Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/314)
  • Patent number: 5795497
    Abstract: A thiouracil derivative represented by the following general formula (1) or (2) ##STR1## (wherein, R.sup.1 and R.sup.2 each are a hydrogen atom or an alkyl group, and at least one of R.sup.1 and R.sup.2 is a hydrogen atom, and R.sup.3 is a hydrogen atom, an alkyl group or a phenyl group, and R.sup.4 is a bivalent saturated hydrocarbon group having 2 to 12 carbon atoms, Z is --COO--, CH.sub.2 O-- or --C.sub.6 H.sub.4 --CH.sub.2 O--, and R.sup.5 is a hydrogen atom or a methyl group), and a metal surface-treating agent for bonding a metal, particularly a noble metal to a resin or the like in high adhesive strength and in high water resistance and high durability which contains the above thiouracil derivative and an organic solvent such as acetone or ethanol.
    Type: Grant
    Filed: April 18, 1997
    Date of Patent: August 18, 1998
    Assignee: Tokuyama Corporation
    Inventors: Mikio Kimura, Masayuki Aizawa
  • Patent number: 5792868
    Abstract: Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar.Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.
    Type: Grant
    Filed: March 18, 1994
    Date of Patent: August 11, 1998
    Assignee: Ajinomoto Co., Inc.
    Inventors: Kunisuke Izawa, Yoshihito Koguchi, Hiroshi Shiragami
  • Patent number: 5777118
    Abstract: Cyclic acetals of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 and R.sup.2 are hydrogen, unsubstituted or substituted alkyl or phenyl; additionally R.sup.1 and R.sup.2 together are an unsubstituted or substituted C.sub.2 -C.sub.6 -alkylene chain;Y is oxygen or sulfur;A has the meaning as given in claim 1;a process for preparing the acetals I and their use for the production of crop protection compositions are described.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: July 7, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Hartmann Konig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5753594
    Abstract: 3-Halo-3-hetarylcarboxylic acid derivatives having the formula I ##STR1## in which R is a formyl group, a group CO.sub.2 H or a radical which can be hydrolyzed to COOH, and the remaining substituents have the following meanings:R.sup.2 and R.sup.3 are halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy or C.sub.1 -C.sub.4 -alkylthio;X is nitrogen or CR.sup.13, where R.sup.13 is hydrogen or together with R.sup.3 forms an alkylene or alkenylene chain in which in each case one methylene group is replaced by oxygen;R.sup.4 is an unsubstituted or substituted five- or six-membered heteroaromatic ring which contains one to three nitrogen atoms and/or one sulfur or oxygen atom;R.sup.5 is hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl or phenyl;Y is sulfur, oxygen or a single bond; andZ is halogen.The derivatives I having herbicidal and plant-growth regulating properties.
    Type: Grant
    Filed: December 1, 1995
    Date of Patent: May 19, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Albrecht Harreus, Matthias Bratz, Joachim Rheinheimer, Uwe Josef Vogelbacher, Hans Theobald, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen, Wilhelm Rademacher
  • Patent number: 5750532
    Abstract: The disclosed invention is compounds represented by the formula ##STR1## and pharmacetically acceptable acid salts thereof, wherein each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, loweralkyl-sulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl, hydroxyiminoloweralkyl hydroxyloweralkyl or carbonyl; or 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining member of the ring being at least one carbon, and optionally sulfur or oxygen,X and Y are each independently a bond, ##STR2## each Q is independently a divalent substituted or unsubstituted, straight or branched chain lower alkanediyl, lower alkanediyl-cycloalkanediyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofura
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: May 12, 1998
    Assignee: Schering Corporation
    Inventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
  • Patent number: 5747500
    Abstract: 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: Grant
    Filed: June 18, 1996
    Date of Patent: May 5, 1998
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jong-Chan Son, III-Young Lee, Byung-II Bae, Jeong-Sik Han, Joong-Kwon Choi, Yung-Bok Chae
  • Patent number: 5728833
    Abstract: A process for the preparation of a compound of formula (I):HetSCH.sub.2 CH.sub.2 CH.dbd.CF.sub.2 (I)wherein Het is an optionally substituted 5- or 6-membered heterocyclic ring, which comprises reacting a compound of formula (II):HetSH (II)with a compound of formula (III):CF.sub.2 .dbd.CHCH.sub.2 CH.sub.2 L (III)wherein L is chlorine or bromine or a group --OSO2R.sup.a wherein R.sup.a is a C1-4 alkyl group or a phenyl group optionally substituted by a C1-4 alkyl group.
