Six-membered Hetero Ring Consists Of Oxygen, Nitrogen And Carbon (e.g., 1,2-oxazines, Etc) Patents (Class 544/63)
  • Patent number: 9650341
    Abstract: The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: May 16, 2017
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Publication number: 20150111883
    Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).
    Type: Application
    Filed: October 21, 2014
    Publication date: April 23, 2015
    Inventors: Jaekyoo Lee, Jang-Sik Choi, Hae-Jun Hwang, Ho-Juhn Song, Jung-Ho Kim, Se-Won Kim, Jong Sung Koh, Jaesang Lee, Tae-Im Lee, Yung-Geun Choi, Sung-Ho Park, In Yong Lee, Byung-Chul Suh, Paresh Devidas Salgaonkar, Dong-Sik Jung
  • Publication number: 20150030618
    Abstract: The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: May 5, 2014
    Publication date: January 29, 2015
    Applicant: SEATTLE GENETICS, INC.
    Inventors: Hans-Georg LERCHEN, Lars Linden, Sherif El Sheikh, Jörg Willuda, Charlotte C. Kopitz, Joachim Schuhmacher, Simone Greven, Christoph Mahlert, Beatrix Stelte-Ludwig, Sven Golfier, Rudolf Beier, Iring Heisler, Axel Harrenga, Karl-Heinz Thierauch, Sandra Bruder, Heike Petrul, Hannah Jörissen, Sandra Borkowski
  • Publication number: 20150023989
    Abstract: The present application relates to new antibody drug conjugates (ADCs) of N,N dialkylauristatins directed against the target FGFR2, drug metabolites of said ADCs, a method for producing said ADCs, the use of said ADCs for the treatment and/or prevention of illnesses as well as the use of said ADCs for producing pharmaceuticals for the treatment and/or prevention of illnesses, particularly of hyperproliferative and/or angiogenic diseases such as carcinosis. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.
    Type: Application
    Filed: December 12, 2012
    Publication date: January 22, 2015
    Inventors: Hans-Georg Lerchen, Stefanie Hammer, Axel Harrenga, Charlotte Christine Kopitz, Carl Friedrich Nising, Anette Sommer, Beatrix Stelte-Luowig, Christoph Mahlert, Joachim Schuhmacher, Sven Golfier, Simone Greven, Sandra Bruder
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Publication number: 20140336173
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(?O)—NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR2R10, —C(?O)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: December 10, 2012
    Publication date: November 13, 2014
    Inventors: Dirk Brohm, Melanie Heroult, Marie-Pierre Collin, Walter Hübsch, Mario Lobell, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer
  • Publication number: 20140288046
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: April 11, 2014
    Publication date: September 25, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • Patent number: 8835427
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, Y1, Y2, Y3, G, J, X1 and X2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: September 16, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Andris Juris Liepa, Robert James Pasteris, Thomas Martin Stevenson
  • Publication number: 20140228564
    Abstract: Disclosed is a process of enantioselectively forming an aminoxy compound of Formula (3) In formula (3) R1 is one of an aliphatic group and an alicyclic group. R2 is one of hydrogen, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group and an arylalicyclic group. R3 is one of hydrogen, halogen, hydroxyl, and an aliphatic group with a main chain having 1 to about 10 carbon atoms. The respective aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic groups of R1, R2, and R3 comprise 0 to about 3 heteroatoms independently selected from the group consisting of N, O, S, Se and Si. The process includes contacting a carbonyl compound of Formula (1) and a nitroso compound of Formula (2) in the presence of a chiral catalyst.
    Type: Application
    Filed: February 5, 2014
    Publication date: August 14, 2014
    Applicant: Nanyang Technological University
    Inventors: Guofu ZHONG, Min LU, Di ZHU, Pei Juan CHUA, Bin TAN
  • Patent number: 8784684
    Abstract: A compound which has a benzoxazinone ring and an aromatic ring that directly bonds to the benzoxazinone ring, and has a mesogenic core substituted by a substituent having a polymerizable functional group is excellent in terms of durability, colorless, and exhibits a high ?n while having an azomethine bond.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: July 22, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Satoshi Shimamura, Mitsuyoshi Ichihashi
  • Publication number: 20140127240
    Abstract: The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.
    Type: Application
    Filed: April 20, 2012
    Publication date: May 8, 2014
    Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbH
    Inventors: Hans-Georg Lerchen, Lars Linden, Sherif El Sheikh, Jörg Willuda, Charlotte C. Kopitz, Joachim Schuhmacher, Simone Greven, Christoph Mahlert, Beatrix Stelte-Ludwig, Sven Golfier, Rudolf Beier, Iring Heisler, Axel Harrenga, Karl-Heinz Thierauch, Sandra Bruder, Heike Petrul, Hannah Jörißen, Sandra Brokowski
  • Patent number: 8680335
    Abstract: Disclosed is a process of enantioselectively forming an aminoxy compound of Formula (3) In formula (3) R1 is one of an aliphatic group and an alicyclic group. R2 is one of hydrogen, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group and an arylalicyclic group. R3 is one of hydrogen, halogen, hydroxyl, and an aliphatic group with a main chain having 1 to about 10 carbon atoms. The respective aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic groups of R1, R2, and R3 comprise 0 to about 3 heteroatoms independently selected from the group consisting of N, O, S, Se and Si. The process includes contacting a carbonyl compound of Formula (1) and a nitroso compound of Formula (2) in the presence of a chiral catalyst.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: March 25, 2014
    Assignee: Nanyang Technological University
    Inventors: Guofu Zhong, Min Lu, Di Zhu, Pei Juan Chua, Bin Tan
  • Patent number: 8633183
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Siegfried Schneider, Dirk Kessler, Lars van der Veen, Tobias Wunberg
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Publication number: 20130324412
    Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.
    Type: Application
    Filed: August 8, 2013
    Publication date: December 5, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
  • Publication number: 20130310365
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 21, 2013
    Applicant: Janssen Pharmaceutical NV
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
  • Patent number: 8580778
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: November 12, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Mario Jeske, Ingo Flamme, Friederike Stoll, Hartmut Beck, Metin Akbaba
  • Patent number: 8580956
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: November 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
  • Patent number: 8575391
    Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
    Type: Grant
    Filed: April 1, 2010
    Date of Patent: November 5, 2013
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Yoshiaki Isshiki, Yasunori Kohchi, Eisaku Mizuguchi, Hitoshi Iikura, Yasuaki Matsubara, Shinji Tsujii, Nobuo Shimma, Masanori Miwa, Satoshi Aida, Masami Kohchi, Takeshi Murata, Kosuke Aso
  • Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Patent number: 8536328
    Abstract: The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: September 17, 2013
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Publication number: 20130237522
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
  • 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: 8476257
    Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Grant
    Filed: December 3, 2008
    Date of Patent: July 2, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
  • Publication number: 20130158000
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: December 14, 2012
    Publication date: June 20, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventor: BAYER INTELLECTUAL PROPERTY GmbH
  • Patent number: 8450485
    Abstract: Novel benzoxazole derivatives are provided to reduce driving voltage of light-emitting elements, and to reduce power consumption of light-emitting elements, light-emitting devices, and electronic devices. A benzoxazole derivative represented by the general formula (G1) is provided. Since the benzoxazole derivative represented by the general formula (G1) has an electron-injecting property, the benzoxazole derivative can be suitably used for light-emitting elements, light-emitting devices, and electronic devices.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: May 28, 2013
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Sachiko Kawakami, Hiroko Nomura, Takahiro Ushikubo, Satoshi Seo
  • Publication number: 20130116236
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: November 6, 2012
    Publication date: May 9, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8426403
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: April 23, 2013
    Inventors: Zhaoning Zhu, William J. Greenlee, Xianhai Huang, Brian A. McKittrick, John W. Clader, Mark D. McBriar, Anandan Palani
  • Patent number: 8344136
    Abstract: The present invention relates to a process for the preparation of Brinzolamide, or 2H-thieno[3,2-e]-1,2-thiazin-6-sulfonamide, 4-(ethyl amino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)-via intermediates 2,3-dihydro-4H-thieno[3,2-e]-1,2-thiazin-4-ones, 1,1-dioxide. Further objects of the present invention are the intermediates mentioned above and other intermediates of the synthesis.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: January 1, 2013
    Assignee: PHF S.A.
    Inventors: Alessandro Falchi, Ottorino De Lucchi, Andrea Castellin
  • Publication number: 20120329787
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein Q, Z, R2, R3 and R4 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: June 22, 2011
    Publication date: December 27, 2012
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventor: THOMAS MARTIN STEVENSON
  • Publication number: 20120309752
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, Y1, Y2, Y3, G, J, X1 and X2 are as defined in the disclosure.
    Type: Application
    Filed: January 7, 2011
    Publication date: December 6, 2012
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Andris Juris Liepa, Robert James Pasteris, Thomas Martin Stevenson
  • Publication number: 20120264755
    Abstract: The present application discloses a compound of the formula (I) wherein Q is optionally substituted pyridyl; p is 0-6. Y is formulae (i), (ii) and (iii) where X is ?O, ?S and ?N—CN, r is 1-12, R is —Z-A, Z is a single bond, —S(?O)2—, >P?O, >C?O, —C(?O)NH—, and —C(?S)NH—; and A is hydrogen, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, and heteroaryl; B is a single bond, —NRN—, —S(?O)2— and —O—; wherein RN is selected from hydrogen, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, and heteroaryl; s is 0-6; and Cy is aryl, cycloalkyl, heterocyclyl, and heteroaryl. The compounds are useful for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT).
    Type: Application
    Filed: June 9, 2010
    Publication date: October 18, 2012
    Applicant: TopoTarget
    Inventors: Mette K. Christensen, Fredrik Bjorkling
  • Patent number: 8268754
    Abstract: There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted dihydroazole compound of General Formula (1) or a salt thereof: where A1, A2, A3 and A4 are independently C—Y or N, A5 is —CH2—, etc., G1 is a benzene ring, etc., G2 is G2-1, G2-6, G2-9, etc., X is a halogen atom, C1-2haloalkyl, etc., Z is methyl, —NH2, etc., R1 is —C(O)R1a, etc., R1a is C1-4alkyl, etc., R2 is H, C1-4alkyl, etc., R3 is C1-2haloalkyl, etc., R4 is H, cyano, methyl, etc., m is an integer of 1, 2, 3, etc., n is an integer of 0 or 1; and a pest control agent comprising the compound or the salt thereof.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: September 18, 2012
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi Mita, Eitatsu Ikeda, Hiroaki Takahashi, Mitsuaki Komoda
  • Publication number: 20120225847
    Abstract: The present application discloses novel squaric acid derivatives of the formula A: from —C(?O)—, —S(?O)2—, —C(?S)— and —P(?O)(R5)—; B: -, —O—, —NR6— and —C(?O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankyl
    Type: Application
    Filed: June 24, 2009
    Publication date: September 6, 2012
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Publication number: 20120214783
    Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Application
    Filed: May 3, 2012
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pierre L. BEAULIEU, Pasquale FORGIONE, Alexandre GAGNON, Cedrickx GODBOUT, Marc-Andre JOLY, Montse LLINAS-BRUNET, Julie NAUD, Martin POIRIER, Jean RANCOURT
  • Patent number: 8105504
    Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula (I) wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: January 31, 2012
    Assignee: BASF SE
    Inventors: Michèle Gerster, Peter Nesvadba
  • Publication number: 20120010172
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 31, 2009
    Publication date: January 12, 2012
    Applicant: McDERMOTT WILL & EMERY LLP
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Patent number: 8088788
    Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: January 3, 2012
    Assignee: 3M Innovative Properties Company
    Inventors: Tushar A. Kshirsagar, Karl J. Manske, Larry R. Krepski, Joan T. Moseman, George W. Griesgraber, Sarah Johannessen Slania, Scott E. Langer, Philip D. Heppner
  • Patent number: 8084645
    Abstract: A compound of the present invention, or a pharmaceutically acceptable salt thereof is indicated by formula (1) below: wherein, R1, R2, R3, R4, R5, R6, Q, R8, and R9 have the same meanings as R1, R2, R3, R4, R5, R6, Q, R8, and R9 in the specification.
    Type: Grant
    Filed: September 16, 2004
    Date of Patent: December 27, 2011
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Yoshiaki Isshiki, Yasunori Kohchi, Kazuo Hattori, Nobuo Shimma, Masanori Miwa, Naohito Inagaki, Hitoshi Iikura, Yasuaki Matsubara
  • Publication number: 20110313152
    Abstract: The present invention provide a tetrazolyl oxime derivative represented by formula (1) (in formula (1), X represents a halogen atom or the like, n1 represents an integer of 0 to 5, A represents a tetrazolyl group, Het represents a group represented by formula (4) or the like, in formula (4), R represents a halogen atom or the like, n2 represents an integer of 0 to 3, Z represents a group represented by formula (a), in formula (a), R50-R53 represents a hydrogen atom or the like, n3 represents an integer of 0 to 2, n4 represents 1 or 2, n5 represents 0 or 1) or salt thereof, and a plant disease control agent containing the same as an active ingredient.
