At 2-position And At 4- Or 6-position Patents (Class 544/309)
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Patent number: 6008160Abstract: The invention relates to novel substituted aminouracils of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are each as defined in the claims,to the preparation thereof and to their use as herbicides.Type: GrantFiled: February 25, 1998Date of Patent: December 28, 1999Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark Wilhelm Drewes, Markus Dollinger
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Patent number: 5962372Abstract: This invention relates to N-cyanoaryl compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z have the meanings given in the description and their use as herbicides and insecticides.Type: GrantFiled: September 24, 1996Date of Patent: October 5, 1999Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark Wilhelm Drewes, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen
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Patent number: 5959109Abstract: Ligand inhibitors for increasing levels of free corticotropin-releasing factor (CRF) in the brain. Such ligand inhibitors cause release of CRF from the CRF/CRF-binding protein complex. Administration of the ligand inhibitors provide improvement in learning and memory, result in decreased food intake and/or provide treatment for diseases associated with low levels of CRF in the brain, notably Alzheimer's disease.Type: GrantFiled: May 15, 1996Date of Patent: September 28, 1999Assignee: Neurocrine Biosciences, Inc.Inventors: Jeffrey P. Whitten, James R. McCarthy, Zhengyu Liu, Charles Q. Huang, Philip E. Erickson, Dominic P. Behan
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Patent number: 5945406Abstract: Compounds of formula (I): ##STR1## wherein: R is halogen;Y is hydrogen, NH.sub.2, SH or OH;X is: ##STR2## wherein: either R.sub.1 or R.sub.2 is a bond, with the other being hydrogen;either R.sub.3 or R.sub.4 is hydrogen, with the other being hydrogen, OH, OAc or NHAc;R.sub.5 is OH or OAc;either R.sub.7 or R.sub.8 is hydrogen, with the other being OH or OAc;R.sub.9 is hydrogen, CH.sub.2 OH or CH.sub.2 OAc;with the proviso that when R.sub.4 is OH, OAc or NHAc then R.sub.8 is hydrogen;and enantiomers of such compounds, are disclosed. Pharmaceutical formulations comprising such compounds, their use in the treatment of various disease states, and methods of treatment employing the compounds are also provided.Type: GrantFiled: December 23, 1997Date of Patent: August 31, 1999Assignee: Oxford Glycosciences (UK) Ltd.Inventor: Stephen Martin Courtney
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Patent number: 5935907Abstract: The invention is related to a novel phenylacetylene derivates of formula: ##STR1## wherein X represents hydrogen, halogen, optionally substituted C.sub.1-6 alkyl; Y represents hydrogen, halogen, cyano, nitro, optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkoxy, optionally substituted C.sub.1-6 alkylthio, C.sub.3-8 cycloalkylthio, C.sub.1-6 alkylsulfinyl, optionally substituted C.sub.1-6 alkylsulfonyl, C.sub.3-8 cycloalkylsulfonyl, C.sub.1-6 alkylsulfonyloxy, optionally substituted sulfonamide, optionally substituted carboxamide, etc., or Y may form together with Z which is bonded to the vicinal carbon atom a 5- or 6-membered ring; n is 0 or 1; Z represents hydrogen or halogen; m is 1 or 2; R represents hydrogen, halogen, C.sub.1-6 alkyl, tri(C.sub.1-6 alkyl)silyl, COOR.sup.c or CONR.sup.d R.sup.e ; Q represents a heterocyclic group, and their use as herbicid.Type: GrantFiled: March 24, 1998Date of Patent: August 10, 1999Assignee: Nihon Bayer Agrochem K.K.Inventors: Akihiko Yanagi, Shin-ichi Narabu, Toshio Goto, Seishi Ito, Natsuko Minegishi, Tatsuya Yamaoka, Chieko Ueno
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Patent number: 5932730Abstract: Carboxylic acid derivatives ##STR1## where R-R.sup.6, 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.Type: GrantFiled: March 27, 1997Date of Patent: August 3, 1999Assignee: BASF AktiengesellschaftInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: 5929046Abstract: The present invention provides certain 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR1## wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hetero atom chosen from O, N, or S, or a substituted derivative thereof; or (ii) phenyl or a substituted derivative thereof,R.sup.2 is selected from H, C.sub.1 -C.sub.5 alkyl, halogen or NH.sub.2,R.sup.4 and R.sup.5 which are the same or different are selected fromH, NH.sub.2 or NO.sub.n where n=1 or 2, or R.sup.4 and R.sup.5 together with the pyrimidine ring form a 5-or 6-membered ring structure containing one or more heterocyclic atoms, and pharmaceutically acceptable salts thereof, exhibit the ability to deplete O.sup.6 -alkylguanine-DNA alkyltransferase (ATase) activity.Type: GrantFiled: December 15, 1995Date of Patent: July 27, 1999Assignee: Cancer Research Campaign Technology LimitedInventors: Thomas Brian Hamilton McMurry, Robert Stanley McElhinney, Dorothy Josephine Donnelly, Paul Murray, Christophe Carola, Rhoderick Hugh Elder, Jane Kelly, Geoffrey Paul Margison, Joseph Anthony Rafferty, Amanda Jean Watson, Mark Andrew Willington
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Patent number: 5919732Abstract: There are described novel substituted 3-arylamino-6-trifluoromethyluracils of the formula I, processes for their preparation, and methods of controlling monocotyledonous and dicotyledonous harmful plants in agricultural and silvicultural crops. ##STR1## In formula I, the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are not only hydrogen, alkyl and haloalkyl, but can also have further meanings, R.sup.5 is alkyl or amino, and X is CH or N.Type: GrantFiled: February 9, 1998Date of Patent: July 6, 1999Assignee: Hoechst Schering AgrEvo GmbHInventors: Reinhold Puttner, Jurgen Bohner, Hansjorg Krahmer
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Patent number: 5914399Abstract: A method for producing 5-isopropyluracil at a high yield in a short time, wherein N-(2-cyano-3-methylbutanoyl)urea is reduced in a 10-15% aqueous sulfuric acid solution in the presence of palladium carbon at 30-45.degree. C., heated for ring closure reaction and added to a 50-70% aqueous sulfuric acid solution to give 5-isopropyluracil having a high purity.Type: GrantFiled: October 20, 1998Date of Patent: June 22, 1999Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Hiroki Ueno, Michio Matsuda, Susumu Nishizawa
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Patent number: 5912261Abstract: Carboxyalkyl heterocyclic derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component are useful pharmaceuticals for the treatment of diabetic complications such as diabetic neuropathy, diabetic cataracts and retinopathy, diabetic nephropathy, diabetic dermopathy, and other diabetic microangiopathy. The compounds of the present invention are represented by the following general formula (A): ##STR1## The compounds of the present invention exhibit excellent inhibitory action towards aldose reductase with a high enzyme selectivity. Accordingly, they are useful as drugs for the therapy and prevention of various types of diabetic complications without substantially inhibiting aldehyde reductase.Type: GrantFiled: December 19, 1995Date of Patent: June 15, 1999Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Takayuki Kotani, Kaoru Okamoto, Yasuhiro Nagaki
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Patent number: 5889014Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds have the formula: ##STR1## wherein: R.sub.1 and R.sub.2 may be the same or different and each is selected from the group consisting of hydrogen, saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety;R.sub.3 is hydrogen, halogen, or a saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl group, a cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 7 carbon atoms in the cycloalkyl moiety;R.sub.Type: GrantFiled: September 20, 1996Date of Patent: March 30, 1999Assignee: Euro-Celtique, S.A.Inventors: David John Cavalla, Lloyd J. Dolby, Mark Chasin
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Patent number: 5888940Abstract: Substituted benzothiazoles I and their salts ##STR1## used as herbicides and for the desiccation/abscission of plants.Type: GrantFiled: February 17, 1998Date of Patent: March 30, 1999Assignee: BASF AktiengesellschaftInventors: Elisabeth Heistracher, Gerhard Hamprecht, Olaf Menke, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Patent number: 5877181Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: August 13, 1997Date of Patent: March 2, 1999Assignee: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Patent number: 5874467Abstract: The present invention relates to phenylacetic acid derivatives of the formula I ##STR1## and their salts. The invention additionally relates to processes and intermediates for preparing these compounds and compositions containing them for controlling animal pests and harmful fungi.Type: GrantFiled: July 31, 1996Date of Patent: February 23, 1999Inventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5817664Abstract: The present invention relates to a group of 5-substituted uracil derivatives which are inactivators of uracil reductase and which are particularily useful in cancer chemotherapy, especially in combination with antimetabolite antineoplastic agents such as 5-fluorouracil (5-FU).Type: GrantFiled: June 6, 1995Date of Patent: October 6, 1998Assignee: Glaxo Wellcome Inc.Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
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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: 5807864Abstract: This invention relates to the use of 2-thioxotetrahydropyrimidin-4-one derivatives to increase HDL cholesterol concentration and as therapeutic compositions for treating atherosclerotic conditions such as dyslipoproteinemias and coronary heart disease. The compounds of this invention are represented by the formula: ##STR1## wherein: R is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkynyl; andR.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, halogen or lower alkyl.Type: GrantFiled: February 27, 1997Date of Patent: September 15, 1998Assignee: American Home Products CorporationInventors: Sie-Yearl Chai, Hassan M. Elokdah, Theodore S. Sulkowski
