Benzene Ring Bonded Directly To The Diazole Ring Patents (Class 548/377.1)
  • Patent number: 9376420
    Abstract: The present invention provides a 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt effectively increases the LXR transcriptional activity, and therefore can be usefully applied for preventing or treating a dysfunction in cholesterol metabolism, such as cholesterol gallstone, hyperlipidemia, or coronary atherosclerosis.
    Type: Grant
    Filed: October 23, 2013
    Date of Patent: June 28, 2016
    Assignee: YUHAN CORPORATION
    Inventors: Chan-Sun Park, Young-Hwan Kim, Gyu-Jin Lee, Youn Hur, Eun-Hye Jung, Hee-Jae Tak, Seung-Yub Shin, Ho-Jin Lee, Chun-Ho Lee, Koo-Yeon Lee
  • Patent number: 9283226
    Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ? with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: March 15, 2016
    Assignees: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hannah Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
  • Patent number: 9034911
    Abstract: The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: May 19, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Lee Alani Selvey, Marlon Carlos, Paul Maffuid, Yun Shan, William L. Betts, III, Deam Windate Given, III, Ryan M. Hart, Zezhi Jesse Shao
  • Patent number: 9023882
    Abstract: 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.
    Type: Grant
    Filed: June 12, 2012
    Date of Patent: May 5, 2015
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Publication number: 20150119395
    Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.
    Type: Application
    Filed: April 4, 2013
    Publication date: April 30, 2015
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Patent number: 9012478
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 21, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Publication number: 20150105429
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene
  • Patent number: 8993612
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: March 31, 2015
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Kanthikiran V S Varanasi, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
  • Publication number: 20150073141
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.
    Type: Application
    Filed: July 15, 2014
    Publication date: March 12, 2015
    Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter I. Dosa
  • Patent number: 8969552
    Abstract: The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH?N—, —CH?CH— or —N?CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: March 3, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry
  • Patent number: 8957094
    Abstract: A therapeutic agent or prophylactic agent has an analgesic effect on both nociceptive pain and neuropathic pain and is effective in treatment of fibromyalgia. The agent includes as an effective ingredient a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: February 17, 2015
    Assignee: Toray Industries, Inc.
    Inventors: Chihiro Yoshida, Kaoru Nakao
  • Publication number: 20150045389
    Abstract: The present invention is a screening assay for identifying inhibitors of Pseudomonas aeruginosa CFTR Inhibitory Factor as well as compounds identified by the screening assay for use in compositions and methods for ameliorating or treating a respiratory disease such as cystic fibrosis or secondary infection thereof.
    Type: Application
    Filed: April 9, 2013
    Publication date: February 12, 2015
    Inventors: Dean R. Madden, Christopher D. Bahl, Bruce D. Hammock, Christophe Morisseau
  • Publication number: 20150018337
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 29, 2014
    Publication date: January 15, 2015
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20150011527
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Application
    Filed: June 11, 2014
    Publication date: January 8, 2015
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Publication number: 20140364398
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER INC.
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Publication number: 20140323538
    Abstract: Compounds according to formula I: wherein Ar is a fused aryl group, R1 is selected from alkyl and aryl amides, CF3, and CH2OH, and R2 is selected from hydrogen, —C(?O)CH2NH2, and —C(?O)CH2CH2NH2 are described. The compounds are effective for inhibiting p21-activated kinases, and can be used for prevention and treatment of cancer.
    Type: Application
    Filed: March 31, 2014
    Publication date: October 30, 2014
    Applicant: Ohio State Innovation Foundation
    Inventors: Ching-Shih Chen, Matthew David Ringel, Motoyashi Saji, Yihui Ma
  • Publication number: 20140309200
    Abstract: The present invention comprises compounds and compositions thereof for enhanced drug delivery. Pro-drug and double pro-drug derivatives of corticosteroids non-steroid anti-inflammatory drugs (NSAIDs), and ruboxistaurin for delivery to the eye are provided. The compounds and compositions are useful for treating various ocular diseases, including ocular diseases effecting the posterior segments of the eye. In addition, the present invention is directed to particle in particle carrier formulations for sustained release of therapeutic agents.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 16, 2014
    Inventors: Uday B. Kompella, Sarath Yandrapu, Ashish Thakur
  • Patent number: 8859781
    Abstract: The present invention provides NO-releasing NONOate(nitrogen bound)sulfonamide-linked-coxib anti-cancer agents, having the structure of Formula (I): wherein R1, X, L, R2, R3, R4, and Z are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis or acne, using a compound of Formula (I).
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: October 14, 2014
    Assignee: Euclises Pharmaceuticals, Inc.
    Inventors: Eduardo J. Martinez, John J. Talley, Kevin D. Jerome, Terri L. Boehm
  • Publication number: 20140275049
    Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 18, 2014
    Inventors: Thomas John Bleisch, David Andrew Coates, Norman Earle Hughes, Scott Alan Jones, Bryan Hurst Norman
  • Publication number: 20140264166
    Abstract: Metal extractants of 2-hydroxyphenyldiazole compounds according to Formula (2): and tautomers and salts thereof, are disclosed, wherein substituents R5, R7, R9, and R10 are as defined herein.
    Type: Application
    Filed: May 27, 2014
    Publication date: September 18, 2014
    Applicant: Cytec Technology Corp.
    Inventors: John Campbell, Ronald Matthys Swart, Lucy Emeleus, Susan Owens
  • Publication number: 20140256771
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
  • Publication number: 20140243335
    Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d 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: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
  • Publication number: 20140243338
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Inventors: Mimi L. Quan, Zilun Hu, Cailan Wang
  • Publication number: 20140221448
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X 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: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Amy X. Ding
  • Patent number: 8771682
    Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: July 8, 2014
    Assignee: Technische Universtität Dresden
    Inventors: Christian Bökel, Thomas Weidemann
  • Publication number: 20140171469
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: June 19, 2014
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Patent number: 8754115
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X 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: August 31, 2011
    Date of Patent: June 17, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Jeffrey Keith Long, Paula Louise Sharpe, Amy X Ding
  • Publication number: 20140163032
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Application
    Filed: February 18, 2014
    Publication date: June 12, 2014
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: BRADLEY TEEGARDEN, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, HONNAPPA JAYAKUMAR, THUY-ANH Tran, Sonja Strah-Pleynet, Jay Xu
  • Publication number: 20140163009
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Application
    Filed: January 23, 2012
    Publication date: June 12, 2014
    Applicant: CHDI Foundation
    Inventors: Christopher A Luckhurst, Alen F Haughan, Perla Breccia, Andrew J Stott, Roland W Burli, Samantha J Hughes, Ignacio Munoz-Sanjuan, Celia Dominguez
  • Publication number: 20140155357
    Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: June 14, 2013
    Publication date: June 5, 2014
    Inventors: Paul Abato, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Mark Grier, Laura Honeyman, Mohamed Y. Ismail, Mark L. Nelson, Kwasi Ohemeng, Jingwen Pan
  • Patent number: 8741944
    Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: June 3, 2014
    Assignee: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang
  • Patent number: 8735398
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: May 27, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
  • Publication number: 20140135320
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: Jacobus Pharmaceutical Company, Inc.
    Inventors: Gavin David Heffernan, David Penman Jacobus, Kurt William Saionz, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Patent number: 8722717
    Abstract: The present invention constitutes new 3-triazolylphenyl-substituted sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, X, R1, R2 and n are as defined in the description, to their use as acaricides and insecticides for controlling animal pests, and to processes for preparing them.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: May 13, 2014
    Assignee: Bayer CropScience AG
    Inventors: Bernd Alig, Stefan Antons, Reiner Fischer, Norbert Lui, Adeline Köhler, Arnd Voerste, Ulrich Görgens
  • Publication number: 20140128408
    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 peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
    Type: Application
    Filed: January 31, 2012
    Publication date: May 8, 2014
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Jay H. Kalin, Kyle V. Butier, Joel Bergman, Wayne W. Hancock
  • Patent number: 8691806
    Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
    Type: Grant
    Filed: June 28, 2012
    Date of Patent: April 8, 2014
    Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limited
    Inventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hannah Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
  • Patent number: 8686184
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 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 process and intermediates for preparing such compounds.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: April 1, 2014
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20140066487
    Abstract: The present invention relates to novel compounds and compositions having antiviral activity. The invention also relates to methods for the therapeutic or prophylactic treatment of viral infections in mammals.
    Type: Application
    Filed: November 5, 2013
    Publication date: March 6, 2014
    Applicant: Biotron Limited
    Inventors: Gary Dinneen Ewart, Wayne Morris Best
  • Patent number: 8642625
    Abstract: A therapeutic agent or prophylactic agent is effective for therapy of urine storage disorders, by which agent improvement of side effects due to an anticholinergic action is attained as well as which agent also has an analgesic effect. The agent includes as an effective ingredient a cyclohexane derivative exemplified by the formula below, a pharmaceutically acceptable salt thereof, or a prodrug thereof.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: February 4, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Nana Hareyama, Satoru Yoshikawa, Kaoru Nakao
  • Patent number: 8642626
    Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: February 4, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto
  • Publication number: 20140024650
    Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shoji Fukumoto, Osamu Ujikawa, Shinji Morimoto, Yasutomi Asano, Satoshi Mikami, Norihito Tokunaga, Masakuni Kori, Toshihiro Imaeda, Koichiro Fukuda, Shinji Nakamura, Kouichi Iwanaga
  • Publication number: 20140018544
    Abstract: The present invention provides NO-releasing NONOate(nitrogen bound)sulfonamide-linked-coxib anti-cancer agents, having the structure of Formula (I): wherein R1, X, L, R2, R3, R4, and Z are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis or acne, using a compound of Formula (I).
    Type: Application
    Filed: July 12, 2013
    Publication date: January 16, 2014
    Inventors: Eduardo J. Martinez, John J. Talley, Kevin D. Jerome, Terri L. Boehm
  • Publication number: 20140018403
    Abstract: The present disclosure provides NO-releasing guanidine-coxib anti-cancer agents, having the structure of Formula (I): wherein R1, R11, Z and L are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis, acne, or a disease mediated by arginine deficiency using a compound of Formula (I).
    Type: Application
    Filed: July 12, 2013
    Publication date: January 16, 2014
    Inventors: Eduardo J. Martinez, John J. Talley, Terri L. Boehm
  • Publication number: 20140005231
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein L is —C(R12a)R12b—C(R13a)R13b—, wherein the carbon atom bonded to R12a and R12b is also bonded to the carboxamide nitrogen atom in Formula 1; or 1,2-phenylene optionally substituted with up to 4 substituents independently selected from halogen and C1-C2 alkyl; and A, Z, R1, R2, n, G and Q 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. Also disclosed are methods for controlling a phytophagous nematode comprising contacting the nematode or its environment with a nematocidally effective amount of a compound of Formula 1 wherein L is —C(R12a)R12b—C(R13a)R13b; and A, Z, R1, R2, n, G and Q are as defined in the disclosure.
    Type: Application
    Filed: June 19, 2013
    Publication date: January 2, 2014
    Inventors: JAMES FRANCIS BEREZNAK, Steven Gutteridge, Ravisekhara P. Reddy, Andrew Edmund Taggi, Matthew James Campbell, Moumita Kar, Johan A. J. Desaeger
  • Patent number: 8598212
    Abstract: A therapeutic agent or prophylactic agent for Alzheimer's disease has an effect to inhibit or delay the progress of Alzheimer's disease and exhibits a long-lasting therapeutic effect on Alzheimer's disease even when used for a long period of time. The therapeutic agent or prophylactic agent for Alzheimer's disease includes as an effective ingredient a cyclohexane derivative exemplified by the formula below, or a pharmaceutically acceptable salt thereof or a prodrug thereof.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: December 3, 2013
    Assignee: Toray Industries, Inc.
    Inventors: Kaoru Nakao, Yohei Miyamoto, Naohiro Yamada
  • Patent number: 8592476
    Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of ?-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: November 26, 2013
    Assignee: ProteoTech, Inc.
    Inventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan Snow, Lesley Larsen
  • Publication number: 20130296355
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8575362
    Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: November 5, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Mark S. Bednarz, Hugh Alfred Burgoon, Jr., Shinya Iimura, Ramanaiah C. Kanamarlapudi, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang
  • Publication number: 20130289004
    Abstract: A method of treating infection by Staphylococcus in a subject by administering a pharmaceutical composition including a celecoxib derivative of formula I or a pharmaceutically acceptable salt thereof is described. The preparation of numerous celecoxib derivatives for testing as potential anti-staphylococcal agents is also described.
    Type: Application
    Filed: October 31, 2011
    Publication date: October 31, 2013
    Applicant: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang, Samuel K. Kulp
  • Publication number: 20130289025
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: March 20, 2013
    Publication date: October 31, 2013
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang