Sulfur Attached Indirectly To The Diazine Ring By Nonionic Bonding (e.g., Thiamines, Etc.) Patents (Class 544/327)
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Patent number: 6150370Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: ##STR1## where Ar, W, X, Y, Z, R.sub.1 and R.sub.2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.Type: GrantFiled: August 26, 1997Date of Patent: November 21, 2000Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
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Patent number: 6136971Abstract: The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M.sub.1 XCH.sub.2 CH.sub.2 YR.sub.5 and removing the protecting group, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, Z, X, Y, M, M.sub.1 and W are defined herein.Type: GrantFiled: July 15, 1999Date of Patent: October 24, 2000Assignee: Roche Colorado CorporationInventors: Peter J. Harrington, Hiralal N. Khatri, Bradley S. Dehoff
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Patent number: 6103902Abstract: The present invention is concerned with a novel process for the carbamoylation of substituted pyridines, especially with a process for the preparation of compounds of formula I ##STR1## wherein R.sup.4 to R.sup.8 represent hydrogen, lower-alkoxy or halogen; or optionally salts thereof.Type: GrantFiled: August 9, 1999Date of Patent: August 15, 2000Assignee: Hoffmann-La Roche Inc.Inventor: Uwe Klinkhammer
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Patent number: 6096768Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: April 29, 1999Date of Patent: August 1, 2000Assignee: Rhone-Poulenc Rorer LimitedInventors: Michael John Ashton, David Charles Cook, Garry Fenton, Susan Jacqueline Hills, Ian Michael McFarlane, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Nigel Vicker
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Patent number: 6096751Abstract: The present invention relates to new substituted 1, 2, 3, 4-tetrahydro-5-nitro-pyrimidines of the formula (I) ##STR1## wherein Het, R.sup.1, R.sup.2, R.sup.3 and A are as defined herein,to processes for their preparation, and to their use as pesticides and ectoparasiticides.Type: GrantFiled: May 7, 1999Date of Patent: August 1, 2000Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Hermann Uhr, Johannes Kanellakopulos, Ernst-Rudolf Gesing, Hilmar Wolf, Andreas Turberg, Norbert Mencke, Christoph Erdelen, Ulrike Wachendorff-Neumann, Jurgen Hartwig
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Patent number: 6093718Abstract: This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.Type: GrantFiled: February 12, 1999Date of Patent: July 25, 2000Assignee: Zeneca LimitedInventors: David Waterson, Elaine Sophie Elizabeth Stokes, George Robert Brown, Nicholas John Newcombe
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Patent number: 6083955Abstract: Novel arylethenesulfonamide derivative having a high affinity for drugs, especially endoserine receptors, and represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs comprising the same as the active ingredient, especially endoserine receptor antagonist, whereinAr: optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group;X: oxygen atom, sulfur atom or a group represented by a formula --NH--;Y: oxygen atom or sulfur atom;R.sub.1 : hydrogen atom, optionally halogen-substituted lower alkyl group, cycloalkyl group, optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group.R.sub.2 : lower alkyl group, lower alkenyl group or lower alkynyl group where each of which may be substituted with one to three substituent(s) selected from a group consisting of hydroxyl group, lower alkoxy group, cycloalkyl group, halogen atom, carboxyl group and lower alkoxycarbonyl group;R.sub.Type: GrantFiled: June 19, 1998Date of Patent: July 4, 2000Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hironori Harada, Jun-ichi Kazami, Susumu Watanuki, Ryuji Tsuzuki, Katsumi Sudou, Akihiro Tanaka
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Patent number: 6060468Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, p, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.Type: GrantFiled: October 3, 1997Date of Patent: May 9, 2000Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
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Patent number: 6054459Abstract: The present invention relates to new substitued 1,2,3,4-tetrahydro-5-nitro-pyrimidines of the formula (I) ##STR1## in which Het represents optionally substituted pyridyl or thiazolyl,R.sup.1 represents C.sub.1-4 -alkyl,R.sup.2 represents C.sub.1-4 -alkyl,R.sup.1 and R.sup.2 together with the adjacent atoms form a saturated 5- or 6-membered ring which optionally contains N or O as further hetero atom and which is optionally substituted,A represents straight-chain or branched alkylene having at least 2 C atoms which is optionally substituted by phenyl, halogen, OH, CN or the radical NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 represent hydrogen, C.sub.1-4 -alkyl or phenyl, and which is optionally interrupted,R.sup.3 represents one of the radicals ##STR2## wherein the variables are herein below defined.Type: GrantFiled: October 23, 1998Date of Patent: April 25, 2000Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Hermann Uhr, Johannes Kanellakopulos, Ernst-Rudolf Gesing, Hilmar Wolf, Andreas Turberg, Norbert Mencke, Christoph Erdelen, Ulrike Wachendorff-Neumann, Jurgen Hartwig
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Patent number: 6046330Abstract: This invention relates to complexes of ultraviolet absorbers with quaternary ammonium compounds which are substantially free from unwanted salts. Such complexes are formed through ionic bonds formed between the two compounds. The inventive complexes are then removed of substantially all excess inorganic salt so as to obtain an UV absorber compound which exhibits improved light- and washfastness properties, which easily coats subject surfaces, which provides excellent non-fogging and non-cracking characteristics, and which also possesses anti-static, anti-microbial, and anti-abrasion properties. This invention also concerns methods of making and utilizing such inventive ultraviolet absorbing complexes.Type: GrantFiled: April 24, 1998Date of Patent: April 4, 2000Inventors: Jessica Ann Qinghong, Edward Zhao Ziaodong
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Patent number: 6043248Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sub.4 is selected from the group consisitng of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase.Type: GrantFiled: October 17, 1997Date of Patent: March 28, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Gary J. Cleek, David R. Graber
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Patent number: 6030976Abstract: The present invention is concerned with compounds of formula I ##STR1## wherein Z, R.sup.1 and R.sup.2 are as defined herein, as well as their pharmaceutically acceptable salts as therapeutically active substances against central nervous system disorders and for the production of corresponding medicaments.Type: GrantFiled: June 3, 1998Date of Patent: February 29, 2000Assignee: Hoffman-La Roche Inc.Inventors: Michael Bos, Thierry Godel, Claus Riemer, Andrew Sleight
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Patent number: 6024937Abstract: The present invention provides aromatic amine substituted metal chelating compounds, chelates and chelate-targeting moiety conjugates formed from the chelating compounds, and methods for making and using these compounds. Metals capable of being chelated by the chelating compounds include radionuclides, such as .sup.99m Tc and .sup.186188 Re.Type: GrantFiled: June 5, 1995Date of Patent: February 15, 2000Assignee: NeoRx CorporationInventors: Sudhakar Kasina, Eric Yau, John M. Reno
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Patent number: 5935978Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: July 28, 1993Date of Patent: August 10, 1999Assignee: Rhone-Poulenc Rorer LimitedInventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Michael John Ashton, David Charles Cook, Susan Jacqueline Hills, Ian Michael McFarlane, Nigel Vicker
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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: 5922726Abstract: The novel 6-thienyl pyridines and 4-thienyl pyrimidines of formula I: ##STR1## (A, R.sub.1 to R.sub.5 and Z are defined in the specification) show selective herbicidal activity.The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.Type: GrantFiled: July 15, 1997Date of Patent: July 13, 1999Assignee: American Cyanamid CompanyInventors: Stefan Scheiblich, Thomas Maier, Helmut Siegfried Baltruschat, Joseph Luke Pont
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Patent number: 5919928Abstract: A phenanthridine derivative metal complex of formula 1 having a large absorption in the near-infrared range and a reduced absorption in the visible range, which phenanthridine derivative metal complex is used in a transparent recording medium: ##STR1## where M is a metal atom, and X is a negative ion.Type: GrantFiled: September 18, 1997Date of Patent: July 6, 1999Assignee: Nippon Paper Industries, Co., Ltd.Inventors: Reiji Ohashi, Yukiko Ryu, Tomoaki Nagai, Hidetoshi Yoshioka
