Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
Barbituric acid or derivative (including thioanalogs) (Class 514/270)
Nitrogen bonded directly to the 1,3-diazine at 2-position (Class 514/272)
Chalcogen bonded directly to pyrimidine at 2-position (Class 514/274)
  • 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
  • PRMT5 INHIBITORS AND USES THEREOF
    Publication number: 20140213582
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 31, 2014
    Applicant: EPIZYME, INC.
    Inventors: KENNETH W. DUNCAN, RICHARD CHESWORTH, MICHAEL JOHN MUNCHHOF
  • Plant treatment compositions particularly effective in the control of on rice crops, and methods for their use
    Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • 6-ALKYL-N-(PYRIDIN-2-YL)-4-ARYLOXYPICOLINAMIDE ANALOGS AS MGLUR5 NEGATIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING THE SAME
    Publication number: 20140206707
    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: Application
    Filed: March 5, 2012
    Publication date: July 24, 2014
    Applicant: VANDERBILT UNIVERSITY
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates, Brian A. Chauder
  • Process for preparing bosentan
    Patent number: 8785461
    Abstract: The present invention relates to a novel intermediate useful in the preparation of bosentan and to processes for the preparation of said intermediate and bosentan. The invention further relates to compositions comprising bosentan prepared according to the processes of the invention and their use in the treatment of endothelin-receptor mediated disorders.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: July 22, 2014
    Assignee: Generics [UK] Limited
    Inventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Vikas Padalkar, Hemant Mande
  • GPR 119 agonists
    Patent number: 8785463
    Abstract: The present invention relates to novel GPR 119 agonists of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: July 22, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pandurang Zaware
  • 5-hydroxypyrimidine-4-carboxamide derivative
    Patent number: 8785462
    Abstract: The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by formula (1): [wherein, R1: formula (1A): [wherein, R4 and R5: H, halogen, or alkyl; R6: H, halogen, alkyl, or the like; R7: substitutable hydroxyalkyl, substitutable hydroxyhalo alkyl, substitutable alkoxyalkyl, or the like; substituent group ?: oxo, hydroxy, amino, or the like; ring Q1: a monocyclic heterocyclic group; ring Q2: a monocyclic hydrocarbon ring group, or a monocyclic heterocyclic group; ring Q3: a monocyclic hydrocarbon ring group, or a monocyclic heterocyclic group; X: a single bond, methylene, ethylene, or the like]; R2: alkyl, or methylsulfanyl; and R3: H, or methyl], or the like.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: July 22, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Takeshi Kuribayashi, Hideki Kubota, Naoki Tanaka, Takeshi Fukuda, Takashi Tsuji, Riki Goto
  • Pyrimidine derivatives that inhibit FAK/PTK2
    Patent number: 8785464
    Abstract: The present invention includes compounds of general formula (1) wherein A, X, R1 and R2 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Bodo Betzemeier, Ioannis Sapountzis
  • HETEROCYCLIC-SUBSTITUTED BENZOFURAN DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20140199263
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 17, 2014
    Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
  • Inhibitors of P38 map kinase
    Patent number: 8778953
    Abstract: Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is —N? or —CH?; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z is O or 1; —X1-L1-Y— is a linker radical or bond; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 are as defined in the claims.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: July 15, 2014
    Assignee: Chroma Therapeutics Ltd.
    Inventors: David Festus Charles Moffat, Stephen John Davies, Stephane Pintat
  • Aqueous concentrate formulations containing saflufenacil and glyphosate
    Patent number: 8778838
    Abstract: The present invention relates to aqueous concentrate formulations for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its anhydrate; N-(phosphonomethyl)glycine in the form of its free acid, in the form of the ammonium salt or a substituted ammonium salt or a mixture thereof; at least two different non-ionic surfactants with at least one of them comprising an ethylene oxide polymer moiety or an ethylene oxide/C3-C4-alkylene oxide block copolymer moiety, and water; wherein the pH-value of the formulation is below 6.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: July 15, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Sven Adam, Klaus Kolb, Juergen Jakob, Bernd Sievernich, Joerg Steuerwald, Steven Bowe, Joseph Zawierucha, Rex Liebl
  • Phenylpyridine derivative and medicinal agent comprising same
    Patent number: 8778954
    Abstract: Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPAR?-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: July 15, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Toru Miura, Seiichi Sato, Hajime Yamada, Junya Tagashira, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
  • 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
  • DETECTION AND USE OF LOW MOLECULAR-WEIGHT MODULATORS OF THE COLD-MENTHOL RECEPTOR TRPM8
    Publication number: 20140194433
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • SPIROLACTAM DERIVATIVES AND USES OF SAME
    Publication number: 20140194424
    Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.
    Type: Application
    Filed: December 12, 2013
    Publication date: July 10, 2014
    Inventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma
  • GPR 119 agonists
    Patent number: 8772302
    Abstract: The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pandurang Zaware, Mukul Jain
  • Pharmaceutical composition containing an anti-nucleating agent
    Patent number: 8771733
    Abstract: Pharmaceutical compositions suitable for oral administration in solid dosage forms are described. The compositions comprise an effective amount of a drug compound in the form of a salt, wherein the drug salt is characterized by conversion to a less soluble form of the drug compound under certain pH conditions, and an anti-nucleating agent.
    Type: Grant
    Filed: December 2, 2005
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Maria T. Cruanes, Wei Xu, Laura M. Artino, Honggang Zhu
  • Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid
    Patent number: 8772483
    Abstract: Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed. Pharmaceutical dosage forms and methods of their use are also disclosed.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: July 8, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Qun Li, Weifeng Hu, Xiaogen Yang, Jiangqiong Zhao, Matthew Mangzhu Zhao
  • 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
    Patent number: 8772482
    Abstract: Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: July 8, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
  • NOVEL BENZAMIDES, PRODUCTION THEREOF, AND USE THEREOF AS MEDICAMENTS
    Publication number: 20140187539
    Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.
    Type: Application
    Filed: March 4, 2014
    Publication date: July 3, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger WAGNER, Elke LANGKOPF, Frank HIMMELSBACH, Rolf GOEGGEL, Birgit JUNG
  • SYNERGISTIC FUNGICIDAL COMPOSITIONS
    Publication number: 20140187508
    Abstract: A synergistic fungicidal mixture contains a fungicidally effective amount of a compound of Formula I and at least one fungicide selected from the group consisting of tricyclazole, azoxystrobin, carpropamid, probenazole, kasugamycin, and boscalid.
    Type: Application
    Filed: December 28, 2013
    Publication date: July 3, 2014
    Applicant: Dow AgroScience LLC
    Inventors: DAVID OUIMETTE, RICHARD K. MANN, JOHN TODD MATHIESON, OLAVO CORREA da SILVA
  • CRYSTALLINE FORMS OF BOSENTAN SALTS AND PROCESSES FOR THEIR PREPARATION
    Publication number: 20140187568
    Abstract: The present invention relates to crystalline forms of bosentan salts and processes for their preparation.
    Type: Application
    Filed: March 4, 2014
    Publication date: July 3, 2014
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Rakesh SINGH, Anu MITTAL, Gopal Singh BISHT, Mahavir Singh KHANNA, Rajesh Kumar THAPER, Mohan PRASAD
  • AGRICULTURAL OR HORTICULTURAL FUNGICIDE COMPOSITION AND METHOD FOR CONTROLLING PLANT PATHOGEN
    Publication number: 20140187567
    Abstract: A composition having a stable and high fungicidal effect against a cultivated crop infected by a plant pathogen is provided. An agricultural or horticultural fungicide composition containing, as active ingredients, (a) fluazinam or its salt and (b) a strobilurin compound or its salt is provided; in addition, a method for controlling a plant pathogen by applying the subject agricultural or horticultural fungicide composition to a plant or a soil is provided; and furthermore, a method for controlling a plant pathogen by applying (a) fluazinam or its salt and (b) a strobilurin compound or its salt to a plant or a soil is provided.
    Type: Application
    Filed: May 25, 2012
    Publication date: July 3, 2014
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Koji Sugimoto, Takanori Suzuki, Koudai Yamamoto
  • Fungicidal substituted 1--1H-[1,2,4]triazole compounds
    Publication number: 20140187423
    Abstract: The present invention relates to substituted 1-{2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-2-alkoxy-hexyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.
    Type: Application
    Filed: August 14, 2012
    Publication date: July 3, 2014
    Applicant: BASF SE
    Inventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Mueller, Wassilios Grammenos, Thomas Grote
  • CRYSTALLINE FORMS OF BOSENTAN SALTS AND PROCESSES FOR THEIR PREPARATION
    Publication number: 20140187569
    Abstract: The present invention relates to crystalline forms of bosentan salts and processes for their preparation.
    Type: Application
    Filed: March 4, 2014
    Publication date: July 3, 2014
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Rakesh SINGH, Anu MITTAL, Gopal Singh BISHT, Mahavir Singh KHANNA, Rajesh Kumar THAPER, Mohan PRASAD
  • Pyrimidline derivatives having immune modulating properties that act via TLR7 for the treatment of viral or allergic diseases and cancers
    Patent number: 8765939
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: July 1, 2014
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Nicholas J. Bennett, Thomas McInally, Tobias Mochel, Stephen Thom, Anna-Karin Tidén
  • Antihypertensive pharmaceutical composition
    Patent number: 8765776
    Abstract: Provided is an antihypertensive pharmaceutical composition containing Fimasartan, a pharmaceutically acceptable salt thereof, a solvate thereof or a hydrate thereof as an angiotensin II receptor blocker, and Amlodipine, an isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof or a hydrate thereof as a calcium channel blocker.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: July 1, 2014
    Assignee: Boryung Pharmaceutical Co., Ltd.
    Inventors: Seung Ho Kim, Ji Han Kim, Je Hak Kim, Kyung Wan Nam, Yong Ha Chi, Joo Han Lee, Soo Heui Paik, So Jeong Yi, Tae Eun Kim, Seo Hyun Yoon, Joo Youn Cho, Sang Goo Shin, In Jin Jang, Kyung Sang Yu
  • Methods of treating bone mass diseases
    Patent number: 8759364
    Abstract: The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.
    Type: Grant
    Filed: March 30, 2009
    Date of Patent: June 24, 2014
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Gerard Karsenty, Patricia F. Ducy, Yuli Xie, Donald Landry, Vijay Kumar Yadav
  • Substituted bicyclic amines for the treatment of diabetes
    Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs
    Patent number: 8758822
    Abstract: The present invention relates to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, and more particularly, to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, including a first step of dissolving a biodegradable polymer in a non-volatile polar organic solvent, a second step of adding poorly soluble drugs to water and the biodegradable polymer solution to produce a dispersion, and a third step of adding the dispersion to emulsifier solutions in a batch under the condition of low mechanical energy level stirring.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: June 24, 2014
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Bong Hyun Chung, Yong Taik Lim, Jung Hyun Han
  • Organic compounds
    Patent number: 8759346
    Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: June 24, 2014
    Assignee: Novartis AG
    Inventors: Mathias Frederiksen, Dominik Feuerbach, Konstanze Hurth, Manuel Koller, Bernard Lucien Roy
  • Use of deoxyelephantopin (DET) and analogues thereof for treatment of melanoma
    Patent number: 8754121
    Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: June 17, 2014
    Assignee: Academia Sinica
    Inventors: Lie-Fen Shyur, Wen-Wan Chao, Ya-Wen Cheng
  • PIM KINASE INHIBITORS AND PREPARATION METHODS AND USE IN MEDICINAL MANUFACTURE THEREOF
    Publication number: 20140162999
    Abstract: PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds as represented by Formula I. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.
    Type: Application
    Filed: February 10, 2014
    Publication date: June 12, 2014
    Applicant: Jikai Biosciences, Inc.
