Polycyclo Heterocyclic Ring System Containing Ring Nitrogen Patents (Class 548/181)
  • 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
  • Publication number: 20130274179
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.
    Type: Application
    Filed: April 11, 2013
    Publication date: October 17, 2013
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: Silas Bond, Rosliana Halim, Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding
  • Publication number: 20130274294
    Abstract: The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: December 19, 2011
    Publication date: October 17, 2013
    Inventors: David Carcache, Manuel Koller, Silvio Ofner, David Orain, Johanne Renaud
  • Patent number: 8552205
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Publication number: 20130261129
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Application
    Filed: March 29, 2013
    Publication date: October 3, 2013
    Applicant: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Wei, Lijuan Jane Wang
  • Patent number: 8546588
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: October 1, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 8546389
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: October 1, 2013
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
  • Patent number: 8546336
    Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: October 1, 2013
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Mark G. Charest, Christine Hiu-Tung Chen, Miao Dai, Feng He, Huangshu Lei, Ly Luu Pham, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming David Wang, Fan Yang, Leigh Zawel
  • Publication number: 20130253021
    Abstract: The present invention provides methods of making and using 5-(2-(indol-3-yl)-2-oxoethylidene)-3-phenyl-2-thioxothiazolidin-4-one derivatives having HIV-1 or JSP-1 inhibitory activity.
    Type: Application
    Filed: March 22, 2013
    Publication date: September 26, 2013
    Applicants: The Johns Hopkins University, Southern Methodist University
    Inventors: Edward R. Biehl, Sukanta Kamila, Ted M. Dawson
  • Patent number: 8524753
    Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.
    Type: Grant
    Filed: January 31, 2012
    Date of Patent: September 3, 2013
    Assignee: AbbVie Inc.
    Inventors: Dale J. Kempf, Charles A. Flentge, John T. Randolph, Peggy Huang, Larry L. Klein
  • Publication number: 20130203756
    Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 24, 2011
    Publication date: August 8, 2013
    Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen
  • Publication number: 20130196968
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Publication number: 20130197011
    Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Riccardo GIOVANNINI, Barbara BERTANI, Marco FERRARA, Iain LINGARD, Rocco MAZZAFERRO, Holger ROSENBROCK
  • Publication number: 20130186468
    Abstract: The photoelectric conversion device described herein includes a working electrode having a dye-supported metal oxide electrode in which a dye is supported on a metal oxide layer. The dye includes a structure represented by general formula (I) wherein A is a structure having a maximum absorption wavelength ?max of 350 to 500 nm in a methanol solution; B is a cyanine skeleton having a maximum absorption wavelength ?max of 500 to 700 nm in a methanol solution; Z1 is any one divalent linking group selected from —CONR—, —NRCO—, —SO2NR—, and —NRSO2—; R in Z1 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or an arylalkyl group having 7 to 20 carbon atoms; Y1 and Y2 are each independently an alkylene group having 1 to 8 carbon atoms, or a single bond, and may be the same or different; r is 1 or 2; m and n are each independently an integer of 0 to 2; and (m+n) is 1 or more.
    Type: Application
    Filed: September 27, 2011
    Publication date: July 25, 2013
    Applicants: ADEKA CORPORATION, TDK CORPORATION
    Inventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Yohei Aoyama, Kensaku Akimoto, Tatsuya Ishida, Toru Yano
  • Publication number: 20130178505
    Abstract: Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.
    Type: Application
    Filed: June 28, 2011
    Publication date: July 11, 2013
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Michael Chorev, Bertal Huseyin Aktas, Jose A. Halperin, Gerhard Wagner
  • Publication number: 20130165446
    Abstract: The present invention addresses the problem of finding a compound having both PPAR activation activity and angiotensin receptor antagonistic activity. The present invention is a benzo- or pyrido-imidazole derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, or a ester or amide thereof (where A is biphenyl methyl-imidazolyl, biphenyl methyl-benzimidazolyl, or the like, B is divalent benzimidazolyl or the like, C is carboxyl or the like, E is divalent phenyl, naphthyl, or the like, G is a dangling bond, oxygen, or the like, Q is oxygen or sulfur, n is an integer from 1 to 6, p is an integer from 1 to 6, V is a dangling bond, oxygen, or the like, and R is hydrogen, alkyl, or the like).