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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: 5889012Abstract: Substituted cycloalkylamino and cycloalkoxy heterocycles, processes for preparing them and their use as pesticides The invention relates to (I) ##STR1## in which R.sup.1 to R.sup.5, A, X, E, U, p and n are as defined in claim 1, to processes for their preparation and their use as pesticides, such as insecticides, acaricides and fungicides.Type: GrantFiled: October 16, 1995Date of Patent: March 30, 1999Assignee: Hoechst-Schering AgrEvo GmbHInventors: Martin Markl, Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin, Adolf Linkies, Dieter Bernd Reuschling
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Patent number: 5883253Abstract: The invention relates to a process for the prepn of ortho-sulfocarboxylic acids, which comprises: a) in a first reaction step, diazotizing an aromatic o-aminosulfonic acid in the presence of an acid and nitrite in water, in an organic solvent or in a mixture thereof, to an o-diazonium sulfonate, and, b) in a second reaction step, reacting the o-diazonium sulfonate in the presence of a palladium catalyst in water, in an organic solvent or in a mixture thereof, with carbon monoxide, under overpressure, to an aromatic o-sulfocarboxylic acid. The invention also relates to a process for the preparation of sulfonylureas using o-sulfocarboxylic acids as intermediates. Thus, 4-methoxyaniline-2-sulfonic acid was diazotized and treated with CO to give 97% 4-methoxybenzoic acid 2-sulfonic acid.Type: GrantFiled: June 19, 1997Date of Patent: March 16, 1999Assignee: Novartis AGInventors: Urs Siegrist, Manfred Muller, Jean Brunisholz
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Patent number: 5880130Abstract: The invention concerns pyrimidine derivatives of formula wherein m is 1, 2 or 3; each R.sup.1 is independently hydrogen, hydroxy, (un)substituted amino, nitro, halogeno, cyano, carboxy, (un)substituted carbamoyl, ureido, (1-4C) alkoxycarbonyl, (un)substituted (1-4C)alkyl, (un)substituted (1-4C)alkoxy, (1-3C)alkylenedioxy, (1-4C)alkylthio, (1-4C)alkylsulphinyl, (1-4C)alkyl-sulphonyl, (2-4C)alkanoyloxy; n is 1, 2 or 3; and each R.sup.2 is independently hydrogen, hydroxy, halogeno, trifluoromethyl, trifluoromethoxy, amino, nitro, cyano, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkylamino, di-?(1-4C)alkyl!amino, (1-4C)alkylthio, (1-4C)alkylsulphinyl, (1-4C)alkylsulphonyl, (2-4C)alkanoylamino, (2-4C)alkanoyl or (1-3C)alkylenedioxy; or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of cell-proliferation diseases.Type: GrantFiled: June 7, 1996Date of Patent: March 9, 1999Assignee: Zeneca LimitedInventor: Andrew Peter Thomas
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Patent number: 5877120Abstract: A nicotinic acid derivative represented by general formula (I) or (II), a salt thereof, and a herbicide containing the same as the active ingredient, wherein A represents substituted phenyl, or 5- or 6- membered heterocycle, e.g., thienyl or pyridyl; R represents hydroxy, optionally substituted alkoxy or optionally substituted benzyloxy; R.sup.1 and R.sup.2 represent each independently alkoxy or halogen; R.sup.3 and R.sup.4 represent each independently hydrogen, hydroxy, cyano or alkoxycarbonyl, or they may be combined together to represent oxygen; X represents halogen, alkyl or alkoxy; n represents 0, 1 or 2; and Z represents methine or nitrogen. The compound and salts thereof can control annual or perennial weed growing on the land where various crops such as rice plant, wheat, cotton and corn grow for a wide period ranging from the pre-emergence to growth in a remarkably small dose.Type: GrantFiled: September 18, 1996Date of Patent: March 2, 1999Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masahiro Miyazaki, Sumio Yokota, Yoshihiro Ito, Nobuyuki Ohba, Nobuhide Wada, Shigehiko Tachikawa, Takeshige Miyazawa
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Patent number: 5869084Abstract: Multi-vitamin and mineral supplements for administration to lactating, non-lactating, and menopausal women, which comprise specific regimens of critical nutritional agents. The supplements are specifically tailored to meet nutritional requirements and maintain a woman's health during each stage of life.Type: GrantFiled: June 7, 1995Date of Patent: February 9, 1999Assignee: K-V Pharmaceuticals Co.Inventors: George N. Paradissis, R. Saul Levinson, Gary Heeter, Robert C. Cuca, Patrick Paul Vanek
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Patent number: 5852023Abstract: Cyclohexylamino and cycloalkoxy nitrogen heterocycles, processes for their preparation, and their use as pesticides and fungicides.The invention relates to compounds of the formulaAr--X-E-Qin which Ar is substituted or unsubstituted 4-pyridyl or 4-pyrimidinyl; X is NH, O, S, SO or SO.sub.2 ; E is a bond or alkanediyl; and Q is a substituted cycloalkyl or 4-piperidyl.The invention also relates to processes and intermediates for their preparation, to compositions comprising them and to their use as pesticides and fungicide.Type: GrantFiled: March 27, 1996Date of Patent: December 22, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Wolfgang Schaper, Gerhard Krautstrunk, Werner Knauf, Ulrich Sanft, Manfred Kern, Sergej Pasenok, Dieter Bernd Reuschling, Adolf Heinz Linkies, Werner Bonin
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Patent number: 5824624Abstract: New herbicidal pyridine and pyrimidine derivatives of general formula (I), ##STR1## wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R.sup.1 or each R.sup.1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R.sup.2 or each R.sup.2 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.Type: GrantFiled: December 6, 1996Date of Patent: October 20, 1998Assignee: American Cyanamid CompanyInventors: Axel Kleeman, Helmut Siegfried Baltruschat, Thelka Hulsen
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Patent number: 5780473Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin.Type: GrantFiled: July 25, 1996Date of Patent: July 14, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
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Patent number: 5773616Abstract: Disclosed are compounds encompassed by the following general formula: ##STR1## wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; andR.sub.5 and R.sub.6 is are optionally substituted organic substituents; orNR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various orgainic or inorganic groups,which compounds can be used in the treatment of neuropsychological disorders.Type: GrantFiled: June 5, 1995Date of Patent: June 30, 1998Assignee: Neurogen CorporationInventors: Jun Yuan, Andrew Thurkauf
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Patent number: 5760038Abstract: Compounds of the formula ##STR1## in which the symbols are as defined herein, inhibit the activity of endothelin.Type: GrantFiled: February 6, 1995Date of Patent: June 2, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
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Patent number: 5747423Abstract: The novel 6-thienyl pyridines and 4-thienyl pyrimidines of formula I: ##STR1## (A, R.sub.1 to R.sub.5 and Z are defined in the specification) show selective herbicidal activity.The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.Type: GrantFiled: July 15, 1996Date of Patent: May 5, 1998Assignee: American Cyanamid CompanyInventors: Stefan Scheiblich, Thomas Maier, Helmut Siegfried Baltruschat, Joseph Luke Pont
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Patent number: 5739333Abstract: Novel sulfonamide derivatives of the formula ?I!: ##STR1## wherein Ring A and Ring B are substituted or unsubstituted monocyclic, bicyclic or tricyclic hydrocarbon, or substituted or unsubstituted heterocyclic group, Q is single bond, --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is --0--, --S-- or --NH--, Alk is lower alkylene or alkenylene, Z is --O-- or --NH --, R is substituted or unsubstituted aromatic heterocyclic or aryl, R.sup.1 is H, substituted or unsubstituted amino, substituted or unsubstituted lower alkyl, alkenyl, alkynyl, substituted or unsubstituted lower alkylthio, or alkoxy, or substituted or unsubstituted heterocyclic or aryl, or pharmaceutically acceptable salts thereof, which are useful in the prophylaxis or treatment of disorders associated with endothelin activities such as hypertension, pulmonary hypertension, renal hypertension, Raynaud disease, bronchial asthma, gastric ulcer, chronic heart failure, etc.Type: GrantFiled: May 9, 1996Date of Patent: April 14, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
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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: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
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Patent number: 5712393Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.Type: GrantFiled: November 24, 1995Date of Patent: January 27, 1998Assignee: SynthelaboInventors: Jean Michel Altenburger, Gilbert Lassalle
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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: 5698694Abstract: A process for preparation of substituted phthalides, heterocyclic phthalides and derivatives thereof by reacting an aromatic carboxylic acid mono- or di-anion with a reactive derivative of a pyrimidine carboxylic acid.Type: GrantFiled: October 25, 1996Date of Patent: December 16, 1997Assignee: Sandoz Ltd.Inventors: Takeo Hokama, Ian S. Cloudsdale, Werner Langer, Hermann Schneider
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Patent number: 5696053Abstract: Salts of the formula (I) ##STR1## in which n is 0, 1, 2 or 3,R is halogen, alkyl or alkoxy, mainly in each case independently of other substituents R in the event that n is greater than 1,R.sup.1 is a substituted or unsubstituted hydrocarbon radical or a substituted or unsubstituted heterocyclic radical,R.sup.2 is an acyl radical,R.sup.3 is hydrogen or C.sub.1 -C.sub.5 -alkyl,M.sym. is a metal or ammonium ion,X and Y independently of one another are halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or C.sub.1 -C.sub.6 -alkylthio, each of the three last-mentioned radicals being unsubstituted or substituted by one or more radicals selected from the group consisting of halogen, C.sub.1 -C.sub.4 -alkoxy and C.sub.1 -C.sub.4 -alkylthio, or are C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.6 -alkynyloxy, mono- or di(C.sub.1 -C.sub.Type: GrantFiled: May 30, 1995Date of Patent: December 9, 1997Assignee: Hoechst AktiengesellschaftInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 5677310Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl-S-, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.Type: GrantFiled: February 5, 1996Date of Patent: October 14, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck
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Patent number: 5668140Abstract: Substituted 4-aminopyrimidines, processes for their preparation, and their use as pesticidesThe invention relates to substituted 4-aminopyrimidines of the formula ##STR1## in which: R.sup.1 is hydrogen, halogen, alkyl or cycloalkyl,R.sup.2 is hydrogen, alkyl, halogen, trifluoromethyl, alkoxy, haloalkoxy, alkoxyalkyl, alkylthio, alkylthioalkyl, alkylamino, dialkylamino or cycloalkylamino,R.sup.3 is hydrogen, alkyl, alkoxy, haloalkoxy, alkylthio, halogen, nitro or dialkylamino,R.sup.4 is hydrogen or optionally substituted carbamoyl;R.sup.5 is hydrogen, (C.sub.1 -C.sub.8)alkyl or (C.sub.3 -C.sub.6)cycloalkyl; andQ has the meaning defined in the description, and their salts. The invention furthermore relates to processes for their preparation and to their use as pesticides.Type: GrantFiled: June 5, 1995Date of Patent: September 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Gerhard Salbeck, Heinz Ehrhardt, Peter Braun, Werner Knauf, Burghard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen
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Patent number: 5646269Abstract: The present invention is directed to improved methods to synthesize oligonucleotide analogs having an acetal linkage, such as a 3',5'-formacetal (3' --O--CH.sub.2 --O-- 5'), 3',5'-thioformacetal (3' --S--CH.sub.2 --O-- 5') or an analogous 2',5' linkage between adjacent nucleoside analog residues. Compositions comprising 5', 3' and 2' phosphinate nucleoside analogs useful in the methods are also provided.Type: GrantFiled: April 28, 1994Date of Patent: July 8, 1997Assignee: Gilead Sciences, Inc.Inventors: Mark D. Matteucci, Jiancun Zhang
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Patent number: 5616537Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## (wherein R is a hydroxyl group, R.sup.3 or R.sup.4 is an alkoxy group, W is an oxygen atom, Yn is a hydrogen atom, Z is a methine group, and A is a 5- or 6-membered heterocyclic ring which may be substituted, and a herbicide, are presented. When used for paddy field treatment, upland soil treatment and foliage treatment, the condensed heterocyclic derivative of the present invention exhibits excellent herbicidal activities against gramineous and non-gramineous weeds without adversely affecting crop plants.Type: GrantFiled: March 1, 1994Date of Patent: April 1, 1997Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Sumio Yokota, Masafumi Matsuzawa, Nobuyuki Ohba, Toshihiro Nagata, Shigehiko Tachikawa, Takeshige Miyazawa, Katsutada Yanagisawa
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Patent number: 5610304Abstract: Sulfonamide compounds of formula (I) or a pharmacologically acceptable salt thereof: ##STR1## exhibit excellent antitumor activity and low toxicity.Type: GrantFiled: May 26, 1995Date of Patent: March 11, 1997Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
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Patent number: 5604181Abstract: Herbicidal compounds of formula (I) and salts thereof, where A is --N.dbd. or --CH.dbd.; X is --OH, --OR.sup.10, --SH, --SR.sup.10, --SCN, NH.sub.2, --NHacyl, --CH.sub.2 OH, --CH.sub.2 OR.sup.9 or --CN; R.sup.1 and R.sup.2, which may be the same or different, each represent alkyl, alkoxy, haloalkyl, haloalkoxy, halo, alkylamino or dialkylamino; R.sup.3 is --CN, --COOR.sup.5, --CONR.sup.6 R.sup.7, --CSNH.sub.2, --CHO, --CH.dbd.Z, --CH(Oalkyl).sub.2, --CH.sub.2 OH, --CH.sub.2 OR.sup.9, --COSR.sup.4a, --CS.sub.2 R.sup.4a, or a substituted or unsubstituted 5- or 6-membered heterocyclic group linked via a ring carbon atom which is between two ring heteroatoms; R.sup.4 and R.sup.4a, which may be the same or different, are each H, or a substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl or heteroaryl group; R.sup.Type: GrantFiled: March 8, 1995Date of Patent: February 18, 1997Assignee: Agrevo UK LimitedInventors: Thomas L. Hough, Peter S. Gates
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Patent number: 5595992Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH Or S(O).sub.q where q=0, 1 or 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.Type: GrantFiled: September 12, 1994Date of Patent: January 21, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Rainer Preuss, Wolfgang Schaper, Martin M arkl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
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Patent number: 5585381Abstract: A pyrimidine derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, or --NHR.sup.11 group; R.sup.2 is a hydrogen or halogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, --(CH.sub.2).sub.m C.sub.6 H.sub.5, --NH.sub.2, --NHR.sup.12, --NH(CH.sub.2).sub.n C.sub.6 H.sub.5, --NH(CH.sub.2).sub.p C.sub.6 H.sub.4 --OR.sup.13, --N(R.sup.14)(CH.sub.2).sub.q C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.15, --NHC(.dbd.O)(CH.sub.2).sub.r C.sub.6 H.sub.5, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --OR.sup.16, or --O(CH.sub.2).sub.s C.sub.6 H.sub.5 group; R.sup.3 is --COOH, --COOR.sup.17, hydroxyl, --OR.sup.18, --NH.sub.2, --N(R.sup.19).sub.2, --NHR.sup.20, azole, or sulfonic acid group; R.sup.11 is alkyl of 1 to 6 carbon atoms or haloalkyl of 1 to 6 carbon atoms; R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, and R.sup.Type: GrantFiled: May 31, 1995Date of Patent: December 17, 1996Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Mikiro Yanaka, Fuyuhiko Nishijima, Hiroyuki Enari, Michihito Ise
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Patent number: 5571815Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.Type: GrantFiled: March 11, 1993Date of Patent: November 5, 1996Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, deceased, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter L ummen, Werner Bonin
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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: 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: 5527886Abstract: Fiber-reactive compounds of the formulaX-O.sub.2 S-W.sub.1 [F.sub.c ]W.sub.2 -NR-Z,and water-soluble salts thereof each cation of which is independently a non-chromophoric cation, and mixtures of such compounds or water-soluble salts,whereinFc is a chromophore-containing radical of a monoazo, disazo, polyazo, formazan, anthraquinone, dioxazine, phenazine or azomethine dye, which is in metal-free or metal complex form,each of W.sub.1 and W.sub.2 is independently a direct bond or a bridging group which is attached to a carbon atom of an aromatic carbocyclic ring or to a carbon or nitrogen atom of an aromatic heterocyclic ring present in F.sub.c,X is --CH.dbd.CH.sub.2 or --C.sub.2-4 alkylene--Y, wherein Y is hydroxy or a group which can be split off under alkaline conditions,R is hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkyl monosubstituted by hydroxy, halo, cyano, --SO.sub.3 H, --OSO.sub.3 H or --COOH, andZ is ##STR1## with the provisos as set forth herein.Type: GrantFiled: June 16, 1992Date of Patent: June 18, 1996Assignee: Sandoz Ltd.Inventors: Gunther Auerbach, Markus Dorr, Paul Doswald, Markus Gisler, Werner Koch, Helmut A. Moser, Roland Wald
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Patent number: 5525604Abstract: A 4-aminopyrimidine of the formula (I): ##STR1## wherein A is a bond, C1-4 alkylene or C1-4 oxyalkylene;Y is a bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenylene or phenyl(C1-4)alkylene;Z is a bond or vinylene;R1 is 4-15 membered heterocyclic ring containing one or two nitrogen atom;R2 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one or two of oxygen or one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) C1-4 alkoxy,(iv) hydroxy(C1-4 alkoxy) or(v) hydroxy;R3 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one oxygen, one sulfur, or one nitrogen and one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) formula:CH2.dbd.CH(X)--whereinX is halogen.(iv) hydrogen.l is 1 or 2.and some compounds are excluded.and acid addition salts thereof, salts thereof; have inhibitory effect on cGMP-PDE, or additionally on TXA2 synthetase.Type: GrantFiled: August 24, 1994Date of Patent: June 11, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Sung J. Lee, Yoshitaka Konishi, Orest T. Macina, Kigen Kondo, Dingwei T. Yu, Tamara A. Miskowski
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Patent number: 5519139Abstract: 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: GrantFiled: May 23, 1995Date of Patent: May 21, 1996Assignee: Shionogi & Co., Ltd.Inventors: Toshikazu Ohtsuka, Moriyasu Masui, Takami Takeda, Michio Masuko, Katsuaki Ohba