Acyclic Ethylenic Or Acetylenic Unsaturation Containing Patents (Class 544/306)
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Patent number: 8900785Abstract: A charge control agent comprises a barbituric acid derivative represented by the following general formula (1): wherein R1 to R8 are alkyl groups, cycloalkyl groups or aryl groups, V, W, X, Y and Z are carbon atoms or nitrogen atoms, at least two of which being carbon atoms, and p, q, r, s and t are the numbers of 0 or 1.Type: GrantFiled: September 2, 2011Date of Patent: December 2, 2014Assignee: Hodogaya Chemical Co., Ltd.Inventors: Ikuo Kimura, Masami Ito, Masaya Tojou, Kanae Hiraishi, Masafumi Asakai
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Publication number: 20130157190Abstract: [Problems] To provide a charge control agent which contains no heavy metal component, therefore, does not adversely affect the environment and, besides, is colorless or is light-colored lending itself well to be applied to colored toners, and is little affected by the environmental conditions, and exhibits the effect of imparting high charging power even when it is used for polymerized toners. [Means for Solution] The charge control agent comprises a barbituric acid derivative represented by the following general formula (1): wherein R1 to R8 are alkyl groups, cycloalkyl groups or aryl groups, V, W, X, Y and Z are carbon atoms or nitrogen atoms, at least two of which being carbon atoms, and p, q, r, s and t are the numbers of 0 or 1.Type: ApplicationFiled: September 2, 2011Publication date: June 20, 2013Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Ikuo Kimura, Masami Ito, Masaya Tojou, Kanae Hiraishi, Masafumi Asakai
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Publication number: 20130078256Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: November 20, 2012Publication date: March 28, 2013Applicant: Korea Research Institute of Chemical TechnologyInventor: Korea Research Institute of Chemical Technology
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Patent number: 8314091Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.Type: GrantFiled: August 19, 2008Date of Patent: November 20, 2012Assignees: MSD OSS B.V., Pharmacopeia, Inc.Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
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Publication number: 20120046309Abstract: The present invention relates to the identification of inventive pyrimidine-2,4,6-triones (PYT compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the inventive PYT compounds.Type: ApplicationFiled: May 5, 2010Publication date: February 23, 2012Applicants: NORTHWESTERN UNIVERSITY, CAMBRIA PHARMACEUTICALS, INC.Inventors: Donald R. Kirsch, Radhia Benmohamed, Anthony C. Arvanites, Richard I. Morimoto, Richard B. Silverman, Guoyao Xia
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Patent number: 7119201Abstract: The present invention relates to triaryl-oxy-aryloxy-pyrimidine-2,4,6-trione; metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, W, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 28, 2003Date of Patent: October 10, 2006Assignee: Pfizer IncInventors: Lawrence Alan Reiter, Kevin Daniel Freeman-Cook
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Patent number: 6759101Abstract: Compounds that are useful as components in liquid crystal compositions, particularly in ferroelectric liquid crystal compositions. Compounds of the invention are rod-like molecules with a mesogenic (generally linear) core to which an alkene tail and an alkyl or alkoxy tail with a perfluoroalkyl terminal portion are bonded. Compounds of the invention can contain a variety of one, two or three ring cores, wherein the rings maybe aromatic or alicyclic. Alkenes of the invention are useful as components to improve LC properties of mixtures, for example, to lower melting point of lower freezing point, of LC compositions.Type: GrantFiled: January 3, 2001Date of Patent: July 6, 2004Assignee: Displaytech, Inc.Inventors: Neil Gough, Rohini Vohra, Michael Wand, Kundalika More, William N. Thurmes
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Patent number: 6706723Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, A, B and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: October 25, 2001Date of Patent: March 16, 2004Assignee: Pfizer, Inc.Inventors: Mark C. Noe, Lawrence A. Reiter, Martin J. Wythes
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Patent number: 6573269Abstract: The present invention provides compounds of formula I, which are effective in absorbing ultraviolet radiation and can be used as sunscreen agents: wherein R1 and R2 are each independently C2-C18 alkyl, C5-C7 cycloalkyl, or C2-C18 alkyl in which at least one methylene group is replaced by oxygen; R3 is hydrogen, C1-C18 alkyl, C2-C18 alkyl in which at least one methylene group is replaced by oxygen, C1-C18 alkyl carbonyl, C3-C18 alkenyl, C3-C18 alkynyl, or a group YS; R4 is hydrogen, C1-C8 alkyl or a group OR3; Y is a linker group; and S is a silane-, an oligosiloxane- or a polysiloxane-moiety.Type: GrantFiled: September 1, 2000Date of Patent: June 3, 2003Assignee: Roche Vitamins Inc.Inventor: Ulrich Huber
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Patent number: 6562542Abstract: An image-forming material is described, comprising on an support an acid-generating agent selected from a sulfonic acid ester of a specific structure generating an acid by the action of heat and the polymer thereof, and a compound causing a light absorption change in the absorption region of from 350 to 700 nm by an intramolecular or intermolecular reaction by the action of an acid. The image-forming material has a high sensitivity and excellent storage stability and gives low haze and good images in the case of performing image formation using a high-output laser light.Type: GrantFiled: March 28, 2001Date of Patent: May 13, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Atsuhiro Ohkawa, Seiya Sakurai
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Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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Patent number: 6121303Abstract: A compound of formula I ##STR1## wherein R.sub.1 is nitro, halogeno or cyano group and R.sub.2 is a group selected from ##STR2## wherein Y and Z are independently oxygen, sulfur or NR, wherein R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group and X.sub.1 and X.sub.2 are NR, where R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group, or a pharmaceutically acceptable salt or ester thereof. Pharmaceutical compositions are also disclosed.Type: GrantFiled: February 23, 1999Date of Patent: September 19, 2000Assignee: Orion-yhtyma OyInventors: Reijo Backstrom, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
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Patent number: 5747500Abstract: Novel 2,4-pyrimidinedione compounds, and pharmaceutically acceptable salts thereof which possess good antiviral activities, and specifically represented by the following formula(I): ##STR1## wherein: R.sup.1 represents an unsubstituted or substituted allyl group represented by CH.sub.2 CH.dbd.CR.sup.5 R.sup.6 or an unsubstituted or substituted propargyl group represented by CH.sub.2 C.tbd.CR.sup.7 wherein R.sup.5, R.sup.6 and R.sup.7 are each independently a hydrogen atom; a methyl group optionally substituted with a halogen atom, or a C.sub.1-10 carbonyloxy, hydroxy, azido, cyano, optionally substituted amino, optionally substituted phosphonyl, optionally substituted phenyl, C.sub.3-10 heteroaryl, C.sub.1-3 alkoxy or benzyloxy radical; a C.sub.2-10 alkyl or alkenyl group; a cyclopropyl group; an optionally substituted phenyl group; a C.sub.3-10 heteroaryl group; a C.sub.1-10 ester group; or an optionally substituted C.sub.1-10 alkylamide group;R.sup.2 represents a halogen atom, an optionally substituted C.Type: GrantFiled: June 18, 1996Date of Patent: May 5, 1998Assignee: Korea Research Institute of Chemical TechnologyInventors: Jong-Chan Son, III-Young Lee, Byung-II Bae, Jeong-Sik Han, Joong-Kwon Choi, Yung-Bok Chae
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Patent number: 5736563Abstract: A method destroys or impairs target cells that have selectively accumulated a photosensitizing agent. The target cells are in the bloodstream of an intact animal, which bloodstream and animal further contain non-target cells. Radiation is applied transcutaneously to at least a portion of the intact animal at an intensity effective to impair or destroy selectively the target cells and to leave non-target cells relatively unimpaired. Target cells include leukemia cells, virus-containing cells, parasite-containing cells, and microorganisms such as bacteria, parasites and free viruses.Type: GrantFiled: November 8, 1995Date of Patent: April 7, 1998Assignee: Quadra Logic Technologies, Inc.Inventor: Anna M. Richter
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Patent number: 5707995Abstract: Compounds of formula (I) in which X.sup.1 and X.sup.2 each represents oxygen; S(O).sub.n, n being 0, 1 or 2; or CO, CH.sub.2 or NR, R being hydrogen or alkyl; R.sup.1 and R.sup.10 are each hydrogen or halogen; R.sup.2 and R.sup.9 are each hydrogen, halogen, cyano, nitro, alkyl, halo-alkyl, alkoxy, alkylthio, amino, mono- or di-alkylamino, alkoxyalkyl, haloalkoxyalkyl or alkoxycarbonyl; R.sup.3 and R.sup.8 are each hydrogen, chlorine, alkyl, haloalkyl, haloalkenyl, halo-alkynyl, haloalkoxy, haloalkoxycarbenyl, haloalkylthio, haloalkoxyalkyl, haloalkylsulphinyl, or haloalkylsulphonyl, nitro or cyano; R.sup.4 and R.sup.7 are each hydrogen, halogen, alkyl or alkoxy; R.sup.5 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulphonyl or phenyl; and R.sup.6 is hydrogen or, when R.sup.5 is hydrogen, alkyl; provided that either each phenyl is unsubstituted or at least one of R.sup.3 and R.sup.8 is not hydrogen, have useful pesticidal activity.Type: GrantFiled: July 24, 1995Date of Patent: January 13, 1998Assignee: American Cyanamid CompanyInventors: David Munro, Royston Davis, Janet Anne Day, Jacqueline Anne Wilkin, William W. Wood
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Patent number: 5614541Abstract: New catechol derivatives and pharmaceutically acceptable salts and esters thereof useful as pharmaceutical antioxidants are disclosed. Cellular damage by oxygen derived radicals is a significant factor in heart disease, rheumatoid arthritis, cancer, inflammatory disease, transplant rejection reactions and ischemia.Type: GrantFiled: October 18, 1994Date of Patent: March 25, 1997Assignee: Orion-yhtym a OyInventors: Reijo B ackstr om, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
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Patent number: 5466813Abstract: Imine dyes useful in photographic materials have the formula ##STR1## wherein R.sup.1, E.sup.1, E.sup.2, L.sup.1, L.sup.2, L.sup.3,D and m are defined as in the specification.Solid particle dispersions of dyes of formula (I) that contain at least one base-ionizable functional group such as carboxy, sulfonamido, or sulfamoyl are useful as filter dyes in photographic elements.Type: GrantFiled: July 20, 1993Date of Patent: November 14, 1995Assignee: Eastman Kodak CompanyInventors: Donald R. Diehl, Margaret J. Helber, Hugh Williamson
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Patent number: 5459265Abstract: There is disclosed a silver halide photographic light-sensitive material having a hydrophilic colloid layer containing a dye which is photochemically inactive and can readily be decolored and/or eluted in a photographic processing course. The silver halide photographic light-sensitive material comprises a hydrophilic colloid layer containing at least one dye dispersed in the form of a solid fine particle represented by Formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2, L.sub.1, L.sub.2, L.sub.3 are defined in the disclosure.In a preferred embodiment, the maximum absorption wavelength .lambda.max of the dye in the hydrophilic colloid layer satisfies the following equation:.lambda.max>[.lambda.max(DMF)+20.times.(n+1)] nmwherein .lambda.max(DMF) and n are defined in the disclosure. There is also disclosed an oxonol compound which is useful as a dye.Type: GrantFiled: March 23, 1994Date of Patent: October 17, 1995Assignee: Fuji Photo Film Co., Ltd.Inventors: Koji Wariishi, Keiichi Suzuki
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Patent number: 5371062Abstract: The present invention relates to new substituted azines, of the general formula (I) ##STR1## in which n, Q.sup.1, Q.sup.2, Q.sup.3, R.sup.1, R.sup.2, R.sup.3, X, Y and Z have the meanings given in the description, to a plurality of processes for their preparation, and to their use as herbicides.Type: GrantFiled: April 1, 1993Date of Patent: December 6, 1994Assignee: Bayer AktiengesellschaftInventors: Roland Andreee, Mark W. Drewes, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5362733Abstract: Compounds of formula(I) ##STR1## wherein R.sub.1 is nitro, halo, cyano and R.sub.2 is a group selected from ##STR2## wherein Y is oxygen or sulfur; X.sub.1 is NR wherein R is hydrogen, C.sub.1-8 alkyl or phenyl and pharmaceutically acceptable salts thereof are useful in the prevention or treatment of tissue damage induced by lipid peroxidation.Type: GrantFiled: October 23, 1992Date of Patent: November 8, 1994Assignee: Orion-yhtyma OyInventors: Reijo Backstrom, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
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Patent number: 5348954Abstract: Heterocylic chelating agents and salts thereof of formula I: ##STR1## wherein X represents a bond, O or S, or a group CHR.sup.1 or NR.sup.3 ; R.sup.1 represents H, a group OR.sup.3 or NR.sup.3 R.sup.3, or an alkyl or alkoxyalkyl group optionally substituted by a hydroxyl group or by a group NR.sup.3 R.sup.3 or CON.sup.3 R.sup.3 ;each R.sup.2 represents H, or an alkyl or alkoxy group optionally substituted by a hydroxyl or alkoxy group;each R.sup.3 represents H, an optionally hydroxylated alkyl group or a group CH.sub.2 Y;Y represents a group COZ, CON(OH)R.sup.4, POZ.sub.2 or SO.sub.2 Z;Z represents a group OR.sup.4, NR.sup.4 R.sup.4 or ##STR2## where each R.sup.11 is H, a hydroxyl group or an optionally hydroxylated alkyl group, s is 0, 1 or 2, and W is CHR.sup.11, NR.sup.11 or an oxygen atom; andeach R.sup.4 represents H, or an optionally mono- or poly-hydroxylated alkyl, alkoxyalkyl or polyalkoxyalkyl group;with the provisos that where s is 0 then W is CHR.sup.11 and that where X represents a bond or CHR.Type: GrantFiled: July 24, 1991Date of Patent: September 20, 1994Assignee: Nycomed Imaging ASInventors: Torsten Almen, Arne Berg, Harald Dugstad, Jo Klaveness, Klaus D. Krautwurst, Pal Rongved
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Patent number: 5262385Abstract: A compounds represented by the formula ##STR1## wherein X represents a fluorine atom,W represents an oxygen atom, sulfur atom or group --OCH.sub.2 --,Z.sup.1 and Z .sup.2 each represent a nitrogen atom or group CH, but when Z.sup.1 is a nitrogen atom, Z.sup.2 represents a nitrogen atom or group CH and when Z.sup.1 is a group CH, Z.sup.2 represents a nitrogen atom,R.sup.1 and R.sup.2 each independently represent either a hydrogen atom, halogen atom or mono- or dilower alkyl-substituted amino, or a lower alkyl, lower alkoxy or lower alkylthio each of which may be substituted with a halogen atom,R.sup.3 and R.sup.4 form together with the carbon atoms to which they bind respectively a 5- to 8-membered carbon ring.Type: GrantFiled: July 23, 1991Date of Patent: November 16, 1993Assignee: Mitsubishi Petrochemical Co., Ltd.Inventors: Atsushi Goh, Sachio Kudo, Yorio Kumamoto, Michi Watanabe, Takako Takahashi, Takako Aoki, Norishige Toshima, Keiji Endo, Hideshi Mukaida, Shinji Kawaguchi, Rika Higurashi
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Patent number: 5262386Abstract: Pyrimidinyl- and triazinyl-salicylamides of the formula I ##STR1## in which the meanings of the radicals are described in claim 1, and the salts of compounds of the formula I which have a free hydroxycarbonyl group have a herbicidal and plant-growth regulating action. They are suitable as active substances in weed killers and in compositions for positively influencing the growth of crop plants.Type: GrantFiled: December 20, 1991Date of Patent: November 16, 1993Assignee: Ciba-Geigy CorporationInventors: Christoph Luthy, Raymond Fisher