    Type: Grant
    Filed: August 4, 1994
    Date of Patent: March 17, 1998
    Assignee: Zeneca Limited
    Inventors: Michael Drysdale Turnbull, Nigel James Willetts, Steven Fitzjohn, Prafula Govind Kholia, Alison Mary Smith, Roger Salmon, Harjinder Singh Bansal
  • Patent number: 5726128
    Abstract: 1. A benzyloxypyrimidine derivative of the formula (I): ##STR1## wherein R.sup.1 represents hydrogen, a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.3 -C.sub.5 alkenyloxy, C.sub.1 -C.sub.4 alkylthio, or cyano;each X, which may be identical or different if n is greater than 1, represents a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, or C.sub.1 -C.sub.4 haloalkyl;each Y, which may be identical or different if m is greater than 1, represents a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, or C.sub.1 -C.sub.4 haloalkoxy;G represents O or S; andn and m each independently represent an integer of 0 to 5.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: March 10, 1998
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Hisashi Kanno, Yoshikazu Kubota, Tsutomu Sato, Masato Arahira
  • Patent number: 5723473
    Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: March 3, 1998
    Assignee: Zeneca Limited
    Inventor: Brian Leslie Pilkington
  • Patent number: 5723412
    Abstract: A 2-benzyloxy-4-phenoxypyrimidine derivative represented by the formula (I): ##STR1## wherein R.sup.1 represents hydrogen, a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.3 -C.sub.5 alkenyloxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkylthio, cyano, or phenyl;each X, which may be identical or different if n is greater than 1, represents a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, or C.sub.1 -C.sub.4 alkoxy;each Y, which may be identical or different if m is greater than 1, represents a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio, or C.sub.1 -C.sub.4 haloalkylthio; andn and m each independently represent an integer of 0 to 5, which is useful as a herbicide.
    Type: Grant
    Filed: July 13, 1995
    Date of Patent: March 3, 1998
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Hisashi Kanno, Yoshikazu Kubota, Tsutomu Sato, Masato Arahira
  • Patent number: 5723471
    Abstract: A fungicidal compound of formula (I) or a stereoisomer thereof, wherein R is H or CH.sub.3, A is CH or N, and B is OCH.sub.3 or NHCH.sub.3.
    Type: Grant
    Filed: August 7, 1996
    Date of Patent: March 3, 1998
    Assignee: Zeneca Limited
    Inventor: Paul John De Fraine
  • Patent number: 5723609
    Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## wherein R.sub.2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; or trifluoromethyl; R.sub.5 is alkyl; R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.
    Type: Grant
    Filed: March 13, 1989
    Date of Patent: March 3, 1998
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: William A. Slusarchyk, Robert Zahler
  • Patent number: 5721241
    Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y H is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is H or an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 24, 1998
    Assignees: Mahmoud H. el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
    Inventors: Mahmoud H. el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
  • Patent number: 5714437
    Abstract: Novel compounds of the formula ?1! are disclosed, wherein X is hydrogen, fluorine or chlorine; Y is fluorine, chlorine or bromine; R.sup.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.2 and Q are various groups. Also disclosed are herbicidal compositions containing these compounds as active ingredients and methods for controlling unfavorable weeds by application of these compounds.
    Type: Grant
    Filed: August 30, 1995
    Date of Patent: February 3, 1998
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Minoru Takano, Masayuki Enomoto, Kazuo Saito, Satoru Kizawa
  • Patent number: 5714606
    Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: February 3, 1998
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Oscar L. Acevedo, Normand Hebert
  • Patent number: 5707995
    Abstract: 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: Grant
    Filed: July 24, 1995
    Date of Patent: January 13, 1998
    Assignee: American Cyanamid Company
    Inventors: David Munro, Royston Davis, Janet Anne Day, Jacqueline Anne Wilkin, William W. Wood
  • Patent number: 5696265
    Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 9, 1997
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Choung Un Kim, John C. Martin, Bing Uh Luh, Peter F. Misco
  • Patent number: 5693771
    Abstract: In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.
    Type: Grant
    Filed: March 13, 1996
    Date of Patent: December 2, 1997
    Assignee: Gilead Sciences, Inc.
    Inventors: Petr Alexander, Ernest J. Prisbe
  • Patent number: 5693798
    Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 2, 1997
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w
    Inventors: Choung Un Kim, John C. Martin, Bing Uh Luh, Peter F. Misco
  • Patent number: 5688778
    Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl;B is a purine or pyrimidine base.optionally R is taken together with X' to complete a cyclic phosphonate having the formula ##STR2## A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR3## wherein X and X' are the same or different and are hydrogen or alkyl, the dashed line is an optional bond,Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z are taken together to form an epoxide or cyclopropyl, andB is a purine or pyrimidine base.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: November 18, 1997
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Choung Un Kim, John C. Martin, Bing Uh Luh, Peter F. Misco
  • Patent number: 5686629
    Abstract: An improved method for the preparation of acyclic nucleotide analogues comprises first condensing a cyclic carbonate with a purine or pyrimidine base and then reacting the alkylated base with an activated phosphonate. Novel cyclic carbonates are employed to yield the desired phosphonylmethoxyalkyl nucleotide analogues.
    Type: Grant
    Filed: December 27, 1995
    Date of Patent: November 11, 1997
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Kenneth M. Kent
  • Patent number: 5686611
    Abstract: Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A compound of formula (VI) ##STR2## wherein X is halogen, Y is S-phenyl, Se-phenyl or halogen and B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, 2-acetamido-6-diphenylcarbamoylpurine, 6-N-dimethylamino-methyladenine or 6-N-pivaloyladenine.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 11, 1997
    Assignees: Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Choung Un Kim, John C. Martin, Bing Uh Luh, Peter F. Misco
  • Patent number: 5683966
    Abstract: Herbicidal 3-(substituted-benzyl)-1-methyl-6-trifluoromethyluracils, compositions containing them, and methods of using them to control undesired plant growth, including use to control weeds in certain crops, are disclosed.
    Type: Grant
    Filed: June 10, 1996
    Date of Patent: November 4, 1997
    Assignee: FMC Corporation
    Inventor: Marvin J. Konz
  • Patent number: 5681794
    Abstract: The invention relates to new N-cyanoaryl-nitrogen heterocycles of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z have the meanings given in the description,to a plurality of processes for their preparation, to their use as herbicides and to novel intermediates.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: October 28, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark-Wilhelm Drewes, Albrecht Marhold, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5661106
    Abstract: 3-(Het)aryloxy(thio)carboxylic acid derivatives of the formula I ##STR1## where R.sup.1 is hydrogen, COOH or a radical which can be hydrolyzed to give COOH;R.sup.2 and R.sup.3 are each halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.14, where R.sup.14 is hydrogen or, together with R.sup.3, forms a 3-membered or 4-membered alkylene or alkenylene chain, in each of which a methylene group is replaced by oxygen;R.sup.4 is alkyl, cycloalkyl, cycloalkenyl, alkenyl or alkynyl, each of which is unsubstituted or substituted;an unsubstituted or substituted five-membered or six-membered heteroaromatic structure containing one to three nitrogen atoms or one sulfur or oxygen atom;unsubstituted or substituted phenyl or naphthyl;R.sup.4 and R.sup.5, together with the neighboring carbon atom, form a 3-membered to 8-membered ring which may contain an oxygen or sulfur atom and which is unsubstituted or substituted;R.sup.
    Type: Grant
    Filed: October 19, 1995
    Date of Patent: August 26, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Bratz, Norbert Meyer, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Wilhelm Rademacher
  • Patent number: 5631259
    Abstract: Cycloalkyltriols containing heterocyclic substituents, in particular cyclopentyl- and cyclohexyltriols containing heterocyclic substituentsCompounds of the formulae I and II ##STR1## in which the substituents A, R.sup.1, R.sup.2 and R.sup.3 and n have the meanings given, have an antiviral and antiparasitic action.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 20, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard J ahne, Irvin Winkler, Matthias Helsberg, Heinz H anel
  • Patent number: 5629454
    Abstract: Conformationally locked 4',6'-cyclopropane-fused carbocyclic nucleoside analogues. The compounds are prepared by condensing a cyclopropane-fused carbocyclic allylic alcohol with substituted purine or pyrimidine bases. The condensation products are then modified to produce the adenosine, guanosine, cytidine, thymidine and uracil nucleoside analogues. The compounds are therapeutically useful as antimetabolites, or in the preparation of anti-metabolic agents.
    Type: Grant
    Filed: September 23, 1994
    Date of Patent: May 13, 1997
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Victor E. Marquez, Juan B. Rodriguez, Marc C. Nicklaus, Joseph J. Barchi, Jr., Maqbool A. Siddiqui
  • Patent number: 5618793
    Abstract: Compounds of the formula ##STR1## wherein R.sub.3, R.sub.4, J, K, Z, and Het are as set forth herein are described.The compounds of formula I are useful as agents in the treatment of fungal infections.
    Type: Grant
    Filed: August 1, 1995
    Date of Patent: April 8, 1997
    Assignee: Schering Corporation
    Inventors: Alan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
  • Patent number: 5610300
    Abstract: Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 11, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Karl-Heinz Altmann, Ren e Imwinkelried, Albert Eschenmoser
  • Patent number: 5602077
    Abstract: A method is disclosed for controlling the growth of undesired vegetation in a plantation crop by applying to the locus of the crop an effective amount of a compound of formula I ##STR1## and A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y and Z are as defined in the disclosure. Also disclosed are novel substituted heterocyclic compounds and their agriculturally suitable compositions which are generally useful as herbicides, as well as methods of their use as general or selective preemergent or postemergent herbicides, or as plant growth regulants.
    Type: Grant
    Filed: July 13, 1994
    Date of Patent: February 11, 1997
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Kofi S. Amuti, Wonpyo Hong, Joseph E. Semple
  • Patent number: 5602181
    Abstract: Naphthyl ethers of the general formula I ##STR1## where the index and the substituents have the meanings defined in the specification.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: February 11, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Reinhard Kirstgen, Hartmann K onig, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5599771
    Abstract: 3-Aryluracil derivatives of formula I ##STR1## wherein W is a group of the formula ##STR2## wherein the bond to the ring nitrogen atom is made via the carbon atom; wherein R.sub.1 to R.sub.9 are as defined in claim 1, are suitable as active ingredients in weed control compositions.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: February 4, 1997
    Assignee: Ciba-Geigy Corporation
    Inventor: Jean Wenger
  • Patent number: 5599770
    Abstract: A herbicidal composition comprising a herbicidally effective amount of a 2-benzyloxypyrimidine derivative represented by the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are each independently H, a halogen, hydroxyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.3 -C.sub.5 alkenyloxy, C.sub.3 -C.sub.5 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, or phenyl;n is an integer of 0 to 5; andeach X which may be identical or different if n is greater than 1, is a halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.7 -C.sub.9 aralkyloxy, phenyl, hydroxymethyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or nitro, andan adjuvant.
    Type: Grant
    Filed: June 21, 1995
    Date of Patent: February 4, 1997
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Yoshikazu Kubota, Hisashi Kanno, Tsutomu Sato, Masato Arahira
  • Patent number: 5593945
    Abstract: The invention relates to new N-cyanoaryl-nitrogen heterocycles of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z have the meanings given in the description,to a plurality of processes for their preparation, to their use as herbicides and to novel intermediates.
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: January 14, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark-Wilhelm Drewes, Albrecht Marhold, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5556976
    Abstract: A method of forming a crosslinked cellulose product is disclosed wherein cellulose fibers are exposed to a solution that includes a catalyst and a crosslinking agent selected from the group consisting of a cyclic N-sulfatoimide or cyclic N-phosphatoimide; a dimethoxyethanal; a mixture of glyoxal and imidazolidone; a diethanol; or a periodate. Specific examples of the crosslinking agents of the present invention include pyridinium N-sulfatosuccinimide; 2,2'-sulfonyldiethanol; sodium periodate; a mixture of dimethoxyethanal and urea; and a mixture of glyoxal and 2-imidazolidone. An acid or base catalyst, as appropriate, may be used with the crosslinking agent to increase the crosslinking reaction rate. In especially preferred embodiments, cellulose fibers are exposed to the crosslinking agent and catalyst, then separated into individualized fibers in a fiberizer.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: September 17, 1996
    Inventor: Richard A. Jewell
  • Patent number: 5550132
    Abstract: Novel hydroxyalkylammonium-pyrimidine of the formula ##STR1## and nucleoside derivatives have been found to be useful as inhibitors of inflammatory cytokines. They can be used, inter alia, in the therapy of septic shock, cachexia, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and AIDS. The compounds are typically prepared by reaction of an iodo substituted nucleoside with the appropriately substituted hydroxyalkylamine.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: August 27, 1996
    Assignees: University of North Carolina, Macronex, Inc.
    Inventors: Bradley J. Benson, Xiannong Chen, George J. Cianciolo, Jose-Luis Diaz, Khalid S. Ishaq, Susan L. Morris-Natschke, Ronald J. Uhing, Henry Wong
  • Patent number: 5539116
    Abstract: The present invention relates to a method of preparing BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, .beta.-BCH-189 and related compounds. Furthermore, the steochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched .beta.-BCH-189 and its analogs.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: July 23, 1996
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Woo-Baeg Choi
  • Patent number: 5527764
    Abstract: Compounds having the structural formula ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl, R.sub.2 is C.sub.1 -C.sub.4 alkyl or haloalkyl, R.sub.3 and R.sub.4 are hydrogen or halogen, and R.sub.5 is hydrogen or COOR.sub.6 wherein R.sub.6 is C.sub.1 -C.sub.8 linear or branched alkyl, alkenyl, or alkynyl, and compositions comprising the compounds. The compounds and compositions are useful as herbicides, desiccants and defoliants.
    Type: Grant
    Filed: September 15, 1994
    Date of Patent: June 18, 1996
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./Ltee
    Inventors: Dong Dao-cong, Alan W. Dalrymple
  • Patent number: 5521147
    Abstract: Herbicidal 3-(benzofuran-7-yl)-6-haloalkyluracils of the formula ##STR1## in which M is fluoroalkyl (C.sub.1-6); D is hydrogen, alkyl (C.sub.1-6), or alkoxy(C.sub.1-6)-carbonyl; E is hydrogen or alkyl (C.sub.1-6), or D and E taken together are --CH.sub.2 CH.sub.2 --; R is hydrogen, amino, alkyl (C.sub.1-6), 2-alkenyl (C.sub.3-6), 2-alkynyl (C.sub.3-6), alkoxy(C.sub.1-6)methyl, benzyl, amino, fluoroalkyl (C.sub.1-6), alkoxy (C.sub.1-6)-carbonylmethyl; or cyanoalkyl (C.sub.1-6) having preferably one cyano group; X is hydrogen, fluorine, chlorine, bromine, cyano, alkyl(C.sub.1-6), haloalkyl(C.sub.1-6), haloalkoxy(C.sub.1-6), or alkoxy(C.sub.1-6); Y is hydrogen, alkyl (C.sub.1-6), fluorine, chlorine, or bromine; and Z is CH.sub.2, C.dbd.O, C.dbd.S, --CH(OH)--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --(C.dbd.O)CH.sub.2 --; or C.dbd.N--O--R' wherein R' is alkyl(C.sub.1-6).
    Type: Grant
    Filed: February 3, 1995
    Date of Patent: May 28, 1996
    Assignee: FMC Corporation
    Inventor: George Theodoridis
  • Patent number: 5519139
    Abstract: There is disclosed a novel 4-aminopyrimidine derivative containing an optionally esterified carboxyl group at the 5-position which has potent fungicidal activity as well as insecticidal and miticidal activity. The compound is useful as agricultural fungicides, insecticides and miticides.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: May 21, 1996
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshikazu Ohtsuka, Moriyasu Masui, Takami Takeda, Michio Masuko, Katsuaki Ohba
  • Patent number: 5519134
    Abstract: Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.
    Type: Grant
    Filed: January 11, 1994
    Date of Patent: May 21, 1996
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Oscar L. Acevedo, Normand Hebert
  • Patent number: 5514798
    Abstract: An improved method for the preparation of acyclic nucleotide analogues comprises first condensing a cyclic carbonate with a purine or pyrimidine base and then reacting the alkylated base with an activated phosphonate. Novel cyclic carbonates are employed to yield the desired phosphonylmethoxyalkyl nucleotide analogues.
    Type: Grant
    Filed: February 13, 1995
    Date of Patent: May 7, 1996
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Kenneth M. Kent
  • Patent number: 5512678
    Abstract: The present invention provides novel 5-(1-fluorovinyl)-1H-pyrimidine-2,4-dione derivatives which are useful as antineoplastic agents by themselves or in conjunctive therapy with the antineoplastic agent 5-fluorouracil.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: April 30, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: James R. McCarthy, Donald P. Matthews, Jeffrey S. Sabol
  • Patent number: 5496824
    Abstract: The present invention provides a pharmaceutical agent having a high pharmaceutical potency against varicella-zoster viruses and herpes simplex viruses, compositions containing the same, and methods for treating varicella-zoster viruses using the same.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: March 5, 1996
    Assignee: Ajinomoto Co., Inc.
    Inventors: Tomoyuki Onishi, Chika Mukai, Takaaki Sekiyama, Takashi Tsuji, Satoshi Iwayama, Masahiko Okunishi
  • Patent number: 5486610
    Abstract: Pyrimidinylbenzenesulfonyl chloride compounds of the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 haloalkyl;X is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.8 alkoxy, or halogen;Y is hydrogen or halogen;R.sup.3 is hydrogen, halogen or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl.The compounds are useful as intermediates in the preparation of herbicides.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: January 23, 1996
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Richard J. Strunk, Allyn R. Bell
  • Patent number: 5476855
    Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging.
    Type: Grant
    Filed: November 2, 1993
    Date of Patent: December 19, 1995
    Assignees: Mahmoud H. el Kouni, Fardos N. M. Naguib, F. Schinazi
    Inventors: Mahmoud el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
  • Patent number: 5470975
    Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.
    Type: Grant
    Filed: January 11, 1994
    Date of Patent: November 28, 1995
    Assignee: E.R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5461152
    Abstract: Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.
    Type: Grant
    Filed: June 28, 1993
    Date of Patent: October 24, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Karl-Heinz Altmann, Rene Imwinkelried, Albert Eschenmoser
  • Patent number: 5461060
    Abstract: The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I'] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: ##STR1## and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: October 24, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tadashi Miyasaka, Hiromichi Tanaka, Erik D. A. De Clercq, Masanori Baba, Richard T. Walker, Masaru Ubasawa
  • Patent number: 5459144
    Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, X, Q, Y, W, and W' are as described herein. These compounds have antiviral activity, and certain of these compounds have antiinflammatory activity and are PAF inhibitors.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: October 17, 1995
    Assignee: Schering Corporation
    Inventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace