Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/302)
-
Patent number: 6498164Abstract: A compound of the formula wherein the substituents are as defined in the specification and solvates and salts thereof useful for treating bone and cartilage diseases.Type: GrantFiled: October 19, 2000Date of Patent: December 24, 2002Assignee: Aventis Pharma S.A.Inventors: Kunikazu Sakai, Yusuke Satoh
-
Patent number: 6444682Abstract: Nucleotide or base analogues having structure (3) or (4) wherein X═O or NH or S and each R6 is independently H or alkyl or alkenyl or alkoxy or aryl or a reporter moiety.Type: GrantFiled: April 18, 2000Date of Patent: September 3, 2002Assignee: Nycomed Amersham PLCInventors: Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
-
Patent number: 6387914Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.Type: GrantFiled: April 24, 2001Date of Patent: May 14, 2002Assignee: ARYx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
-
Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
-
Patent number: 6281219Abstract: The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.Type: GrantFiled: July 12, 1999Date of Patent: August 28, 2001Assignee: American Cyanamid Co.Inventors: Salvatore John Cuccia, William Wakefield Wood, Brian Lee Buckwalter, John Francis Chiarello, Linda Barbara Fleming
-
Patent number: 6265578Abstract: A compound of formula I wherein R1 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryloxy or alkylalkoxy, and R2 is aryloxy, or a pharmaceutically acceptable salt of an acidic compound of formula I, or a prodrug thereof. The compounds of formula I and their aforementioned salts and prodrugs can be used in the treatment or control of cancer associated with overexpresison of gelatinase-A and/or gelatinase-B, particularly skin cancer, breast cancer, prostate cancer, colon cancer, lung cancer, and gastric cancer. The compounds of the invention are also useful for other diseases associated with unregulated degradation of extracellular matrix, including rheumatoid arthritis, osteoarthritis, multiple sclerosis, corneal ulceration, periodontal disease and the like.Type: GrantFiled: January 17, 2000Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Louise Helen Foley, Robert Edward Palermo, Ping Wang
-
Patent number: 6254669Abstract: A compound of the Formula (1) and salts thereof: wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially ink jet printing inks, for reducing color bleed between adjacent printed regions. Also claimed are inks containing a compound of the Formula (1), a method of ink jet printing using the inks, a substrate printed with the ink and an ink jet printer cartridge containing the ink.Type: GrantFiled: August 5, 1999Date of Patent: July 3, 2001Assignee: Zeneca LimitedInventors: Aidan Joseph Lavery, Prahalad Manibhai Mistry, Ronald Wynford Kenyon
-
Patent number: 6235903Abstract: A process for preparing endothelin receptor antagonists of the sulfanyl type of the general formula I by nucleophilic reaction of a carboxylic acid derivative of the formula II with a sulfide of the formula III to give endothelin receptor antagonists of the formula I.Type: GrantFiled: August 23, 2000Date of Patent: May 22, 2001Assignee: BASF AktiengesellschaftInventors: Wilhelm Amberg, Rolf Jansen, Dagmar Klinge
-
Patent number: 6232325Abstract: This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid 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: November 12, 1999Date of Patent: May 15, 2001Assignee: Berlex Laboratories, Inc.Inventors: Monica Kochanny, Michael M. Morrissey, Howard P. Ng
-
Patent number: 6177437Abstract: The invention is directed to novel 6-aromatic substituted uracil compounds of formula I therapeutic compositions comprising the compounds, and methods of treating Herpes simplex virus Type I and Type II recurrent infections and Herpes simplex virus Type I and Type II encephalitis in humans using the compounds and/or therapeutic compositions.Type: GrantFiled: September 1, 1999Date of Patent: January 23, 2001Assignee: University of Massachusetts Medical CenterInventor: George E. Wright
-
Patent number: 6114546Abstract: The present invention provides an aminomethylene derivative represented by general formula (I): ##STR1## wherein A is a cyclic oxo group selected from the group consisting of following general formulae (a), (b), (c), (d) and (e): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represent H, an alkyl group or the like; R.sup.6, R.sup.7 and R.sup.8 each independently represent an alkyl group or the like; R.sup.1 and R.sup.2 or R.sup.7 and R.sup.8 may combine with each other to form a tetramethylene group or the like; R represents an alkyl group optionally containing OH or O; and n is an integer of 0 to 4, a process for the same, and the use thereof. The derivatives have an excellent ultraviolet absorption ability and a high optical stability.Type: GrantFiled: March 26, 1999Date of Patent: September 5, 2000Assignee: Chemipro Kasei Kaisha, LimitedInventors: Heinosuke Yasuda, Naohiko Hukuoka
-
Patent number: 6103898Abstract: Cyclic urea derivatives of the formula I ##STR1## in which X, X', Y, Y' and Z can have various meanings, are prepared by a) reacting a urea derivative of the formula II ##STR2## with a diketone of the formula III ##STR3## and b) hydrogenating the product from step a) in the presence of a metal-containing catalyst.Type: GrantFiled: September 28, 1998Date of Patent: August 15, 2000Assignee: BASF AktiengesellschaftInventors: Andreas Kramer, Wolfgang Siegel
-
Patent number: 6103732Abstract: Carboxylic acid derivatives of the formula I ##STR1## where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.Type: GrantFiled: October 8, 1998Date of Patent: August 15, 2000Assignee: BASF AktiengesellschaftInventors: Wilhelm Amberg, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Ernst Baumann, Liliane Unger, Manfred Raschack, Stefan Hergenroder, Sabine Schult
-
Patent number: 6093820Abstract: A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I ##STR1## with an alkylating agent of structure III ##STR2## in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N'-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.Type: GrantFiled: October 2, 1997Date of Patent: July 25, 2000Assignee: Taro Pharmaceutical Industries Ltd.Inventors: Daniela Gutman, Hershel Herzog
-
Patent number: 6087498Abstract: There is provided a process for the preparation of unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds. The unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds are useful as pesticidal agents.Type: GrantFiled: March 16, 1999Date of Patent: July 11, 2000Assignee: American Cyanamid CompanyInventors: William Wakefield Wood, Salvatore John Cuccia, Robert Brigance
-
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
-
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
-
Patent number: 5889013Abstract: The present invention relates to novel pyrimidine acyclonucleoside derivatives represented by the following general formula (I), antiviral agents containing the derivatives as the active ingredients and processes of preparation thereof. ##STR1## wherein R.sup.1 is ethyl or isopropyl; R.sup.2 is (3,5 dimethylphenyl)selenenyl; R.sup.3 is phenyl or methyl; X is oxygen; and Y is oxygen.Type: GrantFiled: January 4, 1996Date of Patent: March 30, 1999Assignee: Sunkyong Industries Co., Inc.Inventors: Dae-Kee Kim, Jongsik Gam, Ganghyeok Kim, Young-Woo Kim, Namkyu Lee, Jinsoo Lim, Hun-Taek Kim, Key Hyup Kim
-
Patent number: 5849910Abstract: This invention provides an improved process for the preparation of unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds having the structural formula I ##STR1## The unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds are useful as pesticidal agents.Type: GrantFiled: September 5, 1997Date of Patent: December 15, 1998Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
-
Patent number: 5840892Abstract: A novel process for the preparation of substituted pyrimidine derivatives of the general formula: ##STR1## in which a halopyrimidine is reacted in the presence of a sulfinate with a compound selected from the series: ##STR2## The compounds of the general formula I are precursors of, for example, compounds with herbicidal activity.Type: GrantFiled: April 8, 1997Date of Patent: November 24, 1998Assignee: Lonza AGInventors: Yves Bessard, Gerhard Stucky
-
Patent number: 5804584Abstract: Disclosed are therapeutic compounds having the formula:(R)j-(core moiety),including resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one to three, the core moiety is either non-cyclic or comprises at least one five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, C.sub.1-6 alkyl or C.sub.1-6 alkenyl, and at least one R has the formula I: ##STR1## n is an integer from seven to twenty and at least one of X or Y is --OH. The other of X or Y, which is not --OH, is hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --, and each W.sub.1, W.sub.2, and W.sub.3 is independently hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --. The X, Y, W.sub.1, W.sub.2, or W.sub.Type: GrantFiled: June 6, 1995Date of Patent: September 8, 1998Assignee: Cell Therapeutics, Inc.Inventors: Gail E. Underiner, David Porubek, J. Peter Klein, Paul Woodson
-
