Ring Sulfur In The Additional Hetero Ring Patents (Class 514/342)
  • DEUTERIUM-ENRICHED PIOGLITAZONE
    Publication number: 20140243377
    Abstract: The present application describes deuterium-enriched pioglitazone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: DEUTERX, LLC
    Inventor: Anthony W. Czarnik
  • SUBSTITUTED AROMATIC COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES
    Publication number: 20140242120
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Yu Xie
  • COMPOUNDS, COMPOSITIONS, AND METHODS FOR PREVENTING METASTASIS OF CANCER CELLS
    Publication number: 20140242026
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Inventors: Robert Shalwitz, Kevin Gene Peters
  • Compounds and methods for inhibiting phosphate transport
    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
  • Respiratory disease treatment
    Patent number: 8815837
    Abstract: There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and/or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and kit.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: August 26, 2014
    Assignee: Pulmagen Therapeutics (Inflammation) Limited
    Inventors: Harry Finch, Craig Fox, Mohammed Sajad, Monique Bondil Van Niel, Andrew Forrest
  • RXR AGONIST COMPOUNDS AND METHODS
    Publication number: 20140235676
    Abstract: A method of treating a psychiatric or cognitive developmental disorder in a subject, includes administering to the subject a therapeutically effective amount of at least one RXR agonist.
    Type: Application
    Filed: October 15, 2012
    Publication date: August 21, 2014
    Inventor: Gary E. Landreth
  • Methods and Compositions for the Treatment of Body Weight Related Disorders
    Publication number: 20140235646
    Abstract: The present invention relates to methods for reducing body weight in an animal in need thereof via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. Also provided are methods for increasing thermogenesis without reducing lean body mass during weight loss in an animal by administering of a therapeutically effective amount of the compounds described.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 21, 2014
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Al-Elheiga, Mizuki Watanabe
  • COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS
    Publication number: 20140235637
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: InterMune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • PESTICIDAL COMPOSITION COMPRISING A PYRIDYLETHYLBENZAMIDE DERIVATIVE AND AN INSECTICIDE COMPOUND
    Publication number: 20140235442
    Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Inventors: Heike HUNGENBERG, Gilbert LABOURDETTE, Albert SCHIRRING, Burkhard SCHUETZ, Anne SUTY-HEINZE, Wolfgang THIELERT, Martin VAUPEL
  • Pyridine Derivatives
    Publication number: 20140235652
    Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.
    Type: Application
    Filed: November 13, 2013
    Publication date: August 21, 2014
    Applicant: Endo Pharmaceuticals Inc.
    Inventors: Roger A. Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
  • PYRIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE
    Publication number: 20140235608
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 26, 2012
    Publication date: August 21, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: John Lloyd, Jeniffer X. Qiao, Heather Finlay, James Neels, Zulan Pi, Carol Hui Hu, Tammy C. Wang
  • Selective subtype alpha 2 adrenergic agents and methods for use thereof
    Patent number: 8809379
    Abstract: The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: August 19, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Ling Li, Wenkui K. Fang, Janet A. Takeuchi, Smita Bhat
  • Metalloenzyme inhibitor compounds
    Patent number: 8809378
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: August 19, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
  • Deubiquitinase inhibitors and methods for use of the same
    Patent number: 8809377
    Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: August 19, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
  • Formulation
    Patent number: 8808720
    Abstract: A product comprising microcapsules which themselves comprise (a) a polymeric shell; and (b) a core which comprises (i) a solid agrochemical dispersed in a matrix and (ii) a water-immiscible liquid characterized in that the matrix is distributed non-continuously throughout the water-immiscible liquid.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: August 19, 2014
    Assignee: Syngenta Limited
    Inventors: Patrick Joseph Mulqueen, Anne Waller, Julia Lynne Ramsay, Geoffrey William Smith
  • TETRASUBSTITUTED CYCLOHEXYL COMPOUNDS AS KINASE INHIBITORS
    Publication number: 20140228363
    Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
  • THIAZOLE DERIVATIVES AND USE THEREOF
    Publication number: 20140228365
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: Merck Serono S.A.
    Inventors: Anna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Heterocyclic Compounds for the Treatment of CF
    Publication number: 20140228376
    Abstract: The present invention provides pyridin-oxadiazole/thiadiazole derivatives of Formula I wherein A is N or CR 4a; and (ii) or (iii) which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Kamlesh Jagdis Bala, Rebecca Butler, Stephen Paul Collingwood, Edward Charles Hall, Lee Edwards, Darren Mark Legrand, Katrin Spiegel
  • Thiazole derivatives and use thereof
    Patent number: 8802861
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: January 11, 2005
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate
    Publication number: 20140221433
    Abstract: The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions.