    Inventor: Yu GE
  • Compositions and Methods for the Production of Pyrimidine and Pyridine Compounds with BTK Inhibitory Activity
    Publication number: 20140162983
    Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
    Type: Application
    Filed: June 10, 2012
    Publication date: June 12, 2014
    Applicant: Merck Patent GmbH
    Inventors: Brian L. Hodous, Lesley Liu-Bujalski, Reinaldo Jones, Donald Bankston, Theresa L. Johnson, Igor Mochalkin, Ngan Nguyen, Hui Qiu, Andreas Goutopoulos, Nadia Brugger
  • Use of Tetrahydropyrimidines
    Publication number: 20140163053
    Abstract: A method of treatment of postoperative inflammatory stress and pain comprising administering a tetrahydropyrimidine selected from ectoine and/or hydroxyectoine to a patient in need of such treatment.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 12, 2014
    Applicant: Bitop Aktiengesellschaft
    Inventors: Rene Tolba, Gerhild van Echten-Deckert, Georg Lentzen, Andress Bilstein
  • sGC stimulators
    Patent number: 8748442
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: June 10, 2014
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R Iyengar, Ara Mermerian, Angelika Fretzen
  • Crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]THIO]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfonamide
    Patent number: 8748603
    Abstract: There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: June 10, 2014
    Assignee: AstraZeneca AB
    Inventors: Britt Anne Ingela Gullberg, Thomas Peter Larsson, Jeffrey Paul Stonehouse
  • Metalloenzyme inhibitor compounds
    Patent number: 8748461
    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: June 10, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
  • ?3 adrenergic receptor agonists
    Patent number: 8748433
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
  • Synergistic fungicidal mixtures
    Patent number: 8748339
    Abstract: The present invention relates to a composition, comprising a 5-amino-3-oxo-2,3-dihydro-pyrazole of the formula I as defined in the claims and the description and at least one active compound II selected from groups A) to I) in a synergistically effective amount.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: June 10, 2014
    Assignee: BASF SE
    Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Egon Haden
  • COMPOUNDS AND METHODS
    Publication number: 20140155419
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 5, 2014
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
  • TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20140155413
    Abstract: The present invention is directed to compounds of formula I and 1a: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 5, 2014
    Inventors: Barbara Hanney, Peter Manley, Michael T. Rudd, John M. Sanders, Shawn J. Stachel, Darrell Henze
  • NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
    Publication number: 20140155370
    Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
    Type: Application
    Filed: June 28, 2013
    Publication date: June 5, 2014
    Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
  • Methods to produce polymer nanoparticles and formulations of active ingredients
    Patent number: 8741808
    Abstract: The present invention provides a composition including a polymer nanoparticle and at least one agricultural active compound incorporated with the nanoparticle, wherein the nanoparticle are less than 100 nm in diameter, and the polymer includes a polyelectrolyte.
    Type: Grant
    Filed: January 15, 2013
    Date of Patent: June 3, 2014
    Assignee: Vive Crop Protection Inc.
    Inventors: Fugang Li, Hung Hoang Pham, Darren J. Anderson
  • Oxime derivatives
    Patent number: 8742117
    Abstract: The present invention relates to novel oxime derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: June 3, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Mukul R. Jain, Pandurang Zaware
  • ACTIVE COMPOUND COMBINATIONS
    Publication number: 20140148338
    Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a thiazolylisoxazoline of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Application
    Filed: June 4, 2012
    Publication date: May 29, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Sebastian Hoffmann, Pierre Wasnaire, Ulrike Wachendorff-Neumann
  • INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS
    Publication number: 20140148462
    Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: November 25, 2013
    Publication date: May 29, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias ECKHARDT, Elke LANGKOPF, Holger WAGNER
  • NITRIC OXIDE RELEASING AMINO ACID ESTER FOR TREATMENT OF PULMONARY HYPERTENSION AND OTHER RESPIRATORY CONDITIONS
    Publication number: 20140148438
    Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.
    Type: Application
    Filed: September 22, 2011
    Publication date: May 29, 2014
    Inventor: Michael Farber
  • SPECIFIC CARBOXAMIDES AS KCNQ2/3 MODULATORS
    Publication number: 20140148468
    Abstract: The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
    Type: Application
    Filed: November 27, 2013
    Publication date: May 29, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder