Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly Or Indirectly To The Acridine Ring System By Nonionic Bonding Patents (Class 546/104)
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Publication number: 20100112545Abstract: Novel trans-1,2-diphenylethylene derivatives are synthesized which can be used to form nanoparticles-monomer-nanomolecule-receptor nanosensors. These trans-1,2-diphenyl-ethylene derivatives are soluble in both water and organic solvents, highly fluorescent and can be synthesized in high yields. The trans-1,2-diphenylethylene derivatives are bonded to a nanoparticle, a nanomolecule bonded to the derivative and a receptor bonded to the nanomolecule to form a nanosensor that can be used to detect chemical and biological agents.Type: ApplicationFiled: July 13, 2007Publication date: May 6, 2010Inventors: Subra Muralidharan, Chun Wang
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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: 20090264463Abstract: Inhibitors of Protein Phosphatase-1 have been shown to slow replication of HIV-1. Inhibitors of PP 1 and their use for treatment or prevention of HIV-1 infections are disclosed.Type: ApplicationFiled: April 15, 2009Publication date: October 22, 2009Inventors: Sergei Nekhai, Dmytro Borysovich Kovalskyy
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Publication number: 20090186155Abstract: An ink for ink-jet recording includes a luminescence marker which emits light by oxidization. It may be determined whether the ink for ink-jet recording is used for recording the ink-jet recorded object with a simple method such as an evaluation of luminescence by oxidation, without requiring a special equipment.Type: ApplicationFiled: January 21, 2009Publication date: July 23, 2009Applicant: BROTHER KOGYO KABUSHIKI KAISHAInventor: Michiko Aoyama
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Patent number: 7511064Abstract: The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament and for the manufacture of a medicament for treatment of a disease state which can be alleviated by treatment with a 5-HT2B antagonist.Type: GrantFiled: April 19, 2006Date of Patent: March 31, 2009Assignee: Biofrontera Bioscience GmbHInventors: Hermann Lubbert, Christoph Ullmer, Emile Bellott, Mark Froimowitz, Douglas Gordon
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Publication number: 20090074673Abstract: The disclosure provides, in part, compositions and methods for producing cellular labels for tracking cells by MRI. The disclosure provides, in part, methods for labeling, detecting and quantifying cell numbers in vivo.Type: ApplicationFiled: July 10, 2008Publication date: March 19, 2009Applicant: Carnegie Mellon UniversityInventors: Jelena Janjic, Eric T. Ahrens
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Patent number: 7442790Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: June 28, 2007Date of Patent: October 28, 2008Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Publication number: 20080199973Abstract: In accordance with the present invention, it has been discovered that introduction of hydrophilic sulfoalkyl substituents and/or hydrophilic linkers derived from homocysteic acid, cysteic acid, glycine peptides, tetraethylene oxide, and the like, offset the hydrophobicity of the acridinium ring system to produce a more soluble label which can be attached to an antibody at higher loading before precipitation and aggregation problems are encountered. Additional compounds described herein contain linkers derived from short peptides and tetraethylene oxide which increase aqueous solubility due to hydrogen bonding with water molecules. The present invention also embraces reagents for multiple acridinium labeling for signal amplification composed of a peptide bearing several acridinium esters with sulfonate groups at regularly spaced intervals for increased solubility. The invention also embraces assays employing the above-described compounds.Type: ApplicationFiled: November 7, 2007Publication date: August 21, 2008Inventors: Ramon Evangelista, Martha Garrity
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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: 7300930Abstract: 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, 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 acceptablType: GrantFiled: June 22, 2005Date of Patent: November 27, 2007Assignee: Cancer Research Technology LimitedInventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
