5-position Is Unsubstituted Or Alkyl Substituted Only Patents (Class 544/312)
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5900483Abstract: A process for the separation of phenyluracil compounds is provided.The process according to the present invention comprises treating with a weakly-basic substance a mixture of a halogenophenyluracil compound (I) and a cyanophenyluracil compound (II): ##STR1## wherein X is a hydrogen or fluorine atom, Y is a chlorine or bromine atom, and R is an alkyl group containing 1 to 3 carbon atoms, to separate the compounds (I) and (II).Type: GrantFiled: August 24, 1998Date of Patent: May 4, 1999Assignee: Nissan Chemical Industries, Ltd.Inventors: Yoshiyuki Kusuoka, Yoshihiro Kudo, Norio Tanaka, Jun Satow
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Patent number: 5874382Abstract: Compounds of Formula I and II, and their agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X is a direct bond; O; S; NH; N(C.sub.1 -C.sub.3 alkyl); N(C.sub.1 -C.sub.3 haloalkyl); or N(allyl);R.sup.1 is H; F; Cl; or Br;R.sup.2 is H; F; Cl; Br; CF.sub.3 ; nitro; or cyano;R.sup.4 is H; C.sub.1 -C.sub.3 alkyl; or halogen;R.sup.5 is H; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; halogen; S(O).sub.2 (C.sub.1 -C.sub.6 alkyl); or C(.dbd.O)R.sup.8 ; orR.sup.4 and R.sup.5 are taken together along with the carbon to which they are attached to form a spiro-cyclopropane ring;and R.sup.3, R.sup.8, and J are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formulae I and II and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I or II.Type: GrantFiled: January 23, 1998Date of Patent: February 23, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Balreddy Kamireddy, William Mark Murray
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Patent number: 5861395Abstract: Novel compounds of the formula: ##STR1## are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: ##STR2## wherein R.sup.1, R.sup.3 and R.sup.4 are each independently selected from halo. Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.Type: GrantFiled: September 11, 1997Date of Patent: January 19, 1999Assignee: Schering CorporationInventors: Arthur G. Taveras, Alan K. Mallams, Adriano Afonso, Stacy W. Remiszewski, F. George Njoroge, Ronald Doll, Tarik Lalwani, Carmen Alvarez
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Patent number: 5847137Abstract: The invention relates to a novel process for preparing substituted aryluracils by reacting aminoalkenoic esters with arylurethanes and then with sulfonamides, and additionally to novel 4-(alkoxycarbonylamino)-2,5-difluorobenzonitriles.Type: GrantFiled: October 27, 1997Date of Patent: December 8, 1998Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark Wilhelm Drewes, Bernd Gallenkamp
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Patent number: 5817811Abstract: Processes are described for preparing substituted N-ethylglycine derivatives of the formula ##STR1## in which PG is an amino protecting group which is labile towards weak acids and is of the urethane type or the trityl type, X is NH or O, and B' represents bases which are customary in nucleotide chemistry and whose exocyclic amino and/or hydroxyl groups are protected by suitable known protecting groups, and the salts thereof.Type: GrantFiled: September 3, 1996Date of Patent: October 6, 1998Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breipohl, Eugen Uhlmann, David William Will
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Patent number: 5817814Abstract: This invention describes a method for preparing benzyluracils using methyl benzylcarbamates as intermediates. The method comprises the steps of contacting an alkali metal salt of an ester of 3-amino-4,4,4-trifluoro-2-butenoic acid with a methyl benzylcarbamate I to provide a benzyluracil II. ##STR1## where R, W, V, X and Y are as described in the specification.Type: GrantFiled: May 1, 1997Date of Patent: October 6, 1998Assignee: FMC CorporationInventors: Marvin J. Konz, Harvey R. Wendt
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Patent number: 5807862Abstract: Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY--(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.Type: GrantFiled: June 7, 1995Date of Patent: September 15, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Alistair J. Leigh, Gail E. Underiner, Anil M. Kumar
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Patent number: 5801182Abstract: Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula:CORE MOIETY --(R).sub.jIn these compounds, j is an integer from one to three; the core moiety is a cyclic core, the cyclic core being non-cyclic or at least one five- to seven-member non-heterocyclic ring or heterocycle; and R is selected from the group consisting of amine, hydrogen, halogen, hydroxyl, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic group or formula I. At least one R having formula I: ##STR1## In formula I, n is an integer from four to twenty; and each R.sub.1 or R.sub.2 is independently hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or cyclic or heterocyclic group.Type: GrantFiled: June 7, 1995Date of Patent: September 1, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar, Lance H. Ridgers
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Patent number: 5792868Abstract: 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: GrantFiled: March 18, 1994Date of Patent: August 11, 1998Assignee: Ajinomoto Co., Inc.Inventors: Kunisuke Izawa, Yoshihito Koguchi, Hiroshi Shiragami
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Patent number: 5783576Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.Type: GrantFiled: August 9, 1996Date of Patent: July 21, 1998Assignee: Boehringer Ingelheim KGInventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
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Patent number: 5759957Abstract: The invention relates to novel N-cyanoaryl nitrogen heterocycles of general formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z have the meanings given in the description, several processes for producing them, their use as herbicides and insecticides and novel intermediate products.Type: GrantFiled: July 8, 1996Date of Patent: June 2, 1998Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark Wilhelm Drewes, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen
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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: 5726128Abstract: 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: GrantFiled: September 8, 1995Date of Patent: March 10, 1998Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Hisashi Kanno, Yoshikazu Kubota, Tsutomu Sato, Masato Arahira
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Patent number: 5723473Abstract: 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: GrantFiled: April 11, 1995Date of Patent: March 3, 1998Assignee: Zeneca LimitedInventor: Brian Leslie Pilkington
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Patent number: 5723471Abstract: 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: GrantFiled: August 7, 1996Date of Patent: March 3, 1998Assignee: Zeneca LimitedInventor: Paul John De Fraine
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Patent number: 5708000Abstract: The present invention pertains to the field of organic chemistry, and particularly therapeutic chemistry. The invention provides cis-form 5-(cytosinyl-1) 1,3-oxathiolanes of general formula (I), wherein R is an acyl or aralkoyl radical, derivatized from a nitrogen monocyclic or bicyclic heterocycle, and the hydroxymethyl group in position 2 is in cis position in relation to the plane defined by positions 2 and 5. The compounds of general formula (I) are useful as active ingredients in pharmaceutical compositions, particularly with antiviral activity.Type: GrantFiled: March 25, 1996Date of Patent: January 13, 1998Assignee: Laboratoire LaphalInventors: Anne Sophie Charvet-Faury, Michel Camplo, Jean Louis Kraus
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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: 5700805Abstract: Substituted 1-amino-3-phenyluracils I ##STR1## where the variables have the following meanings: R.sup.1 =H, F, Cl; Y=O, S; Z=--CH=N--OH, --CH=N--O--(alkyl),--CH=N--O--(alkylene)--O--(alkyl), --CH=N--O--CH.sub.2 --COOH,--CH=N--O--CH(alkyl)--COOH, --CH=N--O--CH.sub.2 --CO--O--(alkyl),--CH=N--O--CH(alkyl)--CO--O--(alkyl), --CH=N--O--CH.sub.2 --CO--O=O-- (alkylene)--O--(alkyl), --CH=N--O--CH(alkyl)--CO--O-- (alkylene)--O--(alkyl), --CH=CH--CO--O--(alkyl), --CH=CH-- CO--O--(alkylene)--O--(alkyl),--CH=C(Cl)--CO--O--(alkyl), --CH=C(Br)--CO--O--(alkyl),--CH=C(Cl)--CO--O--(alkylene)--O--(alkyl),--CH=C(Br)--CO--O--(alkylene)--O--(alkyl), --CH=C(CH.sub.3)--CO--O--(alkyl),--CH=C(CH.sub.3)--CO--O--(alkylene)--O--(alkyl), --CH?X.sup.1 -(alkyl)! ?X.sup.2 -(alkyl)! or a radical ##STR2## X.sup.1 -X.sup.6 =O, S; R.sup.2 -R.sup.11 =H, alkyl, vinyl, alkoxycarbonyl are described.Use: herbicides; desiccation/defoliation of plants.Type: GrantFiled: February 15, 1996Date of Patent: December 23, 1997Assignee: BASF AktiengesellschaftInventors: Peter Schafer, Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5686629Abstract: 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: GrantFiled: December 27, 1995Date of Patent: November 11, 1997Assignee: Gilead Sciences, Inc.Inventors: Norbert W. Bischofberger, Kenneth M. Kent
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Patent number: 5683966Abstract: 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: GrantFiled: June 10, 1996Date of Patent: November 4, 1997Assignee: FMC CorporationInventor: Marvin J. Konz
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Patent number: 5635508Abstract: The invention discloses compounds of formula I It has now been found that compounds of formula I ##STR1## wherein R.sub.1 is hydrogen, methyl, ethyl or trifluoromethyl, andR.sub.2 is hydrogen, methyl, ethyl, C.sub.1-4 alkylthio, C.sub.1-4 alkoxy, or di-C.sub.1-4 alkylamino, andR.sub.3 is C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, aryl, heteroaryl, aryl-C.sub.1-4 alkyl, heteroaryl-C.sub.1-4 alkyl, aryloxy-C.sub.1-4 alkyl, aryloxyaryl, arylaryl, heteroaryl, aryl-C.sub.1-4 alkoxyaryl, aryl-C.sub.1-4 alkoxy-C.sub.1-4 alkyl, heteroaryloxyaryl, aryloxy-C.sub.1-4 alkylaryl or aryl substituted by a group selected from --C(CH.sub.3).dbd.N--O--CH.sub.2 --aryl, --C(CH.sub.3).dbd.N--O--CH(CH.sub.3)--aryl, --C(CH.sub.3).dbd.N--C.sub.1-4 alkoxy, --C(CH.sub.3).dbd.N--C.sub.3-4 alkenyloxy, --C(CH.sub.3).dbd.N--C.sub.3-4 alkynyloxy, or --CH.sub.2 --O--N.dbd.C(CH.sub.Type: GrantFiled: May 8, 1995Date of Patent: June 3, 1997Inventors: Martin Eberle, Fritz Schaub, Gerald W. Craig
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Patent number: 5610300Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 11, 1997Assignee: Ciba-Geigy CorporationInventors: Karl-Heinz Altmann, Ren e Imwinkelried, Albert Eschenmoser
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Patent number: 5602077Abstract: 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: GrantFiled: July 13, 1994Date of Patent: February 11, 1997Assignee: E. I. Du Pont de Nemours and CompanyInventors: Kofi S. Amuti, Wonpyo Hong, Joseph E. Semple
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Patent number: 5602181Abstract: Naphthyl ethers of the general formula I ##STR1## where the index and the substituents have the meanings defined in the specification.Type: GrantFiled: October 12, 1994Date of Patent: February 11, 1997Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Reinhard Kirstgen, Hartmann K onig, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5599771Abstract: 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: GrantFiled: December 16, 1994Date of Patent: February 4, 1997Assignee: Ciba-Geigy CorporationInventor: Jean Wenger
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Patent number: 5599770Abstract: 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: GrantFiled: June 21, 1995Date of Patent: February 4, 1997Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Yoshikazu Kubota, Hisashi Kanno, Tsutomu Sato, Masato Arahira
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Patent number: 5585490Abstract: This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: n is 0, 1 or 2, and R.sub.1, R.sub.2, X, Y and W are variables.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: April 5, 1993Date of Patent: December 17, 1996Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Alan Hutchison, Vinod Singh
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Patent number: 5559081Abstract: Herbicidal sulfonamides of the formula: ##STR1## and salts thereof, where: A represents a substituted or unsubstituted benzene ring, or a 5- or 6-membered substituted or unsubstituted heteroaromatic ring; Q is --O--, --S-- or a group --CXX'--; X and X', which may be the same or different, are each hydrogen, halogen, cyano, an optionally-substituted alkyl group, or a group --OR.sup.a, --SR.sup.a, or --COR.sup.b ; or one of X and X' represents hydroxy and the other is as defined above; or X and X' together represent .dbd.O or .dbd.S; R.sup.a is an optionally-substituted alkyl, aryl or acyl group; R.sup.b is an optionally-substituted alkyl or aryl group, or a group --OR.sup.c or --NR.sup.c R.sup.d ; R.sup.c and R.sup.d, which may be the same or different, are each hydrogen, or an optionally-substituted alkyl or aryl group; Y is nitrogen or a group CR.sup.9 ; R.sup.1 is an optionally-substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, benzoheterocyclyl or amino group; R.sup.Type: GrantFiled: May 6, 1994Date of Patent: September 24, 1996Assignee: Agrevo UK LimitedInventors: Peter S. Gates, Graham P. Jones, David E. Saunders
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Patent number: 5550132Abstract: 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: GrantFiled: June 22, 1994Date of Patent: August 27, 1996Assignees: 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
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Patent number: 5536837Abstract: The present invention provides an N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring represented by formula [I]: ##STR1## wherein R.sup.1 represents an alkyl group, an alkenyl group, or the like, R.sup.2 represents a hydrogen atom, an alkyl group, or the like, R.sup.3 and R.sup.4 represent independently an alkyl group, alkoxy group, or the like, and X and Y represent independently a methyne group or a nitrogen atom; or the salt of the same, a method for producing the same, and a biocide containing the same as an active ingredient. The N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring according to the present invention exhibits superior effects against blight caused by plant pathogenic fungi belonging to Oomycetes such as downy mildew, late blight, or the like in a low concentration as well as controls weeds occurring in paddy fields and plowed fields.Type: GrantFiled: May 18, 1995Date of Patent: July 16, 1996Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Ikumi Urushibata, Takumi Yoshimura, Takeshi Deguchi, Norihisa Yonekura, Junetsu Sakai, Shigeru Hayashi
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Patent number: 5527763Abstract: A herbicide containing a pyrimidine or triazine derivative of the formula (I): ##STR1## [wherein A is a furan ring, a pyrimidine ring, a 1,2,4-triazine ring or the like which may suitably be substituted, R is a hydroxyl group or a lower alkoxy group, each of R.sup.1 and R.sup.2 which may be the same or different, is a halogen atom, a lower alkyl group or a lower alkoxy group, W is an oxygen atom or a sulfur atom, and Z is nitrogen or a methine group] and its salt, as an active ingredient, is presented. The pyrimidine or triazine derivative of the present invention has excellent herbicidal effects against noxious weeds in paddy fields, upland fields and non-agricultural fields.Type: GrantFiled: December 8, 1993Date of Patent: June 18, 1996Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masahiro Miyazaki, Masafumi Matsuzawa, Takumi Yoshimura, Kuniaki Shimizu, Shigehiko Tachikawa
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Patent number: 5525724Abstract: A process for the preparation of chloropyrimidines of the formula ##STR1## in which the substituents may be alkyl, cycloalkyl, aryl or radicals containing heteroatoms, but in which at least one of the substituents R.sup.1 to R.sup.4 must be Cl, which involves:reacting a hydroxy-pyrimidine or its tautomeric keto form with phosphoryl chloride in the presence of an amine or amine hydrochloride;recovering phosphoryl chloride after the reaction by adding phosphorus pentachloride and distilling the phosphoryl chloride; andseparating the chloropyrimidine from the amine hydrochloride by addition of a solvent which will dissolve the chloropyrimidine but not the amine hydrochloride and removing the amine hydrochloride.Type: GrantFiled: February 27, 1995Date of Patent: June 11, 1996Assignee: Huels AktiengesellschaftInventor: Artur Hunds
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Patent number: 5521147Abstract: 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: GrantFiled: February 3, 1995Date of Patent: May 28, 1996Assignee: FMC CorporationInventor: George Theodoridis
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Patent number: 5516905Abstract: A method of inhibiting replication of mycoplasmal and Gram-positive bacteria is described. Useful new compounds for in vivo and in vitro inhibition and therapy for infections utilize HPUra-like compounds are also provided. These include a number of novel 3-substituted uracil and isocytosine compounds, and 10-substituted guanine and adenine compounds.Type: GrantFiled: August 30, 1994Date of Patent: May 14, 1996Assignee: University of Massachusetts Medical CenterInventors: Neal C. Brown, George Wright
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Patent number: 5514694Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula Y--CO--AA.sup.2 --AA.sup.1 --CO--NH--X. Processes for the synthesis of peptidyl .alpha.-ketoamide derivatives.Type: GrantFiled: June 24, 1993Date of Patent: May 7, 1996Assignee: Georgia Tech Research CorpInventors: James C. Powers, Zhaozhao Li, Girish S. Patil, Der-Lun Chu
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Patent number: 5514798Abstract: 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: GrantFiled: February 13, 1995Date of Patent: May 7, 1996Assignee: Gilead Sciences, Inc.Inventors: Norbert W. Bischofberger, Kenneth M. Kent
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Patent number: 5486610Abstract: 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: GrantFiled: March 17, 1994Date of Patent: January 23, 1996Assignee: Uniroyal Chemical Company, Inc.Inventors: Richard J. Strunk, Allyn R. Bell
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Patent number: 5486521Abstract: The present invention is directed to a novel class of pyrimidinyl aryl ketone oximes having excellent herbicidal and insecticidal activity.The novel compounds are represented by the structures I, Ia and Ib shown immediately below.Herbicidal activity is particularly directed against "weed-like" grasses and broadleaf weeds while the insecticidal properties are particularly active against rice planthoppers and aphids.Type: GrantFiled: March 21, 1994Date of Patent: January 23, 1996Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd., LteeInventors: Walter G. Brouwer, Alan W. Dalrymple, Ethel E. Felauer, Paul T. McDonald
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Patent number: 5475105Abstract: Abstract of the Disclosure: Compounds of the formula I ##STR1## where R.sup.1, R.sup.2, n , R.sup.3, A, X, Y and Z have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling diseases , i.e., as neuroleptics, antidepressants, sedatives, hypnotics, CNS protectives or muscle relaxants.Type: GrantFiled: December 16, 1994Date of Patent: December 12, 1995Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Liiane Unger, Berthold Behl, Hans-Juergen Teschendorf, Rainer Munschauer
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Patent number: 5475109Abstract: Dioxobutanoic acids substituted with piperidine or similar N-substituted saturated cycloalkyls are found to inhibit the cap-dependent endonuclease of influenza virus. These compounds are useful in the prevention or treatment of infection by influenza virus and the treatment of influenza, either as compound, pharmaceutically acceptable salts,. pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating influenza and methods of preventing or treating infection by influenza virus are also described.Type: GrantFiled: October 17, 1994Date of Patent: December 12, 1995Assignee: Merck & Co., Inc.Inventors: Harold G. Selnick, Gerald S. Ponticello, John J. Baldwin, Joanne E. Tomassini
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Patent number: 5470975Abstract: 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: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5461060Abstract: 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: GrantFiled: September 3, 1993Date of Patent: October 24, 1995Assignee: 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: 5461152Abstract: 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: GrantFiled: June 28, 1993Date of Patent: October 24, 1995Assignee: Ciba-Geigy CorporationInventors: Karl-Heinz Altmann, Rene Imwinkelried, Albert Eschenmoser
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Patent number: 5446013Abstract: Pyrimidinyl- or triazinyloxy- (or -thio)-carboxylic acid derivatives, processes for their preparation, and their use as herbicides or plant growth regulatorsCompounds of the formula (I) ##STR1## in which A is ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X and Y are as defined in claim 1 are suitable as selective herbicides and plant growth regulators.Type: GrantFiled: December 17, 1993Date of Patent: August 29, 1995Assignee: Hoechst AktiengesellschaftInventors: Frank Zurmuhlen, Klaus Bauer, Hermann Bieringer
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Patent number: 5439874Abstract: The invention relates to novel substituted bicyclo[3.1.0]hexanes of the formula ##STR1## in which R.sup.1 represents, e. g., hydroxyl or alkoxy,R.sup.2 to R.sup.8 represent, e. g., hydrogen or alkyl,R.sup.9 and R.sup.10 represent, e.g., methyl or methoxy,X represents, e.g., oxygen,Y represents, e.g., oxygen or sulphur andZ represents, e.g., CH or N,as well as salts of the free acid (R.sup.1 =OH) and their further functional derivatives, and furthermore to processes and novel intermediates for their preparation, and to their use as herbicides.In addition, a novel process is described for preparing certain 2-keto-bicyclo[3.1.0]hexanes, which are required as intermediates, starting from correspondingly substituted .alpha.,.beta.-unsaturated carbonyl compounds (of the methacrolein type) and .beta.-keto acid esters (of the acetoacetic acid ester type).Type: GrantFiled: July 21, 1993Date of Patent: August 8, 1995Assignee: Bayer AktiengesellschaftInventors: Mark W. Drewes, Rolf Kirsten, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5424275Abstract: Novel biphenyl derivatives represented by the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X.sup.1, X.sup.2, X.sup.3 and Y are as defined hereinafter.Type: GrantFiled: October 14, 1993Date of Patent: June 13, 1995Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Toru Uekawa, Naonori Hirata, Kazuo Saito, Hiroyuki Yogai
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Patent number: 5420099Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.Type: GrantFiled: December 21, 1992Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventor: Trevor W. Newton
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Patent number: 5411964Abstract: A phenylalanine-glycine compound of formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described. The novel conjugate of the phenylalanine-glycine compound and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered alone or as a mixture with phenylalanine.Type: GrantFiled: March 15, 1993Date of Patent: May 2, 1995Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Koichi Niimura, Takako Kawabe, Takao Ando, Kenichi Saito
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Patent number: 5401711Abstract: The present invention provides a herbicidal composition containing a novel pyrimidine derivative having the formula (1), ##STR1## wherein R.sup.1 is a trifluoromethanesulfonyioxy group, an ethenyl group which may be substituted, or an ethynyl group which may be substituted; R.sup.2 is a hydrogen atom, an alkyl group, 2-trimethylsilyl ethyl group; R.sup.3 and R.sup.4 are the same or different, and are a methoxy group or a halogen atom; X is an oxygen atom or a sulfur atom; and Z is a methine group; or its salt, as an active ingredient.The pyrimidine derivative of the present invention exhibits an excellent herbicidal effect against noxious weeds which grow in paddy fields, upland fields and non-agricultural fields.Type: GrantFiled: February 1, 1993Date of Patent: March 28, 1995Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masahiro Sato, Koichiro Kaku, Shigehiko Tachikawa