Unsaturated Ring Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/109)
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Patent number: 9035057Abstract: 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: GrantFiled: December 16, 2010Date of Patent: May 19, 2015Assignee: Washington UniversityInventors: Robert H. Mach, Mark Mintun, Wenhua Chu, Laura Dugan
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Publication number: 20140191208Abstract: 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: ApplicationFiled: August 20, 2013Publication date: July 10, 2014Applicant: SAMSUNG DISPLAY CO., LTD.Inventors: Seul-Ong Kim, Dong-Woo Shin
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Publication number: 20140151670Abstract: 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: ApplicationFiled: July 19, 2013Publication date: June 5, 2014Applicant: LG CHEM, LTD.Inventors: Dong Hoon Lee, Minyoung Kang, Jungi Jang, Boonjae Jang, Minseung Chun, Kidong Koo
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Publication number: 20140073058Abstract: 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: ApplicationFiled: August 8, 2013Publication date: March 13, 2014Applicant: Biotium, Inc.Inventors: Fei Mao, Wai-Yee Leung
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Publication number: 20140039001Abstract: 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: ApplicationFiled: October 11, 2013Publication date: February 6, 2014Applicant: TAKEDA GMBHInventors: Ulrich KAUTZ, Matthias WEBEL, Christian SCHEUFLER, Rolf-Peter HUMMEL
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Publication number: 20130096152Abstract: 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: ApplicationFiled: December 7, 2012Publication date: April 18, 2013Applicant: NYCOMED GMBHInventor: NYCOMED GMBH
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Publication number: 20130079522Abstract: 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: ApplicationFiled: December 16, 2010Publication date: March 28, 2013Applicant: WASHINGTON UNIVERSITYInventors: Robert H. Mach, Mark Mintun, Wenhua Chu, Laura Dugan
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Publication number: 20130012597Abstract: 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: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Applicant: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATIONInventors: Naoko Shimada, Atsushi Maruyama
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Publication number: 20120316342Abstract: 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: ApplicationFiled: January 31, 2011Publication date: December 13, 2012Inventors: Masanori Baba, Yuichi Hashimoto, Hiroshi Aoyama, Kazuyuki Sugita, Masahiko Nakamura, Atsushi Aoyama, Yasuo Urata
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Patent number: 8329906Abstract: 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: GrantFiled: July 27, 2009Date of Patent: December 11, 2012Assignee: Nycomed GmbHInventor: Ulrich Kautz
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Publication number: 20110269705Abstract: 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: ApplicationFiled: December 4, 2009Publication date: November 3, 2011Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
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Publication number: 20110257169Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.Type: ApplicationFiled: May 19, 2011Publication date: October 20, 2011Applicant: NYCOMED GmbHInventor: Ulrich KAUTZ
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Publication number: 20110257221Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.Type: ApplicationFiled: May 19, 2011Publication date: October 20, 2011Applicant: NYCOMED GMBHInventor: Ulrich KAUTZ
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Publication number: 20110190480Abstract: 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: ApplicationFiled: April 11, 2011Publication date: August 4, 2011Inventors: Nikolai (Mykola) IGNATYEV, Urs Welz-Biermann, Helge Willner, Maik Finze, Eduard Bernhardt, Andriy Kucheryna
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Publication number: 20110156017Abstract: 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: ApplicationFiled: September 24, 2009Publication date: June 30, 2011Inventors: Dong-Hoon Lee, Hyun Nam, Jun-Gi Jang, Seong-So Kim, Tae-Yoon T Park
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Publication number: 20110012092Abstract: 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: ApplicationFiled: December 24, 2008Publication date: January 20, 2011Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Hiroshi Yamamoto, Takashi Arakane
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Publication number: 20100216772Abstract: 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: ApplicationFiled: October 5, 2004Publication date: August 26, 2010Inventors: Stefano Pegoraro, Martin Lang, Juliane Feurle, Jürgen Krauss
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Patent number: 7585872Abstract: 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: GrantFiled: February 17, 2005Date of Patent: September 8, 2009Assignee: NYCOMED GmbHInventor: Ulrich Kautz
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Publication number: 20080312237Abstract: 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: ApplicationFiled: July 18, 2008Publication date: December 18, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
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Publication number: 20080161339Abstract: Compounds of the formula I in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.Type: ApplicationFiled: March 9, 2005Publication date: July 3, 2008Applicant: ALTANA PHARMA AGInventor: Ulrich Kautz
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Publication number: 20080119505Abstract: 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: ApplicationFiled: January 31, 2006Publication date: May 22, 2008Applicant: ALTANA Pharma AGInventors: Ulrich Kautz, Beate Schmidt, Dieter Flockerzi, Maria Vittoria Chiesa, Armin Hatzelmann, Christof Zitt, Johannes Barsig, Andrea Wohlsen, Degenhard Marx, Hans-Peter Kley
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Patent number: 7329676Abstract: 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: GrantFiled: August 28, 2003Date of Patent: February 12, 2008Assignee: Nycomed GmbHInventors: Ulrich Kautz, Beate Schmidt
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Patent number: 7074782Abstract: 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: GrantFiled: August 21, 2003Date of Patent: July 11, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M. C. Golec
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Patent number: 7067667Abstract: 3,4-dihydroquinoline derivatives, a process for their production and their use in pharmaceutical agents.Type: GrantFiled: October 29, 2003Date of Patent: June 27, 2006Assignee: Schering AktiengesellschaftInventors: Stefan Jaroch, Hartmut Rehwinkel, Peter Holscher, Detlev Sülzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Mcdougall McDonald