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Patent number: 7297555Abstract: In accordance with the present invention, it has been discovered that introduction of hydrophilic sulfoalkyl substituents and/or hydrophilic linkers derived from homocysteic acid, cysteic acid, glycine peptides, tetraethylene oxide, and the like, offset the hydrophobicity of the acridinium ring system to produce a more soluble label which can be attached to an antibody at higher loading before precipitation and aggregation problems are encountered. Additional compounds described herein contain linkers derived from short peptides and tetraethylene oxide which increase aqueous solubility due to hydrogen bonding with water molecules. The present invention also embraces reagents for multiple acridinium labeling for signal amplification composed of a peptide bearing several acridinium esters with sulfonate groups at regularly spaced intervals for increased solubility. The invention also embraces assays employing the above-described compounds.Type: GrantFiled: July 14, 2005Date of Patent: November 20, 2007Assignee: Quest Diagnostics Investments IncorporatedInventors: Ramon Evangelista, Martha Garrity
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Patent number: 7122671Abstract: A compound for use as a chemiluminescent label in immunoassay comprises an aryl acridinium ester linked to an N-succinimidyl moiety. The compound is conveniently linked to a monoclonal antibody or other protein and is used in a two-site immunoassay for the quantitation of an antigen of interest, by initiation of the luminescent reaction and subsequent measurement of the photonic emission of the immune complex formed during the immunological reaction.Type: GrantFiled: May 31, 1995Date of Patent: October 17, 2006Assignee: University College Cardiff Consultants LimitedInventors: Anthony Keith Campbell, James Stuart Woodhead, Ian Weeks
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Patent number: 7060711Abstract: The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament and for the manufacture of a medicament for treatment of a disease state which can be alleviated by treatment with a 5-HT2B antagonist.Type: GrantFiled: October 25, 2002Date of Patent: June 13, 2006Assignee: Biofrontera Bioscience GmbHInventors: Hermann Lubbert, Christoph Ullmer, Emile Bellott, Mark Froimowitz, Douglas Gordon
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Patent number: 7041674Abstract: A compound of formula 1 wherein X?, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in pharmaceutical compositions, and methods of treating patients using them.Type: GrantFiled: November 20, 2003Date of Patent: May 9, 2006Assignee: Boehringer Ingelhiem Pharma GmbH & Co. KGInventors: Steffen Breitfelder, Matthias Hoffmann, Matthias Grauert, Michael P. Pieper, Georg Speck
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Patent number: 6995262Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.Type: GrantFiled: July 24, 2000Date of Patent: February 7, 2006Assignee: Bayer CropScience AGInventors: Geert Deroover, Michael Missfeldt, Lydia Simon
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Patent number: 6994980Abstract: A novel chemiluminescent compound is provided. In one embodiment, the novel compound is employed in an assay to detect analytes. The assay to detect analytes includes the steps of binding the novel compound to the analyte and detecting the novel compound.Type: GrantFiled: March 22, 2004Date of Patent: February 7, 2006Assignee: Quest Diagnostics Investments Inc.Inventors: Phillip P. Miller, Martha Garrity
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Patent number: 6924373Abstract: The present invention relates to DNA labeling reagents comprising a furocoumarin derivative and a detectable group with or without bound via a binding enhancer, and acridinium-9-carboxamide derivatives for use as chemiluminescent labels. The present invention also relates to a process of preparing DNA labeling compound.Type: GrantFiled: May 2, 2003Date of Patent: August 2, 2005Assignee: AsiaGen CorporationInventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
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Patent number: 6924154Abstract: In accordance with the present invention, it has been discovered that introduction of hydrophilic sulfoalkyl substituents and/or hydrophilic linkers derived from homocysteic acid, cysteic acid, glycine peptides, tetraethylene oxide, and the like, offset the hydrophobicity of the acridinium ring system to produce a more soluble label which can be attached to an antibody at higher loading before precipitation and aggregation problems are encountered. Additional compounds described herein contain linkers derived from short peptides and tetraethylene oxide which increase aqueous solubility due to hydrogen bonding with water molecules. The present invention also embraces reagents for multiple acridinium labeling for signal amplification composed of a peptide bearing several acridinium esters with sulfonate groups at regularly spaced intervals for increased solubility. The invention also embraces assays employing the above-described compounds.Type: GrantFiled: August 20, 2002Date of Patent: August 2, 2005Assignee: Quest Diagnostics Investments IncorporatedInventors: Ramon Evangelista, Martha Garrity
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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: 6858162Abstract: Diodes and switches are combined in a single molecular species. Thus, the single molecular species is capable of performing more than one function. A single molecular species having both diode and switch functionalities is provided. The molecular species is represented by the formula: where A and B are non-identical conducting moieties, I is an insulating bridge between A and B, CL and CR are connectors to left and right electrodes, respectively, and “+” and “?” represent a rotatable dipolar moiety. Further, a diode-switch combination is provided, comprising the single molecular species. The teachings herein provide a set of principles to combine diodes and switches within one molecular species. Further, with the present teachings, only a single molecular species is needed for the fabrication of viable moletronic devices such as crossbar memory arrays. Consequently, device fabrication is easier and cheaper, and the device itself less faulty and more reliable.Type: GrantFiled: April 1, 2002Date of Patent: February 22, 2005Assignee: Hewlett-Packard Development Company, L.P.Inventor: Pavel Kornilovich
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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: 6858742Abstract: The present invention relates to DNA labeling reagents comprising a furocoumarin derivative and a detectable group with or without bound via a binding enhancer, and acridinium-9-carboxamide derivatives for use as chemiluminescent labels. The present invention also relates to a process of preparing DNA labeling compound.Type: GrantFiled: October 22, 2003Date of Patent: February 22, 2005Assignee: AsiaGEN CorporationInventors: George Chin-Sheng Chou, Yu-Cheng Wu, Po-Ya Hsu
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Patent number: 6800656Abstract: The present invention provides a compound of the formula and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. Wherein: X=O, (CH2)m, S, SO, SO2, NH, NR8; Y=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Z=NH, O, NR8, S, SO, SO2; The remaining substituents are described in the specification.Type: GrantFiled: July 5, 2002Date of Patent: October 5, 2004Assignee: Warner Lambert CompanyInventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
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Publication number: 20040122233Abstract: Bistable molecules are provided with at least one photosensitive functional group. As thus constituted, the bistable molecules are photopatternable, thereby allowing fabrication of micrometer-scale and nanometer-scale circuits in discrete areas without relying on a top conductor as a mask. The bistable molecules may comprise molecules that undergo redox reactions, such as rotaxanes and catenanes, or may comprise molecules that undergo an electric-field-induced band gap change that causes the molecules, or a portion thereof, to rotate, bend, twist, or otherwise change from a substantially fully conjugated state to a less conjugated state. The change in states in the latter case results in a change in electrical conductivity.Type: ApplicationFiled: October 30, 2003Publication date: June 24, 2004Inventors: Patricia A. Beck, Xiao-An Zhang, Zhang-Lin Zhou
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Patent number: 6740649Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.Type: GrantFiled: September 16, 2002Date of Patent: May 25, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
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Patent number: 6723851Abstract: A novel chemiluminescent compound is provided. In one embodiment, the novel compound is employed in an assay to detect analytes. The assay to detect analytes includes the steps of binding the novel compound to the analyte and detecting the novel compound.Type: GrantFiled: October 31, 2001Date of Patent: April 20, 2004Assignee: Quest Diagnostics Investment IncorporatedInventors: Phillip Miller, Martha Garrity
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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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Publication number: 20040038294Abstract: In accordance with the present invention, it has been discovered that introduction of hydrophilic sulfoalkyl substituents and/or hydrophilic linkers derived from homocysteic acid, cysteic acid, glycine peptides, tetraethylene oxide, and the like, offset the hydrophobicity of the acridinium ring system to produce a more soluble label which can be attached to an antibody at higher loading before precipitation and aggregation problems are encountered. Additional compounds described herein contain linkers derived from short peptides and tetraethylene oxide which increase aqueous solubility due to hydrogen bonding with water molecules. The present invention also embraces reagents for multiple acridinium labeling for signal amplification composed of a peptide bearing several acridinium esters with sulfonate groups at regularly spaced intervals for increased solubility. The invention also embraces assays employing the above-described compounds.Type: ApplicationFiled: August 20, 2002Publication date: February 26, 2004Applicant: Quest Diagnostic Investments IncorporatedInventors: Ramon Evangelista, Martha Garrity
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Patent number: 6664043Abstract: The present invention is generally directed to detectable chemiluminescent acridinium ester labels having hydrophilic modifiers; to compositions, complexes and/or conjugates which include such labels; and to processes for performing bioanalytical assays for target analytes which use such labels. Assays for folate, theophylline, and tobramycin (using such labels with hydrophilic modifiers such as nonionic polyethylene glycol and polyionic spermine disulfonate and polyionic spermine dicarboxylate) are described in detail.Type: GrantFiled: July 3, 2001Date of Patent: December 16, 2003Assignee: Bayer CorporationInventors: Anand Natrajan, David Sharpe, Qingping Jiang
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Publication number: 20030229073Abstract: The present invention provides a compound of the formula (I) and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. In said formula, X=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Y=O, (CH2)m, S, SO, SO2, NH, NR8; Z=NH, O, NR8, S, SO, SO2. The remaining substituents are described in the specification.Type: ApplicationFiled: July 5, 2002Publication date: December 11, 2003Inventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
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Publication number: 20030207344Abstract: Ethers and esters of cyanohydrins that contain optically detectable moieties are highly effective for detecting, monitoring, and measuring the activity of enzymes that cause the cleavage of certain types of substrates. The cyanohydrins function as proaldehydes and proketones, spontaneously converting to aldehydes and ketones, respectively, which provide a large increase in optical detectability relative to both the starting esters and ethers and the cyanohydrins.Type: ApplicationFiled: January 7, 2003Publication date: November 6, 2003Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Bruce D. Hammock, Guomin Shan, Rong Zhang
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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
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Publication number: 20030092060Abstract: A novel chemiluminescent compound is provided. In one embodiment, the novel compound is employed in an assay to detect analytes. The assay to detect analytes includes the steps of binding the novel compound to the analyte and detecting the novel compound.Type: ApplicationFiled: October 31, 2001Publication date: May 15, 2003Applicant: Quest Diagnostics Investments, Inc.Inventors: Miller Phillip P., Garrity Martha
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Publication number: 20030089920Abstract: In accordance with the present invention, nanometer-scale reversible electronic switches are provided that can be assembled to make cross-bar circuits that provide memory, logic, and communications functions. The electronic switches, or crossed-wire devices, comprise a pair of crossed wires that form a junction where one wire crosses another at an angle other than zero degrees and at least one connector species connecting the pair of crossed wires in the junction. The junction has a functional dimension in nanometers, wherein at least one connector species and the pair of crossed wires forms an electrochemical cell.Type: ApplicationFiled: November 7, 2002Publication date: May 15, 2003Inventors: Alexandre M. Bratkovski, Pavel Kornilovich, R. Stanley Williams, Xiao-An Zhang
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Publication number: 20030045538Abstract: 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: ApplicationFiled: February 28, 2001Publication date: March 6, 2003Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH of IndiaInventors: Ramaiah Danaboyina, Varghese Eldho Nadukkudy, Joseph Joshy
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Publication number: 20030032801Abstract: A compound having the structural formula 1Type: ApplicationFiled: May 7, 2001Publication date: February 13, 2003Inventors: Ai J. Lin, Jian Guan, Dennis E. Kyle, Wilbur K. Milhous
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Patent number: 6512119Abstract: In accordance with the present invention, nanometer-scale reversible electronic switches are provided that can be assembled to make cross-bar circuits that provide memory, logic, and communications functions. The electronic switches, or crossed-wire devices, comprise a pair of crossed wires that form a junction where one wire crosses another at an angle other than zero degrees and at least one connector species connecting the pair of crossed wires in the junction. The junction has a functional dimension in nanometers, wherein at least one connector species and the pair of crossed wires forms an electrochemical cell. The connector species comprises a bistable molecule having a general formula given by The bistable molecules evidence high switching speed. Such molecules are essentially stable against switching due to thermal fluctuations.Type: GrantFiled: January 12, 2001Date of Patent: January 28, 2003Assignee: Hewlett-Packard CompanyInventors: Alexandre M. Bratkovski, Pavel Kornilovich, R. Stanley Williams, Xiao-An Zhang
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Publication number: 20020173651Abstract: This invention relates to process for producing annulated pyridine bases by reacting cyclic ketones with aliphatic aldehyde in presence of ammonia in gaseous phase in the presence of a catalyst. This process provides an eco-friendly, more economical and highly selective heterogeneous method.Type: ApplicationFiled: March 27, 2001Publication date: November 21, 2002Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Shivanand Janardan Kulkarni, Kondapuram Vijaya Raghavan, Radha Rani Vippagunta, Srinivas Nagabandi
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Publication number: 20020119992Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: 1Type: ApplicationFiled: December 18, 2001Publication date: August 29, 2002Inventors: Harold G. Selnick, James C. Barrow, Philippe G. Nantermet, Peter D. Williams, Kenneth J. Stauffer, Philip E. Sanderson, Kenneth E. Rittle, Matthew M. Morrissette, Catherine M. Wiscount, Lekhanh O. Tran, Terry A. Lyle, Donnette D. Staas
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Publication number: 20020103217Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: January 8, 2002Publication date: August 1, 2002Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6417005Abstract: Fluoroionophores that are functionalised with reactive groups and correspond to the formula I—R1—F—R2—G, wherein I is a monovalen residue of an ionophore, wherein F is a divalent residue of a fluorophore, wherein G is a functional group and R1 and R2 are each independently of the other a direct bond or a bridging group. The fluoroionophores may be covalently bound to carrier materials and are used as active components in polymer membranes of optical sensors for the detection of ions. The sensors are distinguished by a long usable life and a high degree of sensitivity.Type: GrantFiled: December 7, 1998Date of Patent: July 9, 2002Assignee: Novartis AGInventors: Steven Mark Barnard, Adrian Waldner, David Reinhoudt, Joseph Berger
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Patent number: 6417402Abstract: The present invention relates to squaraine dye containing terminal aminoanthracene or acridine groups and to a process for preparation thereof.Type: GrantFiled: September 26, 2001Date of Patent: July 9, 2002Assignee: Council of Scientific and Industrial ResearchInventors: Suresh Das, George Thomas Kakkudiyil, Biju Vasudevan Pillai, Santosh Unni, Suresh Velate
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Patent number: 6414152Abstract: A compound for use as a chemiluminescent label in immunoassay comprises an aryl acridinium ester linked to an N-succinimidyl moiety. The compound is conveniently linked to a monoclonal antibody or other protein and is used in a two-site immunoassay for the quantitation of an antigen of interest, by initiation of the luminescent reaction and subsequent measurement of the photonic emission of the immune complex formed during the immunological reaction.Type: GrantFiled: October 24, 1994Date of Patent: July 2, 2002Assignee: University of Wales College of Medicine of Heath ParkInventors: Anthony Keith Campbell, James Stuart Woodhead, Ian Weeks
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Patent number: 6413984Abstract: The invention concerns compounds of formula (I) wherein: A represents either a hydrogen atom or a hydroxyl group; B represents a pyrrolidin-2-yl (D) or 2-piperidyl (E), B capable of being substituted by one or two R5 groups; R1 represents a hydrogen atom, a C1-C6 alkyl, a C2-C6 alkenyl, a C1-C2 perfluoroalkyl or a C1-C6 fluoroalkyl group; R2, R3 or R4, independently of one another, represent a hydrogen atom, a C1-C6 alkyl, group or a C2-C6 alkenyl group, or R1 and R2 can together form a C1-C6 alkylene chain, or a C3-C6 alkenylene chain; R5 represents a C1-C6 alkyl group, and R6 represents a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, C3-C6 cycloalkyl, C3-C6 cycloalkenyl or a benzyl.Type: GrantFiled: August 1, 2001Date of Patent: July 2, 2002Assignee: Sanofi-SynthelaboInventors: Christophe Philippo, Alain Braun, Philippe R. Bovy
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Patent number: 6410732Abstract: Synthetic processes and intermediates are disclosed for the preparation of N-arylacridancarboxylic acid derivatives. The derivatives are esters, thioesters, amides and sulfonimides. A key feature of the processes is the preparation of N-aryl substituted intermediates by formation of a bond between the nitrogen atom of the acridan ring and a carbon atom of another aromatic or heteroaromatic ring compound. The arylation reaction is catalyzed by a palladium catalyst. The N-arylacridancarboxylic acid derivatives are useful in methods for producing light and in assays for peroxidase enzymes and enzyme inhibitors and in assays employing enzyme-labeled specific binding pairs.Type: GrantFiled: January 25, 2001Date of Patent: June 25, 2002Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Robert A. Eickholt, Richard S. Handley
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Publication number: 20020058687Abstract: Therapeutically active compositions of matter are described which are useful for treating or preventing diseases and conditions comprising inflammatory diseases including joint inflammation, Crohn's disease, and inflammatory bowel disease; respiratory diseases such as chronic obstructive pulmonary disease (COPD) including asthma, chronic bronchitis, and pulmonary emphysema; infectious diseases including endotoxic shock and toxic shock syndrome; immune diseases including systemic lupus erythematosis and psoriasis; and other diseases including bone resorption diseases and reperfusion injury; wherein said composition of matter comprises a compound which is an inhibitor of phosphodiesterase isozyme 4 (PDE4) and wherein an indazole is one essential component of said compound's overall chemical structure, and wherein said indazole constitutes a bioisosteric replacement of a catechol component or functional derivative thereof in a known compound having the same said therapeutic activity and the same remaining said cType: ApplicationFiled: September 20, 1999Publication date: May 16, 2002Inventor: ANTHONY MARFAT
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Publication number: 20020037254Abstract: The invention relates to conjugates, comprising a fluorescent compound and a carrier, wherein the compound and the carrier are connected via an acidic ester or an acidic amide bond and the compound has an excitation wavelength of 630 nm or more and/or 450 nm or less. The invention also relates to the production of said conjugates and to the use thereof.Type: ApplicationFiled: August 4, 2000Publication date: March 28, 2002Inventors: HANNSJORG SINN, HANS-HERMANN SCHRENK, ANDREAS WUNDER, GERD STEHLE
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Patent number: 6355803Abstract: This application relates to long-wavelength acridinium compounds having electron-donating groups, which may either be: (a) Part of an extended conjugation system attached by appropriate functional groups to the acridinium nucleus, with coplanarity of the attached functional group and the acridone moiety during light emission (geometry requirement), said functional group consisting of at least one aromatic ring and one electron-donating atom or group with an extra pair of electrons which can readily delocalize into the extended &pgr; system to which the heteroatom is directly attached or built into, and establish stable extended resonance with the electron-withdrawing carbonyl moiety of the light emitting acridone.Type: GrantFiled: August 10, 1999Date of Patent: March 12, 2002Assignee: Bayer CorporationInventors: Anand Natrajan, Qingping Jiang, David Sharpe, Say-Jong Law
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Publication number: 20010031869Abstract: Synthetic processes and intermediates are disclosed for the preparation of N-arylacridancarboxylic acid derivatives. The derivatives are esters, thioesters, amides and sulfonimides. A key feature of the processes is the preparation of N-aryl substituted intermendiates by formation of a bond between the nitrogen atom of the acridan ring and a carbon atom of another aromatic or heteroaromatic ring compound. The arylation reaction is catalyzed by a palladium catalyst. The N-arylacridancarboxylic acid derivatives are useful in methods for producing light and in assays for peroxidase enzymes and enzyme inhibitors and in assays employing enzyme-labeled specific binding pairs.Type: ApplicationFiled: January 25, 2001Publication date: October 18, 2001Inventors: Hashem Akhavan-Tafti, Robert A. Eickholt, Richard S. Handley
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Patent number: RE39047Abstract: A light emitting method of an acridinium ester, comprising reacting said acridinium ester and a superoxide anion, and a method of detecting a substance to be examined, comprising detecting a light emitted by reacting a superoxide anion with an acridinium ester used as a label am described. It is possible to carry out the reaction not under strongly alkaline conditions but around the neutral point and to generate strong luminescence which is stable over a long period of time.Type: GrantFiled: March 8, 2001Date of Patent: March 28, 2006Assignee: Mitsubishi Kagaku Iatron, Inc.Inventors: Masuo Aizawa, Michiko Ikariyama, Eiry Kobatake, Minoru Ogasawara, Mitsunao Tanaka, Yoshihito Ikariyama