    Type: Application
    Filed: May 11, 2011
    Publication date: June 27, 2013
    Inventors: Takashi Fujita, Hiroyoshi Horikoshi, Michael Anthony Cawthorne
  • Patent number: 8470817
    Abstract: Compounds for treating, preventing or managing cancer are disclosed. Also provided are methods for using the compounds in treatment of various cancers. Also provided are methods of treatment using the compounds together with another chemotherapy, radiation therapy, hormonal therapy, biological therapy, or immunotherapy. Pharmaceutical compositions suitable for use in the methods are also disclosed.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: June 25, 2013
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventor: Anantha Sudhakar
  • Patent number: 8445690
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: May 21, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
  • Publication number: 20130123243
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Application
    Filed: October 18, 2012
    Publication date: May 16, 2013
    Inventor: Celtaxsys, Inc.
  • Publication number: 20130116240
    Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
    Type: Application
    Filed: September 26, 2012
    Publication date: May 9, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventor: Japan Tobacco Inc.
  • Patent number: 8436023
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z 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: Grant
    Filed: June 9, 2011
    Date of Patent: May 7, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
  • Patent number: 8426604
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: April 23, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
  • Patent number: 8420679
    Abstract: Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotrophin releasing factor (CRF) antagonists.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: April 16, 2013
    Assignee: Sanofi
    Inventors: Evelyne Fontaine, Michel Geslin, Danielle Gully, Antoine Pradines, Pierre Roger
  • Patent number: 8415480
    Abstract: The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: April 9, 2013
    Assignee: Merck Serono SA
    Inventors: Patrick Naxos Page, Catherine Jorand-Lebrun, Anna Quattropani, Vincent Pomel, Matthias Schwarz, Estelle Hamelin, Russell J. Thomas
  • Patent number: 8410281
    Abstract: Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: April 2, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Hidekazu Matsuya, Hiroki Okada
  • Patent number: 8404859
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: March 26, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
  • Patent number: 8394843
    Abstract: Compounds are provided which have the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture which contain such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to activate glucokinase.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: March 12, 2013
    Assignee: Takeda California, Inc.
    Inventors: Jun Feng, Stephen L. Gwaltney, Robert J. Skene, Mingnam Tang, Sheldon X. Cao, David J. Hossfield, Jeffrey A. Stafford
  • Publication number: 20130052138
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Application
    Filed: March 27, 2012
    Publication date: February 28, 2013
    Applicant: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Publication number: 20130053403
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.
    Type: Application
    Filed: April 25, 2011
    Publication date: February 28, 2013
    Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
  • Patent number: 8383831
    Abstract: The dye for a dye-sensitized solar cell, which dye is a compound classified into melocyanine dyes and has a structure in which an electron donor unit and an electron acceptor unit are connected with conjugated double bonds, provided by this invention, has excellent photoelectric conversion efficiency and excellent durability, and according to this invention, there can be provided a semiconductor electrode sensitized by the dye and a dye-sensitized solar cell using the semiconductor electrode.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: February 26, 2013
    Assignee: Mitsubishi Paper Mills Limited
    Inventors: Masakazu Takata, Koichi Sumioka, Takaaki Kozai
  • Patent number: 8362032
    Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: January 29, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Aarti Sameer Kawatkar, Tara Whitney, Timothy D. Neubert, Nicole Hilgraf, Andreas P. Termin, Esther Martinborough
  • Patent number: 8362035
    Abstract: This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: January 29, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thilo Berkenbusch, Carl Alan Busacca, Burkhard Jaeger, Richard J. Varsolona
  • Publication number: 20130012719
    Abstract: Azolines are oxidized in the presence of a copper-containing catalyst to azoles in the presence of molecular oxygen. A synthetic scheme converting azolines azoles is also provided.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: University of Southern California
    Inventors: Travis J. Williams, Anna C. Dawsey, Vincent Li, Kimberly C. Hamilton, Jianmei Wang
  • Publication number: 20130005663
    Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 3, 2013
    Applicant: NOVARTIS AG
    Inventors: Mark G. CHAREST, Christine Hiu-Tung CHEN, Zhuoliang CHEN, Miao DAI, Feng HE, Huangshu LEI, Ly Luu PHAM, Sushil Kumar SHARMA, Christopher Sean STRAUB, Run-Ming David WANG, Fan YANG, Leigh ZAWEL
  • Patent number: 8344010
    Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: January 1, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: V. S. Prasadarao Lingam, Abraham Thomas, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 8344018
    Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: January 1, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Chandrasekar Venkataramani
  • Publication number: 20120316148
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.
    Type: Application
    Filed: June 7, 2012
    Publication date: December 13, 2012
    Applicant: Dynamix Pharmaceuticals LTD.
    Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
  • Patent number: 8329913
    Abstract: An object of the present invention is to provide novel carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof having an excellent adipose tissue weight reducing effect, hypoglycemic effect, and hypolipidemic effect, which are useful as a preventive and/or therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral adiposity, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and the like.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: December 11, 2012
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Masakazu Murata, Yoshihiko Itokazu, Ryu Nakao
  • 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: 20120309738
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 6, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
  • Patent number: 8318948
    Abstract: Disclosed is a novel fluorene derivative and an organic electronic device using the same. The organic electronic device has excellent efficiency, driving voltage, and a lifespan.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: November 27, 2012
    Assignee: LG Chem, Ltd.
    Inventors: Jae-Soon Bae, Dong-Hoon Lee, Dae-Woong Lee, Sung-Kil Hong, Hyun Nam, Chang-Hwan Kim
  • Patent number: 8318774
    Abstract: 3-((Thiazol-2-yl)amino)propylproiolamide compounds of the formula I: wherein the variables are as defined herein, are useful to prevent or treat a disease or disorder involving mGluR5 receptor regulation. Also disclosed are pharmaceutical compositions containing the compounds and methods of making the compounds.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: November 27, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Michael Haurand, Klaus Schiene, Sven Kühnert, Melanie Reich
  • Patent number: 8314247
    Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: November 20, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
  • Patent number: 8309586
    Abstract: Disclosed are new compounds of formula (1) exhibiting excellent activity for glucokinase, pharmaceutical compositions having the same as an active ingredient, and a method of using the same as an active ingredient for lowering blood glucose level: in which the substituents are as defined herein.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: November 13, 2012
    Assignee: LG Life Sciences Ltd.
    Inventors: Soon Ha Kim, Sung Bae Lee, Seung Hyun Yoon, Mi Kyoung Cho, Kyoung Hee Kim, Heui Sul Park, Hyoung Jin Kim
  • Patent number: 8303863
    Abstract: A fine particle which contains a compound represented by formula (1): wherein R1a and R1b may be the same or different, and each independently represent an alkyl group, an aryl group, or a heteroaryl group; R2 and R3 each independently represent a hydrogen atom or a substituent, and at least one of R2 and R3 is an electron withdrawing group; R2 may be bonded to R3 to form a ring; R4 represents a hydrogen atom, an alkyl group, an aryl group, a heteroaryl group, a substituted boron, or a metal atom; and R4 may be covalently bonded or coordinately bonded to at least one among R1a, R1b and R3.
    Type: Grant
    Filed: March 27, 2009
    Date of Patent: November 6, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Kazumi Nii, Shunya Kato, Yoshihiro Jimbo
  • Publication number: 20120264760
    Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
    Type: Application
    Filed: June 6, 2012
    Publication date: October 18, 2012
    Applicants: University of Georgia Research Foundation, Inc., Brandeis University
    Inventors: Lizbeth K. Hedstrom, Boris Striepen
  • Publication number: 20120263712
    Abstract: The present invention relates to a compound of formula (I) or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
    Type: Application
    Filed: June 5, 2012
    Publication date: October 18, 2012
    Applicant: NOVARTIS AG
    Inventors: Robin Alec FAIRHURST, Vito GUAGNANO, Patricia IMBACH, Giorgio CARAVATTI, Pascal FURET
  • Patent number: 8283474
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: October 9, 2012
    Assignee: Glaxo Group Limited
    Inventors: Anna Maria Capelli, Giovanna Tedesco
  • Publication number: 20120252740
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.
    Type: Application
    Filed: July 2, 2010
    Publication date: October 4, 2012
    Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
  • Publication number: 20120252853
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: March 30, 2012
    Publication date: October 4, 2012
    Applicant: H. Lundbeck A/S
    Inventors: Anette Graven Sams, Jørgen Eskildsen, Jesper Frank Bastlund