Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/420)
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Patent number: 6852866Abstract: Disclosed is an invention concerning triazolyloligosaccharides, oligosaccharides wherein the bonding between the saccharide groups is via a triazole group and methods for their preparation.Type: GrantFiled: August 15, 2003Date of Patent: February 8, 2005Assignee: E. I. du Pont de Nemours and CompanyInventor: Subramaniam Sabesan
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Patent number: 6833462Abstract: An acrylate compound of formula (4): is produced by allowing an acrylic acid compound of formula (1): to react with an unsaturated compound of formula (2) or (3): In formulae (1) through (4), R1 and R2 are H or F, R3 is H, F, or an alkyl, alkenyl, fluoroalkyl or fluoroalkenyl group, R4 and R5 are H, halogen, or an alkyl, alkenyl, halogenated alkyl or halogenated alkenyl group; and X and Y are an unsubstituted or substituted hydrocarbon group, and dashed line - - - means that X and Y may be bonded together to form a cyclic structure.Type: GrantFiled: November 26, 2002Date of Patent: December 21, 2004Assignee: Tosoh CorporationInventors: Shinichi Ishikawa, Hisao Eguchi
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Patent number: 6686481Abstract: The present invention relates to a process to prepare semi synthetic statins, to intermediates formed during said process and to highly purified simvastatin produced by the process.Type: GrantFiled: July 26, 2001Date of Patent: February 3, 2004Assignee: Plus Chemicals, B.V.Inventors: Szabo Csaba, Ferenc Korodi, Melczer Istvan, Szabolcs Salyi, David Leonov
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Publication number: 20030187063Abstract: Compounds represented by the formula: 1Type: ApplicationFiled: November 8, 2002Publication date: October 2, 2003Inventors: Pooran Chand, Yarlagadda S Babu, R S Rowland, Tsu-Hsing Lin
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Publication number: 20030083523Abstract: A compound represented by the following general formula (I): 1Type: ApplicationFiled: June 18, 2002Publication date: May 1, 2003Applicant: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Makoto Kawamura, Noriko Chiba, Kazutoshi Watanabe
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Patent number: 6489343Abstract: The present invention relates to compounds of the formula (I): wherein R1 is fluorine or trifluoromethyl; R2 is fluorine or trifluoromethyl; R3 is methyl or hydroxymethyl; R4 represents a variety of substituents; and n is zero, 1 or 2; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.Type: GrantFiled: August 20, 2001Date of Patent: December 3, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
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Patent number: 6451766Abstract: Compounds of formula (I) or their salts or esters: [wherein R1 is alkyl or haloalkyl; R2 and R3 each represents hydrogen or aliphatic acyl; X is hydroxy, halogen, alkoxy, or a group of formula RaO—, where Ra is aliphatic acyl; Y is a group of formula RbRcN— or RbRcN—O—, where Rb and Rc each is hydrogen or alkyl; and Z is oxygen or sulfur] have excellent sialidase inhibitory activity and are therefore useful for the treatment and prevention of influenza and other viral diseases where the replication of the virus is susceptible to sialidase inhibitors.Type: GrantFiled: October 3, 2001Date of Patent: September 17, 2002Assignee: Sankyo Company, LimitedInventors: Takeshi Honda, Yoshiyuki Kobayashi, Makoto Yamashita
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Patent number: 6436930Abstract: The present invention relates to antifungal compounds having the structural formula: and pharmaceutically acceptable salts, solvates and prodrugs thereof. The present invention further relates to pharmaceutical compositions containing said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof, for use in the treatment of a fungal infection in an animal host.Type: GrantFiled: September 14, 2001Date of Patent: August 20, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Michael Serrano-Wu, Xuhua Du, Neelakantan Balasubramanian, Denis R. St. Laurent