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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: 5780630Abstract: The compound 1 -methyl-6-trifluoromethyl-2,4(1H,3H)-pyrimidinedione is a novel compound useful in the preparation of pesticidal uracils. A route to the compound is disclosed, as is its use to prepare a known herbicide.Type: GrantFiled: May 30, 1997Date of Patent: July 14, 1998Assignee: FMC CorporationInventor: John W. Lyga
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Patent number: 5780506Abstract: The present invention relates to phenylacetic acid derivatives of the formula I ##STR1## and their salts. The invention additionally relates to processes and intermediates for preparing these compounds and compositions containing them for controlling animal pests and harmful fungi.Type: GrantFiled: July 31, 1996Date of Patent: July 14, 1998Inventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5763606Abstract: The present invention relates to a process for producing predominantly pure cis nucleoside analogues of formula (I), wherein X is S, or O; Y is S, CH.sub.2, O or CH(R); wherein R is azido or halogen; and R.sub.2 is a purine or pyrimidine base; via the coupling of a silylated purine or pyrimidine base in the presence of an appropriate Lewis acid with a bicyclic intermediate of formula (III) wherein Z is S or O; followed by conversion of the resulting intermediate of formula (II) to an alkyl ester and reduction to yield a compound of formula (I).Type: GrantFiled: February 2, 1995Date of Patent: June 9, 1998Assignee: BioChem Pharma, Inc.Inventors: Tarek S. Mansour, Colleen A. Evans, Haolun Jin, M. Arshad Siddiqui, Allan H. L. Tse
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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: 5750532Abstract: 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, dihydrofuraType: GrantFiled: May 30, 1995Date of Patent: May 12, 1998Assignee: Schering CorporationInventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
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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: 5747473Type: GrantFiled: August 18, 1995Date of Patent: May 5, 1998Assignee: Medivir ABInventors: Bjorn Olof Classon, Bengt Bertil Samuelsson, Ingemar Sven-Anders Kvarnstrom, Lars Goran Svansson, Stefan Carl Tore Svensson
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Patent number: 5744475Abstract: The invention relates to novel uracil derivatives having excellent inhibiting effects of human derived thymidine phosphorylase and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators, antitumor agents containing such novel compounds, and a process for their preparation and use is described.Type: GrantFiled: November 21, 1996Date of Patent: April 28, 1998Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Shingo Yano, Yukio Tada, Hideki Kazuno, Tsutomu Sato, Junichi Yamashita, Norihiko Suzuki, Tomohiro Emura, Masakazu Fukushima, Tetsuji Asao
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Patent number: 5728833Abstract: 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: GrantFiled: August 4, 1994Date of Patent: March 17, 1998Assignee: Zeneca LimitedInventors: Michael Drysdale Turnbull, Nigel James Willetts, Steven Fitzjohn, Prafula Govind Kholia, Alison Mary Smith, Roger Salmon, Harjinder Singh Bansal
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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: 5723412Abstract: 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: GrantFiled: July 13, 1995Date of Patent: March 3, 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: 5719132Abstract: The present invention is directed to the use of pharmaceutical compositions containing anti-retroviral effective amounts of (a) d4T and (b) 5-fluorouracil or a prodrug, or salt thereof.Type: GrantFiled: June 27, 1996Date of Patent: February 17, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Pin-Fang Lin, Yi-Fei Gong
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Patent number: 5717096Abstract: A novel process for the preparation of a 2-alkoxy-6-(trifluoromethyl)pyrimidin-4-ol of the general formula: ##STR1## in which R is a C.sub.1 -C.sub.8 -alkyl group. In the process, cyanamide is reacted with the appropriate alcohol in the presence of hydrogen chloride to give the corresponding alkoxyisourea hydrochloride, which is then converted with ethyl trifluoroacetoacetate in the presence of an alkali metal hydroxide, which is in water, to the end product of the formula I.Type: GrantFiled: March 25, 1997Date of Patent: February 10, 1998Assignee: Lonza AGInventors: Beat Schmidt, Gerhard Stucky
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Patent number: 5714499Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 17, 1994Date of Patent: February 3, 1998Assignee: Corvas International, Inc.Inventors: Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
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Patent number: 5714606Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.Type: GrantFiled: August 15, 1996Date of Patent: February 3, 1998Assignee: ISIS Pharmaceuticals, Inc.Inventors: Oscar L. Acevedo, Normand Hebert
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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: 5700295Abstract: The invention relates to compounds of formula ##STR1## wherein the variables have the meanings given in the claims. The compounds are suitable for use as UV absorbers for the photochemical stabilisation of undyed, dyed or printed textile fiber materials and for enhancing the sun protection factor thereof.Type: GrantFiled: October 11, 1995Date of Patent: December 23, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Francesco Fuso, Gerhard Reinert
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Patent number: 5686456Abstract: The present invention provides methods for treating Pneumocystis carinii pneumonia in a subject in need of such treatment. The methods comprise administering to a subject in need thereof, a pyrimidine of Formula I. ##STR1## wherein the variables are as defined in the specification.Type: GrantFiled: November 28, 1995Date of Patent: November 11, 1997Assignees: The University of North Carolina, Georgia State University Research Foundation, Inc., Auburn UniversityInventors: David W. Boykin, Christine C. Dykstra, Richard R. Tidwell, James E. Hall, W. David Wilson, Arvind Kumar
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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: 5684011Abstract: The invention provides novel compounds of formula (I) having nematicidal, insecticidal, acaricidal and fungicidal properties, compositions comprising them and processes and intermediates for their preparation: ##STR1## wherein R.sup.1 is --S(O).sub.n CH.sub.2 CH.sub.2 CH.dbd.CF.sub.2 ;n is selected from 0, 1 and 2;R.sup.2, R.sup.3, and R.sup.4 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted aryloxy, optionally substituted arylalkoxy, alkoxy, alkenyloxy, alkynyloxy, hydroxyalkyl, alkoxyalkyl, alkylthio, alkenylthio, alkynylthio, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkenyloxy, haloalkynyloxy, haloalkylthio, haloalkenylthio, haloalkynylthio, halogen, hydroxy, cyano, nitro, --NR.sup.5 R.sup.6, --NR.sup.7 COR.sup.8, --NR.sup.9 SO.sub.2 R.sup.10, --N(SO.sub.2 --R.sup.11)(SO.sub.2 --R.sup.12), --COR.sup.13, --CONR.sup.14 R.sup.15, --COOR.sup.16, --OCOR.sup.17, --OSO.Type: GrantFiled: May 24, 1996Date of Patent: November 4, 1997Assignee: Zeneca LimitedInventors: Steven Fitzjohn, Michael Peter Robinson, Michael Drysdale Turnbull
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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: 5681794Abstract: 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: GrantFiled: September 30, 1994Date of Patent: October 28, 1997Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark-Wilhelm Drewes, Albrecht Marhold, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5658930Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 7, 1995Date of Patent: August 19, 1997Assignee: Corvas International, Inc.Inventors: Susan Yoshiko Tamura, Joseph Edward Semple, William Charles Ripka, Robert John Ardecky, Yu Ge, Stephen H. Carpenter, Terence K. Brunck
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Patent number: 5656645Abstract: The present invention discloses heterocyclic aromatic peptide aldehydes which have an oxopyrimidine or oxopyridine group and an argininal tail which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: Corvas International, Inc.Inventors: Susan Yoshiko Tamura, Joseph Edward Semple, William Charles Ripka, Robert John Ardecky, Yu Ge, Stephen H. Carpenter, Terence K. Brunck
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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: 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: 5593945Abstract: 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: GrantFiled: August 11, 1994Date of Patent: January 14, 1997Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark-Wilhelm Drewes, Albrecht Marhold, Hans-Joachim Santel, Markus Dollinger
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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: 5545835Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pylidinedicarboxylic acids.Type: GrantFiled: November 4, 1994Date of Patent: August 13, 1996Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5543147Abstract: A crystalline modification of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine prepared by cooling a solution of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine in water, an organic solvent or in a mixture thereof with a cooling agent at a rate not below 6.degree. C./min to crystallization followed by separation of the obtained crystals and drying them. The crystalline modification has high antiinflammatory and wound-healing activity and is an active substance in medicaments used for treatment of burns and wounds of various organs.Type: GrantFiled: November 17, 1994Date of Patent: August 6, 1996Assignee: Nikolai B. LeonidovInventors: Nikolai B. Leonidov, Nikolai G. Selezenev