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Patent number: 5246938Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.5 R.sup.6, hydroxy, acylamino, --CO.sub.2 R.sup.4, --O(CH.sub.2).sub.m CO.sub.2 R.sup.4, phenyl, phenoxy, benzyl or benzyloxy, the phenyl group or phenyl moiety of the benzyl group being optionally substituted in the ring; or R.sup.2 and R.sup.3 when taken together form a 5 - or 6-membered ring; m is 1 or 2; R.sup.4 and R.sup.6 are hydrogen or C.sub.1-4 alkyl; R.sup.5 is C.sub.1-4 alkyl; n is 0, 1 or 2; provided that when n is 0, R.sup.1, R.sup.2 and R.sup.3 are not all hydrogen, or when n is 0 and R.sup.2 is hydrogen, R.sup.1 and R.sup.3 are not both methyl, or when n is 0 and R.sup.2 and R.sup.3 are both hydrogen, R.sup.1 is not methyl; are useful as nematicides.Type: GrantFiled: March 18, 1992Date of Patent: September 21, 1993Assignee: Imperial Chemical Industries PLCInventors: Michael D. Turnbull, John Finney
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Patent number: 5246914Abstract: Salicyloyl(thio)ether derivatives of the formula I, ##STR1## where is oxygen or sulfur and Z is carbon or nitrogen, and the radicals R.sup.1 to R.sup.4 and A have the meanings given in the disclosure, and processes and intermediates for preparing compounds I.Type: GrantFiled: August 7, 1992Date of Patent: September 21, 1993Assignee: BASF AktiengesellschaftInventors: Uwe J. Vogelbacher, Joachim Rheinheimer, Thomas Saupe, Norbert Meyer, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5225550Abstract: It is possible, by using symmetrical formaldehyde acetals of the formula ##STR1## in which the substituents R.sup.1 -R.sup.3 have the specified meanings, advantageously to introduce the substituent ##STR2## into nitrogen-containing heterocyclic systems to form acyclic nucleoside analogs.Type: GrantFiled: June 25, 1991Date of Patent: July 6, 1993Assignee: Hoechst AktiengesellschaftInventor: Gerhard Jahne
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Patent number: 5201937Abstract: Salicylic acid derivatives of the formula I ##STR1## (R.sup.1 is succinimidoxy; unsubstituted or substituted hetaryl; OR.sup.5 where R.sup.5 is substituted or unsubstituted cycloalkyl, alkyl, alkenyl, alkynyl, phenyl or substituted methyleneamino; OR.sup.8 where R.sup.8 is hydrogen, alkali metal or alkaline earth metal cation, ammonium or organic ammonium;R.sup.2 and R.sup.3 are each C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.2 -haloalkoxy and/or C.sub.1 -C.sub.4 -alkylthio;R.sup.4 is ethynyl or unsubstituted or substituted vinyl;X is oxygen or sulfur;Z is nitrogen or methine)are used as herbicides and bioregulators.Type: GrantFiled: October 16, 1991Date of Patent: April 13, 1993Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Karl Eicken, Uwe J. Vogelbacher, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5178663Abstract: Disclosed is a 3-alkoxyalkanoic acid compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl group, a halo-lower alkyl group or a cyano-lower alkyl group; R.sup.2 represents hydrogen atom or a lower alkyl group; R.sup.3 represents a lower alkyl group or a cycloalkyl group; or R.sup.2 and R.sup.3 are mutually bonded to represent a cycloalkyl group; R.sup.4 represents hydrogen atom, a lower alkyl group or a lower alkynyl group; R.sup.5 represents a lower alkoxy group, a lower alkyl group, a halogen atom or a halo-lower alkyl group; R.sup.6 represents a lower alkoxy group or a lower alkyl group; andX represents oxygen atom or sulfur atom,or an alkali addition salt thereof, processes for preparing the same and herbicides containing the same as an active ingredient(s).Type: GrantFiled: October 18, 1991Date of Patent: January 12, 1993Assignee: UBE Industries, Ltd.Inventors: Katsumasa Harada, Takaaki Abe, Yuji Akiyoshi, Hiroshi Shiraishi, Kaoru Yamamoto
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Patent number: 5169856Abstract: The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.Type: GrantFiled: February 6, 1989Date of Patent: December 8, 1992Assignee: Takeda Chemical Industries, Inc.Inventors: Giichi Goto, Akinobu Nagaoka
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Patent number: 5141943Abstract: 5-benzyl barbiturate compounds for use as water-soluble uridine phosphorylase inhibitors are disclosed. These compounds are useful for reducing the toxicity and anemia induced by antiviral drugs such as AZT, as well as for potentiating anticancer drugs and combatting their host-toxicity.Type: GrantFiled: April 12, 1990Date of Patent: August 25, 1992Assignee: Brown University Research FoundationInventors: Fardos N. M. Naguib, Mahmoud H. el Kouni, Raymond Panzica, Sungman Cha
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Patent number: 5112835Abstract: 6-substitutted acyclopyrimidine nucleoside derivatives represented by the following general formula I: ##STR1## wherein R.sup.1 represents a hydrogen or halogen atom or a group of alkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl; R.sup.2 represents a group of arylthio, alkylthio, cycloalkylthio, aryl sulfoxide, alkyl sulfoxide, cycloalkyl sulfoxide, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy; R.sup.3 represents a hydroxyalkyl group of which alkyl portion may contain an oxygen atom; X represents an oxygen or sulfur atom or amino group; Y represents an oxygen or sulfur atom; and A represents .dbd.N-- or --NH-- or pharmaceutically acceptable salts thereof, processes for their preparation and antiviral agents containing them as active ingredients.Type: GrantFiled: November 21, 1989Date of Patent: May 12, 1992Assignee: Mitsubishi Kasei CorporationInventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
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Patent number: 5099020Abstract: The present invention provides methods and compositions for assaying biological samples, such as human serum, for barbiturates. In one aspect, analogs of barbiturates derivatized with fluorescein and analogs of barbiturates derivatized with immunogenic polypeptides are provided. The fluorescent analogs are employed as tracers in a competitive homogeneous immunoassay, i.e., a fluorescence polarization immunoassay, for detecting barbiturates. The immunogenic analogs are employed to make anti-barbiturate antiserum of the invention for use in the immunoassay method. Intermediates for preparing the fluorescent and immunogenic analogs are also provided. Further provided are test kits, comprising a fluorescent tracer and an antiserum according to the invention, for analyzing biological samples by fluorescence polarization immunoassay for the presence of a barbiturate.Type: GrantFiled: June 27, 1990Date of Patent: March 24, 1992Assignee: Abbott LaboratoriesInventors: Jonathan Grote, Hsiang Hu
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Patent number: 4937344Abstract: A merocyanine dye having the formula: ##STR1## wherein: R.sub.1 and R.sub.2 independently are H, alkyl, alkoxy or arylR.sub.7 and R.sub.8 are H orany of R.sub.1 and R.sub.2, R.sub.1 and R.sub.7, R.sub.2 and R.sub.8 can together comprise the atoms necessary to form a fused aromatic ring on the benzene radical to which they are attached;R.sub.5 and R.sub.6 comprise alkyl of from 1-18 carbon atoms provided that the sum of the carbon atoms in R.sub.5 and R.sub.6 is at least 8;R.sub.9 is an alkylene group of 2-9 nuclear carbon and hetero atoms; andZ.sup.+ is a cation.This dye is useful in a method for inactivating viruses comprising contacting the viruses with the compound and exposing the resulting mixture to visible light to excite and inactivate the viruses. The compounds are also useful in the irradiation-induced inactivation of leukemia cells.Type: GrantFiled: June 8, 1988Date of Patent: June 26, 1990Assignee: Eastman Kodak CompanyInventors: Wolfgang H. H. Gunther, Frederick J. Sauter
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Patent number: 4906750Abstract: A merocyanine dye having the formula: ##STR1## wherein: R.sub.1 and R.sub.2 independently are H, alkyl, alkoxy or aryl; R.sub.7 and R.sub.8 are H orany of R.sub.1 and R.sub.2, R.sub.1 and R.sub.7, and R.sub.2 and R.sub.8 can together comprise the atoms necessary to form a fused aromatic ring on the benzene radical to which they are attached and with the stipulation that only one of R.sub.1 and R.sub.2 can be H;R.sub.5 and R.sub.6 comprise alkyl of from 1-18 carbon atoms, provided that the sum of the carbon atoms in R.sub.5 and R.sub.6 together is at least 8;R.sub.9 is an alkylene group of 2-9 nuclear carbon and hetero atoms; andZ.sup.+ is a cation.This dye is useful in a method for inactivating viruses comprising contacting the viruses with the compound and exposing the resulting mixture to visible light to excite and inactivate the viruses. The compounds are also useful in the irradiation-induced inactivation of leukemia cells.Type: GrantFiled: June 8, 1988Date of Patent: March 6, 1990Assignee: Eastman Kodak CompanyInventors: Wolfgang H. H. Gunther, Frederick J. Sauter
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Patent number: 4889552Abstract: A 2-phenoxypyrimidine derivative having the formula: ##STR1## wherein R is a formyl group or --COOR.sup.1 wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a 2-methylsulfonylethyl group, a diethoxypropyl group, a lower alkenyl group, a lower alkynyl group, a haloalkyl group, a haloalkenyl group, an alkoxyalkyl group, a hydroxyalkyl group, a cycloalkyl group, a phenyl group or ##STR2## wherein Y is a halogen atom, a methyl group or a methoxy group and n is 0, 1 or 2; and X is a halogen atom, an alkynyloxy group, an alkenyloxy group, an alkylthio group, an alkoxyalkyloxy group, a haloalkoxy group, an acetyloxy group, a benzoyloxy group, a formyl group, a trifluoromethyl group, a carboxyl group, an alkoxycarbonyl group, a dialkylamino group, a dimethoxymethyl group, ##STR3## wherein R.sup.2 is a hydrogen atom or a methyl group, Z is a chlorine atom or an alkyl group and m is 0, 1 or 2, or ##STR4## wherein R.sup.Type: GrantFiled: April 13, 1988Date of Patent: December 26, 1989Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Nobuhide Wada, Yoshihiro Saito, Shoji Kusano, Yasufumi Toyokawa, Takeshige Miyazawa, Satoru Takahashi
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Patent number: 4885366Abstract: A merocyanine dye having the formula: ##STR1## wherein: R.sub.1 and R.sub.2 independently are H, alkyl, alkoxy or aryl,R.sub.7 and R.sub.8 are H or any of R.sub.1 and R.sub.2, R.sub.1 and R.sub.7, R.sub.2 and R.sub.8 can together comprise the atoms necessary to form a fused aromatic ring on the benzene radical to which they are attached;R.sub.5 and R.sub.6 comprise alkyl of from 1-18 carbon atoms provided that the sum of the carbon atoms in R.sub.5 and R.sub.6 is at least 8;R.sub.9 is an alkylene group of 2-9 nuclear carbon and hetero atoms; andZ.sup.+ is a cation.This dye is useful in a method for inactivating viruses comprising contacting the viruses with the compound and exposing the resulting mixture to visible light to excite and inactivate the viruses. The compounds are also useful in the irradiation-induced inactivation of leukemia cells.Type: GrantFiled: June 8, 1988Date of Patent: December 5, 1989Assignee: Eastman Kodak CompanyInventors: Wolfgang H. H. Gunther, Frederick J. Sauter
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Patent number: 4427437Abstract: A process of inhibiting the growth of, severely damaging, or killing plants which process comprises applying to the plant or to the growth medium thereof an effective amount of a composition comprising as active ingredient a compound of formula I: ##STR1## wherein A, B and D are independently chosen from the group consisting of hydrogen, halogen, hydroxy, nitro, cyano, thiocyano, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, optionally substituted alkenyloxy, optionally substituted alkynyloxy, optionally substituted alkylthio, optionally substituted cycloalkyl, optionally substituted amino, optionally substituted phenyl, carboxy, alkoxycarbonyl, optionally substituted carbamoyl, sulfo, alkylsulfonyl and optionally substituted sulfamoyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.Type: GrantFiled: September 5, 1978Date of Patent: January 24, 1984Assignee: ICI Australia LimitedInventors: Alexander Serban, Keith G. Watson, Richard B. Warner
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Patent number: 4412856Abstract: The novel compounds of the formula I are useful selective herbicides for postemergence application in crops of cereals, maize and rice.In formula I, ##STR1## A is an unsubstituted or substituted amino group, Q is a C.sub.2 -C.sub.6 alkylene bridge, Y is an oxygen or sulfur atom or an unsubstituted or substituted nitrogen atom, and Z is an unsubstituted or substituted phenyl, naphthyl or heterocyclic radical, which phenyl radical, containing the bridge member Y, can additionally carry one to four further substituents.Type: GrantFiled: May 22, 1981Date of Patent: November 1, 1983Assignee: Ciba-Geigy CorporationInventors: Hans-Georg Brunner, Rolf Schurter, Henry Szczepanski