The Hetero Ring Is Six-membered Patents (Class 549/356)
  • Patent number: 10899996
    Abstract: The use as fragrance ingredient of 4—methylene—2—(2—methylprop—1—enyl)—tetrahydropyran.
    Type: Grant
    Filed: July 25, 2018
    Date of Patent: January 26, 2021
    Assignee: GIVAUDAN SA
    Inventor: Marc Liniger
  • Patent number: 10815167
    Abstract: A process for the double-bond isomerization of olefins is disclosed. The process may include contacting a hydrocarbon stream including olefins with a ?-alumina-titania isomerization catalyst to convert at least a portion of the olefin to its positional isomer. The ?-alumina-titanic isomerization catalysts disclosed herein may also have the activity to convert alcohol into additional olefins, while having increased resistance to oxygenate poisons.
    Type: Grant
    Filed: May 21, 2018
    Date of Patent: October 27, 2020
    Assignee: Lummus Technology Inc.
    Inventors: Bala Ramachandran, Sukwon Choi, Robert J. Gartside
  • Patent number: 9994540
    Abstract: The invention relates to a method for producing 2-substituted 4-methyl-tetrahydropyrans of general formula (I) from starting materials containing at least one 2-substituted 4,4-dimethyl-1,3-dioxane of general formula (II).
    Type: Grant
    Filed: April 8, 2015
    Date of Patent: June 12, 2018
    Assignee: BASF SE
    Inventors: Stefan Rüdenauer, Timon Stork
  • Patent number: 9346779
    Abstract: The present invention relates to a method for producing dehydro rose oxide by reacting isoprenol and prenal in the presence of at least one sulfonic acid of formula R1—SO3H as catalyst, wherein R1 is selected from phenyl which carries 2 or 3 C1-C4-alkyl substituents, phenyl which carries one C8-C20-alkyl substituent and optionally also 1 or 2 C1-C4-alkyl substituents, and naphthyl which optionally carries 1 or 2 C1-C4-alkyl substituents.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: May 24, 2016
    Assignee: BASF SE
    Inventors: Marcus G. Schrems, Jan Eggert, Jan U. Müller, Jan-Dirk Arndt, Günter Gottwald, Volker Hütt
  • Patent number: 9346780
    Abstract: Disclosed is a process for preparing dihydro-2H-pyran derivatives of formula I: wherein R1 and R2 are defined herein. The process of the invention provides the compound of formula I in concise cascade reactions and in one pot. The compound of formulae I prepared by the process of the invention and its further transformed derivatives are useful for making pharmaceutical composition for the treatment of proliferative diseases.
    Type: Grant
    Filed: October 10, 2013
    Date of Patent: May 24, 2016
    Assignee: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION
    Inventors: Pandurang V. Chouthaiwale, Fujie Tanaka
  • Publication number: 20150141667
    Abstract: The present invention provides catalysts, methods, and reactor systems for converting oxygenated hydrocarbons to oxygenated compounds. The invention includes methods for producing cyclic ethers, monooxygenates, dioxygenates, ketones, aldehydes, carboxylic acids, and alcohols from oxygenated hydrocarbons, such as carbohydrates, sugars, sugar alcohols, sugar degradation products, and the like, using catalysts containing palladium, molybdenum, tin, and tungsten. The oxygenated compounds produced are useful in the production of liquid fuels, chemicals, and other products.
    Type: Application
    Filed: December 30, 2014
    Publication date: May 21, 2015
    Inventors: Brian Blank, Randy Cortright, Taylor Beck, Elizabeth Woods, Mike Jehring
  • Patent number: 9034921
    Abstract: A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: May 19, 2015
    Assignee: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon Kim, Dong Ho Hong, Misuk Kang
  • Publication number: 20150133680
    Abstract: A method of making an anti-Markovnikov addition product is carried out by reacting an acid with an alkene or alkyne in a dual catalyst reaction system to the exclusion of oxygen to produce said anti-Markovnikov addition product; the dual catalyst reaction system comprising a single electron oxidation catalyst in combination with a hydrogen atom donor catalyst. Compositions useful for carrying out such methods are also described.
    Type: Application
    Filed: May 6, 2013
    Publication date: May 14, 2015
    Inventors: David A. Nicewicz, David S. Hamilton, Andrew J. Perkowski
  • Publication number: 20150094233
    Abstract: The present invention provides a compound represented by the formula (I): or a salt thereof; and a method of quantitatively analyzing an amino group-containing target substance, including labeling a target substance in samples by using, as a labeling compound, two or more of such compounds having a mutually different mass due to isotope labeling, to confer a mass difference to the target substance between two or more samples, and the like.
    Type: Application
    Filed: March 28, 2013
    Publication date: April 2, 2015
    Inventors: Shigeru Matsukawa, Kazumi Narita, Yasushi Arakawa, Haruki Shimodaira
  • Patent number: 8987479
    Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: March 24, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Charles Chase, Atsushi Endo, Francis G. Fang, Jing Li
  • Patent number: 8969597
    Abstract: The present invention relates to a process for preparing Nebivolol and, more in particular, to a fractional distillation method of a mixture of stereoisomers of formula intermediates useful in the preparation of nebivolol.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: March 3, 2015
    Assignee: Zach System S.p.A.
    Inventors: Livius Cotarca, Johnny Foletto, Paolo Maragni, Giorgio Soriato, Daniele Urbani, Massimo Verzini
  • Patent number: 8962679
    Abstract: Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: February 24, 2015
    Assignees: The Administrators of the Tulane Educational Fund, Xavier University of Louisiana
    Inventors: Guangdi Wang, Matthew E. Burow, Stephen M. Boue, Thomas E. Wiese, Quan Jiang
  • Patent number: 8952054
    Abstract: The invention provides methods for the identification of small molecules that inhibit MUC1 oligomerization, and the functions flowing therefrom. In addition, small molecules that prevent MUC1 oligomerization are disclosed. Identified molecules will find use in treating a variety of MUC1-related inflammatory conditions, including MUC1-related cancers.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: February 10, 2015
    Assignees: Dana-Farber Cancer Institute, Inc., Genus Oncology, LLC
    Inventors: Donald W. Kufe, Surender Kharbanda
  • Patent number: 8937097
    Abstract: Methods for making trans-(?)-?9-tetrahydrocannabinol and trans-(+)-?9-tetrahydrocannabinol are disclosed herein. In one embodiment, a trans-(?)-?9-tetrahydrocannabinol composition is prepared by allowing a composition comprising (±)-?9)-tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(?)-?9-tetrahydrocannabinol composition comprising at least about 99% by weight of trans-(?)-?9-tetrahydrocannabinol based on the total amount of trans-(?)-?9-tetrahydrocannabinol and trans-(+)-?9-tetrahydrocannabinol. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of a trans-(?)-?9-tetrahydrocannabinol having a purity of at least about 98% based on the total weight of cannabinoids.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: January 20, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Arie L. Gutman, Marina Etinger, Irina Fedotev, Ram Khanolkar, Gennady A. Nisnevich, Boris Pertsikov, Igor Rukhman, Boris Tishin
  • Patent number: 8933116
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: January 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
  • Patent number: 8916063
    Abstract: A liquid crystal composition and an AM liquid crystal display device are described. The liquid crystal composition has a negative dielectric anisotropy, contains a specific compound having a large negative dielectric anisotropy as a first component and a two-ring compound having a small viscosity as a second component, and may further contain a specific compound having a large negative dielectric anisotropy as a third component, a specific compound having a small viscosity as a fourth component and a specific compound having a large negative dielectric anisotropy as a fifth component. The AM liquid crystal display device includes the liquid crystal composition.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: December 23, 2014
    Assignees: JNC Corporation, JNC Petrochemical Corporation
    Inventors: Yasuyuki Goto, Kazuhiko Saigusa, Norikatsu Hattori
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • Patent number: 8901124
    Abstract: The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: December 2, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Cornelius Hermann, Joshua Kennedy-Smith, Matthew C. Lucas, Fernando Padilla, Michael Soth
  • Patent number: 8883821
    Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: November 11, 2014
    Assignee: Pierre Fabre Medicament
    Inventors: El Bachir Kaloun, Karim Bedjeguelal, Rémi Rabot, Anna Kruczynski, Philippe Schmitt, Michel Perez, Nicolas Rahier
  • Patent number: 8877759
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: September 4, 2012
    Date of Patent: November 4, 2014
    Assignee: Vertex Pharnaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
  • Patent number: 8877761
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: April 18, 2012
    Date of Patent: November 4, 2014
    Assignee: Pfizer Inc.
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
  • Patent number: 8846956
    Abstract: The present invention relates to a process for the preparation of a composition enriched in cis-2-(2-methylprop-1-enyl)-4-methyltetrahydropyran, comprising the catalytic hydrogenation of 2-(2-methylprop-1-enyl)-4-methylenetetrahydropyran in the presence of hydrogen and a heterogeneous catalyst comprising ruthenium.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: September 30, 2014
    Assignee: BASF SE
    Inventors: Thomas Heidemann, Lucia Königsmann
  • Patent number: 8834744
    Abstract: The invention relates to a liquid-crystalline medium comprising one or more compounds of the formula I in which R0, X0 and L1-6 have the meanings indicated in Claim 1, and to the use thereof in electro-optical liquid-crystal displays.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: September 16, 2014
    Assignee: Merck Patent GmbH
    Inventors: Michael Wittek, Brigitte Schuler, Reiffenrath Volker, Mark Goebel, Markus Czanta
  • Patent number: 8815941
    Abstract: Compounds of structural formula (I) useful for the treatment or prophylaxis of viral infection, particularly viral influenza are provided Pharmaceutical preparations thereof and methods for their preparation are also described. The therapeutic effect is achieved via inhibition of viral neuraminidases, also known as viral sialidases. These neuraminidases are classified under the GH34 family of viral enzymes.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: August 26, 2014
    Assignee: The University of British Columbia
    Inventors: Stephen Withers, Andrew Graham Watts, Jin Hyo Kim, Tom Wennekes
  • Patent number: 8809554
    Abstract: The present invention is directed to a process for the preparation of sulfamide derivatives.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: August 19, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Yong Gong, Hartmut B. Zinser
  • Patent number: 8791118
    Abstract: The invention provides new pyridopyrazine compounds according to formula (I) which are highly selective as Ras-Raf-Mek-Erk signal transduction pathway inhibitors and in particular are highly selective Erk inhibitors.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: July 29, 2014
    Assignee: Aeterna Zentaris GmbH
    Inventors: Matthias Gerlach, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
  • Patent number: 8791119
    Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Sanofi
    Inventors: Sylvain Cote Des Combes, Jacques Froissant, Jean-Francois Gibert, Frank Marguet, Christophe Pacaud, Frédéric Puech, Antoine Ravet
  • Patent number: 8778988
    Abstract: A method of making an endoperoxide from a diene and oxygen in the presence of a photocatalyst having an excited state lifetime of at least 100 nanoseconds, the endoperoxide being represented by the formula: where R1 is an aryl substituted with at least one group selected from the group consisting of alkoxy, hydroxyl, halogen, carbamate, sulfonamide, silyloxy, amide, and combinations thereof or a substituted or unsubstituted heteroaryl, R2 is hydrogen, alkyl, alkynyl, or aryl, R3 is hydrogen, alkyl, alkynyl, or aryl, R4 is alkynyl or aryl, R5 is hydrogen or a substituent, R6 is hydrogen or a substituent, and A1, A2, and A3 are the same or different atoms and form a divalent group that combines with the two carbon atoms of the endoperoxide ring to form a saturated or unsaturated, substituted or unsubstituted ring system of a size of from five to six atoms.
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: July 15, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Tehshik P. Yoon, Jonathan D. Parrish, Michael A. Ischay
  • Patent number: 8772323
    Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: July 8, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
  • Patent number: 8754244
    Abstract: The present invention relates to new rhodamine compounds and their use as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: June 17, 2014
    Assignee: Illumina Cambridge Limited
    Inventors: Nikolai Nikolaevich Romanov, Xiaohai Liu
  • Patent number: 8748484
    Abstract: An anti-cancer ruthenium complex containing organometallic triruthenium with two maltol ligands is claimed.
    Type: Grant
    Filed: April 9, 2012
    Date of Patent: June 10, 2014
    Assignee: Research Foundation of The City University of New York
    Inventor: Varattur Dayal Reddy
  • Patent number: 8741947
    Abstract: The present invention provides a compound of the formula (I) or (II, wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: June 3, 2014
    Assignee: The United States of America, as represented by the Secretary of the Department of Health and Human Services
    Inventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
  • Patent number: 8716292
    Abstract: The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments. A general representation of the 2-(heteroaryl)amino-riminophenazines is shown below.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: May 6, 2014
    Assignee: Global Alliance for TB Drug Development
    Inventors: Kai Liu, Christopher B. Cooper, Haihong Huang, Chun Li, Binna Liu, Yang Liu, Zhenkun Ma, Jingbin Wang, Dali Yin, Dongfeng Zhang, Gang Zhang, Hao Zhang
  • Patent number: 8703784
    Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyun Zhao, Andrew McRiner
  • Publication number: 20140107353
    Abstract: The present invention provides methods, reactor systems, and catalysts for converting in a continuous process biomass to less complex oxygenated compounds for use in downstream processes to produce biofuels and chemicals. The invention includes methods of converting the components of biomass, such as hemicellulose, cellulose and lignin, to water-soluble materials, including lignocellulosic derivatives, cellulosic derivatives, hemicellulosic derivatives, carbohydrates, starches, polysaccharides, disaccharides, monosaccharides, sugars, sugar alcohols, alditols, polyols, diols, alcohols, ketones, cyclic ethers, esters, carboxylic acids, aldehydes, and mixtures thereof, using hydrogen and a heterogeneous liquefaction catalyst.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: Virent, Inc.
    Inventors: Ming Qiao, Randy D. Cortright, John Kania, Elizabeth Woods
  • Publication number: 20140107352
    Abstract: The present invention relates to a process for the integrated preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyrans and of 2-substituted 4-methyltetrahydropyrans.
    Type: Application
    Filed: October 14, 2013
    Publication date: April 17, 2014
    Applicant: BASF SE
    Inventors: Timon Stork, Oskar Röder, Klaus Ebel, Ralf Pelzer, Wolfgang Krause, Karl Beck
  • Patent number: 8686142
    Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: April 1, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frank Chavez, James P. Edwards, Brad M. Savall, Jianmei Wei, Ronald L. Wolin
  • Patent number: 8680159
    Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
  • Patent number: 8658646
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: February 25, 2014
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
  • Patent number: 8658794
    Abstract: The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: February 25, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Adrianus Petrus Antonius de Man, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Hans Cornelis Andreas Raaijmakers, Jacobus Cornelis Henricus Maria Wijkmans
  • Patent number: 8614215
    Abstract: The present invention is related to quinoxaline compounds of Formula (I) in particular for the treatment 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: February 21, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Serono SA
    Inventors: Pascale Gaillard, Vincent Pomel, Isabelle Jeanclaude-Etter, Jerome Dorbais, Jasna Klicic, Cyril Montagne
  • Patent number: 8604034
    Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: December 10, 2013
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Anderson
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8575203
    Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
    Type: Grant
    Filed: April 19, 2011
    Date of Patent: November 5, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Christiane Kofink, Darryl McConnell
  • Patent number: 8575367
    Abstract: The present disclosure relates to the preparation of acrylate, alkacrylate, allyl, and polycarbonate derivatives of hydroxy ketal esters, and uses thereof.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: November 5, 2013
    Assignee: Segetis, Inc.
    Inventors: Sergey Selifonov, Brian Daniel Mullen, Douglas Alan Wicks, Vivek Badarinarayana
  • Patent number: 8574456
    Abstract: The invention relates to a liquid-crystalline medium comprising one or more compounds of the formula I in which R0, X0 and L1-6 have the meanings indicated in Claim 1, and to the use thereof in electro-optical liquid-crystal displays.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: November 5, 2013
    Assignee: Merck Patent GmbH
    Inventors: Michael Wittek, Brigitte Schuler, Volker Reiffenrath, Mark Goebel, Markus Czanta
  • Patent number: 8546591
    Abstract: The present invention relates to a process for the preparation of cis-2-(2-methylprop-1-enyl)-4-methyltetrahydropyran comprising the catalytic hydrogenation of 2-(2-methylprop-1-enyl)-4-methylenetetrahydropyran in the presence of hydrogen and a heterogeneous catalyst comprising ruthenium on a support and subsequently bringing the compounds obtained in this way into contact with a strongly acidic cation exchanger.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: October 1, 2013
    Assignee: BASF SE
    Inventors: Lucia Koenigsmann, Juergen Schubert, Andreas Walch, Guenther Gottwald, Martin Kamasz, Ekkehard Schwab, Klaus-Peter Pfaff, Michael Slany
  • Patent number: 8536349
    Abstract: A process of preparing cyclic ethers is described. The process involves the reaction of at least one organic compound such as a dioi or a polyol which it has at least one pair of hydroxyl groups separated by 4 or 5 carbon atoms, and which is capable of being converted into an ether linkage, with an organic carbonate in the presence of a base. The base is an alkoxy, a carbonate or a hydroxide base or is a mixture of such bases. At least one of the hydroxyl groups of the organic compound is not a tertiary hydroxyl group.
    Type: Grant
    Filed: July 14, 2008
    Date of Patent: September 17, 2013
    Assignee: Givaudan S.A.
    Inventors: Hanamanthsa Shankarsa Bevinakatti, Christopher Paul Newman, Simon Ellwood, Pietro Tundo, Fabio Arico, Martin Schroeder
  • Patent number: 8518945
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X? and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: August 27, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
  • Patent number: 8507492
    Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: August 13, 2013
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Fultz, Rama K. Narla, Sabita Sankar, Jan Elsner