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Patent number: 6392061Abstract: This invention relates to novel processes for making (2S, 3S, 5S) oxetanone derivative lipase inhibitor compounds and intermediates therefor, which processes for producing such derivatives that are useful as lipase inhibitors are capable of being scaled to commercial quantities. Further the invention relates to processes for producing salts and for producing pharmaceutical compositions compounds comprising at least one such oxetanone derivative or salt, as well as methods for using such compounds and compositions for inhibiting lipases.Type: GrantFiled: April 23, 2001Date of Patent: May 21, 2002Assignee: Zpro Chemical, Inc.Inventor: John Jason Gentry Mullins
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Patent number: 6271425Abstract: A novel process for producing alcohols, characterized by reacting an organic halide represented by the formula R—X (wherein R means an organic residue and X means a halogen atom) with oxygen molecules in the presence of an organotin compound and a reducing agent and optionally in the presence of a free-radical inhibitor in an amount up to 0.3 equivalent based on the organic halide to obtain an alcohol represented by the general formula R—OH (wherein R has the same meaning as the above).Type: GrantFiled: September 7, 1999Date of Patent: August 7, 2001Assignees: Fujisawa Pharmaceutical Co., Ltd.Inventors: Eiichi Nakamura, Masaya Sawamura
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Patent number: 6147231Abstract: A process for producing a compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen or alkyl, and R is hydrogen or alkyl, which comprises removing the protective group (P) of hydroxyl of a compound of the formula (II): ##STR2## wherein P is a protective group of hydroxyl, .about. indicates an E-isomer, Z-isomer or a mixture thereof, and the other symbols are as defined above; and an intermediate for the production of the compound of the formula (I).Type: GrantFiled: October 16, 1998Date of Patent: November 14, 2000Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Takami Murashi
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Patent number: 6136986Abstract: The invention relates to a process for preparing substituted chroman derivatives of the general formula VII, ##STR1## where X is the group --CN, --COOR.sup.3, --CHO, --CH.sub.2 OR.sup.7 or --CH(OR.sup.8).sub.2,R.sup.2 is a C.sub.1 -C.sub.23 -alkyl, C.sub.2 -C.sub.23 -alkenyl, C.sub.6 -C.sub.18 -aryl or C.sub.7 -C.sub.18 -aralkyl radical,R.sup.3 is hydrogen or an optionally substituted C.sub.1 -C.sub.4 -alkyl radical,R.sup.4, R.sup.5, R.sup.6 are, independently of one another, hydrogen or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.7 is hydrogen or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.8 is a C.sub.1 -C.sub.4 -alkyl radical, or the two radicals are a C.sub.2 -C.sub.6 -alkylene radical which links the two oxygen atoms to form a cyclic acetal and is optionally branched or may carry one or two carboxyl groups, cyclohexyl or phenyl radicals,and to the novel intermediates of the process.Type: GrantFiled: December 13, 1999Date of Patent: October 24, 2000Assignee: BASF AktiengesellschaftInventors: Rainer Sturmer, Kai-Uwe Baldenius
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Patent number: 6136853Abstract: PURPOSE: To produce a novel antibiotic substance zofimarin having antimicrobial activity against fungi and obtain an antimicrobial agent containing the antibiotic substance zofimarin as an active constituent, by cultivating a microorganism, belonging to the genus Zopfiella and capable of producing the zofimarin.CONSTITUTION: An ascomycete belonging to the genus Zopfiella, e.g. Zopfiella marina; is cultivated. The cultivation is carried out according to general fungi, but artifical seawater is used in place of tap water in a liquid culture medium. A carbon source, nitrogen source, inorganic salt, etc., are added, and a defoaming agent is suitably used to carry out the cultivation at 20-30.degree. C. by the spinner culture method with aeration. After completing the cultivation, microbial cells are removed, and the resultant product in the supernatant liquid or filtrate is extracted and purified to afford the aimed zofimarin.Type: GrantFiled: March 6, 1999Date of Patent: October 24, 2000Assignee: Merck & Co., Inc.Inventors: James M. Balkovec, Bruno Tse
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6051723Abstract: The present invention relates to new 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrofuranone derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded form an unsubstituted or substituted 5- to 7-membered ring which is interrupted by at least one hetero atom,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or one of the groups ##STR2## E represents a metal ion equivalent or an ammonium ion, L represents oxygen or sulphur,M represents oxygen or sulphur andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in the description, to processes for their preparation, and to their use as pesticides.Type: GrantFiled: August 13, 1998Date of Patent: April 18, 2000Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Gunther Beck, Hermann Hagemann, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wolfram Andersch, Norbert Mencke, Andreas Turberg
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Patent number: 6040463Abstract: Sordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.Type: GrantFiled: September 24, 1997Date of Patent: March 21, 2000Assignee: Merck & Co., Inc.Inventors: James M. Balkovec, Bruno Tse
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Patent number: 6025519Abstract: Cyclobutane-1,2-dicarboxylic esters of the formula: ##STR1## in which R.sup.1 is a C.sub.1-8 -alkyl group, an optionally substituted mono- or bicyclic cycloaliphatic group having 3 to 10 ring carbon atoms, an optionally substituted aryl or arylalkyl group or an optionally substituted saturated heterocyclic group and R.sup.2 is either C.sub.1-4 -alkyl or both radicals R.sup.2 together form a group of the formula --(CH.sub.2).sub.n --(n is 2 to 4), are prepared from the corresponding maleic or fumaric esters and ketene acetals in the presence of a Lewis acid and a sterically hindered base. The reaction is stereoselective when optically active maleic or fumaric esters are employed. The cyclobutane-1,2-dicarboxylic esters (I), in particular those having trans configuration, are intermediates in the synthesis of pharmaceutically active compounds.Type: GrantFiled: July 20, 1998Date of Patent: February 15, 2000Assignee: Lonza, Ltd.Inventor: Andreas Brunner
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Patent number: 6001823Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.Type: GrantFiled: June 5, 1995Date of Patent: December 14, 1999Inventors: Scott Hultgren, Meta Kuehn, Zheng Xu, Derek Ogg, Mark Harris, Matti Lepisto, Jan Kihlberg, Charles Hal Jones
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Patent number: 5990156Abstract: Compounds of formula (I), ##STR1## wherein R.sup.1 represents OR.sup.5, SR.sup.5, NR.sup.5 R.sup.6, N(OR.sup.5)R.sup.6 or N(NR.sup.5 R.sup.6)R.sup.6 ; X represents OH, N.sub.3, NR.sup.3 R.sup.4 or NR.sup.4 CO.sub.2 R.sup.15 ; Y represents H or NHR.sup.2 ; R.sup.2 represents a group SO.sub.2 R.sup.7 or COR.sup.7 ; R.sup.3 represents H, C.sub.1-6 alkyl or C(.dbd.NR.sup.8)NR.sup.9 R.sup.10 ; R.sup.4 represents H or C.sub.1-6 alkyl; R.sup.5 represents H, C.sub.1-20 alkyl, C.sub.3-8 cycloalkyl, C.sub.2-20 alkenyl, C.sub.2-20 alkynyl, CHR.sup.11 COR.sup.12 or C.sub.1-20 alkyl substituted by one or more groups selected from NR.sup.13 R.sup.14, NR.sup.13 COR.sup.14, CO.sub.2 R.sup.13, OR.sup.13, C.sub.3-8 cycloalkyl and optionally substituted aryl; each R.sup.6 independently represents H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-20 alkynyl, aryl or C.sub.1-4 alkyl substituted by one or more groups selected from NR.sup.13 R.sup.14, COR.sup.13, C.sub.3-8 cycloalkyl, CN, N.sub.3, OR.sup.Type: GrantFiled: January 12, 1998Date of Patent: November 23, 1999Assignee: Biota Scientific Management PTY Ltd.Inventors: Peter Cherry, Peter Howes, Paul Smith, Stephen Sollis
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Patent number: 5972996Abstract: 4-Cyano-4-deformylsordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.Type: GrantFiled: July 28, 1998Date of Patent: October 26, 1999Assignee: Merck & Co., Inc.Inventors: Jennifer Nielsen-Kahn, Bruce Tse
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Patent number: 5935995Abstract: Compounds of the formula Iglycosyl-Y?--C(.dbd.Y)--X--!.sub.p --W(R).sub.n --Z--C(.dbd.Y)-active compound (I)are described which are suitable for the treatment of carcinomatous diseases, autoimmune diseases and chronic inflammatory diseases such as rheumatoid arthritis.Type: GrantFiled: March 11, 1997Date of Patent: August 10, 1999Assignee: Heochst AktiengesellschaftInventors: Klaus Bosslet, Jorg Czech, Manfred Gerken, Rainer Straub, Claude Monneret, Jean-Claude Florent, Frederic Schmidt
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Patent number: 5869523Abstract: Process for the preparation of 6-(substitutedaminopropionyl)-derivatives of forskolinProcess for the manufacture of 6.beta.Type: GrantFiled: July 22, 1991Date of Patent: February 9, 1999Assignee: Hoechst AktiengesellschaftInventors: Noel John de Souza, Adolf D'Sa, Samba Laxminarayan Kattige, Gulab Bajirao Padwal, Jurgen Blumbach
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Patent number: 5820783Abstract: Chiral compounds of the formula I ##STR1## where R.sup.1 is hydrogen or --Y--Z--Y.sup.1,R.sup.2 is ##STR2## and X is hydrogen, fluorine, chlorine, bromine, iodine, hydroxyl or OR.sup.1, whereY is a direct bond, CO or C.sub.2 - to C.sub.8 -alkylene in which nonadjacent carbon atoms may be replaced by O, CO, COO or OCO,Z is a group containing one or more saturated or unsaturated carbocyclic or heterocyclic rings,Y.sup.1 is C.sub.1 - to C.sub.15 -alkyl, C.sub.2 - to C.sub.15 -alkenyl, C.sub.1 - to C.sub.15 -alkoxy, C.sub.2 - to C.sub.15 -alkenyloxy, C.sub.1 - to C.sub.15 -alkanoyloxy or C.sub.3 - to C.sub.15 -alkenoyloxy, it being possible for nonadjacent carbon atoms in these radicals to be replaced by oxygen, OCO or COO, andn is 0, 1 or 2.Type: GrantFiled: July 29, 1997Date of Patent: October 13, 1998Assignee: BASF AktiengesellschaftInventors: Karl Siemensmeyer, Volkmar Vill, Hanns-Walter Tunger, Matthias Paul
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Patent number: 5811028Abstract: A 2H-5,6-optically active dihydropyran derivative represented by the general formula (I) or (I'): ##STR1## wherein Rf represents a fluoroalkyl group having 1 or 2 carbon atoms; a liquid crystal composition and a liquid crystal device comprising the derivative; and a racemic mixture comprising at least one type of the derivative. The derivative is a novel compound which exhibits the liquid crystal property by itself or can be used as an excellent dopant providing a high speed response to a composition comprising it even when the compound does not exhibit the liquid crystal property by itself. The derivative also exhibits a large spontaneous polarization.Type: GrantFiled: August 13, 1997Date of Patent: September 22, 1998Assignee: Kashima Oil CompanyInventors: Tatsushi Ishizuka, Mitsunori Takeda, Masaaki Namekawa, Keizou Itoh
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Patent number: 5808111Abstract: Novel acitretinamide compounds which are soluble and stable in water and useful in aqueous delivery systems, particularly to treat cancer, are provided. The novel acitretinamide compounds, 1-(D-glucopyranosyl)acitretinamide, 1-(D-glucopyranuronosyl)acitretinamide and the metal salts thereof, are hereinafter collectively referred to as the "acitretinamide compounds". The invention also relates to novel methods of making the acitretinamide compounds.Type: GrantFiled: May 6, 1997Date of Patent: September 15, 1998Assignee: The Ohio State Research FoundationInventor: Robert W. Curley, Jr.
