1,2,4-triazoles (including Hydrogenated) Patents (Class 546/272.4)
  • Patent number: 8835464
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: April 5, 2013
    Date of Patent: September 16, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Publication number: 20140256734
    Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 11, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: John David Lawson, Mark Sabat, Nicholas Scorah, Christopher Smith, Phong H. Vu, Haixia Wang
  • Publication number: 20140242028
    Abstract: The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
    Type: Application
    Filed: January 21, 2014
    Publication date: August 28, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Joseph Anthony Bilotta, Zhi Chen, Qingjie Ding, Shawn David Erickson, Eric Mertz, Robert James Weikert
  • Publication number: 20140242135
    Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: April 25, 2012
    Publication date: August 28, 2014
    Applicant: Vanderbilt University
    Inventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
  • Patent number: 8815910
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Publication number: 20140228411
    Abstract: The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.
    Type: Application
    Filed: April 16, 2014
    Publication date: August 14, 2014
    Applicant: Gilead Sciences, Inc.
    Inventor: Gregory Notte
  • Publication number: 20140228412
    Abstract: The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.
    Type: Application
    Filed: April 16, 2014
    Publication date: August 14, 2014
    Applicant: Gilead Sciences, Inc.
    Inventor: Gregory Notte
  • Publication number: 20140228215
    Abstract: This document discloses pesticidal compostions comprising molecules having the following formulas: and processes related thereto.
    Type: Application
    Filed: April 23, 2014
    Publication date: August 14, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Gary D. Crouse, William T. Lambert, Thomas C. Sparks, Vidyadhar B. Hegde
  • Publication number: 20140221332
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Application
    Filed: May 25, 2012
    Publication date: August 7, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat
  • Patent number: 8796271
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Patent number: 8796314
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, CY, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
  • Publication number: 20140200134
    Abstract: The present invention relates to anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: July 17, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Prashant Deshmukh, Karsten Koerber, Wolfgang Von Deyn, Markus Kordes, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Patent number: 8778974
    Abstract: The present invention relates to 1-aryl-3-aniline-5-alkyl-1,2,4-triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: July 15, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, Johannes Wilhelmus John F. Thuring, Pauline Carol Stanislawski, Wei Zhuang, Yves Emiel Maria Van Roosbroeck, Frans Alfons Maria Van Den Keybus
  • Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Patent number: 8748340
    Abstract: This document discloses pesticidal compostions comprising molecules having the following formulas: and processes related thereto.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: June 10, 2014
    Assignee: Dow AgroSciecnes LLC.
    Inventors: Gary D. Crouse, William Thomas Lambert, Thomas C. Sparks, Vidyadhar B. Hegde
  • Publication number: 20140155370
    Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
    Type: Application
    Filed: June 28, 2013
    Publication date: June 5, 2014
    Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
  • Patent number: 8742119
    Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: June 3, 2014
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Publication number: 20140142143
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: May 22, 2014
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Patent number: 8729271
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 20, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun
  • Publication number: 20140128611
    Abstract: In order to produce an intermediate from which a cyclic alcohol compound can be stereoselectively obtained, a method for producing an oxetane compound according to the present invention includes the step of reacting, with a cyanide salt, a compound represented by Formula (I): wherein R1 is selected from a hydrogen atom and an alkyl group optionally having a substituent; X1 is selected from a halogen atom and —OSO2R3 where R3 is selected from an alkyl group optionally having a substituent, a phenyl group, and a naphthyl group; and a ring Z1 represents a cyclic hydrocarbon optionally having a substituent, to obtain a compound represented by Formula (II):
    Type: Application
    Filed: June 6, 2012
    Publication date: May 8, 2014
    Applicant: KUREHA CORPORATION
    Inventors: Kazuhiko Sunagawa, Toru Yamazaki, Emiko Obata
  • Patent number: 8710055
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A, X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: April 29, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Steffen Steurer
  • Patent number: 8703761
    Abstract: The invention relates to compounds of formula (I): where A is an optionally substituted heteroaryl, useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: April 22, 2014
    Assignee: Novartis AG
    Inventors: Cornelia Jutta Forster, Young-Shin Kwak, Katsumasa Nakajima, Bing Wang
  • Publication number: 20140088071
    Abstract: Compounds of Formula (IA) and Formula (IB) are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Application
    Filed: November 2, 2011
    Publication date: March 27, 2014
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Takashi Nakai, Thomas Wai-Ho Lee, Charles Kim, Joel Moore, Nicholas Robert Perl, Jason Rohde
  • Publication number: 20140088148
    Abstract: Small molecule inhibitors of XBP1 splicing by IRE1 are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.
    Type: Application
    Filed: April 4, 2012
    Publication date: March 27, 2014
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Sivanesan Dakshanamurthy, Milton L. Brown, Robert Clarke, Ayesha N. Shahjahan, Jaqueline Smith
  • Patent number: 8680269
    Abstract: The present invention concerns novel heteroaryl-N-aryl thiosemicarbazones and their use in pest control, as insecticides and aca?cides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: March 25, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Annette V. Brown, Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Emily M. Rigsbee, William T. Lambert, Noormohamed M. Niyaz
  • Patent number: 8674109
    Abstract: The present invention concerns novel heteroaryl-N-aryl carbamates and their use in pest control, as insecticides and acaricides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: March 18, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: William T. Lambert, Gary D. Crouse, Thomas C. Sparks, Denise P. Cudworth
  • Patent number: 8658798
    Abstract: Triazolylpyridine ketones expressed by the following formula (I) and use thereof as herbicides.
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: February 25, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Andreas Van Almsick, Shinichi Narabu, Yoshitaka Sato, Kei Domon, Koichi Araki, Shinichi Shirakura, Seiji Ukawa, Teruyuki Ichihara, Chieko Ueno
  • Publication number: 20140045902
    Abstract: The present invention relates to a compound of formula 1 or 2 wherein R1 represents straight-chain or branched C2-C8 alkyl, C2-C8 alkenyl, optionally substituted by at least one substituent selected from the group consisting of hydroxyl, amino or C1-C6 alkyl amino group, or C2-C4 alkynyl, optionally substituted by at least one substituent selected from the group consisting of hydroxyl, amino or C1-C6 alkyl amino group; and R2 represents hydroxyl, C1-C6 alkyl, C1-C6 alkylcarbonyl, di(C1-C6-alkyl)aminomethyl, C3-C6 heterocyclylmethyl or arylaminomethyl, wherein the aryl group is optionally substituted by at least one substituent selected from the group consisting of halogens and C1-C6 alkoxy as well as associated pharmaceutical compositions and uses of the compound or composition in therapy, in particular for the treatment of a disorder or a disease susceptible to inhibition of COX-2.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Applicant: KING SAUD UNIVERSITY
    Inventors: Fars K. Alanazi, Awwad A. Radwan, Ibrahim A. Alsarra
  • Publication number: 20140046053
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 13, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Publication number: 20140042420
    Abstract: It is an object of the present invention to provide a novel triazole derivative. Further, it is another object of the present invention to provide a light-emitting element having high luminous efficiency with the use of the novel triazole derivative. Moreover, it is still another object of the present invention to provide a light-emitting device and electronic devices which have low power consumption. A light-emitting element having high luminous efficiency can be manufactured with the use of a triazole derivative which is a 1,2,4-triazole derivative, in which an aryl group or a heteroaryl group is bonded to each of 3-position, 4-position, and 5-position, and in which any one of the aryl group or heteroaryl group has a 9H-carbazol-9-yl group.
    Type: Application
    Filed: October 28, 2013
    Publication date: February 13, 2014
    Applicant: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko NOMURA, Sachiko KAWAKAMI, Nobuharu OHSAWA, Satoshi SEO
  • Publication number: 20140038936
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: May 7, 2013
    Publication date: February 6, 2014
    Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
  • Patent number: 8642774
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • Publication number: 20140031374
    Abstract: The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear ?-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.
    Type: Application
    Filed: December 8, 2011
    Publication date: January 30, 2014
    Applicant: OSLO University Hospital, HF
    Inventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss, Andrey Edward Voronkov
  • Publication number: 20140024648
    Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Application
    Filed: March 6, 2012
    Publication date: January 23, 2014
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Marjo Pihlavisto, David Smith, Auni Juhakoski, Ferenc Fulop, Laszlo Lazar, Istvan Szatmari, Ferenc Miklos, Zsolt Szakonyi, Lorand Kiss, Marta Palko
  • Publication number: 20140024680
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 23, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventor: Bayer Intellectual Property GmbH
  • Patent number: 8623898
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: January 7, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Akito Yasuhara, Shuji Yamamoto, Hiroshi Ohta, Yoshihisa Shirasaki, Kazunari Sakagami, Masato Hayashi, Tsuyoshi Shibata, Youichi Shimazaki, Yuko Araki, Kumi Abe, Xiang-Min Sun
  • Patent number: 8618285
    Abstract: Novel triazole derivatives of the formula (I), in which R1-R6, and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: January 25, 2006
    Date of Patent: December 31, 2013
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • Publication number: 20130338105
    Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 19, 2013
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Publication number: 20130324560
    Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.
    Type: Application
    Filed: August 7, 2013
    Publication date: December 5, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
  • Patent number: 8598360
    Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: December 3, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, Jr., Gregory Notte
  • Patent number: 8592056
    Abstract: It is an object of the present invention to provide a novel triazole derivative. Further, it is another object of the present invention to provide a light-emitting element having high luminous efficiency with the use of the novel triazole derivative. Moreover, it is still another object of the present invention to provide a light-emitting device and electronic devices which have low power consumption. A light-emitting element having high luminous efficiency can be manufactured with the use of a triazole derivative which is a 1,2,4-triazole derivative, in which an aryl group or a heteroaryl group is bonded to each of 3-position, 4-position, and 5-position, and in which any one of the aryl group or heteroaryl group has a 9H-carbazol-9-yl group.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: November 26, 2013
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Publication number: 20130310378
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: April 23, 2013
    Publication date: November 21, 2013
    Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co KG
    Inventors: AbbVie Deutschland GmbH & Co KG, AbbVie Inc.
  • Publication number: 20130303493
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 14, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 8580961
    Abstract: A 2-phenyl-6-azolylpyridine-based ligand is represented by the following formula (I): wherein, X represents nitrogen or C—R10; R1, R2, R3, R4, R5, R6, R7, R8 and R10 independently represent hydrogen, halogen, a cyano group, an amino group, an optionally substituted aryl group, an optionally substituted heteroaryl group, sulfate, —COOH, an alkoxy group, a carbonyl group, a C1-C10 haloalkyl group, a C1-C12 alkyl group, a C2-C10 alkenyl group, a C2-C10 alkynyl group, a C3-C20 cycloalkyl group, a C3-C20 cycloalkenyl group, a C1-C20 heterocycloalkyl group, or a C1-C20 heterocycloalkenyl group; and R9 represents hydrogen or alkali metal.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 12, 2013
    Assignee: National Tsing Hua University
    Inventors: Yun Chi, Chien-Wei Hsu, Shu-Te Ho
  • Publication number: 20130296378
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: April 5, 2013
    Publication date: November 7, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Publication number: 20130296382
    Abstract: Heteroaromatic compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Jason Burch, Bernard Cote, Natalie Nguyen, Chun Sing Li, Miguel St-Onge, Danny Gauvreau
  • Publication number: 20130296168
    Abstract: Triazolylpyridine ketones expressed by the following formula (1) and use thereof as herbicides.
    Type: Application
    Filed: May 22, 2013
    Publication date: November 7, 2013
    Inventors: Andreas Van Almsick, Shinichi Narabu, Yoshitaka Sato, Kei Domon, Koichi Araki, Shinichi Shirakura, Seiji Ukawa, Teruyuki Ichihara, Chieko Ueno
  • Publication number: 20130288893
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Application
    Filed: March 7, 2013
    Publication date: October 31, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Ann M. Buysse, Noormohamed M. Niyaz, David A. Demeter, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel Knueppel, Akshay Patny, Negar Garizi, Paul Renee LePlae, JR., Frank Wessels, Ronald Ross, JR., Carl DeAmicis, Peter Borromeo
  • Publication number: 20130291227
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Application
    Filed: March 7, 2013
    Publication date: October 31, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Ann M. Buysse, Noormohamed M. Niyaz, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel Knueppel, David A. Demeter, Akshay Patny, Negar Garizi, Paul Renee LePlae, JR., Frank Wessels
  • Publication number: 20130274256
    Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.
    Type: Application
    Filed: October 11, 2012
    Publication date: October 17, 2013
    Applicant: SEQUOIA SCIENCES, INC.
    Inventor: Sequoia Sciences, Inc.