Phenothiazine As Three Cyclos Of Polycyclo Ring System Having At Least Four Cyclos Patents (Class 544/31)
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Patent number: 11569449Abstract: An organic electroluminescence device comprising: a cathode, an anode, and at least one organic layer disposed between the cathode and the anode, wherein at least one layer of the at least one organic layer comprises a compound represented by the following formulas (1-1) and (1-3) or a compound represented by the following formulas (1-2) and (1-3).Type: GrantFiled: December 5, 2018Date of Patent: January 31, 2023Assignee: IDEMITSU KOSAN CO., LTD.Inventors: Ryota Takahashi, Hidetsugu Ikeda, Keita Seda, Yuki Nakano
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Patent number: 11557730Abstract: An organic electroluminescence device comprising: a cathode, an anode, and at least one organic layer disposed between the cathode and the anode, wherein at least one layer of the at least one organic layer comprises a compound represented by the following formulas (1-1) and (1-3) or a compound represented by the following formulas (1-2) and (1-3).Type: GrantFiled: September 6, 2019Date of Patent: January 17, 2023Assignee: IDEMITSU KOSAN CO., LTD.Inventors: Ryota Takahashi, Hidetsugu Ikeda, Keita Seda, Yuki Nakano
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Patent number: 9028728Abstract: The present invention relates to photochromic materials that include one or more indeno-fused naphthopyrans that have particular groups at the 7, 11, and 13 positions thereof, and at the position alpha to the oxygen of the pyran ring thereof. With some embodiments, hydrogen or an alkoxy group is bonded to the 7 position, an optionally substituted phenyl is bonded to the 11 position, two alkyl groups are bonded to the 13 position, and two optionally substituted phenyl groups are bonded to the position alpha to the oxygen of the pyran ring of the indeno-fused naphthopyran compound. The 13 position of the indeno-fused naphthopyrans is free of ether groups in which an ether oxygen is bonded to the 13 position, and hydroxyl. The present invention also relates to photochromic articles and compositions that include such indeno-fused naphthopyrans.Type: GrantFiled: December 8, 2011Date of Patent: May 12, 2015Assignee: Transitions Optical, Inc.Inventors: Kevin E. Bancroft, Anu Chopra, Xiao-Man Dai, Beon-Kyu Kim, David B. Knowles, Jason R. Lewis, Victor A. Montes, Stephen D. Straight, Massimiliano Tomasulo, Barry Van Gemert, Robert W. Walters, Wenjing Xiao, Huayun Yu, Elizabeth A. Zezinka
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Patent number: 8481785Abstract: The invention pertains to new materials based on sterically inhibited donor arylboranes for the improvement of electron injection and electron transport in organic electronic components like organic light-emitting diodes (OLED's), organic field effect transistors (OFET's), and on organic photovoltaics based components, in particular, organic solar cells.Type: GrantFiled: August 23, 2006Date of Patent: July 9, 2013Assignee: Osram Opto Semiconductors GmbHInventor: Andreas Kanitz
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Patent number: 8445483Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,Type: GrantFiled: October 7, 2011Date of Patent: May 21, 2013Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang, John S. Gunn, Larry S. Schlesinger
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Patent number: 8388872Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran of structural formulas I or II, having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.Type: GrantFiled: February 21, 2012Date of Patent: March 5, 2013Assignee: Transitions Optical, Inc.Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, Jr., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Publication number: 20130053555Abstract: The present invention relates to electronic devices, in particular organic electroluminescent devices, comprising compounds of the formula (1), and the corresponding compounds.Type: ApplicationFiled: March 29, 2011Publication date: February 28, 2013Inventors: Amir Hossain Parham, Christof Pflumm, Philipp Stoessel, Arne Buesing, Dominik Joosten
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Publication number: 20130026422Abstract: The present invention relates to a compound according to formula (I), to the use thereof in an electronic device and to an electronic device which comprises one or more compounds according to formula (I).Type: ApplicationFiled: March 16, 2011Publication date: January 31, 2013Applicant: Merck Patent GmbHInventors: Amir Hossain Parham, Christof Pflumm
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Publication number: 20120328530Abstract: A compound of formula (III), or a pharmaceutically acceptable derivative thereof for use in a method of combating and/or detecting a pathogen and/or tumour cells; wherein X is selected from O, S and Se; each of R2, R3 and R4 is independently selected from hydrogen or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; and R1 is selected from halogen, sulfo, acyl, sulfoxy, mercapto, nitro, amino, hydroxy or an optionally substituted alkyl, alkenyl, alkynyl, aryl, amine or alkoxy group; wherein R1 is not methyl or hydrogen when each of R3 and R4 is methyl or hydrogen.Type: ApplicationFiled: March 11, 2011Publication date: December 27, 2012Applicant: PHARMALUCIA LIMITEDInventor: Mark Wainwright
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Patent number: 8308995Abstract: A chromene compound represented by the following formula (1): wherein R1, R2, R3, R4, R5, R6, m, and n are defined in the specification. The chromene compound is rarely deteriorated by exposure.Type: GrantFiled: February 9, 2012Date of Patent: November 13, 2012Assignee: Tokuyama CorporationInventors: Soko Kasai, Shinobu Izumi
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Patent number: 8308996Abstract: A photochromic chromene compound which develops a color of a neutral tint, has high color optical density, a high fading speed and high durability, and has an indeno(2,1-f)naphtho(1,2-b)pyran structure represented by the following formula as the basic skeleton, wherein a sulfur-containing substituent selected from thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group and heteroarylthio group is bonded to the 6-position and/or 7-position carbon atom(s).Type: GrantFiled: August 4, 2010Date of Patent: November 13, 2012Assignee: Tokuyama CorporationInventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi
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Publication number: 20120227802Abstract: The present invention provides a organic compound of the general structural formula 1 and photovoltaic device and photovoltaic layer comprising thereof Said organic compound forms rod-like supramolecules and absorbs electromagnetic radiation in at least one predetermined spectral subrange within a wavelength range from 400 to 3000 nm with excitation of electron-hole pairs. The polycyclic core Cor1, the bridging group B, and the polycyclic core Cor2 form a molecular system selected from the list comprising donor-bridge-acceptor-bridge-donor and acceptor-bridge-donor-bridge-acceptor in which a dissociation of excited electron-hole pairs is carried out. A solution of the organic compound or its salt forms a solid photovoltaic layer on a substrate.Type: ApplicationFiled: March 7, 2012Publication date: September 13, 2012Applicant: Cryscade Solar LimitedInventors: Pavel KHOKHLOV, Pavel Ivan Lazarev, Alexey Nokel
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Patent number: 8263589Abstract: The invention relates generally to the use of diaminophenothiazine compounds to inhibit or reverse the aggregation of synuclein, and for their use in the manufacture of medicaments for this purpose (e.g. for the treatment of Parkinson's Disease). Also provided are related methods of detecting or labelling of aggregated synuclein.Type: GrantFiled: March 28, 2007Date of Patent: September 11, 2012Assignee: Wista Laboratories Ltd.Inventors: Claude Michel Wischik, Janet Elizabeth Rickard, Charles Robert Harrington, David Horsley
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Patent number: 8207146Abstract: The present invention relates to substituted phenothiazines with a double bond and physiologically acceptable salts thereof, and their use as a medicament.Type: GrantFiled: March 16, 2010Date of Patent: June 26, 2012Assignee: Sanofi-AventisInventors: Stefanie Keil, Elisabeth Defossa, Dieter Schmoll, Axel Dietrich, Johanna Kuhlmann-Gottke, Karl-Christian Engel
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Patent number: 8158037Abstract: The present invention provides ophthalmic devices comprising at least one photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic materials. Other non-limiting embodiments relate to methods of making the ophthalmic devices comprising photochromic materials.Type: GrantFiled: September 1, 2010Date of Patent: April 17, 2012Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, Jr., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Patent number: 8158784Abstract: The invention relates to a 1-aza-bicyclo[2.2.2]oct-2-en-3-ylmethyl acetate of the formula (I), wherein said compound is useful as a synthesis intermediate for the production of mequitazine.Type: GrantFiled: January 17, 2008Date of Patent: April 17, 2012Assignee: Pierre Fabre MedicamentInventors: Charles Mioskowski, Vanessa Gonnot, Rachid Baati, Marc Nicolas
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Patent number: 8147725Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.Type: GrantFiled: September 1, 2010Date of Patent: April 3, 2012Assignee: Transitions Optical, IncInventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank Molock, Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Patent number: 8147726Abstract: A chromene compound represented by the following formula (1): wherein R1, R2, R3, R4, R5, R6, m, and n are defined in the specification. The chromene compound is rarely deteriorated by exposure.Type: GrantFiled: May 8, 2009Date of Patent: April 3, 2012Assignee: Tokuyama CorporationInventors: Soko Kasai, Shinobu Izumi
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Publication number: 20120058995Abstract: This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the e//i method comprises the steps of in order: a thiosulfonic acid formation (TSAF) as illustrated below, wherein the reaction is carried out in the presence of a thio sulfate and an oxidizing agent that is or comprises persulfate an oxidative coupling (OC); and a ring closure (RC). The resulting compounds and compositions comprising them (e.g., tablets, capsules) are useful in methods of medical treatment and diagnosis, etc., for example, tauopathies, or Alzheimer's disease (AD).Type: ApplicationFiled: May 11, 2010Publication date: March 8, 2012Applicant: WisTa Laboratories Ltd.Inventors: Christopher Paul Larch, John Mervyn David Storey, Craig Williamson, Colin Marshall, Steven John Kemp
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Publication number: 20100063034Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.Type: ApplicationFiled: September 1, 2009Publication date: March 11, 2010Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman
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Publication number: 20090069308Abstract: The present invention relates to the use of at least one antihistamine agent for the preparation of a medicament for use in the preventive or early treatment of inflammatory syndromes of viral origin, in particular arthritis of the distal joints, more particularly those triggered by togaviruses. The invention also relates to a combination product of at least one antihistamine agent and of at least one antiserotonin agent for its simultaneous, separate or sequential use in preventive or early therapy for inflammatory syndromes of viral origin, in particular arthritis of the distal joints, more particularly those triggered by togaviruses.Type: ApplicationFiled: March 9, 2007Publication date: March 12, 2009Applicant: Pierre Fabre MedicamentInventors: Jean Deregnaucourt, Etienne Andre, Jacky Tisne-Versailles
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Publication number: 20080303003Abstract: The present invention relates to anthracene derivatives, to the use thereof in organic electroluminescent devices, and to organic electroluminescent devices comprising these compounds.Type: ApplicationFiled: November 17, 2006Publication date: December 11, 2008Applicant: MERCK PATENT GMBHInventors: Holger Heil, Philipp Stoessel, Amir Parham, Horst Vestweber
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Patent number: 7235550Abstract: The invention relates to compounds of formula (I): wherein: G1 represents an alkylene chain as defined in the description, A represents R2 and R3 represent hydrogen, alkyl, alkoxy or hydroxy or together form oxo, R4 and R5 represent hydrogen, R1 is as defined in the description, and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.Type: GrantFiled: October 9, 2002Date of Patent: June 26, 2007Assignee: Les Laboratoires ServierInventors: Gérald Guillaumet, Marie-Claude Viaud, Hervé Van de Poel, Philippe Delagrange, Caroline Bennejean, Pierre Renard
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Patent number: 7141566Abstract: The invention relates to compounds of formula (I), the tautomeric and isomeric forms and salts thereof, in addition to a method for production and use thereof in medicaments.Type: GrantFiled: August 23, 2000Date of Patent: November 28, 2006Assignee: Schering AktiengesellschaftInventors: Peter Hölscher, Hartmut Rehwinkel, Stefan Jaroch, Detlev Sülzle, Margrit Hillmann, Gerardine Anne Burton, Fiona Mcdougall McDonald
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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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Publication number: 20040254372Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: ApplicationFiled: February 9, 2004Publication date: December 16, 2004Inventors: Weizheng Xu, Dana V. Ferraris, Jia-He Li, Vincent J. Kalish
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Patent number: 6821971Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; R2a and R2b units are each independently hydrogen, ethers, amines, amides, carboxylates, or said units can form a double bond, a carbonyl, or R2a and R2b can be taken together to form a substituted or unsubstituted ring comprising from 4 to 8 atoms, said ring selected from the group consisting of: i) carbocyclic; ii) heterocyclic; iii) aryl; iv) heteroaryl; v) bicyclic; and vi) heterobicyclic.Type: GrantFiled: September 18, 2002Date of Patent: November 23, 2004Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Biswanath De
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Publication number: 20030105086Abstract: The invention features compounds that act as antimicrobial agents and/or antimicrobial enhancer agents, compositions that include the antimicrobial enhancer agents of the invention, and methods for treating microbial infections using those compositions.Type: ApplicationFiled: September 6, 2002Publication date: June 5, 2003Inventors: Arthur F. Michaelis, Hawkins V. Maulding
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Patent number: 6514984Abstract: A method is disclosed for the prevention and treatment of Alzheimer's disease by administering to a human in need thereof an effective amount of a substituted tricyclic sPLA2 inhibitor.Type: GrantFiled: April 12, 2000Date of Patent: February 4, 2003Assignee: Eli Lilly and CompanyInventor: August Masaru Watanabe
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Patent number: 6476021Abstract: Novel fused tetracyclic heterocyclic compounds having a potent and highly selective effect of inhibiting cyclic GMP phosphodiesterase (cGMP-PDE) and a high safety; a process for producing the same; drugs characterized by containing at least one of these compounds as the active ingredient, in particular, preventives and/or remedies for pulmonary hypertension, ischemic heart diseases, erectile insufficiency, female sexual dysfunction or diseases against which cGMP-PDE inhibitory effects are efficacious and intermediates useful in producing the above compounds.Type: GrantFiled: May 26, 2000Date of Patent: November 5, 2002Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Masayuki Ohashi, Hidemitsu Nishida, Toshiyuki Shudo
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Patent number: 6468996Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: October 22, 2002Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6426416Abstract: The process for chemically modifying metal-free, colored anthraquinone or condensed anthraquinone compounds or the compounds prepared by said process for improving one or more properties thereof such as water dispersibility, compatibility with other organics, or increased chemical reactivity, wherein the process includes providing material with from 1-6 sulfonylhalide groups or sulfonate ester groups or mixtures thereof, and contacting the material under sulfonamido forming conditions with one or more reactants containing one or more poly(oxyalkylene) moieties, each of the reactants having from 1 to 4 functional amino groups, and each of the poly(oxyalkylene) moieties being comprised of from about 4 to about 200 epoxide reactant residues at least about 50 mole percent of which residues contain 2-4 carbons and wherein the total of said epoxide reactant residues is from about 4 to about 600.Type: GrantFiled: January 6, 2000Date of Patent: July 30, 2002Assignee: Millikan & CompanayInventors: Max Allen Weaver, Edward William Kluger, David Jesse Moody
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Patent number: 6423707Abstract: Novel nitroimidazole compounds are provided that have a substituent linked via an ester linkage. The ester linkage may be obtained by derivation of the hydroxyl group of metronidazole. These nitroimidazole ester analogs have anti-microbial activity, with a number of novel compounds having an anti-microbial activity that is significantly improved with respect to metronidazole.Type: GrantFiled: August 28, 2000Date of Patent: July 23, 2002Assignee: California Pacific Medical CenterInventors: Li-Xi Yang, Hui-Juan Wang, Xiandao Pan
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Publication number: 20020077320Abstract: Novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them.Type: ApplicationFiled: December 6, 2001Publication date: June 20, 2002Applicant: DR. REDDY'S RESEARCH FOUNDATION AND REDDY- CHEMINOR, INC.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6407231Abstract: This invention relates to a novel, technically advantageous process for the preparation of a mixture of alkylated phenothiazines and diphenylamines. Starting from diphenylamine, this is reacted with elemental sulfur in the presence of iodine, and the substance mixture of diphenylamine and phenothiazine is treated with an olefin in the presence of an acid catalyst.Type: GrantFiled: July 5, 2000Date of Patent: June 18, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Samuel Evans, Stephan Allenbach, Paul Dubs
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Patent number: 6166202Abstract: Benzophenoxazine compounds have formula (I) where X is O or NH, Y is NR.sup.1 R.sup.2 or H, R.sup.1 and R.sup.2 are alkyl or -L-A, L is a linker and A may be a reactive group by means of which the compound is linked to a biomolecule. The compounds can be used as fluorescent dyes for labelling biomolecules.Type: GrantFiled: January 15, 1999Date of Patent: December 26, 2000Assignee: Amersham Pharmacia Biotech UK LimitedInventors: Adrian Simmonds, James N Miller, Christopher John Moody, Elizabeth Swann, Mark Samuel Jonathan Briggs, Ian Edward Bruce
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Patent number: 5721254Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: October 18, 1995Date of Patent: February 24, 1998Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
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Patent number: 5693649Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: October 18, 1995Date of Patent: December 2, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
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Patent number: 5688788Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 18, 1995Date of Patent: November 18, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
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Patent number: 5684031Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ; (c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) R.sub.1 is hydrogen or straight, branched or cyclic alkyl, aryl or C(.dbd.NH)--NHR.sub.4 ; and(f) R.sub.2, R.sub.3, and R.sub.4, are independently hydrogen, straight, branched or cyclic alkyl having from one to 10 carbon atoms, or aryl; R.sub.2 and R.sub.3 can be bonded together to form a ring having 5 or 6 atoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: November 4, 1997Assignee: The Procter & Gamble CompanyInventors: John Michael Janusz, James Madison Ridgeway, II
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Patent number: 5668129Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: March 27, 1996Date of Patent: September 16, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
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Patent number: 5574161Abstract: The invention relates to novel derivatives of quinolone-carboxylic acid and naphthyridonecarboxylic acid which are substituted in the 7 position by a 1- (or 5-)amino-methyl-2- (or 3-)oxa-7-aza-bicyclo[3.3.0]oct-7-yl residue, their salts, processes for their preparation and antibacterial agents containing these compounds.Type: GrantFiled: October 7, 1994Date of Patent: November 12, 1996Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Thomas Schenke, Klaus Grohe, Klaus-Dieter Bremm, Rainer Endermann, Karl G. Metzger
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Patent number: 5520848Abstract: A mixture containing phenothiazines which is obtainable by reacting a mixture of diphenylamines comprising______________________________________ 1 to 5% by weight a) diphenylamine of 8 to 18% by b) 4-tert-butyldiphenylamine weight of 21 to 31% by c) one or more compounds selected from weight of i) 4-tert-octyldiphenylamine ii) 4,4'-di-tert-butyldiphenylamine iii) 2,4,4'-tris-tert-butyldiphenylamine 20 to 31% by d) one or more compounds selected from weight of i) 4-tert-butyl-4'-tert-octyldiphenylamine ii) 2,2'- or 2,4'-di-tert-octyldiphenylamine iii) 2,4-di-tert-butyl-4'-tert-octyldiphenylamine, and 15 to 29% by e) the compound weight of i) 4,4'-di-tert-octyldiphenylamine, or the compounds i) 4,4'-di-tert-octyldiphenylamine and ii) 2,4-di-tert-octyl-4'-tert-butyldiphenylamine, ______________________________________with 1 to 200 mol % of elemental sulfur, in the presence of 0.Type: GrantFiled: February 7, 1995Date of Patent: May 28, 1996Assignee: Ciba-Geigy CorporationInventor: Samuel Evans
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Patent number: 5496942Abstract: A process is provided for preparing a tetrahydrobenzimidazole derivative represented by Formula (Ib): ##STR1## wherein Het representa s heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, and a halogen atom; and X.sup.2 represents a single bond connected to the carbon atom of the heterocyclic ring as represented by Het. The process comprises reacting a heterocyclic compound represented by Formula (IIIa):Het--X.sup.2 --H (IIIa)wherein Het and X.sup.2 are as defined above, with a carboxylic acid represented by Formula (II): ##STR2## or a reactive derivative thereof.Type: GrantFiled: February 14, 1994Date of Patent: March 5, 1996Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Mitsuaki Ohta, Tokuo Koide, Takeshi Suzuki, Akira Matsuhisa, Keiji Miyata, Junya Ohmori, Isao Yanagisawa
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Patent number: 5489603Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.Type: GrantFiled: July 15, 1993Date of Patent: February 6, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
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Patent number: 5413737Abstract: A mixture containing phenothiazines which is obtainable by reacting a mixture of diphenylamines comprising______________________________________ 1 to 5% by weight of a) diphenylamine 8 to 18% by weight of b) 4-tert-butyldiphenylamine 21 to 31% by weight of c) one or more compounds selected from i) 4-tert-octyldiphenylamine ii) 4,4'-di-tert-butyldiphenylamine iii) 2,4,4'-tris-tert-butyldiphenylamine 20 to 31% by weight of d) one or more compounds selected from i) 4-tert-butyl-4'-tert-octyldiphenylamine ii) 2,2'- or 2,4'-di-tert- octyldiphenylamine iii) 2,4-di-tert-butyl-4'-tert- octyldiphenylamine, and 15 to 29% by weight of e) the compound i) 4,4'-di-tert-octyldiphenylamine, or the compounds i) 4,4'-di-tert-octyldiphenylamine and ii) 2,4-di-tert-octyl-4'-tert- butyldiphenylamine, ______________________________________with 1 to 200 mol % of elemental sulfur, in the presence of 0.Type: GrantFiled: April 22, 1994Date of Patent: May 9, 1995Assignee: Ciba-Geigy CorporationInventor: Samuel Evans
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Patent number: 5344927Abstract: A tetrahydrobenzimidazole derivative represented by formula (I): ##STR1## wherein Het represents a heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxy group, a nitro group, a hydroxyl group, a lower alkoxycarbonyl group, and a halogen atom; and X represents a single bond or --NH-- which is bonded to the carbon atom or nitrogen atom of the heterocyclic ring, or a pharmaceutically acceptable salt thereof.The compound of formula (I) and a salt thereof exhibits antagonism against 5-HT.sub.3 receptor.Type: GrantFiled: March 30, 1993Date of Patent: September 6, 1994Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Mitsuaki Ohta, Tokuo Koide, Takeshi Suzuki, Akira Matsuhisa, Keiji Miyata, Junya Ohmori, Isao Yanagisawa
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Patent number: 5269954Abstract: The present invention relates to the preparation of antioxidant additives to lubricants and to their use in lubricating compositions. The additives according to the invention have the formula:ArAr'(H)N--(R--X).sub.a --R'Ywhere--Ar and Ar' are identical or different aromatic radicals, R and R', which are identical or different, denote a C.sub.2 -C.sub.18 linear or branched alkylene radical, X denotes an oxygen or sulphur atom or an --NH group, a is an integer between 0 and 5 and Y is chosen from the group consisting of --NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2, which are identical or different, denote a hydrogen atom or a C.sub.1 -C.sub.12 alkyl, alkenyl, cycloalkyl or arylalkyl radical --N.dbd.CH--Ar.sub.1 where Ar.sub.1 is an aryl radical containing at least one phenolic group --NR.sub.1 --CO--Ar.sub.1 and ##STR1## where R.sub.3 denotes a saturated or unsaturated, linear or branched alkyl radical.Type: GrantFiled: November 25, 1991Date of Patent: December 14, 1993Assignee: Elf FranceInventors: Laurent Germanaud, Patrick Azorin, Patrick Turello
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Patent number: 5124332Abstract: Substituted indoles and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: January 28, 1991Date of Patent: June 23, 1992Assignee: Warner-Lambert CompanyInventors: Lawrence D. Wise, David J. Wurtrow
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Patent number: 4990615Abstract: Triphendioxazine and triphendithiazine direct dyestuffs of the formula ##STR1## in which the substituents have the meanings given in the description produce on natural and synthetic OH-- and NH-- containing materials clear blue dyeings having good light and wet properties.Type: GrantFiled: September 12, 1989Date of Patent: February 5, 1991Assignee: Bayer AktiengesellschaftInventors: Hermann Henk, Wolfgang Harms, Peter Wild