Patent number: 5780629Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks. The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.Type: GrantFiled: June 6, 1996Date of Patent: July 14, 1998Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Paul Delavier, Karl Siemensmeyer, Gerhard Wagenblast, Lothar Laupichler, Volkmar Vill
-
Patent number: 5777118Abstract: Cyclic acetals of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 and R.sup.2 are hydrogen, unsubstituted or substituted alkyl or phenyl; additionally R.sup.1 and R.sup.2 together are an unsubstituted or substituted C.sub.2 -C.sub.6 -alkylene chain;Y is oxygen or sulfur;A has the meaning as given in claim 1;a process for preparing the acetals I and their use for the production of crop protection compositions are described.Type: GrantFiled: July 12, 1996Date of Patent: July 7, 1998Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Hartmann Konig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
-
Patent number: 5756740Abstract: A process for the preparation of photographic binary sensitizing dyes, which comprise two separate, nonconjugated chromophores, one of which has the capability of adsorbing to a silver halide grain surface, the other of which is substantially non-adsorbing to silver halide. The process comprises reacting two dye compounds in a solvent in the presence of a 2-halo-1-alkylpyridinium salt and a 4-dialkylaminopyridine.Type: GrantFiled: April 8, 1992Date of Patent: May 26, 1998Assignee: Eastman Kodak CompanyInventors: Lal Chand Vishwakarma, Chin Hsin Chen
-
Patent number: 5753594Abstract: 3-Halo-3-hetarylcarboxylic acid derivatives having the formula I ##STR1## in which R is a formyl group, a group CO.sub.2 H or a radical which can be hydrolyzed to COOH, and the remaining substituents have the following meanings:R.sup.2 and R.sup.3 are halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy or C.sub.1 -C.sub.4 -alkylthio;X is nitrogen or CR.sup.13, where R.sup.13 is hydrogen or together with R.sup.3 forms an alkylene or alkenylene chain in which in each case one methylene group is replaced by oxygen;R.sup.4 is an unsubstituted or substituted five- or six-membered heteroaromatic ring which contains one to three nitrogen atoms and/or one sulfur or oxygen atom;R.sup.5 is hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl or phenyl;Y is sulfur, oxygen or a single bond; andZ is halogen.The derivatives I having herbicidal and plant-growth regulating properties.Type: GrantFiled: December 1, 1995Date of Patent: May 19, 1998Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Albrecht Harreus, Matthias Bratz, Joachim Rheinheimer, Uwe Josef Vogelbacher, Hans Theobald, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen, Wilhelm Rademacher
-
Patent number: 5750469Abstract: Substituted lactic acid derivatives having an N-organic radical in the .beta.-position, of the formula I ##STR1## where substituents R to R.sup.5, X and Y have the meanings mentioned in the description and N is one of the radicals:a) --N.sub.3, --NC, --NCS or --NCOb) ##STR2## where R.sup.14 and R.sup.15 have the meanings described in the descriptionc) ##STR3## in which R.sup.16 is hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl or unsubstituted or substituted phenyl; andB is a group ##STR4## OR.sup.19 or --NR.sup.14 R.sup.15, where R.sup.14, R.sup.15, R.sup.17 and R.sup.19 have the meanings described in the description, or ##STR5## where R.sup.14 and R.sup.15.sub.1, have the abovementioned meanings; or ##STR6## where R.sup.20 and R.sup.21, which can be identical or different, are: hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or phenyl, where the organic radicals can in each case be substituted;or R.sup.20 and R.sup.21 together form an unsubstituted or substituted C.sub.4 -C.sub.Type: GrantFiled: March 1, 1996Date of Patent: May 12, 1998Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Gerber, Wilhelm Rademacher, Helmut Walter, Karl-Otto Westphalen
-
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
-
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
-
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
-
Patent number: 5721241Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y H is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is H or an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging.Type: GrantFiled: June 6, 1995Date of Patent: February 24, 1998Assignees: Mahmoud H. el Kouni, Fardos N. M. Naguib, Raymond F. SchinaziInventors: Mahmoud H. el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
-
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
-
Patent number: 5674870Abstract: Previously unknown anti-tumor, anti-infectious, immune system modulatory and anti-depressive properties of a family of barbituric acid derivatives are provided herein. Preferred derivatives are 4,6(1H, 5H)-pyrimidinedione, 1,3-dibutyldihydro-2thioxo; and 4,5,6(1H)-pyrimidinetrione, 1,3-dibutyldihydro-2thioxo. These compounds are effective for killing tumor cells, especially carcinoma (breast and prostate cancer), lymphoma and leukemia cells; for killing pathogenic organisms, especially viruses; for stimulating T cell formation and for alleviating symptoms of depression and are readily tolerated by the animal being treated.Type: GrantFiled: March 18, 1996Date of Patent: October 7, 1997Inventor: Kirpal S. Gulliya
-
Patent number: 5672567Abstract: Herbicidal substituted hydroxybenzyl-heteroaryl compounds and derivatives thereof of the formula ##STR1## wherein Ar is a substituted or unsubstituted 5- or 6-membered heteroaryl group having 2 or 3 ring nitrogen atoms or a substituted or unsubstituted 5-membered heteroaryl group having two ring heteroatoms, one of the ring heteroatoms being nitrogen and the other being sulfur or oxygen. Herbicidal compositions containing such substituted hydroxybenzyl-heteroaryl compounds and derivatives thereof and methods of controlling undesirable vegetation employing these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the disclosed substituted hydroxybenzyl-heteroaryl derivatives.Type: GrantFiled: March 25, 1996Date of Patent: September 30, 1997Assignee: Zeneca LimitedInventors: Hsiao-Ling M. Chin, Yi-Qiu Wei, Nhan H. Nguyen, David B. Kanne
-
Patent number: 5661106Abstract: 3-(Het)aryloxy(thio)carboxylic acid derivatives of the formula I ##STR1## where R.sup.1 is hydrogen, COOH or a radical which can be hydrolyzed to give COOH;R.sup.2 and R.sup.3 are each halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.14, where R.sup.14 is hydrogen or, together with R.sup.3, forms a 3-membered or 4-membered alkylene or alkenylene chain, in each of which a methylene group is replaced by oxygen;R.sup.4 is alkyl, cycloalkyl, cycloalkenyl, alkenyl or alkynyl, each of which is unsubstituted or substituted;an unsubstituted or substituted five-membered or six-membered heteroaromatic structure containing one to three nitrogen atoms or one sulfur or oxygen atom;unsubstituted or substituted phenyl or naphthyl;R.sup.4 and R.sup.5, together with the neighboring carbon atom, form a 3-membered to 8-membered ring which may contain an oxygen or sulfur atom and which is unsubstituted or substituted;R.sup.Type: GrantFiled: October 19, 1995Date of Patent: August 26, 1997Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Bratz, Norbert Meyer, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Wilhelm Rademacher
-
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
-
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
-
Patent number: 5550241Abstract: The present invention relates to novel adducts of cyclic carbonyl monomers with substituted olefins, which also are useful as solution viscosifiers.Type: GrantFiled: March 18, 1993Date of Patent: August 27, 1996Assignee: Exxon Research and Engineering CompanyInventor: Stanley J. Brois
-
Patent number: 5527804Abstract: Compounds which inhibit the enzyme cholesterol ester hydrolase (CEH) thus inhibit the formation of esterified cholesterol. Esterified cholesterol is absorbed through the intestine and inhibition of the enzyme therefore results in inhibition of cholesterol absorption. The compounds of this invention inhibit cholesterol ester hydrolase and have the formula: ##STR1## wherein Z is --Ar.sup.1, --Ar.sup.1 --Ar.sup.2, --Ar.sup.1 --O--Ar.sup.2, --Ar.sup.1 --S--Ar.sup.2, ##STR2## --Ar.sup.1 --(CH.sub.2).sub.1-20 --Ar.sup.2, --Ar.sup.1 --(CH.sub.2).sub.1-20 --O--Ar.sup.2, --Ar.sup.1 --O--(CH.sub.2).sub.1-20 --Ar.sup.2, --Ar.sup.1 --(CR.sup.6 .dbd.CR.sup.6).sub.1-3 --Ar.sup.2 or --Ar.sup.1 --NR.sup.7 --Ar.sup.2 ; andA is a hydrocarbon linking group which may be interrupted by a heteroatom or a cycloalkyl, aryl, heterocycloalkyl, or an azacycloalkyl group;and R.sup.4 and R.sup.5 are independently alkyl, alkenyl, acyl, alkoxycarbonyl or H or R.sup.4 and R.sup.Type: GrantFiled: June 13, 1994Date of Patent: June 18, 1996Assignee: American Home Products CorporationInventors: Thomas J. Commons, Christa M. LaClair
-
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
-
Patent number: 5507974Abstract: Aromatic, substituted pyrimidine compounds, methods for the preparation thereof, and use thereofCompounds having a pyrimidine ring, of the formula (I) ##STR1## are suitable for nonlinear-optical applications, e.g. for fabricating components for frequency-doubling of light. In the formula, AX is ##STR2## An.sup.- is an anion, B is the pyrimidine(1,4) radical, D is --NH.sub.2, --NH--NH.sub.2, --OR.sup.6, --O(CH.sub.2).sub.p OH, --OH, --NR.sup.5 R.sup.6, --NHR.sup.6, --N.dbd.CH--R.sup.4, --HN--N.dbd.CH--R.sup.4, --NO.sub.2,the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.5 are an alkyl radical having from 1 to 22 carbon atoms or a radical CF.sub.3 (CF.sub.2).sub.m (CH.sub.2).sub.n, R.sup.4 is a phenyl radical which may be substituted, R.sup.6 is an alkyl radical having from 1 to 22 carbon atoms or the radical CF.sub.3 (CF.sub.2).sub.m (CH.sub.2).sub.n, where m is an integer of at least 5, n is an integer of at least zero, and (n+m) is at most 22, or the group (CH.sub.2).sub.Type: GrantFiled: December 9, 1993Date of Patent: April 16, 1996Assignee: Hoechst AktiengesellschaftInventors: Rudolf Gompper, Harald Engel, Donald Lupo
-
Patent number: 5476855Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging.Type: GrantFiled: November 2, 1993Date of Patent: December 19, 1995Assignees: Mahmoud H. el Kouni, Fardos N. M. Naguib, F. SchinaziInventors: Mahmoud el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
-
Patent number: 5459265Abstract: There is disclosed a silver halide photographic light-sensitive material having a hydrophilic colloid layer containing a dye which is photochemically inactive and can readily be decolored and/or eluted in a photographic processing course. The silver halide photographic light-sensitive material comprises a hydrophilic colloid layer containing at least one dye dispersed in the form of a solid fine particle represented by Formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2, L.sub.1, L.sub.2, L.sub.3 are defined in the disclosure.In a preferred embodiment, the maximum absorption wavelength .lambda.max of the dye in the hydrophilic colloid layer satisfies the following equation:.lambda.max>[.lambda.max(DMF)+20.times.(n+1)] nmwherein .lambda.max(DMF) and n are defined in the disclosure. There is also disclosed an oxonol compound which is useful as a dye.Type: GrantFiled: March 23, 1994Date of Patent: October 17, 1995Assignee: Fuji Photo Film Co., Ltd.Inventors: Koji Wariishi, Keiichi Suzuki
-
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
-
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
-
Patent number: 5439825Abstract: Disclosed herein are buffers and methodologies for the capillary zone electrophoretic analysis of hemoglobin and the variants of hemoglobin. In a particularly preferred embodiment, the buffer comprises at least about 100 mM of barbituric acid, derivatives of barbituric acid, combinations of barbituric acid and derivatives of barbituric acid, and combinations of the derivatives of barbituric acid, and has a pH of at least about 8.0.Type: GrantFiled: December 10, 1992Date of Patent: August 8, 1995Assignee: Beckman Instruments, Inc.Inventor: Fu-Tai A. Chen
-
Patent number: 5426090Abstract: A method of combating undesired plant growth in wheat, comprising treating said undesired plant growth with an effective amount of a compound of the formula I ##STR1## in which n is an integer from 1 to 6;m is an integer from 0 to 2n+2;X represents an oxygen or sulphur atom or a sulphinyl or sulphonyl group;R.sup.1, R.sup.2 and R.sup.3 each independently represents a hydrogen or halogen atom, a formyl, cyano, carboxy or azido group, or an optionally substituted C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl, C.sub.1-12 alkoxy, C.sub.2-12 alkenyloxy, C.sub.2-12 alkynyloxy, C.sub.1-12 alkylthio, C.sub.2-12 alkenylthio, C.sub.2-12 alkynylthio, C.sub.1-12 alkylcarbonyl, C.sub.1-12 alkoxycarbonyl, amino, aminoxy or di-C.sub.1-12 alkyliminoxy group;Z represents a hydrogen or halogen atom, a hydroxy group, an optionally substituted C.sub.1-12 alkoxy, C.sub.2-12 alkenyloxy, C.sub.2-12 alkynyloxy, (C.sub.3-8 cycloalkyl)oxy, phenyloxy, C.sub.1-12 alkylthio, C.sub.2-12 alkenylthio, C.sub.Type: GrantFiled: July 12, 1993Date of Patent: June 20, 1995Assignee: Shell Research LimitedInventors: Alastair McArthur, Trevor W. Newton
-
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
-
Patent number: 5420133Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.Type: GrantFiled: March 19, 1993Date of Patent: May 30, 1995Assignee: Merck & Co., Inc.Inventors: Daljit S. Dhanoa, Kenneth J. Fitch, Daniel F. Veber, Thomas F. Walsh, David L. Williams, Jr.
-
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
-
Patent number: RE37623Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula where X is S or Se; Y is H, I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R1 is H or an acyclo tail having the general formula where R2 is H, CH2 OH or CH2 NH2; R3 is OH, NH2, or OCOCH2CH2CO2H; and R4 is O, S, or CH2. The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.Type: GrantFiled: December 1, 1997Date of Patent: April 2, 2002Inventors: Mahmoud H. el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi