Chalcogen Or Nitrogen Attached Directly To The Other Cyclo Of The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/178)
  • Patent number: 10913972
    Abstract: Described are luciferin analogues, methods for making the analogues, kits including the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays.
    Type: Grant
    Filed: July 19, 2019
    Date of Patent: February 9, 2021
    Assignee: Promega Corporation
    Inventors: Lance P. Encell, Mary P. Hall, Michael Killoran, Thomas A. Kirkland, Poncho Meisenheimer, Ce Shi
  • Patent number: 10745365
    Abstract: A method to detect the presence or amount of at least one molecule in a sample which employs a derivative of luciferin or a derivative of a fluorophore is provided. Compounds and compositions for carrying out the methods of the invention are also provided.
    Type: Grant
    Filed: August 22, 2018
    Date of Patent: August 18, 2020
    Assignee: Promega Corporation
    Inventors: James J. Cali, William Daily, Erika Hawkins, Dieter Klaubert, Jianquan Liu, Poncho Meisenheimer, Michael Scurria, John W. Shultz, James Unch, Michael P. Valley, Keith V. Wood, Wenhui Zhou
  • Patent number: 10400264
    Abstract: Described are luciferin analogs, methods for making the analogs, kits including the analogs, and methods of using the compounds for the detection of luminescence in luciferase-based assays.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: September 3, 2019
    Assignee: PROMEGA CORPORATION
    Inventors: Lance P. Encell, Mary P. Hall, Michael Killoran, Thomas A. Kirkland, Poncho Meisenheimer, Ce Shi
  • Patent number: 9814787
    Abstract: This disclosure relates to luciferin amides of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to detect fatty acid amide hydrolase activities in vitro, in live cells, or in vivo.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: November 14, 2017
    Assignee: University of Massachusetts
    Inventor: Stephen C. Miller
  • Patent number: 9434720
    Abstract: Topical formulations and method of using the same are provided. The topical formulation comprises a pyrazolylbenzothiazole derivative of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: September 6, 2016
    Assignee: DIRMIRA (CANADA), INC.
    Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
  • 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
  • Publication number: 20150141657
    Abstract: The present invention provides 2-phenyl benzothiazole linked imidazole compounds of formula A as anti cancer agent against fifty three human cancer cell lines.
    Type: Application
    Filed: February 15, 2012
    Publication date: May 21, 2015
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Kamal Ahmed, Ratna Reddy Challa, Prabhakar Singaraboina
  • Publication number: 20150099883
    Abstract: The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: in the formula, Cy represents an unsubstituted or X-substituted phenyl group or the like, X represents a halogen atom or the like, R1 represents an ethyl group or the like, R2 represents a hydrogen atom or the like, R3 and R4 represents a methyl group or the like, X1 represents a methylthio group or the like, m1 represents an integer of 1 to 4, X2 represents a methyl group or the like, m2 is an integer of 0 to 3.
    Type: Application
    Filed: April 8, 2013
    Publication date: April 9, 2015
    Inventors: Hironori Furukawa, Daisuke Hanai, Tetsuo Tamai, Jun Kanazawa, Katsunori Tanaka, Asaho Nagagata
  • Patent number: 8993561
    Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: March 31, 2015
    Assignee: Sanofi
    Inventor: Alain Pellet
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 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 the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8969580
    Abstract: A diagnostic imaging agent useful for positron emission tomography (PET) imaging as well as to improved hardware for producing such imaging agents is described. Flutemetamol (18F) Injection for the imaging of b amyloid plaques in the brain and methods and devices for preparing same are described including the automated synthesis and purification of [18F]flutemetamol by means of solid phase extraction (SPE).
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: March 3, 2015
    Assignee: GE Healthcare Limited
    Inventors: Eric Horn, Steven Fairway, Dimitrios Mantzilas, Nigel Powell
  • Patent number: 8962854
    Abstract: An object of the present invention to provide a firefly luciferin and firefly luciferin analog that are modified to maintain luminescent activity by luciferase in a firefly bioluminescent system. In particular, it is an object of the present invention to provide a new luminescent substrate for which the emission wavelength in a firefly bioluminescent system is shifted to a longer wavelength than that of a conventional luminescent substrate. The present invention provides a luciferin in which the benzothiazole ring moiety has been modified at the 7-position, a luciferin analog in which the benzene ring moiety has been modified at the 6-position, and a luciferin analog in which the 6-(dialkylamino)-2-naphthalenyl moiety has been modified at the 5-position.
    Type: Grant
    Filed: August 22, 2012
    Date of Patent: February 24, 2015
    Assignee: The University of Electro-Communications
    Inventors: Shigeru Nishiyama, Tsuyoshi Saito, Shojiro Maki, Haruki Niwa
  • 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: 20150038488
    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
  • Publication number: 20150038515
    Abstract: Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 5, 2015
    Inventors: Andrea Cuconati, Haitao Guo, Timothy M. Block, Ju-Tao Guo, Xiaodong Xu, Huagang Lu, Dawei Cai
  • 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: 8895313
    Abstract: Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: November 25, 2014
    Assignee: Wista Laboratories Ltd.
    Inventors: Steven John Kemp, Lynda Jane Storey, John Mervyn David Storey, Janet Rickard, Charles Robert Harrington, Claude Michel Wischik, Scott Clunas, Tobias Kerst Heinrich
  • Publication number: 20140341812
    Abstract: Novel derivatives of imidazopyridinylbenzeneamines and novel derivatives of benzothiazolylbenzeneamines are disclosed that offer improved behavior when used as imaging agents for positron emission tomography of beta-amyloids. Also disclosed is a palladium-catalyzed reaction scheme under microwave conditions for aryl thioethers in general that provides a high ratio of substitution relative to reduction and can be used for the imidazopyridinylbenzeneamine derivatives as well as other compounds of related structure.
    Type: Application
    Filed: March 24, 2014
    Publication date: November 20, 2014
    Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Serv
    Inventors: Lisheng Cai, Victor W. Pike, Robert B. Innis
  • Publication number: 20140343070
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug the
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • 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
  • Publication number: 20140303171
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • 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: 20140275064
    Abstract: The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.
    Type: Application
    Filed: August 17, 2012
    Publication date: September 18, 2014
    Applicant: DIAXONHIT
    Inventors: Bertrand Leblond, Anne-Sophie Casagrande, Laurent Desire, Alicia Foucourt, Thierry Besson
  • 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: 20140242627
    Abstract: Methods, kits and compositions containing a mixture of D-luciferin and L-luciferin for light generation with luciferase are disclosed that have improved stability when stored over time. The mixture of D-luciferin and L-luciferin can be used to detect the presence or amount of ATP or of luciferase in a sample.
    Type: Application
    Filed: February 21, 2014
    Publication date: August 28, 2014
    Applicant: PROMEGA CORPORATION
    Inventors: Michael P. Valley, James J. Cali, Brock Binkowski, Christopher Todd Eggers, Keith V. Woods
  • Publication number: 20140221665
    Abstract: An object of the present invention to provide a firefly luciferin and firefly luciferin analog that are modified to maintain luminescent activity by luciferase in a firefly bioluminescent system. In particular, it is an object of the present invention to provide a new luminescent substrate for which the emission wavelength in a firefly bioluminescent system is shifted to a longer wavelength than that of a conventional luminescent substrate. The present invention provides a luciferin in which the benzothiazole ring moiety has been modified at the 7-position, a luciferin analog in which the benzene ring moiety has been modified at the 6-position, and a luciferin analog in which the 6-(dialkylamino)-2-naphthalenyl moiety has been modified at the 5-position.
    Type: Application
    Filed: August 22, 2012
    Publication date: August 7, 2014
    Applicant: THE UNIVERSITY OF ELECTRO-COMMUNICATIONS
    Inventors: Shigeru Nishiyama, Tsuyoshi Saito, Shojiro Maki, Haruki Niwa
  • Publication number: 20140221319
    Abstract: The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.
    Type: Application
    Filed: April 13, 2012
    Publication date: August 7, 2014
    Applicants: Mayo Foundation for Medical Education and Research, President and Fellows of Harvard College
    Inventors: David A. Sinclair, Nathan L. Price, Eduardo N. Chini, Jon C. Clardy, Shugeng Cao
  • Publication number: 20140193340
    Abstract: This disclosure relates to luciferin amides of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to detect fatty acid amide hydrolase activities in vitro, in live cells, or in vivo.
    Type: Application
    Filed: March 15, 2013
    Publication date: July 10, 2014
    Applicant: University of Massachusetts
    Inventor: Stephen C. Miller
  • Patent number: 8772501
    Abstract: The present invention provides fluorescent dyes that are based on firefly luciferin structure. These dyes are optimally excited at shorter wavelengths and have Stokes shift of at least 50 nm. The fluorescent dyes of the invention are useful for preparation of dye-conjugates, which can be used in detection of an analyte in a sample.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: July 8, 2014
    Assignee: Beckman Coulter, Inc.
    Inventors: Hashem Akhavan-Tafti, Renuka De Silva, Guoping Wang, Robert A. Eickholt, Ravinder Gupta, Lakshmi S. Kaanumalle
  • Patent number: 8765969
    Abstract: The invention provides compounds, compositions, methods, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferins or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. The present method further provides a method for stabilizing and prolonging the luminescent signal in a luciferase-based assay using luciferase stabilizing agents such as reversible luciferase inhibitors.
    Type: Grant
    Filed: July 3, 2008
    Date of Patent: July 1, 2014
    Assignee: Promega Corporation
    Inventors: James J. Cali, Dieter Klaubert, William Daily, Samuel K. Ho, Susan Frackman, Erika Hawkins, Keith V. Wood
  • Publication number: 20140171438
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 19, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventors: Wenxi Pan, Haizhong Tang
  • Patent number: 8754233
    Abstract: Topical formulations and method of using the same are provided. The topical formulation comprises a pyrazolylbenzothiazole derivative of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.
    Type: Grant
    Filed: February 25, 2013
    Date of Patent: June 17, 2014
    Assignee: Dermira (Canada), Inc.
    Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
  • Patent number: 8754216
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: June 17, 2014
    Assignee: OPKO Health, Inc.
    Inventors: Sapna S. Shah, Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Neng-Yang Shih
  • Publication number: 20140154716
    Abstract: A method to detect the presence or amount of at least one molecule in a sample which employs a derivative of luciferin or a derivative of a fluorophore is provided. Compounds and compositions for carrying out the methods of the invention are also provided.
    Type: Application
    Filed: June 10, 2013
    Publication date: June 5, 2014
    Inventors: James J. Cali, William Daily, Erika Hawkins, Dieter Klaubert, Jianquan Liu, Poncho Meisenheimer, Michael Scurria, John W. Shultz, James Unch, Michael P. Valley, Keith V. Wood, Wenhui Zhou
  • Patent number: 8722887
    Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: May 13, 2014
    Assignee: Abbvie Bahamas, Ltd.
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20140121371
    Abstract: This disclosure relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated, iodinated, astatinated and radiofluorinated aromatic compounds.
    Type: Application
    Filed: October 25, 2013
    Publication date: May 1, 2014
    Applicant: Ground Fluor Pharmaceuticals, Inc.
    Inventor: Stephen G. DiMagno
  • Patent number: 8703938
    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. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: April 22, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
  • Publication number: 20140018325
    Abstract: Compounds of Formula I are disclosed wherein R1, R2, R3A, R3B, R4A, R4B, R5A, R5B, R6A, R6B, R8 and R9 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 27, 2011
    Publication date: January 16, 2014
    Inventors: Michael John Boyd, Carmela Molinaro, Amelia Roy, Vouy Linh Truong
  • Publication number: 20140018326
    Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 27, 2011
    Publication date: January 16, 2014
    Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
  • Patent number: 8629285
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: January 14, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
  • Publication number: 20140005385
    Abstract: According to the present invention, a tetrazoyloxime derivative and a salt thereof, which are excellent in a control effect against plant disease injury, and a plant disease controlling agent containing the same as an active ingredient are provided.
    Type: Application
    Filed: August 29, 2013
    Publication date: January 2, 2014
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Takeo Kobori, Hazumi Nomura, Ichirou Urihara, Hiroyasu Hosokawa, Atsunori Isshiki, Syuichi Ito, Jun Inagaki, Kazushige Fujii
  • 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
  • Publication number: 20130345196
    Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.
    Type: Application
    Filed: May 24, 2012
    Publication date: December 26, 2013
    Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
  • Patent number: 8586759
    Abstract: Methods and systems to generate 6-amino-6-deoxy-D-luciferin precursor, 2-cyano-6-aminobenzothiazole and related compounds and derivatives.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: November 19, 2013
    Assignee: Lawrence Livermore National Security, LLC
    Inventors: Amy L. Gryshuk, Julie Perkins, John V. LaTour
  • Publication number: 20130302248
    Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.
    Type: Application
    Filed: June 25, 2013
    Publication date: November 14, 2013
    Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharla, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
  • Publication number: 20130287699
    Abstract: The present disclosure features a condensation reaction and a luciferin-unmasking reaction that can be carried out under physiological conditions. In general, the condensation reaction involves reacting a bicyclic reactant with an aminothiol derivative, generating a luciferin or luciferin derivative. A luciferin can provide detectable luminescence. A luciferin derivative can be unmasked to provide detectable luminescence in a luciferin-unmasking reaction. The present disclosure provides bicyclic reactants and aminothiol derivatives suitable for use in the condensation reaction. The condensation and luciferin-unmasking reactions find use in a variety of applications, which are also provided.
    Type: Application
    Filed: January 15, 2013
    Publication date: October 31, 2013
    Inventors: Christopher J. Chang, Carolyn R. Bertozzi, Genevieve C. van de Bittner, Elena A. Dubikovskaya
  • Patent number: 8558003
    Abstract: The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4?-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: October 15, 2013
    Assignee: The General Hospital Corporation
    Inventors: David R. Elmaleh, Timothy M. Shoup, Alan J. Fischman
  • Patent number: 8558004
    Abstract: The present invention relates to reagents and methods for influenza virus detection. These reagents and methods disclosed in the present invention enable simple, rapid, specific and sensitive detection of influenza virus types A and B. These reagents are N-acetylneuraminic acid-firefly luciferin conjugates which can be cleaved by influenza virus neuraminidase.
    Type: Grant
    Filed: February 2, 2011
    Date of Patent: October 15, 2013
    Assignee: Cellex, Inc.
    Inventors: Xing-Xiang Li, Tianxin Wang
  • Publication number: 20130245025
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: January 3, 2013
    Publication date: September 19, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130245008
    Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
    Type: Application
    Filed: November 18, 2011
    Publication date: September 19, 2013
    Applicant: SANOFI
    Inventor: Alain Pellet