Chalcogen Bonded Directly To Triazine Ring Carbon Patents (Class 544/219)
  • 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: 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
  • Publication number: 20130018155
    Abstract: A polymer compound having a constituent unit represented by the following formula (P-a) and having a molecular weight of 5×102 to 1×107: (wherein Ar2 represents an aromatic group optionally having a substituent, R2 represents a direct bond or an organic group optionally having only an oxygen atom as a hetero atom, E represents a hetero atom, R3 represents a monovalent hydrocarbon group or a hydrogen atom, mt and nt represent each independently an integer of 1 or more, and lt represents an integer of 1 to 3. Each of a plurality of R3s, Es and lts may be mutually the same or different. When there exist a plurality of mts, these may be mutually the same or different. When there exist a plurality of groups in parentheses appended with mt and nt, these may be mutually the same or different.).
    Type: Application
    Filed: March 31, 2011
    Publication date: January 17, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Kenta Tanaka, Masahiro Fujioka
  • Publication number: 20120316171
    Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.
    Type: Application
    Filed: November 4, 2010
    Publication date: December 13, 2012
    Inventor: Tamas Oravecz
  • Patent number: 8222409
    Abstract: A nitrogen-containing heterocyclic compound is represented by Formula (I): wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms, or a substituted or unsubstituted alkoxy group having 1 to 20 carbon atoms; A represents a heterocyclic residue that contains at least one nitrogen atom and forms a six-membered aromatic heterocyclic ring; and n represents an integer of from 1 to 3.
    Type: Grant
    Filed: September 2, 2009
    Date of Patent: July 17, 2012
    Assignee: Fuji Xerox Co., Ltd.
    Inventors: Akira Imai, Hidekazu Hirose, Koji Horiba, Takeshi Agata, Katsuhiro Sato
  • Publication number: 20120175598
    Abstract: The present invention provides a carbazole derivative of formula (I) for an organic electroluminescent device: wherein Y represents a heteroatom selected from N, O, P, S, or a bicyclic or tricyclic heterocyclic ring; and Ar1 and Ar2 each independently represent an alkyl or aryl substituted or unsubstituted aromatic hydrocarbon, or an alkyl or aryl substituted or unsubstituted heterocyclic aromatic hydrocarbon.
    Type: Application
    Filed: December 5, 2011
    Publication date: July 12, 2012
    Applicant: E-RAY OPTOELECTRONICS TECHNOLOGY CO., LTD.
    Inventors: Banumathy Balaganesan, Kun-Feng Chiang, Huang-Ming Guo, Po-Wei Hsu
  • Publication number: 20120142878
    Abstract: A resin with a favorable index of refraction and transparency even without using heavy atoms or inorganic oxide fine particles by means of a polymerizable monomer having a 1,3,5-triazine ring represented by formula 1. (In formula 1: A is a group represented by formula 2, (in formula 2: R1 represents a hydrogen atom or a methyl group, T represents an alkylene having 1-10 carbon atoms, and R2 represents O or NH), and B1 and B2 are each independently groups represented by formula 3, formula 4, or formula 5 (in formulas 3-5: R3, R4, and R5 represent an alkyl group having 1-10 carbon atoms, an aryl group, or an aryloxy group, n1 and n3 are integers from 0-5, and n2 is an integer from 0-7, however when there are at least two of each of R3, R4, and R5, these may be the same or different from each other).
    Type: Application
    Filed: August 6, 2010
    Publication date: June 7, 2012
    Inventors: Kenichi Osawa, Takuro Oda
  • Patent number: 8193351
    Abstract: Compounds represented by formula (1) shown below, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such compounds are provided.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: June 5, 2012
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Takuo Tsukuda, Ken-Ichi Kawasaki, Susumu Komiyama, Yoshiaki Isshiki, Yasuhiko Shiratori, Kiyoshi Hasegawa, Takaaki Fukami, Takaaki Miura, Naomi Ono, Toshikazu Yamazaki, Young-Jun Na, Dong-Oh Yoon, Sung-Jin Kim
  • Patent number: 8178593
    Abstract: The invention provides B-sides of urethane formulations, wherein the B-sides comprise both alcohol and epoxy moieties. Also provided are urethane formulations comprising the B-side of the invention, as well as A-sides comprising isocyanate molecules.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: May 15, 2012
    Assignee: The Curators of the University of Missouri
    Inventors: Galen Suppes, Fu-Hung Hsieh, Yuan-Chan Tu, Pimphan Kiatsimkul
  • Publication number: 20120088911
    Abstract: where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
    Type: Application
    Filed: October 6, 2011
    Publication date: April 12, 2012
    Applicant: Abbott GmbH & Co. KG
    Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack, Andrea Hager-Wernet
  • Patent number: 8114992
    Abstract: The present invention is directed towards a method for the production of 2,4,6-trimercapto-1,3,5-triazine (TMT-H3). In particular, the method of the subject matter relates to the operation of acidifying the salts of 2,4,6-trimercapto-1,3,5-triazine in aqueous solution and in a defined pH range.
    Type: Grant
    Filed: July 3, 2006
    Date of Patent: February 14, 2012
    Assignee: Evonik Degussa GmbH
    Inventors: Peter Werle, Martin Trageser, Michael Beck
  • Publication number: 20120035278
    Abstract: The present invention relates to a process for preparing aminotriazine alkoxylates, which comprises at least one aminotriazine alkoxylate (a) being admixed with at least one aminotriazine (b) and reacted with at least one alkylene oxide (c), wherein the aminotriazine alkoxylate (a) is obtainable by reacting at least one aminotriazine (d) with at least one alkylene oxide (e) and/or at least one alkylene carbonate (g), and optionally at least one aminotriazine alkoxylate (f).
    Type: Application
    Filed: August 3, 2011
    Publication date: February 9, 2012
    Applicant: BASF SE
    Inventors: Andreas Kunst, Sebastien Garnier, Lionel Gehringer, Achim Löffler
  • Patent number: 8076477
    Abstract: Use of an affinity adsorbent for the separation, removal, isolation, purification, characterisation, identification or quantification of a proteinaceous material, wherein the affinity adsorbent is a compound of formula (III), wherein R1 is H, alkyl, aryl, hydroxyalkyl, cyciohexyl, amino or a heterocyclic group which is optionally substituted with one or more of alkyl, aryl, alkoxy, aryloxy, acyloxy, acylamino, amino, OH, CO2H, sulphonyl, carbamoyl, sulphamoyl, alkylsuiphonyl and halogen; one X is N and the other is N, C—Cl or C—CN; Y is O, S or NR2; Z is O, S or NR3; R2 and R3 are each H, alkyl, hydroxyalkyl, benzyl or ?-phenylethyl; Q is benzene, naphthalene, benzthiazole, benzoxazole, 1-phenylpyrazole, indazoie or benzimidazoie; R4, R5 and R6 are each H, OH, alkyl, aryl, heterocyclic, alkoxy, aryloxy, amino, acyloxy, acylamino, CO2H, sulphonic acid, carbamoyl, suiphamoyl, alkylsulphonyl or halogen, or two or more of R4, R5 and R6 are linked to form a cyclic structure; U and V are the same or different C1-10
    Type: Grant
    Filed: March 2, 2007
    Date of Patent: December 13, 2011
    Assignee: ProMetic BioSciences Ltd.
    Inventors: Jason Richard Betley, Helen Tatton, Kelly Le Riche, Matthew Webb
  • Patent number: 8030484
    Abstract: Compounds of formula (I) wherein R1 and R2 are the same or different and are each optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl groups; R3 is hydrogen or an aryl group substituent or R3 is a solid support optionally attached via a spacer; Z represents an oxygen atom, a sulphur atom or NR4; Y represents an oxygen atom, a sulphur atom or NR5; in which R4 and R5, which may be the same or different, represent hydrogen, optionally substituted alkyl containing 1 to 6 carbon atoms, optionally substituted phenyl, optionally substituted benzyl or optionally substituted ?-phenylethyl; and one of X1 and X2 represents a nitrogen atom and the other of X1 and X2 represents a nitrogen atom or CR6, in which R6 represents hydrogen or an aryl group substituent; are useful for the affinity binding of a prion protein.
    Type: Grant
    Filed: July 25, 2005
    Date of Patent: October 4, 2011
    Assignee: Prometic Biosciences Limited
    Inventors: James Christopher Pearson, Helen Rosemary Tatton, Patrick Vasconcelos Gurgel
  • Patent number: 8022221
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: September 20, 2011
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
  • Patent number: 8008484
    Abstract: Compounds of the formula (I), wherein Z represents C—R7 or N, and R5 represents alkyl that may be optionally substituted, alkenyl, alkynyl, cycloalkyl or alkoxycarbonylamino, are useful as agricultural and horticultural fungicides.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: August 30, 2011
    Assignee: Bayer CropScience AG
    Inventors: Koichi Araki, Sachio Kudo, Yoshitaka Sato, Masahito Ito, Takuya Gomibuchi, Yasuo Araki, Tetsuya Inuta, Keiji Endo, Shinichi Shirakura, Shin Nakamura
  • Publication number: 20110178294
    Abstract: Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
    Type: Application
    Filed: December 3, 2010
    Publication date: July 21, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Vogelbacher, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Manfred Raschack
  • Publication number: 20110177312
    Abstract: A laminated structure comprising an electrode, a polymer binding layer arranged on the electrode, and an electrically conductive organic material layer arranged on the polymer binding layer, wherein the polymer binding layer comprises an aromatic polymeric compound which has a structure represented by formula (I) [wherein Ar represents a conjugated divalent group which may have a substituent, provided that when there are multiple Ar's, the Ar's may be the same as or different from each other; and n represents an integer of 1 or greater] and has a number average molecular weight of 1×103 to 1×108 inclusive in terms of polystyrene content, the polymer binding layer is bonded to the electrode via a chemical bond between the aromatic polymeric compound and the surface of the electrode, and an electrically conductive organic material that composes a layer included in the electrically conductive organic material layer and arranged adjacent to the polymer binding layer has a number average molecular weight of 3×102
    Type: Application
    Filed: July 29, 2009
    Publication date: July 21, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Kenta Tanaka, Rui Ishikawa, Tomohisa Temma, Hideyuki Higashimura
  • Publication number: 20110105324
    Abstract: What is described are compounds of the formula (I) in which the respective substituents have the meanings given in the description. The compounds of the formula (I) can be used as herbicides and plant growth regulators.
    Type: Application
    Filed: April 11, 2009
    Publication date: May 5, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Christoph Hugh Rosinger, Dieter Feucht, Klaus-Helmut Mueller, Isolde Haeuser-Hahn, Jan Dittgen, Ernst Rudolf Gesing, Christian Waldraff
  • Publication number: 20110098470
    Abstract: The invention relates to a method for producing the trisodium salt of 2,4,6-trimercapto-s-triazine, cyanuric chloride being reacted in an aqueous medium at a temperature of 20 to 70° C. using NaSH, Na2S or a mixture of the two compounds at a pH value of 7 to 11, and subsequently the trisodium salt of 2,4,6-trimercapto-s-triazine being precipitated and cleaved at a pH value of 0.12 and a temperature of 0 to 20° C., characterized in that after the cleavage step of the trisodium salt of 2,4,6-trimercapto-s-triazine the mother liquor is adjusted to a pH value of 6 to 8, wherein the monosodium salt of 2,4,6-trimercapto-s-triazine is precipitated.
    Type: Application
    Filed: April 22, 2009
    Publication date: April 28, 2011
    Applicant: EVONIK DEGUSSA GMBH
    Inventors: Joerg Grimmer, Ruediger Peldszus, Peter Verelst, Roger Vandervee
  • Publication number: 20110045974
    Abstract: The present invention relates to triazinylmethyl sulfonamides of formula I wherein T, R1, R2, R3, A, Y and D are as defined in the claims and to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to processes and intermediates for preparing these compounds.
    Type: Application
    Filed: March 11, 2009
    Publication date: February 24, 2011
    Applicant: BASF SE
    Inventors: Jochen Dietz, Thomas Grote, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Alice Glaettli
  • Publication number: 20110001190
    Abstract: An object of the present invention is to provide a polysiloxane compound that can be developed in an aqueous alkali solution and can yield a cured product or thin film having superior heat-resistant transparency and insulating properties, a curable composition thereof, and a thin film transistor provided with a passivation layer or gate insulator using the same, and the present invention relates to a polysiloxane compound having at least one photopolymerizable functional group in a molecule thereof, and having at least one member selected from the group consisting of an isocyanuric acid backbone structure, a phenolic hydroxyl group and a carboxyl group within the same molecule, to a curable composition containing the polysiloxane compound, and to a cured product thereof.
    Type: Application
    Filed: December 5, 2008
    Publication date: January 6, 2011
    Applicant: KANEKA CORPORATION
    Inventors: Masahito Ide, Takao Manabe, Makoto Seino
  • Publication number: 20100323896
    Abstract: Herbicidal compositions comprising containing sulfonanilides of the formula (I) wherein R1 represents hydrogen, fluorine, chlorine, C1-4 alkyl, C1-4 alkoxy, C3-6 cycloalkyl-C1-4 alkyloxy or C1-4 haloalkoxy, R2 represents hydrogen, fluorine or chlorine, R3 represents hydrogen or fluorine, R4 represents hydrogen or C1-4 alkyl which may be optionally C1-4 alkoxy-substituted, C3-6 alkenyl or C3-6 alkynyl, R5 represents hydrogen, R6 represents hydroxy, fluorine or chlorine, or R5 and R6 may form, together with the carbon to which they are bonded, C?O, and X represents CH or N, provided that the following cases are excluded: (i) R1 represents hydrogen, fluorine or chlorine, R2 represents hydrogen, R3 represents hydrogen, R4 represents hydrogen, R5 represents hydrogen, and R6 represents hydroxy, (ii) R1 represents hydrogen, fluorine or chlorine, R2 represents hydrogen, R3 represents hydrogen, R4 represents hydrogen, and R5 and R6 form C?O together with the carbon to which they are bonded, (iii) R1 represents C1-
    Type: Application
    Filed: August 25, 2010
    Publication date: December 23, 2010
    Applicant: Bayer CropScience AG
    Inventors: Koichi Araki, Yoshitaka Sato, Takuya Gomibuchi, Keiji Endo, Shinichi Shirakura, Shin Nakamura, Christopher Rosinger, Dieter Feucht
  • Publication number: 20100305124
    Abstract: The present invention relates to aminopyridine and aminopyridazine derivatives of the general formula (I) in which R1, X, W and Q have the definitions given in the description, to a number of processes for preparing them, and to their use as insecticides.
    Type: Application
    Filed: April 2, 2010
    Publication date: December 2, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Martin FUSSLEIN, Ernst Rudolf Gesing, Markus Heil, Bernd Alig, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Koichi Araki, Norio Sasaki, Sachio Kudo, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Patent number: 7829703
    Abstract: Novel difluoromethanesulfonamide derivatives of the formula (I) Difluoromethanesulfonamide derivatives represented by the formula wherein X represents halogen, Y represents CH or N, R1 represents hydrogen, and R2 represents hydrogen or hydroxy, or R1 and R2 together may form C?O with the carbon atom to which they are bonded, and their use as herbicide for paddy field weeds.
    Type: Grant
    Filed: August 13, 2008
    Date of Patent: November 9, 2010
    Assignee: Bayer CropScience AG
    Inventors: Koichi Araki, Sachio Kudo, Yoshitaka Sato, Keiji Endo, Shinichi Shirakura, Shin Nakamura
  • Publication number: 20100267686
    Abstract: Carbacephem ?-lactam antibiotics having the following chemical structures (I) and (II) are disclosed: including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R3 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
    Type: Application
    Filed: April 21, 2010
    Publication date: October 21, 2010
    Applicant: Achaogen, Inc.
    Inventors: Allan S. Wagman, Heinz E. Moser
  • Patent number: 7812157
    Abstract: The present invention relates to a thiol compound derivative represented by the following formula (1), a curable composition containing the derivative, and a molded product made of the composition. More particularly, the invention relates to a thiol compound derivative which is added to a polymer having reactivity to a thiol derivative substituent to provide a curable composition, a curable composition containing the derivative and a crosslinkable halogen-containing crosslinking polymer, and a crosslinked molded product of the composition. wherein X1, X2 and X3 are each a group represented by the following formula (2).
    Type: Grant
    Filed: February 28, 2007
    Date of Patent: October 12, 2010
    Assignee: Unimatec Co., Ltd.
    Inventor: Kiyoshi Endo
  • Publication number: 20100233537
    Abstract: The invention relates to a stable secondary battery utilizing as active element the oxidation and reduction cycle of a sterically hindered nitroxide radical, which is bonded to a triazine structural element. Further aspects of the invention are a method for providing such a secondary battery, the use of the respective compounds as active elements in secondary batteries and selected novel nitroxide compounds as such.
    Type: Application
    Filed: March 12, 2007
    Publication date: September 16, 2010
    Inventors: Peter Nesvadba, Lucienne Bugnon
  • Publication number: 20100130687
    Abstract: Certain embodiments described herein are directed to silane coupling agents that may be used, for example, to covalently couple a polymer to a filler. In some examples, devices that include the polymer-silane coupling agent-filler compositions are also described.
    Type: Application
    Filed: November 26, 2008
    Publication date: May 27, 2010
    Applicant: SCHLUMBERGER TECHNOLOGY CORPORATION
    Inventors: Huilin Tu, Agathe Robisson, Julien Ramier
  • Patent number: 7718655
    Abstract: Trisubstituted triazines can be synthesized from cyanuric chloride. These compounds are useful anti-tubulin agents for treating cancer and proliferative diseases.
    Type: Grant
    Filed: June 20, 2003
    Date of Patent: May 18, 2010
    Assignee: New York University
    Inventors: Young-Tae Chang, Alexander Schier, Ho-Sang Moon, Eric Jacobson, Puja Parikh
  • Patent number: 7700605
    Abstract: The invention relates to compounds of the formula I and salts thereof, to a process for their manufacture, to their use in the treatment of (especially cysteine protease, such as UCH-L3- and/or USP-2 dependent) diseases or for the manufacture of pharmaceutical formulations against these diseases, methods of treatment of warm-blooded animals comprising administering the compounds and/or their salts to said animals and pharmaceutical preparations, especially for the treatment of the diseases, comprising said compounds and/or salts.
    Type: Grant
    Filed: July 17, 2006
    Date of Patent: April 20, 2010
    Assignee: Novartis AG
    Inventors: Stefanie Flohr, Pascal Furet, Patricia Imbach, Ulrich Hommel, Hans-Ulrich Litshcer, Shirley Gil Parrado, Ulrich Hassiepen, Johann Zimmermann
  • Patent number: 7652010
    Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: January 26, 2010
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
  • Patent number: 7642303
    Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: January 5, 2010
    Inventors: Thomas L. Shakely, James John Krutak
  • Publication number: 20090325964
    Abstract: The present teachings relate to piperazine metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators having Formula I: wherein the constituent variables are as defined herein. The present teachings further relate to methods for the preparation of the compounds, and to methods for using the compounds for treatment of diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety.
    Type: Application
    Filed: May 22, 2009
    Publication date: December 31, 2009
    Applicant: Wyeth
    Inventors: Matthew Gregory Bursavich, Adam Matthew Gilbert, Joseph Raymond Stock
  • Publication number: 20090318693
    Abstract: Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.
    Type: Application
    Filed: May 29, 2009
    Publication date: December 24, 2009
    Inventors: Barry Forman, Donna Yu
  • Publication number: 20090318692
    Abstract: The present invention provides a process of coupling the compound (2) and compound (3) in the presence of a coupling agent, yielding imatinib of formula (1).
    Type: Application
    Filed: December 19, 2008
    Publication date: December 24, 2009
    Inventors: Jakub Castulik, Petr Benovsky
  • Publication number: 20090305894
    Abstract: Herbicidal compositions comprising containing sulfonanilides of the formula (I), wherein R1 represents hydrogen, fluorine, chlorine, C1-4 alkyl, C1-4 alkoxy, C3-6 cycloalkyl-C1-4 alkyloxy or C1-4 haloalkoxy, R2 represents hydrogen, fluorine or chlorine, R3 represents hydrogen or fluorine, R4 represents hydrogen or C1-4 alkyl which may be optionally C1-4 alkoxy-substituted, C3-6 alkenyl or C3-6 alkynyl, R5 represents hydrogen, R6 represents hydroxy, fluorine or chlorine, or R5 and R6 may form, together with the carbon to which they are bonded, C?O, and X represents CH or N, provided that the following cases are excluded: (i) R1 represents hydrogen, fluorine or chlorine, R2 represents hydrogen, R3 represents hydrogen, R4 represents hydrogen, R5 represents hydrogen, and R6 represents hydroxy, (ii) R1 represents hydrogen, fluorine or chlorine, R2 represents hydrogen, R3 represents hydrogen, R4 represents hydrogen, and R5 and R6 form C?O together with the carbon to which they are bonded, (iii) R1 represents C1-4 a
    Type: Application
    Filed: September 2, 2006
    Publication date: December 10, 2009
    Inventors: Koichi Araki, Yoshitaka Sato, Takuya Gomibuchi, Keiji Endo, Shinichi Shirakura, Shin Nakamura, Christopher Rosinger, Dieter Feucht
  • Publication number: 20090258876
    Abstract: Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.
    Type: Application
    Filed: February 26, 2009
    Publication date: October 15, 2009
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Churlmin SEONG, Chul Min PARK, Soyoung KIM, Wookyu PARK, Nosang PARK
  • Patent number: 7507734
    Abstract: Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: March 24, 2009
    Assignee: Aventis Pharma S.A.
    Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
  • Publication number: 20090062536
    Abstract: A herbicide comprising as an active ingredient a sulfonanilide compound represented by the formula: wherein, R1 represents CHF2 or CH2CF3; R2 represents hydrogen, C1-3 alkyl, 3-propenyl, or 3-propynyl; R3 represents hydrogen; R4 represents hydrogen, hydroxy, or methylthio, or R3 and R4, together with a carbon atom to which they are bonded, may form C?O; R5 represents halogen or methyl; X represents methoxy or chlorine; and Z represents CH or N; with the proviso that, (i) when R1 represents CH2CF3, R2 represents hydrogen, R5 represents bromine or iodine, X represents methoxy, and Z represents CH, (ii) when R1 represents CHF2 and X represents methoxy, R5 represents bromine or iodine, Z represents N, and R2 represents C1-3 alkyl, 3-propenyl, or 3-propynyl, (iii) when R1 represents CHF2 and X represents chlorine, Z represents CH.
    Type: Application
    Filed: August 18, 2008
    Publication date: March 5, 2009
    Inventors: KOICHI ARAKI, Yoshitaka Sato, Shinichi Shirakura, Keiji Endo, Shin Nakamura, Seiji Ukawa, Chieko Ueno
  • Publication number: 20090012091
    Abstract: The present invention relates to a compound represented as the following Formula (I) and a pharmaceutical composition thereof wherein all substituents are as defined in the specification; and also relates to a method for treating or lessening the severity of a disease or a condition, comprising administering said compound or said pharmaceutical composition.
    Type: Application
    Filed: June 23, 2008
    Publication date: January 8, 2009
    Applicant: KinaGen, Inc.
    Inventor: Chang Jun Yu
  • Publication number: 20080312084
    Abstract: Novel difluoromethanesulfonamide derivatives of the formula (I) Difluoromethanesulfonamide derivatives represented by the formula wherein X represents halogen, Y represents CH or N, R1 represents hydrogen, and R2 represents hydrogen or hydroxy, or R1 and R2 together may form C?O with the carbon atom to which they are bonded, and their use as herbicide for paddy field weeds.
    Type: Application
    Filed: August 13, 2008
    Publication date: December 18, 2008
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Koichi ARAKI, Sachio KUDO, Yoshitaka SATO, Keiji ENDO, Shinichi SHIRAKURA, Shin NAKAMURA
  • Patent number: 7462715
    Abstract: The present invention provides a 1,3,5-triazine compound represented by the following formula I: This compound can be synthesized easily and more economically and can be used as a dehydrating condensing agent having the property of accumulating at a water interface. In the case where carboxylic acid, amine, alcohol or other reaction substrate is amphiphilic, when mixing the dehydrating condensing agent of the present invention, which is amphiphilic, and the substrate to form various molecular aggregate phase including micelles in an aqueous solution, the substrate and the dehydrating condensing agent can be accumulated at the water interface. As a result, the concentration of the substrate increases locally at the water interface, and condensation reaction can be performed extremely efficiently.
    Type: Grant
    Filed: January 31, 2005
    Date of Patent: December 9, 2008
    Assignee: Japan Science and Technology Agency
    Inventor: Munetaka Kunishima
  • Publication number: 20080242860
    Abstract: The present invention relates to a silver halide color photographic light-sensitive material wherein at least one of light-sensitive silver halide emulsion layers includes a silver halide emulsion having a silver chloride content of at least 95 mol % and a silver iodide content of 0.05 mol % to 0.75 mol % and/or a silver bromide content of 0.05 mol % to 4.00 mol % and further at least one compound represented by the following formula (I): X-(L)n-Y ??Formula (I) wherein X represents a group adsorptive to a silver halide, L represents a divalent connecting group comprising one of an atom and an atomic group including at least one of a carbon atom, a nitrogen atom, a sulfur atom and an oxygen atom, Y denotes a reducible group and n denotes an integer of 0 or 1.
    Type: Application
    Filed: June 3, 2008
    Publication date: October 2, 2008
    Applicant: FUJIFILM CORPORATION
    Inventors: Atsushi Matsunaga, Tadashi Inaba, Shinichi Ichikawa
  • Patent number: 7414011
    Abstract: Disclosed are compounds of the formula (I) or salts thereof in which R1, R2, R3, R4, I, R5, Q, R4, W, X, Y, V and Z, are as defined in the specification, which are suitable for use as herbicides or plant growth regulators. Also disclosed are processes for preparing the compounds of formula (I) or salts thereof.
    Type: Grant
    Filed: September 12, 2005
    Date of Patent: August 19, 2008
    Assignee: Hoechst Schering Agrevo GmbH
    Inventors: Hansjörg Dietrich, Christian Waldraff, Lothar Willms, Hermann Bieringer, Christopher Rosinger, Felix Thürwächter, Thomas Auler
  • Patent number: 7335770
    Abstract: The present invention relates to triazine compounds and their analogs and derivatives, and methods and compositions comprising these compounds. The compounds and compositions of this invention are useful for, among other things, treating pathophysiological conditions arising from inflammatory responses, inhibiting or blocking glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells, inhibiting smooth muscle proliferation, treating vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis, and the like.
    Type: Grant
    Filed: March 24, 2004
    Date of Patent: February 26, 2008
    Assignee: Reddy U5 Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Sesha Sridevi Alluri, Velagala Venkata Rama Murali Krishna Reddy, Manojit Pal, Jangalgar Tirupathy Reddy, Koteswar Rao Yeleswarapu, Gaddam Om Reddy, Potlapally Rajender Kumar
  • Patent number: 7332490
    Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.
    Type: Grant
    Filed: May 25, 2006
    Date of Patent: February 19, 2008
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
  • Patent number: 7332488
    Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: February 19, 2008
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
  • Patent number: RE43748
    Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: October 16, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura