Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 548/217)
  • Patent number: 9744212
    Abstract: The present invention provides a novel composition of matter useful for the treatment of neoplastic diseases. The novel composition is synergistic and comprised of galectin-3C in combination with a proteasome inhibitor, the combination having a pharmacologic activity greater than the expected additive effect of its individual components. Other embodiments of the invention provide novel synergistic compositions of galectin-3C with a proteasome inhibitor capable of reducing or overcoming resistance that develops to the proteasome inhibitor or reducing the adverse side effects from the proteasome inhibitor through increasing the therapeutic efficacy of lower doses.
    Type: Grant
    Filed: February 8, 2016
    Date of Patent: August 29, 2017
    Assignee: Texas Tech University System
    Inventors: Maurizio Chiriva-Internati, Everardo Cobos, Constance John
  • Publication number: 20150148546
    Abstract: Provided is a photosensitive resin composition having high sensitivity and storage stability.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Applicant: FUJIFILM Corporation
    Inventors: Kyouhei SAKITA, Shinji FUJIMOTO, Mikio NAKAGAWA, Kenta YAMAZAKI
  • Patent number: 9024038
    Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: May 5, 2015
    Assignee: Purdue Research Foundation
    Inventors: Arun K. Ghosh, Bruno D. Chapsal, Hiroaki Mitsuya, Cuthbert D. Martyr
  • Publication number: 20150094329
    Abstract: A compound represented by formula (1) and an N-oxide thereof have excellent pest control effect. (In the formula, Het to which R1—S(O)n is bonded represents a five-membered aromatic heterocyclic ring represented by formula H1, H2, H3 or H4 (wherein Y1 represents an oxygen atom or the like; Y2 represents an oxygen atom or the like; G1, G2 and G3 may be the same or different and each represents a nitrogen atom or the like; R1 represents a C1-C6 alkyl group which may have one or more atoms or groups selected from the group X, or the like; and n represents 0, 1 or 2); A1 represents an oxygen atom or the like; A2 represents a nitrogen atom or the like; A3 represents a nitrogen atom or the like; and R2 and R3 may be the same or different and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from the group X, or the like.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 2, 2015
    Inventors: Yoshihiko Nokura, Mai Ito, Chie Shimizu, Hajime Mizuno
  • Patent number: 8993607
    Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: March 31, 2015
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Joseph E. Rice
  • Patent number: 8969349
    Abstract: Provided herein are compounds of formula A-L-B, and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is R1 and R2 together with the carbon atoms to which they are attached form a 1,2-phenylene ring optionally substituted with one or more R11; L is —C(R6)2—C(R6)2—; B is a heteroaromatic group defined herein; and -A1-A2- , A3, R11 and R6 are defined herein. Also disclosed are methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: March 3, 2015
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: John Emmerson Campbell, Michael Charles Hewitt, Philip Jones, Linghong Xie
  • Patent number: 8962835
    Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 24, 2015
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Patent number: 8957219
    Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: February 17, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Shiro Kida, Kyohei Hayashi, Manabu Katou, Naoki Yoshikawa, Akira Kugimiya, Mado Nakajima, Nobuyuki Tanaka
  • Publication number: 20150031694
    Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
  • Publication number: 20150031735
    Abstract: The present invention relates to solid forms of the N-methyl-D-glucamine (meglumine) salt of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one solid form and to the therapeutic or prophylactic use of such solid forms and compositions.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 29, 2015
    Inventors: Richard Frederic Labaudiniere, MICHAEL HENRY O'Neill
  • Publication number: 20150005283
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 1, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Patent number: 8921369
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: December 30, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20140371278
    Abstract: Disclosed are compound of formula (I) and pharmaceutically accepted salts and prodrugs thereof, wherein each of R1, R2, R3, R4, R5, R6, X1 and X2 is as defined in the description. These compounds are protein kinases inhibitors, especially the inhibitors of Mek, which are useful in the treatment of cancers and inflammation of mammals. Disclosed are the treatment methods of cancers and inflammation of mammals as well as pharmaceutical compositions comprising the compounds described herein. The preparation of benzoheterocyclic compounds are disclosed. Disclosed are the preparation of potential drug candidates, such as benzooxazol, benzothiazol, benzothiadiazol and the like.
    Type: Application
    Filed: January 16, 2013
    Publication date: December 18, 2014
    Applicant: TIANJIN BINJIANG PHARMA, INC.
    Inventors: Hongqi Tian, Conghui Ji, Chunlei Liu, Li Kong, Ying Cheng, Gongchao Huang
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Patent number: 8895591
    Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: November 25, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Uchikawa, Tatsuki Koike, Yasutaka Hoashi, Takafumi Takai
  • Patent number: 8884029
    Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: November 11, 2014
    Assignee: Adeka Corporation
    Inventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Mitsuhiro Okada, Toru Yano, Yohei Aoyama, Yusuke Kubota
  • Patent number: 8883833
    Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 11, 2014
    Assignee: Decode Genetics EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
  • Patent number: 8883437
    Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: November 11, 2014
    Assignee: bioMérieux S.A.
    Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20140322278
    Abstract: Compositions and methods are provided for modulating the physiological activation of tissue transglutaminase (TG2); which methods can include inhibiting the activation of TG2 associated with enteric inflammatory disorders, which disorders may include celiac disease, irritable bowel syndrome, Crohn's Disease, dermatitis herpetiformis, and the like. In other embodiments of the invention, methods are provided for reducing undesirable paracellular transport in enteric tissues, in particular the paracellular transport of molecules greater than about 500 mw, e.g. peptides, including without limitation immunogenic gluten peptides.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 30, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Thomas DiRaimondo, Xi Jin, Cornelius Kloeck, Chaitan Khosla
  • Publication number: 20140315945
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Publication number: 20140315881
    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: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Patent number: 8859592
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: October 14, 2014
    Assignee: Syngenta Corp Protection LLC
    Inventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
  • Publication number: 20140296246
    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, R2a, R2b, R3, and X are described herein.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Ruben Martinez, Samuel E. Metobo, Michael R. Mish, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Publication number: 20140288302
    Abstract: A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R1R2)—C(?O)—NR3R4 and a group represented by formula: —R5, a broken line represents presence or absence of a bond, Z is —NR6—, ?N—, —O—, or —S—, R6 is halogen or substituted or unsubstituted alkyl, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen or substituted or unsubstituted alkyl, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.
    Type: Application
    Filed: March 18, 2014
    Publication date: September 25, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji MASUDA, Shiro KIDA, Kyohei HAYASHI, Manabu KATOU, Naoki YOSHIKAWA, Akira KUGIMIYA, Mado NAKAJIMA, Nobuyuki TANAKA
  • Publication number: 20140246094
    Abstract: Asymmetric dyes of the D-?-A type have the Formula (1), including the valence tautomers thereof. The dyes of Formula (1) are suitable for use in dye-sensitized solar cells (DSSC), in photoelectrochemical devices or in photonic devices. A solar cell and a device for photoelectric conversion contain an asymmetric dye of Formula (1). The dyes of Formula (1) are also suitable for conjugating with optically active nanoparticles (NP).
    Type: Application
    Filed: August 24, 2012
    Publication date: September 4, 2014
    Applicant: PIANETA S.R.L.
    Inventor: Giuseppe Caputo
  • Publication number: 20140243310
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: October 23, 2012
    Publication date: August 28, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tohru Yamashita, Takuya Fujimoto, Ryo Mizojiri, Kazuko Yonemori, Hideki Hirose, Zenichi Ikeda, Ikuo Fujimori, Kyoko Toyofuku, Tsuneo Yasuma, Nobuyuki Matsunaga
  • Publication number: 20140221339
    Abstract: The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.
    Type: Application
    Filed: August 17, 2012
    Publication date: August 7, 2014
    Applicant: NIPPON SHINYAKU CO., LTD.
    Inventor: Hironori Otsu
  • Patent number: 8796253
    Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stephen Boyer, Michael Härter, Philip Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
  • Publication number: 20140205537
    Abstract: Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.
    Type: Application
    Filed: June 22, 2012
    Publication date: July 24, 2014
    Applicant: ZENOBIA THERAPEUTICS, INC.
    Inventors: Pierre-Yves Bounaud, Vicki Nienaber, Ruo W. Steensma, John A. Lowe, III
  • Patent number: 8778627
    Abstract: Enzyme substrates and associated technology of the present invention are provided. An enzyme substrate of the invention may comprise a biologically functional fluorescent dye and an enzyme-specific substrate moiety attached in such a way that the functionality of the functional dye is diminished. An enzymatic reaction may cleave at least a portion of the substrate moiety from the enzyme substrate to provide a more functional product dye. This product dye may be nonfluorescent or weakly fluorescent, in general, and relatively fluorescent, in a particular condition, such as when bound to a partner biological molecule or an assembly of partner biological molecules. An enzyme substrate of the present invention may thus be useful in fluorescence detection, and/or in any of a variety of useful applications, such as the detection of enzymatic activity in a cell-free system or in a living cell, the screening of drugs, or the diagnosis of disease.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: July 15, 2014
    Assignee: Biotium, Inc.
    Inventors: Fei Mao, Hui Cen, Wai-Yee Leung
  • Patent number: 8772323
    Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: July 8, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
  • Patent number: 8765731
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: July 1, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, Jr., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
  • Patent number: 8754113
    Abstract: A compound represented by the formula: or its pharmaceutically acceptable salt. Ring A is aromatic carbocycle or aromatic heterocycle, Z is —O— or —S—, R1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2 and R3 are each independently hydrogen, halogen, hydroxy or the like, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R8 is carboxy, cyano, substituted or unsubstituted alkyl or the like, Rx is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, and m is an integer of 0 to 3.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: June 17, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
  • Patent number: 8735597
    Abstract: Disclosed is a novel benzoxazole derivative which has high excitation energy, particularly high triplet excitation energy, and is a bipolar substance. A benzoxazole derivative represented by the following General Formula (G1) is provided. In the formula, R1 and R2 independently represent a hydrogen atom, an alkyl group with 1 to 4 carbon atoms, or a substituted or unsubstituted aryl group with 6 to 13 carbon atoms, substituents of the substituted aryl group may be bonded to form a ring which may form a spiro ring structure, R11 to R14 independently represent a hydrogen atom, a halogen, an alkyl group with 1 to 4 carbon atoms, or an unsubstituted aryl group with 6 to 10 carbon atoms, a bond formed between any two of ?, ?, and ? forms a carbazole skeleton, and n is 0 to 3.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: May 27, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Patent number: 8697911
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: April 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • Patent number: 8691980
    Abstract: A latent fluorophore is derived from salicylic acid, and containing a fluorogenic group and a moiety represented by formula I wherein the fluorogenic group is directly linked to the moiety of formula I or indirectly linked thereto via a linkage structure. In addition, a method of preparing a latent fluorophore, a method of using the same and a kit containing the same are also introduced.
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: April 8, 2014
    Assignee: National Taipei University of Technology
    Inventor: Sheng-Tung Huang
  • Patent number: 8653070
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: February 18, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
  • Publication number: 20140038975
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Application
    Filed: March 27, 2012
    Publication date: February 6, 2014
    Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140031549
    Abstract: This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
    Type: Application
    Filed: October 1, 2013
    Publication date: January 30, 2014
    Applicant: OPKO Health, Inc.
    Inventors: George G. Wu, Gerald Werne, Xiaoyong Fu, Robert K. Orr, Frank Xing Chen, Jian Cui, Victoria M. Sprague, Fucheng Zhang, Ji Xie, Liansheng Zeng, Louis Peter Castellanos, Yuyin Chen, Marc Poirier, Ingrid Mergelsberg
  • Patent number: 8632937
    Abstract: Lithographic printing plate precursor comprising (a) a lithographic substrate with a hydrophilic surface and (b) a radiation-sensitive coating on the hydrophilic surface comprising (i) one or more types of monomers and/or oligomers and/or polymers, each comprising at least one ethylenically unsaturated group accessible to a free-radical polymerization, (ii) at least one sensitizer, and (iii) at least one coinitiator capable of forming free radicals together with the sensitizer, said coinitiator being other than metallocenes, characterized in that the at least one sensitizer comprises a compound of formula (I) wherein at least one of the groups R9 to R12 is a bulky group which has a van der Waals volume of at least 55 ?3.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 21, 2014
    Assignee: Eastman Kodak Company
    Inventors: Bernd Strehmel, Harald Baumann
  • Publication number: 20140005409
    Abstract: A compound represented by the following formula (I): wherein in formula (I), R1 represents a hydrogen atom, an alkyl group, an alkenyl group, an alkoxy group, an alkoxycarbonyl group, an acyl group, a carbamoyl group, a sulfamoyl group, a sulfo group, a cyano group, an aryl group or a heteroaryl group; R2 represents an alkyl group or an aryl group; each of R3 and R4 independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkoxy group, an alkoxycarbonyl group, a carbonyl group or an aryl group; X represents —O—, —S—, —NH—, —NR5—, —CH2—, —CR6H— or —CR6R7—; each of R5 to R7 independently represents an alkyl group or an aryl group; and R1 and any one of R5 to R7, or R3 and R4, may be bonded to each other to form a ring.
    Type: Application
    Filed: September 5, 2013
    Publication date: January 2, 2014
    Applicant: FUJIFILM CORPORATION
    Inventors: Youhei ISHIJI, Masanori HIKITA
  • Patent number: 8618110
    Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: December 31, 2013
    Assignee: VM Discovery Inc.
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20130345222
    Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
    Type: Application
    Filed: May 17, 2013
    Publication date: December 26, 2013
    Inventors: Donald S. Karanewsky, Joseph R. Fotsing, Catherine Tachdjian, Melissa Arellano
  • Patent number: 8614239
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases (e.g., cancer and inflammation).
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: December 24, 2013
    Assignee: Novartis AG
    Inventors: Dinesh Chikkanna, Mark Gary Bock, Clive McCarthy, Henrik Moebitz, Chetan Pandit, Ramulu Poddutorri
  • Publication number: 20130338151
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: December 19, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Patent number: 8609705
    Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: December 17, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsuhiko Iwakoshi, Ippei Uemura
  • Publication number: 20130324717
    Abstract: This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methane compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.
    Type: Application
    Filed: August 5, 2013
    Publication date: December 5, 2013
    Inventors: Jason Clay Pearson, Max Allen Weaver, Jean Carroll Fleischer, Gregory Allan King
  • Publication number: 20130317223
    Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.
    Type: Application
    Filed: November 6, 2012
    Publication date: November 28, 2013
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, David M. Knapp, Eric P. Gillis