Carbonyl, Sulfur, Or Cyano Attached Directly To Thiourea Nitrogen By Nonionic Bonding Patents (Class 564/23)
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Patent number: 8987262Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.Type: GrantFiled: November 16, 2012Date of Patent: March 24, 2015Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de BordeauxInventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
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Publication number: 20140275524Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: DOW AGROSCIENCES LLCInventors: Lindsey G. Fischer, Andrew L. Ward, Ronald Ross, JR., Natalie C. Giampietro, Carl DeAmicis, Yan Hao, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum, Jeff Petkus
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Publication number: 20140194451Abstract: Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit, the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.Type: ApplicationFiled: November 22, 2013Publication date: July 10, 2014Inventors: Qun Lu, Huchen Zhou, Yanhua Chen, Amy Friesland
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Publication number: 20140179681Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.Type: ApplicationFiled: January 8, 2014Publication date: June 26, 2014Inventor: Joseph P. Errico
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Publication number: 20140000807Abstract: Benzoylthiourea or benzoylthiourethane derivatives as cure accelerators in primers for two step adhesive systems are provided.Type: ApplicationFiled: March 5, 2013Publication date: January 2, 2014Applicants: Henkel Ireland Limited, Henkel CorporationInventors: David P. Birkett, Anthony F. Jacobine, Andrew D. Messana, Joel D. Schall, David Mullen, Martin Wyer, Lynnette Hurlburt, Jiangbo Ouyang, Smita Shah
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Patent number: 8501991Abstract: The present invention relates to compounds which activate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions (involving sirtuin function).Type: GrantFiled: September 4, 2007Date of Patent: August 6, 2013Assignees: University Court of the University of Dundee, University Court of the University of St. AndrewsInventors: Sonia Lain, David Phillip Lane, Michael John Raymond Stark, Anna Rose McCarthy, Jonathan James Hollick, Nicholas James Westwood
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Publication number: 20130195796Abstract: Compounds, pharmaceutical compositions and methods for treating viral and bacterial infections, by administering certain thiourea compounds, specifically acylthiourea, carboximidoylthiourea and S-alkyl isothiourea derivatives and analogs, in therapeutically effective amounts are disclosed.Type: ApplicationFiled: February 18, 2011Publication date: August 1, 2013Applicant: Siga Technologies Inc.Inventors: Robert D. Allen, Sean M. Amberg, Dongcheng Dai, Dennis E. Hruby
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Publication number: 20130096138Abstract: Disclosed are novel thiourea or urea derivatives inhibitory of HIV activity. Also provided are a method for preparing the thiourea or urea derivatives, and a pharmaceutical composition for the prophylaxis or therapy of AIDS comprising the derivatives. Having high inhibitory activity against HIV, the thiourea or urea derivatives can be effectively used in the prophylaxis or therapy of AIDS.Type: ApplicationFiled: June 17, 2011Publication date: April 18, 2013Applicant: AVIXGEN INC.Inventors: Ji Chang You, Gyoon Hee Han, Chul Ho Lee, Doo Na Song, Koo Hwan Chung
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Publication number: 20120264756Abstract: This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.Type: ApplicationFiled: August 17, 2010Publication date: October 18, 2012Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: David Cohen, Neil Wagle, Gregory D. Cuny, Jun Xian, Marcie Glicksman, Ross L. Stein, Ekaterina Y. Shishova
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Publication number: 20120149778Abstract: The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar? are as defined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases.Type: ApplicationFiled: June 9, 2010Publication date: June 14, 2012Inventors: Sonia Lain, Nicholas James Westwood, David Philip Lane
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Publication number: 20110275663Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 16, 2009Publication date: November 10, 2011Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
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Publication number: 20110251216Abstract: The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in cancer (e.g., prostate cancer, breast cancer, other solid tumors, multiple myeloma).Type: ApplicationFiled: February 10, 2011Publication date: October 13, 2011Applicant: The Regents of The University of MichiganInventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao
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Publication number: 20110021529Abstract: The present invention relates to compounds which activate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions (involving sirtuin function).Type: ApplicationFiled: September 4, 2007Publication date: January 27, 2011Applicants: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE, UNIVERSITY COURT OF THE UNIVERSITY OF ST. ANDREWSInventors: Sonia Lain, David Phillip Lane, Michael John Raymond Stark, Anna Rose McCarthy, Jonathan James Hollick, Nicholas James Westwood
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Patent number: 7816560Abstract: Long chain N-alkyl amino and imino compounds, oxa-substituted derivatives thereof, and pharmaceutical compositions including such compounds are described. The long chain N-alkyl group is a C8-C16 alkyl group. The long chain N-alkyl compounds and oxa-substituted derivatives thereof can be used in the treatment of viral infections, in particular hepatitis B virus or hepatitis C virus, in a cell or an individual. For example, the long chain N-alkyl compounds or oxa-substituted derivatives thereof can be derived from piperidines, pyrrolidines, phenylamines, pyridines, pyrroles, or amino acids.Type: GrantFiled: August 10, 2000Date of Patent: October 19, 2010Assignees: Thomas Jefferson University, The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics CorporationInventors: Nicole Zitzmann, Terry D. Butters, Frances M. Platt, Gary S. Jacob, Donald H. Picker, Sandra Carrouee, George W. J. Fleet, Raymond A. Dwek, David Durantel, Anand Mehta, Timothy M. Block
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Patent number: 7323496Abstract: Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory diseases, immunological diseases and cancer.Type: GrantFiled: May 7, 2003Date of Patent: January 29, 2008Assignee: Theracos, Inc.Inventors: Partha Neogi, Debedranath Dey, Joseph Fuller, Liang Chen, Ta-Kai Li
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Patent number: 7094807Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: GrantFiled: November 18, 2003Date of Patent: August 22, 2006Assignee: Achillion Pharmaceuticals, Inc.Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Patent number: 6818765Abstract: Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.Type: GrantFiled: October 16, 2001Date of Patent: November 16, 2004Assignee: Universite de LiegeInventors: Jacques Delarge, Jean-Michel Dogne, Bernard Masereel
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Publication number: 20040097593Abstract: Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory diseases, immunological diseases and cancer.Type: ApplicationFiled: May 7, 2003Publication date: May 20, 2004Inventors: Partha Neogi, Debedranath Dey, Joseph C. Fuller, Liang Chen, Ta-Kai Li
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Publication number: 20040087659Abstract: The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: July 11, 2003Publication date: May 6, 2004Inventors: Elisabeth Defossa, Dieter Kadereit, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Karl Schoenafinger
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Patent number: 6723751Abstract: The present invention relates to crystalline forms of the sodium salt of 5-chloro-2-methoxy-N-(2-(4-methoxy-3-methylaminothiocarbonylaminosulfonylphenyl)ethyl)benzamide, processes for their preparation, their use, and pharmaceutical preparations comprising them.Type: GrantFiled: April 14, 2000Date of Patent: April 20, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Heinrich Christian Englert, Uwe Gerlach, Harald Schneider, Tobias Metzenthin
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Patent number: 6511989Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which A, R(1), R(2), X, Y, and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.Type: GrantFiled: November 2, 2001Date of Patent: January 28, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert
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Patent number: 6506937Abstract: Benzenesulfonylureas and -thioureas of the formula I where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto)alk(oxy)yl, E is O or S; Y is —[CR(3)2]n—, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO3 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used an antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: November 29, 2001Date of Patent: January 14, 2003Inventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gögelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 6465444Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.Type: GrantFiled: March 21, 2001Date of Patent: October 15, 2002Assignees: Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd.Inventors: Christopher Bayly, Mitsuru Ohkubo
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Publication number: 20020077486Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 2, 2001Publication date: June 20, 2002Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-MaGuire
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Publication number: 20020058838Abstract: Benzenesulfonylureas and -thioureas of the formula I 1Type: ApplicationFiled: November 29, 2001Publication date: May 16, 2002Applicant: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 6232498Abstract: There are described processes for the preparation of a compound of formula I and novel intermediates in the preparative process.Type: GrantFiled: October 1, 1999Date of Patent: May 15, 2001Assignee: Astra Zeneca UK LimitedInventor: Christopher Goodwin
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Patent number: 5977177Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation and use of pharmaceutical preparations based on these compounds, and medicaments containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.Type: GrantFiled: June 4, 1998Date of Patent: November 2, 1999Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz Gogelein, Joachim Kaiser
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5880155Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation and use of pharmaceutical preparations based on these compounds, and medicaments containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.Type: GrantFiled: February 15, 1996Date of Patent: March 9, 1999Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz Gogelein, Joachim Kaiser
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Patent number: 5776980Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --?CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: November 7, 1996Date of Patent: July 7, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 5747646Abstract: The present invention is a physiologically active, substantially non-immunogenic water soluble polyethylene glycol protein conjugate having the same utility as the protein which forms the conjugate, without having the same properties of producing an immunogenic response possessed by the protein which forms this conjugate.Type: GrantFiled: June 1, 1995Date of Patent: May 5, 1998Assignee: Hoffmann-La Roche Inc.Inventors: John Hakimi, Patricia Kilian, Perry Rosen
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Patent number: 5723075Abstract: A near-infrared absorbent is obtained by heating a dimerized thiourea derivative of Formula ?1! or ?2! and a copper compound: ##STR1## The near-infrared absorbent is used to obtain a near-infrared absorbent resin material having a wide absorption in the near-infrared region, and the absorbent does not substantially decompose at a molding temperature of the resin. Typical examples of the dimerized thiourea derivative are 4,4'-di(benzylthiocarbamoyl)-aminodiphenylmethane, 4,4'-di(benzylthiocarbamoyl)-aminodiphenylhexafluoropropane, and 1,4'-di(dibenzoylthiocarbamoylamino)-2,5-dimethylbenzene, and typical examples of the copper compound are copper stearate and copper .beta.-acryloyloxypropylhydrogenphthalate.Type: GrantFiled: April 19, 1996Date of Patent: March 3, 1998Assignee: Nippon Paper Industries Co., Ltd.Inventors: Hideki Hayasaka, Toshiyuki Takano, Toshimi Satake
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Patent number: 5702850Abstract: A thermosensitive reversible color-developing and disappearing agent includes an aromatic compound having at least one group of the formula, --SO.sub.2 NHCXNH--, wherein X.dbd.O or S atom, and at least one straight chain alkyl group with 11 or more carbon atoms, and is reactive with a dye precursor in a thermosensitive recording material to thereby record colored images on the recording material upon heating imagewise, and make the colored images disappear upon heating to a temperature lower than the colored image-forming temperature.Type: GrantFiled: September 13, 1995Date of Patent: December 30, 1997Assignee: New Oji Paper Co., Ltd.Inventors: Makoto Nishioka, Kazuo Yamane, Masaki Nishimura, Yoshiyuki Takahashi
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Patent number: 5698596Abstract: Substituted benzenesulfonylureas and -thioureas--processes for their preparation and their use as pharmaceuticalsBenzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --?CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: September 3, 1996Date of Patent: December 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 5652268Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation, their use as a medicament or diagnostic, and medicament containing them.Substituted benzenesulfonylureas and -thioureas 1 ##STR1## exhibit effects on the cardiovascular system.Type: GrantFiled: February 15, 1996Date of Patent: July 29, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz Gogelein, Joachim Kaiser
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Patent number: 5633239Abstract: Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit outstanding effects on the cardiovascular system.Type: GrantFiled: February 16, 1996Date of Patent: May 27, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz G ogelein, Joachim Kaiser
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Patent number: 5607976Abstract: Substituted benzenesulfonylureas and -thioureas, processes for their preparation, their use for the production of pharmaceutical preparations, and pharmaceutical preparations containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.Type: GrantFiled: February 8, 1996Date of Patent: March 4, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Uwe Gerlach, Peter Crause, Dieter Mania, Heinz G ogelein, Joachim Kaiser
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Patent number: 5585468Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, substantial thioureas for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.Type: GrantFiled: June 27, 1994Date of Patent: December 17, 1996Assignee: Cytogen CorporationInventors: Daniel J. Coughlin, Benjamin A. Belinka, Jr.
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Patent number: 5574054Abstract: Novel quaternary ammonium salts having utility in the medical field for treating gastrointestinal disorders.Type: GrantFiled: January 12, 1995Date of Patent: November 12, 1996Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Osamu Kitagawa, Katsuyuki Ishii, Seiichi Niwa, Sigeru Ueki, Masao Seiki
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Patent number: 5574069Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto) alk (oxy) yl, E is O or S; Y is --[CR(3).sub.2 ]n-, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: February 23, 1995Date of Patent: November 12, 1996Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
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Patent number: 5476850Abstract: There are described amino-substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## The compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for those cases in which arrhythmias are a result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.Type: GrantFiled: December 5, 1994Date of Patent: December 19, 1995Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser
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Patent number: 5449761Abstract: This invention relates to the preparation and use of novel open-chain or cyclic polypeptide constructs in which two or more polypeptide chains, in an open-chain construct, or one or more chains, in a cyclic construct, are chemically derivatized such that the resulting construct exhibits both metal-binding capability and tissue-, organ- or cell-targeting selectivity. In particular, the polypeptide constructs of the present invention comprise compounds of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone, "P" is a polypeptide capable of targeting particular cells, tissues or organs of the body, "A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group, R, R' and R" may be the same or different and may be hydrogen or an aliphatic group, m is an integer .gtoreq.2, provided that the groups R, R', R', L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain, n is an integer .gtoreq.Type: GrantFiled: September 28, 1993Date of Patent: September 12, 1995Assignee: Cytogen CorporationInventors: Benjamin A. Belinka, Jr., Daniel J. Coughlin, Vernon L. Alvarez, Richard Wood
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Patent number: 5370947Abstract: A reversible electrode of the present invention includes, as a main component thereof, a thiourea compound represented by the following formula (I): ##STR1## (where R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, a hydroxyl group, a cyano group, a carboxyl group, an amino group, an aryl group, an allyl group, an alkyl group, an alkoxy group, a group containing a mercapto group, a group containing a phenyl group, a group having a hetero ring containing O, and a group having a hetero ring containing N) or a polymer having the thiourea compound as its main polymer unit; the reversible electrode utilizing reversible electrochemical oxidation-reduction of sulfur atoms of the thiourea compound or the polymer.Type: GrantFiled: April 30, 1993Date of Patent: December 6, 1994Assignee: Matsushita Electric Industrial Co., Ltd.Inventors: Hiroshi Uemachi, Yoshiko Sato, Tadashi Sotomura, Kenichi Takeyama
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Patent number: 5326856Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, isothiocyanate derived thiocarbonyls for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.Type: GrantFiled: April 9, 1992Date of Patent: July 5, 1994Assignee: Cytogen CorporationInventors: Daniel J. Coughlin, Benjamin A. Belinka, Jr.
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Patent number: 5288758Abstract: New urea derivatives corresponding to the general formula 1 ##STR1## in which: R.sup.1 represents a C.sub.1 -C.sub.4 alkyl group;R.sup.2 represents:a C.sub.5 -C.sub.7 cycloalkyl groupa cycloalkylmethyl group in which the cycloalkyl radical contains from 5 to 7 carbon atomsa benzyl groupa benzyl group in which the aromatic ring bears a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a halogen atom or a nitro group;A represents an oxygen atom or a methylene radical;n represents 1 or 2;X represents an oxygen or sulfur atom;B represents a direct bond, a methylene radical or a carbonyl radical;as well as the therapeutically acceptable salts of these molecules.The invention also relates to the application of the compounds of general formula 1 in therapy, and to the preparation processes.Type: GrantFiled: July 22, 1992Date of Patent: February 22, 1994Assignee: Pierre Fabre MedicamentInventors: Jean-Louis Vidaluc, Dennis Bigg
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Patent number: 5245071Abstract: Compounds of the formula ##STR1## wherein A is a hydrogen atom, a halogen atom, a methyl group, or a methoxy group;B is a hydrogen atom, a halogen atom, a methyl group, or a methoxy group, with the proviso that A and B ar not both a hydrogen atom;X and Y each are an oxygen atom or a sulfur atom;R is a hydrogen atom, an alkyl group, a hydroxy group, an alkoxy group, an alkoxymethyl group, an acyl group, or an alkoxycarbonyl group;R.sub.1 is a hydrogen atom, an alkyl group, a halogen substituted alkyl group, an alkoxy substituted alkyl group, an alkylthio substituted alkyl group, a cyano substituted alkyl group, a 1-cycloalkenyl group, a benzyl group, a halogen substituted benzyl group, a hydroxy group, an alkoxy group, an acyl group, an alkoxycarbonyl group, an alkoxythiocarbonyl group, an alkylsulfonyl group, or a phenylsulfonyl group, while furthermore R and R.sub.1 together with the group ##STR2## indicated in the above formula may form a ring system; and R.sub.Type: GrantFiled: June 3, 1992Date of Patent: September 14, 1993Assignee: Duphar International Research B.V.Inventors: Kobus Wellinga, Rudolf Mulder
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Patent number: 5190961Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.Type: GrantFiled: August 2, 1991Date of Patent: March 2, 1993Assignee: Terumo Kabushiki KaishaInventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
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Patent number: 5155135Abstract: This invention provides benzamide compounds of general formula ##STR1## wherein each of A and B independently represents a hydrogen or halogen atom, X represents an oxygen or a sulphur atom, n is 0, 1, 2, 3 or 4, each Z moiety independently represents a halogen atom or a C.sub.1-6 alkyl group, and Y represents a C.sub.1-6 haloalkyl group, a C.sub.1-6 haloalkoxy group, a group of formula ##STR2## wherein P is 0, 1 or 2, each Z' moiety independently represents a halogen atom or a C.sub.1-6 alkyl group, Y' represents a C.sub.1-6 haloalkyl, C.sub.1-6 haloalkoxy, nitro or cyano group and Q represents N or C-H, or, when n is 2 or 3, Y may also be a halogen atom; processes for their preparation; and their use as pesticides.Type: GrantFiled: December 6, 1989Date of Patent: October 13, 1992Assignee: Shell Internationale Research Maatschappij, B.V.Inventors: Martin Anderson, Antony G. Brinnand, Pieter A. Verbrugge
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Patent number: 5142064Abstract: Compounds of the formula ##STR1## wherein A is a hydrogen atom, a halogen atom, a methyl group, or a methoxy group;B is a hydrogen atom, a halogen atom, a methyl group, or a methoxy group, with the proviso that A and B ar not both a hydrogen atom;X and Y each are an oxygen atom or a sulfur atom;R is a hydrogen atom, an alkyl group, a hydroxy group, an alkoxy group, an alkoxymethyl group, an acyl group, or an alkoxycarbonyl group;R.sub.1 is a hydrogen atom, an alkyl group, a halogen substituted alkyl group, an alkoxy substituted alkyl group, an alkylthio substituted alkyl group, a cyano substituted alkyl group, a 1-cycloalkenyl group, a benzyl group, a halogen substituted benzyl group, a hydroxy group, an alkoxy group, an acyl group, an alkoxycarbonyl group, an alkoxythiocarbonyl group, an alkylsulfonyl group, or a phenylsulfonyl group, while furthermore R and R.sub.1 together with the group ##STR2## indicated in the above formula may form a ring system; and R.sub.Type: GrantFiled: July 7, 1986Date of Patent: August 25, 1992Assignee: Duphar International Research B.V.Inventors: Kobus Wellinga, Rudolf Mulder
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Patent number: 5116875Abstract: A novel benzxoylurea derivative represented by the formula (I) described below, its production and an insecticidal and/or acaricidal composition containing it as an active ingredient: ##STR1## wherein R.sub.1 is a chlorine or fluorine atom, each of R.sub.2 and R.sub.3, wherein may be the same or different, is a fluorine or hydrogen atom, R.sub.4 is a chlorine or hydrogen atom, R.sub.5 is a halogen atom or a methyl or trifluoromethyl group, and X is an oxygen or sulfur atom.Type: GrantFiled: July 25, 1990Date of Patent: May 26, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Tatsuya Mori, Tadashi Ohsumi, Hiroaki Fujimoto, Izumi Fujimoto