At 2-position Patents (Class 544/315)
  • Patent number: 10301288
    Abstract: There are provided compounds of formula (III), or a salt or protected derivative thereof, wherein Z2 represents a structural fragment of formula (V), wherein R1, Ra, Rb, X and Y have meanings given in the description, which compounds have antiinflammatory activity, for example through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: December 4, 2017
    Date of Patent: May 28, 2019
    Assignee: Topivert Pharma Limited
    Inventor: Matthew Colin Thor Fyfe
  • Patent number: 10208017
    Abstract: The present disclosure is directed in part to heterocycles, and their use in treating medical disorders, such as immune inflammatory disorders such as Crohn's disease, ulcerative colitis, rheumatic disorders, psoriasis, and allergies. The compounds are contemplated to modulate T-Cell responses.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: February 19, 2019
    Assignee: Nogra Pharma Limited
    Inventors: Daan Hommes, Auke Verhaar, Gijs Van den Brink, Francesca Viti
  • Patent number: 10196363
    Abstract: A compound of Formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is defined as in the specification.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: February 5, 2019
    Assignee: JAPAN TOBACCO INC.
    Inventors: Masahiro Yokota, Taku Ikenogami, Eiichi Watanabe, Noriyoshi Seki, Shingo Fujioka, Makoto Shiozaki, Masato Noguchi
  • Patent number: 9090605
    Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: July 28, 2015
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer-Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
  • Patent number: 9067893
    Abstract: The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Grant
    Filed: April 28, 2014
    Date of Patent: June 30, 2015
    Assignee: Nivalis Therapeutics, Inc.
    Inventors: Xicheng Sun, Jian Qiu
  • Publication number: 20150144845
    Abstract: Provided is a solvent or solvent composition for organic transistor production that is excellent in solubility of an organic semiconductor material and that can form an organic transistor high in crystallinity. The solvent or solvent composition for organic transistor production according to the present invention is a solvent or solvent composition for organic semiconductor material dissolution, including a solvent A represented by the following formula (A). In the formula (A), R1 to R4 are the same or different, and represent a C1-2 alkyl group. R1 and R4 may be bound to each other to form a ring together with —N(R2)—C(?O)—N(R3)— in the formula.
    Type: Application
    Filed: June 3, 2013
    Publication date: May 28, 2015
    Applicant: DAICEL CORPORATION
    Inventors: Youji Suzuki, Takeshi Yokoo, Yasuyuki Akai
  • Patent number: 9040697
    Abstract: 4,6-dichloro-2-methyl-5-(1-acyl-2-imidazolin-2-yl)-aminopyrimidine is reacted with methanol in the presence of a non-ionic organic base, and moxonidine is obtained directly from the reaction mixture.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: May 26, 2015
    Assignee: AREVIPHARMA GmbH
    Inventors: Harald Hofmeier, Michael Limmert, Heike Heydemüller, Helge Hartenhauer
  • Publication number: 20150133449
    Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
  • Patent number: 8946250
    Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: February 3, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maurizio Pulici, Fabio Zuccotto, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro′, Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Chiara Marchionni, Michele Modugno
  • Publication number: 20150025094
    Abstract: The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, hal
    Type: Application
    Filed: August 1, 2012
    Publication date: January 22, 2015
    Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan University
    Inventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
  • Patent number: 8933090
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: January 13, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
  • Patent number: 8921563
    Abstract: Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: December 30, 2014
    Assignee: Institue of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., China
    Inventors: Yunfeng Li, Rifang Yang, Youzhi Zhang, Yongzhen Li, Zengliang Jin, Peng Li, Li Yuan, Liuhong Yun, Nan Zhao, Cheng Zhang, Xiaodan Xu, Rusheng Zhao, Hongxia Chen, Rui Xue, Juanjuan Qin, Zhenzhen Wang, Jiazhi Yao
  • Patent number: 8889700
    Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: November 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
  • Publication number: 20140336190
    Abstract: This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2, R2b, R3, R4a, R4b, and R5 are described herein.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Patent number: 8859573
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: October 14, 2014
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • Patent number: 8859769
    Abstract: Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.
    Type: Grant
    Filed: February 15, 2011
    Date of Patent: October 14, 2014
    Assignee: Actavis Group PTC EHF
    Inventors: Anil Shahaji Khile, Jayesh Patel, Nikhil Trivedi, Nitin Sharadchandra Pradhan
  • Patent number: 8846689
    Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 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: November 24, 2009
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Ioannis Sapountzis
  • Patent number: 8835426
    Abstract: This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: September 16, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Wei Zhao
  • Patent number: 8754208
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: June 17, 2014
    Assignee: International Business Machines Corporation
    Inventors: James L. Hedrick, Alshakim Nelson, Daniel P. Sanders
  • Publication number: 20140163221
    Abstract: The invention relates to a process for the synthesis of cyclic alkylene ureas comprising reacting in the presence of a basic catalyst, a difunctional amine A having two primary amino groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA, wherein the ratio of the amount of substance Ji(—NH2) of primary amino groups —NH2 in the difunctional amine A to the sum M(C) of the amount of substance n(CD) of carbonate groups of a dialkyl carbonate CD and the amount of substance n(CA) of carbonate groups in an alkylene carbonate CA, is at least more than 2, and to the product obtained by this process.
    Type: Application
    Filed: July 19, 2012
    Publication date: June 12, 2014
    Applicant: Allnex USA Inc.
    Inventors: Ram Gupta, Irina Kobylanska, Urvee Treasurer, Lawrence Flood
  • Patent number: 8729265
    Abstract: The present invention relates to a method of making pyrimidines of formula (III) said method comprising reacting a compound of formula (I) with an oxygen, sulfur or nitrogen nucleophile of formula T-H; and reacting the compound obtained with an amine of formula (II) [HN(R1)R2] to form a compound of formula (III) wherein X1, X2, T, R1 and R2 have the meanings as defined herein.
    Type: Grant
    Filed: August 13, 2010
    Date of Patent: May 20, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenter Linz, Gerd Kraemer
  • Publication number: 20140113908
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY, Beatrix WAGNER
  • Patent number: 8697715
    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: Grant
    Filed: March 1, 2013
    Date of Patent: April 15, 2014
    Assignees: Array BioPharma, Inc., Genentech, 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
  • Patent number: 8691817
    Abstract: The present application relates to novel sulfonamide- or sulfoximine-substituted 1,4-diaryldihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: April 8, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Dirk Schneider
  • Patent number: 8686007
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 1, 2014
    Assignee: Cytokinetics, Inc.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 8642620
    Abstract: The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: February 4, 2014
    Assignee: Sanofi
    Inventors: Harmut Strobel, Paulus Wohlfart, Gerhard Zoller, David William Will
  • Patent number: 8614320
    Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: December 24, 2013
    Assignee: AstraZeneca UK Limited
    Inventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
  • Publication number: 20130324566
    Abstract: The invention provides pyrimidine compounds of general formula (I), which reduce simultaneously the production of nitric oxide (NO) and prostaglandin E2 (PGE2). They have no negative effect on the viability of cells in concentrations decreasing the production of these factors by up to 50%; they are not cytotoxic. Furthermore, a method of preparation of the pyrimidine compounds of general formula (I), carrying 2-formamido group, a pharmaceutical composition comprising the substituted pyrimidine compounds according to the invention, and the use of these compounds for the treatment of inflammatory and cancer diseases are provided.
    Type: Application
    Filed: February 27, 2012
    Publication date: December 5, 2013
    Applicants: USTAV EXPERIMENTALNI MEDICINY AKADEMIE VED CR, V.V.I., USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CR, V.V.I.
    Inventors: Petr Jansa, Antonin Holy, Zdenek Zidek, Eva Kmonickova, Zlatko Janeba
  • Patent number: 8575342
    Abstract: Compounds of formula (I), N-oxides, pharmaceutical acceptable salts, quaternary amines or stereoisomeric forms thereof, and their use as HIV replication inhibitors, In the formula, -a1=a2-a3=a4- and -b1=b2-b3=b4- may be —C?C—C?C—; X1 may be O, NR1, etc.; R1, R2, R2a, R3, R4 and R5 are assorted substituents as defined in the specification.
    Type: Grant
    Filed: September 29, 2005
    Date of Patent: November 5, 2013
    Assignee: Tibotech Pharmaceuticals Ltd.
    Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
  • Patent number: 8552002
    Abstract: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
    Type: Grant
    Filed: June 23, 2005
    Date of Patent: October 8, 2013
    Assignees: Novartis AG, IRM LLC
    Inventors: Qiang Ding, Nathanael Schiander Gray, Bing Li, Yi Liu, Taebo Sim, Tetsuo Uno, Guobao Zhang, Carole Pissot Soldermann, Werner Breitenstein, Guido Bold, Giorgio Caravatti, Pascal Furet, Vito Guagnano, Marc Lang, Paul William Manley, Joseph Schoepfer, Carsten Spanka
  • Patent number: 8546404
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Grant
    Filed: June 5, 2007
    Date of Patent: October 1, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr., Neng-Yang Shih, Hugh Y. Zhu, Robert Sun, Joseph M. Kelly, Ronald J. Doll, Yang Nan, Tong Wang, Jagdish A. Desai, James J-S Wang, Youhao Dong, Vincent S. Madison, Li Xiao, Alan W. Hruza, M. Arshad Siddiqui, Ahmed A. Samatar, Sunil Paliwal, Hon-Chung Tsui, Azim Alan Celebi, Yiji Wu, Sobhana Babu Boga, Abdul-Basit Alhassan, Xiaolei Gao, Liang Zhu, Mehul Patel
  • Patent number: 8512820
    Abstract: Ionic mesogenic compounds of formula (I) can be used to form liquid crystal displays, such as ferroelectric liquid crystal displays, having enhanced anti-image sticking properties. The mesogenic compounds may contain a cationic group such as an ammonium or phosphonium group bonded to an alkyl chain that is terminally bonded to a para-substituted pyrimidyl benzene moiety. The counterion can be an organic or inorganic anion. The compounds can be used either as dopants in art ferroelectric liquid crystal compositions to reduce image sticking, or can be used as the primary or predominant component of a liquid crystal display system. Additional compounds, devices, and methods are disclosed.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: August 20, 2013
    Assignee: Citizen Finetech Miyota Co., Ltd.
    Inventors: Yongqiang Zhang, Su Yang
  • Patent number: 8492542
    Abstract: The present invention is directed to a method producing bicyclic guanidine comprising heating a cyclic thiourea to a temperature ranging from ?140° C. in a substantially non-hydrocarbon solvent to form the bicyclic guanidine.
    Type: Grant
    Filed: May 15, 2008
    Date of Patent: July 23, 2013
    Assignee: PPG Industries Ohio, Inc.
    Inventors: Britt A. Minch, Charles R. Hickenboth, Richard F. Karabin, Steven R. Zawacky, Thomas R. Hockswender, Gregory J. McCollum
  • Patent number: 8476428
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: July 2, 2013
    Assignee: International Business Machines Corporation
    Inventors: James Lupton Hedrick, Alshakim Nelson, Daniel Paul Sanders
  • Patent number: 8470835
    Abstract: The present invention relates to the compound of formula (I): or a salt, preferably a pharmaceutically acceptable salt, thereof; is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate mast cell activation, for instance allergic and inflammatory diseases, as well of potential use in cancer therapy, specifically heme malignancies.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: June 25, 2013
    Assignee: Glaxo Group Limited
    Inventors: Francis Louis Atkinson, Vipulkumar Kantibhai Patel
  • Patent number: 8431710
    Abstract: A process for the manufacture of a cyclic compound of formula (I) which comprises (a) adding an acid halide of formula R1—C(O)—X, to a vinyl ether of formula (II): CH2?CH—OR2, to produce an addition product, and (b) reacting the addition product with a compound of formula (III): Y-A-Z; wherein R1 is a halogenated alkyl group; wherein X is fluorine, chlorine, or bromine; wherein R2 is an alkyl group, an aralkyl group, or an aryl group; wherein Z and Y designate independently carbon or a heteroatom; and wherein A is a linking group between Z and Y comprising 0, 1, 2 or 3 atoms in the cycle.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: April 30, 2013
    Assignee: Solvay SA
    Inventor: Max Braun
  • Patent number: 8410116
    Abstract: Disclosed are bis(styryl)pyrimidine or bis(styryl)benzene compounds, represented by Chemical Formula 1, pharmaceutically acceptable salts, a method for preparing the same, and a pharmaceutical composition for the prevention and treatment of amyloidosis-associated diseases, comprising the same as an active ingredient. Having the ability to inhibit the deposition of beta amyloid and to reduce the toxicity of beta amyloid, the derivatives can improve learning and memory and can be useful in the prevention and treatment of amyloidosis-associated diseases. (wherein R1, R2, R3 and X are as defined in the specification).
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: April 2, 2013
    Assignee: Korea Institute of Science and Technology
    Inventors: Kye Jung Shin, Eun Joo Roh, Yun Suk Lee
  • Publication number: 20130079361
    Abstract: Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula (I): wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions comprising a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions, comprising administering a safe and effective amount of a Formula I compound.
    Type: Application
    Filed: September 24, 2010
    Publication date: March 28, 2013
    Inventors: Robert A. Mitchell, John O. Trent, Pooran Chand, Gilles Hugues Tapolsky
  • Patent number: 8343987
    Abstract: The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction, and heart failure development.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: January 1, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Heike Gielen-Haertwig, Barbara Albrecht, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
  • Patent number: 8334292
    Abstract: Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: December 18, 2012
    Assignee: Cystic Fibrosis Foundation Therapeutics, Inc.
    Inventor: Phoebe Chiang
  • Patent number: 8324231
    Abstract: A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways.
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: December 4, 2012
    Assignee: Exelixis, Inc.
    Inventors: Elena S. Koltun, Patrick Kearney, Naing Aay, Arlyn Arcalas, Wai Ki Vicky Chan, Jeffry Kimo Curtis, Hongwang Du, Ping Huang, Brian Kane, Moon Hwan Kim, Michael Pack, Amy L. Tsuhako, Wei Xu, Cristiana A. Zaharia, Peiwen Zhou
  • Patent number: 8299086
    Abstract: The invention relates to novel pyrimidine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: October 30, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
  • Patent number: 8288402
    Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: October 16, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
  • Publication number: 20120252808
    Abstract: The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: December 13, 2010
    Publication date: October 4, 2012
    Inventors: Scott D. Kuduk, Kelly-Ann S. Schlegel, Zhi-Qiang Yang
  • Patent number: 8263588
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: September 11, 2012
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
  • Patent number: 8222412
    Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: July 17, 2012
    Assignee: AstraZeneca UK Limited
    Inventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
  • Patent number: 8222266
    Abstract: The present invention relates to certain azabicyclo compounds of formula (I)?: wherein the various groups are defined herein and that are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: July 17, 2012
    Assignee: Glaxo Group Limited
    Inventors: Barbara Bertani, Anna Checchia, Romano Di Fabio, Gabriella Gentile, Fabrizio Micheli, Alessandra Pasquarello, Silvia Terreni
  • Patent number: 8217155
    Abstract: The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R1 is —OH or —OCH3; R2 is —H, lower alkyl (e.g. C1-C4 alkyl) or glycosidyl; and R3 and R4 are independently —CH3, —C(O)H or —CH2OR6, wherein R6 is —H or a hydrocarbyl group having 1 to 20 carbon atoms.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: July 10, 2012
    Assignees: Gilead Colorado, Inc., Abbott GmbH & Co. KG
    Inventors: Lawrence S. Melvin, Jr., Martina Ullrich, Hans-Guenther Hege, Jürgen Weymann
  • Patent number: 8178700
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl) carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: May 15, 2012
    Assignee: International Business Machines Corporation
    Inventors: James L. Hedrick, Alshakim Nelson, Daniel P. Sanders
  • Patent number: RE43748
    Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: October 16, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura