Unsaturated Ring Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/109)
  • Patent number: 9035057
    Abstract: Tracers for imaging distribution of reactive oxygen species (ROS) are disclosed. The tracers include radiolabeled dihydroethidine (DHE) analogues. Further disclosed are uses of the compounds, including methods of imaging tissue distribution of ROS in vivo by positron emission tomography (PET). Methods of synthesizing the compounds are also disclosed.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: May 19, 2015
    Assignee: Washington University
    Inventors: Robert H. Mach, Mark Mintun, Wenhua Chu, Laura Dugan
  • Publication number: 20140191208
    Abstract: A carbazole-based compound is represented by Formula 1 and may be used in the organic layer of an organic light-emitting diode. An organic light-emitting diode includes a first electrode, a second electrode, and an organic layer between the first and second electrodes. The organic layer includes an emission layer, and the carbazole-based compound of Formula 1 may be included in the emission.
    Type: Application
    Filed: August 20, 2013
    Publication date: July 10, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Seul-Ong Kim, Dong-Woo Shin
  • Publication number: 20140151670
    Abstract: An exemplary embodiment of the present application provides a new compound and an organic electronic device using the same. The organic electronic device according to an exemplary embodiment of the present application shows excellent characteristics in terms of efficiency, driving voltage, and service life.
    Type: Application
    Filed: July 19, 2013
    Publication date: June 5, 2014
    Applicant: LG CHEM, LTD.
    Inventors: Dong Hoon Lee, Minyoung Kang, Jungi Jang, Boonjae Jang, Minseung Chun, Kidong Koo
  • Publication number: 20140073058
    Abstract: Methods of using dyes and associated technology are provided. A dye, such as a monomeric dye or a dimeric dye, may be used in a nucleic acid gel staining application and/or a nucleic acid detection application. Such a dye and a salt that comprises an anion that is associated with a strong acid and a cation that is associated with a strong base may be used in such an application. A dimeric dye, such as a dimeric dye capable of forming a hairpin-like structure, may be used to stain and/or detect nucleic acids via a release-on-demand mechanism. A dimeric dye having low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, may be used to stain and/or detect nucleic acids.
    Type: Application
    Filed: August 8, 2013
    Publication date: March 13, 2014
    Applicant: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung
  • Publication number: 20140039001
    Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.
    Type: Application
    Filed: October 11, 2013
    Publication date: February 6, 2014
    Applicant: TAKEDA GMBH
    Inventors: Ulrich KAUTZ, Matthias WEBEL, Christian SCHEUFLER, Rolf-Peter HUMMEL
  • Publication number: 20130096152
    Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.
    Type: Application
    Filed: December 7, 2012
    Publication date: April 18, 2013
    Applicant: NYCOMED GMBH
    Inventor: NYCOMED GMBH
  • Publication number: 20130079522
    Abstract: Tracers for imaging distribution of reactive oxygen species (ROS) are disclosed. The tracers include radiolabeled dihydroethidine (DHE) analogues. Further disclosed are uses of the compounds, including methods of imaging tissue distribution of ROS in vivo by positron emission tomography (PET). Methods of synthesizing the compounds are also disclosed.
    Type: Application
    Filed: December 16, 2010
    Publication date: March 28, 2013
    Applicant: WASHINGTON UNIVERSITY
    Inventors: Robert H. Mach, Mark Mintun, Wenhua Chu, Laura Dugan
  • Publication number: 20130012597
    Abstract: The present invention provides a UCST-type thermoresponsive polymer compound which responds to a temperature under physiological conditions and has biofunctionality, and various uses thereof as a thermoresponsive material. Specifically, the invention provides a thermoresponsive material containing, as an active ingredient, a polymer compound represented by Formula (I) below or an addition salt thereof, the thermoresponsive material having an upper critical solution temperature in the range of 5 to 50° C. in an aqueous solution with a salt concentration of at least 1 mM and a pH in the range of 3 to 10.5: wherein m represents an integer of 10 or more; n represents a number satisfying 0.4?n?1; R1 represents hydrogen or succinyl; and R2 represents carbamoyl.
    Type: Application
    Filed: March 22, 2011
    Publication date: January 10, 2013
    Applicant: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION
    Inventors: Naoko Shimada, Atsushi Maruyama
  • Publication number: 20120316342
    Abstract: This invention provides a therapeutic agent for hepatitis C comprising, as an active ingredient, a compound having anti-HCV activity useful in treatment of hepatitis C. The therapeutic agent for hepatitis C comprises, as an active ingredient, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 31, 2011
    Publication date: December 13, 2012
    Inventors: Masanori Baba, Yuichi Hashimoto, Hiroshi Aoyama, Kazuyuki Sugita, Masahiko Nakamura, Atsushi Aoyama, Yasuo Urata
  • Patent number: 8329906
    Abstract: The compounds of a certain formula (1), in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as given in the description, are novel effective PDE4 inhibitors.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: December 11, 2012
    Assignee: Nycomed GmbH
    Inventor: Ulrich Kautz
  • Publication number: 20110269705
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 3, 2011
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
  • Publication number: 20110257221
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.
    Type: Application
    Filed: May 19, 2011
    Publication date: October 20, 2011
    Applicant: NYCOMED GMBH
    Inventor: Ulrich KAUTZ
  • Publication number: 20110257169
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.
    Type: Application
    Filed: May 19, 2011
    Publication date: October 20, 2011
    Applicant: NYCOMED GmbH
    Inventor: Ulrich KAUTZ
  • Publication number: 20110190480
    Abstract: The present invention relates to dyes of the general formula CAT+ Y? (I), where Y? is an anion selected from the group of the cyanoborates, fluoroalkylphosphates, fluoroalkylborates or imidates and CAT+ is a cation selected from the group of the azine, xanthene, polymethine, styryl, azo, tetrazolium, pyrylium, benzopyrylium, thiopyrylium, benzothiopyrylium, thiazine, oxazine, triarylmethane, diarylmethane, methine, acridine, quinoline, isoquinoline or quaternary azafluorenone dyes, for colouring plastics and plastic fibres, for the preparation of flexographic printing inks, as ball-point pen pastes, as stamp ink, for colouring leather and paper, for use in data acquisition systems, reprography, in ink microfilters, in photogalvanics, laser technology and the photo industry.
    Type: Application
    Filed: April 11, 2011
    Publication date: August 4, 2011
    Inventors: Nikolai (Mykola) IGNATYEV, Urs Welz-Biermann, Helge Willner, Maik Finze, Eduard Bernhardt, Andriy Kucheryna
  • Publication number: 20110156017
    Abstract: The present invention provides a novel anthracene derivatives and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent properties in terms of efficiency, a driving voltage, and a life span.
    Type: Application
    Filed: September 24, 2009
    Publication date: June 30, 2011
    Inventors: Dong-Hoon Lee, Hyun Nam, Jun-Gi Jang, Seong-So Kim, Tae-Yoon T Park
  • Publication number: 20110012092
    Abstract: A novel nitrogen-containing heterocyclic derivative having a specific structure. An organic electroluminescence device comprises an organic thin-film layer which is disposed between a cathode and an anode and comprises one or more layers having a light emitting layer. At least one layer of the organic thin-film layer comprises the nitrogen-containing heterocyclic derivative. The organic electroluminescence device exhibits a high luminance and a high luminous efficiency even at a low driving voltage.
    Type: Application
    Filed: December 24, 2008
    Publication date: January 20, 2011
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Hiroshi Yamamoto, Takashi Arakane
  • Publication number: 20100216772
    Abstract: The present invention relates to compounds of the general formula (IV) and (II) and salts and physiologically functional derivatives thereof, wherein X is C—R8 or N; and Z is independently one of the following groups:
    Type: Application
    Filed: October 5, 2004
    Publication date: August 26, 2010
    Inventors: Stefano Pegoraro, Martin Lang, Juliane Feurle, Jürgen Krauss
  • Patent number: 7585872
    Abstract: The compounds of a certain formula (1), in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as given in the description, are novel effective PDE4 inhibitors.
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: September 8, 2009
    Assignee: NYCOMED GmbH
    Inventor: Ulrich Kautz
  • Publication number: 20080312237
    Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Application
    Filed: July 18, 2008
    Publication date: December 18, 2008
    Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
  • Publication number: 20080161339
    Abstract: Compounds of the formula I in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.
    Type: Application
    Filed: March 9, 2005
    Publication date: July 3, 2008
    Applicant: ALTANA PHARMA AG
    Inventor: Ulrich Kautz
  • Publication number: 20080119505
    Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R31, R4, R5, R51 and Har have the meanings indicated in the description, are novel effective PDE4 inhibitors.
    Type: Application
    Filed: January 31, 2006
    Publication date: May 22, 2008
    Applicant: ALTANA Pharma AG
    Inventors: Ulrich Kautz, Beate Schmidt, Dieter Flockerzi, Maria Vittoria Chiesa, Armin Hatzelmann, Christof Zitt, Johannes Barsig, Andrea Wohlsen, Degenhard Marx, Hans-Peter Kley
  • Patent number: 7329676
    Abstract: The compounds of formula I in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as indicated in the description, are novel effective PDE4 inhibitors.
    Type: Grant
    Filed: August 28, 2003
    Date of Patent: February 12, 2008
    Assignee: Nycomed GmbH
    Inventors: Ulrich Kautz, Beate Schmidt
  • Patent number: 7074782
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: July 11, 2006
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M. C. Golec
  • Patent number: 7067667
    Abstract: 3,4-dihydroquinoline derivatives, a process for their production and their use in pharmaceutical agents.
    Type: Grant
    Filed: October 29, 2003
    Date of Patent: June 27, 2006
    Assignee: Schering Aktiengesellschaft
    Inventors: Stefan Jaroch, Hartmut Rehwinkel, Peter Holscher, Detlev Sülzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Mcdougall McDonald
  • Patent number: 6894061
    Abstract: This invention provides a compound of formulae (I) or (II) having the structure or a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.
    Type: Grant
    Filed: November 20, 2003
    Date of Patent: May 17, 2005
    Assignee: Wyeth
    Inventors: Albert John Molinari, Mark Antony Ashwell, Brian Hugh Ridgway, Amedeo Arturo Failli, William Jay Moore
  • Patent number: 6884802
    Abstract: Compounds of formula 1, in which Het is an unsubstituted or R6- and/or R7-substituted pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrimidinyl, pyrazinyl or pyradazinyl radical, or an unsubstituted or R6- and/or R7-substituted fused bi- or tricyclic ring system comprising at least one aromatic ring and up to 4 heteroatoms-selected from the group consisting of O (oxygen), S (sulfur), N (nitrogen)- which is bonded to the phenanthridinyl radical via one of the rings comprising one or more heteroatoms, are active PDE4 inhibitors.
    Type: Grant
    Filed: July 7, 2001
    Date of Patent: April 26, 2005
    Assignee: ALTANA Pharma AG
    Inventor: Beate Schmidt
  • Publication number: 20040038979
    Abstract: Compounds of the formula I, in which Het is an unsubstituted or R6-and/or R7-sustituted pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrimidinyl, pyrazinyl or pyridazinyl radical, or an unsubstituted or R6-and/or R7-substituted fused bi-or tricyclic ring system comprising at least one aromatic ring and up to 4 heteroatoms—selected from the group consisting of O(oxygen), S(sulphur) or N(nitrogen)—which is bonded to the phenanthridinyl radical via one of the rings comprising one or more rheteroatoms, areactive PDE4 inhibitors.
    Type: Application
    Filed: December 9, 2002
    Publication date: February 26, 2004
    Inventor: Beate Schmidt
  • Patent number: 6630483
    Abstract: N-oxides of the compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R6 is an R7- and R8-substituted phenyl radical, they are active bronchial therapeutics.
    Type: Grant
    Filed: June 18, 2002
    Date of Patent: October 7, 2003
    Assignee: Altana Pharma AG
    Inventor: Beate Schmidt
  • Patent number: 6538005
    Abstract: The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, arm novel active bronchial therapeutics.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: March 25, 2003
    Assignee: ALTANA Pharma AG
    Inventor: Beate Gutterer
  • Patent number: 6534518
    Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: March 18, 2003
    Assignee: Altana Pharma AG
    Inventor: Beate Gutterer
  • Patent number: 6534519
    Abstract: The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: March 18, 2003
    Assignee: Altana Pharma AG
    Inventor: Beate Gutterer
  • Patent number: 6479505
    Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and Ar have the meanings indicated in the description, are novel active bronchial therapeutics.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: November 12, 2002
    Assignee: Altana Pharma AG
    Inventor: Beate Gutterer
  • Patent number: 6476025
    Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51, R6, R13 and R20 have the meaning indicated in the description, are novel active bronchial therapeutics
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: November 5, 2002
    Assignee: Altana Pharma AG
    Inventor: Beate Gutterer
  • Patent number: 6191138
    Abstract: Compounds of formula (I), where R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings given in the description, are new active bronchial therapeutic agents.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: February 20, 2001
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Beate Gutterer
  • Patent number: 6127378
    Abstract: Compounds of the formula I in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel efficacious bronchial therapeutics.
    Type: Grant
    Filed: September 3, 1998
    Date of Patent: October 3, 2000
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Beate Gutterer
  • Patent number: 6121279
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R31, R4, R5, R51 and R6 are as defined in the specification. The compounds are phosphodiesterase inhibitors. Also disclosed are pharmaceutical compositions and methods of use of the compounds.
    Type: Grant
    Filed: January 24, 2000
    Date of Patent: September 19, 2000
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Beate Gutterer
  • Patent number: 6015902
    Abstract: Intercalator compounds of formula I-T.sub.m as defined herein are provided which are comprised of intercalator moieties, or substituted intercalator moieties, having one or more functionalized chains, or moieties, and which compounds provide a high affinity for binding to the DNA molecule and show reduced self-quenching, while providing superior transport kinetics. The compounds have been found to provide enhanced fluorescence when bound to a DNA molecule within a fluorescent flow cytometry environment which is about eight to ten times brighter in fluorescence than "bis" structure conventional intercalating agents and other known intercalating agents utilized in flow cytometry environment.
    Type: Grant
    Filed: October 21, 1996
    Date of Patent: January 18, 2000
    Assignee: Abbott Laboratories
    Inventors: Christopher Bieniarz, Jeffrey Bruce Huff, Denis R. Henrard
  • Patent number: 5654298
    Abstract: This invention concerns novel aminopyridinium compounds of the formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are selected from the following combinations: ##STR1## (a) one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl or one of the above defined basic groups;R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R.sup.3 and R.sup.5 are independently hydrogen, alkyl or alkenyl;(b) R.sup.2 is a basic group as defined above, R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; has any of the meanings defined in(a) above; and R.sup.3 is hydrogen, alkyl or alkenyl; and(c) R2 has any of the meanings defined above and R.sup.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: August 5, 1997
    Assignee: Imperial Chemical Industries
    Inventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
  • Patent number: 5629007
    Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in preventing the development of prostatic cancer, or preventing or treating the metastasis to bone of prostatic cancer.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: May 13, 1997
    Assignee: ELi Lilly and Company
    Inventors: James E. Audia, Blake L. Neubauer
  • Patent number: 5621104
    Abstract: The present invention provides for the preparation of compounds,namely, 3-phenanthridinones and their derivatives and their unique ability to inhibit 5-alpha-reductase or their isozymes thereof in mammals enabling said compounds for treating hyperandrogenic conditions of acne, androgenic alopecia, male pattern baldness,female hirsutism,benign prostatic hyperplasia, prostatitis and prostatic cancer.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: April 15, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, William K. Hagmann
  • Patent number: 5599932
    Abstract: Intercalator compounds are provided which are comprised of intercalator moieties, or substituted intercalator moieties, having one or more functionalized chains, or moieties, and which compounds provide a high affinity for binding to the DNA molecule and show reduced self-quenching, while providing superior transport kinetics. The compounds have been found to provide enhanced fluorescence when bound to a DNA molecule within a fluorescent flow cytometry environment which is about eight to ten times brighter in fluorescence than "bis" structure conventional intercalating agents and other known intercalating agents utilized in flow cytometry environment.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 4, 1997
    Assignee: Abbott Laboratories
    Inventors: Christopher Bieniarz, Jeffrey B. Huff, Denis R. Henrard
  • Patent number: 5582984
    Abstract: Phenanthridium compounds are provided which are comprised of intercalators and substituted intercalator segments having a functionalized chain or chains which provide a high affinity for binding to the DNA molecule and show reduced self-quenching, while providing superior transport kinetics. The compounds have been found to provide enhanced fluorescence when bound to a DNA molecule within a fluorescent flow cytometry environment which is about eight to ten times brighter in fluorescence than "bis" structure intercalators and other known intercalators utilized in flow cytometry environment, said enhancement of fluorescence allows a drastic reduction in the amount of intercalator needed for applications of similar sensitivity than those using known intercalators.
    Type: Grant
    Filed: June 29, 1994
    Date of Patent: December 10, 1996
    Assignee: Abbott Laboratories
    Inventors: Christopher Bieniarz, Jeffrey B. Huff, Denis R. Henrard
  • Patent number: 5443986
    Abstract: Activity of enzymes and enzyme conjugates is detected using novel substrates made from a class of fluorophores, generally including quinazolinones (quinazolones), benzimidazoles, benzothiazoles, benzoxazoles, quinolines, indolines, and phenanthridines, having the general formula: ##STR1## where carbon atoms of --C.sup.1 .dbd.C.sup.2 -- are joined to complete a first 5- or 6-membered aromatic ring which optionally contains one of the hetero atoms N, O or S,and carbon atoms of --C.sup.4 --N.dbd.C.sup.3 -- are joined to complete a second 5- or 6-membered aromatic ring that contains a nitrogen between C.sup.3 and C.sup.4 and optionally contains an additional hetero atom N, O or S,where the first and second aromatic rings may be joined by a 5- or 6-membered bridging ring that contains at least the C.sup.2 from the first aromatic ring and the C.sup.
    Type: Grant
    Filed: July 6, 1993
    Date of Patent: August 22, 1995
    Assignee: Molecular Probes, Inc.
    Inventors: Richard P. Haughland, Zhijian Huang, Karen D. Larison, Yu-zhong Zhang
  • Patent number: 5316906
    Abstract: Novel fluorescent precipitating substrates made from a class of fluorophores, generally including quinazolinones (quinazolones), benzimidazoles, benzothiazoles, benzoxazoles, quinolines, indolines, and phenanthridines, having the general formula: ##STR1## where carbon atoms of --C.sup.1 .dbd.C.sup.2 -- are further joined so as to complete a first 5- or 6-membered aromatic ring which may contain at least one of the hetero atoms N, O or S,where carbon atoms of --C.sup.4 --N.dbd.C.sup.3 -- are further joined so as to complete a second 5- or 6-membered aromatic ring that contains at least the nitrogen between C.sup.3 and C.sup.4 and may contain at least one additional hetero atom N, O or S,where the first and second aromatic rings may be joined by a 5- or 6-membered bridging ring that contains at least the C.sup.2 from the first aromatic ring and the C.sup.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: May 31, 1994
    Assignee: Molecular Probes, Inc.
    Inventors: Richard P. Haugland, Yu-zhong Zhang, Stephen T. Yue, Ewald Terpetschnig, Nels A. Olson, John J. Naleway, Karen D. Larison, Zhijian Huang
  • Patent number: 5312921
    Abstract: Novel fluorescent dyes are provided, characterized by having a fluorophore joined to a polycationic chain of at least two positive charges. The dyes are found to provide for high enhancement upon binding to nucleic acid and have strong binding affinities to the nucleic acid, as compared to the fluorophore without the polycationic chain. The dyes find use in detection of dsDNA in gel electrophoresis and solution at substantially higher sensitivities using substantially less dye.
    Type: Grant
    Filed: May 14, 1993
    Date of Patent: May 17, 1994
    Assignee: Regents of the University of California
    Inventors: Alexander N. Glazer, Scott C. Benson
  • Patent number: 5250517
    Abstract: Compounds which are amino acid derivatives and have the formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl or imidazol-4-yl, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: October 5, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Quirico Branca, Albrecht Edenhofer, Eva-Maria Gutknecht, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
  • Patent number: 4959309
    Abstract: A labeled nucleic acid probe comprising (a) a nucleic acid component, (b) a nucleic acid-binding ligand photochemically linked to the nucleic acid component, and (c) a label chemically linked to the nucleic acid-binding ligand. The label can be a specifically bindable ligand such as a hapten or biotin, an enzyme such as a .beta.-galactosidase or horse radish peroxidase, a fluorescent radical, a phycobiliprotein, a luminescent radical, or a radioisotope. The probe can be used in assays of nucleic acids, taking advantage of the ability of the nucleic acid component to hydridize.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: September 25, 1990
    Assignee: Molecular Diagnostics, Inc.
    Inventors: Nanibhushan Dattagupta, Donald M. Crothers
  • Patent number: 4942227
    Abstract: Bifunctional molecules having a DNA intercalator or DNA groove binder linked to ethylene diamine tetraacetic acid such as compounds having the formula: ##STR1## wherein R is methyl or ethyl. Also, the method of cleaving DNA by contact with one of the above-identified molecules in the presence of ferrous ion and oxygen.The process of preparing said molecules by the reaction of P-carboxy methidium halide, p-carboxy ethidium halide, or other DNA intercalator or DNA groove binder with 1-3-diaminopropane followed by condensation with ethylenediamine tetraacetic acid.Distamycin-EDTA.Fe(II)(DE.FE(II)) contains EDTA attached to the amino terminus of the groove binder tripeptide (tris-N-methylpyrrolecarboxamide). De.Fe(II) cleaves DNA contiguous to a five base pair A+T rich sequence. This is a novel and unique molecule and superior in sequence specificity to the naturally occurring antitumor compound used in man, bleomycin which cleaves DNA at a two base pair recognition site. EDTA-distamycin-Fe(II)(ED.
    Type: Grant
    Filed: January 23, 1987
    Date of Patent: July 17, 1990
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Robert P. Hertzberg
  • Patent number: 4929625
    Abstract: Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT.sub.3 -antagonistic activity. In the formula ##STR2## represents an optionally substituted heteroaryl group containing a hetero atom X and --B represents a saturated azabicyclic ring such as quinuclidyl or tropanyl.
    Type: Grant
    Filed: August 1, 1988
    Date of Patent: May 29, 1990
    Assignee: John Wyeth and Brothers Limited
    Inventor: Ian A. Cliffe
  • Patent number: 4665184
    Abstract: Novel bifunctional molecules having a DNA intercalator or DNA groove binder linked to ethylene diamine tetraacetic acid such as compounds having the formula: ##STR1## wherein R is methyl or ethyl. Also, the method of cleaving DNA by contact with one of the above-identified molecules in the presence of ferrous ion and oxygen.The process of preparing said molecules by the reaction of P-carboxy methidium halide, p-carboxy ethidium halide, or other DNA intercalator or DNA groove binder with 1-3-diaminopropane followed by condensation with ethylenediamine tetraacetic acid.Distamycin-EDTA.Fe(II)(DE.FE(II)) contains EDTA attached to the amino terminus of the groove binder tripeptide (tris-N-methylpyrrolecarboxamide). DE.Fe(II) cleaves DNA contiguous to a five base pair A+T rich sequence. This is a novel and unique molecule and superior in sequence specificity to the naturally occurring antitumor compound used in man, bleomycin which cleaves DNA at a two base pair recognition site. EDTA-distamycin-Fe(II)(ED.
    Type: Grant
    Filed: May 7, 1986
    Date of Patent: May 12, 1987
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Robert P. Hertzberg