    Type: Application
    Filed: February 26, 2010
    Publication date: December 22, 2011
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Syuichi Ito, Kazushige Fujii, Hiroyasu Hosokawa, Ichirou Urihara, Atsunori Isshiki
  • Patent number: 8080605
    Abstract: Polymer-filler coupling compounds with the formula B-A-Sx—N are claimed. In these compounds, B is an azaheterocyclic oxygen or sulfur containing moiety, or an allyltin moiety; Sx is a polysulfide, where x is between 2 and about 10; A is a linking atom or group that forms a bridge between B and Sx; and N is a blocking group. Sx can be a disulfide. N can be a conventional blocking group or other group such as -A-B. Methods for using the polymer-filler coupling compounds to modify polymers containing unsaturated carbon-carbon bonds and promote filler dispersion are also claimed. Additionally, vulcanizable rubber compositions containing the polymer-filler coupling compounds and methods for making vulcanized rubber compositions using the polymer-filler coupling compounds are also claimed.
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: December 20, 2011
    Assignee: Bridgestone Corporation
    Inventors: Yasuo Fukushima, William L. Hergenrother, Russell W. Koch
  • Patent number: 8067407
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: November 29, 2011
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Mario Jeske, Ingo Flamme, Friederike Stoll, Hartmut Beck, Metin Akbaba
  • Patent number: 8053572
    Abstract: The present invention relates to a process for preparing known fungicidally effective alkylanilides from acid chlorides and aminoacetophenone via hydroxyalkyl-substituted carboxanilides, alkenylanilides and benzoxazine derivatives.
    Type: Grant
    Filed: March 1, 2006
    Date of Patent: November 8, 2011
    Assignee: Bayer CropScience AG
    Inventor: Alexander Straub
  • Publication number: 20110245156
    Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.
    Type: Application
    Filed: December 9, 2009
    Publication date: October 6, 2011
    Applicant: CYTOKINE PHARMASCIENCES, INC.
    Inventor: Thais M. Sielecki-Dzurdz
  • Patent number: 8026057
    Abstract: Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.
    Type: Grant
    Filed: June 27, 2008
    Date of Patent: September 27, 2011
    Assignee: Affymetrix, Inc.
    Inventors: Glenn Hugh McGall, Anthony Dale Barone
  • Publication number: 20110224429
    Abstract: Disclosed is a process of enantioselectively forming an aminoxy compound of Formula (3) In formula (3) R1 is one of an aliphatic group and an alicyclic group. R2 is one of hydrogen, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group and an arylalicyclic group. R3 is one of hydrogen, halogen, hydroxyl, and an aliphatic group with a main chain having 1 to about 10 carbon atoms. The respective aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic groups of R1, R2, and R3 comprise 0 to about 3 heteroatoms independently selected from the group consisting of N, O, S, Se and Si. The process includes contacting a carbonyl compound of Formula (1) and a nitroso compound of Formula (2) in the presence of a chiral catalyst.
    Type: Application
    Filed: May 18, 2010
    Publication date: September 15, 2011
    Applicant: Nanyang Technological University
    Inventors: Guofu Zhong, Min Lu, Di Zhu, Pei Juan Chua, Bin Tan
  • Patent number: 7998951
    Abstract: The invention encompasses compounds of Formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
    Type: Grant
    Filed: March 3, 2008
    Date of Patent: August 16, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kap-Sun Yeung, John F. Kadow
  • Patent number: 7947802
    Abstract: Benzoxazine monomers comprising at least one pendant group are described. (Co)Polymers comprising at least one benzoxazine monomer having at least one pendant group are also described. In a preferred embodiment, the pendant group is located in a side chain of the benzoxazine monomer or polymer. Methods for preparing the benzoxazine monomers and polymers are described. Compositions comprising the benzoxazine monomers and polymers have numerous uses including optical materials, and in electronic materials as electrically insulating materials, and as fireproof materials.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: May 24, 2011
    Assignee: Case Western Reserve University
    Inventors: Hatsuo Ishida, Pedro Velez-Herrera
  • Patent number: 7947675
    Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • Publication number: 20110105488
    Abstract: The present application relates to pyrrolidine, piperidine, and other nitrogen-containing heterocyclic derivatives and the use of these compounds for treating and preventing pam or inflammation. The analgesic compounds demonstrate efficacy in the treatment of neuropathic pain resulting from a variety of conditions such as diabetic neuropathy, HIV infections, and post-herpetic neuralgia.
    Type: Application
    Filed: March 20, 2009
    Publication date: May 5, 2011
    Applicant: Chlorion Pharma, Inc.
    Inventors: Giorgio Attardo, Sasmita Tripathy