    Type: Application
    Filed: September 26, 2012
    Publication date: August 7, 2014
    Applicant: AICURIS GMBH & CO. KG
    Inventors: Wilfried Schwab, Alexander Birkmann, Kurt Vogtli, Dieter Haag, Andreas Lender, Alfons Grunenberg, Birgit Keil, Joachim Reshe
  • COMPOSITION AND METHOD FOR CONTROLLING HARMFUL ARTHROPODS
    Publication number: 20140221363
    Abstract: The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof, and at least one kind of neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxiam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods.
    Type: Application
    Filed: July 20, 2012
    Publication date: August 7, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Atsushi Iwata, Chie Shimizu, Miki Suzuki
  • RAF KINASE INHIBITORS
    Publication number: 20140221374
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinase mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.
    Type: Application
    Filed: March 16, 2012
    Publication date: August 7, 2014
    Applicant: Ruga Corporation
    Inventors: Jean-Michel Vernier, Stephanie Hopkins, Pierre-Yves Bounaud, Patrick O'Connor, David Matthews, Steve Bender
  • SODIUM CHANNEL BLOCKERS REDUCE GLUCAGON SECRETION
    Publication number: 20140221286
    Abstract: It is discovered that sodium-channel blockers inhibit the secretion of glucagon from pancreatic alpha cells. The present disclosure, based on such discoveries, provides compositions and methods for the treatment of hyperglycemia and related diseases and conditions with Na-channel blockers.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 7, 2014
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Pesticidal composition comprising an alpha-alkoxyphenyl acetic acid derivative and a neonicotinoid compound
    Patent number: 8796176
    Abstract: PROBLEM Provided is a composition for controlling pests having excellent control effect for pests and a method for controlling pests. SOLUTION A composition for controlling pests comprising an ?-alkoxyphenylacetic acid compound and a neonicotinoid compound as active ingredients.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: August 5, 2014
    Assignee: Sumitomo Chemical Company, Ltd
    Inventors: Masanao Takaishi, Atsushi Iwata
  • Substituted benzamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same
    Patent number: 8796295
    Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: Grant
    Filed: September 17, 2010
    Date of Patent: August 5, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates
  • Metalloenzyme inhibitor compounds
    Patent number: 8796001
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: August 5, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
  • Method for better utilizing the production potential of transgenic plants
    Patent number: 8795701
    Abstract: The invention relates to a method for improving the utilization of the production potential of transgenic plants which comprises treating the plant with active compound combinations comprising an active compound from the group of the anthranilamides and at least one further insecticide.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer CropScience AG
    Inventors: Wolfram Andersch, Christian Funke, Heike Hungenberg, Wolfgang Thielert
  • Heteroaryls and uses thereof
    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
  • Pyrrolidine derivatives, pharmaceutical compositions and uses thereof
    Publication number: 20140213568
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: January 22, 2014
    Publication date: July 31, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • 2-alkoxy-substituted dicyanopyridines and their use
    Patent number: 8791146
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: July 29, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Walter Hübsch, Daniel Meibom, Alexandros Vakalopoulos, Barbara Albrecht-Küpper, Peter Nell, Katja Zimmermann, Frank Süβmeier, Joerg Keldenich
  • SELECTIVE SUBTYPE ALPHA 2 ADRENERGIC AGENTS AND METHODS FOR USE THEREOF
    Publication number: 20140206701
    Abstract: The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptor.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 24, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, KEN CHOW, TODD M. HEIDELBAUGH, SANTOSH C. SINHA, PHONG X. NGUYEN, SMITA S. BHAT, WENKUI K. FANG
  • CYCLIC PROTEIN TYROSINE KINASE INHIBITORS
    Publication number: 20140206691
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
  • Phenylalanine amide derivatives useful for treating insulin-related diseases and conditions
    Patent number: 8785468
    Abstract: Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: July 22, 2014
    Assignee: Amgen Inc.
    Inventors: Xiaohui Du, Zice Fu, Jonathan B. Houze, XianYun Jiao, Yong-Jae Kim, Leping Li, Jinqian Liu, Mike Elias Lizarzaburu, Julio C. Medina, Wang Shen, Simon Turcotte, Ming Yu
  • Pharmaceutical preparation of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide
    Patent number: 8784887
    Abstract: The invention relates to a pharmaceutical preparation for oral administration comprising N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide or its hydrates and/or solvates, as well as an acid, a method for its production as well as the use of this preparation for the treatment and/or prophylaxis of diseases which are caused by herpes viruses, in particular diseases which are caused by herpes simplex viruses.
    Type: Grant
    Filed: September 27, 2007
    Date of Patent: July 22, 2014
    Assignee: Aicuris GmbH & Co. KG
    Inventors: Tobias Laich, Katrin Liebelt
  • Methods and compositions for locally increasing body fat
    Patent number: 8778981
    Abstract: Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: July 15, 2014
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Pesticidal composition comprising a pyridylethylbenzamide derivative and an insecticide compound
    Patent number: 8778835
    Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: July 15, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Heike Hungenberg, Gilbert Labourdette, Albert Schirring, Burkhard Schuetz, Anne Suty-Heinze, Wolfgang Thielert, Martin Vaupel
  • Pyridinonyl PDK1 inhibitors
    Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
  • Substituted heteroaryl inhibitors of B-RAF
    Patent number: 8778929
    Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: July 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
  • Use of active substance combinations for controlling animal pests
    Patent number: 8778837
    Abstract: The invention relates to the novel use of known active substance combinations which consist firstly of 3,4-dichloro-2?-cyano-1,2-thiazole-5-carboxanilide, of the formula which is known, and secondly further known insecticidal active substances, for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: November 27, 2008
    Date of Patent: July 15, 2014
    Assignee: Bayer CropScience AG
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Heike Hungenberg, Wolfgang Thielert
  • Compositions and methods for the treatment of metabolic disorders
    Patent number: 8778976
    Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: July 15, 2014
    Assignee: Baylor College of Medicine
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Qian Mao, Shinji Kamisuki, Akira Kugimiya
  • COMPOSITION FOR TREATING ATHEROSCLEROSIS AND A PREPARATION METHOD THEREOF
    Publication number: 20140194474
    Abstract: Disclosed are a composition for preventing and treating atherosclerosis which includes chalcone compound. In particular, the chalcone compound bound with 2-hydroxyl in ring A and 4?-methyoxy in ring B has versatile therapeutic potentials on anti-atherosclerosis by acting as PPAR? inducer, p44/42 MAPK inhibitor and cell cycle blocker and does not show toxicity to human aortic smooth muscle cells (HASMCs). In addition, the chalcone compound exhibits synergistic effect with the PPAR? ligand (rosiglitazone) to inhibit cell proliferation and the upregulation of cyclin D1, cyclin D3, interleukin-1? (IL-1?) and interleukin-6 (IL-6) induced by oxidized low density lipoprotein (Ox-LDL).
    Type: Application
    Filed: March 10, 2014
    Publication date: July 10, 2014
    Applicant: Kaohsiung Medical University
    Inventors: Yang-Chang WU, Fang-Rong Chang, Tusty-Jiuan Hsieh, Suh-Hang Juo, An-Shen Lin, Ying-Chi Du
  • HETEROARYLMETHYL AMIDES
    Publication number: 20140194436
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Application
    Filed: February 24, 2014
    Publication date: July 10, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
  • Alkylamine-substituted dicyanopyridine and amino acid ester prodrugs thereof
    Patent number: 8772498
    Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: July 8, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Alexandros Vakalopoulos, Daniel Meibom, Barbara Albrecht-Küpper, Katja Zimmermann, Jörg Keldenich, Hans-Georg Lerchen, Peter Nell, Frank Süβmeier, Ursula Krenz
  • Inhibitors of hepatitis C virus polymerase
    Patent number: 8771665
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 8, 2014
    Assignee: Cocrystal Discovery, Inc.
    Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • COMPOSITION AND METHOD FOR CONTROLLING HARMFUL ARTHROPODS
    Publication number: 20140187541
    Abstract: The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising a carboxylic acid compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxiam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods.
    Type: Application
    Filed: July 20, 2012
    Publication date: July 3, 2014
    Inventors: Atsushi Iwata, Chie Shimizu, MIki Suzuki
  • PYRIDYLPHENYL COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES
    Publication number: 20140187586
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 3, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Zhiqiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
  • PYRROLIDINE-1,2-DICARBOXAMIDE DERIVATIVES
    Publication number: 20140186469
    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: February 27, 2014
    Publication date: July 3, 2014
    Applicant: NOVARTIS AG
    Inventors: Robin Alec Fairhurst, Vito Guagnano, Patricia Imbach-Weese, Giorgio Caravatti, Pascal Furet
  • 3-hydroxyisothiazole 1-oxide derivatives
    Patent number: 8765752
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 1, 2014
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventor: Munetaka Ohkouchi
  • Novel Heterocyclic Compounds as Bromodomain Inhibitors
    Publication number: 20140179648
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: Shuang Liu, Bryan Cordell Duffy, John Frederick Quinn, May Xiaowu Jiang, Ruifang Wang, Gregory Scott Martin, He Zhao, Bruce Francis Molino, Peter Ronald Young
  • NON-ATP DEPENDENT INHIBITORS OF EXTRACELLULAR SIGNAL-REGULATED KINASE (ERK)
    Publication number: 20140179743
    Abstract: A compound, having the formula A-1: Wherein R1 and R2 are defined herein. Methods of using the compound and compositions containing the compound are provided.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Paul S. Shapiro, Alexander D. MacKerell, JR., Steven Fletcher