Bicyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/121)
  • Patent number: 8969376
    Abstract: The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O—, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: March 3, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Eiji Kawanishi, Mitsuya Hongu, Yoshihito Tanaka
  • Patent number: 8884029
    Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: November 11, 2014
    Assignee: Adeka Corporation
    Inventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Mitsuhiro Okada, Toru Yano, Yohei Aoyama, Yusuke Kubota
  • Publication number: 20140303379
    Abstract: Luminescent solar concentrator (LSC) comprising at least one disubstituted benzoselenadiazole compound having general formula (I): R1, R2, R3, R4 and R5, equal to or different from each other, represent a hydrogen atom; or they are selected from linear or branched C1-C20, preferably C1-C10, alkyl groups, cycloalkyl groups optionally substituted, aryl groups optionally substituted, linear or branched C1-C20, preferably C1-C10, alkoxyl groups, optionally substituted; or R1 and R2, can be possibly bound to each other so as to form, together with the carbon atoms to which they are bound, a cycle or a polycyclic system containing from 3 to 14 carbon atoms, preferably from 4 to 6 carbon atoms, saturated, unsaturated, or aromatic, possibly containing one or more heteroatoms such as, for example, oxygen, sulfur, nitrogen, silicon, phosphorous, selenium; or R3 and R4, can be possibly bound to each other so as to form, together with the carbon atoms to which they are bound, a cycle or a polycyclic system containing fro
    Type: Application
    Filed: July 5, 2012
    Publication date: October 9, 2014
    Inventors: Samuele Santarelli, Roberto Fusco, Antonio Proto, Luciano Caccianotti
  • Publication number: 20140296524
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: May 5, 2014
    Publication date: October 2, 2014
    Applicant: Nanoquantum Sciences, Inc.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Publication number: 20140243534
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: NANOQUANTUM SCIENCES, INC.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Patent number: 8703938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: April 22, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
  • Publication number: 20120232237
    Abstract: Compounds of Formula (I): (formula (I)) where: X1 and X2 are the same or different and each is independently Cl, Br, I, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group; and, Y is O, S, Se, NR1, R1C—CR2 or R1C?CR2, wherein R1 and R2 are the same or different and are each independently H or an organic group, are useful as monomers to produce oligomers or polymers that are useful in organic electronic devices.
    Type: Application
    Filed: November 3, 2010
    Publication date: September 13, 2012
    Inventors: Zhao Li, Jianfu Ding, Jianping Lu, Ye Tao
  • Publication number: 20120149743
    Abstract: Derivatives of selenophene and selenazole heterocycles are disclosed. The compounds are useful as inhibitors of D-amino acid oxidase (DAO) and in the treatment of neurodegenerative and psychiatric diseases and disorders.
    Type: Application
    Filed: June 2, 2009
    Publication date: June 14, 2012
    Applicant: Ironwood Pharmaceuticals, Inc
    Inventor: Regina Graul
  • Publication number: 20110275683
    Abstract: Derivatives of selenophene and selenazole heterocycles are disclosed. The compounds are useful as inhibitors of D-amino acid oxidase (DAO) and in the treatment of neurodegenerative and psychiatric diseases and disorders.
    Type: Application
    Filed: June 2, 2009
    Publication date: November 10, 2011
    Applicant: Ironwood Pharmaceuticals, Inc
    Inventor: Regina Graul
  • Patent number: 7947506
    Abstract: A hydroxyquinolone compound formulated as a fluorescent dye for protein detection, assay, quantitation, etc. The hydroxyquinolone compound may be modified, for example, by adding or removing sulfate groups, changing hydrocarbon chain lengths, etc. to result in more desirable properties such as enhanced binding to basic proteins, enhanced solubility, etc. The dye has enhanced sensitivity over commercially available protein stains, and may be used to stain proteins in solution, proteins separated on gels, proteins transferred to solid supports, etc. Methods of using the dyes are also disclosed.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: May 24, 2011
    Assignee: Pierce Biotechnology, Inc.
    Inventors: Brian David Wolf, Surbhi Desai, Peter T. Czerney, Frank G. Lehmann, Bernd G. Schweder, Matthias S. Wenzel
  • Patent number: 7820829
    Abstract: The present invention relates to new bisbenzisoselenazolonyl derivatives of the following general formula (I), wherein R is C4-5-alkylene, and their pharmaceutically acceptable salts. The inventive derivatives have antineoplastic, anti-inflammatory and antithrombotic activities.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: October 26, 2010
    Assignee: Peking University
    Inventor: Huihui Zeng
  • Patent number: 7799927
    Abstract: An indolestyryl compound. The indolestyryl compound has formula (I): wherein Z1 comprises benzene, naphthalene, or heterocyclic ring containing O, S, or N, R2 comprises H, halogen atoms, C1-5 alkyl, nitro, ester, carboxyl, sulfo, sulfonamide, sulfuric ester, amide, C1-3 alkoxy, amino, alkylamino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, R3, R4, R5, and R6 comprise H, alkyl, aralkyl, or heterocyclic ring containing O, S, or N, R7 and R8 comprise H or alkyl, R10 comprises H, alkyl, halogen atoms, nitro, hydroxyl, amino, ester, or substituted or non-substituted sulfonyl, W comprises carbon or nitrogen, Y comprises carbon, oxygen, sulfur, selenium, —NR, or —C(CH3)2, m is 1˜3, and X1 comprises an anionic group or an anionic organometallic complex, wherein R3 and R4 are joined to a nitrogen atom or R5 and R6 are joined together to form a ring, and R bonded to nitrogen is C1-5 alkyl.
    Type: Grant
    Filed: April 26, 2006
    Date of Patent: September 21, 2010
    Assignee: Industrial Technology Research Institute
    Inventors: Shin-Shin Wang, Chien-Wen Chen, Jong-Lieh Yang, Chii-Chang Lai, Hui-Ping Tsai, Wen-Ping Chu, Wen-Yih Liao, Chien-Liang Huang, Tzuan-Ren Jeng, Ching-Yu Hsieh, An-Tse Lee
  • Patent number: 7745632
    Abstract: A cyanine compound represented by the general formula (I), (VI) or (VII): wherein ring-A1 is an optionally substituted benzene or naphthalene ring; B is a group represented by the general formula (II) or (III); R1 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or an aryl group having 6 to 30 carbon atoms; R2 is a substituent represented by the general formula (IV); and Y1 is a hydrogen atom, an organic group having 1 to 30 carbon atoms, or a substituent represented by the general formula (IV): wherein ring-A2 is the same as the ring-A1 in the general formula (I); Y4 and Y5 each are independently the same as Y1 in the general formula (I); X2 is the same as X1 in the general formula (I); R10 is the same as R1 in the general formula (I); R11 is the same as R2 in the general formula (I); R23 and R24 are the same as R21 and R22 in the formulas (II) and (III); n is an integer of 0 to 6; the polymethine chain may have a subst
    Type: Grant
    Filed: April 4, 2006
    Date of Patent: June 29, 2010
    Assignee: Adeka Corporation
    Inventors: Yohei Aoyama, Koichi Shigeno
  • Publication number: 20100120873
    Abstract: An object of the present invention is to find a novel medicinal use of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof. 2-Phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof exhibits an excellent inhibitory effect on neovascularization in the choroid and also has a protective effect on retinal pigment epithelial cell damage, and therefore is useful as a prophylactic or therapeutic agent for age-related macular degeneration.
    Type: Application
    Filed: May 23, 2008
    Publication date: May 13, 2010
    Inventors: Shin-ichiro Hirai, Atsushi Yoshida
  • Patent number: 7709653
    Abstract: Asymmetric cyanine compounds represented by general formula I are provided, wherein X, n, R1, R2, R3, R4 and Y? are as defined in the specification. They have a maximum absorption peak at about 640 nm which may not change with ambient temperature. When the compounds bind a nucleic acid to form a dye/nucleic acid complex, the fluorescence intensity of the complexes will increased rapidly, so that they can be used as a staining agent for nucleic acids in flow cytometers. Their spectra are in the near-infrared region, which can effectively reduce the interference from background fluorescence and improve the accuracy of detection. Moreover, the compounds provided can also be used as a staining agent for blood reticulocytes.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: May 4, 2010
    Assignee: Shenzhen Mindray Bio-Medical Electronics Co. Ltd.
    Inventor: Shao Jianhui
  • Patent number: 7671211
    Abstract: A substrate for thioredoxin reductase which comprises a compound represented by the following general formula (I) or (I?): wherein R1 and R2 independently represent a hydrogen atom, a halogen atom, a trifluoromethyl group and the like; R3 represents an aryl group, an aromatic heterocyclic group and the like; R4 represents a hydrogen atom, a hydroxyl group, a —S-?-amino acid group and the like; R5 represents a hydrogen atom or a C1-C6 alkyl group; Y represents oxygen atom or sulfur atom; n represents an integer of from 0 to 5; and the selenium atom may be oxidized, whose example includes 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a ring-opened form thereof. The substrate is reduced by thioredoxin reductase in the presence of NADPH and enhances peroxidase activity of thioredoxin reductase.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: March 2, 2010
    Inventors: Arne Holmgren, Marjan H. Amiri, Hiroyuki Masayasu
  • Patent number: 7625758
    Abstract: Protein dyes whose molecular structure is that of a coumarin moiety coupled to a quaternary ammonium heterocycle through a vinyl or polyvinyl linkage demonstrate the ability to associate with proteins in a non-covalent, non-specific manner at low pH, where the associated form displays a significantly higher fluorescence emission than the unassociated form. This makes the dyes useful as selective labels for proteins at the low pH and eliminates the need for the removal of extraneous components from the medium in which the proteins reside prior to detection.
    Type: Grant
    Filed: January 26, 2005
    Date of Patent: December 1, 2009
    Inventor: Thomas R. Berkelman
  • Patent number: 7601744
    Abstract: The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Grant
    Filed: September 27, 2006
    Date of Patent: October 13, 2009
    Assignee: Wyeth
    Inventors: Casey Cameron McComas, Puwen Zhang, Eugene John Trybulski, An Thien Vu, Eugene Anthony Terefenko
  • Patent number: 7598385
    Abstract: The present disclosure provides the asymmetric cyanine fluorescent dyes of formula I in which X, n, R1, R2, R3, R4, R5 and Y? are as defined in the specification. The present disclosure also provides conjugates of the fluorescent dyes, methods for preparation thereof, compositions comprising the fluorescent dyes, and methods for staining biological samples using the fluorescent dyes and compositions thereof.
    Type: Grant
    Filed: December 31, 2007
    Date of Patent: October 6, 2009
    Assignee: Shenzhen Mindray Biomedical Electronics Co., Ltd.
    Inventors: Xiaojun Peng, Tong Wu, Jiangli Fan, Shiguo Sun, Bingshuai Wang, Bing Xu, Jianhui Shao
  • Publication number: 20090123567
    Abstract: The present invention relates to new bisbenzisoselenazolonyl derivatives of the following general formula (I), wherein R is C4-5-alkylene, and their pharmaceutically acceptable salts. The inventive derivatives have antineoplastic, anti-inflammatory and antithrombotic activities.
    Type: Application
    Filed: January 9, 2009
    Publication date: May 14, 2009
    Applicant: Peking University
    Inventor: Huihui Zeng
  • Publication number: 20090105313
    Abstract: An object of the present invention is to provide a new medicinal use of 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof. 2-Phenyl-1,2-benzisoselenazol-3(2H)-one or a salt thereof exhibits an excellent prevention and improvement effect in corneal disorder models, and is therefore useful as a preventive or therapeutic agent for a keratoconjunctival disorder such as dry eye, superficial punctate keratopathy, corneal epithelial defects, corneal erosion, corneal ulcer, conjunctival epithelial defects, keratoconjunctivitis sicca, superior limbic keratoconjunctivitis, filamentary keratoconjunctivitis, keratitis or conjunctivitis.
    Type: Application
    Filed: May 17, 2006
    Publication date: April 23, 2009
    Inventors: Atsushi Yoshida, Shinichirou Hirai, Masatsugu Nakamura
  • Patent number: 7495019
    Abstract: The present invention relates to new bisbenzisoselenazolonyl derivatives of the following general formulae (I), (II) or (III) and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: June 10, 2002
    Date of Patent: February 24, 2009
    Assignee: Peking University
    Inventor: Huihui Zeng
  • Patent number: 6995262
    Abstract: 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: Grant
    Filed: July 24, 2000
    Date of Patent: February 7, 2006
    Assignee: Bayer CropScience AG
    Inventors: Geert Deroover, Michael Missfeldt, Lydia Simon
  • Patent number: 6908726
    Abstract: Infrared absorbing compounds that absorb at 800 nm±50 nm and at 1050 nm±50 nm, the two different regions of the infrared spectrum typically used for imaging, are disclosed. Thermally imageable elements that comprise these infrared absorbing compounds can be imaged with radiation in either of these two regions of the infrared spectrum. The elements are especially useful as lithographic printing plate precursors.
    Type: Grant
    Filed: April 7, 2003
    Date of Patent: June 21, 2005
    Assignee: Kodak Polychrome Graphics LLC
    Inventors: Lee Korionoff, Ting Tao, Kevin B. Ray
  • Patent number: 6900218
    Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: May 31, 2005
    Assignee: Galileo Pharmaceuticals, Inc.
    Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani
  • Patent number: 6815459
    Abstract: The present invention provides novel seleno compounds containing nitrone moiety, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have similar or superior lipid peroxidation (LPO) inhibition activity to the reference compounds. While showing lower toxicity and better water solubility, they also effectively inhibit the cerebral neuronal cell death caused by ROS and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: November 9, 2004
    Assignee: Sam-Sung Electronics Co., Ltd.
    Inventors: Sung-Bo Ko, Eu-Gene Oh, Eon-Kyeom Kim, Won-Yeob Kim, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, Moo-Ho Won, Myung-Bok Wie
  • Publication number: 20040197697
    Abstract: Infrared absorbing compounds that absorb at 800 nm±50 nm and at 1050 nm±50 nm, the two different regions of the infrared spectrum typically used for imaging, are disclosed. Thermally imageable elements that comprise these infrared absorbing compounds can be imaged with radiation in either of these two regions of the infrared spectrum. The elements are especially useful as lithographic printing plate precursors.
    Type: Application
    Filed: April 7, 2003
    Publication date: October 7, 2004
    Inventors: Lee Korionoff, Ting Tao, Kevin B. Ray
  • Publication number: 20040047806
    Abstract: A new class of alpha-cyanomethine and alpha-cyanopolymethine dyes is provided having moieties which serve for the covalent attachment to biological substrates and resulting in the fluorescent labeling of the substrates. The labeled substrates are useful in analytical techniques for the detection and measurement of biological and clinical compounds of interest. Of particular interest is a class of methine molecules which are non-fluorescent in buffer solutions but intensely fluoresce when they enter a cell.
    Type: Application
    Filed: September 9, 2003
    Publication date: March 11, 2004
    Inventor: Spyros Theodoropulos
  • Publication number: 20040014981
    Abstract: A compound of the formula (I) is provided: (I), wherein Z is O, S, or NR35 wherein R35 is H or alkyl; R1-R5 are each independently H, alkyl, halo, carboxyl, amino, or SO331 Cat+, wherein Cat+ is a cation and at least one of R1-R5 is SO3−Cat+; R6 and R7 are each H, alkyl, or optionally, together with the (a) group to which they are bonded, form a ring; m and n are each independently integers from 0 to 5; X and Y are each independently O, S, Se or CR19R20, wherein R19 and R20 are each independently alkyl, or optionally form a ring together with the carbon atom to which they are bonded; R8 and R13 are each independently alkyl, (CH2)rR25 or (CH2)rR18; wherein at least one of R8 and R13 (CH2)rR18 and wherein r is an integer from 1 to 50, and R25 is a functional group that does not directly react with a carboxyl, hydroxyl, amino or a thiol group, and R18 is a functional group that can react with 1
    Type: Application
    Filed: January 28, 2003
    Publication date: January 22, 2004
    Inventors: Ananda G. Lugade, Narasimhachari Narayanan, Daniel R. Draney
  • Publication number: 20030220502
    Abstract: The present invention provides low molecular weight fluorescent labeling complexes with large wavelength shifts between absorption of one dye in the complex and emission from another dye in the complex. These complexes can be used, for example, for multiparameter fluorescence cell analysis using a single excitation wavelength. The low molecular weight of the complex permits materials labeled with the complex to penetrate cell structures for use as probes. The labeling complexes are synthesized by covalently attaching through linkers at least one cyanine fluorochrome to another low molecular weight fluorochrome to form energy donor-acceptor complexes. Resonance energy transfer from an excited donor to fluorescent acceptor provides wavelength shifts up to 300 nm. The fluorescent labeling complexes preferably contain reactive groups for the labeling of functional groups on target compounds, such as derivatized oxy and deoxy polynucleic acids, antibodies, enzymes, proteins and other materials.
    Type: Application
    Filed: November 20, 2002
    Publication date: November 27, 2003
    Inventors: Alan S. Waggoner, Swati R. Mujumdar, Ratnakar B. Mujumdar
  • Publication number: 20030220337
    Abstract: The present invention provides novel seleno compounds containing nitrone moiety, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have similar or superior lipid peroxidation (LPO) inhibition activity to the reference compounds. While showing lower toxicity and better water solubility, they also effectively inhibit the cerebral neuronal cell death caused by ROS and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Application
    Filed: June 6, 2003
    Publication date: November 27, 2003
    Inventors: Sung-Bo Ko, Eu-Gene Oh, Eon-Kyeom Kim, Won-Yeob Kim, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, Moo-Ho Won, Myung-Bok Wie
  • Publication number: 20030191161
    Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydrobenzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.
    Type: Application
    Filed: March 31, 2003
    Publication date: October 9, 2003
    Inventors: Stefan Petry, Karl-Heinz Baringhaus, Swen Hoelder, Guenter Mueller
  • Publication number: 20030165942
    Abstract: The invention relates to fluorescent dyes (fluorophores) based on polymethines for use in optical measurement and detection procedures, in particular those employing fluorescence, for example in medicine, in pharmacology and in the biological, materials and environmental sciences.
    Type: Application
    Filed: December 5, 2002
    Publication date: September 4, 2003
    Applicant: Dyomics GmbH
    Inventors: Peter Czerney, Matthias Wenzel, Bernd Schweder, Frank Lehmann
  • Publication number: 20030143159
    Abstract: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologues. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350-1300 nm, the exact range being dependent upon the particular dye. Use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.
    Type: Application
    Filed: January 9, 2001
    Publication date: July 31, 2003
    Applicant: Mallinckrodt Inc.
    Inventors: Samuel I. Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj
  • Publication number: 20030091861
    Abstract: Disclosed is a material for a light emitting device excellent in color purity, good in light emitting characteristics and excellent in stability, which consists of a compound represented by the following general formula (I):
    Type: Application
    Filed: August 21, 2002
    Publication date: May 15, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Hisashi Okada, Toshihiro Ise
  • Patent number: 6525040
    Abstract: The invention is directed to novel cyclic organoselenium compounds useful as antioxidants, pharmaceutical compositions containing them, and methods for their preparation.
    Type: Grant
    Filed: May 16, 2000
    Date of Patent: February 25, 2003
    Assignee: Oxis Isle of Man, Limited
    Inventors: Irene Erdelmeier, Catherine Tailhan-Lomont, Marc Moutet, Jean Chaudiere, Jean-Claude Yadan
  • Publication number: 20030022094
    Abstract: The invention provides a negative image-recording material for heat-mode exposure systems, which comprises (A) an IR absorbent including cyanine dye having a substituent that contains an atom having an atomic weight of at least 28 such as halogen atom, or a substituent that contains a non-covalent electron pair such as carbonyl group, (B) a radical generator and (C) a radically-polymerable compound, and which is imagewise exposed to IR rays for image formation thereon.
    Type: Application
    Filed: January 15, 2002
    Publication date: January 30, 2003
    Inventors: Ippei Nakamura, Tadahiro Sorori
  • Publication number: 20030013847
    Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
    Type: Application
    Filed: May 3, 2002
    Publication date: January 16, 2003
    Inventors: Bing Wang, Guy Miller, Wei Zhang, Satyanarayana Janagani, Jiangao Song
  • Patent number: 6461747
    Abstract: Disclosed is a material for a light emitting device excellent in color purity, good in light emitting characteristics and excellent in stability, which consists of a compound represented by the following general formula (I): L&Parenopenst;A)m  (I) wherein A represents a heterocyclic group in which two or more aromatic heterocycles are condensed; m represents an integer of 2 or more, and the heterocyclic groups represented by A may be the same or different; and L represents a connecting group.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: October 8, 2002
    Assignee: Fuji Photo Co., Ltd.
    Inventors: Hisashi Okada, Toshihiro Ise
  • Publication number: 20020127502
    Abstract: A heterocyclic compound corresponding to formula (I) 1
    Type: Application
    Filed: November 5, 2001
    Publication date: September 12, 2002
    Inventor: Michael Missfeldt
  • Patent number: 6407083
    Abstract: Compounds represented by the following formula I: in which: R1 to R5 can have various meanings of which alkyl, substituted or non-substituted aryl, and m is equal to 0 or 1, X is selected from (CR6R7)n in which n=0 or 1, and CO are disclosed. These compounds are useful as anti-tumor drugs, especially with pro-oxidizing activity.
    Type: Grant
    Filed: August 28, 2000
    Date of Patent: June 18, 2002
    Assignee: Oxis International, Inc.
    Inventors: Jinzhu Xu, Georges Appere, Jean Chaudiere, Jean-Claude Yadan
  • Patent number: 6335036
    Abstract: A granular pharmaceutical preparation prepared by granulating finely powdered Ebselen(2-phenyl-1,2-benzisoselenazol-3(2H)-one) using a hydrophilic polymer, and an aqueous suspension thereof. The Ebselen granular pharmaceutical preparation of the present invention is excellent in its performance as an oral preparation for use in stomach tube administration. That is, since it can be dispersed easily and uniformly when suspended in water or an aqueous solution before its use, and the suspension can be maintained in excellent dispersed state, preparation and tube administration of the drug solution can be made easily. Also, its dose is accurate because the administration can be effected with no drug or drug solution remained in the tube after the administration. In addition, the granular pharmaceutical preparation of the present invention is also suited for its large scale production, because it can be produced without employing special apparatuses and production steps.
    Type: Grant
    Filed: April 23, 1996
    Date of Patent: January 1, 2002
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Hiroaki Nakagami, Taketoshi Keshikawa
  • Patent number: 6057310
    Abstract: Compounds represented by the following formula I: ##STR1## in which: R.sup.1 to R.sup.5 can have various meanings of which alkyl, substituted or non-substituted aryl, and m is equal to 0 or 1, X is selected from (CR.sup.6 R.sup.7).sub.n in which n=0 or 1, and CO are disclosed. These compounds are useful as anti-tumor drugs, especially with pro-oxidizing activity.
    Type: Grant
    Filed: July 22, 1998
    Date of Patent: May 2, 2000
    Assignee: Oxis Isle of Man, Limited
    Inventors: Jinzhu Xu, Georges Appere, Jean Chaudiere, Jean-Claude Yadan
  • Patent number: 6001825
    Abstract: Compounds represented by the following formula I: ##STR1## in which: R.sup.1 to R.sup.5 can have various meanings of which alkyl, substituted or non-substituted aryl, and m is equal to 0 or 1, X is selected from (CR.sup.6 R.sup.7).sub.n in which n=0 or 1, and CO are disclosed. These compounds are useful as anti-tumor drugs, especially with pro-oxidizing activity.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: December 14, 1999
    Assignee: Oxis Isle of Man, Limited
    Inventors: Jinzhu Xu, Georges Appere, Jean Chaudiere, Jean-Claude Yadan
  • Patent number: 5968920
    Abstract: The invention concerns novel benzisoselen-azoline and -azine derivatives. These novel derivatives have the following general formula (II): ##STR1## where: R.sup.1 to R.sup.8 and R.sup.10 have various meanings, in particular H, alkyl, etc . . . ; ##STR2## Y.sup.- represents the anion of a pharmaceutically acceptable anion; n=0, 1; m=0, 1, 2; p=1, 2, 3; q=2, 3, 4; r=0, 1; and their pharmaceutically acceptable salts of acids or bases; there being no more than one substituent R.sup.9 in each molecule with general formula II. These novel derivatives can be used in medication.
    Type: Grant
    Filed: January 30, 1996
    Date of Patent: October 19, 1999
    Assignee: Oxis Isle of Man, Limited
    Inventors: Irene Erdelmeier, Jean Chaudiere, Marc Moutet, Jean-Claude Yadan
  • Patent number: 5935927
    Abstract: The present invention relates generally to methods and compositions for treating amyloidogenic diseases such as Alzheimer's disease and the development of type II diabetes, in which deposition of amyloid in organs such as the brain and pancreas interfere with neurological function and insulin release, respectively. The methods and compositions are directed toward increasing the activity of scavenger cells within the body at recognizing and removing amyloid deposits from affected tissues and organs. Scavenger cells may be targeted to amyloid deposits by means of spontaneously-occurring chemical modifications called advanced glycosylation endproducts (AGEs). Compositions are described which increase scavenger cell activity towards AGE-modified amyloid.
    Type: Grant
    Filed: August 10, 1996
    Date of Patent: August 10, 1999
    Assignee: The Picower Institute For Medical Research
    Inventors: Michael P. Vitek, Anthony Cerami, Richard J. Bucala, Peter C. Ulrich, Helen Vlassara, Xini Zhang
  • Patent number: 5718845
    Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: February 17, 1998
    Assignee: Enichem S.p.A.
    Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
  • Patent number: 5708181
    Abstract: An object of the present invention is to provide a novel compound which is suitably usable as a photochromic material.The compound of the present invention is a salt of a spiropyran compound and an acidic compound, the spiropyran compound being represented by the formula ##STR1## wherein R.sup.1 means a C.sub.1 to C.sub.20 alkyl group, an aralkyl group, a hydroxyethyl group, an acryloxyethyl group or a methacryloxyethyl group, R.sup.2 to R.sup.7 each mean a hydrogen atom, a C.sub.1 to C.sub.6 alkyl group or the like, R.sup.8 means a hydrogen atom, a vinyl group, a group --CH.sub.2 OR.sup.9 or a group --CH.sub.2 OCOC(R.sup.10).dbd.CH.sub.2 (wherein R.sup.9 means a hydrogen atom or a C.sub.1 to C.sub.4 alkyl group and R.sup.10 means a hydrogen atom or a methyl group), and X means an oxygen atom or a sulfur atom.
    Type: Grant
    Filed: November 8, 1995
    Date of Patent: January 13, 1998
    Assignee: Otsuka Kagaku Kabushiki Kaisha
    Inventors: Hiroshi Hama, Shinji Nakano
  • Patent number: 5667764
    Abstract: Compounds are provided having the capability of binding therapeutically active substances to lipid containing bio-compatible particles, such as cells or viruses. These compounds include a bio-affecting moiety, comprising a therapeutically active substance, which is linked via a linking moiety to at least one hydrocarbon substituent selected so that the compounds is sufficiently non-polar to impart lipid binding capability to the compound. Thus, compounds of the invention are useful for site-selective delivery of therapeutic agents, and retention thereof at the selected site.Methods are provided for using various compounds of the invention in treatment of diseases or other pathological conditions. For example, methods are provided for treatment of: (1) post-angioplasty restenosis; (2) rheumatoid arthritis; (3) tumor cell proliferation, particularly tumor cells associated with ovarian cancer; and (4) psoriasis.
    Type: Grant
    Filed: May 15, 1992
    Date of Patent: September 16, 1997
    Assignee: Zynaxis, Inc.
    Inventors: Gregory A. Kopia, Paul K. Horan, Brian D. Gray, David E. Troutner, Katharine A. Muirhead, Kamleshkumar A. Sheth, Chia-En Lin, Zhizhou Yu, Bruce D. Jensen, Sue Ellen Slezak
  • Patent number: RE38169
    Abstract: Attaching certain ligands to antisense probes will hyperstabilize sense-antisense duplexes. Such a hyperstabilized duplex is resistant to melting of the strands from one another, to unwinding of the strands, and to the action of nucleases. Applications include antiretroviral action, antireverse-transcriptase action, antiviral action, antiparasitical action, antibacterial action, antifungal action, anticancer action, anti-oncogene action, and other applications where it is desired to inhibit gene expression at the genomic or messenger RNA level. The preferred ligands are certain minor-groove-binding agents, exemplified by CC-1065 and synthetic CC-1065 analogs.
    Type: Grant
    Filed: July 26, 2000
    Date of Patent: July 1, 2003
    Assignee: Board of Supervisors of Louisana State University and Agricultural and Mechanical College
    Inventor: David H. Swenson