Ring Oxygen In The Additional Hetero Ring Patents (Class 546/281.7)
  • Patent number: 10455835
    Abstract: A new method for the control and prevention of sugar beet leaf spot caused by Cercospora beticola (CERCBE) in a sugar beet plant has been discovered. The method involves applying effective amounts of Formula I to sugar beets.
    Type: Grant
    Filed: December 28, 2013
    Date of Patent: October 29, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: David Ouimette, John Todd Mathieson, Greg Kemmitt
  • Patent number: 10308622
    Abstract: The present disclosure relates to a method for effecting catalytic selective oxidation in liquid phase comprising a perfluorinated solvent and an olefinic compound with molecular oxygen to produce an epoxide. The method may provide enhanced selectivity to the epoxide of greater than 60%. The olefinic compound may be ethylene, propylene, butenes, 1-octene, butadiene, allyl chloride, allyl alcohol, styrene, and the like. The perfluorinated solvent may be perfluoro methyldecalin, perfluorodecalin, perfluoroperhydrophenanthrene, perfluoro (butyltetrahydrofuran), isomers thereof, or a combination thereof. In some embodiments, the method includes catalytically epoxidizing, in a liquid phase comprising a perfluorinated solvent, propylene with molecular oxygen to produce propylene oxide.
    Type: Grant
    Filed: January 24, 2018
    Date of Patent: June 4, 2019
    Assignee: Lyondell Chemical Technology, L.P.
    Inventors: Sandor Nagy, Barbara Kimmich, Justin E. Turner, Nicholas Bruschi, George R. Horvat
  • Patent number: 10144728
    Abstract: A process for the alkylation of picolinamides with substituted chloroacylals to produce a structure of Formula (III), wherein the reaction is performed in the presence of a phase-transfer catalyst and an inorganic halide co-catalyst.
    Type: Grant
    Filed: October 3, 2016
    Date of Patent: December 4, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Matthew J. Jansma, Timothy J. Adaway, Michael Lee Trippeer
  • Patent number: 9955691
    Abstract: This disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: May 1, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Timothy A. Boebel, Yu Lu, Kevin G. Meyer, Chenglin Yao, John F. Daeuble, Sr., Karla Bravo-Altamirano, Benjamin M. Nugent
  • Patent number: 9686984
    Abstract: This disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: June 27, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Kyle A. DeKorver, Johnathan E. DeLorbe, Kevin G. Meyer, Chenglin Yao, Ronald J. Heemstra, Karla Bravo-Altamirano, John F. Daeuble, Sr.
  • Patent number: 9629365
    Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: April 25, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Fangzheng Li, Kevin G. Meyer, James M. Renga, Chenglin Yao, Jeremy Wilmot, Jessica Herrick, Karla Bravo-Altamirano, Timothy A. Boebel
  • Patent number: 9247741
    Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: February 2, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Jonathan E. DeLorbe, Kyle A. DeKorver, Kevin G. Meyer, Chenglin Yao, Jeremy Wilmot, Ian O'Callaghan, Ronald J. Heemstra, William H. Dent, III, Rebecca Lyn K. C. LaLonde
  • Patent number: 9199978
    Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: December 1, 2015
    Assignee: CHINESE PLA GENERAL HOSPITAL
    Inventors: Kunluu He, Song Li, Wu Zhong, Juan Liu, Lili Wang, Xin Li, Guoliang Hu, Jie Wang, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Ruijun Li, Chunlei Liu, Jie Tang
  • Publication number: 20150112079
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Application
    Filed: December 31, 2014
    Publication date: April 23, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru KAMBE, Toru MARUYAMA, Shinsaku YAMANE, Satoshi NAKAYAMA, Kousuke TANI
  • Publication number: 20150094341
    Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.
    Type: Application
    Filed: September 29, 2014
    Publication date: April 2, 2015
    Inventors: Fangzheng Li, Kevin G. Meyer, James M. Renga, Chenglin Yao, Jeremy Wilmot, Jessica Herrick, Karla Bravo-Altamirano, Timothy Boebel
  • Publication number: 20150094339
    Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.
    Type: Application
    Filed: September 29, 2014
    Publication date: April 2, 2015
    Inventors: Timothy P. Martin, Kevin G. Meyer, Benjamin Nugent, Chenglin Yao, W. John Owen, Anne M. Wilson, Ian O'Callaghan, Jeremy Wilmot, Johnathan E. DeLorbe, William Dent, III
  • Publication number: 20150072396
    Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 12, 2015
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Patent number: 8969343
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: March 3, 2015
    Assignee: Quanticel Pharmaceuticals, Inc.
    Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
  • Publication number: 20140315913
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20140296073
    Abstract: Compounds of the formula (I) or salts thereof, in which (R1)m, (R2)n, R3 and R4 as defined in Claim 1 are suitable as herbicides for the control of harmful plants or as plant growth regulators. The compounds can be prepared by the processes of Claim 7.
    Type: Application
    Filed: October 29, 2012
    Publication date: October 2, 2014
    Inventors: Harald Jakobi, Marc Mosrin, Hansjörg Dietrich, Elmar Gatzweiler, Isolde Häuser-Hahn, Ines Heinemann, Christopher Hugh Rosinger
  • Publication number: 20140296208
    Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R5, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Applicants: Topivert Pharma Limited, Respivert Limited
    Inventors: Thomas Matthew BAKER, Matthew Colin Thor FYFE, Gareth William HARBOTTLE, Vedran HASIMBEGOVIC, Premji MEGHANI, Aaron RIGBY, Colin SAMBROOK-SMITH, Stephen Malcolm THOM
  • Publication number: 20140275171
    Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Application
    Filed: May 28, 2014
    Publication date: September 18, 2014
    Inventors: Kevin G. Meyer, JR., Karla Bravo-Altamirano, James M. Renga, Jessica Herrick, Benjamin Nugent, Timothy Boebel, Fangzheng Li, Nick X. Wang, W. John Owen, Paul Graupner, Chenglin Yao, Ronald J. Heemstra
  • Patent number: 8835462
    Abstract: The disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: September 16, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Kevin G. Meyer, W. John Owen, James M. Renga, Chenglin Yao, Benjamin M. Nugent, Jeremy Wilmot, Fangzheng Li, Karla Bravo-Altamirano
  • Patent number: 8815914
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: August 26, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Anette Graven Sams, Jorgen Eskildsen, Ask Püschl
  • Patent number: 8809319
    Abstract: Nitromethylene analogues of imidacloprid and divalent and oxabridged heterocyclic neonicotinoid compounds constructed by dialdehydes, preparation methods and uses thereof are disclosed. Compounds represented by formula (A) or (B), their optical isomers or agrochemically acceptable salts are provided. Agrochemical compositions comprising the said compounds, their optical isomers or agrochemically acceptable salts, the uses of the said agrochemical compositions and the preparation methods of the said compounds, their optical isomers or agrochemically acceptable salts are also disclosed. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm and armyworm.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: August 19, 2014
    Assignee: East China University of Science and Technology
    Inventors: Xuhong Qian, Zhong Li, Xusheng Shao, Xiaoyong Xu, Zhiping Xu, Gonghua Song
  • Patent number: 8785479
    Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: July 22, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Kevin G. Meyer, Karla Bravo-Altamirano, James M. Renga, Jessica Herrick, Benjamin M. Nugent, Timothy A. Boebel, Fangzheng Li, Nick X. Wang, W. John Owen, Paul R. Graupner, Chenglin Yao, Ronald J. Heemstra
  • Publication number: 20140187588
    Abstract: The disclosure relates to macrocyclic picolinamides of Formula (I) and to the use of these compounds as fungicides.
    Type: Application
    Filed: December 27, 2013
    Publication date: July 3, 2014
    Inventors: Rebecca Lalonde, Kevin G. Meyer, Fangzheng Li, Jeremy Wilmot, Karla Bravo-Altamirano, Chenglin Yao, Iain O'Callaghan, Jessica Herrick, Kyle DeKorver, Yu Lu
  • Publication number: 20140186873
    Abstract: Disclosed herein are isotopically labeled antifungal antibiotics and related compounds. Also disclosed are methods for synthesizing these isotopically labeled molecules and using the same to study the distribution of these compounds in the biosphere as well as the products formed by the breakdown of these isotopically labeled compounds.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Inventors: Ronald Ross, Jr., Peter Lee Johnson, Kevin G. Meyer
  • Publication number: 20140121367
    Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
    Type: Application
    Filed: April 9, 2012
    Publication date: May 1, 2014
    Inventors: Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
  • Publication number: 20140088046
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: September 5, 2013
    Publication date: March 27, 2014
    Applicant: ZOETIS LLC
    Inventors: Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
  • Patent number: 8673904
    Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: March 18, 2014
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • Publication number: 20140057919
    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: October 31, 2013
    Publication date: February 27, 2014
    Applicant: Pfizer Inc.
    Inventors: Usa Reilly, Michael Joseph Melnick, Matthew Frank Brown, Mark Stephen Plummer, Justin Ian Montgomery, Ye Che, Loren Michael Price
  • Publication number: 20140057916
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
  • Publication number: 20140010897
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: January 9, 2014
    Inventors: Anette Graven Sams, Jorgen Eskildsen, Ask Püschl
  • Publication number: 20130324577
    Abstract: Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Application
    Filed: January 26, 2012
    Publication date: December 5, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru Kambe, Isamu Sugimoto
  • Publication number: 20130296373
    Abstract: The disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Application
    Filed: May 6, 2013
    Publication date: November 7, 2013
    Applicant: Dow AgroSciences LLC
    Inventors: Kevin G. Meyer, W. John Owen, James M. Renga, Chenglin Yao, Benjamin M. Nugent, Jeremy Wilmot, Fangzheng Li, Karla Bravo-Altamirano
  • Publication number: 20130296375
    Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Application
    Filed: May 6, 2013
    Publication date: November 7, 2013
    Applicant: Dow AgroSciences LLC
    Inventors: Kevin G. Meyer, Karla Bravo-Altamirano, James M. Renga, Jessica Herrick, Benjamin M. Nugent, Timothy A. Boebel, Fangzheng Li, Nick X. Wang, W. John Owen, Paul R. Graupner, Chenglin Yao, Ronald J. Heemstra
  • Publication number: 20130296371
    Abstract: The disclosure relates to macrocyclic picolinamides of Formula I and their use as fungicides.
    Type: Application
    Filed: May 6, 2013
    Publication date: November 7, 2013
    Applicant: Dow AgroSciences LLC
    Inventors: Kevin G. Meyer, Fangzheng Li, James M. Renga, W. John Owen, Benjamin M. Nugent, Chenglin Yao, Nick X. Wang
  • Publication number: 20130245101
    Abstract: Therapeutic conjugates containing a statin or a modified statin (collectively “statin”) linked to a therapeutic agent (also referred to as a drug herein) are targeted to the liver by the statin or modified statin and thereby deliver the therapeutic agent to liver cells
    Type: Application
    Filed: April 24, 2013
    Publication date: September 19, 2013
    Inventors: Gregory L. Verdine, Yoshihiko Norimine, Lourdes Gude-Rodriguez
  • Publication number: 20130196987
    Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.
    Type: Application
    Filed: October 30, 2012
    Publication date: August 1, 2013
    Applicant: EISAI CO., LTD.
    Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
  • Publication number: 20130131036
    Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Application
    Filed: October 23, 2012
    Publication date: May 23, 2013
    Applicant: AbbVie Inc.
    Inventor: AbbVie Inc.
  • Publication number: 20130131056
    Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 23, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8404855
    Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: March 26, 2013
    Assignee: Bayer CropScience AG
    Inventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Rolf Pontzen, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Thomas Müller, Christian Arnold, Erich Sanwald
  • Publication number: 20130065876
    Abstract: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Application
    Filed: September 11, 2012
    Publication date: March 14, 2013
    Inventors: Uwe Grether, Paul Hebeisen, Peter Mohr, Fabienne Ricklin, Stephan Roever
  • Publication number: 20130012530
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20120316195
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 16, 2010
    Publication date: December 13, 2012
    Applicant: NOVARTIS AG
    Inventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
  • Publication number: 20120316147
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: June 1, 2012
    Publication date: December 13, 2012
    Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
  • Publication number: 20120270852
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2? are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2? together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4? are each independently hydrogen or lower alkyl, or R4 and R4? together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
    Type: Application
    Filed: April 11, 2012
    Publication date: October 25, 2012
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20120232083
    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: March 7, 2012
    Publication date: September 13, 2012
    Inventors: Usa REILLY, Michael MELNICK, Matthew F. BROWN, Mark S. PLUMMER, Justin MONTGOMERY, Ye CHE, Loren PRICE
  • Patent number: 8247572
    Abstract: Compounds of the formula: are described wherein: A1 is ascorbic acid, dehydroascorbic acid, ascorbyl-2-phosphate, an analog thereof, or a salt thereof; L is a linking group coupled to A1 at the C5 or C6 position thereof; and B1 is an active agent such as an imaging agent or therapeutic agent (e.g. a bisphosphonate), along with pharmaceutically acceptable salts and prodrugs thereof. The compounds are useful for, among other things, improving cartilage uptake of active agents administered for joint diseases such as osteoarthritis and rheumatoid arthritis, and for improving gastrointestinal absorption of bisphosphonates.
    Type: Grant
    Filed: April 21, 2006
    Date of Patent: August 21, 2012
    Assignee: Duke University
    Inventors: Virginia Byers Kraus, Amy Lynn McNulty, Eric John Toone
  • Publication number: 20120157314
    Abstract: The present invention relates to novel, herbicidally active picolinic acid derivatives of the formula (I) and to processes for preparation thereof. The present invention further provides for the use thereof as a herbicide, especially as a herbicide for selective control of weed plants in useful plant crops, and as a plant growth regulator alone or in combination with safeners and/or in a mixture with other herbicides.
    Type: Application
    Filed: October 21, 2011
    Publication date: June 21, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Hartmut AHRENS, Marco BRÜNJES, Hansjörg DIETRICH, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Stefan LEHR, Dirk SCHMUTZLER
  • Publication number: 20120035149
    Abstract: Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.
    Type: Application
    Filed: December 16, 2009
    Publication date: February 9, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Qun-Yong Zhou, Jia-Da Li, Qi Huang
  • Patent number: 8106212
    Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: January 31, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Beck, Olga Malsam, Ralf Nauen, Ulrich Görgens, Thomas Müller, Christian Arnold, Erich Sanwald
  • Patent number: 8106211
    Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: January 31, 2012
    Assignee: Bayer CropScience AG
    Inventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Rolf Pontzen, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Thomas Müller, Christian Arnold, Erich Sanwald