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Patent number: 5786385Abstract: A 2-(1-nonen-3,5,7-triynyl)3-hydroxy tetrahydropyran (cunaniol) particularly that having the formula: ##STR1## or a corresponding anhydrocunaniol or cunanione, for use in therapy, especially as a reversible heart blocking agent or neuromuscular active or in neurofunction generally; or for use as a pesticide or mycobactericide.Type: GrantFiled: May 10, 1996Date of Patent: July 28, 1998Inventor: Conrad Gorinsky
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Patent number: 5709817Abstract: Described herein are chiral compounds of the formula I ##STR1## where R.sup.1 is hydrogen or --Y--Z--Y.sup.1,R.sup.2 is ##STR2## and X is hydrogen, fluorine, chlorine, bromine, iodine, hydroxyl or OR.sup.1, whereY is a direct bond, CO or C.sub.2 - to C.sub.8 -alkylene in which nonadjacent carbon atoms may be replaced by O, CO, COO or OCO,Z is a group containing one or more saturated or unsaturated carbocyclic or heterocyclic rings,Y.sup.1 is C.sub.1 - to C.sub.15 -alkyl, C.sub.2 - to C.sub.15 -alkenyl, C.sub.1 - to C.sub.15 -alkoxy, C.sub.2 - to C.sub.15 -alkenyloxy, C.sub.1 - to C.sub.15 -alkanoyloxy or C.sub.3 - to C.sub.15 -alkenoyloxy, it being possible for nonadjacent carbon atoms in these radicals to be replaced by oxygen, OCO or COO, andn is 0, 1 or 2.Type: GrantFiled: November 24, 1995Date of Patent: January 20, 1998Assignee: BASF AktiengesellschaftInventors: Karl Siemensmeyer, Volkmar Vill, Hanns-Walter Tunger, Matthias Paul
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Patent number: 5698137Abstract: A 2H-5,6-optically active dihydropyran derivative represented by the general formula (I) or (I'): ##STR1## wherein Rf represents a fluoroalkyl group having 1 or 2 carbon atoms; a liquid crystal composition and a liquid crystal device comprising the derivative; and a racemic mixture comprising at least one type of the derivative. The derivative is a novel compound which exhibits the liquid crystal property by itself or can be used as an excellent dopant providing a high speed response to a composition comprising it even when the compound does not exhibit the liquid crystal property by itself. The derivative also exhibits a large spontaneous polarization.Type: GrantFiled: April 15, 1996Date of Patent: December 16, 1997Assignee: Kashima Oil CompanyInventors: Tatsushi Ishizuka, Mitsunori Takeda, Masaaki Namekawa, Keizou Itoh
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Patent number: 5674811Abstract: A cyanoketone derivatives of the following formula (1) ##STR1## which are characterized by excellent herbicidal activity and effectiveness against a variety of broad leafed weeds, including barnyard grass, green foxtail, velvet leaf, livid amaranth and hairy beggar ticks.Type: GrantFiled: October 6, 1994Date of Patent: October 7, 1997Assignee: Tokuyama CorporationInventors: Toshio Kitajima, Tadashi Kobutani, Shozo Kato, Masao Yamaguchi, Masahiko Ishizaki, deceased
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Patent number: 5665518Abstract: The present invention provides a vinylmonomer represented with the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a methyl group, R.sup.2 represents a dihydric, bridged cyclic hydrocarbon group having a carbon number in the range of 7 to 13 both inclusive, R.sup.3 represents a group to be decomposed by acid or a hydrogen atom, X represents an alkylene group or a coupling group composed of an oxygen-carbon bond, and Y represents an alkylene group or a coupling group composed of a carbon-carbon bond. A photoresist obtained by polymerizing a monomer in accordance with the invention has a high transparency to FUV having a wavelength of at greatest 220 nm, high sensitivity and resolution to FUV, and a high dry etching resistance, and hence is suitable for exposure light such as FUV having a wavelength of at greatest 220 nm and, in particular, ArF excimer laser.Type: GrantFiled: January 19, 1996Date of Patent: September 9, 1997Assignee: NEC CorporationInventors: Katsumi Maeda, Kaichiro Nakano, Takeshi Ohfuji, Etsuo Hasegawa
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Patent number: 5656656Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.Type: GrantFiled: May 23, 1995Date of Patent: August 12, 1997Assignee: Dompe Farmaceutici S.p.A.Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
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Patent number: 5648379Abstract: Derivatives and analogues of 2-deoxy-2,3-didehydro-N-acetyl neuraminic acid, pharmaceutical formulations thereof, methods for their preparation and their use in the treatment of viral infections, in particular influenza, are described.Type: GrantFiled: October 19, 1994Date of Patent: July 15, 1997Assignee: Biota Scientific Management Pty., Ltd.Inventors: Laurence Mark Von Itzstein, Wen-Yang Wu, Tho Van Phan, Basil Danylec, Betty Jin, Peter Malcolm Colman, Joseph Noozhumurry Varghese
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Patent number: 5629265Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.Type: GrantFiled: June 22, 1994Date of Patent: May 13, 1997Assignee: Tokuyama CorporationInventors: Masahiko Ishizaki, Seiji Nagata, Junji Takenaka
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Patent number: 5625069Abstract: A process of preparing 2-cyano-3,5-dimethyl-4-methoxypyridine. The process includes the steps of: acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-carboxamido-3,5-dimethyl-4(1H)-pyridone; methylating 2-carboxamido-3,5-dimethyl-4(1H)-pyridone to obtain 2-carboxamido-3,5-dimethyl-4-methoxypyridine; and dehydrating said 2-carboxamido-3,5-dimethyl-4-methoxypyridone to obtain 2-cyano-3,5-dimethyl-4-methoxypyridine.Type: GrantFiled: July 22, 1996Date of Patent: April 29, 1997Assignee: Development Center for BiotechnologyInventors: Shan-Yen Chou, Tsai-Mien Huang, Shyh-Fong Chen, Hao Ku
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Patent number: 5616713Abstract: A process of preparing 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine including the steps of acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone; halogenating 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone to obtain 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine; methoxylating 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine to obtain 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine; and reducing 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine to obtain 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine.Type: GrantFiled: July 22, 1996Date of Patent: April 1, 1997Assignee: Development Center for BiotechnologyInventors: Shan-Yen Chou, Tsai-Mien Huang, Shyh-Fong Chen, Hao Ku
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Patent number: 5597938Abstract: A novel process for the production of a compound represented by the formula: ##STR1## wherein Z and Z' each represents a protective group for the hydroxyl group; R.sup.1 represents a hydrogen atom or an alkyl group; R.sup.2 represents an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a group represented by the formula --B--D (in which B is an alkylene group and D is a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenoxy group or a cycloalkyl group), a substituted or unsubstituted phenyl group or a substituted or unsubstituted phenoxy group; R.sup.3 and R.sup.4 each represents a hydrogen atom, an alkyl group or an alkoxy group; R.sup.5 represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, a cyano group, an amino group, a hydroxyl group or a group represented by a formula --COOR.sup.8 ; R.sup.6 represents a group represented by a formula --COOR.sup.9, a cyano group, a hydroxyl group, a group represented by a formula --OCOR.sup.Type: GrantFiled: August 10, 1995Date of Patent: January 28, 1997Assignees: Taisho Pharmaceutical Co., Ltd., Fumie SatoInventor: Fumie Sato
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Patent number: 5597932Abstract: The invention is drawn to a compound having the following formula ##STR1## in which X.sup.1 and X.sup.2, which may be the same or different, represent hydrogen or a hydroxy-protecting group, X.sup.4 is hydrogen, A is selected from --COOAlkyl and CH.sub.2 OH, and B is a hydroxy group, or A and B, when taken together, represent an oxo group. These compounds are useful as intermediates in the production of 19-nor vitamin D derivatives.Type: GrantFiled: May 16, 1995Date of Patent: January 28, 1997Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Heinrich K. Schnoes, Kato L. Perlman, Rolf E. Swenson
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Patent number: 5573999Abstract: .beta.-Substituted cinnamic acid derivatives of the formula 1, ##STR1## where R.sup.1 is alkyl, chlorine or bromine, --X-- is --O--, --S--, ##STR2## m is 0 or 1, --Y is --OR.sup.4, --O--N.dbd.CR.sup.5 R.sup.6, --NR.sup.7 R.sup.8, --N(OR.sup.9)R.sup.10 or --SR.sup.11, where the above-mentioned substituents R.sup.2 to R.sup.11 are alkyl, and R.sup.2, and R.sup.3 and R.sup.5 to R.sup.11 can also be hydrogen,Z is halogen, nitro, cyano, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, hetarylalkyl, hetaryloxyalkyl, hetarylthioalkyl, alkenyl, aralkenyl, aryloxyalkenyl, arylthioalkenyl, hetarylalkenyl, hetaryloxyalkenyl, hetarylthioalkenyl, alkynyl, arylalkynyl, hetarylalkynyl, aryl, hetaryl, arylazo, acylamino, --OR.sup.12, --SR.sup.13, --SOR.sup.14, --SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22, R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--, N.dbd.CR.sup.27 R.sup.28, --CH.sub.2 --OCOR.sup.39 or --NR.sup.37 R.Type: GrantFiled: May 15, 1995Date of Patent: November 12, 1996Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Horst Wingert, Wolfgang von Deyn, Wassilios Grammenos, Hartmann Koenig, Harald Rang, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5563274Abstract: A process of preparing optically active alpha-chlorocarboxylic esters having the formula: ##STR1## from an optically active alpha-hydroxy carboxylic ester having the formula: ##STR2## in which process, an alpha-hydroxy carboxylate of formula II is brought into contact with phosgene and a compound chosen from amides, lactams and ureas, wherein R.sub.1 is an optionally substituted hydrocarbyl residue and R is preferably a methyl group.Type: GrantFiled: December 3, 1993Date of Patent: October 8, 1996Assignee: Rhone-Poulenc ChimieInventors: Jean-Roger Desmurs, Pascal Metivier, Genevieve Padilla, Harivelo Rajoharison
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Patent number: 5536845Abstract: Process for the preparation of the acrylates chosen from those of formula ##STR1## those of formula ##STR2## and those of the formula ##STR3## useful in the production of new polymers and copolymers.Type: GrantFiled: April 21, 1994Date of Patent: July 16, 1996Assignee: AtochemInventors: Marie-Christine Berthe, Paul Caubere, Yves Fort
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Patent number: 5525745Abstract: The invention describes intermediates for use in the synthesis of 1.alpha.-hydroxy-19-nor-vitamin D compounds. The intermediates have the following formula: ##STR1## The disclosed process includes (a) the construction of a 5,8-diol-6-yne intermediate by joining ring-A and ring-C/D portions of the desired end product via the condensation of an acetylenic derivative containing the C/D-ring portion of the desired end product with a cyclic dihydroxy ketone representing the A-ring of the desired end product; (b) the partial reduction of the 6,7 acetylenic triple bond linkage between the A and C/D ring portions to obtain a 5,8-diol-6-ene intermediate; and (c) the reductive removal of the 5,8-oxygen functions to generate the required 5,7-diene end product from which the desired 7-trans(7E)-isomer is purified directly, or after optional double bond isomerization of the 7-cis(7Z)-isomer employing a novel thiophenol-promoted isomerization step.Type: GrantFiled: March 27, 1995Date of Patent: June 11, 1996Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Heinrich K. Schnoes, Fariba Aria
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Patent number: 5468870Abstract: Dye-donor element for use according to thermal dye sublimation transfer comprising a support having thereon a dye layer containing a dye corresponding to the following formula ##STR1## wherein Z represents CN, COOR.sup.1 or CONR.sup.2 R.sup.3 ;R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, or R.sup.2 and R.sup.3 together represent the necessary atoms to close a heterocyclic nucleus or substituted heterocyclic nucleus;Y represents OR.sup.4 or NR.sup.5 R.sup.6 or CN;R.sup.4 represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, SO.sub.2 R.sup.7, COR.sup.7, CSR.sup.7, POR.sup.7 R.sup.8 ;R.sup.5 and R.sup.6 each independently has one of the significances given to R.sup.4 or represent substituted or unsubstituted amino, or R.sup.5 and R.sup.Type: GrantFiled: October 20, 1994Date of Patent: November 21, 1995Assignee: AGFA-GAVAERT, N.V.Inventor: Luc J. Vanmaele
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Patent number: 5446062Abstract: Compounds of the structure ##STR1## where W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.6 and R.sup.7 are hydrogen or alkyl, or R.sup.6 and R.sup.7, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## Z is --CH.sub.2 --, oxygen, sulfur, or --NR.sup.9, L.sup.1 and L.sup.2 are selected from a valence bond, alkylene, propenylene, and propynylene; R.sup.1 and R.sup.2 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is selected from oxygen, >NR.sup.10, and ##STR4## L.sup.3 is selected from alkylene of one to three carbon atoms, propenylene, propynylene, ##STR5## and R.sup.3, R.sup.4, and R.sup.5 are hydrogen or alkyl of one to four carbon atoms inhibit the synthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.Type: GrantFiled: November 12, 1993Date of Patent: August 29, 1995Assignee: Abbott LaboratoriesInventors: Joseph F. Dellaria, Anwer Basha, Lawrence A. Black, Linda J. Chernesky, Wendy Lee
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Patent number: 5411985Abstract: Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia.Type: GrantFiled: May 17, 1993Date of Patent: May 2, 1995Assignee: Merck & Co., Inc.Inventors: Gerald F. Bills, Otto D. Hensens, Jerrold M. Liesch, Russel B. Lingham, Jon D. Polishook, Michael J. Salvatore, Susan L. Raghoobar
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Patent number: 5399724Abstract: Novel acyclic terpene compounds useful as intermediates for producing sarcophytol A which have an anti-carcinogenic promotor activity and anti-tumor activity, which compounds are shown by the following general formula (I): ##STR1## [wherein R.sup.1 is a hydrogen atom, 1-alkoxyalkyl group, tetrahydrofuryl group, tetrahydropyranyl group or acyl group; R.sup.2 is a group of formula: --CHO, --CH.sub.2 OR.sup.3 or ##STR2## (wherein R.sup.3 is a hydrogen atom, 1-alkoxyalkyl group, tetrahydrofuryl group, tetrahydropyranyl group or acyl group; and R.sup.4 is C.sub.1 to C.sub.4 alkyl group) with the proviso that R.sup.1 and R.sup.3 do not represent the same substituents simultaneously; when R.sup.1 is a hydrogen atom, R.sup.3 is not acetyl group or tetrahydropyranyl group; and when R.sup.2 is a group of formula: ##STR3## R.sup.1 is not a hydrogen atom).Type: GrantFiled: September 28, 1993Date of Patent: March 21, 1995Assignee: Mitsubishi Kasei CorporationInventors: Hisao Takayanagi, Yasunori Kitano, Yasuhiro Morinaka
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Patent number: 5385917Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.Type: GrantFiled: July 16, 1993Date of Patent: January 31, 1995Assignee: Mitsubishi Kasei CorporationInventors: Hiroaki Ueno, Masahiko Morioka, Fumiko Hatanaka
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Patent number: 5382675Abstract: A tetrahydropyran-4-yloxy-alkanoic acid of formula III ##STR1## wherein R.sub.2 is hydrogen or C.sub.1-4 alkyl and R.sub.3 is hydrogen or C.sub.1-4 alkyl.Type: GrantFiled: April 28, 1994Date of Patent: January 17, 1995Assignee: Ciba-Geigy CorporationInventor: Oskar Wacker
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Patent number: 5380882Abstract: The invention relates to compounds of formula I ##STR1## wherein A is a radical of formula ##STR2## R.sub.1 and R.sub.2 are each independently of the other hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen or a radical of formula ##STR3## wherein X is --O--, --CH.sub.2 --, --C(CH.sub.3).sub.2 -- or --SO.sub.2 --, and R.sub.3 and R.sub.4 are each independently of the other hydrogen, C.sub.1 -C.sub.4 alkyl or phenyl, as well as compositions comprising these compounds.The compositions are particularly suitable for making integrated circuits.Type: GrantFiled: March 30, 1993Date of Patent: January 10, 1995Assignee: Ciba-Geigy CorporationInventor: Alfred Steinmann
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Patent number: 5360817Abstract: Derivatives and analogues of 2-deoxy-2,3-didehydro-N-acetyl neuraminic acid, pharmaceutical formulations thereof, methods for their preparation .and their use in the treatment of viral infections, in particular influenza, are described.Type: GrantFiled: November 10, 1992Date of Patent: November 1, 1994Assignee: Biota Scientific Management Pty LtdInventors: Laurence M. von Izstein, Wen-Yang Wu, Tho V. Phan, Basil Danylec, Betty Jin
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Patent number: 5350765Abstract: Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, or benzo[b]thienyl, A.sub.1 is propynyl, methylene, or a direct link to X, X is oxy, thio, sulfonyl, or NR.sub.4, A.sub.2 is selected from ##STR2## where Y is hydrogen, halogen, or nitrile; Z is hydrogen, R.sub.1 is alkyl, and R.sub.2 is hydrogen or alkyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.Type: GrantFiled: August 30, 1993Date of Patent: September 27, 1994Assignee: Abbott LaboratoriesInventors: Joseph F. Dellaria, Jimmie L. Moore, Dee W. Brooks