Chalcogen Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/103)
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Patent number: 11932603Abstract: Hydrophilic, high quantum yield, chemiluminescent acridinium compounds with increased light output, improved stability, fast light emission and decreased non specific binding are disclosed. The chemiluminescent acridinium esters possess hydrophilic, branched, electron-donating functional groups at the C2 and/or C7 positions of the acridinium nucleus.Type: GrantFiled: April 7, 2022Date of Patent: March 19, 2024Assignee: Siemens Healthcare Diagnostics Inc.Inventors: Anand Natrajan, David Sharpe, Qingping Jiang, David Wen
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Patent number: 8987296Abstract: 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: GrantFiled: October 29, 2013Date of Patent: March 24, 2015Assignees: Oregon Health & Science University, The United States of America DBA The Department of Veterans AffairsInventors: Michael K. Riscoe, Rolf W. Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
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Publication number: 20140235631Abstract: 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: ApplicationFiled: July 26, 2013Publication date: August 21, 2014Inventors: Antonius Martinus Gustave Bunt, Olaf van Tellingen
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Publication number: 20140225083Abstract: 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: ApplicationFiled: October 15, 2013Publication date: August 14, 2014Applicants: 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
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Publication number: 20140093453Abstract: 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: ApplicationFiled: September 19, 2013Publication date: April 3, 2014Applicants: 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 ALTERNATIVESInventors: Jean-Michel CHEZAL, Frederic DOLLE, Jean-Claude MADELMONT, Aurelie MAISONIAL, Elisabeth MIOT-NOIRAULT, Nicole MOINS, Janine PAPON, Bertrand KUHNAST, Bertrand TAVITIAN, Raphael BOISGARD
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Publication number: 20140058099Abstract: 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: ApplicationFiled: March 2, 2012Publication date: February 27, 2014Applicant: KYUSHU UNIVERSITY NATIONAL UNIVERSITY CORPORATIONInventors: Atsushi Wakamiya, Hidetaka Nishimura, Yasujiro Murata, Tatsuya Fukushima, Hironori Kaji
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Patent number: 8630703Abstract: 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: GrantFiled: March 8, 2012Date of Patent: January 14, 2014Assignee: Technion Research & Development Foundation LimitedInventors: Yehuda G. Assaraf, Yamit Adar Turgeman, Andrzej M. Skladanowski, Arjan W. Griffioen, Henk Verheul, Kristy Gotink, Hubert Van Den Bergh, Patrycja Nowak-Sliwinska
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Patent number: 8592447Abstract: 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: GrantFiled: November 13, 2007Date of Patent: November 26, 2013Assignees: Oregon Health & Science University, The United States of America, as represented by the Department of Veterans AffairsInventors: Michael K. Riscoe, Rolf Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
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Publication number: 20130225517Abstract: 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: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: University of Iowa Research FoundationInventor: University of Iowa Research Foundation
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Publication number: 20130190497Abstract: 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: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventor: The Trustees of Columbia University in the City of New York
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Publication number: 20130102627Abstract: 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: ApplicationFiled: April 8, 2011Publication date: April 25, 2013Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Jonathan Higgins, Gregory D. Cuny, Marcie Glicksman, Debasis Patnaik, Maxime Robin, Ross L. Stein, Jun Xian
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Publication number: 20130023521Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.Type: ApplicationFiled: January 17, 2011Publication date: January 24, 2013Applicant: HYBRIGENICS SAInventors: Roman Lopez, Frederic Colland
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Publication number: 20120231459Abstract: 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: ApplicationFiled: April 12, 2012Publication date: September 13, 2012Applicant: GEN-PROBE INCORPORATEDInventors: Kenneth A. BROWNE, Ian WEEKS
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Publication number: 20120136155Abstract: 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: ApplicationFiled: November 17, 2010Publication date: May 31, 2012Applicant: ADEKA CORPORATIONInventors: Yoshie Makabe, Yuta Okuyama
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Publication number: 20110177105Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.Type: ApplicationFiled: August 13, 2010Publication date: July 21, 2011Inventors: Roman Lopez, Frédéric Colland
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Publication number: 20110105554Abstract: 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, 7Type: ApplicationFiled: November 21, 2008Publication date: May 5, 2011Applicant: KINARIS BIOMEDICALS GMBHInventors: Dietmar Manstein, Roman Fedorov, Georgios Tsiavaliaris, Hans-Joachim Knölker, René Martin, Juliane Kirst, Herwig Gutzeit, Markus Böhl
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Publication number: 20110044899Abstract: 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: ApplicationFiled: January 28, 2009Publication date: February 24, 2011Applicants: 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 CYCLOPHARMAInventors: Jean-Michel Chezal, Frederic Dolle, Jean-Claude Madelmont, Aurelie Maisonial, Elisabeth Miot-Noirault, Nicole Moins, Janine Papon, Bertrand Kuhnast, Bertrand Tavitian, Raphael Boisgard
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Publication number: 20110039289Abstract: 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: ApplicationFiled: March 14, 2008Publication date: February 17, 2011Inventors: Pierre Graves, John A. Smith
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Patent number: 7879995Abstract: 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: GrantFiled: November 20, 2008Date of Patent: February 1, 2011Assignee: Fujfilm CorporationInventors: Jun Ogasawara, Tatsuya Igarashi, Satoshi Sano
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Patent number: 7829714Abstract: 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: GrantFiled: July 30, 2004Date of Patent: November 9, 2010Assignee: GE Healthcare LimitedInventors: John Gerard Whateley, Rahman Aziz Ismail, Peter Gordon Laughton
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Patent number: 7820843Abstract: 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: GrantFiled: December 11, 2008Date of Patent: October 26, 2010Assignee: Materia, Inc.Inventors: Richard L. Pederson, Jason K. Woertink, Christopher M. Haar, David E. Gindelberger, Yann Schrodi
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Publication number: 20100204186Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.Type: ApplicationFiled: April 22, 2010Publication date: August 12, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventor: Mark L. Nelson
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Publication number: 20100144780Abstract: 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: ApplicationFiled: November 17, 2006Publication date: June 10, 2010Inventor: Kirill Gennadievich Surkov
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Publication number: 20100137354Abstract: 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: ApplicationFiled: May 9, 2008Publication date: June 3, 2010Inventors: Wieslaw M. Cholody, Yi Zang, Karina E. Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel, Norman E. Ohler, Sheela K. Chellappan, Janak Padia
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Publication number: 20100069428Abstract: 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: ApplicationFiled: November 13, 2007Publication date: March 18, 2010Inventors: Michael K. Riscoe, Rolf Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
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Publication number: 20100061928Abstract: 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: ApplicationFiled: July 27, 2007Publication date: March 11, 2010Applicants: Institut National De La Sante et De La Recherche Medicale (INSERM), Universite D'Auvergne Clermont 1Inventors: Jean-Claude Madelmont, Jean-Michel Chezal, Nicole Moins, Jean-Claude Teulade, Olivier Chavignon
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Publication number: 20090240026Abstract: 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: ApplicationFiled: July 3, 2007Publication date: September 24, 2009Applicant: NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITYInventors: Masumi Taki, Masahiko Sisido
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Patent number: 7579468Abstract: 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: GrantFiled: September 14, 2006Date of Patent: August 25, 2009Assignee: PainCeptor Pharma CorporationInventors: Kazimierz Babinski, Rahul Vohra, Xilin Cui, Daniel Scott Auld, Nachhattarpal Gill
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Publication number: 20080234254Abstract: 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: ApplicationFiled: June 7, 2005Publication date: September 25, 2008Applicant: UNIVERSITY OF LEEDSInventors: Ronald Grigg, Andrew Cook
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Publication number: 20080146544Abstract: 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: ApplicationFiled: February 25, 2008Publication date: June 19, 2008Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
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Publication number: 20080139788Abstract: 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: ApplicationFiled: November 21, 2007Publication date: June 12, 2008Applicant: GE HEALTHCARE UK LIMITEDInventors: JOHN ANTHONY SMITH, RICHARD MARTIN WEST
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Publication number: 20080124751Abstract: 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: ApplicationFiled: September 11, 2007Publication date: May 29, 2008Applicant: NEW YORK UNIVERSITYInventors: Young-Tae Chang, Young-Hoon Ahn
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Patent number: 7351807Abstract: Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions.Type: GrantFiled: July 3, 2001Date of Patent: April 1, 2008Assignee: Mallinckrodt Inc.Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
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Patent number: 7312209Abstract: 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: GrantFiled: December 20, 2002Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
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Patent number: 7160896Abstract: 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 salType: GrantFiled: July 6, 2001Date of Patent: January 9, 2007Assignee: Cancer Research Technology LimitedInventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reskza
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Patent number: 7144843Abstract: 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: GrantFiled: January 31, 2002Date of Patent: December 5, 2006Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kazuhiko Oyama, Takeshi Teraoka, Kazumi Yamamoto
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Patent number: 7067668Abstract: 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: GrantFiled: November 19, 2003Date of Patent: June 27, 2006Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kazumi Yamamoto, Takeshi Teraoka, Michiaki Iwata, Keiichi Imamura, Hiroshi Kurihara, Norio Sasaki, Yoshihiro Usui, Nobumitsu Sawai
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Patent number: 7022855Abstract: 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: GrantFiled: October 9, 2003Date of Patent: April 4, 2006Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kazumi Yamamoto, Kazuhiko Oyama, Masayo Sakai, Ryo Horikoshi
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Patent number: 6900322Abstract: 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: GrantFiled: May 10, 1999Date of Patent: May 31, 2005Assignee: Solvay Pharmaceuticals GmbHInventors: Michael Reggelin, Timo Heinrich, Bernd Junker, Jochen Antel, Ulf Preuschoff
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Patent number: 6872828Abstract: 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: GrantFiled: December 20, 2001Date of Patent: March 29, 2005Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Renuka de Silva, Wenhua Xie
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Patent number: 6858733Abstract: 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: GrantFiled: July 25, 2002Date of Patent: February 22, 2005Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Renuka de Silva, Wenhua Xie
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Patent number: 6821983Abstract: This invention relates to 9-anilinoacridine compounds, and more particularly to their synthesis and their use in pharmaceutical compositions for treating diseases.Type: GrantFiled: July 30, 2003Date of Patent: November 23, 2004Assignee: Academia SinicaInventors: Tsann-Long Su, Jang-Yang Chang, Ting-Chao Chou
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Publication number: 20040229899Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: January 6, 2004Publication date: November 18, 2004Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20040191792Abstract: 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: ApplicationFiled: December 1, 2003Publication date: September 30, 2004Inventors: John Anthony Smith, Richard Martin West
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Publication number: 20040073025Abstract: 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: ApplicationFiled: August 5, 2003Publication date: April 15, 2004Inventors: 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
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Publication number: 20040053955Abstract: Compounds having the formula (I), 1Type: ApplicationFiled: December 20, 2002Publication date: March 18, 2004Inventors: Edwin J. Iwanowicz, Scott H. Watterson, Ping Chen, T. G. Murali Dhar, Henry H. Gu, Yufen Zhao
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Patent number: 6706722Abstract: 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: GrantFiled: July 20, 2001Date of Patent: March 16, 2004Assignee: Zentaris AGInventors: Peter Emig, Eckhard Günther, Bernd Nickel, Gerhard Bacher, Silke Baasner, Thomas Beckers, Beate Aue
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4-Quinolinol derivatives and agrohorticultural bactericides containing the same as active ingredient
Patent number: 6680282Abstract: 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: GrantFiled: March 21, 2000Date of Patent: January 20, 2004Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kazumi Yamamoto, Takeshi Teraoka, Michiaki Iwata, Keiichi Imamura, Hiroshi Kurihara, Norio Sasaki, Yoshihiro Usui, Nobumitsu Sawai -
Publication number: 20030207909Abstract: 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: ApplicationFiled: April 4, 2003Publication date: November 6, 2003Inventors: Stephen Neidle, Richard John Harrison, Llyod Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
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Patent number: 6630481Abstract: 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: GrantFiled: February 28, 2001Date of Patent: October 7, 2003Assignee: Council of Scientific and Industrial Research of IndiaInventors: Ramaiah Danaboyina, Varghese Eldho Nadukkudy, Joseph Joshy