Chalcogen Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/103)
  • Patent number: 8987296
    Abstract: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: March 24, 2015
    Assignees: Oregon Health & Science University, The United States of America DBA The Department of Veterans Affairs
    Inventors: Michael K. Riscoe, Rolf W. Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
  • Publication number: 20140235631
    Abstract: The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells).
    Type: Application
    Filed: July 26, 2013
    Publication date: August 21, 2014
    Inventors: Antonius Martinus Gustave Bunt, Olaf van Tellingen
  • Publication number: 20140225083
    Abstract: A compound for an organic optoelectronic device represented by Chemical Formula 1 wherein groups R1-R4, Ar1, Ar2, L1, L2, X, n1, and n2 are described in the specification.
    Type: Application
    Filed: October 15, 2013
    Publication date: August 14, 2014
    Applicants: Cheil Industries Inc., Samsung Electronics Co., Ltd.
    Inventors: Sang Mo KIM, Jhun Mo SON, Ho Suk KANG, Yong Sik JUNG, Hyeon Ho CHOI, Kyu Young HWANG
  • Publication number: 20140093453
    Abstract: The present invention relates to the compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4)alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or a group of formula (?): —Y—Z—W—R11??(?) wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a —N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.
    Type: Application
    Filed: September 19, 2013
    Publication date: April 3, 2014
    Applicants: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), LABORATOIRES CYCLOPHARMA, UNIVERSITE D'AUVERGNE CLERMONT 1, COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES
    Inventors: Jean-Michel CHEZAL, Frederic DOLLE, Jean-Claude MADELMONT, Aurelie MAISONIAL, Elisabeth MIOT-NOIRAULT, Nicole MOINS, Janine PAPON, Bertrand KUHNAST, Bertrand TAVITIAN, Raphael BOISGARD
  • Publication number: 20140058099
    Abstract: The compounds represented fey the following general formula is is thermally stable and has excellent characteristics as a charge transport material [Ar1 represents a single bond, a benzene ring, etc.; X1 represents a linking group that links via an oxygen atom, a sulfur atom, a carbon atom, a nitrogen atom, a phosphorus atom or a silicon atom; either one of L1 and L2, and L3 and L4 bond to each other to represent a linking group that links via an oxygen atom, a sulfur atom, a carbon atom, a nitrogen atom, a phosphorus atom or a silicon atom; the other of L1 and L2, and L3 and L4 represent a hydrogen atom or a substituent; Y1 represents a linking group that links via a nitrogen atom, a boron atom or a phosphorus atom; R1, R2, R5 to R7 and R10 to R12 represent a hydrogen atom or a substituent; and n1 indicates an integer of 2 or more.].
    Type: Application
    Filed: March 2, 2012
    Publication date: February 27, 2014
    Applicant: KYUSHU UNIVERSITY NATIONAL UNIVERSITY CORPORATION
    Inventors: Atsushi Wakamiya, Hidetaka Nishimura, Yasujiro Murata, Tatsuya Fukushima, Hironori Kaji
  • Patent number: 8630703
    Abstract: Hydrophobic weak base compounds such as hydrophobic weak base chemotherapeutic agents (which are not an anthracycline) for use in the treatment of medical conditions such as proliferative disease or disorder in a subject, in combination with illumination of a region in a body of the subject which is characterized by the presence of proliferating cells, are disclosed. The hydrophobic weak base compound and a wavelength of illumination are selected such that the hydrophobic weak base compound acts as a therapeutically effective photosensitizer when exposed to the illumination.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: January 14, 2014
    Assignee: Technion Research & Development Foundation Limited
    Inventors: Yehuda G. Assaraf, Yamit Adar Turgeman, Andrzej M. Skladanowski, Arjan W. Griffioen, Henk Verheul, Kristy Gotink, Hubert Van Den Bergh, Patrycja Nowak-Sliwinska
  • Patent number: 8592447
    Abstract: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.
    Type: Grant
    Filed: November 13, 2007
    Date of Patent: November 26, 2013
    Assignees: Oregon Health & Science University, The United States of America, as represented by the Department of Veterans Affairs
    Inventors: Michael K. Riscoe, Rolf Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
  • Publication number: 20130225517
    Abstract: The invention provides compounds of formula I: or salts thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I and therapeutic methods for treating cancer.
    Type: Application
    Filed: February 22, 2013
    Publication date: August 29, 2013
    Applicant: University of Iowa Research Foundation
    Inventor: University of Iowa Research Foundation
  • Publication number: 20130190497
    Abstract: The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond ? is absent and bond ? is present, or Y is H, X is CH, bond ? is present, and bond ? is absent; atom Z is a carbon and bonds ?, ? and ? are present, or is a nitrogen and bonds ?, ? and ? are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ?O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: The Trustees of Columbia University in the City of New York
    Inventor: The Trustees of Columbia University in the City of New York
  • Publication number: 20130102627
    Abstract: The present disclosure is directed to compounds of Formula I: which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.
    Type: Application
    Filed: April 8, 2011
    Publication date: April 25, 2013
    Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventors: Jonathan Higgins, Gregory D. Cuny, Marcie Glicksman, Debasis Patnaik, Maxime Robin, Ross L. Stein, Jun Xian
  • Publication number: 20130023521
    Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.
    Type: Application
    Filed: January 17, 2011
    Publication date: January 24, 2013
    Applicant: HYBRIGENICS SA
    Inventors: Roman Lopez, Frederic Colland
  • Publication number: 20120231459
    Abstract: A novel method is disclosed for simultaneous detection and quantification of two or more nucleic acid targets, without need for amplification. The method depends on spectral-temporal resolution of chemiluminescence emitted from independent hybridization-induced chemiluminescent signal (HICS) probes. The utility of this method has been demonstrated by use of resolvable N-linked acridinium and 2,7-dimethoxyacridinium ester labeled probes in a homogeneous assay for sensitive and simultaneous independent quantification of several bacterial and fungal target sequences. Compositions and kits for practicing the method of the present invention are also disclosed.
    Type: Application
    Filed: April 12, 2012
    Publication date: September 13, 2012
    Applicant: GEN-PROBE INCORPORATED
    Inventors: Kenneth A. BROWNE, Ian WEEKS
  • Publication number: 20120136155
    Abstract: Disclosed are a photo-acid generator having high developing properties, a cationic polymerization initiator having high curing properties, and a resist composition and a cationically polymerizable composition containing the photo-acid generator and the cationic polymerization initiator, respectively. Described are a noble aromatic sulfonium salt compound of general formula (I) and a photo-acid generator, a cationic polymerization initiator, a resist composition, and a cationically polymerizable composition containing the compound. In formula (I), R1 to R10 are each an optionally substituted C1-C18 alkyl, etc.; R11 to R17 are each an optionally substituted C1-C18 alkyl, etc.; R18 is an optionally substituted C1-C18 alkyl, etc.; and X1? is a monovalent anion.
    Type: Application
    Filed: November 17, 2010
    Publication date: May 31, 2012
    Applicant: ADEKA CORPORATION
    Inventors: Yoshie Makabe, Yuta Okuyama
  • Publication number: 20110177105
    Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.
    Type: Application
    Filed: August 13, 2010
    Publication date: July 21, 2011
    Inventors: Roman Lopez, Frédéric Colland
  • Publication number: 20110105554
    Abstract: The present invention provides a method of designing a modulator of a myosin, the method comprising molecular modeling of a compound such that the modeled compound interacts with at least three amino acid residues of said myosin, said residues being selected from (a) ranges K265-V268, V411-L441, N588-Q593, D614-T629, and V630-E646 of SEQ ID NO: 2, said myosin comprising or consisting of (i) the sequence of SEQ ID NO: 2; (ii) the sequence encoded by the sequence of SEQ ID NO: 1; (iii) a sequence being at least 40% identical to the sequence of SEQ ID NO: 2 or to the sequence encoded by the sequence of SEQ ID NO: 1; or (iv) a sequence encoded by a sequence being at least 40% identical to the sequence of SEQ ID NO: 1; wherein said sequence of (iii) or (iv) comprises said three amino acid residues, and wherein said residues comprise K265; or (b) ranges of any one of SEQ ID NOs: 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 7
    Type: Application
    Filed: November 21, 2008
    Publication date: May 5, 2011
    Applicant: KINARIS BIOMEDICALS GMBH
    Inventors: Dietmar Manstein, Roman Fedorov, Georgios Tsiavaliaris, Hans-Joachim Knölker, René Martin, Juliane Kirst, Herwig Gutzeit, Markus Böhl
  • Publication number: 20110044899
    Abstract: A compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4) alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6) alkenyl group or a group of formula (y): wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.
    Type: Application
    Filed: January 28, 2009
    Publication date: February 24, 2011
    Applicants: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, UNIVERSITE D'AUVERGNE CLERMONT 1, LABORATOIRES CYCLOPHARMA
    Inventors: Jean-Michel Chezal, Frederic Dolle, Jean-Claude Madelmont, Aurelie Maisonial, Elisabeth Miot-Noirault, Nicole Moins, Janine Papon, Bertrand Kuhnast, Bertrand Tavitian, Raphael Boisgard
  • Publication number: 20110039289
    Abstract: A method of making a fluorogenic peptide with an acridone fluorophor is provided, the method comprising the steps of: (a) providing an acridone derivative, said acridone derivative having first and second reactive groups (or precursors thereof), (b) providing a solid phase support provided with reactive species for reacting with the first reactive group of the acridone derivative (c) causing the solid phase support and acridone derivative to react so that the acridone derivative is attached to the solid phase support (d) providing the peptide or reagents for the formation of the peptide, and (e) subsequent to step (c), causing the reaction of the second acridone reactive group with the peptide or one or more of the reagents for the formation of the peptide.
    Type: Application
    Filed: March 14, 2008
    Publication date: February 17, 2011
    Inventors: Pierre Graves, John A. Smith
  • Patent number: 7879995
    Abstract: An organic electroluminescent device, which has, between a pair of electrodes, at least one organic layer including a light-emitting layer, in which the organic layer contains a specific tetraphenylene compound, and in which the light-emitting layer contains a phosphorescent material; and a specific tetraphenylene compound that can be used in the device.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: February 1, 2011
    Assignee: Fujfilm Corporation
    Inventors: Jun Ogasawara, Tatsuya Igarashi, Satoshi Sano
  • Patent number: 7829714
    Abstract: The present invention relates to compounds useful for measuring aromatase activity. The invention further provides methods for measuring aromatase activity and for screening test agents which modulate aromatase activity. A kit is also provided for use in such screening methods.
    Type: Grant
    Filed: July 30, 2004
    Date of Patent: November 9, 2010
    Assignee: GE Healthcare Limited
    Inventors: John Gerard Whateley, Rahman Aziz Ismail, Peter Gordon Laughton
  • Patent number: 7820843
    Abstract: Chelating ligand precursors for the preparation of olefin methathesis catalysts are disclosed. The resulting catalysts are air stable monomeric species capable of promoting various methathesis reactions efficiently, which can be recovered from the reaction mixture and reused. Internal olefin compounds, specifically beta-substituted styrenes, are used as ligand precursors. Compared to terminal olefin compounds such as unsubstituted styrenes, the beta-substituted styrenes are easier and less costly to prepare, and more stable since they are less prone to spontaneous polymerization. Methods of preparing chelating-carbene methathesis catalysts without the use of CuCl are disclosed. This eliminates the need for CuCl by replacing it with organic acids, mineral acids, mild oxidants or even water, resulting in high yields of Hoveyda-type methathesis catalysts.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: October 26, 2010
    Assignee: Materia, Inc.
    Inventors: Richard L. Pederson, Jason K. Woertink, Christopher M. Haar, David E. Gindelberger, Yann Schrodi
  • Publication number: 20100204186
    Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.
    Type: Application
    Filed: April 22, 2010
    Publication date: August 12, 2010
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventor: Mark L. Nelson
  • Publication number: 20100144780
    Abstract: The invention relates to salts of 1-alkylamino-1-deoxypolyols and 9-oxoacridine-10-acetic acid of the general formula (I): wherein A+ is (II) wherein R is selected from the group consisting of ethyl, propyl, butyl, medicinal preparations comprising as an active ingredient salts of formula (I) and/or a mixture of said salt of formula (I) or 9-oxoacridine-10-acetic acid of the formula: and one or more 1-alkylamino-1-deoxypolyols of the general formula (II): wherein: R is selected from the group consisting of ethyl, propyl, butyl.
    Type: Application
    Filed: November 17, 2006
    Publication date: June 10, 2010
    Inventor: Kirill Gennadievich Surkov
  • Publication number: 20100137354
    Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
    Type: Application
    Filed: May 9, 2008
    Publication date: June 3, 2010
    Inventors: Wieslaw M. Cholody, Yi Zang, Karina E. Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel, Norman E. Ohler, Sheela K. Chellappan, Janak Padia
  • Publication number: 20100069428
    Abstract: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.
    Type: Application
    Filed: November 13, 2007
    Publication date: March 18, 2010
    Inventors: Michael K. Riscoe, Rolf Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
  • Publication number: 20100061928
    Abstract: The present invention relates to the use of a compound of formula (I): in which R1 represents a radionuclide, Ar represents an aromatic nucleus, m is an integer varying from 2 to 4, R2 and R3 represent, independently of one another, a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or an aryl group chosen from a phenyl, benzyl, imidazolyl, pyridyl, pyrimidinyl, pyrazinyl, indolyl, indazolyl, furyl and thienyl group, and their addition salts with pharmaceutically acceptable acids, in the preparation of a radiopharmaceutical composition intended for the diagnosis and/or treatment of melanoma.
    Type: Application
    Filed: July 27, 2007
    Publication date: March 11, 2010
    Applicants: Institut National De La Sante et De La Recherche Medicale (INSERM), Universite D'Auvergne Clermont 1
    Inventors: Jean-Claude Madelmont, Jean-Michel Chezal, Nicole Moins, Jean-Claude Teulade, Olivier Chavignon
  • Publication number: 20090240026
    Abstract: An object of the present invention is to provide a novel fluorescent amino acid derivative which can be synthesized by simple steps, can be excited particularly by a blue laser ray region of visible light, and has an improved light stability. Another object is to provide a production method of the fluorescent amino acid derivative. These objects can be achieved by a fluorescent amino acid derivative which is an acridone derivative substituted with an amino acid to comprise an electrophilic substituent group between the amino acid and the acridone derivative.
    Type: Application
    Filed: July 3, 2007
    Publication date: September 24, 2009
    Applicant: NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY
    Inventors: Masumi Taki, Masahiko Sisido
  • Patent number: 7579468
    Abstract: Disclosed are compositions which modulate the interaction with nerve growth factor and precursors thereof with neurotrophic receptors. Also disclosed are methods of using the compositions of the invention, including methods of administration.
    Type: Grant
    Filed: September 14, 2006
    Date of Patent: August 25, 2009
    Assignee: PainCeptor Pharma Corporation
    Inventors: Kazimierz Babinski, Rahul Vohra, Xilin Cui, Daniel Scott Auld, Nachhattarpal Gill
  • Publication number: 20080234254
    Abstract: The present invention relates to a benzamide derivative comprising a head, spacer and cap group wherein the spacer includes a benzene ring substituted with an additional spacer and wherein the additional spacer is an unsaturated group.
    Type: Application
    Filed: June 7, 2005
    Publication date: September 25, 2008
    Applicant: UNIVERSITY OF LEEDS
    Inventors: Ronald Grigg, Andrew Cook
  • Publication number: 20080146544
    Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
    Type: Application
    Filed: February 25, 2008
    Publication date: June 19, 2008
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Publication number: 20080139788
    Abstract: Disclosed are new acridone dye derivatives having characteristic fluorescence lifetimes. Also disclosed are methods for labelling target biological materials employing the acridone dyes and use of the labelled materials in biological assays.
    Type: Application
    Filed: November 21, 2007
    Publication date: June 12, 2008
    Applicant: GE HEALTHCARE UK LIMITED
    Inventors: JOHN ANTHONY SMITH, RICHARD MARTIN WEST
  • Publication number: 20080124751
    Abstract: The present invention relates to a rosamine derivative compound, as described herein, having the following structure: Also disclosed are methods of making such compounds and for using them for detection and imaging.
    Type: Application
    Filed: September 11, 2007
    Publication date: May 29, 2008
    Applicant: NEW YORK UNIVERSITY
    Inventors: Young-Tae Chang, Young-Hoon Ahn
  • Patent number: 7351807
    Abstract: Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions.
    Type: Grant
    Filed: July 3, 2001
    Date of Patent: April 1, 2008
    Assignee: Mallinckrodt Inc.
    Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
  • Patent number: 7312209
    Abstract: Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ?O and ?S; W is —C(?O)—, —S(?O)—, or —S(O)2—; or W may be —CH2— if X is —C(?O)—; X is selected from —CH2—, —N(R4)—, and —O—, except that when W is —CH2—, X is —C(?O)—; Y is a bond or —C(R40)(R45)—; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and R1, R2, R24, and R25 are as defined in the specification.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: December 25, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
  • Patent number: 7160896
    Abstract: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ?O, L is —H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula —N(RN)Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable sal
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: January 9, 2007
    Assignee: Cancer Research Technology Limited
    Inventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reskza
  • Patent number: 7144843
    Abstract: An objective of the present invention is to provide a harmful organism control agent that possesses excellent control effect against harmful organisms and can be safely used. The present invention provides a compound of formula (1) or a salt thereof. The present invention also provides a harmful organism control agent comprising the compound of formula (1). wherein R1, n, R2, and R3 are as defined in the specification.
    Type: Grant
    Filed: January 31, 2002
    Date of Patent: December 5, 2006
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kazuhiko Oyama, Takeshi Teraoka, Kazumi Yamamoto
  • Patent number: 7067668
    Abstract: A new agricultural and horticultural fungicide having an excellent control effect is provided. 4-Quinolinol derivatives represented by the following formula: or agriculturally and horticulturally acceptable acid addition salts thereof.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: June 27, 2006
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kazumi Yamamoto, Takeshi Teraoka, Michiaki Iwata, Keiichi Imamura, Hiroshi Kurihara, Norio Sasaki, Yoshihiro Usui, Nobumitsu Sawai
  • Patent number: 7022855
    Abstract: An objective of the present invention is to provide an ectoparasite control agent for homothermic animals, which has high control effect and is safe. The compounds according to the present invention are compounds represented by formula (I) and salts thereof: wherein R1 represents optionally substituted alkyl; optionally substituted alkenyl; optionally substituted alkynyl; OR5 wherein R5 represents optionally substituted alkyl, optionally substituted alkenyl, or optionally substituted alkynyl; or SR5 wherein R5 is as defined above, R2 represents optionally substituted alkyl, any one of R3 and R4 represents hydrogen and the other represents fluorine, chlorine, bromine, or CF3, and X represents fluorine or chlorine.
    Type: Grant
    Filed: October 9, 2003
    Date of Patent: April 4, 2006
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kazumi Yamamoto, Kazuhiko Oyama, Masayo Sakai, Ryo Horikoshi
  • Patent number: 6900322
    Abstract: A method for stereochemically controlled production of azacyclic compounds of general formula (I) in which the substituents have the meanings given in the specification. The invention also relates to intermediate products of this method and to novel azacyclenes.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: May 31, 2005
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Michael Reggelin, Timo Heinrich, Bernd Junker, Jochen Antel, Ulf Preuschoff
  • Patent number: 6872828
    Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes or peroxide-producing enzymes and in assays employing enzyme-labeled specific binding pairs.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: March 29, 2005
    Assignee: Lumigen, Inc.
    Inventors: Hashem Akhavan-Tafti, Renuka de Silva, Wenhua Xie
  • Patent number: 6858733
    Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence rapidly by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes or peroxide-producing enzymes and in assays employing enzyme-labeled specific binding pairs.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: February 22, 2005
    Assignee: Lumigen, Inc.
    Inventors: Hashem Akhavan-Tafti, Renuka de Silva, Wenhua Xie
  • Patent number: 6821983
    Abstract: This invention relates to 9-anilinoacridine compounds, and more particularly to their synthesis and their use in pharmaceutical compositions for treating diseases.
    Type: Grant
    Filed: July 30, 2003
    Date of Patent: November 23, 2004
    Assignee: Academia Sinica
    Inventors: Tsann-Long Su, Jang-Yang Chang, Ting-Chao Chou
  • Publication number: 20040229899
    Abstract: The present invention relates to compounds of formula (I) 1
    Type: Application
    Filed: January 6, 2004
    Publication date: November 18, 2004
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Publication number: 20040191792
    Abstract: Disclosed are new acridone dye derivatives having characteristic fluorescence lifetimes. Also disclosed are methods for labelling target biological materials employing the acridone dyes and use of the labelled materials in biological assays.
    Type: Application
    Filed: December 1, 2003
    Publication date: September 30, 2004
    Inventors: John Anthony Smith, Richard Martin West
  • Publication number: 20040073025
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)—N(R25)CH(R30)—wherein the nitrogen atom is attached to R1, and R25 and R30 are independently selected from the group consisting of hydrogen, C3-6cycloalkyl, and C1-6alkyl, or 2) wherein the nitrogen atom is attached to R1, and m is 0, 1, or 2.
    Type: Application
    Filed: August 5, 2003
    Publication date: April 15, 2004
    Inventors: Harold G Selnick, Mary Beth Young, Philippe G Nantermet, James C Barrow, Peter D Williams, Terry A Lyle, Donnette D Staas, Kenneth J Stauffer, Philip E Sanderson
  • Publication number: 20040053955
    Abstract: Compounds having the formula (I), 1
    Type: Application
    Filed: December 20, 2002
    Publication date: March 18, 2004
    Inventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
  • Patent number: 6706722
    Abstract: The invention relates to novel acridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: March 16, 2004
    Assignee: Zentaris AG
    Inventors: Peter Emig, Eckhard Günther, Bernd Nickel, Gerhard Bacher, Silke Baasner, Thomas Beckers, Beate Aue
  • Patent number: 6680282
    Abstract: A new agricultural and horticultural fungicide having an excellent control effect is provided. 4-Quinolinol derivatives represented by the following formula: or agriculturally and horticulturally acceptable acid addition salts thereof.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: January 20, 2004
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kazumi Yamamoto, Takeshi Teraoka, Michiaki Iwata, Keiichi Imamura, Hiroshi Kurihara, Norio Sasaki, Yoshihiro Usui, Nobumitsu Sawai
  • Publication number: 20030207909
    Abstract: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent.
    Type: Application
    Filed: April 4, 2003
    Publication date: November 6, 2003
    Inventors: Stephen Neidle, Richard John Harrison, Llyod Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
  • Patent number: 6630481
    Abstract: The present invention provides a series of novel bifunctional molecules based on viologen linked acridine, bisacridine and bisacridinium salts of the general formula 1 (1a, 1b, 1c and 1d) and or pharmaceutically acceptable derivatives thereof, which can be used as phototherapeutic and catalytic photoactivated DNA cleaving agents. These molecules are very stable and exhibit high solubility in buffer at physiological conditions. They undergo strong binding with DNA through intercalation and groove binding interactions and show remarkably high affinity for poly(dA).poly(dT) sequences. Upon photoactivation, they cleave DNA catalytically and selectively at guanine (G) sites in duplex DNA exclusively through cosensitization mechanism with a preference for 5′-G over 3′-G. They induce unusally high specificity of cleavage at G site of the AG two base bulge sequences.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: October 7, 2003
    Assignee: Council of Scientific and Industrial Research of India
    Inventors: Ramaiah Danaboyina, Varghese Eldho Nadukkudy, Joseph Joshy
  • Publication number: 20030166925
    Abstract: The present invention provides a novel compound having a superior acetylcholinesterase inhibitory action.
    Type: Application
    Filed: November 25, 2002
    Publication date: September 4, 2003
    Inventors: Yoichi Iimura, Takashi Kosasa