agent (A), the tanning agent (A) being at least one compound of formula (I), wherein X signifies fluorine, chlorine and/or (+NR3)0-1, wherein R is a substituted C1 to C6 alkyl group or an unsubstituted C1 to C6 alkyl group, an unsubstituted C6 to C10 aryl group or a substituted C6 to C10 aryl group or a C5 to C6 heteroaryl group, R1 signifies hydrogen, C1-8 alkyl or an alkyleneoxy radical of formula (Ia), —(—C2-3alkylene-O—)q—H??(Ia) R2 signifies substituted or unsubstituted C2 to C8 alkylenesulphonic acid, substituted or unsubstituted C2 to C8 alkylenecarboxylic acid or an alkyleneoxy radical of formula (Ib), —(—C2-3alkylene-O—)m—Y??(Ib) or an alkylene sulfonyl alkyleneoxy radical of formula (Ic), —(C2-3alkylene-O)p—C2-3alkylene-SO2CH2CH2O—Y??(Ic) m signifies 1 or 2, p signifies 0 or 1, q is of from 1 to 10, Y signifies hydrogen or —SO3M, M signifies
    Type: Application
    Filed: October 5, 2011
    Publication date: August 29, 2013
    Applicant: CLARIANT FINANCE (BVI) LIMITED
    Inventors: Claus Reineking, Roberta Gamarino, Licia Trimarco, Maurizio Quaglierini, Markus Gisler, Rainer Nusser
  • Patent number: 8513326
    Abstract: The present invention relates, generally, to monomers containing carbamate-methacrylates or derivatives of carbamate-methacrylates, processes for making the monomers, and compositions comprising the monomers. The present invention also relates to methods of using the monomers, such as in dental applications, and in particular, dental restorative resins.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: August 20, 2013
    Assignee: Septodont Confi-Dental
    Inventors: Marianela Trujillo-Lemon, Kristin Lindsay Wall, Kristina Esquibel, Jordan Boulden, Amy J. Docktor, Zachary R. Shelton, Cora Bracho-Troconis
  • Patent number: 8465673
    Abstract: A humidity dependence improver for polymer film, comprising a compound of the following formula (1) or (2): wherein Ra, Rb and Rc represent an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group; X1 to X6 represent a single bond or a divalent linking group; R1 to R6 represent a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: June 18, 2013
    Assignee: FUJIFILM Corporation
    Inventors: Takayasu Yasuda, Masato Nagura
  • Patent number: 8445490
    Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: April 13, 2011
    Date of Patent: May 21, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Annapurna Pendri, Zhongxing Zhang, Weixu Zhai, Guo Li, Samuel Gerritz, Paul Michael Scola, Li-Qiang Sun, Qian Zhao, Eric Mull
  • Publication number: 20130090326
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
    Type: Application
    Filed: October 15, 2010
    Publication date: April 11, 2013
    Applicant: Rib-X Pharmaceuticals, Inc.
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Yanming Du, Sandra Sinishtaj, Yuanqing Tang, Brian T. Wimberly
  • Patent number: 8389717
    Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, and Ar are as defined in the specification and claims, or to pharmaceutically active acid addition salts of such compounds. Compounds of formula I are modulators for amyloid beta and may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: March 5, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Erwin Goetschi, Synese Jolidon, Thomas Luebbers
  • Patent number: 8389739
    Abstract: Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor ? (ROR?) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR? results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: March 5, 2013
    Assignee: Orphagen Pharmaceuticals
    Inventors: Scott Thacher, Xiaolin Li, Robert Babine, Bruno Tse
  • Patent number: 8383812
    Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
    Type: Grant
    Filed: October 11, 2010
    Date of Patent: February 26, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney, Victor W. Rosso, Jun Li
  • Patent number: 8367823
    Abstract: The present invention includes methods, articles, compositions and colorant dyes and pigments that include biocidal N-halamine dye composition having two or more heterocyclic ring structures attached to one or more N-halamine groups, wherein one or more halogens associate with the one or more one or more N-halamine groups to affect biocidal activity.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: February 5, 2013
    Assignee: Board of Regents, The University of Texas System
    Inventors: Yuyu Sun, Jie Luo
  • Patent number: 8362236
    Abstract: The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: January 29, 2013
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Nobuo Shimma, Takuo Tsukuda, Hiroshi Koyano, Atsushi Suda, Tadakatsu Hayase, Kihito Hada, Ken-Ichi Kawasaki, Susumu Komiyama, Naomi Ono, Toshikazu Yamazaki, Ryoichi Saitoh, Masami Kohchi, Kiyoshi Hasegawa
  • Patent number: 8362241
    Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: January 29, 2013
    Assignee: Amgen Inc.
    Inventors: Noel D'Angelo, Fang-Tsao Hong, Mark H. Norman, Adrian L. Smith, Seifu Tadesse
  • Patent number: 8334382
    Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: December 18, 2012
    Assignee: Neurogen Corporation
    Inventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
  • Patent number: 8318702
    Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.
    Type: Grant
    Filed: July 4, 2008
    Date of Patent: November 27, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Yutaka Kondoh, Kazuhiko Iikubo, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani, Itsuro Shimada, Takahiro Matsuya, Kazuo Kurosawa, Akio Kamikawa, Hiroyuki Mano
  • Patent number: 8309551
    Abstract: The present application relates to novel azabicyclic compounds, processes for their preparation, their use alone or in combinations for the treatment and/or prevention of diseases, and their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: September 1, 2007
    Date of Patent: November 13, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hartmut Schirok, Joachim Mittendorf, Johannes-Peter Stasch, Frank Wunder, Friederike Stoll, Karl-Heinz Schlemmer
  • Patent number: 8278443
    Abstract: The present invention relates to a resin composition for an optical film, comprising a polyarylate resin and an amino resin having a triazine structure, and to an optical film prepared by using the same. By using the resin composition for an optical film, a thickness direction retardation can be controlled, while having a negative value, during a step of fabricating the optical film, an in-plane retardation can be controlled, and the optical film can be used as a substrate of a display instead of a glass substrate without an additional retardation compensation film.
    Type: Grant
    Filed: January 4, 2008
    Date of Patent: October 2, 2012
    Assignee: LG Chem, Ltd.
    Inventors: Sang-Uk Ryu, Dong-Ryul Kim, Dae-Woo Nam
  • Patent number: 8262945
    Abstract: Photochromic compositions are disclosed comprising a polymeric material, a photochromic dye, a hydroxyphenyl triazine UV absorber and, optionally, a further light stabilizer selected from the sterically hindered amines. These systems provide a reversible photochromic effect and show improved light stabilization and color fastness.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: September 11, 2012
    Assignee: BASF SE
    Inventors: Mara Destro, Dario Lazzari, Dirk Simon, Manuele Vitali
  • Patent number: 8227465
    Abstract: The present patent application relates to novel combinations of a triazine derivative and of an insulin secretion stimulator.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: July 24, 2012
    Assignee: Poxel SAS
    Inventors: Gérard Moinet, Daniel Cravo, Didier Mesangeau