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Patent number: 6894061Abstract: 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: GrantFiled: November 20, 2003Date of Patent: May 17, 2005Assignee: WyethInventors: Albert John Molinari, Mark Antony Ashwell, Brian Hugh Ridgway, Amedeo Arturo Failli, William Jay Moore
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Patent number: 6884802Abstract: 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: GrantFiled: July 7, 2001Date of Patent: April 26, 2005Assignee: ALTANA Pharma AGInventor: Beate Schmidt
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Publication number: 20040038979Abstract: 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: ApplicationFiled: December 9, 2002Publication date: February 26, 2004Inventor: Beate Schmidt
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Patent number: 6630483Abstract: 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: GrantFiled: June 18, 2002Date of Patent: October 7, 2003Assignee: Altana Pharma AGInventor: Beate Schmidt
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Patent number: 6538005Abstract: 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: GrantFiled: July 12, 2001Date of Patent: March 25, 2003Assignee: ALTANA Pharma AGInventor: Beate Gutterer
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Patent number: 6534518Abstract: 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: GrantFiled: July 12, 2001Date of Patent: March 18, 2003Assignee: Altana Pharma AGInventor: Beate Gutterer
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Patent number: 6534519Abstract: 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: GrantFiled: July 12, 2001Date of Patent: March 18, 2003Assignee: Altana Pharma AGInventor: Beate Gutterer
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Patent number: 6479505Abstract: 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: GrantFiled: July 12, 2001Date of Patent: November 12, 2002Assignee: Altana Pharma AGInventor: Beate Gutterer
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Patent number: 6476025Abstract: 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 therapeuticsType: GrantFiled: July 12, 2001Date of Patent: November 5, 2002Assignee: Altana Pharma AGInventor: Beate Gutterer
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Patent number: 6191138Abstract: 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: GrantFiled: July 31, 1998Date of Patent: February 20, 2001Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Beate Gutterer
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Patent number: 6127378Abstract: 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: GrantFiled: September 3, 1998Date of Patent: October 3, 2000Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Beate Gutterer
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Patent number: 6121279Abstract: 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: GrantFiled: January 24, 2000Date of Patent: September 19, 2000Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Beate Gutterer
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Patent number: 6015902Abstract: 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: GrantFiled: October 21, 1996Date of Patent: January 18, 2000Assignee: Abbott LaboratoriesInventors: Christopher Bieniarz, Jeffrey Bruce Huff, Denis R. Henrard
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Patent number: 5654298Abstract: 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: GrantFiled: April 16, 1991Date of Patent: August 5, 1997Assignee: Imperial Chemical IndustriesInventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
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Patent number: 5629007Abstract: 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: GrantFiled: March 21, 1995Date of Patent: May 13, 1997Assignee: ELi Lilly and CompanyInventors: James E. Audia, Blake L. Neubauer
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Patent number: 5621104Abstract: 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: GrantFiled: September 15, 1995Date of Patent: April 15, 1997Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, William K. Hagmann
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Patent number: 5599932Abstract: 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: GrantFiled: June 5, 1995Date of Patent: February 4, 1997Assignee: Abbott LaboratoriesInventors: Christopher Bieniarz, Jeffrey B. Huff, Denis R. Henrard
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Patent number: 5582984Abstract: 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: GrantFiled: June 29, 1994Date of Patent: December 10, 1996Assignee: Abbott LaboratoriesInventors: Christopher Bieniarz, Jeffrey B. Huff, Denis R. Henrard
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Patent number: 5443986Abstract: 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: GrantFiled: July 6, 1993Date of Patent: August 22, 1995Assignee: Molecular Probes, Inc.Inventors: Richard P. Haughland, Zhijian Huang, Karen D. Larison, Yu-zhong Zhang
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Patent number: 5316906Abstract: 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: GrantFiled: August 23, 1991Date of Patent: May 31, 1994Assignee: 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
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Patent number: 5312921Abstract: 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: GrantFiled: May 14, 1993Date of Patent: May 17, 1994Assignee: Regents of the University of CaliforniaInventors: Alexander N. Glazer, Scott C. Benson
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Patent number: 5250517Abstract: 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: GrantFiled: May 4, 1992Date of Patent: October 5, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albrecht Edenhofer, Eva-Maria Gutknecht, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
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Patent number: 4959309Abstract: 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: GrantFiled: October 9, 1987Date of Patent: September 25, 1990Assignee: Molecular Diagnostics, Inc.Inventors: Nanibhushan Dattagupta, Donald M. Crothers
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Patent number: 4942227Abstract: 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: GrantFiled: January 23, 1987Date of Patent: July 17, 1990Assignee: California Institute of TechnologyInventors: Peter B. Dervan, Robert P. Hertzberg
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Patent number: 4929625Abstract: 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: GrantFiled: August 1, 1988Date of Patent: May 29, 1990Assignee: John Wyeth and Brothers LimitedInventor: Ian A. Cliffe
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Patent number: 4665184Abstract: 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: GrantFiled: May 7, 1986Date of Patent: May 12, 1987Assignee: California Institute of TechnologyInventors: Peter B. Dervan, Robert P. Hertzberg