Six-membered Hetero Ring Consists Of Oxygen, Sulfur, Nitrogen And Carbon (e.g., Oxathiazines, Etc.) Patents (Class 544/2)
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Publication number: 20110071141Abstract: Condensed-ring aryl compounds of formula (I) and use of the same as a agrochemical for controlling noxious organisms wherein (X)mQ, A, R1, (Y)n and the grouping —W1—W2—W3—W4— are as defined herein.Type: ApplicationFiled: March 13, 2009Publication date: March 24, 2011Inventors: Tetsuya Murata, Yasushi Yoneta, Jun Mihara, Kei Domon, Mamoru Hatazawa, Koichi Araki, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Ulrich Görgens, Arnd Voerste, Angela Becker, Eva-Maria Franken, Klaus-Helmut Müller
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Patent number: 7863058Abstract: Disclosed are methods of attaching biologically active compounds to a solid surface, comprising modifying the solid surface using triazine chloride and attaching the biologically active compound to the triazine moiety.Type: GrantFiled: February 2, 2009Date of Patent: January 4, 2011Assignee: Illumina, Inc.Inventors: Chanfeng Zhao, Igor Kozlov, Galina Steinberg-Tatman
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Publication number: 20100331283Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
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Publication number: 20100298242Abstract: The invention relates to the use of sweeteners for masking the salty taste of compositions as well as compositions containing salt and defined sweeteners, the amount of sweeteners being suitable for masking the salty taste of the composition.Type: ApplicationFiled: July 26, 2006Publication date: November 25, 2010Inventors: Reiner Postges, Richard Ammer, Joerg Breitkreutz, Dorothee Grueneberg Klinkowski
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Patent number: 7829701Abstract: The invention discloses a kind of sulfonation cyclization technique for synthesizing acesulfame potassium for continuous production without stirring and special equipment for this technique. An injection pump is adopted to directly inject the sulfonation raw material and sulfonating agent into autoclave for sulfonation cyclization reaction under high velocity. Moreover, the reciprocating pump is adopted to deliver part of materials in autoclave to condenser designed outside the autoclave for cooling, followed by delivering the cooled materials to another input end of injection pump which together with sulfonation raw material and sulfonating agent is injected into autoclave through high-velocity injection by injection pump. The apparatus is composed of autoclave, injection pump, reciprocating pump and condenser.Type: GrantFiled: September 18, 2007Date of Patent: November 9, 2010Assignee: Suzhou Hope Technology Co., LtdInventors: Jicai Liu, Lingwen Kong, Zhongxiang Bao, Xiaoping Chen
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Patent number: 7829563Abstract: The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved, like sleep disorders.Type: GrantFiled: February 27, 2008Date of Patent: November 9, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Henner Knust, Parichehr Malherbe, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20100267703Abstract: The present invention relates to novel benzoxathiazine derivatives of the formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to several processes for preparation thereof and to the use thereof as insecticides and/or acaricides in combination with further compositions such as penetrants and/or ammonium or phosphonium salts.Type: ApplicationFiled: December 11, 2009Publication date: October 21, 2010Applicant: BAYER CROPSCIENCE AGInventors: Bernd Alig, Klaus-Helmut Müller, Eva-Maria Franken, Ulrich Görgens, Arnd Voerste
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Publication number: 20100249401Abstract: The present invention relates to a novel process for the preparation of a sterically hindered nitroxyl ether from the corresponding sterically hindered nitroxyl radical by reacting it with a carbonyl compound and a hydroperoxide. The compounds prepared by this process are effective stabilizers for polymers against harmful effects of light, oxygen and/or heat, as flame-retardants for polymers and as polymerization regulators.Type: ApplicationFiled: June 25, 2007Publication date: September 30, 2010Inventors: Kai-Uwe Schöning, Walter Fischer, Abdel-Ilah Basbas, Alexander Dichtl
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Publication number: 20100086955Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: ApplicationFiled: October 1, 2009Publication date: April 8, 2010Inventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
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Publication number: 20100063275Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): using a quinuclidine-based catalyst or an optionally 3-substituted N-methyl pryrrolidine-based catalyst.Type: ApplicationFiled: October 2, 2007Publication date: March 11, 2010Applicant: SYNGENTA LIMITEDInventors: Gillan Beveridge, Ewan Campbell Boyd, Jack Hugh Vass, Alan John Whitton
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Patent number: 7662957Abstract: A high quality 3,4-dihydro-1,2,3-oxathiazin-4-one-2,2-dioxide compound or a salt thereof is obtained easily and efficiently.Type: GrantFiled: August 2, 2007Date of Patent: February 16, 2010Assignee: Daicel Chemical Industries, Ltd.Inventors: Akira Saito, Yuki Ishiguro, Yasushi Yamamoto
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Publication number: 20090318686Abstract: A method for producing a high quality potassium salt of 3,4-dihydro-1,2,3-oxathiazin-4-one-2,2-dioxide compound easily and efficiently is provided. The producing method of the invention includes the steps of neutralizing 3,4-dihydro-1,2,3-oxathiazin-4-one-2, 2-dioxide compound represented by the following formula (1) (wherein R1 and R2 are the same as or different from each other and are hydrogen atom or an organic group inert to the reaction) with potassium hydroxide in a mixed solvent of water and a water soluble organic solvent to form a potassium salt of 3,4-dihydro-1,2,3-oxathiazin-4-one-2,2-dioxide compound represented by the following formula (2) and, during the neutralization, precipitating potassium sulfate derived from sulfuric acid contained in the compound represented by Formula (1) as an impurity.Type: ApplicationFiled: August 2, 2007Publication date: December 24, 2009Inventors: Akira Saito, Atsushi Mori
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Publication number: 20090318685Abstract: A high quality 3,4-dihydro-1,2,3-oxathiazin-4-one-2,2-dioxide compound or a salt thereof is obtained easily and efficiently.Type: ApplicationFiled: August 2, 2007Publication date: December 24, 2009Inventors: Akira Saito, Yuki Ishiguro, Yasushi Yamamoto
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Patent number: 7635792Abstract: Polyfluorene polymers and copolymers having substantial amounts (10-100%) of fluorenes coupled at the 2 and 5 positions of fluorene are useful as active layers in OLED devices where triplet energies >2.10 eV are required.Type: GrantFiled: October 14, 2008Date of Patent: December 22, 2009Assignee: General Electric CompanyInventors: James Anthony Cella, Joseph John Shiang, Elliott West Shanklin, Paul Michael Smigelski
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Patent number: 7608658Abstract: This invention discloses a process for manufacturing an elastomeric article by liquid injection molding, said process comprising the steps of: (I) heating a curable composition comprised of (1) a liquid polymer comprised of repeat units that are derived from a conjugated diolefin monomer, wherein said liquid polymer has a weight average molecular weight which is within the range of 5,000 to 100,000, and wherein the liquid polymer is functionalized with an amine moiety, (2) a carbonyl inhibited platinum catalyst, and (3) a tetrakis(dialkyl siloxy) silane crosslinking agent, to a temperature which is within the range of 30° C. to 100° C.; (II) injecting the heated curable composition into a mold at a temperature which is within the range of 100° C. to 210° C. to produce the elastomeric article; and (III) removing the elastomeric article from the mold.Type: GrantFiled: November 7, 2008Date of Patent: October 27, 2009Assignee: The Goodyear Tire & Rubber CompanyInventors: Michael Joseph Rachita, Vanessa Marika Guscoff, Lawson Gibson Wideman
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Patent number: 7531668Abstract: A compound represented by the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents —N—, —CH—, et al; Y1 represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.Type: GrantFiled: September 30, 2005Date of Patent: May 12, 2009Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takao Suzuki, Minoru Moriya, Shunji Sakuraba, Sayaka Mizutani, Hisashi Iwaasa, Akio Kanatani
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Patent number: 7507730Abstract: Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier, which have the structure stereoisomers including enantiomers thereof and diastereomers thereof, or a pharmaceutically acceptable salt thereof, wherein Q is alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl or which is aryl, substituted aryl, heteroaryl or substituted heteroaryl; R3 is wherein R1, R2, R4, R5, R6, R7, R8, R9 and R10 are defined herein. Methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds are also provided.Type: GrantFiled: August 28, 2006Date of Patent: March 24, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Wei Han, Zilun Hu
