Benzene Ring Containing Patents (Class 564/228)
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Patent number: 11001554Abstract: Methods for removing an oxyanion from an aqueous source containing said oxyanion, comprising contacting said aqueous source with an aqueous-insoluble hydrophobic solution containing an oxyanion extractant compound dissolved in an aqueous-insoluble hydrophobic solvent to result in formation of an oxyanion salt of said extractant compound and extraction of said oxyanion salt into said aqueous-insoluble hydrophobic solution, wherein said extraction results in an extraction affinity (D) of said oxyanion of at least 1, wherein D is the concentration ratio of said oxyanion in the organic phase divided by the concentration of said oxyanion in the aqueous phase; wherein said extractant compound has the following composition: wherein at least one of R1-R10 is or contains a hydrocarbon (R) group containing at least 4, 5, 6, 7, 8, 9, 10, 11, or 12 carbon atoms.Type: GrantFiled: March 29, 2019Date of Patent: May 11, 2021Assignee: UT-Battelle, LLCInventors: Neil J. Williams, Radu Custelcean, Charles A. Seipp, Bruce A. Moyer, Ross Ellis, Carter W. Abney
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Patent number: 8497306Abstract: The invention relates to pharmaceutically acceptable salts of guanylhydrazone-containing compounds, for example, Semapimod. The invention also relates to pharmaceutically acceptable compositions comprising the salts and methods for their use.Type: GrantFiled: October 31, 2007Date of Patent: July 30, 2013Assignee: Ferring B.V.Inventor: Thais M. Sielecki-Dzurdz
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Publication number: 20110251428Abstract: The invention relates to chlorine Guanabenz derivatives for treating prion-based diseases. More specifically, it relates to the use of the molecule of formula (I) wherein R?H or Cl and the phenyl group is at least substituted twice, or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for treating prion-based diseases.Type: ApplicationFiled: October 3, 2007Publication date: October 13, 2011Inventors: Marc Blondel, Stéphane Bach, Didier Vilette, Vincent Beringue, Déborah Tribouillard
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Patent number: 7932422Abstract: The invention relates to chlorine Guanabenz derivatives for treating Huntington's disease and other polyglutamine expansion associated diseases. More specifically, it relates to the use of the molecule of formula (I) wherein R?H or Cl and the phenyl group is at least substituted twice, or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for treating polyglutamine expansion associated diseases.Type: GrantFiled: October 3, 2007Date of Patent: April 26, 2011Inventors: Anne Bertolotti, Marc Blondel
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Publication number: 20110015437Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: ACURE PHARMA ABInventors: Torbjörn Lundstedt, Anna Skottner, Elisabeth Seifert
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Publication number: 20100130495Abstract: The present invention relates to novel compounds of formula I and therapeutically acceptable salts thereof, their pharmaceutical compositions, processes for making them and their use as therapeutic methods for treatment and/or prevention of various diseases.Type: ApplicationFiled: November 6, 2009Publication date: May 27, 2010Applicant: ASTRAZENECA ABInventors: Rickard FORSBLOM, Kim PAULSEN, Didier ROTTICCI, Ellen SANTANGELO, Magnus WALDMAN
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Publication number: 20100036166Abstract: The invention relates to chlorine Guanabenz derivatives for treating Huntington's disease and other polyglutamine expansion associated diseases. More specifically, it relates to the use of the molecule of formula (I) wherein R?H or Cl and the phenyl group is at least substituted twice, or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for treating polyglutamine expansion associated diseases.Type: ApplicationFiled: October 3, 2007Publication date: February 11, 2010Inventors: Anne Bertolotti, Marc Blondel
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Publication number: 20100029773Abstract: The present invention relates to a method of identifying a compound for inhibiting aggregation of proteins involved in diseases linked to protein aggregation and/or neurodegenerative diseases, comprising the steps of: (a) bringing into contact a labeled monomeric protein and a differently labeled aggregate of said protein in the (1) presence and (2) absence of a candidate inhibitor of aggregation, (b) determining the amount of co-localized labels, representing the extent of binding of the monomeric proteins to the aggregates of said protein; and (c) comparing the result obtained in the presence and absence of said compound, wherein a decrease of co-localized labels in the presence of said compound is indicative of the compound's ability to inhibit aggregation of said protein. Moreover, the present invention relates to a pharmaceutical composition containing said inhibitor of aggregation as well as to a kit.Type: ApplicationFiled: May 24, 2005Publication date: February 4, 2010Applicants: LUDWIG-MAXIMILIANS-UNIVERSITAT MUNCHEN, MAX-PLANCK-GESELLSCHAFT FUR FORDERUNG DER WISSENSCHAFTEN E.V.Inventors: Uwe Bertsch, Armin Giese, Hans Kretzschmar, Paul Tavan, Thomas Hirschberger, Jan Bieschke, Petra Weber, Konstanze F. Winklhofer, Jörg Tatzelt, Ulrich F. Hartl, Gerda Mitterregger-Kretzschmar, Tobias Johannes Högen
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Publication number: 20040068017Abstract: Small organic molecules capable of effecting a “pharmacological trabeculocanalotomy” in an eye by means of reducing juxtacanalicular meshwork as a barrier to outflow of aqueous. The small organic molecules increase Gelatinase A activity in ocular cells by increasing cell membrane expression of membrane-type matrix metalloproteinases (MT-MMPs) to increase aqueous outflow as a treatment for primary open angle glaucoma.Type: ApplicationFiled: September 27, 2002Publication date: April 8, 2004Inventors: Bruce Alan Pfeffer, Rosemarie Beth Flick, Naveed Bin Kamal Shams, Stephen Paul Bartels
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Publication number: 20020123649Abstract: The invention relates to a novel method for producing robenidine and salts thereof of the general formula 1Type: ApplicationFiled: July 6, 2001Publication date: September 5, 2002Inventors: Paul Hanselmann, Stefan Hildbrand
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Publication number: 20010056123Abstract: Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.Type: ApplicationFiled: December 8, 2000Publication date: December 27, 2001Applicant: AJINOMOTO CO., INCInventors: Tadakiyo Nakagawa, Kazuyuki Sagi, Kaoru Yoshida, Yumiko Fukuda, Masataka Shoji, Shunji Takehana, Takashi Kayahara, Akira Takahara
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Patent number: 6180676Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: January 30, 2001Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6136987Abstract: This invention relates to the use of arylguanidinium xanthogenates as vulcanization accelerators, to a process for the production thereof and to the arylguanidinium xanthogenates.Type: GrantFiled: October 25, 1999Date of Patent: October 24, 2000Assignee: Rhein Chemie Rheinau GmbHInventors: Thomas Fruh, Ludger Heiliger, Hermann Lohwasser
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Patent number: 5891909Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 27, 1997Date of Patent: April 6, 1999Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Bruce E. Tomczuk, Carl Illig
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Patent number: 5837737Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 7, 1995Date of Patent: November 17, 1998Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
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Patent number: 5753684Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: May 19, 1998Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5744641Abstract: 4-Sulfonyl- or 4-sulfinylbenzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.6 and n have the meanings indicated, and their physiologically acceptable salts exhibit antiarrhythmic properties and, act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: August 9, 1996Date of Patent: April 28, 1998Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rolf Gericke, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
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Patent number: 5698563Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises bis(guanylhydrazone) of the formula ##STR1## capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: January 13, 1995Date of Patent: December 16, 1997Assignee: Alteon Inc.Inventors: Dilip R. Wagle, Michael E. Lankin, David H. Shih
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Patent number: 5646188Abstract: A compound of general formula I ##STR1## wherein n is 1 or 2; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy or halogeno;R.sub.5 is hydrogen, substituted or unsubstituted C.sub.1-4 alkyl, amino or NR.sub.6 R.sub.7 ;R.sub.3, R.sub.4, R.sub.6 and R.sub.7 are each independently hydrogen or (CH.sub.2).sub.m --[NH(CH.sub.2).sub.x ].sub.y --NHR.sub.11 wherein m is from 0-5, y is from 0-5 and each x is independently from 1-5 and R.sub.11 is hydrogen or C(NH)NH.sub.2 ;provided that when R.sub.3 and R.sub.4 are both hydrogen, R.sub.5 is amino or NR.sub.6 R.sub.7 ; pharmaceutically acceptable salts and optically active isomers thereof.Type: GrantFiled: July 5, 1995Date of Patent: July 8, 1997Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Gad Gilad, Varda Gilad, Jeffrey Sterling, Yaacov Herzig, David Lerner, Alex Veinberg, Isaac Milman, Nina Finkelstein
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Patent number: 5639911Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.Type: GrantFiled: June 7, 1995Date of Patent: June 17, 1997Assignee: Ciba-Geigy CorporationInventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
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Patent number: 5599984Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: September 29, 1994Date of Patent: February 4, 1997Assignee: The Picower Institute For Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5494934Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Medicine products.Type: GrantFiled: November 4, 1991Date of Patent: February 27, 1996Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Guillaume de Nanteuil
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Patent number: 5461076Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: November 30, 1994Date of Patent: October 24, 1995Inventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
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Patent number: 5403955Abstract: Novel mordants based upon a polyethyleneimine backbone and either pendant phosphonium or quaternized-nitrogen compounds are disclosed. The mordants find use in stopping or controlling ink-bleeding into ink-jet receptors and photographic films.Type: GrantFiled: April 28, 1994Date of Patent: April 4, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventor: Omar Farooq
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Patent number: 5395855Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: March 28, 1994Date of Patent: March 7, 1995Assignee: Ciba-Geigy CorporationInventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
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Patent number: 5296498Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: January 19, 1993Date of Patent: March 22, 1994Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Guillaume de Nanteuil
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Patent number: 5118709Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.Type: GrantFiled: August 29, 1990Date of Patent: June 2, 1992Assignee: Ciba-Geigy CorporationInventors: Erfinders J. Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
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Patent number: 4870210Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## R is hydrogen, lower alkyl, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di- lower alkylamino, nitro, hydroxy, carboxy, lower alkoxycarbonyl, lower alkoxy or halo;R.sup.2 is hydrogen or lower alkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other inflammatory conditions.Type: GrantFiled: December 18, 1987Date of Patent: September 26, 1989Assignee: American Home Products CorporationInventor: John H. Musser
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Patent number: 4731383Abstract: The invention relates to new aminoguanidine derivatives of the general formula (I), ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each represent hydrogen or halogen atom, C.sub.1-4 alkyl, nitro, trifluoromethyl or C.sub.1-4 alkoxy group,R.sup.4 and R.sup.5 represent a C.sub.1-4 alkyl group, furthermore NR.sup.4 R.sup.5 may form a 5 to 7 membered saturated heterocyclic group containing either one or two nitrogen atoms or a nitrogen and an oxygen atom and being optionally substituted by one or two methyl, hydroxymethyl or hydroxyethyl groups,R.sup.6 and R.sup.7 each represent a hydrogen atom, normal or branched C.sub.1-4 alkyl or C.sub.2-4 alkenyl group,and to their pharmaceutically acceptable acid addition salts as well as to a process for the preparation thereof.The new compounds of the invention possess valuable antiarrhythmic activity and are devoid of the undesired circulatory side effects of the known antiarrhythmic compounds.Type: GrantFiled: October 29, 1986Date of Patent: March 15, 1988Assignee: Biogal GyogyszergyarInventors: Istvan Erczi, Jeno Marosfalvi, Gyorgy Rabloczky, Andras Varro, Maria Kuhar nee Kurthy, Istvan Elekes, Laszlo Szatmary, Laszlo Jaszlits
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Patent number: 4705782Abstract: The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2, CF.sub.3 or the group --NR.sub.5 R.sub.6,whereby two substituents taken together may also represent a methylene-dioxy group,X represents a member selected from ##STR2## --CH.sub.2 --CH.sub.2 -- and --CH.dbd.CH--, n has the value 0, 1 or 2,R.sub.3 represents one of the moieties: ##STR3## and R.sub.2, R.sub.4, R.sub.5 and R.sub.6 represent hydrogen or alkyl(1-6 C),and pharmaceutically acceptable salts thereof, suitable in the treatment of heartfailure.Type: GrantFiled: March 26, 1986Date of Patent: November 10, 1987Assignee: Akzo N.V.Inventors: Robert T. Logan, James Redpath, Robert G. Roy
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Patent number: 4665085Abstract: Compounds having the formula (I) wherein R.sub.1 and R.sub.2 are a hydrogen atom, an alkyl group or a hydroxy group, or else R.sub.1 and R.sub.2 form together a bivalent ethylene or trimethylene radical; R.sub.3 is a halogen atom, an alkyl group, an alkoxy group, a mono- or polyhydroxylated alkyl group, an amino group, a mono- or di-alkyl amino group, an acetamido or sulfonamido group; R.sub.1 is a hydroxy group, a mono- or polyhydroxylated alkyl group, an amino group, a mono- or dialkyl amino group, an acetamido or sulfonamido group; R.sub.4 being in the position 3, 4 or 5 and A is a bridge having from 1 to 3 links selected among the groups having the formula (II), --NH--,--N.dbd.--O-- and --S--. R.sub.5 represents an hydrogen atom, an alkyl group, a hydroxy group or an alkoxy group as well as the addition salts thereof with pharmaceutically acceptable acids. Said compound may be used in therapeutical treatment as antihypertensive agents, particularly in the ocular field.Type: GrantFiled: March 12, 1985Date of Patent: May 12, 1987Assignee: Laboratoires Chauvin-BlacheInventors: Claude Coquelet, Elisabeth Battais, Claude Bonne, Daniel Sincholle
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Patent number: 4575560Abstract: The invention is insecticidal diaminoguanidine hydrazone compounds which are also effective antifeeding agents for insects and methods for their preparation.Type: GrantFiled: February 25, 1985Date of Patent: March 11, 1986Assignee: American Cyanamid CompanyInventors: Roger W. Addor, Donald P. Wright, Jr., Jack K. Siddens, John J. Hand
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Patent number: 4474806Abstract: Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.Type: GrantFiled: May 10, 1982Date of Patent: October 2, 1984Assignee: Merck & Co., Inc.Inventors: Thomas R. Beattie, Shu S. Yang
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Patent number: 4331680Abstract: Novel compounds are described which are substituted benzophenone hydrazones. They have pesticidal activity, especially against insects and acarids, and pesticidal compositions and methods are described. Methods of making the compounds, and novel intermediates, are also described.Type: GrantFiled: August 25, 1980Date of Patent: May 25, 1982Assignee: The Boots CompanyInventors: David P. Giles, John C. Kerry, Antonin Kozlik, Bryan H. Palmer, Stephen W. Shutler, Robert J. Willis
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Patent number: 4258181Abstract: This disclosure describes anthracene-9,10-bis-carbonyl-hydrazones and derivatives thereof useful as antibacterial agents, for inhibiting the growth of transplanted mouse tumors, and for inducing the regression and/or palliation of leukemia and related cancers.Type: GrantFiled: May 7, 1979Date of Patent: March 24, 1981Assignee: American Cyanamid CompanyInventors: Keith C. Murdock, Frederick E. Durr