Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/420)
  • Patent number: 6852866
    Abstract: 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: Grant
    Filed: August 15, 2003
    Date of Patent: February 8, 2005
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Subramaniam Sabesan
  • Patent number: 6833462
    Abstract: 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: Grant
    Filed: November 26, 2002
    Date of Patent: December 21, 2004
    Assignee: Tosoh Corporation
    Inventors: Shinichi Ishikawa, Hisao Eguchi
  • Patent number: 6686481
    Abstract: 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: Grant
    Filed: July 26, 2001
    Date of Patent: February 3, 2004
    Assignee: Plus Chemicals, B.V.
    Inventors: Szabo Csaba, Ferenc Korodi, Melczer Istvan, Szabolcs Salyi, David Leonov
  • Publication number: 20030187063
    Abstract: Compounds represented by the formula: 1
    Type: Application
    Filed: November 8, 2002
    Publication date: October 2, 2003
    Inventors: Pooran Chand, Yarlagadda S Babu, R S Rowland, Tsu-Hsing Lin
  • Publication number: 20030083523
    Abstract: A compound represented by the following general formula (I): 1
    Type: Application
    Filed: June 18, 2002
    Publication date: May 1, 2003
    Applicant: Mitsubishi Chemical Corporation
    Inventors: Ryoichi Ando, Makoto Kawamura, Noriko Chiba, Kazutoshi Watanabe
  • Patent number: 6489343
    Abstract: 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: Grant
    Filed: August 20, 2001
    Date of Patent: December 3, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 6451766
    Abstract: 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: Grant
    Filed: October 3, 2001
    Date of Patent: September 17, 2002
    Assignee: Sankyo Company, Limited
    Inventors: Takeshi Honda, Yoshiyuki Kobayashi, Makoto Yamashita
  • Patent number: 6436930
    Abstract: 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: Grant
    Filed: September 14, 2001
    Date of Patent: August 20, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael Serrano-Wu, Xuhua Du, Neelakantan Balasubramanian, Denis R. St. Laurent
  • Patent number: 6392061
    Abstract: 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: Grant
    Filed: April 23, 2001
    Date of Patent: May 21, 2002
    Assignee: Zpro Chemical, Inc.
    Inventor: John Jason Gentry Mullins
  • Patent number: 6271425
    Abstract: 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: Grant
    Filed: September 7, 1999
    Date of Patent: August 7, 2001
    Assignees: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Eiichi Nakamura, Masaya Sawamura
  • Patent number: 6147231
    Abstract: 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: Grant
    Filed: October 16, 1998
    Date of Patent: November 14, 2000
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Takase, Hiroyuki Kai, Takami Murashi
  • Patent number: 6136986
    Abstract: 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: Grant
    Filed: December 13, 1999
    Date of Patent: October 24, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Rainer Sturmer, Kai-Uwe Baldenius
  • Patent number: 6136853
    Abstract: 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: Grant
    Filed: March 6, 1999
    Date of Patent: October 24, 2000
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Bruno Tse
  • Patent number: 6057342
    Abstract: 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: Grant
    Filed: July 7, 1997
    Date of Patent: May 2, 2000
    Assignee: Dupont Pharmaceutical Co.
    Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
  • Patent number: 6051723
    Abstract: 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: Grant
    Filed: August 13, 1998
    Date of Patent: April 18, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Thomas Bretschneider, Gunther Beck, Hermann Hagemann, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wolfram Andersch, Norbert Mencke, Andreas Turberg
  • Patent number: 6040463
    Abstract: 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: Grant
    Filed: September 24, 1997
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Bruno Tse
  • Patent number: 6025519
    Abstract: 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: Grant
    Filed: July 20, 1998
    Date of Patent: February 15, 2000
    Assignee: Lonza, Ltd.
    Inventor: Andreas Brunner
  • Patent number: 6001823
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: December 14, 1999
    Inventors: Scott Hultgren, Meta Kuehn, Zheng Xu, Derek Ogg, Mark Harris, Matti Lepisto, Jan Kihlberg, Charles Hal Jones
  • Patent number: 5990156
    Abstract: 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: Grant
    Filed: January 12, 1998
    Date of Patent: November 23, 1999
    Assignee: Biota Scientific Management PTY Ltd.
    Inventors: Peter Cherry, Peter Howes, Paul Smith, Stephen Sollis
  • Patent number: 5972996
    Abstract: 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: Grant
    Filed: July 28, 1998
    Date of Patent: October 26, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Jennifer Nielsen-Kahn, Bruce Tse
  • Patent number: 5935995
    Abstract: 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: Grant
    Filed: March 11, 1997
    Date of Patent: August 10, 1999
    Assignee: Heochst Aktiengesellschaft
    Inventors: Klaus Bosslet, Jorg Czech, Manfred Gerken, Rainer Straub, Claude Monneret, Jean-Claude Florent, Frederic Schmidt
  • Patent number: 5869523
    Abstract: Process for the preparation of 6-(substitutedaminopropionyl)-derivatives of forskolinProcess for the manufacture of 6.beta.
    Type: Grant
    Filed: July 22, 1991
    Date of Patent: February 9, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Noel John de Souza, Adolf D'Sa, Samba Laxminarayan Kattige, Gulab Bajirao Padwal, Jurgen Blumbach
  • Patent number: 5820783
    Abstract: 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: Grant
    Filed: July 29, 1997
    Date of Patent: October 13, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl Siemensmeyer, Volkmar Vill, Hanns-Walter Tunger, Matthias Paul
  • Patent number: 5811028
    Abstract: 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: Grant
    Filed: August 13, 1997
    Date of Patent: September 22, 1998
    Assignee: Kashima Oil Company
    Inventors: Tatsushi Ishizuka, Mitsunori Takeda, Masaaki Namekawa, Keizou Itoh
  • Patent number: 5808111
    Abstract: 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: Grant
    Filed: May 6, 1997
    Date of Patent: September 15, 1998
    Assignee: The Ohio State Research Foundation
    Inventor: Robert W. Curley, Jr.
  • Patent number: 5786385
    Abstract: 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: Grant
    Filed: May 10, 1996
    Date of Patent: July 28, 1998
    Inventor: Conrad Gorinsky
  • Patent number: 5709817
    Abstract: 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: Grant
    Filed: November 24, 1995
    Date of Patent: January 20, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl Siemensmeyer, Volkmar Vill, Hanns-Walter Tunger, Matthias Paul
  • Patent number: 5698137
    Abstract: 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: Grant
    Filed: April 15, 1996
    Date of Patent: December 16, 1997
    Assignee: Kashima Oil Company
    Inventors: Tatsushi Ishizuka, Mitsunori Takeda, Masaaki Namekawa, Keizou Itoh
  • Patent number: 5674811
    Abstract: 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: Grant
    Filed: October 6, 1994
    Date of Patent: October 7, 1997
    Assignee: Tokuyama Corporation
    Inventors: Toshio Kitajima, Tadashi Kobutani, Shozo Kato, Masao Yamaguchi, Masahiko Ishizaki, deceased
  • Patent number: 5665518
    Abstract: 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: Grant
    Filed: January 19, 1996
    Date of Patent: September 9, 1997
    Assignee: NEC Corporation
    Inventors: Katsumi Maeda, Kaichiro Nakano, Takeshi Ohfuji, Etsuo Hasegawa
  • Patent number: 5656656
    Abstract: 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: Grant
    Filed: May 23, 1995
    Date of Patent: August 12, 1997
    Assignee: Dompe Farmaceutici S.p.A.
    Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
  • Patent number: 5648379
    Abstract: 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: Grant
    Filed: October 19, 1994
    Date of Patent: July 15, 1997
    Assignee: 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
  • Patent number: 5629265
    Abstract: 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: Grant
    Filed: June 22, 1994
    Date of Patent: May 13, 1997
    Assignee: Tokuyama Corporation
    Inventors: Masahiko Ishizaki, Seiji Nagata, Junji Takenaka
  • Patent number: 5625069
    Abstract: 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: Grant
    Filed: July 22, 1996
    Date of Patent: April 29, 1997
    Assignee: Development Center for Biotechnology
    Inventors: Shan-Yen Chou, Tsai-Mien Huang, Shyh-Fong Chen, Hao Ku
  • Patent number: 5616713
    Abstract: 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: Grant
    Filed: July 22, 1996
    Date of Patent: April 1, 1997
    Assignee: Development Center for Biotechnology
    Inventors: Shan-Yen Chou, Tsai-Mien Huang, Shyh-Fong Chen, Hao Ku
  • Patent number: 5597938
    Abstract: 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: Grant
    Filed: August 10, 1995
    Date of Patent: January 28, 1997
    Assignees: Taisho Pharmaceutical Co., Ltd., Fumie Sato
    Inventor: Fumie Sato
  • Patent number: 5597932
    Abstract: 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: Grant
    Filed: May 16, 1995
    Date of Patent: January 28, 1997
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Kato L. Perlman, Rolf E. Swenson
  • Patent number: 5573999
    Abstract: .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: Grant
    Filed: May 15, 1995
    Date of Patent: November 12, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Horst Wingert, Wolfgang von Deyn, Wassilios Grammenos, Hartmann Koenig, Harald Rang, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5563274
    Abstract: 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: Grant
    Filed: December 3, 1993
    Date of Patent: October 8, 1996
    Assignee: Rhone-Poulenc Chimie
    Inventors: Jean-Roger Desmurs, Pascal Metivier, Genevieve Padilla, Harivelo Rajoharison
  • Patent number: 5536845
    Abstract: 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: Grant
    Filed: April 21, 1994
    Date of Patent: July 16, 1996
    Assignee: Atochem
    Inventors: Marie-Christine Berthe, Paul Caubere, Yves Fort
  • Patent number: 5525745
    Abstract: 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: Grant
    Filed: March 27, 1995
    Date of Patent: June 11, 1996
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Fariba Aria
  • Patent number: 5468870
    Abstract: 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: Grant
    Filed: October 20, 1994
    Date of Patent: November 21, 1995
    Assignee: AGFA-GAVAERT, N.V.
    Inventor: Luc J. Vanmaele
  • Patent number: 5446062
    Abstract: 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: Grant
    Filed: November 12, 1993
    Date of Patent: August 29, 1995
    Assignee: Abbott Laboratories
    Inventors: Joseph F. Dellaria, Anwer Basha, Lawrence A. Black, Linda J. Chernesky, Wendy Lee
  • Patent number: 5411985
    Abstract: 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: Grant
    Filed: May 17, 1993
    Date of Patent: May 2, 1995
    Assignee: 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
  • Patent number: 5399724
    Abstract: 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: Grant
    Filed: September 28, 1993
    Date of Patent: March 21, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Hisao Takayanagi, Yasunori Kitano, Yasuhiro Morinaka
  • Patent number: 5385917
    Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: January 31, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Hiroaki Ueno, Masahiko Morioka, Fumiko Hatanaka
  • Patent number: 5382675
    Abstract: 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: Grant
    Filed: April 28, 1994
    Date of Patent: January 17, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Oskar Wacker
  • Patent number: 5380882
    Abstract: 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: Grant
    Filed: March 30, 1993
    Date of Patent: January 10, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Alfred Steinmann
  • Patent number: 5360817
    Abstract: 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: Grant
    Filed: November 10, 1992
    Date of Patent: November 1, 1994
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Laurence M. von Izstein, Wen-Yang Wu, Tho V. Phan, Basil Danylec, Betty Jin
  • Patent number: 5350765
    Abstract: 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: Grant
    Filed: August 30, 1993
    Date of Patent: September 27, 1994
    Assignee: Abbott Laboratories
    Inventors: Joseph F. Dellaria, Jimmie L. Moore, Dee W. Brooks