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Patent number: 7504499Abstract: Disclosed are methods of attaching biologically active compounds to a solid surface, comprising modifying the solid surface using triazine chloride and attaching the biologically active compound to the triazine moiety.Type: GrantFiled: November 10, 2005Date of Patent: March 17, 2009Assignee: Illumina, Inc.Inventors: Chanfeng Zhao, Igor Kozlov, Galina Steinberg-Tatman
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Publication number: 20090005363Abstract: The present invention relates to novel nicotinic acid derivatives, of formula (I) wherein the substituents are defined in the specification, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.Type: ApplicationFiled: December 18, 2006Publication date: January 1, 2009Inventors: Ralf Glatthar, David Orain, Carsten Spanka
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Patent number: 7408059Abstract: A method produces a 3,4-dihydro-1,2,3-oxathiazin-4-one-2,2-dioxide compound of following formula (2): wherein R1 and R2 are the same as or different from each other and are each hydrogen atom or an organic group inert to the reaction; and R3 is hydrogen atom or an organic group inert to the reaction, or a salt thereof, by subjecting a beta-ketoamide-N-sulfonic acid of following Formula (1): wherein R1, R2 and R3 are as defined above; and X is hydrogen atom, or a salt thereof, to cyclization in the presence of an acid anhydride with or without further subjecting the cyclized product to hydrolysis, in which the cyclization is continuously carried out using a continuous flow reactor.Type: GrantFiled: February 16, 2005Date of Patent: August 5, 2008Assignee: Daicel Chemical industries, Ltd.Inventors: Kenji Kobayashi, Hitoshi Watanabe, Noboru Kamei, Yasushi Yamamoto
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Publication number: 20080171737Abstract: The present invention is directed to cyclic sulfonamide derivatives of formula I: or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: December 12, 2007Publication date: July 17, 2008Applicant: WyethInventors: Andrew Fensome, Joel Adam Goldberg, Casey Cameron McComas, Charles William Mann, Edward George Melenski, Joseph Peter Sabatucci, Richard Page Woodworth
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Patent number: 7301028Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 12, 2003Date of Patent: November 27, 2007Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Mark E. Fraley
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Patent number: 7294650Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).Type: GrantFiled: December 15, 2004Date of Patent: November 13, 2007Assignee: Glaxo Group LimitedInventor: Keith Biggadike
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Patent number: 7259258Abstract: Disclosed are methods of attaching biologically active compounds to a solid surface, comprising modifying the solid surface using triazine chloride and attaching the biologically active compound to the triazine moiety.Type: GrantFiled: December 17, 2003Date of Patent: August 21, 2007Assignee: Illumina, Inc.Inventors: Igor Kozlov, Chanfeng Zhao, Galina Steinberg-Tatman
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Patent number: 7196108Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.Type: GrantFiled: March 6, 2003Date of Patent: March 27, 2007Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Richard M. Fine, Lyle W. Spruce, James W. Zapf
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Patent number: 7141562Abstract: Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R2 is aryl or heteroaryl, and R1, R3, R4, R5, R6, R7, R8, R9, Ra, Rb, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.Type: GrantFiled: November 6, 2003Date of Patent: November 28, 2006Assignee: Roche Palo Alto LLCInventors: Hans Maag, Meng Sui, Shu-Hai Zhao
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Patent number: 7105660Abstract: An intramolecular amidation processes for substrates such as sulfamates using chiral and non-chiral metalloporphyrin complexes which can maximize catalytic activity, enhance efficiency, stereoselectivity and speed of amidation reactions is described. The chiral metalloporphyrin catalyzed amidation of sulfamates exhibits excellent cis-selectivity, affording cyclic sulfamidates with high enantiomeric excess values.Type: GrantFiled: March 3, 2004Date of Patent: September 12, 2006Assignee: University of Hong KongInventors: Chi-Ming Che, Jiang-Lin Liang
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Patent number: 7053109Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: July 10, 2002Date of Patent: May 30, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Patent number: 6867298Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.Type: GrantFiled: May 8, 2003Date of Patent: March 15, 2005Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
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Patent number: 6852885Abstract: There is provided a method for obtaining a target organic compound such as an alkyladamantyl ester efficiently by purifying a crude organic compound which contains, as impurities, sublimable materials which start to sublime at temperatures lower than a boiling point of the target organic compound by use of such a simple method as distillation during its production process, without being adversely affected by adherence of the sublimable materials. The distillation is carried out in the presence of a compound having a boiling point which is lower than a boiling point of the target organic compound, e.g., a carbonyl-group-containing compound. For example, 2-methyl-2-adamantyl methacrylate (boiling point: 92° C./0.3 mmHg) containing sublimable impurities such as adamantane (sublimation starting temperature: room temperature or lower) is distilled in the presence of 1,3-dimethyl-2-imidazolidinone (boiling point: 225° C.).Type: GrantFiled: January 26, 2001Date of Patent: February 8, 2005Assignee: Tokuyama CorporationInventors: Hiromasa Yamamoto, Masao Yamaguchi, Hideki Kikuchi
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Patent number: 6849623Abstract: Complex compounds or adducts of xanthine derivatives, for example propentofylline or pentoxyfylline, or phenazone derivatives, for example phenazone, propylphenazone and aminophenazone, and acesulfame-H, in which the components are present in a molar ratio of 1:1 or 1:2, have a pleasantly sweet taste and are suitable for numerous applications, for example in pharmaceuticals. The compounds can be prepared from the dissolved components by simple reaction.Type: GrantFiled: June 7, 2002Date of Patent: February 1, 2005Assignee: Nutrinova Nutrition Specialties & Food Ingredients GmbHInventor: Andreas Burgard
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Patent number: 6797522Abstract: The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain, cyclic or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In a preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier. In addition, the invention includes methods of preparing synthetic receptors and synthetic receptor libraries. The synthetic library may be linked with identifiers such that the library comprises a plurality of different synthetic receptor members.Type: GrantFiled: March 12, 1998Date of Patent: September 28, 2004Assignee: The Trustees of Columbia University in the City of New YorkInventors: W. Clark Still, Ge Li, Helma Wennemers
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Patent number: 6759544Abstract: Complex compounds containing acesulfame have good antimicrobial action, in particular antibacterial action, and are distinguished by the fact that they are complex compounds of metallic elements such as zinc, copper, silver, or nonmetallic quaternary ammonium cations, such as the cetylpyridinium cation, with acesulfame. The invention also relates to a process for preparing the compounds and their use in the oral hygiene sector.Type: GrantFiled: June 7, 2002Date of Patent: July 6, 2004Assignee: Nutrinova Nutrition Specialties & Food Ingredients GmbHInventor: Andreas Burgard
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Patent number: 6734304Abstract: The invention relates to a novel process for preparing known asymmetrical 4,6-bis(aryloxy)pyrimidine derivatives.Type: GrantFiled: September 17, 2002Date of Patent: May 11, 2004Assignee: Bayer AktiengesellschaftInventors: Holger Weintritt, Uwe Stelzer, Herbert Gayer, Walter Hübsch
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Patent number: 6727359Abstract: Acesulfame-K is a widely used sweetener in food and beverage. It is prepared by using the substituted sodium phenoxide or substituted phenol as the starting substance to synthesize the following three intermediates: a substituted phenoxide sulfonylchloride(I), a substituted phenoxide sulfonylamide(II) and an acetoacetamide-N-sulfonyl-substituted phenoxide(III). Particularly, II was prepared by using the liquid or gaseous ammonia to react with I under the action of some catalysts in a reaction column. III was prepared by using II to react with diketene. Acesulfame-K was prepared by ring-closure in III with methanol solution of KOH or K2CO3.Type: GrantFiled: July 25, 2002Date of Patent: April 27, 2004Assignee: BDL CorporationInventors: Nianshou Tian, Haiming Liu
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Publication number: 20040077874Abstract: The invention is directed to polymerizable vinyl compounds having halogenated aromatic groups and to a method of synthesizing such compounds. In particular, the invention is directed to polymerizable aromatic vinyl compounds wherein, except for the vinylic hydrogen atoms, aromatic C—H bonds are replaced by C—X bonds, where X is a halogen or other selected substituent having a de minimus number, if any, of C—H bonds; for example, without limitation, highly fluorinated fluoroalkanes. In addition, the compounds of the invention have a de minimus number, if any, of N—H and O—H bonds.Type: ApplicationFiled: September 22, 2003Publication date: April 22, 2004Inventors: Olivier Arnoud, Marc Moroni, Stephane Roux
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Publication number: 20040019204Abstract: The present invention relates to novel intramolecular amidation processes for substrates such as sulfamate esters using chiral and non-chiral metalloporphyrin complexes, which can maximize catalytic activity and enhance efficiency, stereoselectivity and speed of amidation of these substrates. The intramolecular amidation of sulfamate ester exhibits excellent cis-selectivity, affording cyclic sulfamidates with high ee values catalyzed by chiral metalloporphyrin.Type: ApplicationFiled: July 23, 2002Publication date: January 29, 2004Inventors: Chi-Ming Che, Jiang-Lin Liang
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Patent number: 6562811Abstract: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di(C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33, or —NR34R35; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 18, 2001Date of Patent: May 13, 2003Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Detecting reagent for double-stranded nucleic acid and double-stranded nucleic acid detecting method
Patent number: 6528648Abstract: The present invention provides a novel detecting reagent for double-stranded nucleic acid, and a method of using it to detect double-stranded nucleic acid formed by hybridization with a probe, with absolutely no labeling of the target nucleic acid. The detecting reagent for double-stranded nucleic acid of the invention is characterized by comprising, in the same molecule, a naphthalenediimide group which is intercalatable into double-stranded nucleic acid and a &bgr;-diketone group capable of forming a lanthanoid metal complex.Type: GrantFiled: December 5, 2001Date of Patent: March 4, 2003Assignee: Waseda University and RikenInventors: Kazuko Matsumoto, Takahiko Nojima, Hideo Tashiro, Yasumitsu Kondoh, Shigeori Takenaka -
Patent number: 6436927Abstract: The present invention involves certain 8-ureido and 8-thioureido, 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the chemokine, Interleukin-8.Type: GrantFiled: July 7, 1999Date of Patent: August 20, 2002Assignee: SmithKline Beecham CorporationInventors: Hong Nie, Katherine L. Widdowson
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Patent number: 6407097Abstract: The invention relates to novel methoximinomethyloxathiazines, to two processes for their preparation and to their use as pesticides.Type: GrantFiled: October 30, 2000Date of Patent: June 18, 2002Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Ulrich Heinemann, Bernd-Wieland Krüger, Klaus Stenzel
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Patent number: 6271235Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: August 7, 2001Assignee: Agouron Pharmaceuticals, Inc.Inventors: Bruce A. Dressman, James E. Fritz, Stephen W. Kaldor, Vincent J. Kalish, Siegfried Heinz Reich, Michael J. Rodriguez, Timothy A. Shepherd, John H. Tatlock, Louis Nickolaus Jungheim
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Patent number: 6268311Abstract: 1-Amino-3-benzyluracils I (X=oxygen, sulfur; R1=C1-C4-haloalkyl; R2=H, halogen; R3, R7=H, CN, SCN, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-haloalkylthio; R4=H, CN, SCN, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-haloalkylthio, C1-C6-alkylaminocarbonyl; R5=H, CN, NO2, halogen, OH, C1-C4-alkoxy, NH2, C1-C6-alkyl-amino; R6=H, CN, NO2, halogen, OH, C1-C4-alkoxy, NH2, C1-C6-alkyl-amino, CHO) and their salts are used as herbicides and for the desiccation/defoliation of plants.Type: GrantFiled: March 17, 1998Date of Patent: July 31, 2001Assignee: BASF AktiengesellschaftInventors: Olaf Menke, Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schäfer, Cyrill Zagar, Norbert Götz, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Patent number: 6265398Abstract: The present invention relates to novel substituted pyridines/pyrimidines of the formula I where A is CH or N; X is NH, O or S(O)q where q is 0, 1 or 2; Y1, Y2 and Y3 independently of one another are a group of the formula —O—, —CO—, —CNR6—, —S(O)r— or —N(O)lR6— where l is 0 or 1 and where r is 0, 1 or 2, or a group of the formula CR7R8, or Y1 or Y3 replace a direct bond; Z is a direct bond, NR9, O, S(O)s where s is 0, 1 or 2, OSO2, SO2O, NR10SO2, SO2NR11, SiR12R13 or where U is a direct bond, NR14 or O; W is oxygen or sulfur; V is a direct bond, NR15 or oxygen; m and n and 0, 1, 2, 3 or 4; where the radicals R1 to R15 have the meaning given in the description, to processes for their preparation, to their use as pesticides, fungicides and ovicides and to their use as veterinary medicaments.Type: GrantFiled: October 23, 1998Date of Patent: July 24, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Ralf Braun, Wolfgang Schaper, Herbert Stark, Rainer Preuss, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin
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Patent number: 6245934Abstract: Method for preparing a salt of aspartylphenylalanine methyl ester from N-protected aspartylphenylalanine methyl ester involving cleaving off the protective group by treatment with an acid, in the course of which, first of all, N-protected aspartylphenylalanine methyl ester is caused to react in an aqueous medium and in the presence of methanol at a temperature of from 0 to 80° C. with from 0.8 to 2 equivalents of acesulphamic acid for at least such a time that the conversion to the salt of aspartylphenylalanine methyl ester and acesulphamic acid has been completed to an adequate degree, and then the salt formed in the first step is isolated in precipitated form at a temperature of 30° C. or lower.Type: GrantFiled: December 6, 1999Date of Patent: June 12, 2001Assignee: DSM NVInventors: Jacob Van Soolingen, Wilhelmus H. J. Boesten
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Patent number: 6063917Abstract: A process for the production of a compound of formula ##STR1## wherein R.sup.a denotes hydrogen or silyl;R.sup.b denotes a group of formula --OR.sup.e, whereinR.sup.e denotes hydrogen or alkyl; andR.sup.c and R.sup.d together denote a bond;in free form or in salt form,which process comprises the step of spitting, in the presence of ozone, the double bond in position 3 of the ring structure of a compound of formula III ##STR2## wherein R.sub.2 and R.sub.3 are the same or different and independently of each other denote hydrogen or an organic group, and X.sup.- denotes the anion of an inorganic or organic acid and optionally silylating the amine group in position 7 of the ring system.Type: GrantFiled: September 30, 1998Date of Patent: May 16, 2000Assignee: Biochemie Gesellschaft m.b.H.Inventors: Gerd Ascher, Johannes Ludescher, Hubert Sturm, Josef Wieser
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Patent number: 6020335Abstract: An (N-(pyridinylmethyl)-heterocyclic)ylideneamine compound of the formula ##STR1## wherein R.sup.3, A, and B are as described below, and its pharmaceutically acceptable salts and prodrugs. Compounds of the formula I and their pharmaceutically acceptable salts and prodrugs are useful in the treatment of addictive disorders, such as the use of tobacco or other nicotine containing products, neurological and mental disorders such as senile dementia of the Alzheimer's type, Parkinson's disease, attentional hyperactivity disorder, anxiety, obesity, Tourette's Syndrome and ulcerative colitis.Type: GrantFiled: November 4, 1997Date of Patent: February 1, 2000Assignee: Pfizer IncInventors: Arthur A. Nagel, Steven W. Goldstein, Stanley Jung, Peter H. Dorff
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Patent number: 5962437Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus and herpes viruses, is disclosed. The method comprising administering to a subject in need of such treatment an infection-combating amount of a phospholipid or phospholipid derivative.Type: GrantFiled: May 2, 1997Date of Patent: October 5, 1999Assignee: Wake Forest UniversityInventors: Louis S. Kucera, Susan L. Morris-Natschke, Khalid S. Ishaq
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Patent number: 5922113Abstract: Use of 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides having the formula ##STR1## wherein n is 0, 1 or 2; R.sup.1 is hydrogen, C.sub.1-4 alkyl or benzyl; and R represents (a) phenyl; phenyl substituted with 1 to 3 substituents independently selected from hydroxyl, halo, C.sub.1-12 alkyl, C.sub.5-6 cycloalkyl, trihalomethyl, phenyl, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, tetrahydropyranyloxy, phenoxy, C.sub.1-4 alkylcarbonyl, phenylcarbonyl, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, carboxy or its alkali metal salt, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkylaminocarbonyl, phenylaminocarbonyl, tolylaminocarbonyl, morpholinocarbonyl, amino, nitro, cyano, dioxolanyl or C.sub.1-4 alkyloxyiminomethyl; naphthyl; pyridinyl; thienyl, preferably when n is not 2; furanyl; or thienyl or furanyl substituted with one to three substituents independently selected from C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, C.sub.1-4 alkylthio, halo, cyano, formyl, acetyl, benzoyl, nitro, C.sub.Type: GrantFiled: October 16, 1997Date of Patent: July 13, 1999Assignee: Janssen Pharmaceutica, N.V.Inventor: Jozef Frans Elizabetha Van Gestel
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika