Plural 1,3-diazine Rings Patents (Class 544/296)
  • SERINE/THREONINE KINASE INHIBITORS
    Publication number: 20130252934
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 26, 2013
    Applicants: Genentech, Inc., Array BioPharma Inc.
    Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
  • Combination comprising macitentan and paclitaxel for treating multi-drug resistant ovarian cancer
    Patent number: 8541433
    Abstract: The invention relates to the combination of an endothelin receptor antagonist of formula (I) with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: September 24, 2013
    Assignee: Actelion Pharmaceuticals, Ltd.
    Inventors: Martine Clozel, Urs Regenass
  • Substituted Heterocyclic Compounds
    Publication number: 20130244999
    Abstract: The present invention relates to substituted heterocyclic compounds of Formula I: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.
    Type: Application
    Filed: May 6, 2013
    Publication date: September 19, 2013
    Applicant: Incyte Corporation
    Inventors: Colin Zhang, Ding-quan Qian, Jincong Zhuo, Wenqing Yao
  • PROCESS FOR THE PREPARATION OF BOSENTAN MONOHYDRATE
    Publication number: 20130245259
    Abstract: The invention relates to improved processes for the preparation of bosentan monohydrate which provide higher yield and purity.
    Type: Application
    Filed: March 16, 2012
    Publication date: September 19, 2013
    Applicant: Natco Pharma Limited
    Inventors: Amala Kishan Kompella, Srinivasu Kasa, Veera Swamy Balina, Subhash Kusumba, Kali Satya Bhujanga Rao Adibhatla, Venkaiah Chowdary Nannapaneni
  • Crystalline forms of bosentan
    Patent number: 8530488
    Abstract: The present invention relates to novel crystalline forms of bosentan and processes for their preparation. Further, the invention relates to pharmaceutical compositions comprising said crystalline forms and use of said compositions in the treatment of patients suffering from endothelin receptor mediated disorders, for example, cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: September 10, 2013
    Assignee: Generics [UK] Limited
    Inventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Prakash Bansode, Dattatraya Shinde, Sunanda Phadtare
  • DERIVATIVES OF PYRAZOLOPHENYL-BENZENESULFONAMIDE COMPOUNDS AND USE THEREOF AS ANTITUMOR AGENTS
    Publication number: 20130217715
    Abstract: Substituted pyrazolophenyl-benzenesulfonamide compounds of formula (I) are described, wherein m, R1, R2, R3, and R4 are defined in the description, which modulate the activity of protein kinases, These compounds find utility in treating diseases caused by deregulated protein kinase activity, such as cancer and cell proliferative disorders.
    Type: Application
    Filed: August 2, 2011
    Publication date: August 22, 2013
    Inventors: Maurizio Pulici, Chiara Marchionni, Gabriella Traquandi, Alessandra Scolaro, Daniele Donati
  • IMIDAZOPYRIDINE DERIVATIVES AS JAK INHIBITORS
    Publication number: 20130216498
    Abstract: New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: December 23, 2010
    Publication date: August 22, 2013
    Inventors: Paul Robert Eastwood, Jacob Gonzales Rodriguez, Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Victor Giulio Matassa
  • Pyrimidinyl-propionic acid derivatives and their use as PPAR agonists
    Patent number: 8513233
    Abstract: The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compounds. The compounds are useful as PPAR? agonist, through activating PPAR-RXR heterodimers that interacts with specific DNA response elements within promoter regions of target gene, particularly in the treatment and prevention of polycystic kidney and cancer.
    Type: Grant
    Filed: October 11, 2007
    Date of Patent: August 20, 2013
    Assignee: Shanghai Institute of Materia Medica, CAS
    Inventors: Jianhua Shen, Changlin Mei, Hualiang Jiang, Bin Dai, Yangliang Ye, Xishan Xiong, Jing Tang, Lili Fu
  • BICYCLIC HETEROARYL KINASE INHIBITORS AND METHODS OF USE
    Publication number: 20130203755
    Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.
    Type: Application
    Filed: May 24, 2011
    Publication date: August 8, 2013
    Applicant: UNIVERSITY OF ROCHESTER
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
  • USE OF ALS INHIBITOR HERBICIDES FOR CONTROL OF UNWANTED VEGETATION IN ALS INHIBITOR HERBICIDE TOLERANT BETA VULGARIS PLANTS
    Publication number: 20130190179
    Abstract: The present invention relates generally to the use of biological or chemical control agents with for controlling insects and nematodes and to methods particularly useful for combating insects or nematodes and/or increasing crop yield in plants that are at least partially resistant to one or more parasitic nematodes or insects.
    Type: Application
    Filed: October 13, 2011
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ruediger Hain, Gerhard Johann, Guenter Donn
  • sGC STIMULATORS
    Publication number: 20130178475
    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: Application
    Filed: March 10, 2011
    Publication date: July 11, 2013
    Applicant: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: Joel Moore, James Jia, Takashi Nakai, Charles Kim, Thomas Wai-Ho Lee, Jane Yang
  • NOVEL GLP-1 RECEPTOR MODULATORS
    Publication number: 20130178420
    Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 11, 2013
    Applicant: RECEPTOS, INC.
    Inventor: RECEPTOS, INC.
  • Method of synthesis of Bosentan, its polymorphic forms and its salts
    Patent number: 8481730
    Abstract: The present invention relates to alkaline earth metal salts of bosentan, anyhdrous bosentan, polymorphic forms thereof, amorphous bosentan and processes for preparing them. The present invention further relates to a process for the preparation of bosentan and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: January 2, 2009
    Date of Patent: July 9, 2013
    Assignee: CIPLA Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Ashwini Amol Sawant
  • INHIBITORS OF SYK AND JAK PROTEIN KINASES
    Publication number: 20130165431
    Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Application
    Filed: October 23, 2012
    Publication date: June 27, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • Nitrogen-containing heteroaryl derivatives
    Patent number: 8470820
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: June 25, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento, Eric Vieira
  • MATERIAL FOR ORGANIC ELECTROLUMINESCENCE DEVICE AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME
    Publication number: 20130153874
    Abstract: Provided are an organic electroluminescence device, which: shows high luminous efficiency; is free of any pixel defect; and has a long lifetime, and a material for an organic electroluminescence device for realizing the device. The material for an organic electroluminescence device is a compound of a specific structure having a ?-conjugated heteroacene skeleton crosslinked with a carbon atom, nitrogen atom, or oxygen atom. The organic electroluminescence device has one or more organic thin film layers including a light emitting layer between a cathode and an anode, and at least one layer of the organic thin film layers contains the material for an organic electroluminescence device.
    Type: Application
    Filed: February 5, 2013
    Publication date: June 20, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventor: IDEMITSU KOSAN CO., LTD.
  • Dihydropyrimidinones
    Patent number: 8461160
    Abstract: This invention relates to dihydropyrimidinones of the formula wherein X and R1 to R7 are as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: June 11, 2013
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: David Banner, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Fabienne Ricklin, Mark Rogers-Evans
  • CO-CRYSTAL INTERMEDIATES OF ROSUVASTATIN AND METHODS OF USING SAME
    Publication number: 20130143890
    Abstract: Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.
    Type: Application
    Filed: December 3, 2012
    Publication date: June 6, 2013
    Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventor: F.I.S. Fabbrica Italiana Sintetici S.p.A.
  • SUBSTITUTED PYRIMIDINONE-PHENYL-PYRIMIDINYL COMPOUNDS
    Publication number: 20130143906
    Abstract: The present disclosure provides pyrimidinone-phenyl-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4 and R5 are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 6, 2013
    Applicant: CONFLUENCE LIFE SCIENCES, INC.
    Inventor: CONFLUENCE LIFE SCIENCES, INC.
  • NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
    Publication number: 20130143892
    Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: June 6, 2012
    Publication date: June 6, 2013
    Applicants: NEUROCRINE BIOSCIENCES, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Armin HECKEL, Frank HIMMELSBACH, Elke LANGKOPF, Bernd NOSSE, Neil J. ASHWEEK, Nicole HARRIOTT
  • Gonadotropin Releasing Hormone Receptor Antagonist, Preparation Method Thereof And Pharmaceutical Composition Comprising The Same
    Publication number: 20130137661
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Application
    Filed: November 19, 2010
    Publication date: May 30, 2013
    Applicant: SK CHEMICALS CO. LTD.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLES AS OREXIN RECEPTOR MODULATORS
    Publication number: 20130137672
    Abstract: Certain disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo[3.2.0]heptane are described, which are useful as orexin inhibitors. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: October 21, 2010
    Publication date: May 30, 2013
    Inventors: Bryan James Branstetter, Michael A. Letavic, Kiev S. Ly, Dale A. Rudolph, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman
  • MATERIALS FOR ELECTRONIC DEVICES
    Publication number: 20130126792
    Abstract: The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices and electronic devices comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I).
    Type: Application
    Filed: July 12, 2011
    Publication date: May 23, 2013
    Applicant: Merck Patent GmbH
    Inventors: Irina Martynova, Adam W. Franz, Christof Pflumm, Amir Hossain Parham, Arne Buesing, Rémi Manouk Anémian, Anja Gerhard
  • PYRAZINE KINASE INHIBITORS
    Publication number: 20130131040
    Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: November 23, 2012
    Publication date: May 23, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • 2-Thiopyrimidinones
    Publication number: 20130123230
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Application
    Filed: November 7, 2012
    Publication date: May 16, 2013
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Sulfonyl amide derivatives for the treatment of abnormal cell growth
    Patent number: 8440822
    Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: May 14, 2013
    Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
  • NOVEL HETEROCYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME
    Publication number: 20130112946
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein X1 and X2, X1 and R1 to R10 are defined as in the specification.
    Type: Application
    Filed: February 29, 2012
    Publication date: May 9, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Bum-Woo Park, Yoon-Hyun Kwak, Sun-Young Lee, Chang-Ho Lee, Se-Jin Cho
  • Dihydropyrimidone amides as P2X7 modulators
    Patent number: 8435990
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5, Ra and Rb are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: May 7, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Christine E. Brotherton-Pleiss, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker
  • CONDENSED-CYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME
    Publication number: 20130105769
    Abstract: A condensed-cyclic compound represented by Formula 1, and an organic light-emitting device including the condensed-cyclic compound. wherein R1 and R2, Ar1 through Ar4, L1 and L2, X1 and X2, and a and b are defined as in the specification.
    Type: Application
    Filed: May 22, 2012
    Publication date: May 2, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Jin-O Lim, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Sang-Hyun Han, Soo-Yon Kim, Hee-Joo Ko
  • Method for inhibiting melanin production and whitening skin with pyrimidlypyrazole compounds or pharmaceutically acceptable salts thereof
    Patent number: 8426435
    Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein, R1, R3, R4, and R6 are each independently C1-3 alkyl; and R2 and R5 are each independently a hydrogen atom or C1-3 alkyl.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: April 23, 2013
    Assignee: Shiseido Company Ltd.
    Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
  • Pyrazolopyridine, Pyrazolopyrazine, Pyrazolopyrimidine, Pyrazolothiophene and Pyrazolothiazole Compounds as MGLUR4 Allosteric Potentiators, Compositions, and Methods of Treating Neurological Dysfunction
    Publication number: 20130096110
    Abstract: Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Application
    Filed: February 11, 2011
    Publication date: April 18, 2013
    Applicant: VANDERBILT UNIVERSITY
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
  • Substituted 5-fluoro-1H-pyrazolopyridines and their use
    Patent number: 8420656
    Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: April 16, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
  • Fused heterocyclic ring compound
    Patent number: 8410089
    Abstract: A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, A1: CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: —COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: April 2, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kentaro Rikimaru, Hiroshi Imoto, Masahiro Kamaura
  • Selective NR2B Antagonists
    Publication number: 20130079338
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: September 24, 2012
    Publication date: March 28, 2013
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventor: Bristol-Myers Squibb Company
  • Electroluminescent Device
    Publication number: 20130079517
    Abstract: Disclosed are electroluminescent devices that comprise organic layers that contain certain organic compounds containing one or more pyrimidine moieties. The organic compounds containing one or more pyrimidine moieties are suitable components of blue-emitting, durable, organo-electroluminescent layers. The electroluminescent devices may be employed for full color display panels in for example mobile phones, televisions and personal computer screens.
    Type: Application
    Filed: October 18, 2012
    Publication date: March 28, 2013
    Applicant: BASF SE
    Inventor: BASF SE
  • PYRIMIDINE CYCLOHEXYL GLUCOCORTICOID RECEPTOR MODULATORS
    Publication number: 20130072486
    Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: March 16, 2012
    Publication date: March 21, 2013
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
  • COMPOUNDS USEFUL AS RAF KINASE INHIBITORS
    Publication number: 20130065858
    Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
    Type: Application
    Filed: October 22, 2012
    Publication date: March 14, 2013
    Applicants: SUNESIS PHARMACEUTICALS, INC., MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: MILLENNIUM PHARMACEUTICALS, INC., SUNESIS PHARMACEUTICALS, INC.
  • NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS
    Publication number: 20130059830
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 16, 2011
    Publication date: March 7, 2013
    Inventors: Fa-Xiang Ding, Jinlong Jiang, Dong-Ming Shen, Zhi-Cai Shi, Min Shu, Cangming Yang
  • PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE
    Publication number: 20130059839
    Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.
    Type: Application
    Filed: April 18, 2011
    Publication date: March 7, 2013
    Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
    Inventors: Nicholas J. Lawrence, Roberta Pireddu, Said M. Sebti
  • HETEROCYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE CONTAINING THE SAME
    Publication number: 20130048955
    Abstract: A heterocyclic compound represented by one of Formulae 1-4 below and an organic light-emitting device including an organic layer that includes the heterocyclic compound. The heterocyclic compounds have excellent light-emitting characteristics and excellent electron transporting characteristics, and thus may be used as electron injecting materials or electron transporting materials suitable for all-color fluorescent and phosphorescent devices, such as red, green, blue, and white fluorescent and phosphorescent devices. In particular, the heterocyclic compounds are efficiently used as light-emitting materials of green, blue, and while fluorescent devices. By using the heterocyclic compounds, organic light-emitting devices having high efficiency, low driving voltage, high brightness, and long lifespan may be prepared.
    Type: Application
    Filed: April 4, 2012
    Publication date: February 28, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Sun-Young Lee, Yoon-Hyun Kwak, Bum-Woo Park, Jong-Hyuk Lee, Jin-Young Yun
  • HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20130053362
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
    Type: Application
    Filed: July 18, 2012
    Publication date: February 28, 2013
    Applicants: INTELLKINE, LLC, INFINITY PHARMACEUTICALS, INC.
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Substituted 4-hydroxypyrimidine-5-carboxamides
    Patent number: 8372857
    Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: February 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina Madsen-Duggan
  • AMIDE DERIVATIVES BEARING A CYCLOPROPYLAMINOACARBONYL SUBSTITUENT USEFUL AS CYTOKINE INHIBITORS
    Publication number: 20130035346
    Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Application
    Filed: September 27, 2012
    Publication date: February 7, 2013
    Applicant: AstraZeneca AB
    Inventor: AstraZeneca AB
  • SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
    Publication number: 20130029987
    Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
    Type: Application
    Filed: April 20, 2012
    Publication date: January 31, 2013
    Inventors: Brydon L. Bennett, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mehran F. Moghaddam, Mark A. Nagy, Stephen Norris, David A. Paisner, Marianne Sloss, William J. Romanow, Yoshitaka Satoh, Jayashree Tikhe, Won Hyung Yoon, Mercedes Delgado
  • CERTAIN KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
    Publication number: 20130029988
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Application
    Filed: January 20, 2011
    Publication date: January 31, 2013
    Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Dirk Winkler, Frederick Brookfield, Paula C. De Aguiar Pena
  • Bispyrimidines for electronic applications
    Patent number: 8362246
    Abstract: The present invention relates to compounds of formula a process for their production and their use in electronic devices, especially electroluminescent devices. When used as electron transport material in electroluminescent devices, the compounds of formula I, or II may provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.
    Type: Grant
    Filed: December 9, 2011
    Date of Patent: January 29, 2013
    Assignee: BASF SE
    Inventors: Thomas Schaefer, Heinz Wolleb, Christian Schildknecht, Soichi Watanabe, Christian Lennartz
  • SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS
    Publication number: 20130023502
    Abstract: The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
    Type: Application
    Filed: January 25, 2012
    Publication date: January 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Georg Dahmann, Dennis Fiegen, Martin Fleck, Matthias Hoffmann, Jasna Klicic, Stephen Peter East, Spencer Charles R. Napier, John Scott
  • FAK INHIBITORS
    Publication number: 20130017194
    Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 17, 2013
    Applicant: Cancer Therapeutics CRC Pty Limited
    Inventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
  • SOLUBLE GUANYLATE CYCLASE ACTIVATORS
    Publication number: 20130012511
    Abstract: The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
    Type: Application
    Filed: March 22, 2011
    Publication date: January 10, 2013
    Inventors: Darby Schmidt, Subharekha Raghavan, John Stelmach, Jian Guo, Jonathan Groeper, Linda Brockunier, Keith Rosauer, Hong Shen, Rui Liang, Fa-Xiang Ding
  • Pyrimidine Sulphonamide Derivatives as Chemokine Receptor Modulators
    Publication number: 20130012490
    Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston